Benign Prostatic Hypertrophy

Benign Prostatic Hypertrophy
Practice Essentials
Benign prostatic hyperplasia (BPH), also known as benign prostatic hypertrophy, is a histologic diagnosis
characterized by proliferation of the cellular elements of the prostate. Chronic bladder outlet
obstruction (BOO) secondary to BPH may lead to urinary retention, renal insufficiency, recurrent urinary
tract infections, gross hematuria, and bladder calculi.
Signs and symptoms
When the prostate enlarges, it may constrict the flow of urine. Nerves within the prostate and bladder
may also play a role in causing the following common symptoms:
Urinary frequency
Urinary urgency
Hesitancy - Difficulty initiating the urinary stream; interrupted, weak stream
Incomplete bladder emptying - The feeling of persistent residual urine, regardless of the frequency
of urination
Straining - The need strain or push (Valsalva maneuver) to initiate and maintain urination in order
to more fully evacuate the bladder
Decreased force of stream - The subjective loss of force of the urinary stream over time
Dribbling - The loss of small amounts of urine due to a poor urinary stream
See Clinical Presentation for more detail.
Diagnosis
Digital rectal examination
The digital rectal examination (DRE) is an integral part of the evaluation in men with presumed BPH.
During this portion of the examination, prostate size and contour can be assessed, nodules can be
evaluated, and areas suggestive of malignancy can be detected.
Laboratory studies
Urinalysis - Examine the urine using dipstick methods and/or via centrifuged sediment evaluation
to assess for the presence of blood, leukocytes, bacteria, protein, or glucose
Urine culture - This may be useful to exclude infectious causes of irritative voiding and is usually
performed if the initial urinalysis findings indicate an abnormality
Prostate-specific antigen - Although BPH does not cause prostate cancer, men at risk for BPH are
also at risk for this disease and should be screened accordingly (although screening for prostate
cancer remains controversial)
Electrolytes, blood urea nitrogen (BUN), and creatinine - These evaluations are useful screening
tools for chronic renal insufficiency in patients who have high postvoid residual (PVR) urine
volumes; however, a routine serum creatinine measurement is not indicated in the initial
evaluation of men with lower urinary tract symptoms (LUTS) secondary to BPH
[1]

Ultrasonography
Ultrasonography (abdominal, renal, transrectal) and intravenous urography are useful for helping to
determine bladder and prostate size and the degree of hydronephrosis (if any) in patients with urinary
retention or signs of renal insufficiency. Generally, they are not indicated for the initial evaluation of
uncomplicated LUTS.
Endoscopy of the lower urinary tract
Cystoscopy may be indicated in patients scheduled for invasive treatment or in whom a foreign body or
malignancy is suspected. In addition, endoscopy may be indicated in patients with a history of sexually
transmitted disease (eg, gonococcal urethritis), prolonged catheterization, or trauma.
IPSS/AUA-SI
The severity of BPH can be determined with the International Prostate Symptom Score (IPSS)/American
Urological Association Symptom Index (AUA-SI) plus a disease-specific quality of life (QOL) question.
Questions on the AUA-SI for BPH concern the following:
Incomplete emptying
Frequency
Intermittency
Urgency
Weak stream
Straining
Nocturia
Other tests
Flow rate - Useful in the initial assessment and to help determine the patients response to
treatment
PVR urine volume - Used to gauge the severity of bladder decompensation; it can be obtained
invasively with a catheter or noninvasively with a transabdominal ultrasonic scanner
Pressure flow studies - Findings may prove useful for evaluating for BOO
Urodynamic studies - To help distinguish poor bladder contraction ability (detrusor underactivity)
from BOO
Cytologic examination of the urine - May be considered in patients with predominantly irritative
voiding symptoms
See Workup for more detail.
Management
Pharmacologic treatment
Agents used in the treatment of BPH include the following:
Alpha-1receptor blockers
Alpha-adrenergic receptor blockers
Phosphodiesterase-5 enzyme inhibitors
5-alpha reductase inhibitors
Anticholinergic agents
Surgery
Transurethral resection of the prostate (TURP) - The criterion standard for relieving BOO
secondary to BPH
Open prostatectomy - Reserved for patients with very large prostates (>75 g), patients with
concomitant bladder stones or bladder diverticula, and patients who cannot be positioned for
transurethral surgery
Minimally invasive treatment
Transurethral incision of the prostate (TUIP)
Laser treatment - Used to cut or destroy prostate tissue
Transurethral microwave therapy (TUMT) - Generates heat that causes cell death in the prostate,
leading to prostatic contraction and volume reduction
Transurethral needle ablation of the prostate (TUNA)
High-intensity ultrasonographic energy therapy - Currently in the clinical trial stage
Prostatic stents - Flexible devices that expand when put in place to improve the flow of urine past
the prostate
Laparoscopic prostatectomy
See Treatment and Medication for more detail.
Image library

Normal prostate anatomy. The prostate is located at the apex of the bladder and surrounds the proximal
urethra.

Background
Benign prostatic hyperplasia (BPH), also known as benign prostatic hypertrophy, is a histologic
diagnosis characterized by proliferation of the cellular elements of the prostate. Cellular
accumulation and gland enlargement may result from epithelial and stromal proliferation,
impaired preprogrammed cell death (apoptosis), or both.
BPH involves the stromal and epithelial elements of the prostate arising in the periurethral and
transition zones of the gland (see Pathophysiology). The hyperplasia presumably results in
enlargement of the prostate that may restrict the flow of urine from the bladder.
BPH is considered a normal part of the aging process in men and is hormonally dependent on
testosterone and dihydrotestosterone (DHT) production. An estimated 50% of men demonstrate
histopathologic BPH by age 60 years. This number increases to 90% by age 85 years.
The voiding dysfunction that results from prostate gland enlargement and bladder outlet
obstruction (BOO) is termed lower urinary tract symptoms (LUTS). It has also been commonly
referred to as prostatism, although this term has decreased in popularity. These entities overlap;
not all men with BPH have LUTS, and likewise, not all men with LUTS have BPH.
Approximately half of men diagnosed with histopathologic BPH demonstrate moderate-to-severe
LUTS.
Clinical manifestations of LUTS include urinary frequency, urgency, nocturia (awakening at
night to urinate), decreased or intermittent force of stream, or a sensation of incomplete
emptying. Complications occur less commonly but may include acute urinary retention (AUR),
impaired bladder emptying, the need for corrective surgery, renal failure, recurrent urinary tract
infections, bladder stones, or gross hematuria. (See Clinical Presentation.)
Prostate volume may increase over time in men with BPH. In addition, peak urinary flow, voided
volume, and symptoms may worsen over time in men with untreated BPH (see Workup). The
risk of AUR and the need for corrective surgery increases with age.
Patients who are not bothered by their symptoms and are not experiencing complications of BPH
should be managed with a strategy of watchful waiting. Patients with mild LUTS can be treated
initially with medical therapy. Transurethral resection of the prostate (TURP) is considered the
criterion standard for relieving bladder outlet obstruction (BOO) secondary to BPH. However,
there is considerable interest in the development of minimally invasive therapies to accomplish
the goal of TURP while avoiding its adverse effects (see Treatment and Management).
Anatomy
The prostate is a walnut-sized gland that forms part of the male reproductive system. It is located
anterior to the rectum and just distal to the urinary bladder. It is in continuum with the urinary
tract and connects directly with the penile urethra. It is therefore a conduit between the bladder
and the urethra. (See the image below.)
Normal prostate anatomy. The prostate is located at the apex of the bladder
and surrounds the proximal urethra.
The gland is composed of several zones or lobes that are enclosed by an outer layer of tissue
(capsule). These include the peripheral, central, anterior fibromuscular stroma, and transition
zones. BPH originates in the transition zone, which surrounds the urethra.
Pathophysiology
Prostatic enlargement depends on the potent androgen dihydrotestosterone (DHT). In the prostate
gland, type II 5-alpha-reductase metabolizes circulating testosterone into DHT, which works
locally, not systemically. DHT binds to androgen receptors in the cell nuclei, potentially
resulting in BPH.
In vitro studies have shown that large numbers of alpha-1-adrenergic receptors are located in the
smooth muscle of the stroma and capsule of the prostate, as well as in the bladder neck.
Stimulation of these receptors causes an increase in smooth-muscle tone, which can worsen
LUTS. Conversely, blockade of these receptors (see Treatment and Management) can reversibly
relax these muscles, with subsequent relief of LUTS.
Microscopically, BPH is characterized as a hyperplastic process. The hyperplasia results in
enlargement of the prostate that may restrict the flow of urine from the bladder, resulting in
clinical manifestations of BPH. The prostate enlarges with age in a hormonally dependent
manner. Notably, castrated males (ie, who are unable to make testosterone) do not develop BPH.
The traditional theory behind BPH is that, as the prostate enlarges, the surrounding capsule
prevents it from radially expanding, potentially resulting in urethral compression. However,
obstruction-induced bladder dysfunction contributes significantly to LUTS. The bladder wall
becomes thickened, trabeculated, and irritable when it is forced to hypertrophy and increase its
own contractile force.
This increased sensitivity (detrusor overactivity [DO]), even with small volumes of urine in the
bladder, is believed to contribute to urinary frequency and LUTS. The bladder may gradually
weaken and lose the ability to empty completely, leading to increased residual urine volume and,
possibly, acute or chronic urinary retention.
In the bladder, obstruction leads to smooth-muscle-cell hypertrophy. Biopsy specimens of
trabeculated bladders demonstrate evidence of scarce smooth-muscle fibers with an increase in
collagen. The collagen fibers limit compliance, leading to higher bladder pressures upon filling.
In addition, their presence limits shortening of adjacent smooth muscle cells, leading to impaired
emptying and the development of residual urine.
The main function of the prostate gland is to secrete an alkaline fluid that comprises
approximately 70% of the seminal volume. The secretions produce lubrication and nutrition for
the sperm. The alkaline fluid in the ejaculate results in liquefaction of the seminal plug and helps
to neutralize the acidic vaginal environment.
The prostatic urethra is a conduit for semen and prevents retrograde ejaculation (ie, ejaculation
resulting in semen being forced backwards into the bladder) by closing off the bladder neck
during sexual climax. Ejaculation involves a coordinated contraction of many different
components, including the smooth muscles of the seminal vesicles, vasa deferentia, ejaculatory
ducts, and the ischiocavernosus and bulbocavernosus muscles.
Epidemiology
BPH is a common problem that affects the quality of life in approximately one third of men older
than 50 years. BPH is histologically evident in up to 90% of men by age 85 years. As many as 14
million men in the United States have symptoms of BPH. Worldwide, approximately 30 million
men have symptoms related to BPH.
The prevalence of BPH in white and African-American men is similar. However, BPH tends to
be more severe and progressive in African-American men, possibly because of the higher
testosterone levels, 5-alpha-reductase activity, androgen receptor expression, and growth factor
activity in this population. The increased activity leads to an increased rate of prostatic
hyperplasia and subsequent enlargement and its sequelae
Prognosis
In the past, chronic end-stage BOO often led to renal failure and uremia. Although this
complication has become much less common, chronic BOO secondary to BPH may lead to
urinary retention, renal insufficiency, recurrent urinary tract infections, gross hematuria, and
bladder calculi.
Patient Education
For patient education information, see the Prostate Health Center and Kidneys and Urinary
System Center, as well as Enlarged Prostate, Bladder Control Problems, and Inability to Urinate
History
The diagnosis of benign prostatic hyperplasia (BPH) can often be suggested on the basis of the
history alone. Special attention to the following features is essential to making the correct
diagnosis:
Onset and duration of symptoms
General health issues (including sexual history)
Fitness for any possible surgical interventions
Severity of symptoms and how they are affecting quality of life
Medications
Previously attempted treatments
Symptoms often attributed to BPH can be caused by other disease processes, and a history and
physical examination are essential in ruling out other etiologies of (lower urinary tract symptoms
(LUTS) (see Diagnostic Considerations).
When the prostate enlarges, it may act like a "clamp on a hose," constricting the flow of urine.
Nerves within the prostate and bladder may also play a role in causing the following common
symptoms:
Urinary frequency - The need to urinate frequently during the day or night (nocturia),
usually voiding only small amounts of urine with each episode
Urinary urgency - The sudden, urgent need to urinate, owing to the sensation of imminent
loss of urine without control
Hesitancy - Difficulty initiating the urinary stream; interrupted, weak stream
Incomplete bladder emptying - The feeling of persistent residual urine, regardless of the
frequency of urination
Straining - The need strain or push (Valsalva maneuver) to initiate and maintain urination
in order to more fully evacuate the bladder
Decreased force of stream - The subjective loss of force of the urinary stream over time
Dribbling - The loss of small amounts of urine due to a poor urinary stream
A sexual history is important, as epidemiologic studies have identified LUTS as an independent
risk factor for erectile dysfunction and ejaculatory dysfunction.
[2]

Physical Examination
Conduct a focused physical examination to assess the suprapubic area for signs of bladder
distention and a neurological examination for sensory and motor deficits.
The digital rectal examination (DRE) is an integral part of the evaluation in men with presumed
BPH. During this portion of the examination, prostate size and contour can be assessed, nodules
can be evaluated, and areas suggestive of malignancy can be detected. The normal prostate
volume in a young man is approximately 20 g.
A more precise volumetric determination can be made using transrectal ultrasonography (TRUS)
of the prostate.
Decreased anal sphincter tone or the lack of a bulbocavernosus muscle reflex may indicate an
underlying neurological disorder.
The prostate is examined using the index finger of the dominant hand. The finger is placed
through the anus after relaxation of the anal sphincter, and the prostate is palpated
circumferentially (analogous to a windshield wiper movement).
In general, an estimation of the number of index finger pads that one can sweep over the rectal
surface of the prostate during DRE is a useful way for nonurologist examiners to communicate
estimated gland size. Anecdotally, each fingerbreadth correlates to approximately 15-20 g of
tissue. For example, one can report the prostate size as "2-3 fingerbreadths wide" when charting
in the medical record or communicating with a colleague. Most asymptomatic men have glands
of 2 fingerbreadths or less.
In addition, pelvic floor tone, the presence or absence of fluctuance (ie, prostate abscess), and
pain sensitivity of the gland (prostatodynia/prostatitis) can be assessed.
Complications
Complications related to bladder outlet obstruction (BOO) secondary to BPH include the
following:
Urinary retention
Renal insufficiency
Recurrent urinary tract infections
Gross hematuria
Bladder calculi
Renal failure or uremia (rare in current practice)
Diagnostic Considerations
Symptoms often attributed to benign prostatic hyperplasia (BPH) can be caused by any of the
following conditions:
Cystitis
Prostatitis
Prostatodynia
Prostatic abscess
Overactive bladder (OAB)
Carcinoma of the bladder
Foreign bodies in the bladder (stones or retained stents)
Urethral stricture due to trauma or a sexually transmitted disease
Prostate cancer
Neurogenic bladder
Pelvic floor dysfunction
Excluding these entities based on findings from a thorough history and appropriately directed
diagnostic studies is essential.
Differential Diagnoses
Bladder Cancer
Bladder Stones
Bladder Trauma
Chronic Pelvic Pain
Interstitial Cystitis
Neurogenic Bladder
Prostatitis, Bacterial
Radiation Cystitis
Urethral Strictures
Urinary Tract Infection, Males
Approach Considerations
In 2011, the American Urological Association (AUA) published a 2010 update to their
Guideline on the Management of Benign Prostatic Hyperplasia. The update included an
algorithm for the diagnosis and basic treatment of LUTS, which is presented below.
[1]

Basic management of lower urinary tract symptoms (LUTS)
in men
A prospective, multicenter study in 3 European countries called the Diagnosis
Improvement in PrimAry Care Trial (D-IMPACT) found that in three quarters of the men
aged 50 years and older who spontaneously reported LUTS to their general practitioner,
those who were given an in-office diagnostic algorithm that included just the objective
variables of age, PSS, and PSA were accurately diagnosed for BPH by their general
practitioner.
[3]

Urinalysis
Examine the urine using dipstick methods and/or via centrifuged sediment evaluation to
assess for the presence of blood, leukocytes, bacteria, protein, or glucose.
Urine Culture
This may be useful to exclude infectious causes of irritative voiding and is usually
performed if the initial urinalysis findings indicate an abnormality.
Prostate-Specific Antigen
Although BPH does not cause prostate cancer, men at risk for BPH are also at risk for prostate
cancer and should be screened accordingly. Screening for prostate cancer remains controversial
and should done after an informed discussion between the physician and patient.
The 2010 update of the American Cancer Society (ACS) guideline for early detection of prostate
cancer stresses the importance of involving men in the decision whether to test for prostate
cancer. The ACS notes that PSA testing may reduce the likelihood of dying from prostate cancer
but poses serious risks, particularly of treatment of prostate cancer that would not have caused ill
effects if left undetected.
[4]

The ACS recommends that men receive information about the uncertainties, risks, and potential
benefits associated with prostate cancer screening. After this discussion, if the patient wishes to
proceed with screening (ie, prostate-specific antigen [PSA] testing and digital rectal examination
[DRE] for prostate cancer), the ACS recommends proceeding with screening at the following
ages:
Starting at age 50 years in men who are expected to live at least 10 more years
Starting at age 45 years in men at high risk for prostate cancer (African-Americans and men with
a close relative with prostate cancer)
A physician should discuss the risks and benefits of PSA screening with the patient. Notably,
men with larger prostates may have slightly higher PSA levels.
Electrolytes, BUN, and Creatinine
These evaluations are useful screening tools for chronic renal insufficiency in patients who have
high postvoid residual (PVR) urine volumes. A routine serum creatinine measurement is not
indicated in the initial evaluation of men with lower urinary tract symptoms (LUTS) secondary
to BPH.
[1]

Ultrasonography
Ultrasonography (abdominal, renal, transrectal) and intravenous urography are useful for helping
determine bladder and prostate size and the degree of hydronephrosis (if any) in patients with
urinary retention or signs of renal insufficiency. Generally, they are not indicated for the initial
evaluation of uncomplicated LUTS.
Transrectal ultrasonography (TRUS) of the prostate is recommended in selected patients, to
determine the dimensions and volume of the prostate gland. The success of certain minimally
invasive treatments may depend on the anatomical characteristics of the gland. In patients with
elevated PSA levels, TRUS-guided biopsy may be indicated.
Imaging of the upper tracts is indicated in patients who present with concomitant hematuria, a
history of urolithiasis, an elevated creatinine level, high PVR volume, or history of upper urinary
tract infection.
Other imaging studies, such as CT scanning and MRI, have no role in the evaluation and
treatment of uncomplicated BPH.
American Urological Association Guidelines
The American Urological Association (AUA) has developed rigorous clinical practice guidelines
for BPH based on the 1994 Agency for Healthcare Research and Quality clinical practice
guidelines for BPH. In 2006, the AUA Practice Guidelines Committee updated the 1994
evidence-based guidelines for the diagnosis and treatment of BPH originally created under the
auspices of the United States Department of Health and Human Services Agency for Health Care
Policy and Research.
[5, 6]

The AUA 2010 BPH guideline update lowered the age of the Index Patient from age 50 years or
older to age 45 years or older. Two algorithms were published: the algorithm for diagnosis and
basic management of LUTS in the Approach section above, and an algorithm for detailed
management of bothersome LUTS that persists after basic management, shown below.
[1]

Benign prostatic hyperplasia (BPH) diagnosis and treatment
algorithm.
These panels have established the following categories to classify diagnostic tests and studies. A
recommended test is one that should be performed on every patient, whereas an optional test is
of proven value in selected patients.
Recommended tests
A medical history should be taken to qualify and quantify voiding dysfunction. Identification of
other causes of voiding dysfunction and medical comorbidities are essential to properly assess
the condition and to determine conditions that may complicate treatment.
The physical examination consists of a focused physical examination and a neurologic
examination. The physical examination includes a DRE to measure prostate size and to assess for
abnormalities. The neurological examination is geared toward lower-extremity neurologic and
muscular function, as well as anal sphincter tone. Examination of the phallus and foreskin
occasionally reveals meatal stenosis, unretractable foreskin, penile ulcers, or foreign bodies such
as warts.
PSA testing should be offered to any patient with a 10-year life expectancy in whom the
diagnosis of prostate cancer would change management.
The severity of BPH can be determined with the International Prostate Symptom Score
(IPSS)/American Urological Association Symptom Index (AUA-SI) plus a disease-specific
quality of life (QOL) question. The AUA-SI for BPH is a set of 7 questions that has been
adopted worldwide and yields reproducible and quantifiable information regarding symptoms
and response to treatment. Questions concern incomplete emptying, frequency, intermittency,
urgency, weak stream, straining, and nocturia.
The IPSS uses the same 7 questions as the AUA-SI, with the addition of an eighth question,
known as the bother score, which is designed to assess perceived disease-specific QOL. The
AUA-SI/IPSS questionnaire is available online. Based on the sum of the score for all 8
questions, patients are classified as 0-7 (mildly symptomatic), 8-19 (moderately symptomatic), or
20-35 (severely symptomatic).
Optional tests
Flow rate is useful in the initial assessment and to help determine the response to treatment. It
may be performed prior to embarking on any active treatments, including medical treatment.
A maximal flow rate (Qmax) is the single best measurement, but a low Qmax does not help
differentiate between obstruction and poor bladder contractility. For more detailed analysis, a
pressure flow study (urodynamic testing) is required. A Qmax value of greater than 15 mL/s is
considered by many to be normal. A value of less than 7 mL/s is widely accepted as low.
The results of flow rate measurements are somewhat effort- and volume-dependent. Therefore,
the best plan to make a reasonable determination of significance is to obtain at least 2 tracings
with at least 150 mL of voided volume each time.
Obtain postvoid residual urine in order to gauge the severity of bladder decompensation. It can
be obtained invasively with a catheter or noninvasively with a transabdominal ultrasonic scanner.
A high PVR (ie, 350 mL) may indicate bladder dysfunction and/or bladder outlet obstruction and
may predict a poor response to treatment.
Although pressure flow studies are somewhat invasive, requiring catheterization of the urethra
and placement of a transrectal pressure transducer, the findings may prove useful for evaluating
for bladder outlet obstruction (BOO).
Urodynamic studies are the only way to help distinguish poor bladder contraction ability
(detrusor underactivity) from outlet obstruction. BOO is characterized by high intravesical
voiding pressures (>60 cm water) accompanied by low urine flow rates (Qmax < 15 mL/s).
Cytologic examination of the urine may be considered in patients with predominantly irritative
voiding symptoms. Risk factors for bladder cancer (smoking, previous bladder cancer) should
alert the physician to consider this noninvasive test.
Tests that are not recommended
Routine measurement of serum creatinine is not indicated in the initial evaluation of men with
LUTS secondary to BPH.
Endoscopy of the Lower Urinary Tract
Cystoscopy may be indicated in patients scheduled for invasive treatment or in whom a foreign
body or malignancy is suspected. In addition, endoscopy may be indicated in patients with a
history of sexually transmitted disease (eg, gonococcal urethritis), prolonged catheterization, or
trauma. Findings may suggest urethral stricture as the cause of BOO, instead of BPH.
Flexible cystoscopy can be easily performed in several minutes in an office-based setting using
topical gel-based intraurethral anesthesia without sedation. The appearance of the gland alone on
cystoscopy cannot make the diagnosis of obstruction but can help the clinician decide on
treatment modalities if intervention is warranted.
Histologic Findings
BPH is characterized by a varying combination of epithelial and stromal hyperplasia in the
prostate. Some cases demonstrate an almost pure smooth-muscle proliferation, although most
demonstrate a fibroadenomyomatous pattern of hyperplasia.
In the bladder, obstruction leads to smooth-muscle-cell hypertrophy. Biopsy specimens of
trabeculated bladders demonstrate evidence of scarce smooth-muscle fibers with an increase in
collagen.
Approach Considerations
Patients with mild symptoms (IPSS/AUA-SI score < 7) or moderate-to-severe symptoms
(IPSS/AUA-SI score 8) of benign prostatic hyperplasia (BPH) who are not bothered by their
symptoms and are not experiencing complications of BPH should be managed with a strategy of
watchful waiting. In these situations, medical therapy is not likely to improve their symptoms
and/or quality of life (QOL). In addition, the risks of treatment may outweigh any benefits.
Patients managed expectantly with watchful waiting are usually re-examined annually.
Transurethral resection of the prostate (TURP) has long been accepted as the criterion standard
for relieving bladder outlet obstruction (BOO) secondary to BPH. In current clinical practice,
most patients with BPH do not present with obvious surgical indications; instead, they often have
milder lower urinary tract symptoms (LUTS) and, therefore, are initially treated with medical
therapy.
The era of medical therapy for BPH dawned in the mid 1970s with the use of nonselective alpha-
blockers such as phenoxybenzamine. The medical therapeutic options for BPH have evolved
significantly over the last 3 decades, giving rise to the receptor-specific alpha-blockers that
comprise the first line of therapy.
Alpha-1Receptor Blockade in Benign Prostatic Hyperplasia
A significant component of LUTS secondary to BPH is believed to be related to the smooth-
muscle tension in the prostate stroma, urethra, and bladder neck. The smooth-muscle tension is
mediated by the alpha-1-adrenergic receptors; therefore, alpha-adrenergic receptorblocking
agents should theoretically decrease resistance along the bladder neck, prostate, and urethra by
relaxing the smooth muscle and allowing passage of urine.
BPH is predominantly a stromal proliferative process, and a significant component of prostatic
enlargement results from smooth-muscle proliferation. The stromal-to-epithelial ratio is
significantly greater in men with symptomatic BPH than in those with asymptomatic BPH.
The 3 subtypes of the alpha-1 receptor include 1a, 1b, and 1c. Of these, the alpha-1a receptor is
most specifically concentrated in the bladder neck and prostate. Provided that the alpha-1a
subtype is predominant in the prostate, bladder neck, and urethra, but not in other tissues, drugs
that are selective for this receptor (ie, tamsulosin) may have a potential therapeutic advantage.
Tamsulosin is considered the most pharmacologically uroselective of the commercially available
agents because of its highest relative affinity for the alpha-1a receptor subtype. In 2008, the US
Food and Drug Administration (FDA) approved a new alpha-1a receptor selective blocker,
silodosin (Rapaflo). It is indicated for treatment of the signs and symptoms of BPH.
The efficacy of the titratable alpha-blockers doxazosin and terazosin (Hytrin) is dose-dependent.
Maximum tolerable doses have not been defined for any alpha-blocker; however, the higher the
dose, the more likely the adverse events (orthostatic hypotension, dizziness, fatigue, ejaculatory
disorder, nasal congestion). Despite the requirement for dose titration and blood pressure
monitoring, these older, often less costly, alpha-blockers appear to be equally effective to
tamsulosin and alfuzosin, and the 2010 AUA guidelines state that they remain reasonable choices
for patients with moderate-to-severe LUTS due to BPH.
[1]

An approximately 4- to 6-point improvement is expected in IPSS/AUA-SI scores when alpha-
blockers are used. Interestingly, alpha-blocker therapy has not been shown to reduce the overall
long-term risk for acute urinary retention (AUR) or BPH-related surgery.
[7]

Hellstrom and Sikka reported in 2006 that the acute administration of tamsulosin effects
ejaculatory function and ejaculate volume. Nearly 90% of study subjects experienced decreased
ejaculate volume, and approximately 35% experienced anejaculation. In their study, subjects
treated with alfuzosin or placebo did not experience anejaculation.
[8]

Alpha-adrenergic receptor blockers
The alpha-blocking agents administered in BPH studies can be subgrouped according to receptor
subtype selectivity and the duration of serum elimination half-lives, as follows:
Nonselective alpha-blockers - phenoxybenzamine
Selective short-acting alpha-1 blockers - prazosin, alfuzosin, indoramin
Selective long-acting alpha-1 blockers - terazosin, doxazosin, slow-release (SR)
alfuzosin.
Partially subtype (alpha-1a)selective agents tamsulosin, silodosin
Nonselective alpha-blockers
Phenoxybenzamine was the first alpha-blocker studied for BPH. It is nonselective, antagonizing
both the alpha 1- and alpha 2-adrenergic receptors, which results in a higher incidence of adverse
effects. Because of the availability of more alpha-1-receptorspecific agents, phenoxybenzamine
is currently not often used for the treatment of BPH. The 2010 update to the AUA guideline for
BPH retains the statement that insufficient data exist for a recommendation of
phenoxybenzamine or of prazosin for treatment of LUTS secondary to BPH. This statement was
originally published in the 2003 AUA BPH guidelines.
[1]

Phosphodiesterase-5 enzyme inhibitors
Statistically significant symptomatic improvements have been reported for patients with BPH
receiving tadalafil. It has also been approved for the treatment of simultaneous BPH and erectile
dysfunction (ED). Phosphdiesterase-5 (PDE5) inhibitors are known to mediate smooth muscle
relaxation in the lower urinary tract.
Intraoperative floppy iris syndrome
Intraoperative floppy iris syndrome (IFIS) is characterized by miosis, iris billowing, and prolapse
in patients undergoing cataract surgery who have taken or currently take alpha-1-blockers. It is
particularly prevalent among patients taking tamsulosin. The 2010 AUA guideline recommends
that clinicians ask patients about planned cataract surgery when offering alpha-blocker therapy
for LUTS due to BPH. Alpha-blockers should not be initiated until cataract surgery is
completed.
[1]
Patients currently on alpha-blocker therapy must disclose this to their
ophthalmologist prior to cataract surgery so that the appropriate preoperative and intraoperative
precautions can be taken. Experienced ophthalmologists can thereby reduce the risk of
complications from IFIS.
[9, 1]

In a review by Bell et al, exposure to tamsulosin within 14 days of cataract surgery was
significantly associated with serious postoperative ophthalmic adverse events, specifically IFIS
and its complications (ie, retinal detachment, lost lens or fragments, endophthalmitis). No
significant associations were noted with exposure to other alpha-blocker medications or to
previous exposure to tamsulosin or other alpha-blockers.
[10]

5-Alpha-Reductase Inhibitors in Benign Prostatic Hyperplasia
Hormonal medical management emerged from the discovery of a congenital form of
pseudohermaphroditism secondary to DHT deficiency (due to a lack of 5-alpha-reductase
activity). This deficiency produced a hypoplastic prostate. The two types of 5-alpha-reductase
include type 1 (predominantly located in extraprostatic tissues, such as skin and liver) and type 2
(predominant prostatic reductase).
Inhibition of 5-alpha-reductase type 2 blocks the conversion of testosterone to DHT, resulting in
lower intraprostatic levels of DHT. This leads to inhibition of prostatic growth, apoptosis, and
involution. The exact role of 5-alpha-reductase type 1 in normal and abnormal prostatic
development is undefined. 5-Alpha-reductase inhibitors improve LUTS by decreasing prostate
volumes; thus, patients with larger prostates may achieve a greater benefit. Further, maximal
reduction in prostate volume requires 6 months of therapy.
5-Alpha reductase inhibitors
Finasteride (Proscar), a 4-aza-steroid, has demonstrated 5-alpha type IIblocking activity,
resulting in the inhibition of DHT-receptor complex formation. This effect causes a profound
decrease in the concentration of DHT intraprostatically, resulting in a consistent decrease in
prostate size. One third of men treated with this agent exhibit improvements in urine flow and
symptoms.
Dutasteride (Avodart) has an affinity for both type 1 and type 2 5-alpha-reductase receptors. The
significance of blockage of type 1 receptors is currently unknown.
Both finasteride and dutasteride actively reduce DHT levels by more than 80%, improve
symptoms, reduce the incidence of urinary retention, and decrease the likelihood of surgery for
BPH. Adverse effects are primarily sexual in nature (decreased libido, erectile dysfunction,
ejaculation disorder).
Both finasteride and dutasteride may reduce serum prostate-specific antigen (PSA) values by as
much as 50%. The decrease in PSA is typically maximally achieved when the maximal decrease
in prostatic volume is noted (6 months). Thus, one must take this into account when using PSA
to screen for prostate cancer.
One prospective, randomized, double-blind study by the Enlarged Prostate International
Comparator Study (EPICS) was conducted to compare the efficacy of dutasteride to that of
finasteride in men with symptomatic BPH. While this study was conducted over the course of
only one year, the data suggest that both of these drugs were similarly effective in reducing
prostate volume, improving Qmax, and LUTS for this population. The long-term outcomes are
yet to be investigated.
[11]

Because these drugs interfere with the metabolism of testosterone, they are contraindicated in
children and pregnant females. In addition, pregnant females or those who are considering
conception should not handle crushed or broken tablets because of the potential for absorption
and subsequent potential risk to a male fetus.
In patients with LUTS and enlarged prostates, 5-alpha-reductase inhibitors are believed to be
appropriate and effective treatment.
5-Alpha reductase inhibitors and prostate cancer
On June 9, 2011, the US Food and Drug Administration (FDA) announced revisions to the
prescribing information for 5-alpha reductase inhibitors (5-ARIs). These agents include
finasteride (Proscar, Propecia) and dutasteride (Avodart, Jalyn). 5-ARIs are indicated for benign
prostatic hypertrophy and alopecia.
Data from 2 large, randomized, controlled trials observed an increased risk of being diagnosed
with a more serious form of prostate cancer (high-grade prostate cancer) in trial participants
taking 5-ARIs. The 2 trials are the Prostate Cancer Prevention Trial (PCPT) and the Reduction
by Dutasteride of Prostate Cancer Events (REDUCE) trial. Both of these trials observed a
decreased incidence of prostate cancer overall when preventive treatment included 5-ARIs, but
an increased incidence of high-grade prostate cancer in men taking dutasteride or finasteride
compared with placebo.
[12, 13]

The revised prescribing information recommends that prior to initiating therapy with 5-ARIs,
perform appropriate evaluations to rule out other urological conditions, including prostate
cancer, that might mimic benign prostatic hyperplasia (BPH).
Combination Therapy
The alpha-1-receptor blockers provide rapid relief, while the 5-alpha-reductase inhibitors target
the underlying disease process.
[7]
The Medical Therapy of Prostatic Symptoms (MTOPS) trial
demonstrated that combination therapy reduced the risk of progression and produced a greater
improvement in IPSS than therapy with finasteride or doxazosin alone. The risks of AUR and
BPH-related surgery were reduced with combination therapy or finasteride in comparison with
doxazosin monotherapy.
[14]

The Symptom Management After Reducing Therapy (SMART-1) trial demonstrated that after 6
months of combination therapy, discontinuation of the alpha-1-blocker is possible in men with
moderate LUTS. However, those with severe LUTS may require longer combination therapy.
[14]

Anticholinergic Agents
Historically, anticholinergics were discouraged in men with BPH because of concerns of
inducing urinary retention. Trials have demonstrated a slight increase in PVR; however, AUR
rates were low. Importantly, these trials consisted of patients with low baseline PVR.
The 2010 AUA BPH guidelines recommend anticholinergic agents for management of LUTS in
patients who do not have an elevated PVR and whose LUTS are primarily irritative. Baseline
PVR should be obtained prior to initiation of anticholinergic therapy, to assess for urinary
retention.
[15]
Caution with anticholinergics is recommended with patients whose PVR is greater
than 250-300 mL.
[1]

Landmark Clinical Trials
Numerous phase II and phase III trials of drugs used in the treatment of BPH have been
conducted. A few landmark studies are selected below.
The Proscar Long-Term Efficacy and Safety Study (PLESS), patients treated with finasteride (5
mg/d) were at a significantly lower risk of developing AUR or needing surgery.
[16]
This was a
multicenter, 4-year, double-blind, placebo-controlled study of 3,040 men. Men with PSA levels
of more than 10 ng/mL and those with prostate cancer were excluded.
The Medical Therapy of Prostatic Symptoms (MTOPS) trial demonstrated that combination
therapy with doxazosin and finasteride was well tolerated, and was superior to placebo and
monotherapy with either agent. The primary endpoints of the study were reduction in AUA-SI
score, AUR, recurrent infections, renal insufficiency, incontinence, changes in flow, and PSA
level and a lower rate of invasive treatments. MTOPS was a multicenter, 4- to 6-year, double-
blind, randomized, placebo-controlled trial of 3,047 men with symptomatic BPH.
[17]

