REVATIO INJECTION Dosage & Rx Info

Revatio Injection Generic Name & Formulations

Legal Class

General Description

Sildenafil 10mg/vial; soln for IV inj.

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 Injection Indications

Indications

Pulmonary arterial hypertension (PAH) (WHO Group I) to improve exercise ability and delay clinical worsening, in adults who are temporarily unable to take oral Revatio.

Revatio Injection Dosage and Administration

Adult

Give by IV bolus inj. 10mg three times daily.

Children

Not recommended.

Administration

Give by IV bolus injection.

Nursing Considerations

Give by IV bolus injection. Advise patients to seek immediate medical attention for a sudden loss of vision or hearing while on therapy.

Revatio Injection Contraindications

Contraindications

Concomitant organic nitrates, riociguat.

Revatio Injection Boxed Warnings

Not Applicable

Revatio Injection 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 Injection 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 Injection 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 Injection Adverse Reactions

Adverse Reactions

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

Revatio Injection Clinical Trials

See Literature

Revatio Injection Note