REVATIO ORAL SUSPENSION Dosage & Rx Info

Revatio Oral Suspension Generic Name & Formulations

Legal Class

General Description

Sildenafil 10mg/mL; pwd for oral susp after reconstitution; grape flavor; contains sorbitol.

Pharmacological Class

Phosphodiesterase type 5 inhibitor (cGMP-specific).

How Supplied

Tabs—90; Susp—112mL (w. bottle adapter, oral syringe); Single-use vial (12.5mL)—1

Manufacturer

Pfizer Inc.

Generic Availability

Tabs (YES); Susp, inj (NO)

Mechanism of Action

Sildenafil is an inhibitor of cGMP specific phosphodiesterase type-5 (PDE-5) in the smooth muscle of the pulmonary vasculature, where PDE-5 is responsible for degradation of cGMP. Sildenafil increases cGMP within pulmonary vascular smooth muscle cells resulting in relaxation.

Revatio Oral Suspension Indications

Indications

Pulmonary arterial hypertension (PAH) (WHO Group I) in adults to improve exercise ability and delay clinical worsening. PAH (WHO Group I) in pediatric patients to improve exercise ability and, in pediatric patients too young to perform standardized exercise testing, pulmonary hemodynamics thought to underlie improvements in exercise.

Revatio Oral Suspension Dosage and Administration

Adult

≥18yrs: 20mg three times daily. May titrate dose to a max of 80mg three times daily, if needed, based on symptoms and tolerability.

Children

<1yr: not established. 1–17yrs (≤20kg): 10mg three times daily; (20–45kg): 20mg three times daily; (>45kg): 20mg three times daily. Based on experience in adults, may titrate dose to a max of 40mg three times daily for patients >45kg, if needed, based on symptoms and tolerability.

Revatio Oral Suspension Contraindications

Contraindications

Concomitant organic nitrates, riociguat.

Revatio Oral Suspension Boxed Warnings

Not Applicable

Revatio Oral Suspension Warnings/Precautions

Warnings/Precautions

Pulmonary veno-occlusive disease: not recommended. PAH secondary to sickle cell anemia (risk of vaso-occlusive crisis). Underlying conditions that could be affected by vasodilatory effects (eg, concomitant antihypertensive therapy, BP<90/50, fluid depletion, severe left ventricular outflow obstruction, autonomic dysfunction). Risk of non-arteritic anterior ischemic optic neuropathy; monitor for sudden vision loss. Retinitis pigmentosa: not recommended. Anatomical penile deformation. Predisposition to priapism. Severe hepatic impairment. Active peptic ulcer. Bleeding disorders. Elderly. Pregnancy. Nursing mothers.

Revatio Oral Suspension Pharmacokinetics

Absorption

Mean absolute bioavailability: 41% (25–63%).

Maximum observed plasma concentrations are reached within 30–120 minutes (median 60 minutes) of oral dosing in the fasted state.

When taken with a high-fat meal, the rate of absorption is reduced, with a mean delay in T_max of 60 minutes and a mean reduction in C_max of 29%.

Distribution

Mean steady state volume of distribution: 105 L.

Plasma protein bound: ~96%.

Metabolism

Hepatic (CYP3A, CYP2C9).

Elimination

Fecal (~80%), renal (13%).

Revatio Oral Suspension Interactions

Interactions

See Contraindications. Hypotension with nitrates. Concomitant strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir): not recommended. Antagonized by moderate to strong CYP3A4 inducers (eg, bosentan).

Revatio Oral Suspension Adverse Reactions

Adverse Reactions

Headache, dyspepsia, flushing, pain in limb, myalgia, back pain, diarrhea; priapism, hypotension, vision or hearing loss.

Revatio Oral Suspension Clinical Trials

See Literature

Revatio Oral Suspension Note