In the Alfuzosin Long-Term Efficacy and Safety Study (ALTESS), alfuzosin (10 mg/d)
decreased the risk of LUTS deterioration and significantly improved QOL and peak urinary flow
rate. ALTESS was a 2-year, double-blind, placebo-controlled study of 1,522 men. Notably, these
men had greater risk factors for BPH progression (ie, older age, higher IPSS scores, larger
prostate size, lower Qmax, and higher PVR) than those in the MTOPS trial. Alfuzosin did not
reduce the risk of AUR but tended to reduce the risk of surgery.
[18]

In the international real-life practice study of alfuzosin once daily (ALF-ONE), 3 years of
alfuzosin (10 mg/d) decreased IPSS by one third, with significant improvements in nocturia and
bother score. ALF-ONE was conducted in 689 European men with a mean age of 67.6 years.
Clinical progression of worsening of IPSS (4 points) was seen in 12.4%, AUR in 2.6%, and
requirement of BPH-related surgery in 5.7%. Alfuzosin was well tolerated, with dizziness the
most common adverse effect (4.5%). Notably, symptom worsening during treatment and high
PSA levels appeared to be the best predictors of clinical progression.
[19]

Four-year results in the Combination of Avodart and Tamsulosin (CombAT) study revealed that
for men with prostate volumes of 30-58 mL, combination therapy with dutasteride (dual 5-alpha-
reductase inhibitor) and tamsulosin (alpha-1-blocker) improved symptoms, urinary flow, and
QOL better than monotherapy with either drug, although not in men who had a prostate volume
of 58 mL or more.
[20]
The adverse-effect profile of combination therapy was similar to that of
monotherapy, although drug-related adverse events were more common with combination
therapy.
[21]
CombAT is a 4-year, multicenter, randomized, double-blind, parallel group study of
4,844 men aged 50 years or older with moderate-to-severe BPH symptoms (IPSS 12), prostate
volume of 30 mL or greater, and a PSA level of 1.5-10 ng/mL. This study contributes to the
standard of care shifting towards combined drug therapy in appropriately selected patients, while
better defining the role of the alpha-blockers.
[15]

Phytotherapeutic Agents and Dietary Supplements
Phytotherapeutic agents and dietary supplements are considered emerging therapy by the AUA
Guidelines panel and are not recommended for the treatment of BPH because of the lack of
evidence at this time.
Pharmaceuticals derived from plant extracts are widely used throughout the world for the
treatment of various medical ailments. In 1998, Americans spent a total of $3.65 billion on all
herbal remedies. In France and Germany, plant extracts have a market share of up to 50% of all
drugs prescribed for symptomatic BPH. In the United States, these agents are also popular and
readily available.
The attraction to phytotherapeutic agents appears to be related to the perception of therapeutic
healing powers of natural herbs, the ready availability, and the lack of adverse effects.
Most of the phytotherapeutic agents used in the treatment of LUTS secondary to BPH are
extracted from the roots, seeds, bark, or fruits of plants listed below. Some suggested active
components include phytosterols, fatty acids, lectins, flavonoids, plant oils, and polysaccharides.
Some preparations derive from a single plant; others contain extracts from 2 or more sources.
Each agent has one or more proposed modes of action. The following modes of action are
suggested:
Antiandrogenic effect
Antiestrogenic effect
Inhibition of 5-alpha-reductase
Blockage of alpha receptors
Antiedematous effect
Anti-inflammatory effect
Inhibition of prostatic cell proliferation
Interference with prostaglandin metabolism
Protection and strengthening of detrusor
The origins of phytotherapeutic agents are as follows:
Saw palmetto, (American dwarf palm; Serenoa repens, Sabal serrulata) fruit
South African star grass (Hypoxis rooperi) roots
African plum tree (Pygeum africanum) bark
Stinging nettle (Urtica dioica) roots
Rye (Secale cereale) pollen
Pumpkin (Cucurbita pepo) seeds
Saw palmetto (American dwarf palm)
Extracts of saw palmetto berries are the most popular botanical products for BPH. The active
components are believed to be a mixture of fatty acids, phytosterols, and alcohols. The proposed
mechanisms of action are antiandrogenic effects, 5-alpha-reductase inhibition, and anti-
inflammatory effects.
The recommended dosage is 160 mg orally twice daily. Studies show significant subjective
improvement in symptoms without objective improvements in urodynamic parameters. Minimal
adverse effects include occasional GI discomfort.
The 2010 AUA guidelines, based on more recent studies, do not detect a clinically meaningful
effect of saw palmetto on LUTS. Further clinical trials are underway.
[1]
In fact, in a double-blind,
multicenter, placebo-controlled randomized trial at 11 North American clinical sites, saw
palmetto extract was studied at up to 3 times the standard dose on lower urinary tract symptoms
attributed to BPH. Saw palmetto extract was no more effective than placebo on the American
Urological Association Symptom Index. No clearly attributable adverse effects were identified.
Similar to the Saw Palmetto Treatment for Enlarged Prostates (STEP) study, saw palmetto was
not found to be beneficial for the treatment of LUTS in men.
[22]

African plum tree (P africanum)
Suggested mechanisms of action include inhibition of fibroblast proliferation and anti-
inflammatory and antiestrogenic effects. This extract is not well studied.
Rye (S cereale)
This extract is made from pollen taken from rye plants growing in southern Sweden. Suggested
mechanisms of action involve alpha-blockade, prostatic zinc level increase, and 5-alpha-
reductase activity inhibition. Significant symptomatic improvement versus placebo has been
reported.
Treatment of Concomitant Erectile Dysfunction
It is recommended to first establish the alpha-1 blocker dose before treating the erectile
dysfunction. The medication used to treat erectile dysfunction should be titrated to the lowest
effective dose. Furthermore, sildenafil doses of greater than 25 mg should not be taken within 4
hours of any alpha-blocker.
[23, 24, 25]

In addition to treating erectile dysfunction, sildenafil may improve mild-to-moderate LUTS.
Nitric oxide may mediate relaxation of the prostatic urethra and/or bladder neck. The utility of
phosphodiesterase inhibitors in the treatment of LUTS has yet to be defined.
[26]

Recent trials have addressed the use of long-acting phosphodiesterase type 5 inhibitors (tadalafil)
and have found them to be significantly better than placebo in improving the symptoms of
BPH/LUTS.
Transurethral Resection of the Prostate
TURP is considered the criterion standard for relieving BOO secondary to BPH. The indications
to proceed with a surgical intervention include the following:
AUR
Failed voiding trials
Recurrent gross hematuria
Urinary tract infection
Renal insufficiency secondary to obstruction
Additional indications for surgical intervention include failure of medical therapy, a desire to
terminate medical therapy, and/or financial constraints associated with medical therapy.
However, TURP carries a significant risk of morbidity (18%) and mortality risk (0.23%).
TURP is performed with regional or general anesthesia and involves the placement of a working
sheath in the urethra through which a hand-held device with an attached wire loop is placed.
High-energy electrical cutting current is run through the loop so that the loop can be used to
shave away prostatic tissue. The entire device is usually attached to a video camera to provide
vision for the surgeon.
Although TURP is often successful, it has some drawbacks. When prostatic tissue is cut away,
significant bleeding may occur, possibly resulting in termination of the procedure, blood
transfusion, and a prolonged hospital stay. Patients are usually monitored overnight and
discharged the following morning, with or without a catheter.
Irrigating fluid may also be absorbed in significant quantities through veins that are cut open,
with possible serious sequelae termed transurethral resection syndrome (TUR syndrome).
However, this is very rare and does not occur with saline irrigation used in bipolar devices. A
urinary catheter must be left in place until the bleeding has mostly cleared.
The large working sheath combined with the use of electrical energy may also result in
stricturing of the urethra.
The cutting of the prostate may also result in a partial resection of the urinary sphincteric
mechanism, causing the muscle along the bladder outlet to become weak or incompetent. As a
result, when the patient ejaculates, this sphincteric mechanism cannot keep the bladder
adequately closed. The ejaculate consequently goes backwards into the bladder (ie, retrograde
ejaculation), rather than out the penis. Additionally, if the urinary sphincter is damaged, urinary
incontinence may result.
The nerves associated with erection run along the outer rim of the prostate, and the high-energy
current and/or heat generated by such may damage these nerves, resulting in impotence.
Open Prostatectomy
This procedure is now reserved for patients with very large prostates (>75 g), patients with
concomitant bladder stones or bladder diverticula, and patients who cannot be positioned for
transurethral surgery.
Open prostatectomy requires hospitalization and involves the use of general/regional anesthesia
and a lower abdominal incision. The inner core of the prostate (adenoma), which represents the
transition zone, is shelled out, thus leaving the peripheral zone behind. This procedure may
involve significant blood loss, resulting in transfusion. Open prostatectomy usually has an
excellent outcome in terms of improvement of urinary flow and urinary symptoms.
More recently, laparoscopic simple prostatectomy has been performed at a number of institutions
and appears to be feasible. However, prostatectomy performed in this fashion still appears to be
associated with risk for significant blood loss. Experience to date with this procedure is
limited.
[27]

Minimally Invasive Treatment
There is considerable interest in the development of other therapies to decrease the amount of
obstructing prostate tissue while avoiding the above-mentioned adverse effects associated with
TURP. These therapies are collectively called minimally invasive therapies.
Most minimally invasive therapies rely on heat to destroy prostatic tissue. This heat is delivered
in a limited and controlled fashion, in the hope of avoiding the complications associated with
TURP. They also allow for the use of milder forms of anesthesia, which translates into less
anesthetic risk for the patient.
Heat may be delivered in the form of laser energy, microwaves, radiofrequency energy, high-
intensity ultrasound waves, and high-voltage electrical energy. As in TURP, delivery devices are
usually passed through a working sheath placed in the urethra, although they are usually of a
smaller size than that needed for TURP. Devices may also simply be attached or incorporated
into a urinary catheter or passed through the rectum, from which the prostate may also be
accessed.
Keep in mind that many of these minimally invasive therapies are undergoing constant
improvements and refinements, resulting in increased efficacy and safety. Ask urologists about
the specifics of the minimally invasive therapies that they use and what results they have
experienced.
Transurethral Incision of the Prostate
Transurethral incision of the prostate (TUIP) has been in use for many years and, for a long time,
was the only alternative to TURP. It may be performed with local anesthesia and sedation. TUIP
is suitable for patients with small prostates and for patients unlikely to tolerate TURP well
because of other medical conditions. TUIP is associated with less bleeding and fluid absorption
than TURP. It is also associated with a lower incidence of retrograde ejaculation and impotence
than TURP.
Lasers
Lasers deliver heat to the prostate in various ways. Lasers heat prostate tissue, causing tissue
death by coagulative necrosis, with subsequent tissue contraction; however, laser coagulation of
the prostate in this specific sense has met with limited results.
Lasers have also been used to directly evaporate, or to melt away, prostate tissue, which is more
effective than laser coagulation. Photoselective vaporization of the prostate produces a beam that
does not directly come into contact with the prostate; rather, it delivers heat energy into the
prostate, resulting in destruction/ablation of the prostate tissue.
Potassium-titanyl-phosphate (KTP) and holmium lasers are used to cut and/or enucleate the
prostate, similar to the TURP technique. These are widely used laser techniques.
Transurethral vaporization/ablation with the KTP or holmium laser can be performed with
general or spinal anesthesia and can be performed in an outpatient setting. Catheter time usually
lasts less than 24 hours. Studies suggest that photoselective vaporization of the prostate can
significantly improve and sustain symptomatic and urodynamic outcomes.
This procedure has been quite useful in patients who require anticoagulation for various medical
conditions, since anticoagulation does not need to be interrupted for this procedure, thus further
decreasing patient risk.
[28, 29]

Lasers may be used in a knifelike fashion to directly cut away prostate tissue (ie, holmium laser
enucleation of the prostate), similar to a TURP procedure. The holmium laser allows for
simultaneous cutting and coagulation, making it quite useful for prostate resection. Laser
enucleation of the prostate has proved to be safe and effective for treatment of symptomatic
BPH, regardless of prostate size, with low morbidity and short hospital stay.
TUR syndrome is not seen with this technique, because iso-osmotic saline is used for irrigation.
Additionally, removed prostatic tissue is available for histologic evaluation, whereas
vaporization/ablation technique does not provide tissue for evaluation. Holmium laser
enucleation of the prostate may prove to be the new criterion standard for surgical management
of BPH.
[29, 30]

Laser treatment usually results in decreased bleeding, fluid absorption, and length of hospital
stay, as well as decreased incidence of impotence and retrograde ejaculation when compared
with standard TURP. However, healing from laser treatment does not occur until after a period
when dead cells slough; thus, patients may experience urinary urgency or irritation, resulting in
frequent or uncomfortable urination for a few weeks.
The results of laser therapy vary from one another because not all wavelengths yield the same
tissue effects. For example, interstitial lasers (eg, indigo lasers) are designed to heat tissue within
the confines of the prostate gland and spread radiant energy at relatively low energy levels. They
do not directly involve the urethral portion; thus, irritative symptoms following the procedure are
potentially reduced.
Contact lasers such as KTP or holmium, on the other hand, are designed to cut and vaporize at
extremely high temperatures They usually bring about more relief of urinary symptoms than
treatment with medicines, but not always as much as is provided with TURP. However, KTP
laser vaporization and holmium laser enucleation yield results that rival those of TURP.
Transurethral Microwave Therapy
The use of microwave energy, termed transurethral microwave therapy (TUMT), delivers heat to
the prostate via a urethral catheter or a transrectal route. The surface closest to the probe (the
rectal or urethral surface) is cooled to prevent injury. The heat causes cell death, with subsequent
tissue contraction, thereby decreasing prostatic volume.
TUMT can be performed in the outpatient setting with local anesthesia. Microwave treatment
appears to be associated with significant prostatic swelling; a considerable number of patients
require a urinary catheter until the swelling subsides. In terms of efficacy, TUMT places between
medical therapy and TURP. The 2010 AUA guidelines state TUMT is an effective option for
partially relieving symptoms that may be considered in patients with moderate or severe LUTS
secondary to BPH.
[31]

Transurethral Needle Ablation of the Prostate
Transurethral needle ablation of the prostate (TUNA) involves using high-frequency radio waves
to produce heat, resulting in a similar process of thermal injury to the prostate as previously
described. A specially designed transurethral device with needles is used to deliver the energy.
TUNA can be performed under local anesthesia, allowing the patient to go home the same day.
Similar to microwave treatment, radiofrequency treatment is quite popular, and a number of
urologists have experience with its use. Radiofrequency treatment appears to reliably result in
significant relief of symptoms and better urine flow, although not quite to the extent achieved
with TURP. The 2010 AUA guideline update considers TURP an appropriate and effective
treatment option for moderate or severe LUTS.
[1]

High-Intensity Ultrasound Energy Therapy
High-intensity ultrasound energy therapy delivers heat to prostate tissue, with the subsequent
process of thermal injury. High-intensity ultrasound waves may be delivered rectally or
extracorporeally and can be used with the patient on intravenous sedation. Urinary retention
appears to be common with its use.
High-intensity ultrasound energy also produces moderate results in terms of improvement of the
urinary flow rate and urinary symptoms, although its use is now relatively limited compared with
the more popular TUNA and TUMT.
High-intensity ultrasound is considered investigational at this time and should not be offered
outside of clinical trials.
Mechanical Approaches
Mechanical approaches are used less commonly and are usually reserved for patients who cannot
have a formal surgical procedure. Mechanical approaches do not involve the use of energy to
treat the prostate.
Prostatic stents are flexible devices that can expand when put in place to improve the flow of
urine past the prostate. Complications associated with their use include encrustation, pain,
incontinence, and overgrowth of tissue through the stent, possibly making their removal quite
difficult.
In September 2013, the FDA authorized the marketing of the first permanent implant to relieve
low or blocked urine flow in men aged 50 years and older with an enlarged prostate. The UroLift
system (NeoTract Inc) relieves urine flow by pulling back prostate tissue that is pressing on the
urethra. Approval was based on 2 studies of 274 men with BPH implanted with 2 or more
UroLift sutures.
[32]
The UroLift was successfully inserted in 98% of participants, and a 30%
increase in urine flow and a steady amount of residual urine in the bladder was observed.
Patients reported fewer symptoms and improved quality of life in the 2 years following device
implantation.
Diet
Data from the Prostate Cancer Prevention Trial revealed that a diet low in fat and red meat and
high in protein and vegetables may reduce the risk of symptomatic BPH. Additionally, regular
alcohol consumption was associated with a reduced risk of symptomatic BPH, but this is to be
interpreted cautiously given the untoward effects of excessive alcohol consumption.
[33

Long-term Monitoring
Patients with BPH who have symptoms significant enough to be placed on medication should be
evaluated during office visits to discuss the efficacy of the medication and potential dose
adjustment. These visits should take place at least biannually. Patients should undergo DRE and
PSA screening at least annually.
Medication Summary
The goals of pharmacotherapy for benign prostatic hypertrophy (BPH) are to reduce morbidity
and to prevent complications. The agents used include alpha-adrenergic blockers, 5-alpha-
reductase inhibitors, and various combinations
Alpha-Adrenergic Blockers
Class Summary
These agents block effects of postganglionic synapses at the smooth muscle and exocrine glands.
View full drug information
Phenoxybenzamine (Dibenzyline)

Phenoxybenzamine is a nonselective alpha-adrenergic receptor blocker that antagonizes both
alpha-1 and alpha-2 receptors. This nonselectivity leads to a higher incidence of adverse effects,
which has led to decreased use of this agent in clinical settings. Phenoxybenzamine induces
subjective improvement in urinary flow rates when compared with placebo. It may improve
daytime and nighttime urinary frequency. Symptoms improve in 75% of patients.
Dosing Forms & Strengths
Hypertension Pheochromocytoma
10 mg PO BID initially; increase qOD to 20-40 mg PO BID/TID (sometimes higher doses
necessary)
Bladder Management (Off-label)
Initial 10 mg PO qD; can be increased q5d by 10 mg PO q8-12hr
Other Indications & Uses
Off-label: Raynaud's phenomenon, overactive bladder (neurogenic, prostatic obstruction), shock,
hypertensive emergencies d/t epinephrine
Drug Interactions
Interaction Checker
phenoxybenzamine and
Type a dru

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NAME

Contraindicated (0)
Serious - Use Alternative (4)
sildenafil
sildenafil increases effects of phenoxybenzamine by pharmacodynamic synergism.
Possible serious or life-threatening interaction. Monitor closely. Use alternatives if
available. Risk of hypotension; separate sildenafil >25mg from alpha blocker by 4hr.
tamsulosin
phenoxybenzamine, tamsulosin. Either increases effects of the other by additive
vasodilation. Possible serious or life-threatening interaction. Monitor closely. Use
alternatives if available. Risk of hypotension.
vardenafil
vardenafil increases effects of phenoxybenzamine by pharmacodynamic synergism. High
likelihood serious or life-threatening interaction. Contraindicated unless benefits
outweigh risks and no alternatives available. Never use combination. Risk of
hypotension.
yohimbe
yohimbe increases effects of phenoxybenzamine by pharmacodynamic synergism. High
outweigh risks and no alternatives available. Never use combination.
Significant - Monitor Closely (103)
acebutolol
phenoxybenzamine and acebutolol both increase anti-hypertensive channel blocking.
Potential for dangerous interaction. Use with caution and monitor closely.
aceclofenac
aceclofenac decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
Significant interaction possible, monitor closely. NSAIDs decrease prostaglandin
synthesis.
acemetacin
acemetacin decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
albuterol
phenoxybenzamine, albuterol. Mechanism: pharmacodynamic synergism. Significant
interaction possible, monitor closely. Hypotension, tachycardia.
aldesleukin
aldesleukin increases effects of phenoxybenzamine by pharmacodynamic synergism.
Potential for interaction, monitor. Risk of hypotension.
alfuzosin
alfuzosin and phenoxybenzamine both increase anti-hypertensive channel blocking.
Potential for interaction, monitor.
amifostine
amifostine increases effects of phenoxybenzamine by pharmacodynamic synergism.
amlodipine
phenoxybenzamine and amlodipine both increase anti-hypertensive channel blocking.
arformoterol
phenoxybenzamine, arformoterol. Mechanism: pharmacodynamic synergism. Significant
asenapine
asenapine and phenoxybenzamine both increase anti-hypertensive channel blocking.
aspirin
aspirin decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
aspirin rectal
aspirin rectal decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate decreases effects of phenoxybenzamine by
pharmacodynamic antagonism. Significant interaction possible, monitor closely. NSAIDs
decrease prostaglandin synthesis.
atenolol
phenoxybenzamine and atenolol both increase anti-hypertensive channel blocking.
avanafil
avanafil increases effects of phenoxybenzamine by pharmacodynamic synergism.
Significant interaction possible, monitor closely. Risk of hypotension.
bambuterol
phenoxybenzamine, bambuterol. Mechanism: pharmacodynamic synergism. Significant
benazepril
benazepril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
interaction possible, monitor closely. Exaggerated first dose hypotensive response.
betaxolol
phenoxybenzamine and betaxolol both increase anti-hypertensive channel blocking.
bisoprolol
phenoxybenzamine and bisoprolol both increase anti-hypertensive channel blocking.
captopril
captopril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
carbidopa
carbidopa increases effects of phenoxybenzamine by pharmacodynamic synergism.
Significant interaction possible, monitor closely. Consider decreasing dosage of
antihypertensive agent.
carvedilol
phenoxybenzamine and carvedilol both increase anti-hypertensive channel blocking.
celecoxib
celecoxib decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
celiprolol
phenoxybenzamine and celiprolol both increase anti-hypertensive channel blocking.
choline magnesium trisalicylate
choline magnesium trisalicylate decreases effects of phenoxybenzamine by
clevidipine
phenoxybenzamine and clevidipine both increase anti-hypertensive channel blocking.
diclofenac
diclofenac decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
diflunisal
diflunisal decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
diltiazem
phenoxybenzamine and diltiazem both increase anti-hypertensive channel blocking.
dobutamine
phenoxybenzamine, dobutamine. Mechanism: pharmacodynamic synergism. Significant
dopexamine
phenoxybenzamine, dopexamine. Mechanism: pharmacodynamic synergism. Significant
doxazosin
doxazosin and phenoxybenzamine both increase anti-hypertensive channel blocking.
enalapril
enalapril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
ephedrine
phenoxybenzamine, ephedrine. Mechanism: pharmacodynamic synergism. Significant
ephedrine (pulmonary)
phenoxybenzamine, ephedrine (pulmonary). Mechanism: pharmacodynamic synergism.
Significant interaction possible, monitor closely. Hypotension, tachycardia.
epinephrine
phenoxybenzamine, epinephrine. Mechanism: pharmacodynamic synergism. Significant
epinephrine racemic
phenoxybenzamine, epinephrine racemic. Mechanism: pharmacodynamic synergism.
esmolol
phenoxybenzamine and esmolol both increase anti-hypertensive channel blocking.
etodolac
etodolac decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
etoricoxib
etoricoxib decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
felodipine
phenoxybenzamine and felodipine both increase anti-hypertensive channel blocking.
fenbufen
fenbufen decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
fenoprofen
fenoprofen decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
flurbiprofen
flurbiprofen decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
formoterol
phenoxybenzamine, formoterol. Mechanism: pharmacodynamic synergism. Significant
fosinopril
fosinopril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
ibuprofen
ibuprofen decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
iloperidone
iloperidone increases effects of phenoxybenzamine by pharmacodynamic synergism.
Significant interaction possible, monitor closely.
imidapril
imidapril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
indomethacin
indomethacin decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
isoproterenol
phenoxybenzamine, isoproterenol. Mechanism: pharmacodynamic synergism. Significant
isradipine
phenoxybenzamine and isradipine both increase anti-hypertensive channel blocking.
ketoprofen
ketoprofen decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
ketorolac
ketorolac decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
ketorolac intranasal
ketorolac intranasal decreases effects of phenoxybenzamine by pharmacodynamic
antagonism. Significant interaction possible, monitor closely. NSAIDs decrease
prostaglandin synthesis.
labetalol
phenoxybenzamine and labetalol both increase anti-hypertensive channel blocking.
lacidipine
phenoxybenzamine and lacidipine both increase anti-hypertensive channel blocking.
lercanidipine
phenoxybenzamine and lercanidipine both increase anti-hypertensive channel blocking.
levalbuterol
phenoxybenzamine, levalbuterol. Mechanism: pharmacodynamic synergism. Significant
lisinopril
lisinopril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
lornoxicam
lornoxicam decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
mefenamic acid
mefenamic acid decreases effects of phenoxybenzamine by pharmacodynamic
meloxicam
meloxicam decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
metaproterenol
phenoxybenzamine, metaproterenol. Mechanism: pharmacodynamic synergism.
metoprolol
phenoxybenzamine and metoprolol both increase anti-hypertensive channel blocking.
moexipril
moexipril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
moxisylyte
moxisylyte and phenoxybenzamine both increase anti-hypertensive channel blocking.
nabumetone
nabumetone decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
nadolol
phenoxybenzamine and nadolol both increase anti-hypertensive channel blocking.
naproxen
naproxen decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
nebivolol
phenoxybenzamine and nebivolol both increase anti-hypertensive channel blocking.
nicardipine
phenoxybenzamine and nicardipine both increase anti-hypertensive channel blocking.
nifedipine
phenoxybenzamine and nifedipine both increase anti-hypertensive channel blocking.
nisoldipine
phenoxybenzamine and nisoldipine both increase anti-hypertensive channel blocking.
norepinephrine
phenoxybenzamine, norepinephrine. Mechanism: pharmacodynamic synergism.
oxaprozin
oxaprozin decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
parecoxib
parecoxib decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
penbutolol
phenoxybenzamine and penbutolol both increase anti-hypertensive channel blocking.
perindopril
perindopril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
phentolamine
phenoxybenzamine and phentolamine both increase anti-hypertensive channel blocking.
pindolol
phenoxybenzamine and pindolol both increase anti-hypertensive channel blocking.
pirbuterol
phenoxybenzamine, pirbuterol. Mechanism: pharmacodynamic synergism. Significant
piroxicam
piroxicam decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
prazosin
phenoxybenzamine and prazosin both increase anti-hypertensive channel blocking.
propranolol
phenoxybenzamine and propranolol both increase anti-hypertensive channel blocking.
quinapril
quinapril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
ramipril
ramipril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
salicylates (non-asa)
salicylates (non-asa) decreases effects of phenoxybenzamine by pharmacodynamic
salmeterol
phenoxybenzamine, salmeterol. Mechanism: pharmacodynamic synergism. Significant
salsalate
salsalate decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
silodosin
phenoxybenzamine and silodosin both increase anti-hypertensive channel blocking.
sotalol
phenoxybenzamine and sotalol both increase anti-hypertensive channel blocking.
sulfasalazine
sulfasalazine decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
sulindac
sulindac decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
tadalafil
tadalafil increases effects of phenoxybenzamine by pharmacodynamic synergism.
terazosin
phenoxybenzamine and terazosin both increase anti-hypertensive channel blocking.
terbutaline
phenoxybenzamine, terbutaline. Mechanism: pharmacodynamic synergism. Significant
timolol
phenoxybenzamine and timolol both increase anti-hypertensive channel blocking.
tolfenamic acid
tolfenamic acid decreases effects of phenoxybenzamine by pharmacodynamic
tolmetin
tolmetin decreases effects of phenoxybenzamine by pharmacodynamic antagonism.
synthesis.
trandolapril
trandolapril, phenoxybenzamine. Mechanism: pharmacodynamic synergism. Significant
verapamil
phenoxybenzamine and verapamil both increase anti-hypertensive channel blocking.
zotepine
phenoxybenzamine and zotepine both increase anti-hypertensive channel blocking.
Minor (8)
brimonidine
brimonidine increases effects of phenoxybenzamine by pharmacodynamic synergism.
Minor or non-significant interaction.
butcher's broom
phenoxybenzamine, butcher's broom. Either decreases effects of the other by Mechanism:
pharmacodynamic antagonism. Minor or non-significant interaction.
ethanol
phenoxybenzamine, ethanol. Mechanism: pharmacodynamic synergism. Minor or non-
significant interaction. Risk of hypotension, esp. in Asian pts.
lofexidine
phenoxybenzamine, lofexidine. Either decreases effects of the other by Mechanism:
phenylephrine
phenoxybenzamine, phenylephrine. Either decreases effects of the other by Mechanism:
phenylephrine po
phenoxybenzamine, phenylephrine po. Either decreases effects of the other by
Mechanism: pharmacodynamic antagonism. Minor or non-significant interaction.
tizanidine
tizanidine increases effects of phenoxybenzamine by pharmacodynamic synergism.
Minor or non-significant interaction. Risk of hypotension.
treprostinil
treprostinil increases effects of phenoxybenzamine by pharmacodynamic synergism.
Minor or non-significant interaction.
Adverse Effects
Frequency Not Defined
Orthostatic hypotension
Tachycardia
Dizziness
Drowsiness
Fatigue
Malaise
Sedation
Dry mouth
Nausea
Vomiting
Inhibition of ejaculation
Miosis
Nasal congestion
Contraindications & Cautions
Contraindications
Hypersensitivity to phenoxybenzamine
Any conditions in which fall in BP is undesirable
Cautions
Cerebral or coronary arteriosclerosis, CHF, respiratory infection, renal impairment
Concomitant use of drugs that stimulate alpha/beta receptors (may incr hypotension/tachycardia)
May have carcinogenic potential
First dose effect may occur, causing a sudden and drastic fall in blood pressure after
administering the first dose.
Hypotension/syncope may occur with first few doses or with increase in dose
Minimize by using small first dose at bedtime
Increase dose slowly
Pharmacology
Half-Life: 24 hr
Onset: several hours
Duration: several days
Bioavailability: 20-30%
Metabolism: extensively metabolized in liver
Metabolite: N-phenoxyisopropyl-benzylamine
Excretion: urine & feces
Mechanism of Action
Alpha blocker, noncompetitive alpha-adrenergic blockade of post ganglionic synapses in smooth
muscle, exocrine glands
Patient Education
phenoxybenzamine oral
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have
all possible information about this product. This information does not assure that this product is
safe, effective, or appropriate for you. This information is not individual medical advice and does
not substitute for the advice of your health care professional. Always ask your health care
professional for complete information about this product and your specific health needs.
PHENOXYBENZAMINE - ORAL
(fen-OX-ee-BEN-za-meen)
COMMON BRAND NAME(S): Dibenzyline
USES:
This medication is used to treat high blood pressure and heavy sweating due to a certain tumor of
the adrenal glands (pheochromocytoma). Phenoxybenzamine belongs to a class of drugs known
as alpha blockers. It works by relaxing and widening blood vessels so that blood can flow more
easily.
OTHER USES:
This section contains uses of this drug that are not listed in the approved professional labeling for
the drug but that may be prescribed by your health care professional. Use this drug for a
condition that is listed in this section only if it has been so prescribed by your health care
professional.
This drug may also be used with other medications to treat certain blood circulation problems
(e.g., Raynaud's syndrome).
It is also used to treat certain conditions which involve difficulty urinating (e.g., neurogenic
bladder, partial prostatic obstruction).
HOW TO USE:
Take this medication by mouth with or without food, usually 2 to 3 times daily or as directed by
your doctor.
Dosage is based on your medical condition and response to therapy.
Use this medication regularly in order to get the most benefit from it. To help you remember,
take it at the same times each day. It is important to continue taking this medication even if you
feel well. Most people with high blood pressure do not feel sick.
Do not suddenly stop taking this medication without consulting your doctor. Your condition may
become worse when the drug is suddenly stopped. Your dose may need to be gradually
decreased.
Inform your doctor if your condition worsens (e.g., your routine blood pressure readings
increase).
SIDE EFFECTS:
Stomach upset, nausea, stuffy nose, drowsiness, dizziness or decrease in pupil size may occur. If
any of these effects persist or worsen, notify your doctor or pharmacist promptly.
To lower your risk of dizziness and lightheadedness, get up slowly when rising from a sitting or
lying position.
Remember that your doctor has prescribed this medication because he or she has judged that the
benefit to you is greater than the risk of side effects. Many people using this medication do not
have serious side effects.
Tell your doctor immediately if any of these unlikely but serious side effects occur: fast
heartbeat, fainting, sexual problems in males (e.g., trouble ejaculating), weakness.
For males, in the very unlikely event that you have a painful or prolonged erection lasting 4 or
more hours, stop using this drug and seek immediate medical attention, or permanent problems
could occur.
A very serious allergic reaction to this drug is rare. However, seek immediate medical attention
if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling
(especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above,
contact your doctor or pharmacist.
In the US -
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-
800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side effects
to Health Canada at 1-866-234-2345.
PRECAUTIONS:
Before taking phenoxybenzamine, tell your doctor or pharmacist if you are allergic to it; or to
other alpha blockers (e.g., phentolamine); or if you have any other allergies. This product may
contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your
pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of:
blood vessel disease (e.g., cerebral arteriosclerosis, coronary artery disease), heart disease (e.g.,
congestive heart failure), kidney disease, lung infections.
Before having surgery, tell your doctor or dentist that you are taking this medication.
This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that
requires alertness until you are sure you can perform such activities safely. Limit alcoholic
beverages.
Caution is advised when using this drug in the elderly because they may be more sensitive to its
effects, especially dizziness.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks
and benefits with your doctor.
It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS:
Your doctor or pharmacist may already be aware of any possible drug interactions and may be
monitoring you for them. Do not start, stop, or change the dosage of any medicine before
checking with them first.
Before using this medication, tell your doctor or pharmacist of all prescription and
nonprescription/herbal products you may use, especially of: drugs to treat erectile dysfuntion-ED
or pulmonary hypertension (e.g., sildenafil, tadalafil), epinephrine, other alpha blockers (e.g.,
prazosin), other drugs for high blood pressure (e.g., diuretics, ACE inhibitors, beta blockers).
Tell your doctor or pharmacist if you also take drugs that cause drowsiness such as: certain
antihistamines (e.g., diphenhydramine), anti-seizure drugs (e.g., carbamazepine), medicine for
sleep or anxiety (e.g., alprazolam, diazepam, zolpidem), muscle relaxants, narcotic pain relievers
(e.g., codeine), psychiatric medicines (e.g., chlorpromazine, risperidone, amitriptyline,
trazodone).
Check the labels on all your medicines (e.g., cough-and-cold products, diet aids, nonsteroidal
anti-inflammatory drugs-NSAIDs such as ibuprofen for pain/fever reduction) because they may
contain ingredients that could increase your blood pressure or contain drowsiness-causing
ingredients. Ask your pharmacist about using those products safely.
This document does not contain all possible interactions. Therefore, before using this product,
tell your doctor or pharmacist of all the products you use. Keep a list of all your medications
with you, and share the list with your doctor and pharmacist.
OVERDOSE:
If overdose is suspected, contact a poison control center or emergency room immediately. US
residents can call their local poison control center at 1-800-222-1222. Canada residents can call a
provincial poison control center. Symptoms of overdose may include: fainting, severe weakness,
fast heartbeat.
NOTES:
Do not share this medication with others.
Have your blood pressure checked regularly while taking this medication. Learn how to monitor
your own blood pressure at home, and share the results with your doctor.
MISSED DOSE:
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip
the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.
STORAGE:
Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light and
moisture. Do not store in the bathroom. Keep all medicines away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so.
Properly discard this product when it is expired or no longer needed. Consult your pharmacist or
local waste disposal company for more details about how to safely discard your product.
Information last revised December 2013. Copyright(c) 2013 First Databank, Inc
Prazosin (Minipress)

