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Information about Sildenafil

Sildenafil functions as a selective and competitive inhibitor of type 5 phosphodiesterases (PDE5) on smooth muscle cells in the penis and pulmonary vasculature, and is used extensively for erectile dysfunction and less commonly for pulmonary hypertension.

{livtox}} Sildenafil has been associated with rare instances of clinically apparent liver injury.

Mechanism of action of Sildenafil

Sildenafil (sil den' a fil) is an inhibitor of type 5 phosphodiesterase (PDE5), the enzyme isoform that is found predominantly in the penis and lungs. Inhibition of PDE5 leads to prolongation of activation of cyclic guanosine monophosphate (cGMP), a major mediator of the vasodilatory action of nitric oxide (NO). Inhibition of PDE5 leads to prolongation of smooth muscle relaxation in the corpus cavernosum of the penis (improving erections) and in the pulmonary vasculature (decreasing pulmonary artery pressure).

FDA approval information for Sildenafil

Sildenafil was approved for use in the therapy of erectile dysfunction in the United States in 1998 and is available generically and under the brand name Viagra in tablets of 25, 50 and 100 mg. Worldwide, more than 20 million men have used sildenafil for erectile dysfunction.

Dosage and administration for Sildenafil

The recommended dose is 50 mg as a single dose approximately one hour before sexual activity, with dose increase or decrease based upon tolerance and effectiveness with a recommended maximum frequency of once daily and maximum amount of 100 mg. Sildenafil is also approved for use in pulmonary hypertension as tablets of 20 mg generically and under the brand name Revatio. The recommended dosage for pulmonary hypertension is 20 mg three times daily. An intravenous formulation of sidenafil is also available in 10 mg vials for more emergent treatment of pulmonary artery hypertension, the recommended dosage being 10 mg intravenously three times daily.

Side effects of Sildenafil

Common side effects include dizziness, headache, flushing, hypotension, rhinitis and dyspepsia. Rare, but potentially serious adverse events include vision and hearing loss, hypotension, cardiovascular events and priapism.

PDE 5 inhibitors

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