sildenafil (Rx)
Dosing & Uses.
injectable solution (Revatio)
oral suspension (Revatio)
Erectile Dysfunction.
50 mg PO 1 hour before sexual activity; may be increased to 100 mg or reduced to 25 mg, depending on effectiveness and tolerance; not to exceed 100 mg/day.
Pulmonary Arterial Hypertension.
PO: 5 mg or 20 mg 3 times daily, administered 4-6 hours apart.
IV: 2.5-mg or 10-mg bolus 3 times daily if patient is temporarily unable to take PO.
Recommended PO/IV dose not to be exceeded.
Adding Revatio to bosentan does not have any beneficial effect on exercise capacity.
Dosing Modifications.
Heaptic impairment or severe renal impairment: Use initial dose of 25 mg.
Geriatric Dosing.
Viagra >65 years: 25 mg PO initially 1 hour before sexual activity.
Pulmonary Arterial Hypertension.
Revatio PO: 5 mg or 20 mg 3 times daily, administered 4-6 hours apart IV: 2.5-mg or 10-mg bolus 3 times daily if patient is temporarily unable to take PO Recommended PO/IV dose not to be exceeded Adding Revatio to bosentan does not have any beneficial effect on exercise capacity Clinical trials found no significant difference in response between elderly patients and younger adults; however, cautious dose selection should be considered in elderly because of greater frequency of decreased hepatic, renal, and cardiac function, as well as comorbid conditions and concomitant pharmacotherapy Compared with healthy younger volunteers, healthy elderly volunteers (≥65 years) had reduced clearance of sildenafil, resulting in approximately 84% and 107% higher plasma concentrations of sildenafil and its active N-desmethyl metabolite, respectively.
Not to be prescribed to children (1-17 years) for pulmonary arterial hypertension (PAH); this recommendation against use is based on long-term clinical pediatric trial showing that children taking high doses had higher risk of death than children taking low doses and that low doses were not effective in improving exercise ability (see Cautions)
Interactions.
Interaction Checker.
Contraindicated.
Serious – Use Alternative.
Significant – Monitor Closely.
Adverse Effects.
Postmarketing Reports.
Vaso-occlusive crisis (PAH secondary to sickle-cell anemia)
Nonarteritic anterior ischemic optic neuropathy (NAION)
Contraindications.
Soluble guanylate cyclase (sGC) stimulators (eg, riociguat); concomitant use can cause hypotension.
Coadministration with nitrates.
Coadministration with nitrates (either regularly and/or intermittently) and nitric oxide donors Consistent with the effects of PDE5 inhibition on the nitric oxide/cyclic guanosine monophosphate pathway, PDE5 inhibitors may potentiate the hypotensive effects of nitrates A suitable time interval following PDE5 dosing for the safe administration of nitrates or nitric oxide donors has not been determined.
Elicits vasodilatory properties, resulting in mild and transient decreases in blood pressure.
Use with caution in patients with anatomic deformation of penis (eg, angulation, cavernosal fibrosis, or Peyronie disease), conditions potentially predisposing to priapism (eg, sickle cell anemia, multiple myeloma, or leukemia), cardiovascular disease, bleeding disorders, active peptic ulcer disease, liver disease, renal impairment, multidrug antihypertensive regimens, retinitis pigmentosa, concomitant use of CYP3A4 inhibitors.
Pulmonary vasodilators may significantly worsen cardiovascular status of patients with pulmonary veno-occlusive disease.
Patient taking alpha blocker should be stabilized before starting phosphodiesterase (PDE)-5 inhibitor, which should be initiated at lowest dose; if patient is already taking optimized dose of PDE-5 inhibitor, alpha blocker should be initated at lowest dose to avoid hypotension.
Not to be taken with other PDE-5 inhibitors.
Sudden decrease or loss of hearing, which may be accompanied by tinnitus and dizziness.
Viagra: Patients should stop sildenafil and seek medical care if a sudden loss of vision occurs in 1 or both eyes, which could be a sign of nonarteritic anterior ischemic optic neuropathy (NAION); use with caution, and only when the anticipated benefits outweigh the risks, in patients with a history of NAION; patients with a ”crowded” optic disc may also be at an increased risk of NAION; advise patients to seek immediate medical attention in the event of a sudden loss of vision.
Viagra: Potential for cardiac risk with sexual activity in patients with preexisting cardiovascular disease; therefore, treatment for erectile dysfunction generally should not be instituted in men for whom sexual activity is inadvisable because of their underlying cardiovascular status.
May cause dose-related impairment of color discrimination; use caution in patients with retinitis pigmentosa.
Evaluate underlying causes of erectile dysfunction or BPH before initiating therapy.
Revatio: In small, prematurely terminated study of patients with PAH secondary to sickle-cell disease, vaso-occlusive crises requiring hospitalization were more commonly reported by patients who received sildenafil than by those randomized to placebo; effectiveness of sildenafil in PAH secondary to sickle-cell anemia has not been established; the clinical relevance to men treated for erectile dysfunction with sildenafil is not known.
Revatio: Not for use in children with PAH; increased mortality with increasing doses (hazard ratio 3.5) was observed in randomized, double-blind, placebo-controlled clinical trial of 234 children (1-17 years) with PAH who had mild-to-moderate symptoms at baseline.
Revatio: Epistaxis occurred in 13% of patients with PAH secondary to connective tissue disease (eg, scleroderma); this effect was not seen in idiopathic PAH; incidence was also higher in those receiving concomitant PO vitamin K antagonist therapy (9%) than in those not receiving such therapy (2%)
Pregnancy & Lactation.
Pregnancy category: B.
Lactation: Unknown whether drug is distributed into breast milk.
Pregnancy Categories.
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology.
Mechanism of Action.
Inhibits PDE-5, increasing cyclic guanosine monophosphate cGMP to allow smooth-muscle relaxation.
Absorption.
Peak plasma time: 30-120 min.
Metabolism.
Metabolized in liver by CYP3A4 and (in minor amounts) CYP2C9.
Metabolites: N-desmethyl metabolite (active; possesses 50% of sildenafil’s PDE-5-inhibiting activity)
Elimination.
Half-life: Parent drug, 3-4 hr; active metabolite, 10-70 min.
Excretion: Feces (80%), urine (13%)
Administration.
IV Administration.
Revatio: Administer as an IV bolus.
Oral Administration.
May take with or without food Take as needed, about 1 hr before sexual activity; however, may be taken anywhere from 30 minutes to 4 hr before sexual activity The maximum recommended dosing frequency is once daily.
Tablets or oral suspension: Administer doses 4-6 hr apart.
Revatio tablets or IV solution.
Store at controlled room temperature 20-25°C (68-77°F) Excursions permitted to 15-30°C (59-86°F)
Revatio reconstituted oral suspension.
Store <30°C (86°F) or in a refrigerator between 2-8°C (36-46°F) Do not freeze Discard unused oral suspension after 60 days.
Patient Handout.
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