Anti-hypertensive drugs

 Alpha blockers

 Alpha-blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of

pharmacological agents that act as antagonists on α-adrenergic receptors (α-
adrenoceptors)

MECHANISM OF ACTION

 The α1-adrenoceptor blockers produce vasodilatation by blocking the action of noradrenaline at

post-synaptic α1 receptors in both arteries and veins. This results in a fall in peripheral
resistance, without a compensatory rise in cardiac output. The prototype α1-blocker —
prazosin — is short acting and tends to produce precipitous falls in blood Pressure.

INDICATION

Doctors prescribe alpha blockers to prevent, treat or improve symptoms mainly in these
conditions:

 Pheochromocytoma
 Congestive heart failure
 Erectile dysfunction
 Benign prostatic hyperplasia
 Raynaud's disease
 Post traumatic stress disorder

Contraindications

 There is only one compelling indication for alpha blockers, which is for benign prostatic
hyperplasia.
 Patients who need alpha blockers for BPH, but have a history of hypotension or postural heart
failure, should use these drugs with caution, as it may result in an even greater decrease in
blood pressure or make heart failure even worse.
 The most compelling contraindication is urinary incontinence and overall fluid retention.
 To combat such fluid retention, patients can take a diuretic in combination with the alpha-
blocker.

 In the absence of compelling indications or contraindications, patients should take alpha

blockers as a step 4 therapy to reduce blood pressure, but only if the use of ACE inhibitors,
angiotensin-II receptor blockers, calcium channel blockers, or thazide diuretics (in full dose or in
combinations) have not been efficacious
 Drug interactions

 alpha blockers that are used for the reduction of blood pressure, such as phenoxybenzamine or
phentolamine can have synergy with other drugs that affect smooth muscle, blood vessels, or
drugs used for erectile dysfunction (i.e. sildenafil, tamsulosin, etc.). This stimulates exaggerated
hypotension.
 Alternative alpha blockers, such as prazosin, tamsulosin, doxazosin, or terazosin can have
adverse interactions with beta blockers, erectile dysfunction drugs, anxiolytics, and
antihistamines.
 These interactions can cause dangerous hypotension. Furthermore, in rare cases, drug
interactions can cause irregular, rapid heartbeats or an increase blood pressure.
 Yohimbine can interact with stimulants, hypertension drugs, naloxone, and clonidine.
Interactions with such drugs can cause either an unintended increase in blood pressure or
potentiate an increase in blood pressure.
 Finally, in drugs with both alpha and beta blocking properties, such as carvedilol and labetalol,
interactions with other alpha or beta blockers can exaggerate a decrease in blood pressure.
 there are also drug interactions with carvedilol or labetalol in which blood pressure is increased
unintentionally (such as with cough and cold medications).
 Finally there may also be some alpha/beta blocker drug interactions that can worsen previous
heart failure.

SIDE EFFECT/ADVERSE EFFECT

 Prazosin causes postural hypotension – start 0.5 mg at bed time with increasing dose and upto
10 mg daily, Fluid retention in monotherapy, Headache, dry mouth, weakness, dry mouth,
blurred vision, rash, drowsiness ,failure of ejaculation in males.

Other side effects might include:

 Pounding heartbeat
 Weight gain

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and
examination:

 Assess for contraindications or cautions (e.g. history of allergy to drug, heart blocks,
asthma, pregnancy or lactation status, etc.) to avoid adverse effects.
  Establish baseline physical assessment to monitor for any potential adverse effects.
 Assess the level of orientation and for any complaints of dizziness, paresthesias, or
vertigo to monitor CNS drug effects.
 Assess vital signs, especially pulse and blood pressure to monitor for possible excess
stimulation of the cardiac system.
 Note respiratory rate and auscultate lungs for adventitious sounds to evaluate effects on
bronchi and respirations.
 Monitor laboratory test results (e.g. liver and renal function tests) to determine need for
possible dose adjustment, serum electrolyte levels to evaluate fluid loss and
appropriateness of therapy, and blood glucose to evaluate for hyper- or hypoglycemia.
 Nursing Diagnoses

