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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 |
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