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LEVITRA PHARMACOKINETICS


Vardenafil is rapidly absorbed with approximately 15% absolute bioavailability. A single 20 mg dose of Levitra in healthy volunteers leads to maximum observed plasma concentrations between 30 minutes and 2 hours after oral administration in an empty stomach. In other food-effects, studies showed that fatty meals caused a reduction in C max by 18%-50%. The plasma concentrations measurement in healthy male volunteers after 20 mg dose oral administration is depicted in the picture below.

Vardenafil is approximately 95% bound to plasma proteins. This protein binding is reversible and independent of total drug concentrations. After 1.5 hours of dosing of20 mg Vardenafil dose, a mean of 0.00018% was found in semen of healthy volunteers. Hepatic enzyme CYP3A4 primarily metabolizes Vardenafil along with involvement of the CYP3A5 and CYP2C isoforms. Vardenafil is excreted as metabolites mainly around 91-95% of the dose taken in the feces and 2-6% of the dose taken in the urine.

The table below concludes all the chemical details of Vardenafil;

Systematic (IUPAC) name 4-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl- 3,5,6,8-tetrazabicyclo[4.3.0] nona-3,7,9-trien-2-one
CAS number 224785-90-4
ATC code G04BE09
PubChem 110634
Drug Bank APRD00699
Formula C23H32N6O4S
Bioavailability 15%
Excretion Biliary
Protein binding 95%
Half life 4–5 hours
Metabolism Hepatic (CYP3A4)
Pregnancy cat B3 (Au), B ( U.S. )
Legal status S4 (Au), POM ( UK ), ? >-only ( U.S. )
Routes Oral