These are vital nursing interventions done in patients who are taking nonselective adrenergic
antagonists:

 Do not discontinue abruptly after chronic therapy because hypersensitivity to

catecholamines may develop and patient could have severe reaction; taper drug slowly
over two weeks, monitoring the patient.
 Educate patient about positive lifestyle changes (e.g. diet, exercise, smoking cessation)
to aid in lowering blood pressure.
 Assess heart rate for changes that might suggest arrhythmia. Obtain blood pressure in
various positions to assess for orthostatic hypotension.
 Monitor GI function and need for increased access to bathroom facilities and need for
increased fluid intake related to diarrhea.
 Provide comfort measures to help patient cope with drug effects.
 Provide patient education about drug effects and warning signs to report to enhance
knowledge about drug therapy and promote compliance.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:

 Monitor patient response to therapy (improvement in blood pressure and heart failure).
 Monitor for adverse effects (e.g. CV changes, headache, GI upset, liver failure).
 Evaluate patient understanding on drug therapy by asking patient to name the drug, its
indication, and adverse effects to watch for.
 Monitor patient compliance to drug therapy.
 Classification
 α1-blockers act on α1-adrenoceptors
 α2-blockers act on α2-adrenoceptors

When the term "alpha blocker" is used without further qualification, it can refer to an α1 blocker, an α2
blocker, a nonselective blocker (both α1 and α2 activity), or an α blocker with some β activity.

However, the most common type of alpha blocker is usually an α1 blocker.

Non-selective α-adrenergic receptor antagonists include:

 Phenoxybenzamine
 Phentolamine
 Tolazoline
 Trazodone

Selective α1-adrenergic receptor antagonists include:

 Alfuzosin
 Doxazosin
 Prazosin (inverse agonist)
 Tamsulosin
 Terazosin
 Silodosin

Selective α2-adrenergic receptor antagonists include:

 Atipamezole
 Idazoxan
 Mirtazapine
 Yohimbine

Non-selective α-adrenergic receptor antagonists

1. PHENOXYBENZAMINE HYDROCHLORIDE

Brand name: Dibenzyline

Classifications: AUTONOMIC NERVOUS SYSTEM AGENT; ALPHA-ADRENERGIC ANTAGONIST (BLOCKING

AGENT), SYMPATHOLYTIC; ANTIHYPERTENSIVE AGENT

Prototype: Prazosin
Pregnancy Category: C

Availability

10 mg capsules

Actions

Long-acting alpha-adrenergic blocking agent. Apparently produces noncompetitive blockade of alpha-

adrenergic receptor sites at postganglionic synapse. Alpha-receptor sites are thus unable to react to
endogenous or exogenous sympathomimetic agents.

Therapeutic Effects

Blocks excitatory effects of epinephrine, including vasoconstriction, but does not affect adrenergic
cardiac inhibitory actions. It produces a "chemical sympathectomy" and it can maintain it. Causes
orthostatic hypotension in both normotensive and hypertensive patients.

Uses

Management of pheochromocytoma.

Unlabeled Uses

To improve circulation in peripheral vasospastic conditions such as Raynaud's acrocyanosis and frostbite
sequelae, for adjunctive treatment of shock, hypertensive crisis.

Contraindications

Instances when fall in BP would be dangerous; compensated congestive heart failure; pregnancy
(category C), lactation.

Cautious Use

Marked cerebral or coronary arteriosclerosis, CHF; renal insufficiency; respiratory infections.

Route & Dosage

Management of Pheochromocytoma

Adult: PO 5–10 mg b.i.d., may increase by 10 mg/d at 4-d intervals to desired response (usual range 20–
60 mg/d in 2–3 divided doses)

Child: PO 0.2 mg/kg/d in 1–2 divided doses, may increase by 0.2 mg/kg/d at 4 d intervals to desired
response (usual range 0.4–1.2 mg/kg/d)

Administration

Oral

Give with milk or in divided doses to reduce gastric irritation.

Preserve in airtight containers protected from light.

