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Avanafil

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From Pharmacopedia
PDE5 Inhibitor
Avanafil
Stendra
Avanafil is the newest of the four FDA-approved PDE5 inhibitors (2012). Compared to Sildenafil and Vardenafil, it has a faster onset (~15 min) and is more selective for PDE5 over PDE6 (fewer visual side effects). Compared to Tadalafil, it has a shorter duration, better suited to as-needed use than continuous coverage.

Experience

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Problems

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Titration strategies

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Effects

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Pharmacokinetics

Absorption

Rapid; peak ~30–45 min.

Distribution

Plasma protein binding ~99%.

Metabolism

Hepatic via CYP3A4 (primary), CYP2C9 (minor).

Elimination

Mainly fecal as inactive metabolites.

Interactions

No interactions reported yet.

Monitoring

Blood pressure with concurrent antihypertensives or alpha-blockers.

Patient counseling

Contraindicated with any nitrate (life-threatening hypotension). Caution with alpha-blockers.

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Relevant Literature

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See also

Sildenafil, Tadalafil, Vardenafil

References

Pharmacy
Starting dose
100 mg ~15 min before sexual activity
Preparations
50, 100, 200 mg tabs
US FDA Max
200 mg/d (100 mg/d if on CYP3A4 inhibitors)
Common uses
Classification(s)
Classes
PDE5 Inhibitor
Pharmacology
Routes
Oral
Onset
~15 min (fastest of the PDE5 inhibitors)
Duration
4–6 h
Half-life
~5 h
Bioavailability
Rapid absorption; absolute bioavailability not formally established
Pregnancy
Category C (not relevant; not used in women)
Legal status
Rx-only in US
Purported mechanism
Selective inhibitor of phosphodiesterase type 5 (PDE5); increases cGMP in cavernous smooth muscle, producing erection in response to sexual stimulation.