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Sildenafil is rapidly absorbed after oral administration, with absolute bioavailability of 40%. Plasma concentrations peak within 30 to 120 minutes (median, 60 minutes) of oral dosing in the fasted state.
Sildenafil is primarily metabolized by the cytochrome P450 3A4 (major route) and 2C9 (minor route) hepatic microsomal isoenzymes, which convert it to an active N-desmethyl metabolite that has been shown to possess 50% of the parent drug's potency for inhibiting PDE5. Plasma concentrations of this metabolite are 40% of those seen for sildenafil, so that the metabolite accounts for 20% of the pharmacological effects of sildenafil. Sildenafil and its active metabolite are both highly bound to plasma proteins (96%), and their terminal half-lives are 4 hours each. The mean steady-state volume of distribution for sildenafil is 105 L, indicating distribution into the tissues. Visit our partner to Purchase Viagra.
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