Adverse Effects (1%)

Body as a Whole: Dizziness, fainting, drowsiness, sedation, tiredness, weakness, lethargy, confusion,
headache, shock. CNS: CNS stimulation (large doses). CV: Postural hypotension, tachycardia, palpitation.
GI: Dry mouth. Urogenital: Inhibition of ejaculation. Respiratory: Nasal congestion. Skin: Allergic contact
dermatitis. Special Senses: Miosis, drooping of eyelids.

Interactions

Drug: inhibits effects of methoxamine, norepinephrine, phenylephrine; additive hypotensive effects with
ANTIHYPERTENSIVES.

Pharmacokinetics

Absorption: Variably absorbed (approximately 30%) from GI tract. Onset: 2 h. Peak: 4–6 h. Duration: 3–4
d. Distribution: Accumulates in adipose tissue. Elimination: 80% excreted in urine and bile within 24 h.
Half-Life: 24 h.

Nursing Implications

Assessment & Drug Effects

Monitor BP and note pulse quality, rate, and rhythm in recumbent and standing positions during period
of dosage adjustment. Observe patient closely for at least 4 d from one dosage increment to the next;
hypotension and tachycardia are most likely to occur in standing position.

Drug has cumulative action, thus onset of therapeutic effects may not occur until after 2 wk of therapy,
and full therapeutic effects may not be apparent for several more weeks.

Patient & Family Education

Make position changes slowly, particularly from reclining to upright posture, and dangle legs and
exercise ankles and feet for a few minutes before standing.

Be aware that light headedness, dizziness, and palpitations usually disappear with continued therapy but
may reappear under conditions that promote vasodilation, such as strenuous exercise or ingestion of a
large meal or alcohol.

Pupil constriction, nasal stuffiness, and inhibition of ejaculation generally decrease with continued
therapy.

Do not take OTC medications for coughs, colds, or allergy without approval of physician. Many contain
agents that cause BP elevation.

2. Phentolamine(Regitine)
Phentolamine is used to reverse numbness after dental procedures as well as several other uses. This
medication may be injected into the gums, a vein, or a muscle depending on the condition treated.

Phentolamine is a prescription medication used to reverse numbness after oral and dental procedures,
to prevent and control episodes of dangerously high blood pressure, to prevent and treat accidental
injection of certain drugs under the skin, and also to diagnose a condition called pheochromocytoma.

Phentolamine belongs to a group of medications called vasodilators. These drugs work by causing blood
vessels to expand and allow more blood to flow through them.

Phentolamine is available in an injectable form to be given by a healthcare professional directly into

tissue of the mouth, a muscle, or a vein depending on the condition being treated or diagnosed.

Common side effects of phentolamine include injection site pain, headache, and changes in heart rate.

Phentolamine can also cause dizziness. Do not drive or operate heavy machinery until you know how
phentolamine affects you.

Uses of Phentolamine

Phentolamine is used to reverse numbness after various oral and dental procedures, to prevent and
control episodes of severely high blood pressure, to prevent and treat death of skin tissue in the event
of accidental injection of norepinephrine under the skin, and also to diagnose pheochromocytoma.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Phentolamine Brand Names

Phentolamine may be found in some form under the following brand names:

Common side effects of phentolamine include:

 injection site pain

 dizziness
 nausea
 vomiting
 skin flushing (redness and warmth)
 diarrhea
 weakness
 headache
 change in heart rate

This is not a complete list of phentolamine side effects. Ask your doctor or pharmacist for more
information.
Phentolamine Interactions

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines,
vitamins, and herbal supplements.

Phentolamine Precautions

Serious side effects have been reported with phentolamine including the following:

Altered heart rate. Notify your healthcare provider immediately if you feel like your heart rate is
changing as this may be a sign of a potentially serious side effect of phentolamine.

Strokes. Consult with your physician about your risk for strokes while using phentolamine and if you
have a family history of strokes.

Heart attacks. Consult with your physician about your risk for heart attacks while using phentolamine
and if you have a family history of heart disease.

Severe chest pain. Notify your healthcare provider immediately if you experience severe chest pain.

Loss of conciousness due to extremely low blood pressure. Notify your healthcare provider if you have a
history of low blood pressure before using phentolamine.

