Liqrev Generic Name & Formulations
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.
Pulmonary arterial hypertension (PAH) (WHO Group I) in adults to improve exercise ability and delay clinical worsening.
Liqrev Dosage and Administration
≥18yrs: 20mg three times daily.
<18yrs: not established.
Concomitant organic nitrates, riociguat.
Liqrev Boxed Warnings
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.
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%.
Mean steady state volume of distribution: 105 L.
Plasma protein bound: ~96%.
Fecal (~80%), renal (13%).
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
Headache, dyspepsia, flushing, pain in limb, myalgia, back pain, diarrhea; priapism, hypotension, vision or hearing loss.
Liqrev Clinical Trials
Liqrev Patient Counseling