Prazosin is currently approved for the treatment of hypertension. Prazosin improves urine flow
rates by relaxing smooth muscle. Relaxation is produced by blocking alpha-1 adrenoreceptors in
the bladder neck and prostate. The advantage of prazosin over nonselective alpha-adrenergic
blockers includes a lower incidence of adverse effects. Because of availability of longer-acting,
once-daily selective agents, however, the clinical utility of prazosin for BPH has been reduced.
Prazosin improves urinary flow rate and frequency of micturition. Subjective improvement is
observed in 82% of patients treated. When increasing dosages, administer the first dose of each
increment at bedtime to reduce syncopal episodes. Although doses above 20 mg/d do not usually
increase efficacy, some patients may benefit from up to 40 mg/d.
Dosing & Uses
AdultPediatric
Hypertension
Initial: 1 mg PO q8-12hr
Maintenance: 2-20 mg/day PO divided q8-12hr
PTSD-Related Nightmares & Sleep Disruption
Initial: 1 mg PO qHS
Maintenance: 2-15 mg PO qHS
Benign Prostate Hypertrophy (Off-label)
Initial: 0.5 mg PO q12hr
Maintenance: 2 mg PO q12hr
Raynaud Phenomenon (Off-label)
1-5 PO q12hr
Administration
Give first dose and subsequent increases at bedtime to avoid syncope
Okay with food
Drug Interactions
Interaction Checker
prazosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (0)
pomalidomide
prazosin decreases levels of pomalidomide by P-glycoprotein (MDR1) efflux transporter.
available.
sildenafil
sildenafil increases effects of prazosin by pharmacodynamic synergism. Possible serious
or life-threatening interaction. Monitor closely. Use alternatives if available. Risk of
hypotension; separate sildenafil >25mg from alpha blocker by 4hr.
tamsulosin
prazosin, tamsulosin. Either increases effects of the other by additive vasodilation.
available. Risk of hypotension.
vardenafil
vardenafil increases effects of prazosin by pharmacodynamic synergism. High likelihood
serious or life-threatening interaction. Contraindicated unless benefits outweigh risks and
no alternatives available. Never use combination. Risk of hypotension.
yohimbe
yohimbe increases effects of prazosin by pharmacodynamic synergism. High likelihood
no alternatives available. Never use combination.
acebutolol
prazosin and acebutolol both increase anti-hypertensive channel blocking. Potential for
dangerous interaction. Use with caution and monitor closely. The severity and duration of
hypotension following the first dose of prazosin may be enhanced.
aceclofenac
aceclofenac decreases effects of prazosin by pharmacodynamic antagonism. Significant
interaction possible, monitor closely. NSAIDs decrease prostaglandin synthesis.
acemetacin
acemetacin decreases effects of prazosin by pharmacodynamic antagonism. Significant
aldesleukin
aldesleukin increases effects of prazosin by pharmacodynamic synergism. Potential for
interaction, monitor. Risk of hypotension.
alfuzosin
alfuzosin and prazosin both increase anti-hypertensive channel blocking. Potential for
interaction, monitor.
amifostine
amifostine increases effects of prazosin by pharmacodynamic synergism. Potential for
amlodipine
prazosin and amlodipine both increase anti-hypertensive channel blocking. Potential for
asenapine
asenapine and prazosin both increase anti-hypertensive channel blocking. Potential for
aspirin
aspirin decreases effects of prazosin by pharmacodynamic antagonism. Significant
aspirin rectal
aspirin rectal decreases effects of prazosin by pharmacodynamic antagonism. Significant
aspirin/citric acid/sodium bicarbonate decreases effects of prazosin by pharmacodynamic
atenolol
prazosin and atenolol both increase anti-hypertensive channel blocking. Potential for
dangerous interaction. Use with caution and monitor closely.
avanafil
avanafil increases effects of prazosin by pharmacodynamic synergism. Significant
interaction possible, monitor closely. Risk of hypotension.
benazepril
benazepril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
possible, monitor closely. Exaggerated first dose hypotensive response.
betaxolol
prazosin and betaxolol both increase anti-hypertensive channel blocking. Potential for
bisoprolol
prazosin and bisoprolol both increase anti-hypertensive channel blocking. Potential for
captopril
captopril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
carbidopa
carbidopa increases effects of prazosin by pharmacodynamic synergism. Potential for
interaction, monitor. Therapy with carbidopa, given with or without levodopa or
carbidopa-levodopa combination products, is started, dosage adjustment of the
antihypertensive drug may be required.
carvedilol
prazosin and carvedilol both increase anti-hypertensive channel blocking. Potential for
celecoxib
celecoxib decreases effects of prazosin by pharmacodynamic antagonism. Significant
celiprolol
prazosin and celiprolol both increase anti-hypertensive channel blocking. Potential for
choline magnesium trisalicylate decreases effects of prazosin by pharmacodynamic
clevidipine
prazosin and clevidipine both increase anti-hypertensive channel blocking. Potential for
clonidine
clonidine, prazosin. Either increases toxcity of the other by pharmacodynamic synergism.
Significant interaction possible, monitor closely. Sympatholytic action may worsen sinus
node dysfunction and atrioventricular (AV) block.
diclofenac
diclofenac decreases effects of prazosin by pharmacodynamic antagonism. Significant
diflunisal
diflunisal decreases effects of prazosin by pharmacodynamic antagonism. Significant
diltiazem
prazosin and diltiazem both increase anti-hypertensive channel blocking. Potential for
doxazosin
doxazosin and prazosin both increase anti-hypertensive channel blocking. Potential for
enalapril
enalapril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
esmolol
prazosin and esmolol both increase anti-hypertensive channel blocking. Potential for
etodolac
etodolac decreases effects of prazosin by pharmacodynamic antagonism. Significant
etoricoxib
etoricoxib decreases effects of prazosin by pharmacodynamic antagonism. Significant
felodipine
prazosin and felodipine both increase anti-hypertensive channel blocking. Potential for
fenbufen
fenbufen decreases effects of prazosin by pharmacodynamic antagonism. Significant
fenoprofen
fenoprofen decreases effects of prazosin by pharmacodynamic antagonism. Significant
flurbiprofen
flurbiprofen decreases effects of prazosin by pharmacodynamic antagonism. Significant
fosinopril
fosinopril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
ibuprofen
ibuprofen decreases effects of prazosin by pharmacodynamic antagonism. Significant
iloperidone
iloperidone increases effects of prazosin by pharmacodynamic synergism. Significant
interaction possible, monitor closely.
imidapril
imidapril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
indomethacin
indomethacin decreases effects of prazosin by pharmacodynamic antagonism. Significant
isradipine
prazosin and isradipine both increase anti-hypertensive channel blocking. Potential for
ketoprofen
ketoprofen decreases effects of prazosin by pharmacodynamic antagonism. Significant
ketorolac
ketorolac decreases effects of prazosin by pharmacodynamic antagonism. Significant
ketorolac intranasal decreases effects of prazosin by pharmacodynamic antagonism.
synthesis.
labetalol
prazosin and labetalol both increase anti-hypertensive channel blocking. Potential for
lacidipine
prazosin and lacidipine both increase anti-hypertensive channel blocking. Potential for
lercanidipine
prazosin and lercanidipine both increase anti-hypertensive channel blocking. Potential for
levodopa
levodopa increases effects of prazosin by pharmacodynamic synergism. Significant
interaction possible, monitor closely. Consider decreasing dosage of antihypertensive
agent.
linagliptin
prazosin will decrease the level or effect of linagliptin by P-glycoprotein (MDR1) efflux
transporter. Significant interaction possible, monitor closely. Use of alternative
treatments is strongly recommended when linagliptin is to be administered with a P-gp
inducer.
lisinopril
lisinopril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
lornoxicam
lornoxicam decreases effects of prazosin by pharmacodynamic antagonism. Significant
lurasidone
lurasidone increases effects of prazosin by Other (see comment). Potential for interaction,
monitor. Comment: Potential for increased risk of hypotension with concurrent use.
Monitor blood pressure and adjust dose of antihypertensive agent as needed.
maraviroc
maraviroc, prazosin. Either increases effects of the other by pharmacodynamic
synergism. Significant interaction possible, monitor closely. Increased risk of orthostatic
hypotension.
mefenamic acid
mefenamic acid decreases effects of prazosin by pharmacodynamic antagonism.
synthesis.
meloxicam
meloxicam decreases effects of prazosin by pharmacodynamic antagonism. Significant
metoprolol
prazosin and metoprolol both increase anti-hypertensive channel blocking. Potential for
moexipril
moexipril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
moxisylyte
moxisylyte and prazosin both increase anti-hypertensive channel blocking. Potential for
nabumetone
nabumetone decreases effects of prazosin by pharmacodynamic antagonism. Significant
nadolol
prazosin and nadolol both increase anti-hypertensive channel blocking. Potential for
naproxen
naproxen decreases effects of prazosin by pharmacodynamic antagonism. Significant
nebivolol
prazosin and nebivolol both increase anti-hypertensive channel blocking. Potential for
nicardipine
prazosin and nicardipine both increase anti-hypertensive channel blocking. Potential for
nifedipine
prazosin and nifedipine both increase anti-hypertensive channel blocking. Potential for
nisoldipine
prazosin and nisoldipine both increase anti-hypertensive channel blocking. Potential for
nitroglycerin rectal
nitroglycerin rectal, prazosin. Either increases effects of the other by pharmacodynamic
synergism. Potential for interaction, monitor. Observe for possible additive hypotensive
effects during concomitant use. .
oxaprozin
oxaprozin decreases effects of prazosin by pharmacodynamic antagonism. Significant
parecoxib
parecoxib decreases effects of prazosin by pharmacodynamic antagonism. Significant
penbutolol
prazosin and penbutolol both increase anti-hypertensive channel blocking. Potential for
perindopril
perindopril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
phenoxybenzamine
phenoxybenzamine and prazosin both increase anti-hypertensive channel blocking.
phentolamine
phentolamine and prazosin both increase anti-hypertensive channel blocking. Potential
for interaction, monitor.
pindolol
prazosin and pindolol both increase anti-hypertensive channel blocking. Potential for
piroxicam
piroxicam decreases effects of prazosin by pharmacodynamic antagonism. Significant
propranolol
prazosin and propranolol both increase anti-hypertensive channel blocking. Potential for
quinapril
quinapril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
ramipril
ramipril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
salicylates (non-asa) decreases effects of prazosin by pharmacodynamic antagonism.
synthesis.
salsalate
salsalate decreases effects of prazosin by pharmacodynamic antagonism. Significant
silodosin
prazosin and silodosin both increase anti-hypertensive channel blocking. Potential for
sotalol
prazosin and sotalol both increase anti-hypertensive channel blocking. Potential for
sulfasalazine
sulfasalazine decreases effects of prazosin by pharmacodynamic antagonism. Significant
sulindac
sulindac decreases effects of prazosin by pharmacodynamic antagonism. Significant
tadalafil
tadalafil increases effects of prazosin by pharmacodynamic synergism. Significant
teduglutide
teduglutide increases levels of prazosin by Other (see comment). Significant interaction
possible, monitor closely. Comment: Teduglutide may increase absorption of
concomitant PO medications; caution with with drugs requiring titration or those with a
narrow therapeutic index; dose adjustment may be necessary.
terazosin
prazosin and terazosin both increase anti-hypertensive channel blocking. Potential for
timolol
prazosin and timolol both increase anti-hypertensive channel blocking. Potential for
tolfenamic acid
tolfenamic acid decreases effects of prazosin by pharmacodynamic antagonism.
synthesis.
tolmetin
tolmetin decreases effects of prazosin by pharmacodynamic antagonism. Significant
trandolapril
trandolapril, prazosin. Mechanism: pharmacodynamic synergism. Significant interaction
verapamil
prazosin and verapamil both increase anti-hypertensive channel blocking. Potential for
zotepine
prazosin and zotepine both increase anti-hypertensive channel blocking. Potential for
Minor (8)
brimonidine
brimonidine increases effects of prazosin by pharmacodynamic synergism. Minor or non-
significant interaction.
butcher's broom
prazosin, butcher's broom. Either decreases effects of the other by Mechanism:
ethanol
prazosin, ethanol. Mechanism: pharmacodynamic synergism. Minor or non-significant
interaction. Risk of hypotension, esp. in Asian pts.
lofexidine
prazosin, lofexidine. Either decreases effects of the other by Mechanism:
phenylephrine
prazosin, phenylephrine. Either decreases effects of the other by Mechanism:
phenylephrine po
prazosin, phenylephrine po. Either decreases effects of the other by Mechanism:
tizanidine
tizanidine increases effects of prazosin by pharmacodynamic synergism. Minor or non-
significant interaction. Risk of hypotension.
treprostinil
treprostinil increases effects of prazosin by pharmacodynamic synergism. Minor or non-
Adverse Effects
1-10%
Dizziness (10%)
Drowsiness (8%)
Headache (8%)
Weakness (7%)
Asthenia (6.5%)
Nausea (5%)
Palpitation (5%)
Frequency Not Defined (Selected)
Edema
Syncope
Fever
Rash
Abdominal discomfort/pain
Diarrhea
Vomiting
Abnormal liver function tests
Impotence
Pancreatitis
Urinary incontinence
Contraindications
Hypersensitivity
Cautions
Risk of syncope; has no relation to plasma prazosin concentration
May impair ability to drive/perform hazardous tasks due to dizziness
History of narcolepsy - May exacerbate
Cataract surgery - Linked to intraoperative floppy iris syndrome
Concomitant administration with PDE-5 inhibitor (eg, sildenafil) can result in additive blood
pressure-lowering effects and symptomatic hypotension; initiate PDE-5 inhibitor therapy at
lowest dose
First dose effect may occur, causing a sudden and drastic fall in blood pressure after
administration of the first dose.
Hypotension/syncope may occur with first few doses or with increase in dose; minimize effect
by using small first dose at bedtime; increase dose slowly
Geriatric considerations
Avoid use for hypertension; high risk of orthostatic hypotension (Beers criteria)
May cause significant orthostatic hypotension and syncope; consider lower initial dose;
titrate to response
Adverse effects such as dry mouth and urinary complications can be bothersome in the
elderly
Pharmacology
Mechanism of Action
Alpha-1 blocker inhibits postsynaptic alpha-adrenergic receptors, causing arterial and
venous dilation and a subsequent decrease in blood pressure
Absorption
Bioavailability: 43-82%
Onset: ~2 hr
Duration: 10-24 hr
Peak effect: 2-4 hr
Peak plasma time: 2-3 hr
Distribution
Protein bound: 97%
Metabolism
Hepatic metabolization (extensive)
Elimination
Half-life elimination: 2-3 hr
Excretion: Urine (6-10%); rest in feces (via bile)
Patient Handout
Print w/ Office Info
Print w/out Office Info
560043
Patient Education
prazosin oral
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does
NOT have all possible information about this product. This information does not assure
that this product is safe, effective, or appropriate for you. This information is not
individual medical advice and does not substitute for the advice of your health care
professional. Always ask your health care professional for complete information about
this product and your specific health needs.
PRAZOSIN - ORAL
(PRAZ-oh-sin)
COMMON BRAND NAME(S): Minipress
USES:
Prazosin is used with or without other medications to treat high blood pressure. Lowering
high blood pressure helps prevent strokes, heart attacks, and kidney problems.
Prazosin belongs to a class of medications called alpha blockers. It works by relaxing and
widening blood vessels so blood can flow more easily.
OTHER USES:
This section contains uses of this drug that are not listed in the approved professional
labeling for the drug but that may be prescribed by your health care professional. Use this
drug for a condition that is listed in this section only if it has been so prescribed by your
health care professional.
This drug may also be used to treat certain blood circulation disorders (Raynaud's
phenomenon). Prazosin may also be used to treat problems urinating due to an enlarged
prostate (benign prostatic hyperplasia) or to help your body "pass," or get rid of, kidney
stones through urination.
HOW TO USE:
Take this medication by mouth with or without food, usually two or three times daily or
as directed by your doctor. If stomach upset occurs, take with food or milk. The dosage is
based on your age, medical condition and response to therapy.
Prazosin can occasionally cause sudden fainting after the first dose and anytime that your
dose is increased. To reduce your risk of fainting, the first dose prescribed by your doctor
will be the smallest dose available. You should take this first dose as you are going to
bed. This will decrease the possibility of fainting. Your dose may be gradually increased.
Take your first new dose at bedtime when your dose is increased unless directed
otherwise by your doctor.
Use this medication regularly in order to get the most benefit from it. To help you
remember, take it at the same time(s) each day. If you are taking this medication for high
blood pressure, it is important to continue taking it even if you feel well. Most people
with high blood pressure do not feel sick. It may take up to several weeks before the full
benefit of this drug takes effect.
Do not stop taking this medication without first consulting your doctor. Some conditions
may become worse when the drug is abruptly stopped. Your dose may need to be
gradually decreased.
Tell your doctor if your condition worsens (such as your routine blood pressure readings
increase).
SIDE EFFECTS:
Headache, drowsiness, tiredness, weakness, blurred vision, nausea, vomiting, diarrhea, or
constipation may occur as your body adjusts to the medication. If any of these effects
persist or worsen, tell your doctor or pharmacist promptly.
Lightheadedness or dizziness upon standing may also occur, especially after the first dose
and shortly after taking a dose of the drug during the first week of treatment. To reduce
the risk of dizziness and fainting, get up slowly when rising from a seated or lying
position. If dizziness occurs, sit or lie down immediately. Your dose may need to be
adjusted.
Remember that your doctor has prescribed this medication because he or she has judged
that the benefit to you is greater than the risk of side effects. Many people using this
medication do not have serious side effects.
Tell your doctor immediately if any of these unlikely but serious side effects occur:
pounding heartbeat, fainting, frequent urination, mental/mood changes (such as
depression), swelling of the feet/ankles.
For males, in the very unlikely event you have a painful, prolonged erection (lasting more
than 4 hours), stop using this drug and seek immediate medical attention, or permanent
problems could occur.
A very serious allergic reaction to this drug is rare. However, seek immediate medical
attention if you notice any symptoms of a serious allergic reaction, including: rash,
itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble
breathing.
This is not a complete list of possible side effects. If you notice other effects not listed
above, contact your doctor or pharmacist.
In the US -
Call your doctor for medical advice about side effects. You may report side effects to
FDA at 1-800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side
effects to Health Canada at 1-866-234-2345.
PRECAUTIONS:
Before taking prazosin, tell your doctor or pharmacist if you are allergic to it; or to other
alpha blockers (such as doxazosin, terazosin); or if you have any other allergies. This
product may contain inactive ingredients, which can cause allergic reactions or other
problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history,
especially of: heart problems (such as low blood pressure), kidney disease, uncontrolled
attacks of deep sleep (narcolepsy), prostate cancer.
This drug may make you dizzy or drowsy or cause blurred vision. Do not drive, use
machinery, or do any activity that requires alertness or clear vision until you are sure you
can perform such activities safely. Do not drive or participate in hazardous activities for
24 hours after your first dose, any increase in your dosage, or restarting treatment. If your
doctor prescribes any additional blood pressure drugs, avoid driving and hazardous
activities for 24 hours after your first dose of the new medication. Limit alcoholic
beverages.
To reduce the risk of dizziness and fainting, be careful when standing for long periods.
Avoid getting overheated during exercise and hot weather. When first starting this drug,
avoid situations where you may be injured if you faint.
Before having surgery (including cataract eye surgery), tell your doctor or dentist that
you are taking this medication and about all the products you use (including other
prescription drugs, nonprescription drugs, and herbal products).
Older adults may be more sensitive to the side effects of this drug, especially dizziness
and fainting. These side effects can increase the risk of falling.
During pregnancy, this medication should be used only when clearly needed. Discuss the
risks and benefits with your doctor.
Prazosin passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS:
The effects of some drugs can change if you take other drugs or herbal products at the
same time. This can increase your risk for serious side effects or may cause your
medications not to work correctly. These drug interactions are possible, but do not always
occur. Your doctor or pharmacist can often prevent or manage interactions by changing
how you use your medications or by close monitoring.
To help your doctor or pharmacist give you the best care, be sure to tell your doctor or
pharmacist about all the products you use (including prescription drugs, nonprescription
drugs, and herbal products) before starting treatment with this product. While using this
product, do not start, stop, or change the dosage of any other medicines you are using
without your doctor's approval.
Some of the products that may interact with this drug include: beta blockers (such as
atenolol, metoprolol, propranolol), verapamil, drugs to treat erectile dysfunction-ED or
pulmonary hypertension (such as sildenafil, tadalafil).
Tell your doctor or pharmacist if you also take drugs that cause drowsiness, lower blood
pressure, or make it difficult for you to urinate, such as: certain antihistamines (such as
diphenhydramine), anti-seizure drugs (such as carbamazepine), medicine for sleep or
anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, narcotic pain
relievers (such as codeine), psychiatric medicines (such as chlorpromazine, risperidone,
amitriptyline, trazodone).
Check the labels on all your medicines (such as cough-and-cold products, diet aids,
nonsteroidal anti-inflammatory drugs-NSAIDs for pain/fever reduction) because they
may contain ingredients (such as pseudoephedrine, phenylephrine, chlorpheniramine,
diphenhydramine, clemastine, ibuprofen, naproxen) that could increase your blood
pressure or cause a fast heartbeat. Ask your pharmacist about the safe use of those
products.
This medication may interfere with certain laboratory tests (including
pheochromocytoma screening test), possibly causing false test results. Make sure
laboratory personnel and all your doctors know you use this drug.
This document does not contain all possible interactions. Keep a list of all the products
you use. Share this list with your doctor and pharmacist to lessen your risk for serious
medication problems.
OVERDOSE:
If overdose is suspected, contact a poison control center or emergency room immediately.
US residents can call their local poison control center at 1-800-222-1222. Canada
residents can call a provincial poison control center. Symptoms of overdose may include:
severe drowsiness, slow reactions.
NOTES:
Lifestyle changes such as stress reduction programs, exercise, and dietary changes may
increase the effectiveness of this medicine. Talk to your doctor or pharmacist about
lifestyle changes that might benefit you.
Have your blood pressure and heart rate checked regularly while taking this medication.
Learn how to monitor your own blood pressure, and share the results with your doctor.
MISSED DOSE:
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose,
skip the missed dose and resume your usual dosing schedule. Do not double the dose to
catch up.
STORAGE:
Store at room temperature away from light and moisture. Refer to storage information
printed on the bottle for the exact temperature range. If you have any questions about
storage, ask your pharmacist. Do not store in the bathroom. Keep all medicines away
from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do
so. Properly discard this product when it is expired or no longer needed. Consult your
pharmacist or local waste disposal company for more details about how to safely discard
your product.
Information last revised March 2013. Copyright(c) 2013 First Databank, Inc
Alfuzosin (UroXatral)

Alfuzosin is indicated for the treatment of the signs and symptoms of BPH. Alfuzosin is an
alpha-1 blocker of adrenoreceptors in the prostate. Blockade of adrenoreceptors may cause
smooth muscles in the bladder neck and prostate to relax, resulting in improvement in urine flow
rate and reduction in symptoms of BPH.
Indoramin

This agent is not available in the United States. Indoramin improves urine flow rates by blocking
alpha-1 adrenoreceptors in the bladder neck and prostate, thus relaxing smooth muscle in those
sites. Indoramin also reduces the frequency of micturition.
The advantage of indoramin over nonselective alpha-adrenergic blockers includes lower
incidence of adverse effects. Because of availability of longer-acting, once-daily selective agents,
clinical utility of this agent for BPH has been reduced.
Dosing & Uses
AdultPediatric
Benign Prostatic Hyperplasia (BPH)
10 mg PO qDay taken after same meal
Drug Interactions
Interaction Checker
alfuzosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (16)
atazanavir
atazanavir will increase the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Never use combination.
boceprevir
boceprevir increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination. Increased alfuzosin concentrations can result in
hypotension.
darunavir
darunavir will increase the level or effect of alfuzosin by affecting hepatic/intestinal
delavirdine
delavirdine will increase the level or effect of alfuzosin by affecting hepatic/intestinal
elvitegravir/cobicistat/emtricitabine/tenofovir
elvitegravir/cobicistat/emtricitabine/tenofovir increases levels of alfuzosin by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. Never use combination. Cobicistat is a
CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma
concentrations are associated with serious and/or life-threatening events.
fosamprenavir
fosamprenavir will increase the level or effect of alfuzosin by affecting hepatic/intestinal
idelalisib
idelalisib will increase the level or effect of alfuzosin by affecting hepatic/intestinal
indinavir
indinavir will increase the level or effect of alfuzosin by affecting hepatic/intestinal
itraconazole
itraconazole increases levels of alfuzosin by decreasing metabolism. Never use
combination.
ketoconazole
ketoconazole increases levels of alfuzosin by decreasing metabolism. Never use
combination.
nefazodone
nefazodone will increase the level or effect of alfuzosin by affecting hepatic/intestinal
nelfinavir
nelfinavir will increase the level or effect of alfuzosin by affecting hepatic/intestinal
ritonavir
ritonavir will increase the level or effect of alfuzosin by affecting hepatic/intestinal
saquinavir
saquinavir increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination. Potential for increased toxicity. .
telaprevir
telaprevir increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination. Contraindicated. Potential for hypotension or
cardiac arrhythmia.
tipranavir
tipranavir increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination. Potential for increased toxicity. Tipranavir is used
with ritonavir (boosted therapy) which is a potent CYP3A4 inhibitor.
efavirenz
efavirenz will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Possible serious or life-threatening interaction. Monitor
closely. Use alternatives if available.
etravirine
etravirine will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
isoniazid
isoniazid will increase the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. High likelihood serious or life-threatening interaction.
Contraindicated unless benefits outweigh risks and no alternatives available.
ivacaftor
ivacaftor increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Possible serious or life-threatening interaction. Monitor closely. Use
alternatives if available. Ivacaftor and its M1 metabolite has the potential to inhibit
CYP3A4, may significantly increase systemic exposure to 3A4 substrates.
ondansetron
alfuzosin and ondansetron both increase QTc interval. Possible serious or life-threatening
interaction. Monitor closely. Use alternatives if available. Avoid with congenital long QT
syndrome; ECG monitoring recommended with concomitant medications that prolong
QT interval, electrolyte abnormalities, CHF, or bradyarrhythmias.
quinine
alfuzosin and quinine both increase QTc interval. Possible serious or life-threatening
interaction. Monitor closely. Use alternatives if available.
sildenafil
sildenafil increases effects of alfuzosin by pharmacodynamic synergism. Possible serious
tamsulosin
alfuzosin, tamsulosin. Either increases effects of the other by additive vasodilation.
toremifene
alfuzosin and toremifene both increase QTc interval. Possible serious or life-threatening
interaction. Monitor closely. Use alternatives if available. Concurrent use of toremifene
with agents causing QT prolongation should be avoided. If concomitant use is required
it's recommended that toremifene be interrupted. If interruption not possible, patients
requiring therapy with a drug that prolongs QT should be closely monitored. ECGs
should be obtained for high risk patients.
umeclidinium bromide/vilanterol inhaled
alfuzosin increases toxcity of umeclidinium bromide/vilanterol inhaled by QTc interval.
available. Exercise extreme caution when vilanterol coadministered with drugs that
prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be
potentiated.
vardenafil
vardenafil increases effects of alfuzosin by pharmacodynamic synergism. High likelihood
vilanterol/fluticasone inhaled
alfuzosin increases toxcity of vilanterol/fluticasone inhaled by QTc interval. Possible
serious or life-threatening interaction. Monitor closely. Use alternatives if available.
Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc
interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
yohimbe
yohimbe increases effects of alfuzosin by pharmacodynamic synergism. High likelihood
acebutolol
alfuzosin and acebutolol both increase anti-hypertensive channel blocking. Potential for
hypotension following the first dose of Alfuzosin may be enhanced.
aceclofenac
aceclofenac decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
acemetacin
acemetacin decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
aldesleukin
aldesleukin increases effects of alfuzosin by pharmacodynamic synergism. Potential for
amifostine
amifostine increases effects of alfuzosin by pharmacodynamic synergism. Potential for
amlodipine
alfuzosin and amlodipine both increase anti-hypertensive channel blocking. Potential for
asenapine
alfuzosin and asenapine both increase anti-hypertensive channel blocking. Potential for
aspirin
aspirin decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
aspirin rectal
aspirin rectal decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
aspirin/citric acid/sodium bicarbonate decreases effects of alfuzosin by pharmacodynamic
atenolol
alfuzosin and atenolol both increase anti-hypertensive channel blocking. Potential for
avanafil
avanafil increases effects of alfuzosin by pharmacodynamic synergism. Significant
bedaquiline
alfuzosin and bedaquiline both increase QTc interval. Potential for dangerous interaction.
Use with caution and monitor closely. ECG should be monitored closely
benazepril
benazepril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
betaxolol
alfuzosin and betaxolol both increase anti-hypertensive channel blocking. Potential for
bisoprolol
alfuzosin and bisoprolol both increase anti-hypertensive channel blocking. Potential for
captopril
captopril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
carbamazepine
carbamazepine will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Potential for interaction, monitor.
carbidopa
carbidopa increases effects of alfuzosin by pharmacodynamic synergism. Potential for
interaction, monitor. Monitor for hypotension.
carvedilol
alfuzosin and carvedilol both increase anti-hypertensive channel blocking. Potential for
celecoxib
celecoxib decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
celiprolol
alfuzosin and celiprolol both increase anti-hypertensive channel blocking. Potential for
choline magnesium trisalicylate decreases effects of alfuzosin by pharmacodynamic
cimetidine
cimetidine will increase the level or effect of alfuzosin by affecting hepatic/intestinal
clarithromycin
clarithromycin will increase the level or effect of alfuzosin by affecting hepatic/intestinal
clevidipine
alfuzosin and clevidipine both increase anti-hypertensive channel blocking. Potential for
crizotinib
crizotinib increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Potential for interaction, monitor. Dose reduction may be needed for
coadministered drugs that are predominantly metabolized by CYP3A.
crofelemer
crofelemer increases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Potential for interaction, monitor. Crofelemer has the potential to inhibit
CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because
minimally absorbed.
dabrafenib
dabrafenib will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Potential for dangerous interaction. Use with caution and
monitor closely.
deferasirox
deferasirox will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
diclofenac
diclofenac decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
diflunisal
diflunisal decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
diltiazem
diltiazem will increase the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Significant interaction possible, monitor closely. The
concomitant use of alfuzosin and diltiazem is not recommended. Increased exposure to
alfuzosin may be expected when these two drugs are used together. Pulse and blood
pressure monitoring may be necessary.

alfuzosin and diltiazem both increase anti-hypertensive channel blocking. Potential for
doxazosin
alfuzosin and doxazosin both increase anti-hypertensive channel blocking. Potential for
enalapril
enalapril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
erythromycin base
erythromycin base will increase the level or effect of alfuzosin by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. Potential for interaction, monitor.
erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of alfuzosin by affecting
erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of alfuzosin by affecting
erythromycin stearate
erythromycin stearate will increase the level or effect of alfuzosin by affecting
esmolol
alfuzosin and esmolol both increase anti-hypertensive channel blocking. Potential for
etodolac
etodolac decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
etoricoxib
etoricoxib decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
felodipine
alfuzosin and felodipine both increase anti-hypertensive channel blocking. Potential for
fenbufen
fenbufen decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
fenoprofen
fenoprofen decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
fluoxetine
alfuzosin and fluoxetine both increase QTc interval. Potential for dangerous interaction.
Use with caution and monitor closely.
flurbiprofen
flurbiprofen decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
fosinopril
fosinopril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
haloperidol
haloperidol and alfuzosin both increase QTc interval. Potential for interaction, monitor.
ibuprofen
ibuprofen decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
iloperidone
iloperidone increases effects of alfuzosin by pharmacodynamic synergism. Significant