Do not take phentolamine if you:

 are allergic to phentolamine or to any of its ingredients

 have a history of heart attacks or severe heart disease
 Phentolamine can also cause dizziness. Do not drive or operate heavy machinery until you know
how phentolamine affects you.

Phentolamine Food Interactions

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may
advise you to avoid certain foods. In the case of phentolamine, garlic and licorice should be avoided.

Inform MD

Before taking phentolamine, tell your doctor about all of your medical conditions. Especially tell your
doctor if you:
  are allergic to phentolamine or to any of its ingredients
 have heart disease and/or a history of heart attacks
 are pregnant or plan to become pregnant
 are breastfeeding or plan to breastfeed
 have altered heart rhythms (arrhythmias) such as atrial fibrillation (Afib)
 Tell your doctor about all the medicines you take including prescription and non-prescription
medicines, vitamins, and herbal supplement

3. Tolazoline

Uses of Tolazoline

Tolazoline is used in the treatment of:

 Arteriosclerosis Obliterans
 Causalgia
 Peripheral Vascular Diseases
 Persistent Fetal Circulation Syndrome
 Raynaud Disease
 Scleroderma, Systemic
 Spasm
 Thromboangiitis Obliterans
 Thrombophlebitis

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Tolazoline Brand Names

Tolazoline may be found in some form under the following brand names:

 Priscoline Hydrochloride

Tolazoline Drug Class

 Tolazoline is part of the drug classes:

 Imidazoline derivatives
 Other topical products for joint and muscular pain

Tolazoline Interactions

This is not a complete list of Tolazoline drug interactions. Ask your doctor or pharmacist for more
information.
Tolazoline and Pregnancy

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D,
and X, are used to classify the possible risks to an unborn baby when a medication is taken during
pregnancy.

Tolazoline falls into category C:

In animal studies, pregnant animals were given this medication and had some babies born with
problems. No well-controlled studies have been done in humans, though. Therefore, this medication
may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

OR

There are no well-controlled studies that have been done in pregnant women. Tolazoline should be used
during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

OR

No studies have been done in animals, and no well-controlled studies have been done in pregnant
women. Tolazoline should be given to a pregnant woman only if clearly needed.

Tolazoline Dosage

Take tolazoline exactly as prescribed by your doctor. Follow the directions on your prescription label
carefully.

Tolazoline is available in the following doses:

Tolazoline 25 Mg/ml Intravenous Solution

Forms of Medication

Tolazoline is available in the following forms:

 Injectable Solution
 Oral Tablet

4. Trazodone

Mechanism of action

 Trazodone is an oral antidepressant drug that affects the chemical messengers

(neurotransmitters) within the brain that nerves use to communicate with (stimulate) each
other. The major neurotransmitters are acetylcholine, norepinephrine, dopamine and serotonin.
Many experts believe that an imbalance among the different neurotransmitters is the cause of
depression. Although the exact mechanism of action of trazodone is unknown, it probably
improves symptoms of depression by inhibiting the uptake of serotonin by nerves in the brain.
This results in more serotonin to stimulate other nerves.
  Trazodone also may increase directly the action of serotonin. Trazodone is chemically unrelated
to the selective serotonin reuptake inhibitors (SSRIs), the tricyclic antidepressants (TCAs) or the
monoamine oxidase inhibitors (MAO inhibitors). It is chemically related to nefazodone (Serzone)
and shares its actions. The FDA approved razodone in 1981.

Uses

 Trazodone is approved for the treatment of major depression. However, it is most commonly
used for treating insomnia. Trazodone is also used off-label for treating:
 Cocaine withdrawal
 Alcohol withdrawal
 Prevention of migraine

Side effects

The most common side effects associated with trazodone are:

 Nausea
 Vomiting
 Dizziness
 Insomnia
 Agitation
 Tiredness
 Dry mouth
 Constipation
 Weight change
 Decreased libido
 Priapism, (including clitoral priapism in women) a painful condition in which the penis (or
clitoris) remains in an erect position for a prolonged period has been reported in people taking
trazodone. Priapism occasionally results in permanent impairment of erectile function or
impotence. Patients should be warned of the possibility of priapism and told to discontinue the
drug at once and consult with their doctor if this reaction occurs.
 Trazodone may affect ejaculation, orgasm, and libido.
 Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term
studies in children and adolescents with depression and other psychiatric disorders. Anyone
considering the use of trazodone or any other antidepressant in a child or adolescent must
balance this risk with the clinical need. Patients who are started on therapy should be closely
observed for clinical worsening, suicidality, or unusual changes in behavior.

