| Item |
Information |
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Drug Groups
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approved |
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Description
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Amprenavir is a protease inhibitor used to treat HIV infection. |
| Indication |
For the treatment of HIV-1 infection in combination with other antiretroviral agents. |
| Pharmacology |
Amprenavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Amprenavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs. |
| Affected Organisms |
| • |
Human Immunodeficiency Virus |
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| Biotransformation |
Hepatic. Amprenavir is metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system. The 2 major metabolites result from oxidation of the tetrahydrofuran and aniline moieties. Glucuronide conjugates of oxidized metabolites have been identified as minor metabolites in urine and feces. |
| Absorption |
Rapidly absorbed after oral administration in HIV-1-infected patients with a time to peak concentration (Tmax) typically between 1 and 2 hours after a single oral dose. The absolute oral bioavailability of amprenavir in humans has not been established. |
| Half Life |
7.1-10.6 hours |
| Protein Binding |
Very high (90%). Amprenavir has the highest affinity for alpha(1)-acid glycoprotein. |
| External Links |
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