iloperidone increases effects of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Potential for interaction, monitor. Iloperidone is a time-dependent CYP3A
inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by
CYP3A4.
imidapril
imidapril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
indacaterol, inhaled
indacaterol, inhaled, alfuzosin. QTc interval. Significant interaction possible, monitor
closely. Drugs that are known to prolong the QTc interval may have an increased the risk
of ventricular arrhythmias.
indomethacin
indomethacin decreases effects of alfuzosin by pharmacodynamic antagonism.
synthesis.
isradipine
alfuzosin and isradipine both increase anti-hypertensive channel blocking. Potential for
itraconazole
itraconazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
ketoconazole
ketoconazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
ketoprofen
ketoprofen decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
ketorolac
ketorolac decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
ketorolac intranasal decreases effects of alfuzosin by pharmacodynamic antagonism.
synthesis.
labetalol
alfuzosin and labetalol both increase anti-hypertensive channel blocking. Potential for
lacidipine
alfuzosin and lacidipine both increase anti-hypertensive channel blocking. Potential for
lercanidipine
alfuzosin and lercanidipine both increase anti-hypertensive channel blocking. Potential
lisinopril
lisinopril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
lornoxicam
lornoxicam decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
lurasidone
lurasidone increases effects of alfuzosin by Other (see comment). Potential for
interaction, monitor. Comment: Potential for increased risk of hypotension with
concurrent use. Monitor blood pressure and adjust dose of antihypertensive agent as
needed.
maraviroc
maraviroc, alfuzosin. Either increases effects of the other by pharmacodynamic
hypotension.
mefenamic acid
mefenamic acid decreases effects of alfuzosin by pharmacodynamic antagonism.
synthesis.
meloxicam
meloxicam decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
metoprolol
alfuzosin and metoprolol both increase anti-hypertensive channel blocking. Potential for
mifepristone
mifepristone, alfuzosin. QTc interval. Potential for dangerous interaction. Use with
caution and monitor closely. Use alternatives if available.
mitotane
mitotane decreases levels of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Significant interaction possible, monitor closely. Mitotane is a strong
inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4
substrates for possible dosage adjustments.
moexipril
moexipril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
moxisylyte
alfuzosin and moxisylyte both increase anti-hypertensive channel blocking. Potential for
nabumetone
nabumetone decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
nadolol
alfuzosin and nadolol both increase anti-hypertensive channel blocking. Potential for
naproxen
naproxen decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
nebivolol
alfuzosin and nebivolol both increase anti-hypertensive channel blocking. Potential for
nevirapine
nevirapine will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Significant interaction possible, monitor closely.
nicardipine
alfuzosin and nicardipine both increase anti-hypertensive channel blocking. Potential for
nifedipine
alfuzosin and nifedipine both increase anti-hypertensive channel blocking. Potential for
nisoldipine
alfuzosin and nisoldipine both increase anti-hypertensive channel blocking. Potential for
nitroglycerin rectal, alfuzosin. Either increases effects of the other by pharmacodynamic
olodaterol inhaled
alfuzosin and olodaterol inhaled both increase QTc interval. Significant interaction
possible, monitor closely. Drugs that prolong the QTc interval and may potentiate the
effects of beta2 agonists on the cardiovascular system; increased risk of ventricular
arrhythmias
oxaprozin
oxaprozin decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
parecoxib
parecoxib decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
pasireotide
alfuzosin and pasireotide both increase QTc interval. Potential for dangerous interaction.
Use with caution and monitor closely.
penbutolol
alfuzosin and penbutolol both increase anti-hypertensive channel blocking. Potential for
perindopril
perindopril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
phenoxybenzamine
alfuzosin and phenoxybenzamine both increase anti-hypertensive channel blocking.
phentolamine
alfuzosin and phentolamine both increase anti-hypertensive channel blocking. Potential
pindolol
alfuzosin and pindolol both increase anti-hypertensive channel blocking. Potential for
piroxicam
piroxicam decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
prazosin
alfuzosin and prazosin both increase anti-hypertensive channel blocking. Potential for
propranolol
alfuzosin and propranolol both increase anti-hypertensive channel blocking. Potential for
quinapril
quinapril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
ramipril
ramipril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
rifabutin
rifabutin will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
rifampin
rifampin will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
salicylates (non-asa) decreases effects of alfuzosin by pharmacodynamic antagonism.
synthesis.
salsalate
salsalate decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
silodosin
alfuzosin and silodosin both increase anti-hypertensive channel blocking. Potential for
sorafenib
sorafenib and alfuzosin both increase QTc interval. Significant interaction possible,
monitor closely.
sotalol
alfuzosin and sotalol both increase anti-hypertensive channel blocking. Potential for
st john's wort
st john's wort will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
sulfasalazine
sulfasalazine decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
sulindac
sulindac decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
tadalafil
tadalafil increases effects of alfuzosin by pharmacodynamic synergism. Significant
terazosin
alfuzosin and terazosin both increase anti-hypertensive channel blocking. Potential for
timolol
alfuzosin and timolol both increase anti-hypertensive channel blocking. Potential for
tolfenamic acid
tolfenamic acid decreases effects of alfuzosin by pharmacodynamic antagonism.
synthesis.
tolmetin
tolmetin decreases effects of alfuzosin by pharmacodynamic antagonism. Significant
trandolapril
trandolapril, alfuzosin. Mechanism: pharmacodynamic synergism. Significant interaction
verapamil
alfuzosin and verapamil both increase anti-hypertensive channel blocking. Potential for
zotepine
alfuzosin and zotepine both increase anti-hypertensive channel blocking. Potential for
Minor (70)
amobarbital
amobarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Minor or non-significant interaction.
aprepitant
aprepitant will increase the level or effect of alfuzosin by affecting hepatic/intestinal
armodafinil
armodafinil will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
artemether/lumefantrine
artemether/lumefantrine will decrease the level or effect of alfuzosin by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. Minor or non-significant interaction.
bosentan
bosentan will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
brimonidine
brimonidine increases effects of alfuzosin by pharmacodynamic synergism. Minor or
non-significant interaction.
budesonide
budesonide will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
butabarbital
butabarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
butalbital
butalbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
butcher's broom
alfuzosin, butcher's broom. Either decreases effects of the other by Mechanism:
clobetasone
clobetasone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
conivaptan
conivaptan will increase the level or effect of alfuzosin by affecting hepatic/intestinal
cortisone
cortisone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
cyclosporine
cyclosporine will increase the level or effect of alfuzosin by affecting hepatic/intestinal
darifenacin
darifenacin will increase the level or effect of alfuzosin by affecting hepatic/intestinal
dasatinib
dasatinib will increase the level or effect of alfuzosin by affecting hepatic/intestinal
deflazacort
deflazacort will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
dexamethasone
dexamethasone will decrease the level or effect of alfuzosin by affecting
dhea
dhea will increase the level or effect of alfuzosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Minor or non-significant interaction.
dronedarone
dronedarone will increase the level or effect of alfuzosin by affecting hepatic/intestinal
eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of alfuzosin by affecting
ethanol
alfuzosin, ethanol. Mechanism: pharmacodynamic synergism. Minor or non-significant
ethotoin
ethotoin will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
eucalyptus
eucalyptus will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
fluconazole
fluconazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
fludrocortisone
fludrocortisone will decrease the level or effect of alfuzosin by affecting
fluvoxamine
fluvoxamine will increase the level or effect of alfuzosin by affecting hepatic/intestinal
fosphenytoin
fosphenytoin will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
grapefruit
grapefruit will increase the level or effect of alfuzosin by affecting hepatic/intestinal
griseofulvin
griseofulvin will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
hexobarbital
hexobarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
hydrocortisone
hydrocortisone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
lapatinib
lapatinib will increase the level or effect of alfuzosin by affecting hepatic/intestinal
lofexidine
alfuzosin, lofexidine. Either decreases effects of the other by Mechanism:
lumefantrine
lumefantrine will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
marijuana
marijuana will increase the level or effect of alfuzosin by affecting hepatic/intestinal
mephobarbital
mephobarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
methylprednisolone
methylprednisolone will decrease the level or effect of alfuzosin by affecting
metronidazole
metronidazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
mibefradil
mibefradil will increase the level or effect of alfuzosin by affecting hepatic/intestinal
miconazole vaginal
miconazole vaginal will increase the level or effect of alfuzosin by affecting
modafinil
modafinil will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
nifedipine
nifedipine will increase the level or effect of alfuzosin by affecting hepatic/intestinal
nilotinib
nilotinib will increase the level or effect of alfuzosin by affecting hepatic/intestinal
oxcarbazepine
oxcarbazepine will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
oxiconazole
oxiconazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
pentobarbital
pentobarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
phenobarbital
phenobarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
phenylephrine
alfuzosin, phenylephrine. Either decreases effects of the other by Mechanism:
phenylephrine po
alfuzosin, phenylephrine po. Either decreases effects of the other by Mechanism:
phenytoin
phenytoin will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
posaconazole
posaconazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
prednisolone
prednisolone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
prednisone
prednisone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
primidone
primidone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of alfuzosin by affecting
rifapentine
rifapentine will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
rufinamide
rufinamide will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
secobarbital
secobarbital will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
sitaxentan
sitaxentan will increase the level or effect of alfuzosin by affecting hepatic/intestinal
telithromycin
telithromycin will increase the level or effect of alfuzosin by affecting hepatic/intestinal
tizanidine
tizanidine increases effects of alfuzosin by pharmacodynamic synergism. Minor or non-
topiramate
topiramate will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
treprostinil
treprostinil increases effects of alfuzosin by pharmacodynamic synergism. Minor or non-
triamcinolone
triamcinolone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
troglitazone
troglitazone will decrease the level or effect of alfuzosin by affecting hepatic/intestinal
troleandomycin
troleandomycin will increase the level or effect of alfuzosin by affecting
verapamil
verapamil will increase the level or effect of alfuzosin by affecting hepatic/intestinal
voriconazole
voriconazole will increase the level or effect of alfuzosin by affecting hepatic/intestinal
Adverse Effects
1-10%
Abdominal pain (1-2%)
Back pain (1-2%)
Brochitis (1-2%)
Constipation (1-2%)
Dizziness (5.7%)
Dyspepsia (1-2%)
Fatigue (2.7%)
Headache (3%)
Impotence (1-2%)
Nausea (1-2%)
Pharyngitis (1-2%)
URT infection (3%)
Sinusitis (1-2%)
Upper respiratory infection (3%)
Postmarketing Reports
General disorders: Edema
Cardiac disorders: Tachycardia, chest pain, angina pectoris in patients with pre-existing coronary
artery disease, atrial fibrillation
Gastrointestinal disorders: Diarrhea
Hepatobiliary disorders: Hepatocellular and cholestatic liver injury (including cases with
jaundice leading to drug discontinuation)
Upper respiratory system: Rhinitis
Reproductive system: Priapism
Dermatology: Rash, pruritus, urticaria, angioedema, toxic epidermal necrolysis
Vascular disorders: Flushing
Blood and lymphatic system disorders: Thrombocytopenia
Contraindications
Hypersensitivity
Moderate to severe liver impairment
Coadministration with potent CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir) or
other alpha1-blocking agents
Cautions
Caution in coronary artery disease, liver disease, symptomatic orthostatic hypotension or
coadministration with other drugs that lower blood pressure
May cause syncope (first-dose effect)
Discontinue treatment if angina occurs or worsens
Rule out prostate cancer before initiating therapy (symptoms similar)
Priapism may occur with use
Rule out prostate cancer prior to treatment
Caution with renal impairment (ieg, CrCl <30 mL/min)
Caution with history of prolonged QT syndrome (shown to prolong QT interval)
Intraoperative floppy iris syndrome during cataract surgery reported Advise patient regarding
risk of priapism
Do not chew or crush tablets
Not for use as antihypertensive drug
Pharmacology
Mechanism of Action
Selective antagonist of postsynaptic alpha-1-adrenoceptors; blockade of adrenoreceptors in the
prostate, prostatic capsule, bladder neck and prostatic urethra
Absorption
Bioavailability: 49%
Peak Plasma Time: 8 hr
Peak Plasma Concentration: 13.6 ng/mL
AUC: 194 ng.hr/mL
Distribution
Protein Bound: 82-90%
Vd: 3.2 L/kg
Metabolism
Hepatic P450 enzyme CYP3A4
Elimination
Half-life: 5-10 hr
Excretion: Feces (69%); urine (24%)
Patient Handout
560043
Patient Education
alfuzosin oral
ALFUZOSIN EXTENDED-RELEASE - ORAL
(al-FUE-zoe-sin)
COMMON BRAND NAME(S): Uroxatral
USES:
This medication is used to treat the symptoms of a prostate gland condition called BPH (benign
prostatic hyperplasia, also known as enlarged prostate). It is an alpha blocker that works by
relaxing the muscles in the bladder neck and prostate. Relaxing these muscles leads to relief of
symptoms of BPH such as the feeling of needing to urinate frequently or urgently, difficulty in
beginning the flow of urine, weak stream, and the need to urinate during the middle of the night.
This medication should not be used to treat high blood pressure.
OTHER USES:
professional.
Alfuzosin may also be used to help your body "pass," or get rid of, kidney stones through
urination.
HOW TO USE:
Read the Patient Information Leaflet provided by your pharmacist before you start using
alfuzosin and each time you get a refill. If you have any questions, consult your doctor or
pharmacist.
Take this medication by mouth once daily after a meal or as directed by your doctor. This
medication works best when taken with food. Taking alfuzosin on an empty stomach may
decrease the absorption of this drug and reduce its effectiveness.
Do not crush or chew extended-release tablets. Doing so can release all of the drug at once,
increasing the risk of side effects. Also, do not split the tablets unless they have a score line and
your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing
or chewing.
This medication may cause dizziness and lightheadedness. To avoid injuries such as falls, take
your first dose of alfuzosin with food at bedtime until your body adjusts to the effect of the
medicine. Also, anytime the dosage of this drug is changed, take your first new dose with food at
bedtime.
Use this medication regularly in order to get the most benefit from it. Remember to take it after
the same meal each day.
Inform your doctor if your condition persists or worsens.
SIDE EFFECTS:
Dizziness/lightheadedness, headache, or decreased sexual ability may occur. If any of these
effects persist or worsen, tell your doctor or pharmacist promptly.
Tell your doctor immediately if any of these unlikely but serious side effects occur: unusual
tiredness/weakness, severe stomach/abdominal pain, yellowing eyes/skin, persistent
nausea/vomiting, dark urine.
Seek immediate medical attention if any of these rare but very serious side effects occur: severe
dizziness, fainting, fast/irregular heartbeat, chest pain.
For males, in the very unlikely event you have a painful or prolonged erection lasting 4 or more
hours, stop using this drug and seek immediate medical attention, or permanent problems could
occur.
if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking alfuzosin, tell your doctor or pharmacist if you are allergic to it; or to other alpha
blockers such as doxazosin, prazosin, terazosin; or if you have any other allergies. This product
may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to
your pharmacist for more details.
This medication should not be used if you have certain medical conditions. Before using this
medicine, consult your doctor or pharmacist if you have: liver problems.
other prostate gland problems (e.g., prostate cancer), heart problems (e.g., angina, low blood
pressure), kidney disease.
Alfuzosin may cause a condition that affects the heart rhythm (QT prolongation). QT
prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other
symptoms (such as severe dizziness, fainting) that need medical attention right away.
The risk of QT prolongation may be increased if you have certain medical conditions or are
taking other drugs that may cause QT prolongation. Before using alfuzosin, tell your doctor or
pharmacist of all the drugs you take and if you have any of the following conditions: certain
heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of
certain heart problems (QT prolongation in the EKG, sudden cardiac death).
Low levels of potassium or magnesium in the blood may also increase your risk of QT
prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or
if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about
using alfuzosin safely.
This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires
alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.
To minimize dizziness and lightheadedness, get up slowly when rising from a sitting or lying
position, especially when you first start taking this drug or if your doctor changes your dose.
Also, when you first start taking this drug, avoid situations where you may be injured if you
faint.
Before having surgery (including cataract eye surgery), tell your doctor or dentist that you are
taking this medication.
Older adults may be more sensitive to the side effects of this drug, especially dizziness and QT
prolongation (see above).
During pregnancy, alfuzosin should be used only when clearly needed. Discuss the risks and
benefits with your doctor.
It is unknown if this medication passes into breast milk. Consult your doctor before breast-
feeding.
DRUG INTERACTIONS:
Drug interactions may change how your medications work or increase your risk for serious side
effects. This document does not contain all possible drug interactions. Keep a list of all the
products you use (including prescription/nonprescription drugs and herbal products) and share it
with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines
Some products that may interact with this drug include: drugs to treat erectile dysfunction-ED or
pulmonary hypertension (such as sildenafil, tadalafil, vardenafil), other medications that lower
blood pressure (e.g., atenolol, diltiazem).
Other medications can affect the removal of alfuzosin from your body, which may affect how
alfuzosin works. Examples include azole antifungals (such as itraconazole, ketoconazole),
boceprevir, macrolide antibiotics (such as clarithromycin), nefazodone, HIV protease inhibitors
(such as lopinavir, ritonavir), a certain combination HIV medication
(elvitegravir/cobicistat/emtricitabine/tenofovir), telaprevir, telithromycin, among others.
Many drugs besides alfuzosin may affect the heart rhythm (QT prolongation), including
amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such
as erythromycin), among others. Therefore, before using alfuzosin, report all medications you are
currently using to your doctor or pharmacist.
OVERDOSE:
provincial poison control center. Symptoms of overdose may include: fainting, irregular
heartbeat.
NOTES:
Laboratory and/or medical tests (e.g., prostate exams, prostate-specific antigen or PSA) should
be performed periodically to monitor your progress or check for side effects. Consult your doctor
for more details.
MISSED DOSE:
STORAGE:
Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all
medications away from children and pets.
local waste disposal company for more details.
Information last revised March 2013. Copyright(c) 2013 First Databank, Inc.
Terazosin (Hytrin)

Terazosin is a quinazoline compound that counteracts alpha1-induced adrenergic contractions of
bladder neck, facilitating urinary flow in the presence of BPH. It is indicated for the treatment of
symptomatic BPH and hypertension. Its effect on voiding symptoms and flow rates is dose-
dependent. It improves irritative and obstructive voiding symptoms. Improvement in flow rate is
objective. A Hytrin starter pack is available for easy dosing progression to 5 mg.
Dosing & Uses
AdultPediatricGeriatric
Benign Prostate Hyperplasia
May gradually increase to 5 mg PO qHS; up to 20 mg/day beneficial for some
Dosing considerations
May take with food
Hypertension
Maintenance: 1-5 mg/day or q12hr; may increase to 20 mg/day
May take with food
Dosing Modifications
Hepatic impairment: Use with caution
Drug Interactions
Interaction Checker
terazosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (0)
sildenafil
sildenafil increases effects of terazosin by pharmacodynamic synergism. Possible serious
tamsulosin
terazosin, tamsulosin. Either increases effects of the other by additive vasodilation.
vardenafil
vardenafil increases effects of terazosin by pharmacodynamic synergism. High likelihood
yohimbe
yohimbe increases effects of terazosin by pharmacodynamic synergism. High likelihood
acebutolol
terazosin and acebutolol both increase anti-hypertensive channel blocking. Potential for
dangerous interaction. Use with caution and monitor closely. Additive hypotensive
effects may occur when terazosin is used in combination with acebutolol.
aceclofenac
aceclofenac decreases effects of terazosin by pharmacodynamic antagonism. Significant
acemetacin
acemetacin decreases effects of terazosin by pharmacodynamic antagonism. Significant
aldesleukin
aldesleukin increases effects of terazosin by pharmacodynamic synergism. Potential for
alfuzosin
alfuzosin and terazosin both increase anti-hypertensive channel blocking. Potential for
amifostine
amifostine increases effects of terazosin by pharmacodynamic synergism. Potential for
amlodipine
terazosin and amlodipine both increase anti-hypertensive channel blocking. Potential for
asenapine
asenapine and terazosin both increase anti-hypertensive channel blocking. Potential for
aspirin
aspirin decreases effects of terazosin by pharmacodynamic antagonism. Significant
aspirin rectal
aspirin rectal decreases effects of terazosin by pharmacodynamic antagonism. Significant
aspirin/citric acid/sodium bicarbonate decreases effects of terazosin by pharmacodynamic
atenolol
terazosin and atenolol both increase anti-hypertensive channel blocking. Potential for
avanafil
avanafil increases effects of terazosin by pharmacodynamic synergism. Significant
benazepril
benazepril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
betaxolol
terazosin and betaxolol both increase anti-hypertensive channel blocking. Potential for
bisoprolol
terazosin and bisoprolol both increase anti-hypertensive channel blocking. Potential for
captopril
captopril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
carbidopa
carbidopa increases effects of terazosin by pharmacodynamic synergism. Potential for
carvedilol
terazosin and carvedilol both increase anti-hypertensive channel blocking. Potential for
celecoxib
celecoxib decreases effects of terazosin by pharmacodynamic antagonism. Significant
celiprolol
terazosin and celiprolol both increase anti-hypertensive channel blocking. Potential for
choline magnesium trisalicylate decreases effects of terazosin by pharmacodynamic
clevidipine
terazosin and clevidipine both increase anti-hypertensive channel blocking. Potential for
diclofenac
diclofenac decreases effects of terazosin by pharmacodynamic antagonism. Significant
diflunisal
diflunisal decreases effects of terazosin by pharmacodynamic antagonism. Significant
diltiazem
terazosin and diltiazem both increase anti-hypertensive channel blocking. Potential for
doxazosin
doxazosin and terazosin both increase anti-hypertensive channel blocking. Potential for
enalapril
enalapril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
esmolol
terazosin and esmolol both increase anti-hypertensive channel blocking. Potential for
effects may occur when terazosin is used in combination with esmolol.
etodolac
etodolac decreases effects of terazosin by pharmacodynamic antagonism. Significant
etoricoxib
etoricoxib decreases effects of terazosin by pharmacodynamic antagonism. Significant
felodipine
terazosin and felodipine both increase anti-hypertensive channel blocking. Potential for
fenbufen
fenbufen decreases effects of terazosin by pharmacodynamic antagonism. Significant
fenoprofen
fenoprofen decreases effects of terazosin by pharmacodynamic antagonism. Significant
flurbiprofen
flurbiprofen decreases effects of terazosin by pharmacodynamic antagonism. Significant
fosinopril
fosinopril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
ibuprofen
ibuprofen decreases effects of terazosin by pharmacodynamic antagonism. Significant
iloperidone
iloperidone increases effects of terazosin by pharmacodynamic synergism. Significant
imidapril
imidapril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
indomethacin
indomethacin decreases effects of terazosin by pharmacodynamic antagonism.
synthesis.
isradipine
terazosin and isradipine both increase anti-hypertensive channel blocking. Potential for
ketoprofen
ketoprofen decreases effects of terazosin by pharmacodynamic antagonism. Significant
ketorolac
ketorolac decreases effects of terazosin by pharmacodynamic antagonism. Significant
ketorolac intranasal decreases effects of terazosin by pharmacodynamic antagonism.
synthesis.
labetalol
terazosin and labetalol both increase anti-hypertensive channel blocking. Potential for
lacidipine
terazosin and lacidipine both increase anti-hypertensive channel blocking. Potential for
lercanidipine
terazosin and lercanidipine both increase anti-hypertensive channel blocking. Potential
levodopa
levodopa increases effects of terazosin by pharmacodynamic synergism. Significant
agent.
lisinopril
lisinopril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
lornoxicam
lornoxicam decreases effects of terazosin by pharmacodynamic antagonism. Significant
lurasidone
lurasidone increases effects of terazosin by Other (see comment). Potential for
needed.
maraviroc
maraviroc, terazosin. Either increases effects of the other by pharmacodynamic
hypotension.
mefenamic acid
mefenamic acid decreases effects of terazosin by pharmacodynamic antagonism.
synthesis.
meloxicam
meloxicam decreases effects of terazosin by pharmacodynamic antagonism. Significant
metoprolol
terazosin and metoprolol both increase anti-hypertensive channel blocking. Potential for
moexipril
moexipril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
moxisylyte
moxisylyte and terazosin both increase anti-hypertensive channel blocking. Potential for
nabumetone
nabumetone decreases effects of terazosin by pharmacodynamic antagonism. Significant
nadolol
terazosin and nadolol both increase anti-hypertensive channel blocking. Potential for
naproxen
naproxen decreases effects of terazosin by pharmacodynamic antagonism. Significant
nebivolol
terazosin and nebivolol both increase anti-hypertensive channel blocking. Potential for
nicardipine
terazosin and nicardipine both increase anti-hypertensive channel blocking. Potential for
nifedipine
terazosin and nifedipine both increase anti-hypertensive channel blocking. Potential for
nisoldipine
terazosin and nisoldipine both increase anti-hypertensive channel blocking. Potential for
nitroglycerin rectal, terazosin. Either increases effects of the other by pharmacodynamic
oxaprozin
oxaprozin decreases effects of terazosin by pharmacodynamic antagonism. Significant
parecoxib
parecoxib decreases effects of terazosin by pharmacodynamic antagonism. Significant
penbutolol
terazosin and penbutolol both increase anti-hypertensive channel blocking. Potential for
perindopril
perindopril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
phenoxybenzamine
phenoxybenzamine and terazosin both increase anti-hypertensive channel blocking.
phentolamine
phentolamine and terazosin both increase anti-hypertensive channel blocking. Potential
pindolol
terazosin and pindolol both increase anti-hypertensive channel blocking. Potential for
piroxicam
piroxicam decreases effects of terazosin by pharmacodynamic antagonism. Significant
prazosin
prazosin and terazosin both increase anti-hypertensive channel blocking. Potential for
propranolol
terazosin and propranolol both increase anti-hypertensive channel blocking. Potential for
effects may occur when terazosin is used in combination with propranolol.
quinapril
quinapril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
ramipril
ramipril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
salicylates (non-asa) decreases effects of terazosin by pharmacodynamic antagonism.
synthesis.
salsalate
salsalate decreases effects of terazosin by pharmacodynamic antagonism. Significant
silodosin
silodosin and terazosin both increase anti-hypertensive channel blocking. Potential for
sotalol
terazosin and sotalol both increase anti-hypertensive channel blocking. Potential for
effects may occur when terazosin is used in combination with sotalol.
sulfasalazine
sulfasalazine decreases effects of terazosin by pharmacodynamic antagonism. Significant
sulindac
sulindac decreases effects of terazosin by pharmacodynamic antagonism. Significant
tadalafil
tadalafil increases effects of terazosin by pharmacodynamic synergism. Significant
timolol
terazosin and timolol both increase anti-hypertensive channel blocking. Potential for
tolfenamic acid
tolfenamic acid decreases effects of terazosin by pharmacodynamic antagonism.
synthesis.
tolmetin
tolmetin decreases effects of terazosin by pharmacodynamic antagonism. Significant
trandolapril
trandolapril, terazosin. Mechanism: pharmacodynamic synergism. Significant interaction
verapamil
terazosin and verapamil both increase anti-hypertensive channel blocking. Potential for
zotepine
terazosin and zotepine both increase anti-hypertensive channel blocking. Potential for
Minor (8)
brimonidine
brimonidine increases effects of terazosin by pharmacodynamic synergism. Minor or
butcher's broom
terazosin, butcher's broom. Either decreases effects of the other by Mechanism:
ethanol
terazosin, ethanol. Mechanism: pharmacodynamic synergism. Minor or non-significant
lofexidine
terazosin, lofexidine. Either decreases effects of the other by Mechanism:
phenylephrine
terazosin, phenylephrine. Either decreases effects of the other by Mechanism:
phenylephrine po
terazosin, phenylephrine po. Either decreases effects of the other by Mechanism:
tizanidine
tizanidine increases effects of terazosin by pharmacodynamic synergism. Minor or non-
treprostinil
treprostinil increases effects of terazosin by pharmacodynamic synergism. Minor or non-
Adverse Effects
>10%
Dizziness (10-20%)
Asthenia (2-13%)
1-10%
Hypotension (3-7%)
Rhinitis/nasal congestion (2-6%)
Lightheadedness (3-5%)
Somnolence (3-5%)
Palpitation (4%)
Nausea (2-4%)
Edema (3%)
Sinusitis (3%)
Dyspnea (2-3%)
Fatigue (2.5%)
Headache (2.5%)
Back pain (2.4%)
Flulike syndrome (2.4%)
Tachycardia (2%)
Amblyopia (1-2%)
Blurred vision (1-2%)
Impotence (1-2%)
Syncope (1%)
Contraindications
Hypersensitivity to terazosin, other quinazolines
Cautions
Prostate carcinoma
Liver disease
May cause first-dose syncope/sudden LOC and orthostatic hypotension; minimize effect by
using small first dose at bedtime; increase dose slowly
Concomitant use of other antihypertensives (additive hypotensive effects)
Concomitant administration with PDE-5 inhibitor (eg, sildenafil) can result in additive blood
pressure-lowering effects and symptomatic hypotension; initiate PDE-5 inhibitor therapy at
lowest dose
Risk of priapism (rare but needs medical attention)
Pharmacology
Mechanism of Action
Blocks postsynaptic alpha-1 receptor; alpha blockade causes arterial and venous dilation
Selective agents cause less tachycardia than do nonselective agents
Absorption
Onset (hypertension): 3 hr
Onset (benign prostate hyperplasia): 2 weeks
Duration: 24 hr
Peak response (benign prostate hyperplasia): 4-6 weeks
Peak plasma time: 1 hr
Distribution
Protein bound: 90-94%
Vd: 25-30 L
Metabolism
Metabolized extensively via hydrolysis, O-demethylation, and N-dealkylation in liver
Metabolites: 6- and 7-O-demethyl terazosin, piperazine derivative, diamine metabolite
Elimination
Half-life: 9-12 hr
Renal clearance: 9-12.5 mL/min
Excretion: Feces (55-60%); urine (40%)
Patient Handout
560043
Patient Education
terazosin oral
TERAZOSIN - ORAL
(ter-AY-zoe-sin)
COMMON BRAND NAME(S): Hytrin
USES:
Terazosin is used alone or with other drugs to treat high blood pressure (hypertension). Lowering
high blood pressure helps prevent strokes, heart attacks, and kidney problems. This medication
works by relaxing blood vessels so blood can flow more easily.
Terazosin is also used in men to treat the symptoms of an enlarged prostate (benign prostatic
hyperplasia-BPH). It does not shrink the prostate, but it works by relaxing the muscles in the
prostate and part of the bladder. This helps to relieve symptoms of BPH such as difficulty in
beginning the flow of urine, weak stream, and the need to urinate frequently or urgently
(including during the middle of the night).
Terazosin belongs to a class of drugs known as alpha blockers.
OTHER USES:
professional.
Terazosin may also be used to help your body "pass," or get rid of, kidney stones through
urination. It has also been used to help treat bladder problems in women.
HOW TO USE:
Read the Patient Information Leaflet if available from your pharmacist before you start taking
terazosin and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
Take this medication by mouth with or without food as directed by your doctor, usually once
daily at bedtime.
If you are taking this drug for the first time, do not take more than 1 milligram to start. Terazosin
may cause a sudden drop in your blood pressure, which could lead to dizziness or fainting. This
risk is higher when taking your first dose. Therefore, to avoid injury related to dizziness or
fainting, take your first dose of terazosin at bedtime.
Your doctor will start this medication at a low dose and gradually increase your dose. Any time
your dose is increased or if you restart treatment after you have stopped it, take your first dose at
bedtime unless otherwise directed to lessen the risk of injury related to dizziness or fainting. Also
during these times, avoid situations where you may be injured if you faint.
The dosage is based on your medical condition and response to treatment.
Take this medication regularly to get the most benefit from it. To help you remember, take it at
the same time each day. If you miss taking terazosin for a few days, you may need to restart
treatment at the low dose and gradually increase your dose again. Consult your doctor for more
details.
If you are taking this medication for high blood pressure, it is important to continue taking this
medication even if you feel well. Most people with high blood pressure do not feel sick. Tell
your doctor if your blood pressure readings remain high or increase.
If you are taking this drug for an enlarged prostate, it may take 2 to 4 weeks to see an
improvement in your symptoms, and up to 6 weeks before you see the full benefit of this drug.
Tell your doctor if your condition does not improve or if it worsens.
SIDE EFFECTS:
Dizziness, lightheadedness, tiredness, nausea, drowsiness, blurred vision, headache, or stuffy
nose may occur. If any of these effects persist or worsen, tell your doctor or pharmacist
promptly.
To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or
lying position.
Tell your doctor right away if you have any serious side effects, including: fainting, fast/irregular
heartbeat, burning/tingling in the hands/feet, sexual function problems, swelling of the
ankles/hands/feet, unexpected weight gain.
Rarely, males may have a painful or prolonged erection lasting 4 or more hours. If this occurs,
stop using this drug and get medical help right away, or permanent problems could occur.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you
notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially
of the face/tongue/throat), severe dizziness, trouble breathing.
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking terazosin, tell your doctor or pharmacist if you are allergic to it; or to other alpha
blockers such as doxazosin or prazosin; or if you have any other allergies. This product may
low blood pressure/fainting.
requires alertness until you are sure you can perform such activities safely. You should avoid
driving or hazardous tasks for 12 hours after the first dose, after your dose is increased, and when
this medication is restarted after it has been stopped. Limit alcoholic beverages.
Before having surgery (including cataract eye surgery), tell your doctor or dentist about all the
products you use (including prescription drugs, nonprescription drugs, and herbal products).
Older adults may be more sensitive to the side effects of this drug, especially dizziness, fainting,
and low blood pressure. These side effects can increase the risk of falling.
It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS:
If you are also taking a drug to treat erectile dysfunction-ED or pulmonary hypertension (such as
sildenafil, tadalafil), your blood pressure may get too low which can lead to dizziness or fainting.
Your doctor may need to adjust your medications to minimize this risk.
Check the labels on all your medicines (such as cough-and-cold products, diet aids, or NSAIDs
such as ibuprofen, naproxen) because they may contain ingredients that could increase your
blood pressure. Ask your pharmacist for more details.
OVERDOSE:
provincial poison control center. Symptoms of overdose may include: severe dizziness, fainting.
NOTES:
If you have high blood pressure, lifestyle changes that may help this medication work better
include exercising, stopping smoking, and eating a low-cholesterol/low-fat diet. Consult your
doctor for more details.
Have your blood pressure checked regularly while taking this medication. Learn how to monitor
your own blood pressure at home, and share the results with your doctor.
Laboratory and/or medical tests (such as prostate exams, blood pressure) should be performed
periodically to monitor your progress or check for side effects. Consult your doctor for more
details.
MISSED DOSE:
the missed dose and resume your usual dosing schedule. Do not double the dose to catch up. See
also How to Use section.
STORAGE:
Store at room temperature away from light and moisture. Do not store in the bathroom. Capsules
should be stored between 68-77 degrees F (20-25 degrees C), because they may soften or melt if
stored at higher than recommended temperatures. Keep all medications away from children and
pets.
local waste disposal company.
Doxazosin (Cardura, Cardura XL)

