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QuickView for Indinavir (compound)

Name: Indinavir
PubChem Compound ID: 11954281
Description: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Molecular formula: C38H55N5O9S
Molecular weight: 757.938 g/mol
Indinavir sulfate ethanolate (JAN); Indinavir sulfate ethanolate; Crixivan; D02861; Crixivan (TN)
Name: Indinavir
Name (isomeric): DB00224
Drug Type: small molecule
Description: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Compound J; Indinavir sulfate
Brand: Crixivan
Category: HIV Protease Inhibitors, Anti-HIV Agents
CAS number: 150378-17-9
Indication: Indinavir is an antiretroviral drug for the treatment of HIV infection.
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 th...
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Mechanism of Action: Indinavir inhibits the HIV viral protease enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Absorption: Rapidly absorbed
Protein binding: 60%
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.
Route of elimination: Less than 20% of indinavir is excreted unchanged in the urine.
Half Life: 1.8 (± 0.4) hours
Toxicity: Symptoms of overdose include myocardial infarction and angina pectoris.
Affected organisms: Human Immunodeficiency Virus
Food interaction:
Avoid taking with grapefruit juice
Avoid excessive or chronic alcohol use.
Take on empty stomach: 1 hour before or 2 hours after meals.
Take with a full glass of water.
Drug interaction:
ZolpidemIndinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if indinavir is initiated, discontinued or dose changed.
TrazodoneThe protease inhibitor, Indinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism via CYP3A4. Monitor for changes in Trazodone efficacy/toxicity if Indinavir is initiated, discontinued or dose changed.
St. John's WortSt. John's Wort decreases the effect of indinavir
ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinib
TolterodineIndinavir may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
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