Vardenafil
Vardenafil. PDE5 inhibitor — closer structural analog of sildenafil than tadalafil. CYP3A4 substrate. Greater PDE5 selectivity over PDE6 in vitro… Oral half-life 4 h.
PDE5 inhibitor — closer structural analog of sildenafil than tadalafil. CYP3A4 substrate. Greater PDE5 selectivity over PDE6 in vitro reduces visual side effects vs sildenafil.
PK: ITS CITATION MEASURED A FREEZE-DRIED ORODISPERSIBLE TABLET CO-FORMULATED WITH DAPOXETINE, while this record doses are the standard tablet — and it states none of the four stored values. TWO COLLISIONS WERE AVAILABLE IN THE SOURCES AND THE RECORD FELL FOR NEITHER, WHICH IS WORTH RECORDING: that paper offers only "relative bioavailability values of 100.9 and 85%", and the replacement paper states F beside a competitor — "an absolute bioavailability of 14.5% (vs 40% for sildenafil)" — with the record correctly holding 0.15 rather than 0.40. Its occupancy row does the same, taking 0.7 nM rather than the parenthetical 6.6 nM that is sildenafil. t½ 4.5 is the MIDPOINT of a printed "about 4-5 h" and becomes the verbatim 4. CLASS 6 IS ACQUITTED BY ARITHMETIC: F times dose over V gives 0.0144 mg/L against a measured 0.0171, a 16% shortfall, where double-division would have predicted seven times low. V 208 L is the label steady-state figure, unsupported by any abstract but correctly PAIRED, so removing it while keeping F would be worse than leaving it. ka 1.4 implies a 1.77 h peak against "Tmax approximately 40 min".
Pharmacokinetics
- Oral — t½ 4 h · F 15% · Vd 208 L
Sources: PMID:29325456, PMID:11890515, PMID:15224134, PMID:12638394