Dosage

 For the treatment of depression, the dose for adults is 150-600 mg per day of regular tablets.
 The initial starting dose usually is 150 mg per day, which is increased by 50 mg/day every 3-7
days.
  Trazodone regular tablets are given in one or more daily doses, sometimes with the largest dose
at night.
 The dose of extended release tablets are 150 mg at bedtime initially which is increased by 75
mg/day every 3 days. Extended release tablets should be swallowed whole and not crushed or
chewed. The maximum dose is 375 mg daily.
 As with all antidepressants, it may take several weeks for the full effects of treatment to be
seen. Doses often are adjusted slowly upwards to find the optimal dose.
 Elderly patients and debilitated persons may need lower doses.
 Trazodone should be taken after a meal or light snack to reduce the risk of dizziness. Food also
increases the amount of drug absorbed into the body.
 Doses of 25-75 mg are prescribed for insomnia.

Drug Interaction

 All antidepressants that increase concentrations of serotonin in the brain, including trazodone,
should not be taken with MAO-inhibitors. Drugs in the MAO-inhibitor class include:
 isocarboxazid (Marplan)
 phenelzine (Nardil)
 tranylcypromine (Parnate)
 procarbazine (Matulane)

 Drugs in the MAOI class of drugs can lead to confusion, high blood pressure, and tremor. This
same type of interaction may occur when trazodone is used with selegiline (Eldepryl). If a
patient is switched from trazodone to an MAO inhibitor, allow at least one week after stopping
trazodone before taking the MAO inhibitor.
 Increased blood concentrations of digoxin (Lanoxin) and phenytoin (Dilantin) have been
reported in persons taking trazodone due to a decrease in the metabolism (break-down and
elimination) of these drugs by trazodone.
 Carbamazepine (Tegretol) may decrease blood levels of trazodone by increasing its elimination
from the body. Ketoconazole (Nizoral), ritonavir (Norvir), and indinavir (Crixivan) inhibit the
breakdown of trazodone leading to increased blood levels of trazodone and potential side
effects.

 Drugs that increase serotonin may cause bleeding. Therefore, combining trazodone with aspirin,
nonsteroidal anti-inflammatory drugs, warfarin (Coumadin, Jantoven), or other drugs that affect
bleeding may increase the likelihood of upper gastrointestinal bleeding.

Selective α1-adrenergic receptor antagonists include:

1. Alfuzosin
 Brand Name: Uroxatral

Uses of Alfuzosin:

 In men, it is used to treat the signs of an enlarged prostate.

Dosage/administration
 Take alfuzosin with food with the same meal each day.
 Swallow whole. Do not chew, break, or crush.
 Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.
 To gain the most benefit, do not miss doses.

 Take a missed dose as soon as you think about it.

 If it is close to the time for your next dose, skip the missed dose and go back to your normal
time.
 Do not take 2 doses at the same time or extra doses.

Side effects

 Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with
or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or
talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
 Very bad dizziness or passing out.
 Chest pain that is new or worse.
 Call your doctor right away if you have a painful erection (hard penis) or an erection that lasts
for longer than 4 hours. This may happen even when you are not having sex. If this is not treated
right away, it may lead to lasting sex problems and you may not be able to have sex.

 Dizziness.
 Headache.
 Feeling tired or weak.

If OVERDOSE is suspected:

 If you think there has been an overdose, call your poison control center or get medical care
right away. Be ready to tell or show what was taken, how much, and when it happened.

Storage

 Store at room temperature.

 Protect from light.
 Store in a dry place. Do not store in a bathroom.
 2. DOXAZOSIN
Brand Name: Cardura, Cardura XL, Doxadura

Drug Class: BPH, Alpha Blockers

USES

Doxazosin is a prescription drug indicated for the treatment of hypertension, to lower blood pressure.
Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes
and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs
from a wide variety of pharmacologic classes, including this drug.

