Drug Groups

approved

Description

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

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.

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