Doxazosin is indicated for the treatment of urinary outflow obstruction and irritative symptoms
associated with BPH and hypertension. It inhibits postsynaptic alpha-adrenergic receptors,
resulting in vasodilation of veins and arterioles and a decrease in total peripheral resistance and
blood pressure. It is a long-acting alpha1-blocking agent with a profile similar to that of
terazosin. Doxazosin improves irritative and obstructive voiding symptoms.
Dosing & Uses
AdultPediatricGeriatric
Hypertension
Immediate release: 1-16 mg PO once daily in AM or PM
Extended release: Not indicated for hypertension
Benign Prostatic Hyperplasia
Immediate release: 1-8 mg/day PO
Extended release: 4 mg/day PO initially at breakfast; may be increased to no more than 8 mg/day
PO
Hepatic impairment: Use with caution in mild-to-moderate hepatic dysfunction; do not use in
severe impairment
Dosing Considerations
Give first dose and increase at bedtime to avoid syncope
Hypertension (Off-label)
Immediate release: 1-4 mg PO once daily in AM or PM
Hypertension
Avoid use for hypertension; high risk of orthostatic hypotension (Beers criteria); if used, lower
initial dosages and gradual adjustments are recommended
Immediate release: 0.5-16 mg PO once daily in AM or PM
Extended release: Not indicated for hypertension
Immediate release: 1-8 mg/day PO
Extended release: 4 mg/day PO initially at breakfast; may be increased to no more than 8 mg/day
PO
Drug Interactions
Interaction Checker
doxazosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (1)
boceprevir
boceprevir increases levels of doxazosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination.
sildenafil
sildenafil increases effects of doxazosin by pharmacodynamic synergism. Possible
serious or life-threatening interaction. Monitor closely. Use alternatives if available. Risk
of hypotension; separate sildenafil >25mg from alpha blocker by 4hr.
tamsulosin
doxazosin, tamsulosin. Either increases effects of the other by additive vasodilation.
vardenafil
vardenafil increases effects of doxazosin by pharmacodynamic synergism. High
outweigh risks and no alternatives available. Never use combination. Risk of
hypotension.
yohimbe
yohimbe increases effects of doxazosin by pharmacodynamic synergism. High likelihood
acebutolol
doxazosin and acebutolol both increase anti-hypertensive channel blocking. Potential for
hypotension following the first dose of doxozosin may be enhanced.
aceclofenac
aceclofenac decreases effects of doxazosin by pharmacodynamic antagonism. Significant
acemetacin
acemetacin decreases effects of doxazosin by pharmacodynamic antagonism. Significant
aldesleukin
aldesleukin increases effects of doxazosin by pharmacodynamic synergism. Potential for
alfuzosin
alfuzosin and doxazosin both increase anti-hypertensive channel blocking. Potential for
amifostine
amifostine increases effects of doxazosin by pharmacodynamic synergism. Potential for
amlodipine
doxazosin and amlodipine both increase anti-hypertensive channel blocking. Potential for
asenapine
asenapine and doxazosin both increase anti-hypertensive channel blocking. Potential for
aspirin
aspirin decreases effects of doxazosin by pharmacodynamic antagonism. Significant
aspirin rectal
aspirin rectal decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
aspirin/citric acid/sodium bicarbonate decreases effects of doxazosin by
atenolol
doxazosin and atenolol both increase anti-hypertensive channel blocking. Potential for
avanafil
avanafil increases effects of doxazosin by pharmacodynamic synergism. Significant
benazepril
benazepril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
betaxolol
doxazosin and betaxolol both increase anti-hypertensive channel blocking. Potential for
bisoprolol
doxazosin and bisoprolol both increase anti-hypertensive channel blocking. Potential for
captopril
captopril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
carbidopa
carbidopa increases effects of doxazosin by pharmacodynamic synergism. Potential for
carvedilol
doxazosin and carvedilol both increase anti-hypertensive channel blocking. Potential for
celecoxib
celecoxib decreases effects of doxazosin by pharmacodynamic antagonism. Significant
celiprolol
doxazosin and celiprolol both increase anti-hypertensive channel blocking. Potential for
choline magnesium trisalicylate decreases effects of doxazosin by pharmacodynamic
clevidipine
doxazosin and clevidipine both increase anti-hypertensive channel blocking. Potential for
clonidine
clonidine, doxazosin. Either increases toxcity of the other by pharmacodynamic
synergism. Significant interaction possible, monitor closely. Additive sympatholytic
action may worsen sinus node dysfunction and atrioventricular (AV) block.
diclofenac
diclofenac decreases effects of doxazosin by pharmacodynamic antagonism. Significant
diflunisal
diflunisal decreases effects of doxazosin by pharmacodynamic antagonism. Significant
diltiazem
doxazosin and diltiazem both increase anti-hypertensive channel blocking. Potential for
enalapril
enalapril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
esmolol
doxazosin and esmolol both increase anti-hypertensive channel blocking. Potential for
etodolac
etodolac decreases effects of doxazosin by pharmacodynamic antagonism. Significant
etoricoxib
etoricoxib decreases effects of doxazosin by pharmacodynamic antagonism. Significant
felodipine
doxazosin and felodipine both increase anti-hypertensive channel blocking. Potential for
fenbufen
fenbufen decreases effects of doxazosin by pharmacodynamic antagonism. Significant
fenoprofen
fenoprofen decreases effects of doxazosin by pharmacodynamic antagonism. Significant
flurbiprofen
flurbiprofen decreases effects of doxazosin by pharmacodynamic antagonism. Significant
fosinopril
fosinopril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
ibuprofen
ibuprofen decreases effects of doxazosin by pharmacodynamic antagonism. Significant
iloperidone
iloperidone increases effects of doxazosin by pharmacodynamic synergism. Significant
imidapril
imidapril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
indomethacin
indomethacin decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
isradipine
doxazosin and isradipine both increase anti-hypertensive channel blocking. Potential for
ketoprofen
ketoprofen decreases effects of doxazosin by pharmacodynamic antagonism. Significant
ketorolac
ketorolac decreases effects of doxazosin by pharmacodynamic antagonism. Significant
ketorolac intranasal decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
labetalol
doxazosin and labetalol both increase anti-hypertensive channel blocking. Potential for
lacidipine
doxazosin and lacidipine both increase anti-hypertensive channel blocking. Potential for
lercanidipine
doxazosin and lercanidipine both increase anti-hypertensive channel blocking. Potential
levodopa
levodopa increases effects of doxazosin by pharmacodynamic synergism. Significant
agent.
lisinopril
lisinopril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
lornoxicam
lornoxicam decreases effects of doxazosin by pharmacodynamic antagonism. Significant
lurasidone
lurasidone increases effects of doxazosin by Other (see comment). Potential for
needed.
maraviroc
maraviroc, doxazosin. Either increases effects of the other by pharmacodynamic
hypotension.
mefenamic acid
mefenamic acid decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
meloxicam
meloxicam decreases effects of doxazosin by pharmacodynamic antagonism. Significant
metoprolol
doxazosin and metoprolol both increase anti-hypertensive channel blocking. Potential for
moexipril
moexipril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
moxisylyte
doxazosin and moxisylyte both increase anti-hypertensive channel blocking. Potential for
nabumetone
nabumetone decreases effects of doxazosin by pharmacodynamic antagonism. Significant
nadolol
doxazosin and nadolol both increase anti-hypertensive channel blocking. Potential for
naproxen
naproxen decreases effects of doxazosin by pharmacodynamic antagonism. Significant
nebivolol
doxazosin and nebivolol both increase anti-hypertensive channel blocking. Potential for
nicardipine
doxazosin and nicardipine both increase anti-hypertensive channel blocking. Potential for
nifedipine
doxazosin and nifedipine both increase anti-hypertensive channel blocking. Potential for
nisoldipine
doxazosin and nisoldipine both increase anti-hypertensive channel blocking. Potential for
nitroglycerin rectal, doxazosin. Either increases effects of the other by pharmacodynamic
oxaprozin
oxaprozin decreases effects of doxazosin by pharmacodynamic antagonism. Significant
parecoxib
parecoxib decreases effects of doxazosin by pharmacodynamic antagonism. Significant
penbutolol
doxazosin and penbutolol both increase anti-hypertensive channel blocking. Potential for
perindopril
perindopril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
phenoxybenzamine
doxazosin and phenoxybenzamine both increase anti-hypertensive channel blocking.
phentolamine
doxazosin and phentolamine both increase anti-hypertensive channel blocking. Potential
pindolol
doxazosin and pindolol both increase anti-hypertensive channel blocking. Potential for
piroxicam
piroxicam decreases effects of doxazosin by pharmacodynamic antagonism. Significant
prazosin
doxazosin and prazosin both increase anti-hypertensive channel blocking. Potential for
propranolol
doxazosin and propranolol both increase anti-hypertensive channel blocking. Potential for
quinapril
quinapril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
ramipril
ramipril, doxazosin. Mechanism: pharmacodynamic synergism. Significant interaction
salicylates (non-asa) decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
salsalate
salsalate decreases effects of doxazosin by pharmacodynamic antagonism. Significant
silodosin
doxazosin and silodosin both increase anti-hypertensive channel blocking. Potential for
sotalol
doxazosin and sotalol both increase anti-hypertensive channel blocking. Potential for
sulfasalazine
sulfasalazine decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
sulindac
sulindac decreases effects of doxazosin by pharmacodynamic antagonism. Significant
tadalafil
tadalafil increases effects of doxazosin by pharmacodynamic synergism. Significant
terazosin
doxazosin and terazosin both increase anti-hypertensive channel blocking. Potential for
timolol
doxazosin and timolol both increase anti-hypertensive channel blocking. Potential for
tolfenamic acid
tolfenamic acid decreases effects of doxazosin by pharmacodynamic antagonism.
synthesis.
tolmetin
tolmetin decreases effects of doxazosin by pharmacodynamic antagonism. Significant
trandolapril
trandolapril, doxazosin. Mechanism: pharmacodynamic synergism. Significant
verapamil
doxazosin and verapamil both increase anti-hypertensive channel blocking. Potential for
zotepine
doxazosin and zotepine both increase anti-hypertensive channel blocking. Potential for
Minor (8)
brimonidine
brimonidine increases effects of doxazosin by pharmacodynamic synergism. Minor or
butcher's broom
doxazosin, butcher's broom. Either decreases effects of the other by Mechanism:
ethanol
doxazosin, ethanol. Mechanism: pharmacodynamic synergism. Minor or non-significant
lofexidine
doxazosin, lofexidine. Either decreases effects of the other by Mechanism:
phenylephrine
doxazosin, phenylephrine. Either decreases effects of the other by Mechanism:
phenylephrine po
doxazosin, phenylephrine po. Either decreases effects of the other by Mechanism:
tizanidine
tizanidine increases effects of doxazosin by pharmacodynamic synergism. Minor or non-
treprostinil
treprostinil increases effects of doxazosin by pharmacodynamic synergism. Minor or
Adverse Effects
>10%
Dizziness (5-19%)
Fatigue (8-12%)
Headache (6-10%)
1-10%
Vertigo (7%)
Upper respiratory tract infection (URTI) (5%)
Edema (3-4%)
Rhinitis (3%)
Dyspnea (1-3%)
Abdominal pain (2%)
Hypotension (1-2%)
Nausea (1-2%)
Orthostatic hypotension (dose related) (0.3-2%)
Anxiety (1%)
Palpitations (1%)
Contraindications
Hypersensitivity to doxazosin or other quinazolines
Cautions
Use with caution in liver disease or recent cerebrovascular accident (CVA)
Rule out prostate cancer before initiating therapy
May cause first-dose syncope or sudden loss of consciousness
Risk of orthostatic hypotension (dose dependent)
Potential for hypotension, dry mouth, and urinary complications in elderly
Priapism reported with use
Concomitant use of other antihypertensives (additive hypotensive effects)
Extended-release form not indicated for hypertension
Concomitant administration of immediate-release form with a phosphodiesterase-5 (PDE-5)
inhibitor can result in additive blood pressure lowering effects and symptomatic hypotension
Pharmacology
Mechanism of Action
Hypertension: Blocks postsynaptic alpha1 receptors; alpha blockade causes arterial, arteriolar,
and venous dilation; decreases total peripheral resistance and blood pressure
Benign prostatic hyperplasia (BPH): Blocks alpha1 receptors in prostatic stromal and bladder
tissues; reduces sympathetic tone-induced urethral stricture responsible for BPH symptoms
Absorption
Bioavailability: Immediate release, 65%; extended release, 54-59%
Onset (antihypertensive response): Peak, 4-8 hr
Onset (BPH response): Initial, 2 wk; peak, 4-6 weeks
Duration: 24 hr
Peak plasma time: 2-3 hr
Distribution
Protein bound: 99%
Vd: 1-3.4 L/kg
Metabolism
Metabolized extensively in liver
Metabolites: 6- and 7-O-demethyl metabolites, 6'- and 7'-hydroxy metabolites, other minor
metabolites (activity unknown)
Elimination
Half-life: Immediate release, 22 hr; extended release, 15-19 hr
Dialyzable: HD, no
Total body clearance: 83-140 mL/min
Excretion: Feces (65%), urine (0.6-9%)
Patient Handout
560043
Patient Education
doxazosin oral
DOXAZOSIN EXTENDED-RELEASE TABLET - ORAL
(dox-AZE-oh-sin)
COMMON BRAND NAME(S): Cardura XL
USES:
Doxazosin is used in men to treat the symptoms of an enlarged prostate (benign prostatic
hyperplasia-BPH). It does not shrink the prostate, but it works by relaxing the muscles in the
prostate and part of the bladder. This helps to relieve symptoms of BPH such as difficulty in
beginning the flow of urine, weak stream, and the need to urinate frequently or urgently
(including during the middle of the night).
Doxazosin belongs to a class of drugs known as alpha blockers.
OTHER USES:
professional.
Doxazosin may also be used to help your body "pass," or get rid of, kidney stones through
HOW TO USE:
doxazosin and each time you get a refill. If you have any questions, ask your doctor or
pharmacist.
Take this medication by mouth as directed by your doctor, usually once daily with breakfast.
Doxazosin may cause a sudden drop in your blood pressure, which could lead to dizziness or
fainting, usually within a few hours after you take it. This risk is higher after the first dose, after
your doctor increases your dose, or if you restart treatment after you stop taking it. During these
times, avoid situations where you may be injured if you faint.
Do not crush or chew extended-release tablets. Doing so can release all of the drug at once,
increasing the risk of side effects. Also, do not split the tablets unless they have a score line and
your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing
or chewing.
the same time each day. If you miss taking doxazosin for a few days, you may need to restart
treatment at a lower dose and gradually increase your dose again. Consult your doctor for more
details.
If you are switching from another form of doxazosin to this extended-release form, be sure to
follow your doctor's instructions closely.
SIDE EFFECTS:
Dizziness, lightheadedness, or drowsiness may occur. If any of these effects persist or worsen,
tell your doctor or pharmacist promptly.
lying position.
An empty tablet shell may appear in your stool. This effect is harmless because your body has
already absorbed the medication.
Tell your doctor right away if you have any serious side effects, including: fainting, shortness of
breath, weakness, yellowing eyes/skin, dark urine, easy bleeding/bruising, fever, persistent sore
throat.
Get medical help right away if you have any very serious side effects, including: vision changes,
chest pain, jaw/left arm pain, weakness on one side of the body, slurred speech, confusion.
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking doxazosin, tell your doctor or pharmacist if you are allergic to it; or to other alpha
blockers such as prazosin or terazosin; or if you have any other allergies. This product may
stomach/intestine problems (such as short bowel syndrome, chronic constipation, narrow gut,
slow gut movement), heart disease (such as congestive heart failure, angina, heart attack in last 6
months), liver disease, low blood pressure.
beverages. See also How to Use section.
Before having surgery (including cataract eye surgery), tell your doctor or dentist about all the
products you use (including prescription drugs, nonprescription drugs, and herbal products).
Older adults may be more sensitive to the side effects of this drug, especially dizziness and low
blood pressure. These side effects can increase the risk of falling.
feeding.
DRUG INTERACTIONS:
If you are also taking a drug to treat erectile dysfunction-ED or pulmonary hypertension (such as
sildenafil, tadalafil), your blood pressure may get too low which can lead to dizziness or fainting.
Your doctor may need to adjust your medications to minimize this risk.
Other medications can affect the removal of doxazosin from your body, which may affect how
doxazosin works. Examples include azole antifungals (such as itraconazole, ketoconazole),
boceprevir, macrolide antibiotics (such as clarithromycin), HIV protease inhibitors (such as
lopinavir, ritonavir), among others.
OVERDOSE:
NOTES:
Laboratory and/or medical tests (such as prostate exams, blood pressure) should be performed
details.
MISSED DOSE:
the missed dose and resume your usual dosing schedule. Do not double the dose to catch up. See
also How to Use section.
STORAGE:
Information last revised January 2014. Copyright(c) 2014 First Databank, Inc.

Tamsulosin (Flomax)

Tamsulosin is indicated for the treatment of the signs and symptoms of BPH. It is an alpha-
adrenergic blocker specifically targeted to alpha-1 receptors. Tamsulosin has the advantage of
producing relatively less orthostatic hypotension; it requires no gradual up-titration from the
initial dosage. It inhibits postsynaptic alpha-adrenergic receptors, resulting in vasodilation of
veins and arterioles and a decrease in total peripheral resistance and blood pressure. It improves
irritative and obstructive voiding symptoms.
Dosing & Uses
AdultPediatric
Benign Prostatic Hypertrophy
0.4 mg PO once daily, 30 minutes after same meal each day; if response is inadequate after 2-4
weeks, may be increased to 0.8 mg once daily; if therapy is interrupted, should be resumed at 0.4
mg once daily
Bladder Outlet Obstruction
Relief of symptoms
0.4 mg PO once daily
Ureteral Stones
Facilitation of stone expulsion
0.4 mg PO once daily; discontinued after successful expulsion (average, 1-2 weeks)
Renal impairment
CrCl 10 mL/min: Dosage adjustment not necessary
CrCl <10 mL/min: Not studied
Hepatic impairment
Mild to moderate: Dosage adjustment not necessary
Severe: Not studied
Drug Interactions
Interaction Checker
tamsulosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (1)
boceprevir
boceprevir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
alfuzosin
atazanavir
atazanavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
alternatives if available. Potential for increased toxicity. .
clarithromycin
clarithromycin increases levels of tamsulosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Possible serious or life-threatening interaction. Monitor closely.
Use alternatives if available.
conivaptan
conivaptan increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
alternatives if available.
darunavir
darunavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
delavirdine
delavirdine increases levels of tamsulosin by affecting hepatic/intestinal enzyme
doxazosin
fosamprenavir
fosamprenavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme
idelalisib
idelalisib will increase the level or effect of tamsulosin by affecting hepatic/intestinal
closely. Use alternatives if available. Idelalisib is a strong CYP3A inhibitor; avoid
coadministration with sensitive CYP3A substrates
imatinib
imatinib increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
indinavir
indinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
isoniazid
isoniazid increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
itraconazole
itraconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
ketoconazole
ketoconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
Use alternatives if available. Potential for increased toxicity.
lopinavir
lopinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
alternatives if available. Potential for increased toxicity.
nefazodone
nefazodone increases levels of tamsulosin by affecting hepatic/intestinal enzyme
nelfinavir
nelfinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
nicardipine
nicardipine increases levels of tamsulosin by affecting hepatic/intestinal enzyme
phenoxybenzamine
phentolamine
phentolamine, tamsulosin. Either increases effects of the other by additive vasodilation.
posaconazole
posaconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
prazosin
quinidine
quinidine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
ritonavir
ritonavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
saquinavir
saquinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
silodosin
silodosin, tamsulosin. Either increases effects of the other by additive vasodilation.
telaprevir
telaprevir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
telithromycin
telithromycin increases levels of tamsulosin by affecting hepatic/intestinal enzyme
terazosin
tipranavir
tipranavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
voriconazole
voriconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
abiraterone
abiraterone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
metabolism. Significant interaction possible, monitor closely. Avoid coadministration of
abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise
caution and consider a dose reduction of the CYP2D6 substrate.
amiodarone
amiodarone increases levels of tamsulosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Potential for interaction, monitor. Dose reduction may be neeed for

amiodarone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
metabolism. Potential for interaction, monitor.
aprepitant
aprepitant increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
avanafil
avanafil, tamsulosin. Either increases effects of the other by additive vasodilation.
bicalutamide
bicalutamide increases levels of tamsulosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Potential for interaction, monitor. Dose reduction may be needed
for coadministered drugs that are predominantly metabolized by CYP3A.
bortezomib
bortezomib increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
bupropion
bupropion increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
chloroquine
chloroquine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
chlorpromazine
chlorpromazine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
cimetidine
cimetidine increases levels of tamsulosin by decreasing renal clearance. Significant
interaction possible, monitor closely. Decreases tamsulosin clearance by 26% resulting in
increased AUC (44%).

cimetidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
cinacalcet
cinacalcet increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
clobazam
clobazam increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
clomipramine
clomipramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
clozapine
clozapine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4

clozapine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
cocaine
cocaine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism.
crizotinib
crizotinib increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
crofelemer
crofelemer increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
minimally absorbed.
cyclosporine
cyclosporine increases levels of tamsulosin by affecting hepatic/intestinal enzyme
dabrafenib
dabrafenib will decrease the level or effect of tamsulosin by affecting hepatic/intestinal
monitor closely.
darifenacin
darifenacin increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
delavirdine
delavirdine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
desipramine
desipramine increases levels of tamsulosin by affecting hepatic/intestinal enzyme

desipramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
dexmedetomidine
dexmedetomidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
diltiazem
diltiazem increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
diphenhydramine
diphenhydramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
disulfiram
disulfiram increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
doxycycline
doxycycline increases levels of tamsulosin by affecting hepatic/intestinal enzyme
dronedarone
dronedarone increases levels of tamsulosin by affecting hepatic/intestinal enzyme

dronedarone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
duloxetine
duloxetine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
efavirenz
efavirenz increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
elvitegravir/cobicistat/emtricitabine/tenofovir increases levels of tamsulosin by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. Potential for dangerous interaction. Use
with caution and monitor closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with
CYP3A4 substrates for which elevated plasma concentrations are associated with serious
and/or life-threatening events.

hepatic enzyme CYP2D6 metabolism. Potential for dangerous interaction. Use with
caution and monitor closely. Cobicistat is a CYP2D6 inhibitor; caution with CYP2D6
substrates for which elevated plasma concentrations are associated with serious and/or
life-threatening events.
erythromycin base
erythromycin base increases levels of tamsulosin by affecting hepatic/intestinal enzyme
erythromycin ethylsuccinate increases levels of tamsulosin by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Potential for interaction, monitor. Dose reduction may be
needed for coadministered drugs that are predominantly metabolized by CYP3A.
erythromycin lactobionate increases levels of tamsulosin by affecting hepatic/intestinal
erythromycin stearate increases levels of tamsulosin by affecting hepatic/intestinal
fluconazole
fluconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
fluoxetine
fluoxetine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
grapefruit
grapefruit increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
haloperidol
haloperidol increases levels of tamsulosin by affecting hepatic/intestinal enzyme

haloperidol increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
iloperidone
iloperidone increases levels of tamsulosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Potential for interaction, monitor. Iloperidone is a time-dependent
CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly
eliminated by CYP3A4.
imatinib
imatinib increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
imipramine
imipramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
isoniazid
isoniazid increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
ketoconazole
ketoconazole increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
lapatinib
lapatinib increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
lidocaine
lidocaine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4

lidocaine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
lopinavir
lopinavir increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
lorcaserin
lorcaserin increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
methadone
methadone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
methimazole
methimazole increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
metronidazole
metronidazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
mitotane
mitotane decreases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
nefazodone
nefazodone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
nicardipine
nicardipine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
norfloxacin
norfloxacin increases levels of tamsulosin by affecting hepatic/intestinal enzyme
paroxetine
paroxetine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
pyrimethamine
pyrimethamine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
quinidine
quinidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
quinine
quinine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism.
ranolazine
ranolazine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
ritonavir
ritonavir increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
sertraline
sertraline increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
sildenafil
sildenafil, tamsulosin. Either increases effects of the other by additive vasodilation.
tadalafil
tadalafil, tamsulosin. Either increases effects of the other by additive vasodilation.
terbinafine
terbinafine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
thioridazine
thioridazine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
ticlopidine
ticlopidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
tranylcypromine
tranylcypromine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
trazodone
trazodone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
vardenafil
vardenafil, tamsulosin. Either increases effects of the other by additive vasodilation.
warfarin
warfarin, tamsulosin. Other (see comment). Potential for interaction, monitor. Comment:
Manufacturer's prescribing information states limited in vitro and in vivo studies were
inconclusive; caution advised.
Minor (0)
Adverse Effects
>10%
Headache (19-21%)
Orthostatic hypotension (6-19%)
Rhinitis (13-18%)
Abnormal ejaculation (8-18%)
Dizziness (15-17%)
Arthralgia (11%)
Infection (9-11%)
1-10%
Asthenia (8%)
Back pain (7-8%)
Skin rash (7%)
Pharyngitis (5-6%)
Diarrhea (4-6%)
Myalgia (5%)
Chest pain (4%)
Cough (3-4%)
Somnolence (3-4%)
Nausea (2-4%)
Sinusitis (2-4%)
Abdominal discomfort (2-3%)
Bitter taste (2-3%)
Decreased libido (1-2%)
Insomnia (1-2%)
Priapism (rare)
Signs and symptoms of orthostasis, including syncope
Infrequent reports of dyspnea, palpitations, hypotension, atrial fibrillation, arrhythmia,
tachycardia, skin desquamation (including Stevens-Johnson syndrome), constipation, vomiting
Allergic-type reactions (eg, skin rash, urticaria, pruritus, angioedema, respiratory symptoms)
have been reported with positive rechallenge
Contraindications
Hypersensitivity
Cautions
Use with caution in coronary artery disease, liver disease, general anesthesia
Orthostatic hypotension may occur
Priapism
Prostatic cancer should be ruled out before therapy is initiated
May cause syncope (first-dose effect)
Discontinue if angina symptoms occur or worsen
Intraoperative floppy iris syndrome has been reported in patients receiving alpha1 blockers at
time of cataract surgery; association is unclear
Pharmacology
Mechanism of Action
Blocks alpha1a adrenergic receptor in smooth muscle of prostate, decreasing bladder neck and
urethral resistance
Absorption
Bioavailability: Fasting, 30%
Onset: 4-8 hr
Peak plasma time: With food, 6-7 hr; fasting, 4-5 hr
Distribution
Protein bound: 90%
Vd: 0.2 L/kg or 16 L
Metabolism
Metabolized in liver
Metabolites: Glucuronide and sulfate conjugates (inactive)
Elimination
Half-life: 14-15 hr
Excretion: Urine (76%), feces (21%)
Patient Handout
560043
Patient Education
tamsulosin oral
TAMSULOSIN CAPSULE - ORAL
(tam-sull-OH-sin)
COMMON BRAND NAME(S): Flomax
USES:
This medication is used in men to treat the symptoms of an enlarged prostate (benign prostatic
hyperplasia-BPH). Tamsulosin is known as an alpha-blocker and works by relaxing muscles in
the bladder and prostate. Relaxing these muscles helps to relieve symptoms of BPH such as
difficulty in beginning the flow of urine, weak stream, and the need to urinate frequently or
urgently (including during the middle of the night).
OTHER USES:
professional.
Tamsulosin may also be used to help your body "pass," or get rid of, kidney stones through
HOW TO USE:
this medication and each time you get a refill. If you have any questions, ask your doctor or
pharmacist.
Take this medication by mouth as directed by your doctor, usually once daily, 30 minutes after
the same meal each day. Swallow this medication whole. Do not crush, chew, or open the
capsules.
Use this medication regularly to get the most benefit from it. To help you remember, take it at
the same time each day.
If you have not taken this drug for several days, contact your doctor to see if you need to be
restarted at a lower dose.
It may take up to 4 weeks to notice an improvement in symptoms. Tell your doctor if your
symptoms do not improve after 4 weeks or if they worsen.
SIDE EFFECTS:
Dizziness, lightheadedness, drowsiness, runny/stuffy nose, or ejaculation problems may occur. If
any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Tell your doctor immediately if this rare but serious side effect occurs: fainting.
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking tamsulosin, tell your doctor or pharmacist if you are allergic to it; or if you have
any other allergies. This product may contain inactive ingredients, which can cause allergic
reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history.
beverages.
To reduce the risk of dizziness, lightheadedness, or fainting, get up slowly when rising from a
sitting or lying position, especially when you first start taking this drug or if your doctor changes
your dose. If dizziness occurs, sit or lie down until you feel better. Also, when you first start
taking this drug, avoid situations where you may be injured if you faint.
taking this medication and about all the products you use (including prescription drugs,
nonprescription drugs, and herbal products).
During pregnancy, this medication should be used only when clearly needed. Before using
tamsulosin, talk with your doctor about the risks and benefits.
It is unknown if tamsulosin passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS:
Some products that may interact with this drug include: other alpha-blockers (such as prazosin,
terazosin), drugs to treat erectile dysfunction-ED or pulmonary hypertension (such as sildenafil,
tadalafil, vardenafil).
Other medications can affect the removal of this product from your body, which may affect how
this product works. Examples include azole antifungals (such as ketoconazole), boceprevir,
macrolide antibiotics (such as clarithromycin), nefazodone, HIV protease inhibitors (such as
lopinavir, ritonavir), a certain combination HIV medication
(elvitegravir/cobicistat/emtricitabine/tenofovir), telithromycin, among others.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness including
alcohol, antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as
alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as
codeine).
Check the labels on all your medicines (such as allergy or cough-and-cold products) because
they may contain ingredients that cause drowsiness. Ask your pharmacist about using those
products safely.
OVERDOSE:
NOTES:
Laboratory and/or medical tests (such as prostate exams, prostate-specific antigen-PSA) should
for more details.
MISSED DOSE:
STORAGE:

Silodosin (Rapaflo)

Silodosin is indicated for the treatment of the signs and symptoms of BPH. Silodosin selectively
antagonizes postsynaptic alpha1-adrenergic receptors in the prostate, bladder base, prostatic
capsule, and prostatic urethra. This action induces smooth muscle relaxation and improves urine
flow.

Dosing & Uses
AdultPediatric
8 mg PO qDay
Administration: Take with meal
Renal Impairment
CrCl <50 mL/min: Dose adjustment not necessary
CrCl 30-50 mL/min: 4 mg PO qDay
CrCl <30 mL/min: Contraindicated
Hepatic Impairment
Mild-to-moderate impairment (Child-Pugh class A or B): Dose adjustment not necessary
Severe Impairment: (Child-Pugh class C): Contraindicated (not studied)
Drug Interactions
Interaction Checker
silodosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (1)
boceprevir
boceprevir increases levels of silodosin by affecting hepatic/intestinal enzyme CYP3A4
amobarbital
amobarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
aprepitant
aprepitant will increase the level or effect of silodosin by affecting hepatic/intestinal
Contraindicated unless benefits outweigh risks and no alternatives available. Never use
combination.
armodafinil
armodafinil will decrease the level or effect of silodosin by affecting hepatic/intestinal
artemether/lumefantrine will decrease the level or effect of silodosin by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. High likelihood serious or life-
threatening interaction. Contraindicated unless benefits outweigh risks and no alternatives
available. Never use combination.
atazanavir
atazanavir will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
bosentan
bosentan will decrease the level or effect of silodosin by affecting hepatic/intestinal
budesonide
budesonide will decrease the level or effect of silodosin by affecting hepatic/intestinal
butabarbital
butabarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
butalbital
butalbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
carbamazepine
carbamazepine will decrease the level or effect of silodosin by affecting hepatic/intestinal
cimetidine
cimetidine will increase the level or effect of silodosin by affecting hepatic/intestinal
clarithromycin
clarithromycin will increase the level or effect of silodosin by affecting hepatic/intestinal
clobetasone
clobetasone will decrease the level or effect of silodosin by affecting hepatic/intestinal
conivaptan
conivaptan will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
cortisone
cortisone will decrease the level or effect of silodosin by affecting hepatic/intestinal
cyclosporine
cyclosporine will increase the level or effect of silodosin by affecting hepatic/intestinal
darifenacin
darifenacin will increase the level or effect of silodosin by affecting hepatic/intestinal
darunavir
darunavir will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
dasatinib
dasatinib will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
deflazacort
deflazacort will decrease the level or effect of silodosin by affecting hepatic/intestinal
delavirdine
delavirdine will increase the level or effect of silodosin by affecting hepatic/intestinal
dexamethasone
dexamethasone will decrease the level or effect of silodosin by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. Possible serious or life-threatening
dhea
dhea will increase the level or effect of silodosin by affecting hepatic/intestinal enzyme
diltiazem
diltiazem will increase the level or effect of silodosin by affecting hepatic/intestinal
dronedarone
dronedarone will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
efavirenz
efavirenz will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
erythromycin base
erythromycin base will increase the level or effect of silodosin by affecting
available.
erythromycin ethylsuccinate will increase the level or effect of silodosin by affecting
available.
erythromycin lactobionate will increase the level or effect of silodosin by affecting
available.
erythromycin stearate will increase the level or effect of silodosin by affecting
available.
eslicarbazepine acetate will decrease the level or effect of silodosin by affecting
ethotoin
ethotoin will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
etravirine
etravirine will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
eucalyptus
eucalyptus will decrease the level or effect of silodosin by affecting hepatic/intestinal
fluconazole
fluconazole will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
fludrocortisone
fludrocortisone will decrease the level or effect of silodosin by affecting hepatic/intestinal
fosamprenavir
fosamprenavir will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
fosphenytoin
fosphenytoin will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
grapefruit
grapefruit will increase the level or effect of silodosin by affecting hepatic/intestinal
griseofulvin
griseofulvin will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
hexobarbital
hexobarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
hydrocortisone
hydrocortisone will decrease the level or effect of silodosin by affecting hepatic/intestinal
indinavir
indinavir will increase the level or effect of silodosin by affecting hepatic/intestinal
isoniazid
isoniazid will increase the level or effect of silodosin by affecting hepatic/intestinal
itraconazole
itraconazole will increase the level or effect of silodosin by affecting hepatic/intestinal
ivacaftor
ivacaftor increases levels of silodosin by P-glycoprotein (MDR1) efflux transporter.
available. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp, may
significantly increase systemic exposure to P-gp substrates.
ketoconazole
ketoconazole will increase the level or effect of silodosin by affecting hepatic/intestinal
lapatinib
lapatinib will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
lumefantrine
lumefantrine will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
marijuana
marijuana will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
mefloquine
mefloquine increases levels of silodosin by P-glycoprotein (MDR1) efflux transporter.
available.
mephobarbital
mephobarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
methylprednisolone
methylprednisolone will decrease the level or effect of silodosin by affecting
metronidazole
metronidazole will increase the level or effect of silodosin by affecting hepatic/intestinal
mibefradil
mibefradil will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
miconazole vaginal
miconazole vaginal will increase the level or effect of silodosin by affecting
available. Never use combination.
modafinil
modafinil will decrease the level or effect of silodosin by affecting hepatic/intestinal
nafcillin
nafcillin will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
nefazodone
nefazodone will increase the level or effect of silodosin by affecting hepatic/intestinal
nelfinavir
nelfinavir will increase the level or effect of silodosin by affecting hepatic/intestinal
nevirapine
nevirapine will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
nifedipine
nifedipine will increase the level or effect of silodosin by affecting hepatic/intestinal
nilotinib
nilotinib will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
oxcarbazepine
oxcarbazepine will decrease the level or effect of silodosin by affecting hepatic/intestinal
oxiconazole
oxiconazole will increase the level or effect of silodosin by affecting hepatic/intestinal
pentobarbital
pentobarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
phenobarbital
phenobarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
phenytoin
phenytoin will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
posaconazole
posaconazole will increase the level or effect of silodosin by affecting hepatic/intestinal
prednisolone
prednisolone will decrease the level or effect of silodosin by affecting hepatic/intestinal
prednisone
prednisone will decrease the level or effect of silodosin by affecting hepatic/intestinal
primidone
primidone will decrease the level or effect of silodosin by affecting hepatic/intestinal
quinidine
quinidine will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
transporter. Possible serious or life-threatening interaction. Monitor closely. Use
quinupristin/dalfopristin will increase the level or effect of silodosin by affecting
rifabutin
rifabutin will decrease the level or effect of silodosin by affecting hepatic/intestinal
rifampin
rifampin will decrease the level or effect of silodosin by affecting hepatic/intestinal
rifapentine
rifapentine will decrease the level or effect of silodosin by affecting hepatic/intestinal
combination.
ritonavir
ritonavir will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
rufinamide
rufinamide will decrease the level or effect of silodosin by affecting hepatic/intestinal
secobarbital
secobarbital will decrease the level or effect of silodosin by affecting hepatic/intestinal
sildenafil
sildenafil increases effects of silodosin by pharmacodynamic synergism. Possible serious
sitaxentan
sitaxentan will increase the level or effect of silodosin by affecting hepatic/intestinal
st john's wort
st john's wort will decrease the level or effect of silodosin by affecting hepatic/intestinal
tamsulosin
telithromycin
telithromycin will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
topiramate
topiramate will decrease the level or effect of silodosin by affecting hepatic/intestinal
triamcinolone
triamcinolone will decrease the level or effect of silodosin by affecting hepatic/intestinal
troglitazone
troglitazone will decrease the level or effect of silodosin by affecting hepatic/intestinal
troleandomycin
troleandomycin will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
vardenafil
vardenafil increases effects of silodosin by pharmacodynamic synergism. High likelihood
verapamil
verapamil will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
voriconazole
voriconazole will increase the level or effect of silodosin by affecting hepatic/intestinal
combination.
yohimbe
yohimbe increases effects of silodosin by pharmacodynamic synergism. High likelihood
zafirlukast
zafirlukast will increase the level or effect of silodosin by affecting hepatic/intestinal
acebutolol
silodosin and acebutolol both increase anti-hypertensive channel blocking. Potential for
dangerous interaction. Use with caution and monitor closely. Increased risk of dizziness
and orthostatic hypotension when silodosin is administered concurrently with
antihypertensives.
aceclofenac
aceclofenac decreases effects of silodosin by pharmacodynamic antagonism. Significant
acemetacin
acemetacin decreases effects of silodosin by pharmacodynamic antagonism. Significant
aldesleukin
aldesleukin increases effects of silodosin by pharmacodynamic synergism. Potential for
alfuzosin
alfuzosin and silodosin both increase anti-hypertensive channel blocking. Potential for
amifostine
amifostine increases effects of silodosin by pharmacodynamic synergism. Potential for
amiodarone
amiodarone will increase the level or effect of silodosin by P-glycoprotein (MDR1)
efflux transporter. Significant interaction possible, monitor closely.
amlodipine
silodosin and amlodipine both increase anti-hypertensive channel blocking. Potential for
asenapine
asenapine and silodosin both increase anti-hypertensive channel blocking. Potential for
aspirin
aspirin decreases effects of silodosin by pharmacodynamic antagonism. Significant
aspirin rectal
aspirin rectal decreases effects of silodosin by pharmacodynamic antagonism. Significant
aspirin/citric acid/sodium bicarbonate decreases effects of silodosin by pharmacodynamic
atenolol
silodosin and atenolol both increase anti-hypertensive channel blocking. Potential for
atorvastatin
atorvastatin will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
transporter. Significant interaction possible, monitor closely.
avanafil
avanafil increases effects of silodosin by pharmacodynamic synergism. Significant
benazepril
benazepril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
betaxolol
silodosin and betaxolol both increase anti-hypertensive channel blocking. Potential for
bisoprolol
silodosin and bisoprolol both increase anti-hypertensive channel blocking. Potential for
captopril
captopril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
carbidopa
carbidopa increases effects of silodosin by pharmacodynamic synergism. Potential for
interaction, monitor. Monitor for hypotension.
carvedilol
silodosin and carvedilol both increase anti-hypertensive channel blocking. Potential for
celecoxib
celecoxib decreases effects of silodosin by pharmacodynamic antagonism. Significant
celiprolol
silodosin and celiprolol both increase anti-hypertensive channel blocking. Potential for
choline magnesium trisalicylate decreases effects of silodosin by pharmacodynamic
clarithromycin
clarithromycin will increase the level or effect of silodosin by P-glycoprotein (MDR1)
clevidipine
silodosin and clevidipine both increase anti-hypertensive channel blocking. Potential for
clotrimazole
clotrimazole will decrease the level or effect of silodosin by P-glycoprotein (MDR1)
crizotinib
crizotinib increases levels of silodosin by affecting hepatic/intestinal enzyme CYP3A4

crizotinib increases levels of silodosin by P-glycoprotein (MDR1) efflux transporter.
cyclosporine
cyclosporine will increase the level or effect of silodosin by P-glycoprotein (MDR1)
deferasirox
deferasirox will decrease the level or effect of silodosin by affecting hepatic/intestinal
diclofenac
diclofenac decreases effects of silodosin by pharmacodynamic antagonism. Significant
diflunisal
diflunisal decreases effects of silodosin by pharmacodynamic antagonism. Significant
diltiazem
diltiazem will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux

