LIQREV Dosage & Rx Info | Uses, Side Effects

Liqrev Generic Name & Formulations

Legal Class

General Description

Sildenafil 10mg/mL; oral susp; strawberry-flavored.

Pharmacological Class

Phosphodiesterase type 5 inhibitor (cGMP-specific).

How Supplied

Oral susp—122mL

Manufacturer

CMP Pharma

Mechanism of Action

Sildenafil enhances the effect of nitric oxide (NO) by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum. When sexual stimulation causes local release of NO, inhibition of PDE5 by sildenafil causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil at recommended doses has no effect in the absence of sexual stimulation.

Liqrev Indications

Indications

Pulmonary arterial hypertension (PAH) (WHO Group I) in adults to improve exercise ability and delay clinical worsening.

Liqrev Dosage and Administration

Adult

≥18yrs: 20mg three times daily.

Children

<18yrs: not established.

Liqrev Contraindications

Contraindications

Concomitant organic nitrates, riociguat.

Liqrev Boxed Warnings

Not Applicable

Liqrev 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 (eg, sickle cell disease, multiple myeloma, leukemia). Severe hepatic impairment. Active peptic ulcer. Bleeding disorders. Elderly. Pregnancy. Nursing mothers.

Liqrev 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 Tmax of 60 minutes and a mean reduction in Cmax of 29%.

Distribution

Mean steady state volume of distribution: 105 L.
Plasma protein bound: ~96%.

Metabolism

Hepatic (CYP3A, CYP2C9).

Elimination

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

Liqrev 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).

Liqrev Adverse Reactions

Adverse Reactions

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

Liqrev Clinical Trials

See Literature

Liqrev Note