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Vardenafil

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From Pharmacopedia
PDE5 Inhibitor
Vardenafil
Levitra, Staxyn
Vardenafil is a PDE5 inhibitor very similar to Sildenafil in onset and duration, marketed mainly for erectile dysfunction. Same nitrate contraindication and alpha-blocker caution. Slightly different selectivity profile but in practice the three short-acting PDE5 inhibitors are nearly interchangeable; choice is often driven by patient preference and insurance.

Experience

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Problems

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Titration strategies

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Effects

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Pharmacokinetics

Absorption

~15%; reduced by high-fat meals.

Distribution

Plasma protein binding ~95%.

Metabolism

Hepatic via CYP3A4 (primary).

Elimination

Fecal as metabolites.

Interactions

No interactions reported yet.

Monitoring

Blood pressure; ECG (QT) in congenital long-QT.

Patient counseling

Contraindicated with any nitrate. Avoid in congenital long-QT syndrome or with type-1A/type-3 antiarrhythmics.

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See also

Avanafil, Sildenafil, Tadalafil

References

Summary
Classes
PDE5 Inhibitor
Common uses
Erectile dysfunction0
Pharmacy
Starting dose
10 mg ~1 h before sexual activity
Preparations
2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn)
US FDA Max
20 mg/d
Pharmacology
Routes
Oral
Onset
~30 min
Duration
4–5 h
Half-life
4–5 h
Bioavailability
~15% (extensive hepatic first-pass)
Pregnancy
Category B
Legal status
Rx-only in US
Purported mechanism
Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses).