Viagra (sildenafil citrate): Absorption [Kinetics Pairing] Sildenafil should be administered orally 30 minutes to 4 hours before sexual activity.

Sildenafil is rapidly absorbed in the gut and enters the hepatic vein in high concentrations. Sildenafil makes its first pass through the liver where a large amount of it is metabolized by the cytochrome P450 enzyme system. In a fasting state of oral dosing the maximum observed plasma concentrations are reached within 30 120 minutes (mean 60 minutes), with a mean absolute bioavailability of 41% (range 25-63%). Sildenafils pharmacokinetics is dose-proportional over the recommended dose range. If Sildenafil is taken with a high fat meal the rate of absorption is delayed. The mean delay after a high fat meal in Tmax (the time after administration of a drug when the maximum plasma concentration is reached, when the rate of absorption equals the rate of elimination) of 60 minutes and a mean reduction in Cmax (the maximum plasma concentration of the drug) of 29%. Sildenafil and its key circulating N-desmethyl metabolite are both roughly 96% bound to plasma proteins. Protein binding is independent of total drug concentrations. Grapefruit juice has been found to increase sildenafils bioavailability and tends to delay its absorption. St. Johns Wort may decrease sildenafil levels. In healthy young men after 90 minutes after taking the medication orally, the measurement of sildenafil appearing in semen is less than 0.001%. However in healthy geriatrics over 65 years of age there is a reduced clearance of sildenafil which results in approximately 84% and 107% higher plasma AUC values of sildenafil and the active Ndesmethyl metabolite compared to those in the age group of 18 45 year olds. The hepatic impairment and renal impairment in those > 65 years of age are linked with increased plasma levels. Therefore the oral dose should be careful taken into account in these patients. The manufacturer recommends the following dosing patients with erectile dysfunction: Initial dose for healthy adults is usually 50 mg po once daily 1 hour before sexual activity; dosing range: 25 mg 100 mg po once daily. Elderly dosing > 65 years of age (use with caution) starting dose of 25 mg po once daily should be considered. Sildenafil should not be given concurrently with organic nitrates in any form, regularly or intermittently used due to vasodilator effects. References Lacy, C. F., Armstrong, L. L., Goldman, M. P., & Lance, L. L. (2010-2011). Drug Information Handbook with International Trade Names Index (19th ed.). Hudson, Ohio: Lexi-Comp. Nichols, D. J., Muirhead, G. J., & Hanes, J. A. (2002). Pharmacokinetics of Sildenafil Citrate After Single Oral Doses in Healthy Male Subjects: Absolue Bioavailability, Found Effects and Dose Proportionality. British Journal Clinical Pharmacology , 53, 5s - 12s. Viagra Package Insert. (January 2010). Viagra (sildenafil citrate) Tablets. Retrieved Feb 6, 2011 from http://media.pfizer.com/files/products/uspi_viagra.pdf New York, NY: Pfizer Labs, Division of Pfizer Inc.