 Doxazosin is available under the following different brand names: Cardura, Cardura XL, and
Doxadura.

Dosages of Doxazosin:

Adult and Pediatric Dosages Dosage Forms and Strengths

Tablets

1 mg,2 mg, 4 mg, 8 mg

Tablet, extended release (adult dosage only)4 mg, 8 mg

Adult Dosage:

Immediate release: 1-16 mg orally once daily in the morning or at night

Extended release: not indicated for hypertension

Geriatric Dosage:

 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 orally once daily in the morning or at night
 Extended release: not indicated for hypertension
 Pediatric Dosage: (off-label)

Immediate release: 1-4 mg orally once daily in the morning or at night

Benign Prostatic Hyperplasia

Adult and Geriatric Dosage:

Immediate release: 1-8 mg/day orally

Extended release: 4 mg/day orally initially at breakfast; may be increased to no more than 8 mg/day
orally

Dosing Modifications

 Liver (hepatic) impairment: Use with caution in mild-to-moderate hepatic dysfunction; do not
use in severe impairment

SIDE EFFECTS

 a light-headed feeling, like you might pass out

 severe ongoing stomach pain or bloating
 new or worsening chest pain
 trouble breathing
 a penis erection that is painful or lasts 4 hours or longer.
 Common doxazosin side effects may include:
 low blood pressure, dizziness
 drowsiness
 headache
 feeling weak or tired

3. Prazosin
4. Brand Name: Minipress

Uses of Prazosin:

 It is used to treat high blood pressure.

 It may be given to you for other reasons. Talk with the doctor.
 What do I need to tell my doctor BEFORE I take Prazosin?
 If you have an allergy to prazosin or any other part of prazosin.
 If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell
your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of
breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.

This medicine may interact with other drugs or health problems.

 Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products,
vitamins) and health problems. You must check to make sure that it is safe for you to take
prazosin with all of your drugs and health problems. Do not start, stop, or change the dose of
any drug without checking with your doctor.

Administration
  Take with or without food.
 Keep taking prazosin as you have been told by your doctor or other health care provider, even if
you feel well.
 To gain the most benefit, do not miss doses.

 Take a missed dose as soon as you think about it.

 If it is close to the time for your next dose, skip the missed dose and go back to your normal
time.
 Do not take 2 doses at the same time or extra doses.

Side effects

 Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with
or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or
talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

 Very bad dizziness or passing out.

 Blurred eyesight.
 A fast heartbeat.
 A heartbeat that does not feel normal.
 Low mood (depression).
 Shortness of breath.
 Swelling in the arms or legs.
Call your doctor right away if you have a painful erection (hard penis) or an erection that lasts for longer
than 4 hours. This may happen even when you are not having sex. If this is not treated right away, it may
lead to lasting sex problems and you may not be able to have sex.

What are some other side effects of Prazosin?

 Dizziness.
 Feeling sleepy.
 Feeling tired or weak.
 Headache.
 Upset stomach.

5. Tamsulosin
COMMON BRAND(S): Flomax

Therapeutic actions: Blocks the smooth muscle alpha1-adrenergic receptors in the prostate, prostatic
capsule, prostatic urethra, and bladder neck, leading to relaxation of the bladder and prostate and
improving the flow of urine in cases of benign prostatic hypertrophy. I

Indications

 Treatment of the signs and symptoms of benign prostatic hyper

 Uses
 Tamsulosin is used by 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 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 often or urgently (including during the middle of the night).

Drug interactions
 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.
 Other medications can affect the removal of tamsulosin from your body, which may affect how
tamsulosin works. Examples include azole antifungals (such as itraconazole, ketoconazole),
boceprevir, clarithromycin, cobicistat, HIV protease inhibitors (such as lopinavir, ritonavir),
ribociclib, among others.

Dosages

Available forms: Capsules\u20140.4 mg

ADULTS 0.4 mg PO daily 30 min after the same meal each day; if response is not satisfactory in
2u2013 4 wk, dosage may be increased to 0.8 mg PO daily 30 min after the same meal each day.
PEDIATRIC PATIENTS Safety and efficacy not established.