silodosin and diltiazem both increase anti-hypertensive channel blocking. Potential for
doxazosin
doxazosin and silodosin both increase anti-hypertensive channel blocking. Potential for
dronedarone
dronedarone will increase the level or effect of silodosin by P-glycoprotein (MDR1)
enalapril
enalapril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
erythromycin base
erythromycin base will increase the level or effect of silodosin by P-glycoprotein
(MDR1) efflux transporter. Significant interaction possible, monitor closely.
erythromycin ethylsuccinate will increase the level or effect of silodosin by P-
glycoprotein (MDR1) efflux transporter. Significant interaction possible, monitor closely.
erythromycin lactobionate will increase the level or effect of silodosin by P-glycoprotein
erythromycin stearate will increase the level or effect of silodosin by P-glycoprotein
esmolol
silodosin and esmolol both increase anti-hypertensive channel blocking. Potential for
antihypertensives.
ethotoin
ethotoin will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
etodolac
etodolac decreases effects of silodosin by pharmacodynamic antagonism. Significant
etoricoxib
etoricoxib decreases effects of silodosin by pharmacodynamic antagonism. Significant
felodipine
felodipine will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux

silodosin and felodipine both increase anti-hypertensive channel blocking. Potential for
fenbufen
fenbufen decreases effects of silodosin by pharmacodynamic antagonism. Significant
fenoprofen
fenoprofen decreases effects of silodosin by pharmacodynamic antagonism. Significant
flurbiprofen
flurbiprofen decreases effects of silodosin by pharmacodynamic antagonism. Significant
fluvoxamine
fluvoxamine will increase the level or effect of silodosin by affecting hepatic/intestinal
fosinopril
fosinopril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
fosphenytoin
fosphenytoin will decrease the level or effect of silodosin by P-glycoprotein (MDR1)
ibuprofen
ibuprofen decreases effects of silodosin by pharmacodynamic antagonism. Significant
iloperidone
iloperidone increases effects of silodosin by pharmacodynamic synergism. Significant
imidapril
imidapril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
indinavir
indinavir will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
indomethacin
indomethacin decreases effects of silodosin by pharmacodynamic antagonism.
synthesis.
isradipine
silodosin and isradipine both increase anti-hypertensive channel blocking. Potential for
itraconazole
itraconazole will increase the level or effect of silodosin by P-glycoprotein (MDR1)
ketoconazole
ketoconazole will increase the level or effect of silodosin by P-glycoprotein (MDR1)
ketoprofen
ketoprofen decreases effects of silodosin by pharmacodynamic antagonism. Significant
ketorolac
ketorolac decreases effects of silodosin by pharmacodynamic antagonism. Significant
ketorolac intranasal decreases effects of silodosin by pharmacodynamic antagonism.
synthesis.
labetalol
silodosin and labetalol both increase anti-hypertensive channel blocking. Potential for
lacidipine
silodosin and lacidipine both increase anti-hypertensive channel blocking. Potential for
lapatinib
lapatinib will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
lercanidipine
silodosin and lercanidipine both increase anti-hypertensive channel blocking. Potential
lisinopril
lisinopril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
loratadine
loratadine will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
lornoxicam
lornoxicam decreases effects of silodosin by pharmacodynamic antagonism. Significant
lovastatin
lovastatin will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
lurasidone
lurasidone increases effects of silodosin by Other (see comment). Potential for
needed.
maraviroc
maraviroc, silodosin. Either increases effects of the other by pharmacodynamic
hypotension.
mefenamic acid
mefenamic acid decreases effects of silodosin by pharmacodynamic antagonism.
synthesis.
meloxicam
meloxicam decreases effects of silodosin by pharmacodynamic antagonism. Significant
metoprolol
silodosin and metoprolol both increase anti-hypertensive channel blocking. Potential for
midazolam
midazolam will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
moexipril
moexipril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
moxisylyte
moxisylyte and silodosin both increase anti-hypertensive channel blocking. Potential for
nabumetone
nabumetone decreases effects of silodosin by pharmacodynamic antagonism. Significant
nadolol
silodosin and nadolol both increase anti-hypertensive channel blocking. Potential for
naproxen
naproxen decreases effects of silodosin by pharmacodynamic antagonism. Significant
nebivolol
silodosin and nebivolol both increase anti-hypertensive channel blocking. Potential for
nefazodone
nefazodone will decrease the level or effect of silodosin by P-glycoprotein (MDR1)
nicardipine
nicardipine will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux

silodosin and nicardipine both increase anti-hypertensive channel blocking. Potential for
nifedipine
nifedipine will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux

silodosin and nifedipine both increase anti-hypertensive channel blocking. Potential for
nilotinib
nilotinib will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
nisoldipine
silodosin and nisoldipine both increase anti-hypertensive channel blocking. Potential for
nitroglycerin rectal, silodosin. Either increases effects of the other by pharmacodynamic
oxaprozin
oxaprozin decreases effects of silodosin by pharmacodynamic antagonism. Significant
parecoxib
parecoxib decreases effects of silodosin by pharmacodynamic antagonism. Significant
penbutolol
silodosin and penbutolol both increase anti-hypertensive channel blocking. Potential for
perindopril
perindopril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
phenobarbital
phenobarbital will decrease the level or effect of silodosin by P-glycoprotein (MDR1)
phenoxybenzamine
phenoxybenzamine and silodosin both increase anti-hypertensive channel blocking.
phentolamine
phentolamine and silodosin both increase anti-hypertensive channel blocking. Potential
phenytoin
phenytoin will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
pindolol
silodosin and pindolol both increase anti-hypertensive channel blocking. Potential for
piroxicam
piroxicam decreases effects of silodosin by pharmacodynamic antagonism. Significant
ponatinib
ponatinib increases levels of silodosin by P-glycoprotein (MDR1) efflux transporter.
prazosin
prazosin and silodosin both increase anti-hypertensive channel blocking. Potential for
propranolol
silodosin and propranolol both increase anti-hypertensive channel blocking. Potential for
antihypertensives.
quercetin
quercetin will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
quinapril
quinapril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
ramipril
ramipril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
ranolazine
ranolazine will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
reserpine
reserpine will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
rifampin
rifampin will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
ritonavir
ritonavir will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
salicylates (non-asa) decreases effects of silodosin by pharmacodynamic antagonism.
synthesis.
salsalate
salsalate decreases effects of silodosin by pharmacodynamic antagonism. Significant
saquinavir
saquinavir increases levels of silodosin by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Potential for dangerous interaction. Use with caution and monitor closely.
Potential for increased toxicity. Use alternatives if available.
simvastatin
simvastatin will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
sirolimus
sirolimus will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
sotalol
silodosin and sotalol both increase anti-hypertensive channel blocking. Potential for
antihypertensives.
spironolactone
spironolactone will increase the level or effect of silodosin by P-glycoprotein (MDR1)
st john's wort
st john's wort will decrease the level or effect of silodosin by P-glycoprotein (MDR1)
sulfasalazine
sulfasalazine decreases effects of silodosin by pharmacodynamic antagonism. Significant
sulindac
sulindac decreases effects of silodosin by pharmacodynamic antagonism. Significant
tacrolimus
tacrolimus will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
tadalafil
tadalafil increases effects of silodosin by pharmacodynamic synergism. Significant
terazosin
silodosin and terazosin both increase anti-hypertensive channel blocking. Potential for
timolol
silodosin and timolol both increase anti-hypertensive channel blocking. Potential for
tipranavir
tipranavir increases levels of silodosin by affecting hepatic/intestinal enzyme CYP3A4
Use alternatives if available. Potential for increased toxicity. .
tolfenamic acid
tolfenamic acid decreases effects of silodosin by pharmacodynamic antagonism.
synthesis.
tolmetin
tolmetin decreases effects of silodosin by pharmacodynamic antagonism. Significant
tolvaptan
tolvaptan will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux
trandolapril
trandolapril, silodosin. Mechanism: pharmacodynamic synergism. Significant interaction
trazodone
trazodone will decrease the level or effect of silodosin by P-glycoprotein (MDR1) efflux
vemurafenib
vemurafenib increases levels of silodosin by P-glycoprotein (MDR1) efflux transporter.
verapamil
verapamil will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux

silodosin and verapamil both increase anti-hypertensive channel blocking. Potential for
zotepine
silodosin and zotepine both increase anti-hypertensive channel blocking. Potential for
Minor (8)
brimonidine
brimonidine increases effects of silodosin by pharmacodynamic synergism. Minor or
butcher's broom
silodosin, butcher's broom. Either decreases effects of the other by Mechanism:
ethanol
silodosin, ethanol. Mechanism: pharmacodynamic synergism. Minor or non-significant
lofexidine
silodosin, lofexidine. Either decreases effects of the other by Mechanism:
phenylephrine
silodosin, phenylephrine. Either decreases effects of the other by Mechanism:
phenylephrine po
silodosin, phenylephrine po. Either decreases effects of the other by Mechanism:
tizanidine
tizanidine increases effects of silodosin by pharmacodynamic synergism. Minor or non-
treprostinil
treprostinil increases effects of silodosin by pharmacodynamic synergism. Minor or non-
Adverse Effects
>10%
Retrograde ejaculation (28%)
1-10%
Diarrhea (3%)
Headache (2%)
Insomnia ((1-2%)
Dizziness (3%)
Orthostatic hypotension (3%; increased in patients >65 years)
Nasopharyngitis (2%)
Nasal congestion (2%)
Sinusitis (1-2%)
Skin and subcutaneous tissue disorders: Toxic skin eruption, purpura, skin rash, pruritus,
urticaria
Hepatobiliary disorders: Jaundice, impaired hepatic function associated with increased
transaminase values
Immune system disorders: Allergic-type reactions, not limited to skin reactions including
angioedema
Genitourinary system: Priapism
Contraindications
Hypersensitivity
Severe renal impairment (CrCl <30 mL/min)
Severe hepatic impairment (Child-Pugh Score >10)
Concomitant strong CYP3A4 inhibitors or P-glycoprotein inhibitors
Cautions
Renal impairment, cataract surgery (potential risk of Intraoperative Floppy Iris Syndrome)
Rule out prostate cancer prior to treatment
Risk of orthostatic hypotension with or without syncope with first dose
Additive blood pressure lowering effects and symptomatic hypotension can result from
concomitant administration of PDE-5 inhibitor (eg, sildenafil, tadalafil, vardenafil)
Use with caution in patients with mid-to-moderate hepatic impairment
Use with caution in the elderly (risk of hypotension)
Not indicated for use in women or children
Not for use as hypertensive
Pharmacology
Mechanism of Action
Selective antagonist of postsynaptic alpha-1-adrenoceptors; blocking the alpha1A-
adrenoreceptors in the smooth muscle of the prostate leads to relaxation of the smooth muscle in
the bladder neck and prostate causing an improvement of urine flow and decreased symptom of
BPH.
Pharmacokinetics
Time: 2.6 +/- 0.9 hr
Concentration: (8mg dose) 62 ng/mL
Half-Life: 13 +/- 8 hr
Protein Bound: 97%
Vd: 49.5 L
Clearance: 10 L/hr
Metabolism: glucuronidation, alcohol & aldehyde dehydrogenase, CYP3A4
Excretion: feces & urine
Patient Handout
560043
Patient Education
silodosin oral
SILODOSIN - ORAL
(SIL-oh-DOE-sin)
COMMON BRAND NAME(S): Rapaflo
USES:
This medication is used to treat the symptoms of a prostate gland condition called BPH (benign
prostatic hyperplasia, also known as an enlarged prostate). Silodosin is an alpha-blocker that
works by relaxing the muscles in the bladder neck and prostate. Relaxing these muscles leads to
relief of symptoms of BPH such as the feeling of needing to urinate frequently or urgently, weak
stream, difficulty in beginning the flow of urine, and the need to urinate during the middle of the
night. Silodosin does not shrink the prostate.
OTHER USES:
professional.
Silodosin may also be used to help your body "pass," or get rid of, kidney stones through
urination.
HOW TO USE:
Take this medication by mouth, usually once a day with a meal, or as directed by your doctor.
Ask your doctor if you should take the first dose at bedtime to minimize the chances of getting
dizzy or fainting. After the first dose, take your regularly scheduled dose with the same meal
each day, or take exactly as directed by your doctor.
If you have difficulty swallowing this medication whole, you may sprinkle the entire contents of
a capsule on a small amount (such as a tablespoon) of applesauce just before taking. Swallow the
mixture immediately. Do not chew the mixture, and do not save it for future use. Do not use hot
applesauce. Drink a glass of cool water after each dose.
take it at the same time each day.
Inform your doctor if your symptoms do not improve or if they worsen.
SIDE EFFECTS:
Dizziness or problems ejaculating may occur. If any of these effects persist or worsen, tell your
doctor or pharmacist promptly.
Tell your doctor immediately if any of these rare but serious side effects occur: fainting, vision
changes.
In the unlikely event you have a painful or prolonged erection lasting 4 or more hours, stop using
this drug and seek immediate medical attention, or permanent problems could occur.
if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking silodosin, tell your doctor or pharmacist if you are allergic to it; or if you have any
other allergies. This product may contain inactive ingredients, which can cause allergic reactions
or other problems. Talk to your pharmacist for more details.
kidney disease, liver disease, low blood pressure/fainting.
To avoid dizziness or fainting, get up slowly from a lying or seated position, especially when you
first start taking this drug or if your doctor changes your dosing. Also, when you first start taking
this drug, avoid situations where you may be injured if you faint.
Before having cataract surgery, tell your doctor that you are taking this medication of if you have
ever taken it. Before having any surgery, tell your doctor or dentist that you are taking this
medication.
Caution is advised when using this drug in the elderly because they may be more sensitive to the
effects of this drug, especially dizziness.
During pregnancy, silodosin should be used only when clearly needed. Discuss the risks and
feeding.
DRUG INTERACTIONS:
Some products that may interact with this drug include: other alpha-blocker drugs (such as
doxazosin, prazosin), drugs for high blood pressure, drugs to treat erectile dysfunction-ED or
pulmonary hypertension (such as sildenafil, tadalafil).
Other medications can affect the removal of silodosin from your body, which may affect how
silodosin works. Examples include azole antifungals (such as itraconazole, ketoconazole),
boceprevir, cyclosporine, macrolide antibiotics (such as clarithromycin), HIV protease inhibitors
(such as lopinavir, ritonavir), a certain combination HIV medication
(elvitegravir/cobicistat/emtricitabine/tenofovir), among others.
Check the labels on all your medicines (such as antihistamines including diphenhydramine)
because they may contain ingredients that cause dizziness or urinary problems. Ask your
pharmacist about the safe use of those products.
OVERDOSE:
provincial poison control center.
NOTES:
Keep all medical appointments. Laboratory and/or medical tests (such as blood pressure, prostate
exams including prostate-specific antigen or PSA) should be performed periodically to monitor
your progress or check for side effects. Consult your doctor for more details.
MISSED DOSE:
STORAGE:
Information last revised February 2014. Copyright(c) 2014 First Databank, Inc
5-Alpha-Reductase Inhibitors
Class Summary
These agents are used to treat symptomatic BPH in men with an enlarged prostate. They inhibit
the conversion of testosterone to DHT, causing DHT levels to drop, which, in turn, may decrease
prostate size.
[34, 31]

Finasteride (Proscar)

Finasteride is indicated for the treatment of symptomatic BPH in men with an enlarged prostate.
When combined with doxazosin, it can also reduce the risk of symptomatic progression of BPH.
Finasteride inhibits conversion of testosterone to DHT, causing serum DHT levels to decrease. It
is beneficial in men with prostates larger than 40 g and can improve symptoms and reduce
prostatic size by 20-30%. Reduction in prostate size is sustained for 5 years following treatment.
Finasteride improves urinary flow rate by 2 mL/s.
Dosing & Uses
AdultPediatric
Proscar: 5 mg PO qDay; assess response after 12 weeks to 6 months
Androgenic Alopecia (Men Only)
Propecia: 1 mg PO qDay for at least 3 months
Female Hirsutism (Off-label)
5 mg PO qDay
Renal impairment: Dose adjustment not necessary
Hepatic impairment: Caution in liver dysfunction; monitor
Drug Interactions
Interaction Checker
finasteride and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (0)
carbamazepine
carbamazepine will decrease the level or effect of finasteride by affecting
cimetidine
cimetidine will increase the level or effect of finasteride by affecting hepatic/intestinal
clarithromycin
clarithromycin will increase the level or effect of finasteride by affecting
erythromycin base
erythromycin base will increase the level or effect of finasteride by affecting
erythromycin ethylsuccinate will increase the level or effect of finasteride by affecting
erythromycin lactobionate will increase the level or effect of finasteride by affecting
erythromycin stearate will increase the level or effect of finasteride by affecting
isoniazid
isoniazid will increase the level or effect of finasteride by affecting hepatic/intestinal
itraconazole
itraconazole will increase the level or effect of finasteride by affecting hepatic/intestinal
ketoconazole
ketoconazole will increase the level or effect of finasteride by affecting hepatic/intestinal
nefazodone
nefazodone will increase the level or effect of finasteride by affecting hepatic/intestinal
nevirapine
nevirapine will decrease the level or effect of finasteride by affecting hepatic/intestinal
rifabutin
rifabutin will decrease the level or effect of finasteride by affecting hepatic/intestinal
rifampin
rifampin will decrease the level or effect of finasteride by affecting hepatic/intestinal
st john's wort
st john's wort will decrease the level or effect of finasteride by affecting hepatic/intestinal
Minor (73)
amobarbital
amobarbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
aprepitant
aprepitant will increase the level or effect of finasteride by affecting hepatic/intestinal
armodafinil
armodafinil will decrease the level or effect of finasteride by affecting hepatic/intestinal
artemether/lumefantrine will decrease the level or effect of finasteride by affecting
atazanavir
atazanavir will increase the level or effect of finasteride by affecting hepatic/intestinal
bosentan
bosentan will decrease the level or effect of finasteride by affecting hepatic/intestinal
budesonide
budesonide will decrease the level or effect of finasteride by affecting hepatic/intestinal
butabarbital
butabarbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
butalbital
butalbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
clobetasone
clobetasone will decrease the level or effect of finasteride by affecting hepatic/intestinal
conivaptan
conivaptan will increase the level or effect of finasteride by affecting hepatic/intestinal
cortisone
cortisone will decrease the level or effect of finasteride by affecting hepatic/intestinal
cyclosporine
cyclosporine will increase the level or effect of finasteride by affecting hepatic/intestinal
darifenacin
darifenacin will increase the level or effect of finasteride by affecting hepatic/intestinal
darunavir
darunavir will increase the level or effect of finasteride by affecting hepatic/intestinal
dasatinib
dasatinib will increase the level or effect of finasteride by affecting hepatic/intestinal
deflazacort
deflazacort will decrease the level or effect of finasteride by affecting hepatic/intestinal
delavirdine
delavirdine will increase the level or effect of finasteride by affecting hepatic/intestinal
dexamethasone
dexamethasone will decrease the level or effect of finasteride by affecting
dhea
dhea will increase the level or effect of finasteride by affecting hepatic/intestinal enzyme
diltiazem
diltiazem will increase the level or effect of finasteride by affecting hepatic/intestinal
dronedarone
dronedarone will increase the level or effect of finasteride by affecting hepatic/intestinal
efavirenz
efavirenz will decrease the level or effect of finasteride by affecting hepatic/intestinal
eslicarbazepine acetate will decrease the level or effect of finasteride by affecting
ethotoin
ethotoin will decrease the level or effect of finasteride by affecting hepatic/intestinal
etravirine
etravirine will decrease the level or effect of finasteride by affecting hepatic/intestinal
eucalyptus
eucalyptus will decrease the level or effect of finasteride by affecting hepatic/intestinal
fluconazole
fluconazole will increase the level or effect of finasteride by affecting hepatic/intestinal
fludrocortisone
fludrocortisone will decrease the level or effect of finasteride by affecting
fluvoxamine
fluvoxamine will increase the level or effect of finasteride by affecting hepatic/intestinal
fosamprenavir
fosamprenavir will increase the level or effect of finasteride by affecting
fosphenytoin
fosphenytoin will decrease the level or effect of finasteride by affecting hepatic/intestinal
grapefruit
grapefruit will increase the level or effect of finasteride by affecting hepatic/intestinal
griseofulvin
griseofulvin will decrease the level or effect of finasteride by affecting hepatic/intestinal
hexobarbital
hexobarbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
hydrocortisone
hydrocortisone will decrease the level or effect of finasteride by affecting
indinavir
indinavir will increase the level or effect of finasteride by affecting hepatic/intestinal
lapatinib
lapatinib will increase the level or effect of finasteride by affecting hepatic/intestinal
lumefantrine
lumefantrine will decrease the level or effect of finasteride by affecting hepatic/intestinal
marijuana
marijuana will increase the level or effect of finasteride by affecting hepatic/intestinal
mephobarbital
mephobarbital will decrease the level or effect of finasteride by affecting
methylprednisolone
methylprednisolone will decrease the level or effect of finasteride by affecting
metronidazole
metronidazole will increase the level or effect of finasteride by affecting
mibefradil
mibefradil will increase the level or effect of finasteride by affecting hepatic/intestinal
miconazole vaginal
miconazole vaginal will increase the level or effect of finasteride by affecting
modafinil
modafinil will decrease the level or effect of finasteride by affecting hepatic/intestinal
nelfinavir
nelfinavir will increase the level or effect of finasteride by affecting hepatic/intestinal
nifedipine
nifedipine will increase the level or effect of finasteride by affecting hepatic/intestinal
nilotinib
nilotinib will increase the level or effect of finasteride by affecting hepatic/intestinal
oxcarbazepine
oxcarbazepine will decrease the level or effect of finasteride by affecting
oxiconazole
oxiconazole will increase the level or effect of finasteride by affecting hepatic/intestinal
pentobarbital
pentobarbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
phenobarbital
phenobarbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
phenytoin
phenytoin will decrease the level or effect of finasteride by affecting hepatic/intestinal
posaconazole
posaconazole will increase the level or effect of finasteride by affecting hepatic/intestinal
prednisolone
prednisolone will decrease the level or effect of finasteride by affecting hepatic/intestinal
prednisone
prednisone will decrease the level or effect of finasteride by affecting hepatic/intestinal
primidone
primidone will decrease the level or effect of finasteride by affecting hepatic/intestinal
quinupristin/dalfopristin will increase the level or effect of finasteride by affecting
rifapentine
rifapentine will decrease the level or effect of finasteride by affecting hepatic/intestinal
ritonavir
ritonavir will increase the level or effect of finasteride by affecting hepatic/intestinal
rufinamide
rufinamide will decrease the level or effect of finasteride by affecting hepatic/intestinal
saw palmetto
saw palmetto increases effects of finasteride by pharmacodynamic synergism. Minor or
secobarbital
secobarbital will decrease the level or effect of finasteride by affecting hepatic/intestinal
sitaxentan
sitaxentan will increase the level or effect of finasteride by affecting hepatic/intestinal
telithromycin
telithromycin will increase the level or effect of finasteride by affecting hepatic/intestinal
topiramate
topiramate will decrease the level or effect of finasteride by affecting hepatic/intestinal
triamcinolone
triamcinolone will decrease the level or effect of finasteride by affecting
troglitazone
troglitazone will decrease the level or effect of finasteride by affecting hepatic/intestinal
troleandomycin
troleandomycin will increase the level or effect of finasteride by affecting
verapamil
verapamil will increase the level or effect of finasteride by affecting hepatic/intestinal
voriconazole
voriconazole will increase the level or effect of finasteride by affecting hepatic/intestinal
zafirlukast
zafirlukast will increase the level or effect of finasteride by affecting hepatic/intestinal
Adverse Effects
1-10%
Erectile dysfunction (1.3-8.1%)
Decrease libido (1.8-6.4%)
Breast enlargement (0.5-1.8%)
Ejaculation disorder (0.8-1.2%)
<1%
Breast tenderness (0.4-0.7%)
Rash (0.5%)
Neoplasms: Male breast cancer
Breast disorders: Breast tenderness and enlargement
Nervous system/psychiatric: Depression
Hypersensitivity reactions: Rash, pruritus, urticaria, and angioedema (including swelling of the
lips, tongue, throat, and face)
Reproductive system: Sexual dysfunction that continued after discontinuation of treatment,
including erectile dysfunction, libido disorders, ejaculation disorders, and orgasm disorders;
male infertility and/or poor seminal quality (normalization or improvement of seminal quality
has been reported after discontinuation of finasteride); testicular pain
Contraindications
Hypersensitivity
Women of childbearing potential
Children
Cautions
Use with caution with obstructive uropathy; carefully monitor patients with large residual urinary
volume or severely diminished urinary flow
Use caution in liver disease
May cause decreased serum PSA in presence of prostate cancer; increases in PSA levels from
nadir while on finasteride may signal the presence of prostate cancer and should be carefully
evaluated (even if PSA value within normal range)
Pregnant and potentially pregnant women should not handle crushed or broken tablets
Rare reports of male breast cancer observed with use; any breast tenderness, enlargement, pain,
lumps, nipple discharge or any other type of breast changes should be reported immediately to
healthcare provider
5-ARIs and prostate cancer risk
June 9, 2011: Recent data from 2 large, randomized, controlled trials observed a
reduction in overall incidence of prostate cancer but an increased risk of being diagnosed
with a more serious form of prostate cancer (high-grade prostate cancer) in trial
participants taking 5-alpha reductase inhibitors (5-ARIs)
The 2 trials are the Prostate Cancer Prevention Trial (PCPT) and the Reduction by
Dutasteride of Prostate Cancer Events (REDUCE) trial
The revised prescribing information recommends that prior to initiating therapy with 5-
ARIs, appropriate evaluation should be performed to rule out other urologic conditions,
including prostate cancer, that might mimic benign prostatic hyperplasia (BPH)
Pharmacology
Mechanism of Action
Selective inhibitor of type 1 & type 2 isoforms of 5-alpha-reductase; suppresses serum
dihydrotestosterone levels by inhibiting the conversion of testosterone to dihydrotestosterone
Absorption
Onset: 6 months (BPH); >3 months (hair loss)
Peak plasma time: 2-6 hours
Distribution
Protein bound: 90%
Vd: 76 L
Metabolism
Hepatic CYP3A4
Metabolites: t-butyl side chain monohydroxylate, monocarboxylic acid metabolite (active)
Elimination
Half-life: 6 hours
Excretion: Feces (57%); urine (39%)
Patient Handout
560043
Patient Education
finasteride oral
FINASTERIDE - ORAL
(fin-AS-ter-ide)
COMMON BRAND NAME(S): Proscar
USES:
Finasteride is used to shrink an enlarged prostate (benign prostatic hyperplasia or BPH) in adult
men. It may be used alone or taken in combination with other medications to reduce symptoms
of BPH and may also reduce the need for surgery.
Finasteride may improve symptoms of BPH and provide benefits such as decreased urge to
urinate, better urine flow with less straining, less of a feeling that the bladder is not completely
emptied, and decreased nighttime urination. This medication works by decreasing the amount of
a natural body hormone (DHT) that causes growth of the prostate.
Finasteride is not approved for prevention of prostate cancer. It may slightly increase the risk of
developing a very serious form of prostate cancer. Talk to your doctor about the benefits and
risks.
Women and children should not use this medication.
HOW TO USE:
Read the Patient Information Leaflet provided by your pharmacist before you start taking
finasteride and each time you get a refill. If you have any questions regarding the information,
consult your doctor or pharmacist.
Take this medication by mouth, with or without food, usually once a day, or as directed by your
doctor.
If the tablet is crushed or broken, it should not be handled by a woman who is pregnant or by a
woman who may become pregnant (see also Precautions section).
Use this medication regularly in order to get the most benefit from it. Remember to use it at the
same time each day. Do not stop taking this medication without consulting your doctor.
It may take 6-12 months to notice a benefit.
Inform your doctor if your condition persists or worsens.
SIDE EFFECTS:
Decreased sexual ability/desire may occur. In some men, this medication can decrease the
amount of semen released during sex. This is harmless, but has continued in some men even after
stopping treatment. Finasteride may also increase hair growth. If any of these effects persist or
worsen, notify your doctor or pharmacist promptly.
Tell your doctor immediately if any of these unlikely but serious side effects occur: lump in the
breast, nipple discharge, breast enlargement/tenderness/pain, pain in the testicles, inability to
urinate.
A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it
occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of
the face/tongue/throat), severe dizziness, trouble breathing.
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking finasteride, tell your doctor or pharmacist if you are allergic to it; or if you have
any other allergies. This product may contain inactive ingredients, which can cause allergic
reactions or other problems. Talk to your pharmacist for more details.
liver disease, prostate cancer, infections, urinary problems.
Finasteride should not be used in children.
The drug can be absorbed through the skin. If the film coating of the tablet has been broken or
the tablet crushed, it should not be handled by a woman who is pregnant or planning to become
pregnant. Exposing a developing male infant to finasteride can result in abnormalities of the
genitals.
Finasteride is not recommended for use in women and must not be used during pregnancy. If you
become pregnant or think you may be pregnant, inform your doctor immediately.
This medication is not usually used in women. Therefore, it is unlikely to be used during
pregnancy or breast-feeding. Consult your doctor if you have any questions about this
medication.
DRUG INTERACTIONS:
Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible
drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of
any medicine before checking with them first.
Before using this medication, tell your doctor or pharmacist of all prescription and
nonprescription/herbal products you may use.
This medication can affect the results of the blood test used to detect prostate cancer (prostatic-
specific antigen or PSA levels). Make sure laboratory personnel and your doctors know you use
this drug.
This document does not contain all possible interactions. Therefore, before using this product,
tell your doctor or pharmacist of all the products you use. Keep a list of all your medications
with you, and share the list with your doctor and pharmacist.
OVERDOSE:
NOTES:
Laboratory and/or medical tests (e.g., prostate exams, PSA levels) should be performed
details.
Keep all appointments with your doctor and the laboratory. You should have a complete physical
examination. Follow your doctor's instructions for examining your breasts and testicles, and
report any lumps immediately.
Although early improvement is often seen, at least 6 to 12 months of therapy may be necessary
in some patients to assess whether or not a benefit has occurred. Therefore, it is important to
keep regular doctor appointments and get blood tests as scheduled to make sure this medication
is working.
Many men are born with the condition this drug mimics (prostate glands that are smaller than
usual) and lead normal lives with normal sex drives.
MISSED DOSE:
STORAGE:
Store US product at room temperature below 86 degrees F (30 degrees C) away from light and
moisture in a tightly closed container.
Store Canadian product at room temperature between 59 to 86 degrees F (15 to 30 degrees C)
away from light and moisture in a tightly closed container.
Do not store in the bathroom. Keep all medicines away from children and pets.

Dutasteride (Avodart)

