Vardenafil Hydrochloride Drug Facts

Vardenafil Hydrochloride

Trade Names:
Levitra
- Tablets 2.5 mg
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg

Pharmacology

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.

Pharmacokinetics

Absorption

Rapidly absorbed with bioavailability of about 15%. C _max reached between 30 min and 2 h after an oral dose.

Distribution

Vd _ss is 208 L. Protein binding is about 95%.

Metabolism

Metabolized predominately by CYP3A4 and to a lesser degree by CYP3A5 and CYP2C isoforms. The M1 metabolite accounts for 7% of the total activity.

Elimination

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.

Special Populations

The AUC was 20% to 30% higher in moderate or severe renal 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.

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.

Indications and Usage

Treatment of erectile dysfunction.

Contraindications

Administration with nitrates, nitric oxide donors, or alpha blockers; hypersensitivity to any component of the product.

Dosage and Administration

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.

PO A 5 mg starting dose is recommended.

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.

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.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

Coadministration of these agents with vardenafil is contraindicated.

Patients with congenital QT prolongation and those receiving these agents should avoid use of vardenafil.

Plasma levels of vardenafil may be elevated, increasing the risk of adverse reactions and necessitating dosage adjustment.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Angina pectoris, chest pain, hypertension, hypotension, MI, myocardial ischemia, palpitation, postural hypotension, syncope, tachycardia (less than 2%).

CNS

Headache (15%); dizziness (2%); hypertonia, hypesthesia, insomnia, paresthesia, somnolence, vertigo (less than 2%).

Dermatologic

Photosensitivity reaction, pruritus, rash, sweating (less than 2%).

EENT

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%).

GI

Dyspepsia (4%); nausea (2%); abdominal pain, diarrhea, dry mouth, dysphagia, esophagitis, gastritis, gastroesophageal reflux, vomiting, gamma-glutamyl-transpeptidase increase (less than 2%).

Genitourinary

Abnormal ejaculation, priapism (less than 2%).

Hepatic

Abnormal LFTs (less than 2%).

Lab Tests

Increased creatine kinase (2%).

Musculoskeletal

Arthralgia, back pain, myalgia, neck pain (less than 2%).

Respiratory

Dyspnea, epistaxis (less than 2%).

Miscellaneous

Flushing (11%); accidental injury, flu syndrome (3%); anaphylactic reactions, asthenia, face edema, pain (less than 2%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Not indicated for use in children.

Elderly

Because men 65 yr of age and older may have higher plasma levels, a lower starting dose is recommended.

Hepatic Function

Reduce starting dose in patients with moderate hepatic function impairment.

Cardiac risk

Evaluate CV status, left ventricular outflow obstruction (eg, aortic stenosis), and BP before treatment.

Priapism

Prolonged erections (exceeding 4 h) may occur and require immediate medical assistance.

Special populations

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.

Overdosage

Symptoms

Back pain/myalgia, abnormal vision.

Patient Information

• Instruct patient to read the patient information leaflet before starting therapy and with each refill.
• Advise patient to take prescribed dose 60 min before anticipated sexual activity and not to take more than 1 dose in a 24-h period.
• Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
• Advise patient that sexual stimulation will be required for medication to work and an erection to occur.
• Instruct patient not to change the dose unless advised by health care provider.
• Advise patient to contact health care provider if they are not satisfied with their sexual performance after taking medication or if bothersome adverse reactions occur.
• Instruct patient to stop using and contact health care provider immediately if any of the following occur: dizziness, fainting, chest pain, vision changes, erection persisting longer than 4 h, painful erection.
• Caution patient to avoid using poppers (eg, amyl nitrate, butyl nitrate) while taking this medication.
• Caution patient that the medication is not a male form of birth control, nor does it provide protection against sexually transmitted diseases and to use protective measures as indicated.