6. Terazosin
Brand Names: Hytrin

USES
 used to treat hypertension (high blood pressure), or to improve urination in men with benign
prostatic hyperplasia (enlarged prostate).

Dosage

 Applies to the following strengths: 1 mg; 2 mg; 5 mg; 10 mg

 Usual Adult Dose for Hypertension
Initial dose: 1 mg orally once a day at bedtime
Maintenance dose: 1 to 5 mg orally once a day.
Maximum dose: 20 mg per day.
 Usual Adult Dose for Benign Prostatic Hyperplasia
Initial dose: 1 mg orally once a day at bedtime.
Maintenance dose: Increased in a stepwise fashion to 2 mg, 5 mg, or 10 mg once a day to
achieve desired improvement of symptoms.
SIDE EFFECTS:
  Commonly reported side effects of terazosin include: dizziness. Other side effects include:
asthenia, headache, and peripheral edema.
 More Common: Dizziness

7. Silodosin(Rapaflo)
DOSAGE & INDICATIONS

For the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH).

NOTE: Silodosin is not indicated for the treatment of hypertension.

Oral dosage

Adults
 8 mg PO once daily with a meal.
Geriatric
 Elderly patients may be more sensitive to the effects of silodosin. Adjust dosage based
on clinical response.

MAXIMUM DOSAGE

Adults
 8 mg/day PO.

Elderly
 8 mg/day PO.

Adolescents
 Safety and efficacy have not been established.

Children
 Safety and efficacy have not been established.

Oral Administration
 Administer with a meal.
 Oral Solid Formulations
 Swallow the capsule intact; do not chew or crush.
 Alternatively, the capsule may be opened and the entire contents sprinkled over 1
tablespoonful (15 ml) of applesauce; do NOT sprinkle contents over hot applesauce or
any other food or beverage. Do not subdivide capsule contents. The dose should be
swallowed immediately (within 5 minutes) without chewing and followed by an 8
ounce (240 ml) glass of water.

CONTRAINDICATIONS / PRECAUTIONS
  Silodosin is contraindicated in patients with a hypersensitivity to the drug or any of the
formulation ingredients

AVERSE EFFECTS
Retrograde ejaculation, 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%)

Selective α2-adrenergic receptor antagonists include:

1. Atipamezole (brand name Antisedan)

 a synthetic α2 adrenergic receptor antagonist indicated for the reversal of the sedative and
analgesic effects of dexmedetomidine and medetomidine in dogs. Its reversal effect works by
competing with the sedative for α2-adrenergic receptors and displacing them. It is mainly used
in veterinary medicine, and while it is only licensed for dogs and for intramuscular use, it has
been used intravenously, as well as in cats and other animals.
Mechanism of action

The structures of dexmedetomidine and atipamezole, with the similarities in blue.

 Atipamezole is a competitive antagonist at ɑ2-adrenergic receptors that competes with
dexmedetomidine, an ɑ2-adrenergic receptors agonist. It does not directly interact with
dexmedetomidine; rather, their structural similarity allows atipamezole to easily compete for
receptor binding sites.
 Atipamezole reverses analgesia by blocking norepinephrine feedback inhibition on nociceptors.

Medical uses

 Atipamezole is a veterinary drug whose prime purpose is to reverse the effects of the sedative
dexmedetomidine (as well as its racemic mixture, medetomidine)
 It can also be used to reverse the related sedative xylazine.
 While it reverses both the sedative and analgesic (pain-relieving) effects of dexmedetomidine,
atipamezole may not entirely reverse the cardiovascular depression that dexmedetomidine
causes.