Dutasteride is indicated for the treatment of BPH as monotherapy or in combination with
tamsulosin. Dutasteride improves symptoms, reduces urinary retention, and may decrease the
need for BPH-related surgery. It inhibits 5alpha-reductase isoenzymes types I and II. This agent
suppresses conversion of testosterone to DHT by more than 95%, causing serum DHT levels to
decrease.
Dosing & Uses
AdultPediatric
0.5 mg PO qDay
Renal impairment: Dose adjustment not necessary
Hepatic impairment: Dose adjustment not necessary
Drug Interactions
Interaction Checker
dutasteride and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (0)
carbamazepine
carbamazepine will decrease the level or effect of dutasteride by affecting
cimetidine
cimetidine will increase the level or effect of dutasteride by affecting hepatic/intestinal
clarithromycin
clarithromycin will increase the level or effect of dutasteride by affecting
erythromycin base
erythromycin base will increase the level or effect of dutasteride by affecting
erythromycin ethylsuccinate will increase the level or effect of dutasteride by affecting
erythromycin lactobionate will increase the level or effect of dutasteride by affecting
erythromycin stearate will increase the level or effect of dutasteride by affecting
isoniazid
isoniazid will increase the level or effect of dutasteride by affecting hepatic/intestinal
itraconazole
itraconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
ketoconazole
ketoconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
nefazodone
nefazodone will increase the level or effect of dutasteride by affecting hepatic/intestinal
rifabutin
rifabutin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
rifampin
rifampin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
st john's wort
st john's wort will decrease the level or effect of dutasteride by affecting hepatic/intestinal
Minor (74)
amobarbital
amobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
aprepitant
aprepitant will increase the level or effect of dutasteride by affecting hepatic/intestinal
armodafinil
armodafinil will decrease the level or effect of dutasteride by affecting hepatic/intestinal
artemether/lumefantrine will decrease the level or effect of dutasteride by affecting
atazanavir
atazanavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
bosentan
bosentan will decrease the level or effect of dutasteride by affecting hepatic/intestinal
budesonide
budesonide will decrease the level or effect of dutasteride by affecting hepatic/intestinal
butabarbital
butabarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
butalbital
butalbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
clobetasone
clobetasone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
conivaptan
conivaptan will increase the level or effect of dutasteride by affecting hepatic/intestinal
cortisone
cortisone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
cyclosporine
cyclosporine will increase the level or effect of dutasteride by affecting hepatic/intestinal
darifenacin
darifenacin will increase the level or effect of dutasteride by affecting hepatic/intestinal
darunavir
darunavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
dasatinib
dasatinib will increase the level or effect of dutasteride by affecting hepatic/intestinal
deferasirox
deferasirox will decrease the level or effect of dutasteride by affecting hepatic/intestinal
deflazacort
deflazacort will decrease the level or effect of dutasteride by affecting hepatic/intestinal
delavirdine
delavirdine will increase the level or effect of dutasteride by affecting hepatic/intestinal
dexamethasone
dexamethasone will decrease the level or effect of dutasteride by affecting
dhea
dhea will increase the level or effect of dutasteride by affecting hepatic/intestinal enzyme
diltiazem
diltiazem will increase the level or effect of dutasteride by affecting hepatic/intestinal
dronedarone
dronedarone will increase the level or effect of dutasteride by affecting hepatic/intestinal
efavirenz
efavirenz will decrease the level or effect of dutasteride by affecting hepatic/intestinal
eslicarbazepine acetate will decrease the level or effect of dutasteride by affecting
ethotoin
ethotoin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
etravirine
etravirine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
eucalyptus
eucalyptus will decrease the level or effect of dutasteride by affecting hepatic/intestinal
fluconazole
fluconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
fludrocortisone
fludrocortisone will decrease the level or effect of dutasteride by affecting
fluvoxamine
fluvoxamine will increase the level or effect of dutasteride by affecting hepatic/intestinal
fosamprenavir
fosamprenavir will increase the level or effect of dutasteride by affecting
fosphenytoin
fosphenytoin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
grapefruit
grapefruit will increase the level or effect of dutasteride by affecting hepatic/intestinal
griseofulvin
griseofulvin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
hexobarbital
hexobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
hydrocortisone
hydrocortisone will decrease the level or effect of dutasteride by affecting
indinavir
indinavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
lapatinib
lapatinib will increase the level or effect of dutasteride by affecting hepatic/intestinal
lumefantrine
lumefantrine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
marijuana
marijuana will increase the level or effect of dutasteride by affecting hepatic/intestinal
mephobarbital
mephobarbital will decrease the level or effect of dutasteride by affecting
methylprednisolone
methylprednisolone will decrease the level or effect of dutasteride by affecting
metronidazole
metronidazole will increase the level or effect of dutasteride by affecting
mibefradil
mibefradil will increase the level or effect of dutasteride by affecting hepatic/intestinal
miconazole vaginal
miconazole vaginal will increase the level or effect of dutasteride by affecting
modafinil
modafinil will decrease the level or effect of dutasteride by affecting hepatic/intestinal
nelfinavir
nelfinavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
nevirapine
nevirapine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
nifedipine
nifedipine will increase the level or effect of dutasteride by affecting hepatic/intestinal
nilotinib
nilotinib will increase the level or effect of dutasteride by affecting hepatic/intestinal
oxcarbazepine
oxcarbazepine will decrease the level or effect of dutasteride by affecting
oxiconazole
oxiconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
pentobarbital
pentobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
phenobarbital
phenobarbital will decrease the level or effect of dutasteride by affecting
phenytoin
phenytoin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
posaconazole
posaconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
prednisolone
prednisolone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
prednisone
prednisone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
primidone
primidone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
quinupristin/dalfopristin will increase the level or effect of dutasteride by affecting
rifapentine
rifapentine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
ritonavir
ritonavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
rufinamide
rufinamide will decrease the level or effect of dutasteride by affecting hepatic/intestinal
secobarbital
secobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
sitaxentan
sitaxentan will increase the level or effect of dutasteride by affecting hepatic/intestinal
telithromycin
telithromycin will increase the level or effect of dutasteride by affecting hepatic/intestinal
topiramate
topiramate will decrease the level or effect of dutasteride by affecting hepatic/intestinal
triamcinolone
triamcinolone will decrease the level or effect of dutasteride by affecting
troglitazone
troglitazone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
troleandomycin
troleandomycin will increase the level or effect of dutasteride by affecting
verapamil
verapamil will increase the level or effect of dutasteride by affecting hepatic/intestinal
voriconazole
voriconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
zafirlukast
zafirlukast will increase the level or effect of dutasteride by affecting hepatic/intestinal
Adverse Effects
Adverse reactions decrease with duration of treatment, except for gynecomastia
1-10%
Impotence
Decreased libido
Ejaculation disorder
Breast disorders
<1%
Dizziness
Frequency Not Defined
Cardiac failure
Prostate cancer (high grade)
Immune system disorders: Hypersensitivity reactions, including rash, pruritus, urticaria,
localized edema, serious skin reactions, and angioedema
Psychiatric disorders: Depressed mood
Reproductive system and breast disorders: Testicular pain and testicular swelling
Contraindications
Hypersensitivity
Women
Children
Cautions
Prior to initiating treatment, rule out other urologic conditions
Pregnant women should avoid handling capsules due to risk of absorption through skin
Obstructive uropathy, liver disease
Patient should not donate blood until 6 months after last dose of dutasteride
Dutasteride lowers serum PSA 40-50%; establish new baseline PSA after 3-6 months of
treatment
Monitor for cardiac changes or cardiac failure
June 9, 2011: Recent data from 2 large, randomized, controlled trials observed an
increased risk of being diagnosed with a more serious form of prostate cancer (high-grade
prostate cancer) in trial participants taking 5-alpha reductase inhibitors (5-ARIs)
ARIs, appropriate evaluation should be performed to rule out other urologic conditions,
including prostate cancer, that might mimic benign prostatic hyperplasia
Pharmacology
Mechanism of Action
Selective inhibitor of type 1 and type 2 isoforms of 5-alpha-reductase; suppresses serum
dihydrotestosterone levels by inhibiting the conversion of testosterone to
dihydrotestosterone
Absorption
Onset: 1-2 weeks
Peak plasma time: 2-3 hours
Distribution
Protein bound: 99%
Vd: 300-500 L
Metabolism
Hepatic P450 enzyme CYP3A4 & CYP3A5
Metabolites, major: 4'-hydroxydutasteride, 6-hydroxydutasteride (as active as parent),
1,2'-dihydrodutasteride
Elimination
Half-life: 5 weeks (at steady state)
Excretion: Feces (40%), urine (<1%)
Patient Handout
560043
Patient Education
dutasteride oral
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does
NOT have all possible information about this product. This information does not assure
that this product is safe, effective, or appropriate for you. This information is not
individual medical advice and does not substitute for the advice of your health care
professional. Always ask your health care professional for complete information about
this product and your specific health needs.
DUTASTERIDE - ORAL
(due-TAST-er-ide)
COMMON BRAND NAME(S): Avodart
USES:
This medication is used in men to treat the symptoms of an enlarged prostate (benign
prostatic hyperplasia-BPH). It works by reducing the size of the enlarged prostate. This
helps to relieve symptoms of BPH such as difficulty in beginning the flow of urine, weak
stream, and the need to urinate frequently or urgently (including during the middle of the
night). It may also reduce the need for surgery to treat BPH.
Dutasteride is not approved for prevention of prostate cancer. It may slightly increase the
risk of developing a very serious form of prostate cancer. Talk to your doctor about the
benefits and risks.
This medication should not be used by women or children.
HOW TO USE:
Read the Patient Information Leaflet if available from your pharmacist before you start
taking this medication and each time you get a refill. If you have any questions, ask your
doctor or pharmacist.
Take this medication by mouth with or without food as directed by your doctor, usually
once daily. Swallow the medication whole. Do not crush or chew the capsules.
Use this medication regularly to get the most benefit from it. To help you remember, take
it at the same time each day.
Since this drug can be absorbed through the skin and may harm an unborn baby, women
who are pregnant or who may become pregnant should not handle this medication.
It may take 3 to 6 months to notice an improvement in symptoms. Tell your doctor if
your symptoms do not improve or if they worsen.
SIDE EFFECTS:
Sexual problems (such as decreased sexual interest/ability, decrease in the amount of
semen/sperm), testicle pain/swelling, increased breast size, or breast tenderness may
occur. Sexual problems have continued in some men even after stopping treatment. If any
of these effects persist or worsen, tell your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged
that the benefit to you is greater than the risk of side effects. Many people using this
medication do not have serious side effects.
A very serious allergic reaction to this drug is rare. However, get medical help right away
if you notice any symptoms of a serious allergic reaction, including: rash,
itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble
breathing.
This is not a complete list of possible side effects. If you notice other effects not listed
above, contact your doctor or pharmacist.
In the US -
Call your doctor for medical advice about side effects. You may report side effects to
FDA at 1-800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side
effects to Health Canada at 1-866-234-2345.
PRECAUTIONS:
Before taking dutasteride, tell your doctor or pharmacist if you are allergic to it; or to
finasteride; or if you have any other allergies. This product may contain inactive
ingredients, which can cause allergic reactions or other problems. Talk to your
Before having surgery, tell your doctor or dentist about all the products you use
(including prescription drugs, nonprescription drugs, and herbal products).
Do not donate blood while you are taking this medication and for at least 6 months after
you stop taking it. This will prevent the possibility of your blood being given to a
pregnant woman.
This medication is not usually used in women. Therefore, it is unlikely to be used during
pregnancy or breast-feeding. Consult your doctor if you have any questions about this
medication.
DRUG INTERACTIONS:
The effects of some drugs can change if you take other drugs or herbal products at the
same time. This can increase your risk for serious side effects or may cause your
medications not to work correctly. These drug interactions are possible, but do not always
occur. Your doctor or pharmacist can often prevent or manage interactions by changing
how you use your medications or by close monitoring.
To help your doctor and pharmacist give you the best care, be sure to tell your doctor and
pharmacist about all the products you use (including prescription drugs, nonprescription
drugs, and herbal products) before starting treatment with this product. While using this
product, do not start, stop, or change the dosage of any other medicines you are using
Keep a list of all the products you use. Share the list with your doctor and pharmacist to
reduce your risk for serious medication problems.
OVERDOSE:
If overdose is suspected, contact a poison control center or emergency room immediately.
US residents can call their local poison control center at 1-800-222-1222. Canada
residents can call a provincial poison control center.
NOTES:
Laboratory and/or medical tests (such as prostate exams, prostate-specific antigen-PSA)
should be performed periodically to monitor your progress or check for side effects.
Consult your doctor for more details.
MISSED DOSE:
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose,
skip the missed dose and resume your usual dosing schedule. Do not double the dose to
catch up.
STORAGE:
Store at room temperature away from light and moisture. Do not store in the bathroom.
Keep all medications away from children and pets.
Dutasteride capsules may soften and leak if stored at high temperatures. If your capsules
crack and leak, do not use them. If your skin comes in contact with the leaking capsules,
wash the area immediately with soap and water. Contact your pharmacist for more
information.
Do not flush medications down the toilet or pour them into a drain unless instructed to do
so. Properly discard this product when it is expired or no longer needed. Consult your
pharmacist or local waste disposal company for more details about how to safely discard
your product.
Information last revised May 2013. Copyright(c) 2013 First Databank, Inc.
Phosphodiesterase-5 Enzyme Inhibitors
Class Summary
These agents mediate smooth muscle relaxation in the lower urinary tract, thus improving
the symptoms of BPH.
Tadalafil (Cialis)

PDE5 selective inhibitor. Inhibition of PDE5 increases cGMP activity, which increases
vasodilatory effects of nitric oxide. Sexual stimulation is necessary to activate response.
Tadalafil has been approved by the FDA for the treatment of BPH signs and symptoms.
PDE5 inhibition has been shown to induce smooth muscle relaxation in the lower urinary
tract. It has also been approved for the treatment of simultaneous BPH and ED.
Increased sensitivity for erections may last 36 h with intermittent dosing. Low-dose daily
dosing may be recommended for more frequent sexual activity (ie, twice weekly); men
can attempt sexual activity at anytime between daily doses.
Dosing & Uses
AdultPediatric
Erectile Dysfunction
Cialis
PRN use: 10 mg PO initially before sexual activity, with or without food; may be increased to 20
mg or reduced to 5 mg on basis of efficacy and tolerability; in most patients, maximum dosing
frequency is once daily
Once-daily use: 2.5 mg/day PO in single daily dose, without regard to timing of sexual activity,
with or without food; may be increased to 5 mg/day on basis of efficacy and tolerability
PRN use: Decrease dose with concomitant use of potent CYP3A4 inhibitor (eg, ritonavir,
ketoconazole, itraconazole); not to exceed 10 mg/72 hr
Once-daily use: Decrease dose with concomitant use of potent CYP3A4 inhibitor (eg,
ritonavir, ketoconazole, itraconazole); not to exceed 2.5 mg/day
Treatment of signs and symptoms of benign prostatic hyperplasia (BPH); daily use also indicated
for treatment of patients with both BPH and erectile dysfunction
Cialis
BPH: 5 mg PO once daily
BPH with erectile dysfunction: 5 mg PO once daily, taken at approximately same time each day
without regard to timing of sexual activity
With finasteride for BPH: tadalafil 5 mg plus finasteride 5 mg PO once daily for 26 weeks
Pulmonary Arterial Hypertension
Adcirca
40 mg PO once daily; dividing dose for more frequent dosing is not recommended
Patients also taking ritonavir: 20 mg PO once daily initially for 1 week; may be increased to 40
mg/day on basis of tolerability
If possible, avoid coadministration with CYP3A4 inhibitors; if coadministration is
essential, long-term therapy is indicated, or strong CYP3A4 inhibitors are required,
modify or hold dose
Patients already taking strong CYP3A4 inhibitor who require tadalafil: 20 mg PO once
daily; may be increased to 40 mg/day on basis of tolerability
Patients already taking tadalafil who require strong CYP3A4 inhibitor: Avoid using
tadalafil while starting strong CYP3A4 inhibitor; stop tadalafil 24 hours before starting
strong CYP3A4 inhibitor; after 1 week, resume tadalafil at 20 mg PO once daily; may be
increased to 40 mg/day on basis of tolerability
Geriatric Dosing
Erectile Dysfunction
Cialis
No dosage adjustment is warranted solely on basis of age; however, greater sensitivity to
medications in some older individuals should be considered
Pulmonary Arterial Hypertension
Adcirca
Lower dose or reduced dosing frequency may be required in elderly because of decreased
renal or hepatic clearance
Renal impairment (erectile dysfunction)
Cialis (PRN use)
Mild (CrCl 51 mL/min): No dosage adjustment needed
Moderate (CrCl 30-50 mL/min): Not to exceed 5 mg PO once daily initially; maximum
dosage, 10 mg PO q48hr
Severe (CrCl <30 mL/min and on hemodialysis): Not to exceed 5 mg PO q72hr
Cialis (once-daily use)
CrCl 30 mL/min: No dosage adjustment needed
CrCl <30 mL/min: Not recommended
Renal impairment (pulmonary arterial hypertension)
Adcirca
Mild-to-moderate (CrCl 31-80 mL/min): 20 mg PO once daily initially; may be increased
to 40 mg once daily on basis of tolerability
Severe (CrCl <30 mL/min and on hemodialysis): Avoid use
Hepatic impairment (erectile dysfunction)
Cialis (PRN use)
Mild-to-moderate (Child-Pugh class A or B): Not to exceed 10 mg PO once daily
Severe (Child-Pugh class C): Not recommended
Cialis (once-daily use)
Mild-to-moderate (Child-Pugh class A or B): Data limited; caution advised
Severe (Child-Pugh class C): Not recommended
Hepatic impairment (pulmonary arterial hypertension)
Adcirca
Mild-to-moderate (Child-Pugh class A or B): Consider starting dosage of 20 mg PO once
daily
Severe (Child-Pugh class C): Avoid use
Administration
Erectile dysfunction (PRN use): Take before anticipated sexual activity
Erectile dysfunction (once-daily use): Take at approximately same time each day without regard
to timing of sexual activity
Drug Interactions
Interaction Checker
tadalafil and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (6)
boceprevir
boceprevir increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination. Contraindicated with chronic use for PAH.
Boceprevir can be used with tadalafil for ED; dose should be limited to 10 mg every 72
hr with increased monitoring for adverse reactions.
isosorbide dinitrate
isosorbide dinitrate, tadalafil. Mechanism: additive vasodilation. Never use combination.
Contraindicated. Potentially fatal hypotension. Allow 48h after last tadalafil dose before
nitrate administration.
isosorbide mononitrate
isosorbide mononitrate, tadalafil. Mechanism: additive vasodilation. Never use
combination. Contraindicated. Potentially fatal hypotension. Allow 48h after last tadalafil
dose before nitrate administration.
tadalafil increases effects of nitroglycerin rectal by additive vasodilation. Never use
combination. Use of nitroglycerin within a few days of PDE5 inhibitors is
contraindicated. PDE5 inhibitors have been shown to potentiate the hypotensive effects
of organic nitrates.
riociguat
tadalafil, riociguat. Either increases effects of the other by additive vasodilation. Never
use combination. Coadministration of specific PDE-5 inhibitors (eg sildenafil, tadalafil,
vardenafil) and nonspecific PDE-5 inhibitors (eg theophylline, dipyridamole) is
contraindicated due to risk of hypotension.
telaprevir
telaprevir increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Never use combination. Contraindicated with chronic use for PAH.
Telaprevir can be used with tadalafil for ED; dose should be limited to 10 mg every 72 hr
with increased monitoring for adverse reactions.
amyl nitrite
amyl nitrite, tadalafil. Mechanism: additive vasodilation. High likelihood serious or life-
available. Contraindicated. Potentially fatal hypotension. Allow 48h after last tadalafil
dose before nitrate administration.
atazanavir
atazanavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
Contraindicated unless benefits outweigh risks and no alternatives available. Stop
tadalafil >24 hours prior to protease inhibitor (PI) initiation, restart 7 days after PI
initiation at 20 mg once daily, and increase to 40 mg once daily based on tolerability.
clarithromycin
clarithromycin will increase the level or effect of tadalafil by affecting hepatic/intestinal
closely. Use alternatives if available. For ED limit tadalafil to max of 2.5 mg/day (for
daily use) or 10 mg dose every 72 hr (for use as needed). Avoid concurrent use of
tadalafil for pulmonary HTN in patients taking strong CYP3A4 inhibitors.
darunavir
darunavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
closely. Use alternatives if available. Stop tadalafil >24 hours prior to protease inhibitor
(PI) initiation, restart 7 days after PI initiation at 20 mg once daily, and increase to 40 mg
once daily based on tolerability.
erythromycin base
erythromycin base will increase the level or effect of tadalafil by affecting
interaction. Monitor closely. Use alternatives if available. For ED limit tadalafil to max of
2.5 mg/day (for daily use) or 10 mg dose every 72 hr (for use as needed). Avoid
concurrent use of tadalafil for pulmonary HTN in patients taking strong CYP3A4
inhibitors.
erythromycin ethylsuccinate will increase the level or effect of tadalafil by affecting
inhibitors.
erythromycin lactobionate will increase the level or effect of tadalafil by affecting
inhibitors.
erythromycin stearate will increase the level or effect of tadalafil by affecting
inhibitors.
fosamprenavir
fosamprenavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
idelalisib
idelalisib will increase the level or effect of tadalafil by affecting hepatic/intestinal
indinavir
indinavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
itraconazole
itraconazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
closely. Use alternatives if available. For ED limit tadalafil to max of 2.5 mg/day (for
daily use) or 10 mg dose every 72 hr (for use as needed). Avoid concurrent use of
tadalafil for pulmonary HTN in patients taking strong CYP3A4 inhibitors.
ivacaftor
ivacaftor increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
alternatives if available. Ivacaftor and its M1 metabolite has the potential to inhibit
CYP3A4, may significantly increase systemic exposure to 3A4 substrates.
ketoconazole
ketoconazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
Contraindicated unless benefits outweigh risks and no alternatives available. CYP3A4
inhibitors may reduce tadalafil clearance increasing systemic exposure to tadalafil;
significantly increased levels may result in significant adverse events including severe
hypotension, syncope, visual changes, and priapism.
lopinavir
lopinavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
closely. Use alternatives if available. CYP3A4 inhibitors may reduce tadalafil clearance
increasing systemic exposure to tadalafil; significantly increased levels may result in
significant adverse events including severe hypotension, syncope, visual changes, and
priapism.
nelfinavir
nelfinavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
nicardipine
nicardipine will increase the level or effect of tadalafil by affecting hepatic/intestinal
closely. Use alternatives if available. CYP3A4 inhibitors may reduce tadalafil clearance
increasing systemic exposure to tadalafil; significantly increased levels may result in
significant adverse events including severe hypotension, syncope, visual changes, and
priapism.
nitroglycerin iv
nitroglycerin iv, tadalafil. Mechanism: additive vasodilation. High likelihood serious or
life-threatening interaction. Contraindicated unless benefits outweigh risks and no
alternatives available. Potentially fatal hypotension.
nitroglycerin po
nitroglycerin po, tadalafil. Mechanism: additive vasodilation. High likelihood serious or
life-threatening interaction. Contraindicated unless benefits outweigh risks and no
nitroglycerin sublingual
nitroglycerin sublingual, tadalafil. Mechanism: additive vasodilation. High likelihood
no alternatives available. Potentially fatal hypotension.
nitroglycerin topical
nitroglycerin topical, tadalafil. Mechanism: additive vasodilation. High likelihood serious
or life-threatening interaction. Contraindicated unless benefits outweigh risks and no
nitroglycerin transdermal
nitroglycerin transdermal, tadalafil. Mechanism: additive vasodilation. High likelihood
nitroglycerin translingual
nitroglycerin translingual, tadalafil. Mechanism: additive vasodilation. High likelihood
nitroglycerin transmucosal
nitroglycerin transmucosal, tadalafil. Mechanism: additive vasodilation. High likelihood
pentaerythritol tetranitrate
pentaerythritol tetranitrate, tadalafil. Mechanism: additive vasodilation. High likelihood
ritonavir
ritonavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
acebutolol
tadalafil increases effects of acebutolol by pharmacodynamic synergism. Potential for
acetazolamide
tadalafil increases effects of acetazolamide by pharmacodynamic synergism. Potential for
alfuzosin
tadalafil increases effects of alfuzosin by pharmacodynamic synergism. Significant
aliskiren
tadalafil increases effects of aliskiren by pharmacodynamic synergism. Potential for
amiloride
tadalafil increases effects of amiloride by pharmacodynamic synergism. Potential for
amiodarone
amiodarone will increase the level or effect of tadalafil by affecting hepatic/intestinal
monitor closely. CYP3A4 inhibitors may reduce tadalafil clearance increasing systemic
exposure to tadalafil; increased levels may result in increased associated adverse events.
amlodipine
tadalafil increases effects of amlodipine by pharmacodynamic synergism. Potential for
amobarbital
amobarbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
aprepitant
aprepitant will increase the level or effect of tadalafil by affecting hepatic/intestinal
armodafinil
armodafinil will decrease the level or effect of tadalafil by affecting hepatic/intestinal
artemether/lumefantrine will decrease the level or effect of tadalafil by affecting
asenapine
tadalafil increases effects of asenapine by pharmacodynamic synergism. Potential for
atazanavir
atazanavir increases levels of tadalafil by decreasing metabolism. Significant interaction
possible, monitor closely. Stop tadalafil >24 hours prior to protease inhibitor (PI)
initiation, restart 7 days after PI initiation at 20 mg once daily, and increase to 40 mg
atenolol
tadalafil increases effects of atenolol by pharmacodynamic synergism. Potential for
azilsartan
tadalafil increases effects of azilsartan by pharmacodynamic synergism. Potential for
benazepril
tadalafil increases effects of benazepril by pharmacodynamic synergism. Potential for
betaxolol
tadalafil increases effects of betaxolol by pharmacodynamic synergism. Potential for
bicalutamide
bicalutamide will increase the level or effect of tadalafil by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Significant interaction possible, monitor closely. CYP3A4
increased levels may result in increased associated adverse events.
bisoprolol
tadalafil increases effects of bisoprolol by pharmacodynamic synergism. Potential for
bosentan
bosentan will decrease the level or effect of tadalafil by affecting hepatic/intestinal
budesonide
budesonide will decrease the level or effect of tadalafil by affecting hepatic/intestinal
bumetanide
tadalafil increases effects of bumetanide by pharmacodynamic synergism. Potential for
butabarbital
butabarbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Significant interaction possible, monitor closely. Avoid
combination in pulmonary HTN patients. For patients with ED, monitor response to
tadalafil carefully because of potential for decreased effectiveness.
butalbital
butalbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
candesartan
tadalafil increases effects of candesartan by pharmacodynamic synergism. Potential for
captopril
tadalafil increases effects of captopril by pharmacodynamic synergism. Potential for
carbamazepine
carbamazepine will decrease the level or effect of tadalafil by affecting hepatic/intestinal
carvedilol
tadalafil increases effects of carvedilol by pharmacodynamic synergism. Potential for
chlorthalidone
tadalafil increases effects of chlorthalidone by pharmacodynamic synergism. Potential for
cimetidine
cimetidine will increase the level or effect of tadalafil by affecting hepatic/intestinal
clevidipine
tadalafil increases effects of clevidipine by pharmacodynamic synergism. Potential for
clobetasone
clobetasone will decrease the level or effect of tadalafil by affecting hepatic/intestinal
clonidine
tadalafil increases effects of clonidine by pharmacodynamic synergism. Potential for
clotrimazole
clotrimazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
conivaptan
conivaptan will increase the level or effect of tadalafil by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Significant interaction possible, monitor closely. For ED
limit tadalafil to max of 2.5 mg/day (for daily use) or 10 mg dose every 72 hr (for use as
needed). Avoid concurrent use of tadalafil for pulmonary HTN in patients taking strong
CYP3A4 inhibitors.
crizotinib
crizotinib increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
crofelemer
crofelemer increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
minimally absorbed.
cyclosporine
cyclosporine will increase the level or effect of tadalafil by affecting hepatic/intestinal
dabrafenib
dabrafenib will decrease the level or effect of tadalafil by affecting hepatic/intestinal
monitor closely.
dasatinib
dasatinib will increase the level or effect of tadalafil by affecting hepatic/intestinal
deferasirox
deferasirox will decrease the level or effect of tadalafil by affecting hepatic/intestinal
delavirdine
delavirdine will increase the level or effect of tadalafil by affecting hepatic/intestinal
CYP3A4 inhibitors.
desipramine
desipramine will increase the level or effect of tadalafil by affecting hepatic/intestinal
dexamethasone
dexamethasone will decrease the level or effect of tadalafil by affecting hepatic/intestinal
diltiazem
diltiazem will increase the level or effect of tadalafil by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Potential for interaction, monitor. Risk of hypotension.
doxazosin
tadalafil increases effects of doxazosin by pharmacodynamic synergism. Significant
dronedarone
dronedarone will increase the level or effect of tadalafil by affecting hepatic/intestinal
efavirenz
efavirenz will decrease the level or effect of tadalafil by affecting hepatic/intestinal
elvitegravir/cobicistat/emtricitabine/tenofovir increases levels of tadalafil by affecting
with caution and monitor closely. Adjust tadalafil dose for PAH; if on Stribild, start
tadalafil 20 mg/day; avoid tadalafil when starting Stribild; for ED, a single dose of
tadalafil not exceeding 10 mg in 72 hr.
enalapril
tadalafil increases effects of enalapril by pharmacodynamic synergism. Potential for
eplerenone
tadalafil increases effects of eplerenone by pharmacodynamic synergism. Potential for
eprosartan
tadalafil increases effects of eprosartan by pharmacodynamic synergism. Potential for
eslicarbazepine acetate will decrease the level or effect of tadalafil by affecting
hepatic/intestinal enzyme CYP3A4 metabolism. Significant interaction possible, monitor
closely. Avoid combination in pulmonary HTN patients. For patients with ED, monitor
response to tadalafil carefully because of potential for decreased effectiveness.
esmolol
tadalafil increases effects of esmolol by pharmacodynamic synergism. Potential for
ethacrynic acid
tadalafil increases effects of ethacrynic acid by pharmacodynamic synergism. Potential
for interaction, monitor. Risk of hypotension.
ethanol
ethanol, tadalafil. Either increases effects of the other by additive vasodilation. Potential
for interaction, monitor. Combination may increase risk of orthostatic hypotension,
tachycardia, dizziness and headache.
ethotoin
ethotoin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
etravirine
etravirine will decrease the level or effect of tadalafil by affecting hepatic/intestinal
felodipine
tadalafil increases effects of felodipine by pharmacodynamic synergism. Potential for
fluconazole
fluconazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
fluvoxamine
fluvoxamine will increase the level or effect of tadalafil by affecting hepatic/intestinal
fosinopril
tadalafil increases effects of fosinopril by pharmacodynamic synergism. Potential for
fosphenytoin
fosphenytoin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
furosemide
tadalafil increases effects of furosemide by pharmacodynamic synergism. Potential for
grapefruit
grapefruit will increase the level or effect of tadalafil by affecting hepatic/intestinal
griseofulvin
griseofulvin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
guanabenz
tadalafil increases effects of guanabenz by pharmacodynamic synergism. Potential for
guanfacine
tadalafil increases effects of guanfacine by pharmacodynamic synergism. Potential for
haloperidol
haloperidol will increase the level or effect of tadalafil by affecting hepatic/intestinal
hydralazine
tadalafil increases effects of hydralazine by pharmacodynamic synergism. Potential for
hydrochlorothiazide
tadalafil increases effects of hydrochlorothiazide by pharmacodynamic synergism.
iloperidone
iloperidone increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Potential for interaction, monitor. Iloperidone is a time-dependent CYP3A
inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by
CYP3A4.
imatinib
imatinib will increase the level or effect of tadalafil by affecting hepatic/intestinal
CYP3A4 inhibitors.
indapamide
tadalafil increases effects of indapamide by pharmacodynamic synergism. Potential for
irbesartan
tadalafil increases effects of irbesartan by pharmacodynamic synergism. Potential for
isoniazid
isoniazid will increase the level or effect of tadalafil by affecting hepatic/intestinal
CYP3A4 inhibitors.
isradipine
tadalafil increases effects of isradipine by pharmacodynamic synergism. Potential for
labetalol
tadalafil increases effects of labetalol by pharmacodynamic synergism. Potential for
lapatinib
lapatinib will increase the level or effect of tadalafil by affecting hepatic/intestinal
lisinopril
tadalafil increases effects of lisinopril by pharmacodynamic synergism. Potential for
losartan
tadalafil increases effects of losartan by pharmacodynamic synergism. Potential for
lumefantrine
lumefantrine will decrease the level or effect of tadalafil by affecting hepatic/intestinal
maraviroc
maraviroc, tadalafil. Either increases effects of the other by pharmacodynamic synergism.
Significant interaction possible, monitor closely. Increased risk of orthostatic
hypotension.
marijuana
marijuana will increase the level or effect of tadalafil by affecting hepatic/intestinal
mephobarbital
mephobarbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
metolazone
tadalafil increases effects of metolazone by pharmacodynamic synergism. Potential for
metoprolol
tadalafil increases effects of metoprolol by pharmacodynamic synergism. Potential for
metronidazole
metronidazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
minoxidil
tadalafil increases effects of minoxidil by pharmacodynamic synergism. Potential for
mitotane
mitotane decreases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
modafinil
modafinil will decrease the level or effect of tadalafil by affecting hepatic/intestinal
nadolol
tadalafil increases effects of nadolol by pharmacodynamic synergism. Potential for
nafcillin
nafcillin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
nebivolol
tadalafil increases effects of nebivolol by pharmacodynamic synergism. Potential for
nefazodone
nefazodone will increase the level or effect of tadalafil by affecting hepatic/intestinal
CYP3A4 inhibitors.
nevirapine
nevirapine will decrease the level or effect of tadalafil by affecting hepatic/intestinal
nifedipine
nifedipine will increase the level or effect of tadalafil by affecting hepatic/intestinal

tadalafil increases effects of nifedipine by pharmacodynamic synergism. Potential for
nilotinib
nilotinib will increase the level or effect of tadalafil by affecting hepatic/intestinal
nimodipine
tadalafil increases effects of nimodipine by pharmacodynamic synergism. Potential for
nisoldipine
tadalafil increases effects of nisoldipine by pharmacodynamic synergism. Potential for
nitroprusside sodium
nitroprusside sodium, tadalafil. Mechanism: pharmacodynamic synergism. Significant
interaction possible, monitor closely. Additive hypotensive effects.
norfloxacin
norfloxacin will increase the level or effect of tadalafil by affecting hepatic/intestinal
olmesartan
tadalafil increases effects of olmesartan by pharmacodynamic synergism. Potential for
oxcarbazepine
oxcarbazepine will decrease the level or effect of tadalafil by affecting hepatic/intestinal
pazopanib
pazopanib will increase the level or effect of tadalafil by affecting hepatic/intestinal
penbutolol
tadalafil increases effects of penbutolol by pharmacodynamic synergism. Potential for
pentobarbital
pentobarbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
phenobarbital
phenobarbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
phenoxybenzamine
tadalafil increases effects of phenoxybenzamine by pharmacodynamic synergism.
phentolamine
tadalafil increases effects of phentolamine by pharmacodynamic synergism. Significant
phenytoin
phenytoin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
posaconazole
posaconazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
prazosin
tadalafil increases effects of prazosin by pharmacodynamic synergism. Significant
primidone
primidone will decrease the level or effect of tadalafil by affecting hepatic/intestinal
propranolol
tadalafil increases effects of propranolol by pharmacodynamic synergism. Potential for
quinapril
tadalafil increases effects of quinapril by pharmacodynamic synergism. Potential for
quinupristin/dalfopristin will increase the level or effect of tadalafil by affecting
ramipril
tadalafil increases effects of ramipril by pharmacodynamic synergism. Potential for
reserpine
tadalafil increases effects of reserpine by pharmacodynamic synergism. Potential for
rifabutin
rifabutin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
rifampin
rifampin will decrease the level or effect of tadalafil by affecting hepatic/intestinal
rifapentine
rifapentine will decrease the level or effect of tadalafil by affecting hepatic/intestinal
rufinamide
rufinamide will decrease the level or effect of tadalafil by affecting hepatic/intestinal
sapropterin
sapropterin, tadalafil. Either increases effects of the other by pharmacodynamic
synergism. Potential for interaction, monitor. Possible additive vasorelaxation, leading to
low blood pressure.
saquinavir
saquinavir increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
metabolism. Significant interaction possible, monitor closely. Potential for increased
toxicity. .
secobarbital
secobarbital will decrease the level or effect of tadalafil by affecting hepatic/intestinal
sertraline
sertraline will increase the level or effect of tadalafil by affecting hepatic/intestinal
sildenafil
sildenafil, tadalafil. Other (see comment). Significant interaction possible, monitor
closely. Comment: Avoid combination; duplicate therapy is not recommended.
silodosin
tadalafil increases effects of silodosin by pharmacodynamic synergism. Significant
simeprevir
simeprevir increases levels of tadalafil by affecting hepatic/intestinal enzyme CYP3A4
Dose adjustment of PDE-5 inhibitors may be required when simeprevir is coadministered
with chronically administered sildenafil or tadalafil at doses used for the treatment of
pulmonary arterial hypertension.
sotalol
tadalafil increases effects of sotalol by pharmacodynamic synergism. Potential for
spironolactone
tadalafil increases effects of spironolactone by pharmacodynamic synergism. Potential
for interaction, monitor. Risk of hypotension.
st john's wort
st john's wort will decrease the level or effect of tadalafil by affecting hepatic/intestinal
tamsulosin
telithromycin
telithromycin will increase the level or effect of tadalafil by affecting hepatic/intestinal
CYP3A4 inhibitors.
telmisartan
tadalafil increases effects of telmisartan by pharmacodynamic synergism. Potential for
terazosin
tadalafil increases effects of terazosin by pharmacodynamic synergism. Significant
tetracycline
tetracycline will increase the level or effect of tadalafil by affecting hepatic/intestinal
timolol
tadalafil increases effects of timolol by pharmacodynamic synergism. Potential for
tipranavir
tipranavir will increase the level or effect of tadalafil by affecting hepatic/intestinal
CYP3A4 inhibitors.
tobramycin inhaled
tobramycin inhaled and tadalafil both increase nephrotoxicity and/or ototoxicity.
Potential for dangerous interaction. Use with caution and monitor closely. Avoid
concurrent or sequential use to decrease risk for ototoxicity
topiramate
topiramate will decrease the level or effect of tadalafil by affecting hepatic/intestinal
torsemide
tadalafil increases effects of torsemide by pharmacodynamic synergism. Potential for
trandolapril
tadalafil increases effects of trandolapril by pharmacodynamic synergism. Potential for
triamterene
tadalafil increases effects of triamterene by pharmacodynamic synergism. Potential for
troglitazone
troglitazone will decrease the level or effect of tadalafil by affecting hepatic/intestinal
valsartan
tadalafil increases effects of valsartan by pharmacodynamic synergism. Potential for
vardenafil
vardenafil, tadalafil. Other (see comment). Significant interaction possible, monitor
closely. Comment: Avoid combination; duplicate therapy is not recommended.
verapamil
verapamil will increase the level or effect of tadalafil by affecting hepatic/intestinal
voriconazole
voriconazole will increase the level or effect of tadalafil by affecting hepatic/intestinal
zafirlukast
zafirlukast will increase the level or effect of tadalafil by affecting hepatic/intestinal
Minor (1)
ranolazine
ranolazine will increase the level or effect of tadalafil by affecting hepatic/intestinal
enzyme CYP3A4 metabolism. Minor or non-significant interaction. Ranolazine may
theoretically increase plasma concentrations of CYP3A4 substrates, such as tadalafil.
Adverse Effects
>10%
Headache (11-42%)
Myalgia (1-14%)
Respiratory tract infection (3-13%)
Nasopharyngitis (2-13%)
Dyspepsia (1-13%)
Flushing (1-13%)
Back pain (2-12%)
Nausea (10-11%)
1-10%
Nasal congestion (9%)
Gastroesophageal reflux disease (1-3%)
Hypertension (1-3%)
Bronchitis (2%)
Genitourinary tract infection (2%)
<1%
Amnesia
Angina pectoris
Arthralgia
Change in color vision
Conjunctival hyperemia
Dyspnea
Epistaxis
Contraindications
Concomitant use of any form of organic nitrates (eg, nitroglycerin, isosorbide dinitrate,
isosorbide mononitrate, illicit "poppers"), either regularly or intermittently; may potentiate
hypotensive effect of nitrates
Hypersensitivity, including Stevens-Johnson syndrome and exfoliative dermatitis
Cautions
Anatomic deformation of penis, cardiovascular disease, left ventricular outflow obstruction,
myocardial infarction in preceding 90 days, unstable angina, angina occurring during sexual
intercourse, NYHA class 2 or greater heart failure in preceding 6 months, uncontrolled
arrhythmias, hypotension, uncontrolled hypertension, cerebrovascular accident in preceding 6
months, bleeding disorders, active peptic ulcer disease, liver disease, renal impairment, retinitis
pigmentosa, conditions predisposing to priapism, concomitant use of CYP3A4 inhibitors
May increase risk of sudden vision loss attributed to nonarteritic ischemic optic neuropathy; if
vision problems arise, discontinue, and contact physician
Risk of sudden hearing loss
CYP3A4 inhibitors (eg, erythromycin, ketoconazole, itraconazole, indinavir, ritonavir) may
significantly increase tadalafil serum levels
CYP3A4 inducers (eg, rifampin, St Johns wort) may decrease tadalafil serum levels
Potentiates hypotensive effect of nitrates (see Contraindications)
Concomitant use with alpha blockers (other than tamsulosin 0.4 mg/day) should be stabilized
before initiation of phosphodiesterase (PDE)-5 inhibitors; patients with instability on alpha-
blocker therapy alone are at increased risk for symptomatic hypotension with concurrent PDE-5
inhibitor therapy
Not to be taken with other PDE-5 inhibitors (eg, sildenafil, vardenafil)
Concurrent alcohol consumption may increase risk of orthostatic hypotension
Pharmacology
Mechanism of Action
Erectile dysfunction: Inhibits PDE-5, increasing cyclic guanosine monophosphate (cGMP) to
allow smooth-muscle relaxation and inflow of blood into corpus cavernosum
Pulmonary arterial hypertension (PAH): Inhibits PDE-5, increasing cGMP to allow relaxation of
pulmonary vascular smooth-muscle cells and vasodilation of pulmonary vasculature
Absorption
Duration: 36 hr
Peak plasma time: Erectile dysfunction, 0.5-6 hr; PAH, 2-8 hr
Distribution
Protein bound: 94%
Vd: Erectile dysfunction, 63 L; PAH, 77 L
Metabolism
Metabolized in liver by CYP3A4
Elimination
Half-life: Erectile dysfunction, 15-17.5 hr; PAH (not on bosentan), 35 hr
Total body clearance: Erectile dysfunction, 2.5 L/hr; PAH (not on bosentan), 1.6 L/hr
Excretion: Feces (61%), urine (36%)
Patient Handout
560043
Patient Education
tadalafil oral
TADALAFIL (LUNGS) - ORAL
(ta-DA-la-fil)
COMMON BRAND NAME(S): Adcirca
USES:
Tadalafil is used to treat high blood pressure in the lungs (pulmonary hypertension). It works by
relaxing and widening the blood vessels in your lungs which allows the blood to flow more
easily. Decreasing high blood pressure in the lungs allows your heart and lungs to work better
and improves your ability to exercise.
OTHER USES:
professional.
Tadalafil is also available in another brand for treating erectile dysfunction-ED in men. It may
also be used to treat the symptoms of an enlarged prostate (benign prostatic hyperplasia-BPH).
HOW TO USE:
Read the Patient Information Leaflet provided by your pharmacist before you start taking
tadalafil and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
To treat high blood pressure in the lungs, take this medication by mouth as directed by your
doctor, with or without food, usually once daily.
The dosage is based on your medical condition, response to treatment, and other medications you
may be taking. Be sure to tell your doctor and pharmacist about all the products you use
(including prescription drugs, nonprescription drugs, and herbal products).
the same time each day.
SIDE EFFECTS:
Dizziness, lightheadedness, headache, muscle pain, flushing, nausea, stuffy nose, or stomach
upset may occur. If any of these effects persist or worsen, tell your doctor or pharmacist
promptly.
lying position.
Rarely, sudden decreased vision, including permanent blindness, in one or both eyes (NAION)
may occur. If this serious problem occurs, stop taking tadalafil and get medical help right away.
You have a slightly greater chance of developing NAION if you have heart disease, diabetes,
high cholesterol, certain other eye problems ("crowded disk"), high blood pressure, if you are
over 50, or if you smoke.
Rarely, a sudden decrease or loss of hearing, sometimes with ringing in the ears and dizziness,
may occur. Stop taking tadalafil and get medical help right away if these effects occur.
Get medical help right away if you have any very serious side effects, including: increased
shortness of breath or trouble breathing.
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking tadalafil, tell your doctor or pharmacist if you are allergic to it; or if you have any
other allergies. This product may contain inactive ingredients, which can cause allergic reactions
or other problems. Talk to your pharmacist for more details.
heart problems (such as heart attack or life-threatening irregular heartbeat in the past 6 months,
chest pain/angina, heart failure), stroke in the past 6 months, kidney disease, liver disease, high
or low blood pressure, a severe loss of body water (dehydration), penis conditions (such as
angulation, fibrosis/scarring, Peyronie's disease), history of painful/prolonged erection
(priapism), conditions that may increase the risk of priapism (such as sickle cell anemia,
leukemia, multiple myeloma), eye problems (such as retinitis pigmentosa, sudden decreased
vision, NAION), bleeding disorders, active stomach ulcers, other lung conditions (such as
pulmonary veno-occlusive disease).
Before having surgery, tell your doctor or dentist about all the products you use (including
prescription drugs, nonprescription drugs, and herbal products).
During pregnancy, tadalafil should be used only when clearly needed. Discuss the risks and
feeding.
DRUG INTERACTIONS:
A product that may interact with this drug is: riociguat.
Tadalafil can cause a serious drop in your blood pressure when used with nitrates, which can
lead to dizziness, fainting, and rarely heart attack or stroke. Do not use tadalafil with any of the
following: certain drugs used to treat chest pain/angina (nitrates such as nitroglycerin,
isosorbide), recreational drugs called "poppers" containing amyl or butyl nitrite.
If you are also taking an alpha blocker medication (such as doxazosin, tamsulosin) to treat an
enlarged prostate/BPH or high blood pressure, your blood pressure may get too low which can
lead to dizziness or fainting. Your doctor may adjust your medications to minimize your risk of
low blood pressure.
Other medications can affect the removal of tadalafil from your body, which may affect how
tadalafil works. Examples include azole antifungals (such as itraconazole, ketoconazole),
macrolide antibiotics (such as clarithromycin, erythromycin), HIV protease inhibitors (such as
lopinavir, ritonavir), hepatitis C virus protease inhibitors (such as boceprevir, telaprevir),
rifampin, among others.
Do not take this medication with any other product that contains tadalafil or other similar
medications for erectile dysfunction-ED or pulmonary hypertension (such as sildenafil,
vardenafil).
OVERDOSE:
NOTES:
MISSED DOSE:
STORAGE:
Information last revised May 2014. Copyright(c) 2014 First Databank, Inc.
Combination Products
Class Summary
Various combination products are emerging on the market to improve patient compliance and
symptoms.
Dutasteride and tamsulosin (Jalyn)

