1 Half-life: 4 hr (for sildenafil and active metabolite).

TIME/ACTION PROFILE (vasodilation, ability to produce

sildenafil (sil-den-a-fil) erection)
Revatio, Neogra ROUTE ONSET PEAK DURATION
Classification 30 120
Therapeutic: erectile dysfunction agents, PO within 1 hr min up to 4 hr
vasodilators
Pharmacologic: phosphodiesterase type 5
inhibitors
Pregnancy Category B

Indications
Neogra: Erectile dysfunction. Revatio: Pulmonary
arterial hypertension (WHO Group I).
Action
Neogra: Enhances effects of nitric oxide released during sexual
stimulation. Nitric ox-ide activates guanylate cyclase, which
produces increased levels of cyclic guanosine monophosphate
(cGMP). cGMP produces smooth muscle relaxation of the
corpus cavernosum, which promotes increased blood flow and
subsequent erection. cGMP also leads to vasodilation of the
pulmonary vasculature. Sildenafil inhibits the enzyme
phosphodiesterase type 5 (PDE5), PDE5 inactivates cGMP.
Revatio: Produces vaso-dilation of the pulmonary vascular bed.
Therapeutic Effects: Neogra: Enhanced blood flow to the
corpus cavernosum and erection sufficient to allow sexual
inter-course. Requires sexual stimulation. Revatio: Improved
exercise tolerance and delay worsening of disease.
Pharmacokinetics
Absorption: Rapidly absorbed (41%) after oral
administration; IV administration results in complete
bioavailability.
Distribution: Widely distributed to tissues; negligible
amount in semen.
Protein Binding: 96%.
Metabolism and Excretion: Mostly metabolized by the
liver (by P450 3A4 en-zyme system); one metabolite is active
and accounts for 20% or more of drug effect. Metabolites
excreted mostly (80%) in feces; 13% excreted in urine.
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Concurrent
use of nitrates; Pulmonary veno-occlusive disease; OB,
Pedi: Newborns, women, children; Pedi: Revatio-Chronic
use not recommended for pulmonary hypertension due to
lack of efficacy andqrisk of death.
Use Cautiously in: Serious underlying cardiovascular
disease (including history of MI, stroke, or serious arrhythmia
within 6 mo), cardiac failure, or coronary artery disease with
unstable angina; History of HF, coronary artery disease,
uncontrolled hy-pertension (BP 170/110 mm Hg) or
hypotension (BP 90/50 mm Hg), dehydra-tion, autonomic
dysfunction, or severe left ventricular outflow obstruction;
Pulmo-nary hypertension secondary to sickle cell anemia
(mayqrisk of vaso-occlusive crises); Concurrent treatment with
antihypertensives or glipizide; Renal impairment (CCr 30
mL/min, hepatic impairment; all result inqblood levels;pdose
required with Neogra); Anatomic penile deformity (angulation,
cavernosal fibrosis, Peyronie disease); Conditions associated
with priapism (sickle cell anemia, multiple mye-loma,
leukemia); Bleeding disorders or active peptic ulceration;
History of sudden severe vision loss or at risk for non-arteritic
ischemic optic neuropathy (NAION); mayqrisk of recurrence;
Retinitis pigmentosa; Alpha adrenergic blockers (patients
should be on stable dose of alpha blockers before starting
Canadian drug name. Genetic Implication.
threatening, underlines indicate most frequent. Strikethrough
sildenafil); Geri:qblood levels and may require lower doses;
consider age-related decrease in cardiac, he-patic, and renal
function as well as concurrent drug therapy and chronic
disease states; Lactation: Lactation.
Adverse Reactions/Side Effects
CNS: headache, dizziness, insomnia. EENT: epistaxis, hearing
loss, nasal conges-
tion, vision loss. CV: MYOCARDIAL INFARCTION, SUDDEN DEATH,
hypotension, vaso-oc-
clusive crises. GI: dyspepsia, diarrhea. GU: priapism,
urinary tract infection.
Derm: flushing, rash. MS: mylagia. Neuro:
paresthesias.
Interactions
Drug-Drug: Concurrent use of nitrates may cause
serious, life threatening hy-potension and is contraindicated.
Blood levels and effects, including the risk of hypo-tension may
beqby enzyme inhibitors including cimetidine,
erythromycin, tacrolimus, ketoconazole, itraconazole, and
protease inhibitor antiretro-virals including nelfinavir,