Available forms
 Atipamezole is sold at 5 mg/mL for ease of use: 5 times as much atipamezole as medetomidine
is needed for full reversal, and because medetomidine is sold as 1 mg/mL, 1 mL of atipamezole
reverses 1 mL of medetomidine.
 When the enantiomerically pure version of medetomidine (dexmedetomidine) was released, it
was sold at 0.5 mg/mL, because it was twice as strong as medetomidine. As such, 1 mL of
atipamezole also reverses 1 mL of dexmedetomidine.
Contraindications
 While there are no absolute contraindications to atipamezole, it is recommended against being
given with anticholinergics, as both can cause dramatic increases in heart rate.
Side effects
 Atipamezole's low rate of side effects is due to its high specificity for ɑ2-adrenergic receptors; it
has very little affinity for ɑ1-adrenergic receptors and no affinity for most serotonin, muscarinic,
and dopamine receptors.
 There is occasional vomiting, hypersalivation, and diarrhea. It can potentially cause CNS
excitement, which can lead to tremors, tachycardia (increased heart rate), and vasodilation. The
vasodilation leads to a transient decrease in blood pressure, which (in dogs) increases to normal
within 10 minutes.
 There have been reports of transient hypoxemia.
 The chance of side effect can be minimized by administering atipamezole slowly.

2. Idazoxan

Description
 Idazoxan (INN) is a drug which is used in scientific research. It acts as both a selective α2
adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.

 Idazoxan is a benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens

at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group. It has a role as an
alpha-adrenergic antagonist. It is a benzodioxine and a member of imidazolines.
 Idazoxan has been used in trials studying the basic science of Molecular Imaging, Alzheimer
Disease, and Major Depressive Disorder.
 It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the
imidazoline receptor.
 it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor
antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by
enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area
thought to be involved in the pathogenesis of schizophrenia.

3. Mirtazapine
Brand Names: Remeron, Remeron SolTab

Uses
 Mirtazapine is used to treat depression. It improves mood and feelings of well-being.
Mirtazapine is an antidepressant that works by restoring the balance of natural chemicals
(neurotransmitters) in the brain.

 Mirtazapine is used to treat major depressive disorder.

Dosage: Applies to the following strengths: 15 mg; 30 mg; 45 mg; 7.5 mg

Usual Adult Dose for Depression

 Initial dose: 15 mg orally once a day at bedtime
 Maintenance dose: 15 to 45 mg orally once a day
 Maximum dose: 45 mg/day
Side effects
  Commonly reported side effects of mirtazapine include: severe sedation, constipation,
drowsiness, increased serum cholesterol, weight gain, fatigue, insomnia, increased appetite,
xerostomia, and decreased appetite. Other side effects include: dizziness, increased serum
triglycerides, tremor, dyspepsia, hot flash, palpitations, vertigo, abnormal dreams, bitter taste,
decreased libido, and diaphoresis.
 More Common: Constipation, dizziness

4. Yohimbine
Brand Name: Erex, Testomar, Yocon, Yohimar, Yohimbe, Yohimex

Uses:
Yohimbine increases the amount of blood that is allowed to flow into the penis and prevents blood from
flowing out of the penis. It can cause an erection.

Yohimbine is used to treat and diagnose some types of impotence.

Dosage
Recommended dosage, active amounts, other details
Dosages of 0.2mg/kg bodyweight have been successfully used to increase fat burning without significant
implications on cardiovascular parameters like heart rate and blood pressure. This results in a dosage of:

 14 mg for a 150lb person

 18 mg for a 200lb person
 22 mg for a 250lb person
 Supplementation is most effective between meals or during short term fasting.
Side effects

 Nervous system side effects have included excitation, increased motor activity, tremor, and
dizziness
 Cardiovascular side effects have included elevation in blood pressure and increase in heart rate.
 Gastrointestinal side effects have included nausea and vomiting, commonly reported after
parenteral administration of yohimbine.
 Psychiatric side effects have included irritability and generalized anxiety
 General side effects have included headache and increase in sweating.
 Dermatologic side effects have included skin flushing reported with oral administration.[Ref]
 A severe case of Raynaud's phenomenon has been reported in a 65-year-old man diagnosed
with CREST syndrome (calcinosis, Raynaud's phenomenon, esophageal dysfunction,
sclerodactyly, and telangiectasia). Painful episodes which affected all toes and fingers and his
penis lasted 10 to 15 minutes and were relieved with heat. Symptoms resolved slowly over time
upon discontinuation of yohimbine. Upon rechallenge with yohimbine, the patient developed
more severe Raynaud's phenomenon.