Vardenafil Dosage & Rx Info | Uses, Side Effects

Vardenafil Generic Name & Formulations

Legal Class

General Description

Vardenafil (as HCl) 2.5mg, 5mg, 10mg, 20mg; tabs.

Pharmacological Class

Phosphodiesterase type 5 inhibitor (cGMP-specific).

How Supplied

Contact supplier

Manufacturer

Various generic manufacturers

Mechanism of Action

Vardenafil HCl is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The inhibition of PDE5 enhances erectile function by increasing the amount of cGMP. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 has no effect in the absence of sexual stimulation.

Vardenafil Indications

Indications

Erectile dysfunction.

Vardenafil Dosage and Administration

Adult

Take once daily as needed, about 1hr before sexual activity. Initially 10mg; range: 5–20mg. Elderly (≥65yrs): initially 5mg. Moderate hepatic impairment: initially 5mg; max 10mg. Concomitant ketoconazole 200mg or itraconazole 200mg daily, or erythromycin: max 5mg. Concomitant indinavir, saquinavir, atazanavir, ketoconazole 400mg or itraconazole 400mg daily, clarithromycin: max 2.5mg. Concomitant ritonavir, cobicistat: max 2.5mg/72hrs. Concomitant α-blocker: initially 5mg/day.

Children

Not established.

Vardenafil Contraindications

Contraindications

Concomitant nitrates, or nitric oxide donors. Concomitant guanylate cyclase (GC) stimulators (eg, riociguat).

Vardenafil Boxed Warnings

Not Applicable

Vardenafil Warnings/Precautions

Warnings/Precautions

Not for use in women. Confirm diagnosis before therapy. Congenital QT prolongation: avoid use. Cardiovascular disease (eg, MI, stroke or life-threatening arrhythmia within 6 months; systolic BP <90mmHg or BP >170/110mmHg; unstable angina, LV outflow obstruction, severe heart failure), severe hepatic impairment, on renal dialysis, hereditary degenerative retinal disorders and retinitis pigmentosa: not recommended. Anatomical penile deformation. Predisposition to priapism. History of non-arteritic anterior ischemic optic neuropathy (NAION) or those with "crowded" optic disc. Advise patients to discontinue if sudden vision or hearing loss occurs. Patients for whom sexual activity is inadvisable or contraindicated. Bleeding disorders. Active peptic ulcer. Pregnancy.

Vardenafil Pharmacokinetics

Absorption

Absolute bioavailability: ~15%.

Distribution

Plasma protein bound: ~95%.

Mean steady-state volume of distribution: 208 L.

Metabolism

Hepatic (CYP3A4).

Elimination

Fecal (~91–95%), renal (~2–6%).

Half-life: 4–5 hours.

Vardenafil Interactions

Interactions

See Contraindications. Hypotension with nitrates, GC stimulators. Avoid Class IA (eg, quinidine, procainamide) or Class III (eg, amiodarone, sotalol) antiarrhythmics, others that cause QT prolongation. Additive hypotensive effects with concomitant α-blockers, other antihypertensives; caution. Potentiated by moderate or strong CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, indinavir, cobicistat, saquinavir, atazanavir, ritonavir, grapefruit juice). Concomitant other erectile dysfunction treatments: not recommended.

Vardenafil Adverse Reactions

Adverse Reactions

Headache, flushing, nasal congestion, dyspepsia, sinusitis, flu syndrome, dizziness, increased creatine kinase, nausea, back pain, sudden vision or hearing loss, cardiovascular effects; rare: priapism, prolonged erection.

Vardenafil Clinical Trials

See Literature

Vardenafil Note

Notes

Formerly known under the brand name Levitra.

Vardenafil Patient Counseling