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Co-administration of the HIV protease inhibitor saquinavir, a CYP3A4 inhibitor, at steady state (1200mg 3 times a day) with sildenafil (100mg single dose) resulted in a 140% enhance in sildenafil Cmax and a 210% improve in sildenafil AUC. Primarily Based on these pharmacokinetic outcomes co-administration of sildenafil with ritonavir isn’t advised (see Part four.4) and in any event the maximum dose of sildenafil ought to by no means exceed 25mg inside 48 hours. Co-administration of the HIV protease inhibitor ritonavir, which is a highly potent P450 inhibitor, at regular state (500mg twice daily) with sildenafil (100mg single dose) resulted in a 300% (4-fold) improve in sildenafil Cmax and a 1,000% (11-fold) increase in sildenafil plasma AUC.

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Concomitant use of riociguat with PDE5 inhibitors, including sildenafil, is contraindicated (see section four.3). In medical studies, riociguat has been shown to augment the hypotensive results of PDE5 inhibitors. Single doses of antacid (magnesium hydroxide/aluminium hydroxide) didn’t affect the bioavailability of sildenafil. Cimetidine (800mg), a cytochrome P450 inhibitor and non-specific CYP3A4 inhibitor, caused a 56% improve in plasma sildenafil concentrations when co-administered with sildenafil (50mg) to healthy volunteers. In regular wholesome male volunteers, there was no proof of an effect of azithromycin (500mg daily for 3 days) on the AUC, Cmax, Tmax, elimination rate constant, or subsequent half-life of sildenafil or its principal circulating metabolite.

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We publish probably the most up-to-date information for a medicine according to its licence historical past. The complete physique clearance of sildenafil is forty one L/h with a resultant terminal phase half- lifetime of 3-5 h. The N-desmethyl metabolite is additional metabolised, with a terminal half-life of approximately four h. There was no effect on sperm motility or morphology after single a hundred mg oral doses of sildenafil in healthy volunteers (see part 4.6).

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