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Cimetidine (800 mg), a cytochrome P450 inhibitor and non-specific CYP3A4 inhibitor, triggered a 56% enhance in plasma sildenafil concentrations when co-administered with sildenafil (50 mg) to healthy volunteers. In normal wholesome male volunteers, there was no evidence of an effect of azithromycin (500 mg daily for 3 days) on the AUC, Cmax, tmax, elimination price constant, or subsequent half-life of sildenafil or its principal circulating metabolite. Co-administration of the HIV protease inhibitor saquinavir, a CYP3A4 inhibitor, at regular state (1 200 mg thrice a day) with sildenafil (100 mg single dose) resulted in a 140% increase in sildenafil Cmax and a 210% enhance in sildenafil AUC. Based on these pharmacokinetic results co-administration of sildenafil with ritonavir just isn’t suggested (see section 4.4) and in any event the utmost dose of sildenafil ought to by no means exceed 25 mg inside forty eight hours. Co-administration of the HIV protease inhibitor ritonavir, which is a highly potent P450 inhibitor, at regular state (500 mg twice daily) with sildenafil (100 mg single dose) resulted in a 300% (4-fold) enhance in sildenafil Cmax and a 1 000% (11-fold) enhance in plasma AUC.
We publish essentially the most up-to-date information for a medication based on its licence history. The whole physique clearance of sildenafil is 41 L/h with a resultant terminal section half- life of 3-5 h. The N-desmethyl metabolite is additional metabolised, with a terminal half-life of approximately 4 h. There was no impact on sperm motility or morphology after single 100 mg oral doses of sildenafil in wholesome volunteers (see section four.6).