Trade Names:Levitra- Tablets 2.5 mg- Tablets 5 mg- Tablets 10 mg- Tablets 20 mg
Enhances the effect of nitric oxide at the nerve ending and endothelial cells in the corpus cavernosum by inhibiting phosphodiesterase type 5 in the corpus cavernosum of the penis. This results in vasodilation, increased inflow of blood into the corpora cavernosa, and ensuing penile erection upon sexual stimulation.
Rapidly absorbed with bioavailability of about 15%. C max reached between 30 min and 2 h after an oral dose.
Vd ss is 208 L. Protein binding is about 95%.
Metabolized predominately by CYP3A4 and to a lesser degree by CYP3A5 and CYP2C isoforms. The M1 metabolite accounts for 7% of the total activity.
Excretion as metabolites (91% to 95% in feces; 2% to 6% in urine). Total body Cl is 56 L/h, t ½ is approximately 4 to 5 h.
The AUC was 20% to 30% higher in moderate or severe renal function impairment.Hepatic Function Impairment
Hepatic function impairment is associated with increased plasma levels. A starting dose of 5 mg is recommended in patients with moderate hepatic function impairment and the max dose should not exceed 10 mg.Elderly
In men 65 yr of age and older, the C max and AUC are increased 34% and 52%, respectively, compared with men 18 to 45 yr of age.
Treatment of erectile dysfunction.
Administration with nitrates, nitric oxide donors, or alpha blockers; hypersensitivity to any component of the product.
PO Recommended starting dose is 10 mg approximately 60 min prior to sexual activity. Depending on efficacy and adverse reactions, the dose may be decreased to 5 mg or increased to 20 mg.Geriatric (65 yr of age and older)
PO A 5 mg starting dose is recommended.Hepatic Function ImpairmentAdults
PO A 5 mg starting dose is recommended in patients with moderate hepatic function impairment (max, 10 mg). Do not use in severe hepatic function impairment.Concomitant TherapyAdults
PO In patients receiving ritonavir, do not exceed a single 2.5 mg dose in a 72-h period. In patients receiving indinavir, itraconazole (400 mg/day), or ketoconazole (400 mg/day), do not exceed a single 2.5 mg dose in a 24-h period. In patients receiving erythromycin, itraconazole (200 mg/day), or ketoconazole (200 mg/day), do not exceed a single 5 mg dose in a 24-h period.
Store tablets at controlled room temperature (59° to 86°F).
Coadministration of these agents with vardenafil is contraindicated.Class IA (eg, quinidine, procainamide), class III (eg, amiodarone, sotalol) antiarrhythmic agents
Patients with congenital QT prolongation and those receiving these agents should avoid use of vardenafil.CYP-450 3A4/5 and CYP2C9 (eg, erythromycin, indinavir, itraconazole, ketoconazole, ritonavir)
Plasma levels of vardenafil may be elevated, increasing the risk of adverse reactions and necessitating dosage adjustment.
None well documented.
Angina pectoris, chest pain, hypertension, hypotension, MI, myocardial ischemia, palpitation, postural hypotension, syncope, tachycardia (less than 2%).
Headache (15%); dizziness (2%); hypertonia, hypesthesia, insomnia, paresthesia, somnolence, vertigo (less than 2%).
Photosensitivity reaction, pruritus, rash, sweating (less than 2%).
Rhinitis (9%); sinusitis (3%); tinnitus, pharyngitis, abnormal vision, blurred vision, chromatopsia, color vision changes, conjunctivitis, dim vision, eye pain, glaucoma, photophobia, watery eyes (less than 2%).
Dyspepsia (4%); nausea (2%); abdominal pain, diarrhea, dry mouth, dysphagia, esophagitis, gastritis, gastroesophageal reflux, vomiting, gamma-glutamyl-transpeptidase increase (less than 2%).
Abnormal ejaculation, priapism (less than 2%).
Abnormal LFTs (less than 2%).
Increased creatine kinase (2%).
Arthralgia, back pain, myalgia, neck pain (less than 2%).
Dyspnea, epistaxis (less than 2%).
Flushing (11%); accidental injury, flu syndrome (3%); anaphylactic reactions, asthenia, face edema, pain (less than 2%).
Category B .
Not indicated for use in children.
Because men 65 yr of age and older may have higher plasma levels, a lower starting dose is recommended.
Reduce starting dose in patients with moderate hepatic function impairment.
Evaluate CV status, left ventricular outflow obstruction (eg, aortic stenosis), and BP before treatment.
Prolonged erections (exceeding 4 h) may occur and require immediate medical assistance.
Because there are no clinical data on safety and efficacy, use is not recommended in patients with unstable angina, hypotension, uncontrolled hypertension, recent history of stroke, life-threatening arrhythmia, MI, severe cardiac failure, severe hepatic function impairment, or end stage renal disease or known hereditary degenerative retinal disorder, including retinitis pigmentosa.
Back pain/myalgia, abnormal vision.
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