The combination of dutasteride, a 5-alpha-reductase inhibitor, and tamsulosin, an alpha-
adrenergic antagonist is indicated for benign prostatic hypertrophy in men with an enlarged
prostate. Each cap contains dutasteride 0.5 mg and tamsulosin 0.4 mg.
Dosing & Uses
AdultPediatric
1 capsule PO 30 min after same meal once daily
Swallow capsule whole; do not chew, crush, or split
Drug Interactions
Interaction Checker
dutasteride/tamsulosin and
Type a dru

Interactions Found
Contraindicated
Minor
Sort by :
SEVERITY

NAME

Contraindicated (1)
boceprevir
boceprevir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
alfuzosin
atazanavir
atazanavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
clarithromycin
clarithromycin increases levels of tamsulosin by affecting hepatic/intestinal enzyme
conivaptan
conivaptan increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
darunavir
darunavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
delavirdine
delavirdine increases levels of tamsulosin by affecting hepatic/intestinal enzyme
doxazosin
fosamprenavir
fosamprenavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme
idelalisib
idelalisib will increase the level or effect of tamsulosin by affecting hepatic/intestinal
imatinib
imatinib increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
indinavir
indinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
isoniazid
isoniazid increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
itraconazole
itraconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
ketoconazole
ketoconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
Use alternatives if available. Potential for increased toxicity.
lopinavir
lopinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
alternatives if available. Potential for increased toxicity.
nefazodone
nefazodone increases levels of tamsulosin by affecting hepatic/intestinal enzyme
nelfinavir
nelfinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
nicardipine
nicardipine increases levels of tamsulosin by affecting hepatic/intestinal enzyme
phenoxybenzamine
phentolamine
phentolamine, tamsulosin. Either increases effects of the other by additive vasodilation.
posaconazole
posaconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
prazosin
quinidine
quinidine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
ritonavir
ritonavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
saquinavir
saquinavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
silodosin
telaprevir
telaprevir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
telithromycin
telithromycin increases levels of tamsulosin by affecting hepatic/intestinal enzyme
terazosin
tipranavir
tipranavir increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
voriconazole
voriconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
abiraterone
abiraterone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
metabolism. Significant interaction possible, monitor closely. Avoid coadministration of
abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise
caution and consider a dose reduction of the CYP2D6 substrate.
amiodarone
amiodarone increases levels of tamsulosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Potential for interaction, monitor. Dose reduction may be neeed for

amiodarone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
aprepitant
aprepitant increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
avanafil
avanafil, tamsulosin. Either increases effects of the other by additive vasodilation.
bicalutamide
bicalutamide increases levels of tamsulosin by affecting hepatic/intestinal enzyme
bortezomib
bortezomib increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
bupropion
bupropion increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
carbamazepine
carbamazepine will decrease the level or effect of dutasteride by affecting
chloroquine
chloroquine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
chlorpromazine
chlorpromazine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
cimetidine
cimetidine increases levels of tamsulosin by decreasing renal clearance. Significant
interaction possible, monitor closely. Decreases tamsulosin clearance by 26% resulting in
increased AUC (44%).

cimetidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6

cimetidine will increase the level or effect of dutasteride by affecting hepatic/intestinal
cinacalcet
cinacalcet increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
clarithromycin
clarithromycin will increase the level or effect of dutasteride by affecting
clobazam
clobazam increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
clomipramine
clomipramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
clozapine
clozapine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4

clozapine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
cocaine
cocaine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism.
crizotinib
crizotinib increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
crofelemer
crofelemer increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
minimally absorbed.
cyclosporine
cyclosporine increases levels of tamsulosin by affecting hepatic/intestinal enzyme
dabrafenib
dabrafenib will decrease the level or effect of tamsulosin by affecting hepatic/intestinal
monitor closely.
darifenacin
darifenacin increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
delavirdine
delavirdine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
desipramine
desipramine increases levels of tamsulosin by affecting hepatic/intestinal enzyme

desipramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
dexmedetomidine
dexmedetomidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
diltiazem
diltiazem increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
diphenhydramine
diphenhydramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
disulfiram
disulfiram increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
doxycycline
doxycycline increases levels of tamsulosin by affecting hepatic/intestinal enzyme
dronedarone
dronedarone increases levels of tamsulosin by affecting hepatic/intestinal enzyme

dronedarone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
duloxetine
duloxetine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
efavirenz
efavirenz increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
with caution and monitor closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with
CYP3A4 substrates for which elevated plasma concentrations are associated with serious
and/or life-threatening events.

hepatic enzyme CYP2D6 metabolism. Potential for dangerous interaction. Use with
caution and monitor closely. Cobicistat is a CYP2D6 inhibitor; caution with CYP2D6
substrates for which elevated plasma concentrations are associated with serious and/or
life-threatening events.
erythromycin base
erythromycin base will increase the level or effect of dutasteride by affecting

erythromycin base increases levels of tamsulosin by affecting hepatic/intestinal enzyme
erythromycin ethylsuccinate increases levels of tamsulosin by affecting hepatic/intestinal

erythromycin ethylsuccinate will increase the level or effect of dutasteride by affecting
erythromycin lactobionate will increase the level or effect of dutasteride by affecting

erythromycin lactobionate increases levels of tamsulosin by affecting hepatic/intestinal
erythromycin stearate will increase the level or effect of dutasteride by affecting

erythromycin stearate increases levels of tamsulosin by affecting hepatic/intestinal
fluconazole
fluconazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
isoniazid
isoniazid will increase the level or effect of dutasteride by affecting hepatic/intestinal
fluoxetine
fluoxetine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
grapefruit
grapefruit increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
haloperidol
haloperidol increases levels of tamsulosin by affecting hepatic/intestinal enzyme

haloperidol increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
iloperidone
iloperidone increases levels of tamsulosin by affecting hepatic/intestinal enzyme
CYP3A4 metabolism. Potential for interaction, monitor. Iloperidone is a time-dependent
CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly
eliminated by CYP3A4.
imatinib
imatinib increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
imipramine
imipramine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
isoniazid
isoniazid increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
itraconazole
itraconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
ketoconazole
ketoconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal

ketoconazole increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
lapatinib
lapatinib increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
nefazodone
nefazodone will increase the level or effect of dutasteride by affecting hepatic/intestinal
lidocaine
lidocaine increases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4

lidocaine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
lopinavir
lopinavir increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
lorcaserin
lorcaserin increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
methadone
methadone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
methimazole
methimazole increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
metronidazole
metronidazole increases levels of tamsulosin by affecting hepatic/intestinal enzyme
mitotane
mitotane decreases levels of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4
nefazodone
nefazodone increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
nicardipine
nicardipine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
norfloxacin
norfloxacin increases levels of tamsulosin by affecting hepatic/intestinal enzyme
paroxetine
paroxetine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
pyrimethamine
pyrimethamine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
quinidine
quinidine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
quinine
quinine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism.
ranolazine
ranolazine increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
rifabutin
rifabutin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
rifampin
rifampin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
ritonavir
ritonavir increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
sertraline
sertraline increases levels of tamsulosin by affecting hepatic enzyme CYP2D6
sildenafil
sildenafil, tamsulosin. Either increases effects of the other by additive vasodilation.
st john's wort
st john's wort will decrease the level or effect of dutasteride by affecting hepatic/intestinal
tadalafil
Minor (74)
amobarbital
amobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
aprepitant
aprepitant will increase the level or effect of dutasteride by affecting hepatic/intestinal
armodafinil
armodafinil will decrease the level or effect of dutasteride by affecting hepatic/intestinal
artemether/lumefantrine will decrease the level or effect of dutasteride by affecting
atazanavir
atazanavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
bosentan
bosentan will decrease the level or effect of dutasteride by affecting hepatic/intestinal
budesonide
budesonide will decrease the level or effect of dutasteride by affecting hepatic/intestinal
butabarbital
butabarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
butalbital
butalbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
clobetasone
clobetasone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
conivaptan
conivaptan will increase the level or effect of dutasteride by affecting hepatic/intestinal
cortisone
cortisone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
cyclosporine
cyclosporine will increase the level or effect of dutasteride by affecting hepatic/intestinal
darifenacin
darifenacin will increase the level or effect of dutasteride by affecting hepatic/intestinal
darunavir
darunavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
dasatinib
dasatinib will increase the level or effect of dutasteride by affecting hepatic/intestinal
deferasirox
deferasirox will decrease the level or effect of dutasteride by affecting hepatic/intestinal
deflazacort
deflazacort will decrease the level or effect of dutasteride by affecting hepatic/intestinal
delavirdine
delavirdine will increase the level or effect of dutasteride by affecting hepatic/intestinal
dexamethasone
dexamethasone will decrease the level or effect of dutasteride by affecting
dhea
dhea will increase the level or effect of dutasteride by affecting hepatic/intestinal enzyme
diltiazem
diltiazem will increase the level or effect of dutasteride by affecting hepatic/intestinal
dronedarone
dronedarone will increase the level or effect of dutasteride by affecting hepatic/intestinal
efavirenz
efavirenz will decrease the level or effect of dutasteride by affecting hepatic/intestinal
eslicarbazepine acetate will decrease the level or effect of dutasteride by affecting
ethotoin
ethotoin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
etravirine
etravirine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
eucalyptus
eucalyptus will decrease the level or effect of dutasteride by affecting hepatic/intestinal
fluconazole
fluconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
fludrocortisone
fludrocortisone will decrease the level or effect of dutasteride by affecting
fluvoxamine
fluvoxamine will increase the level or effect of dutasteride by affecting hepatic/intestinal
fosamprenavir
fosamprenavir will increase the level or effect of dutasteride by affecting
fosphenytoin
fosphenytoin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
grapefruit
grapefruit will increase the level or effect of dutasteride by affecting hepatic/intestinal
griseofulvin
griseofulvin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
hexobarbital
hexobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
hydrocortisone
hydrocortisone will decrease the level or effect of dutasteride by affecting
indinavir
indinavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
lapatinib
lapatinib will increase the level or effect of dutasteride by affecting hepatic/intestinal
lumefantrine
lumefantrine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
marijuana
marijuana will increase the level or effect of dutasteride by affecting hepatic/intestinal
mephobarbital
mephobarbital will decrease the level or effect of dutasteride by affecting
methylprednisolone
methylprednisolone will decrease the level or effect of dutasteride by affecting
metronidazole
metronidazole will increase the level or effect of dutasteride by affecting
mibefradil
mibefradil will increase the level or effect of dutasteride by affecting hepatic/intestinal
miconazole vaginal
miconazole vaginal will increase the level or effect of dutasteride by affecting
modafinil
modafinil will decrease the level or effect of dutasteride by affecting hepatic/intestinal
nelfinavir
nelfinavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
nevirapine
nevirapine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
nifedipine
nifedipine will increase the level or effect of dutasteride by affecting hepatic/intestinal
nilotinib
nilotinib will increase the level or effect of dutasteride by affecting hepatic/intestinal
oxcarbazepine
oxcarbazepine will decrease the level or effect of dutasteride by affecting
oxiconazole
oxiconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
pentobarbital
pentobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
phenobarbital
phenobarbital will decrease the level or effect of dutasteride by affecting
phenytoin
phenytoin will decrease the level or effect of dutasteride by affecting hepatic/intestinal
posaconazole
posaconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
prednisolone
prednisolone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
prednisone
prednisone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
primidone
primidone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
quinupristin/dalfopristin will increase the level or effect of dutasteride by affecting
rifapentine
rifapentine will decrease the level or effect of dutasteride by affecting hepatic/intestinal
ritonavir
ritonavir will increase the level or effect of dutasteride by affecting hepatic/intestinal
rufinamide
rufinamide will decrease the level or effect of dutasteride by affecting hepatic/intestinal
secobarbital
secobarbital will decrease the level or effect of dutasteride by affecting hepatic/intestinal
sitaxentan
sitaxentan will increase the level or effect of dutasteride by affecting hepatic/intestinal
telithromycin
telithromycin will increase the level or effect of dutasteride by affecting hepatic/intestinal
topiramate
topiramate will decrease the level or effect of dutasteride by affecting hepatic/intestinal
triamcinolone
triamcinolone will decrease the level or effect of dutasteride by affecting
troglitazone
troglitazone will decrease the level or effect of dutasteride by affecting hepatic/intestinal
troleandomycin
troleandomycin will increase the level or effect of dutasteride by affecting
verapamil
verapamil will increase the level or effect of dutasteride by affecting hepatic/intestinal
voriconazole
voriconazole will increase the level or effect of dutasteride by affecting hepatic/intestinal
zafirlukast
zafirlukast will increase the level or effect of dutasteride by affecting hepatic/intestinal
Adverse Effects
>10%
Orthostasis (16%)
1-10%
Ejaculation disorders (10%)
Dizziness (2%)
Breast enlargement/tenderness (3%)
Impotence (8%)
Decreased libido (4.5%)
Breast disorders (1%)
<1%
Prostate cancer (high grade)
Dutasteride
Immune system disorders: Hypersensitivity reactions, including rash, pruritus, urticaria,
localized edema, serious skin reactions, and angioedema
Psychiatric disorders: Depressed mood
Reproductive system and breast disorders: Testicular pain and testicular swelling
Tamsulosin
Immune system disorders: Hypersensitivity reactions, including rash, urticaria, pruritus,
angioedema, and respiratory problems have been reported with positive rechallenge in
some cases
Cardiac disorders: Palpitations, dyspnea, atrial fibrillation, arrhythmia, and tachycardia
Skin disorders: Skin desquamation, including Stevens-Johnson syndrome
Gastrointestinal disorders: Constipation, vomiting
Reproductive system and breast disorders: Priapism
Vascular disorders: Hypotension
Ophthalmologic disorders: During cataract surgery, a variant of small pupil syndrome
known as intraoperative floppy iris syndrome (IFIS) associated with alpha adrenergic
antagonist therapy
Contraindications
Previously demonstrated, clinically significant hypersensitivity (eg, serious skin reactions,
angioedema, urticaria, pruritus, respiratory symptoms) to dutasteride, other 5 alpha-reductase
inhibitors, or tamsulosin
Pregnancy and women of childbearing potential should not take or handle drug
Children
Cautions
Prior to initiating treatment, rule out other urological conditions
Orthostatic hypotension and/or syncope can occur
Reduces total serum prostate-specific antigen (PSA) concentration by ~50%, evaluate any
confirmed increases in PSA levels from nadir, even if those values are within normal range, for
the presence of prostate cancer
Caution patients about the possibility and seriousness of priapism
Advise patients to not donate blood until 6 months after their last dose
Intraoperative floppy iris syndrome has been observed during cataract surgery after alpha-
adrenergic antagonist exposure
Metabolized by both CYP3A4 and CYP2D6; concomitant use with known inhibitors can cause a
marked increase in plasma levels resulting in an increased incidence of adverse effects; do not
use with strong 3A4 or 2D6 inhibitors (eg, ketoconazole, paroxetine); exercise caution when
coadministered with less potent inhibitors (eg, terbinafine, erythromycin)
Coadministration with PDE-5 inhibitors (eg, sildenafil) can increase risk of hypotension
Coadministration with other alpha-antagonists (eg, doxazosin, terazosin) may cause additive
hypotension
Limited studies showed inconclusive results regarding coadministration of tamsulosin with
warfarin (monitor INR)
June 9, 2011: Recent data from 2 large, randomized, controlled trials observed an
increased risk of being diagnosed with a more serious form of prostate cancer (high-grade
prostate cancer) in trial participants taking 5-alpha reductase inhibitors (5-ARIs)
ARIs, perform appropriate evaluation to rule out other urological conditions, including
prostate cancer, that might mimic benign prostatic hyperplasia (BPH)
Pharmacology
Mechanism of Action
Dutasteride: Selective inhibitor of type 1 and type 2 isoforms of 5-alpha-reductase
Tamsulosin: Alpha-adrenergic antagonist; blocks alpha-1a adrenergic receptor in smooth muscle
of prostate, decreasing bladder neck & urethral resistance
Absorption
Bioavailability: 60% (dutasteride); 10% (tamsulosin)
Peak Plasma Time: 2-3 hr (dutasteride); 4-5 hr fasting; 6-7 hr with food (tamsulosin)
Onset: 1-2 weeks (dutasteride); 4-8 hr (tamsulosin)
Distribution
Protein Bound: 99% (dutasteride and tamsulosin)
Vd: 300-500 L (dutasteride); 0.2 L (tamsulosin)
Metabolism
Dutasteride
Metabolism: hepatic P450 enzyme CYP3A4 and CYP2D6
Metabolites, major: 4'-hydroxydutasteride, 6-hydroxydutasteride (as active as parent),
6,4'-dihydroxydutasteride
Tamsulosin
Metabolism: liver
Metabolites: glucuronide and sulfate conjugates (inactive)
Elimination
Half-Life: 5 weeks at steady state (dutasteride); 14-15 hr (tamsulosin)
Excretion: mainly feces (dutasteride); urine 76%, feces 21% (tamsulosin)
Patient Handout
560043
Patient Education
dutasteride-tamsulosin oral
DUTASTERIDE/TAMSULOSIN - ORAL
(doo-TAS-ter-ide/tam-SOO-loe-sin)
COMMON BRAND NAME(S): Jalyn
USES:
This product is used in men to treat the symptoms of an enlarged prostate (benign prostatic
hyperplasia-BPH). Dutasteride works by reducing the size of the enlarged prostate. Tamsulosin
is known as an alpha-blocker and works by relaxing muscles in the bladder and prostate. This
product helps to relieve symptoms of BPH such as difficulty in beginning the flow of urine,
weak stream, and the need to urinate frequently or urgently (including during the middle of the
night).
Dutasteride is not approved for prevention of prostate cancer. It may slightly increase the risk of
developing a very serious form of prostate cancer. Talk to your doctor about the benefits and
risks.
This medication should not be used by women or children.
HOW TO USE:
this medication and each time you get a refill. If you have any questions, ask your doctor or
pharmacist.
Take this medication by mouth as directed by your doctor, usually once daily, 30 minutes after
the same meal each day. Swallow this medication whole. Do not crush, chew, or open the
capsules.
take it at the same time each day.
Since this drug can be absorbed through the skin and may harm an unborn baby, women who are
pregnant or who may become pregnant should not handle this medication.
It may take up to 4 weeks to notice an improvement in symptoms. Tell your doctor if your
symptoms do not improve after 4 weeks or if they worsen.
SIDE EFFECTS:
Dizziness, lightheadedness, drowsiness, runny/stuffy nose, sexual problems (such as decreased
sexual interest/ability, ejaculation problems, decrease in the amount of semen/sperm), testicle
pain/swelling, increased breast size, or breast tenderness may occur. Sexual problems have
continued in some men even after stopping treatment. If any of these effects persist or worsen,
tell your doctor or pharmacist promptly.
Tell your doctor immediately if this rare but serious side effect occurs: fainting.
In the US -
800-FDA-1088.
PRECAUTIONS:
Before taking this product, tell your doctor or pharmacist if you are allergic to dutasteride or
tamsulosin; or to finasteride; or if you have any other allergies. This product may contain
inactive ingredients, which can cause allergic reactions or other problems. Talk to your
beverages.
To reduce the risk of dizziness, lightheadedness, or fainting, get up slowly when rising from a
sitting or lying position, especially when you first start taking this drug. If dizziness occurs, sit or
lie down until you feel better. Also, when you first start taking this drug, avoid situations where
you may be injured if you faint.
taking this medication and about all the products you use (including prescription drugs,
nonprescription drugs, and herbal products).
Do not donate blood while you are taking this medication and for at least 6 months after you stop
taking it. This will prevent the possibility of your blood being given to a pregnant woman.
This medication should not be used in women. This medication must not be used during
pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant,
tell your doctor immediately.
It is unknown if this medication passes into breast milk. However, this medication should not be
used in women.
DRUG INTERACTIONS:
Some products that may interact with this drug include: other alpha-blockers (such as prazosin,
terazosin), drugs to treat erectile dysfunction-ED or pulmonary hypertension (such as sildenafil,
tadalafil, vardenafil).
Other medications can affect the removal of this product from your body, which may affect how
this product works. Examples include azole antifungals (such as ketoconazole), boceprevir,
macrolide antibiotics (such as clarithromycin), nefazodone, HIV protease inhibitors (such as
ritonavir), a certain combination HIV medication
(elvitegravir/cobicistat/emtricitabine/tenofovir), telithromycin, among others.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness including
alcohol, antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as
alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as
codeine).
Check the labels on all your medicines (such as allergy or cough-and-cold products) because
they may contain ingredients that cause drowsiness. Ask your pharmacist about using those
products safely.
OVERDOSE:
NOTES:
Laboratory and/or medical tests (such as prostate exams, prostate-specific antigen-PSA) should
for more details.
MISSED DOSE:
STORAGE:
The capsules may soften and leak if stored at high temperatures. If your capsules change
color/shape or leak, do not use them. If your skin comes in contact with the deformed or leaking
capsules, wash the area immediately with soap and water. Contact your pharmacist for more
information.
URIMAX-D
Manufacturer
Contents
Pregnancy Category (US FDA)
CIMS Class
ATC Classification
Presentation/Packing

Related Information:
URIMAX-D tab Concise Info

CIMS Abbreviation Index MIMS Abbreviation Index
Manufacturer Cipla
Contents URIMAX-D tab: tamsulosin hydrochloride 0.4 mg, dutasteride 0.5 mg.
Click here to view tamsulosin + dutasteride prescribing information, dosage, adverse drug
reactions...
Pregnancy Category (US
FDA)

Category X: Studies in animals or human beings have demonstrated foetal abnormalities
or there is evidence of foetal risk based on human experience or both, and the risk of the
use of the drug in pregnant women clearly outweighs any possible benefit. The drug is
contraindicated in women who are or may become pregnant.
CIMS Class Drugs for Bladder & Prostate Disorders
ATC Classification G04CA02 - tamsulosin ; Belongs to the class of alpha-adrenoreceptor antagonists. Used in
the treatment of benign prostatic hypertrophy.
G04CB02 - dutasteride ; Belongs to the class of testosterone-5-alpha reductase inhibitors.
Used in the treatment of benign prostatic hypertrophy.

Urimax Overview
Hyoscyamine (also known as daturine) is a tropane alkaloid. It is a secondary metabolite found
in certain plants of the Solanaceae family, including henbane (Hyoscyamus niger), mandrake
(Mandragora officinarum), jimsonweed (Datura stramonium), tomato (Solanum lycopersicum)
and deadly nightshade (Atropa belladonna). It is the levorotary isomer of atropine (third of the
three major nightshade alkaloids) and thus sometimes known as levo-atropine. Hyoscyamine
should not be confused with hyoscine,...

Urimax delayed-release tablets
Generic Name: hyoscyamine/methenamine/methylene blue/phenyl salicylate/sodium biphosphate
(hye-oh-SYE-a-meen/meth-EN-a-meen/METH-i-leen/FEN-ill sa-LI-si-late/SOE-dee-um bye-FOS-
fate)
Brand Name: Urimax and Utira
Overview
Side Effects
Dosage
Interactions
More
o User Reviews
o Support Group Q & A
Urimax delayed-release tablets is used for:
Treating painful and irritating symptoms of the urinary tract due to urinary tract infections or
diagnostic procedures.
Urimax delayed-release tablets is a urinary antiseptic, urinary acidifier, analgesic, and anticholinergic
combination. It works by helping to kill bacteria in the urine, decreasing pain and inflammation, and
reducing muscle spasms in the urinary tract. These actions work together to help relieve discomfort
while urinating.
Do NOT use Urimax delayed-release tablets if:
you are allergic to any ingredient in Urimax delayed-release tablets
you have had a severe allergic reaction (eg, severe rash, hives, difficulty breathing, dizziness) to
aspirin, other salicylate medicines, or a nonsteroidal anti-inflammatory drug (NSAID) (eg,
ibuprofen, naproxen, celecoxib)
you have angle-closure glaucoma, problems with your esophagus, bowel motility problems, a
blockage of your bladder or bowel, severe intestinal problems (eg, ulcerative colitis), severe
bleeding, flu or chickenpox, myasthenia gravis, severe kidney problems, or you are severely
dehydrated
you are taking a sulfonamide (eg, sulfamethoxazole)
Contact your doctor or health care provider right away if any of these apply to you.
Slideshow: 18 Herbal Supplements with Risky Drug Interactions

Herbal and Dietary Supplements Deserve Your Attention
Before using Urimax delayed-release tablets:
Some medical conditions may interact with Urimax delayed-release tablets. Tell your doctor or
pharmacist if you have any medical conditions, especially if any of the following apply to you:
if you are pregnant, planning to become pregnant, or are breast-feeding
if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary
supplement
if you have allergies to medicines, foods, or other substances
if you have constipation, diarrhea, an infection of the stomach or bowel, a hiatal hernia, or
stomach ulcers
if you have nervous system problems, glucose-6-phosphate dehydrogenase (G-6-PD)
deficiency, gout, influenza, Kawasaki syndrome, rheumatic disease, open-angle glaucoma, risk
factors for angle-closure glaucoma, kidney or liver problems, an enlarged prostate, bladder
problems, or you are unable to urinate
if you have a history of stroke or brain blood vessel problems (eg, aneurysm), an irregular
heartbeat, heart blood vessel problems, congestive heart failure, heart valve problems, or other
heart problems
if you are on a low-salt diet
Some MEDICINES MAY INTERACT with Urimax delayed-release tablets. Tell your health care
provider if you are taking any other medicines, especially any of the following:
Anticholinergics (eg, benztropine) because they may increase the risk of Urimax delayed-
release tablets's side effects.
Ketoconazole because it may decrease Urimax delayed-release tablets's effectiveness.
Monoamine oxidase inhibitors (MAOIs) or narcotic pain medicine (eg, codeine) because the risk
of serious side effects may be increased
Medicine for myasthenia gravis (eg, ambenonium), phenothiazines (eg, chlorpromazine),
sulfonamides (eg, sulfamethoxazole), thiazide diuretics (eg, hydrochlorothiazide), or urinary
alkalinizers (eg, sodium bicarbonate) because their effectiveness may be decreased by Urimax
delayed-release tablets
This may not be a complete list of all interactions that may occur. Ask your health care provider if
Urimax delayed-release tablets may interact with other medicines that you take. Check with your
health care provider before you start, stop, or change the dose of any medicine.
How to use Urimax delayed-release tablets:
Use Urimax delayed-release tablets as directed by your doctor. Check the label on the medicine for
exact dosing instructions.
Take Urimax delayed-release tablets by mouth with or without food.
Swallow Urimax delayed-release tablets whole. Do not break, crush, or chew before swallowing.
Do not take antacids or antidiarrheal medicines that has loperamide within 1 hour before or 2
hours after you take Urimax delayed-release tablets.
Drinking extra fluids while you are taking Urimax delayed-release tablets is recommended.
Check with your doctor for instructions.
If you miss a dose of Urimax delayed-release tablets, take it as soon as possible. If it is almost
time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do
not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Urimax delayed-
release tablets.
Important safety information:
Urimax delayed-release tablets may cause dizziness. These effects may be worse if you take it
with alcohol or certain medicines. Use Urimax delayed-release tablets with caution. Do not drive
or perform other possibly unsafe tasks until you know how you react to it.
Do NOT take more than the recommended dose or use for more often than prescribed without
checking with your doctor.
Urimax delayed-release tablets may discolor the urine or stools a blue-green color. This is
normal and not a cause for concern.
Urimax delayed-release tablets contains salicylate. Salicylates have been linked to a serious
illness called Reye syndrome. Do not give Urimax delayed-release tablets to a child or teenager
who has the flu, chickenpox, or a viral infection. Contact your doctor with any questions or
concerns.
Use Urimax delayed-release tablets with caution in the ELDERLY; they may be more sensitive
to its effects, especially excitement, agitation, drowsiness, and confusion.
Urimax delayed-release tablets should not be used in CHILDREN younger than 6 years old;
safety and effectiveness in these children have not been confirmed.
PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will
need to discuss the benefits and risks of using Urimax delayed-release tablets while you are
pregnant. Urimax delayed-release tablets is found in breast milk. If you are or will be breast-
feeding while you use Urimax delayed-release tablets, check with your doctor. Discuss any
possible risks to your baby.
Possible side effects of Urimax delayed-release tablets:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with
your doctor if any of these most COMMON side effects persist or become bothersome:
Dry mouth; flushing; nausea; vomiting.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of
the mouth, face, lips, or tongue); blurred vision; difficulty urinating; dizziness; fast or irregular
heartbeat.
This is not a complete list of all side effects that may occur. If you have questions about side effects,
contact your health care provider. Call your doctor for medical advice about side effects. To report
side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.
If OVERDOSE is suspected:
Proper storage of Urimax delayed-release tablets:
Store Urimax delayed-release tablets between 68 and 77 degrees F (20 and 25 degrees C). Brief
storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store
away from heat, moisture, and light. Do not store in the bathroom. Keep Urimax delayed-release
tablets out of the reach of children and away from pets.
General information:
If you have any questions about Urimax delayed-release tablets, please talk with your doctor,
pharmacist, or other health care provider.
Urimax delayed-release tablets is to be used only by the patient for whom it is prescribed. Do
not share it with other people.
If your symptoms do not improve or if they become worse, check with your doctor.
Check with your pharmacist about how to dispose of unused medicine.
This information is a summary only. It does not contain all information about Urimax delayed-release
tablets. If you have questions about the medicine you are taking or would like more information,
check with your doctor, pharmacist, or other health care provider.
Issue Date: July 2, 2014
Database Edition 14.3.1.001
Copyright 2014 Wolters Kluwer Health, Inc.
More about Urimax (hyoscyamine / methenamine / methylene
blue / phenyl salicylate)
Related treatment guides
Urinary Tract Infection

Reviews
Average User Rating
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Drug Class
Urinary antispasmodics
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medical advice, diagnosis or treatment.
Data sources include Micromedex (updated Aug 13th, 2014), Cerner Multum (updated Aug 17th, 2014), Wolters
Kluwer (updated Aug 4th, 2014) and others. To view content sources and attributions, refer to our editorial policy.
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