| Item |
Information |
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Drug Groups
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approved |
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Description
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A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. [PubChem] |
| Indication |
Indinavir is an antiretroviral drug for the treatment of HIV infection. |
| Pharmacology |
Indinavir 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. Indinavir 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. |
| Toxicity |
Symptoms of overdose include myocardial infarction and angina pectoris. |
| Affected Organisms |
| • |
Human Immunodeficiency Virus |
|
| Biotransformation |
Hepatic. Seven metabolites have been identified, one glucuronide conjugate and six oxidative metabolites. In vitro studies indicate that cytochrome P-450 3A4 (CYP3A4) is the major enzyme responsible for formation of the oxidative metabolites. |
| Absorption |
Rapidly absorbed |
| Half Life |
1.8 (± 0.4) hours |
| Protein Binding |
60% |
| Elimination |
Less than 20% of indinavir is excreted unchanged in the urine. |
| External Links |
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