indinavir, ritonavir, and saquinavir (initial dose of sildenafil
for erectile dysfunction should bepto 25 mg) (concurrent use of
potent CYP3A inhibitors not recommended with oral
Revatio).qrisk of hypotension with al-
CAPITALS indicate life-
Discontinued.
2 Revatio: Monitor hemodynamic parameters and
exercise tolerance prior to and periodically during
pha adrenergic blockers and acute ingestion of alcohol. therapy.
Rifampin, bosentan, barbiturates, carbamazepine,
phenytoin, efavirenz, nevirapine, rifampin or rifabutin
Potential Nursing Diagnoses
maypblood levels and effects; dose adjustments may be
Sexual dysfunction (Indications)
necessary in the treatment of pulmonary arterial
Risk for activity intolerance (Indications)
hypertension.qlevels of bosentan. Use cau-tiously with
glipizide. Mayqrisk of bleeding with warfarin.
Route/Dosage
Neogra (for erectile dysfunction)
PO (Adults): 50 mg taken 1 hr before sexual activity
(range 25 100 mg taken 30 min 4 hr before sexual
activity); not more than once daily; Concurrent use
with al-pha-blocker antihypertensives do not use 50
100 mg dose within 4 hr of alpha blocker, 25-mg dose
may be taken anytime.
PO (Geriatric Patients $65 yr or with concurrent
enzyme inhibitors): 25 mg taken 1 hr before sexual
activity (range 25 100 mg taken 30 min 4 hr before
sex-ual activity); not more than once daily.
Hepatic/Renal Impairment
PO (Adults): 25 mg taken 1 hr before sexual activity
(range 25 100 mg taken 30 min 4 hr before sexual
activity); not more than once daily.
Revatio (for pulmonary arterial hypertension)
IV therapy is indicated for patients unable to take PO therapy
PO (Adults): 20 mg 3 times daily; dose adjustments
may be necessary for concur-rent bosentan,
barbiturates, carbamazepine, phenytoin, efavirenz,
nevirapine, rifam-pin, or rifabutin.
IV (Adults): 10 mg 3 times daily.
NURSING IMPLICATIONS
Assessment
Neogra: Determine erectile dysfunction before
administration. Sildenafil has no effect in the
absence of sexual stimulation.
Implementation
Do not confuse Neogra (sildenafil) with Allegra
(fexofenadine).
PO: Dose for erectile dysfunction is usually administered
1 hr before sexual ac-tivity. May be administered 30 min
4 hr before sexual activity.
Dose for pulmonary arterial hypertension is
administered 3 times daily without regard to food.
Doses should be spaced 4 6 hr apart.
Use syringe provided for accurate dosing of oral
suspension.
IV Administration
Direct IV: Administer undiluted. Solution is clear and
colorless; do not admin-
ister solutions that are discolored or contain a
precipitate. Rate: Administer as a bolus three times
daily.
Patient/Family Teaching
Instruct patient to take sildenafil as directed. For
erectile dysfunction, take ap-proximately 1 hr before
sexual activity and not more than once per day. If taking
sildenafil for pulmonary arterial hypertension, take
missed doses as soon as re-membered unless almost
time for next dose; do not double doses.
Advise patient that Neogra is not indicated for use in
women.
Caution patient not to take sildenafil concurrently with alpha-
adrenergic blockers (unless on a stable dose) or nitrates. If chest
pain occurs after taking sildenafil, instruct patient to seek
immediate medical attention. Advise patient taking silden-afil for
pulmonary arterial hypertension to notify health care professional
of all Rx or OTC medications, vitamins, or herbal products being
taken and to consult with health care professional before taking
other medications.
Instruct patient to notify health care professional
promptly if erection lasts longer than 4 hr or if
experience sudden or decreased vision loss in one or
both eyes or loss or decrease in hearing, ringing in the
ears, or dizziness.
Inform patient that sildenafil offers no protection
against sexually transmitted dis-eases. Counsel
patient that protection against sexually transmitted
diseases and HIV infection should be considered.
Evaluation/Desired Outcomes
Male erection sufficient to allow intercourse.
Increased exercise tolerance.
Why was this drug prescribed for your
patient?
2015 F.A. Taj Pharma India Company