Indinavir

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Crixivan; Belgium: Crixivan; Bulgaria: Crixivan; Cyprus: Crixivan; Czech Republic: Crixivan; Denmark: Crixivan; Estonia: Crixivan; Finland: Crixivan; France: Crixivan; Germany: Crixivan; Greece: Crixivan; Hungary: Crixivan; Ireland: Crixivan; Italy: Crixivan; Latvia: Crixivan; Lithuania: Crixivan; Luxembourg: Crixivan; Malta: Crixivan; Netherlands: Crixivan; Poland: Crixivan; Portugal: Crixivan; Romania: Crixivan; Slovakia: Crixivan; Slovenia: Crixivan; Spain: Crixivan; Sweden: Crixivan; UK: Crixivan.

North America

Canada: Crixivan; USA: Crixivan.

Latin America

Argentina: Avural, Crixivan, Elvenavir, Forli; Brazil: Crixivan, Indinax; Mexico: Aviran, Crixivan, Indilan.

Asia

Japan: Crixivan.

Drug combinations

Chemistry

Indinavir Sulfate: C~36~H~47~N~5~O~4~ H~2~SO~4~. Mw: 711.87. (1) D-erythro-Pentonamide, 2,3,5-trideoxy-N-(2,3-dihydro-2-hydroxy-1H-inden-1-yl)-5-[2-[[(1,1-dimethylethyl)amino]carbonyl]-4-(3-pyridinylmethyl)-1-piperazinyl]-2-(phenylmethyl)-; [1(1S,2R,5(S)]-, sulfate (1:1); (2)(αR,γS,2S)-α-Benzyl-2-(tert-butylcarbamoyl)-γ-hydroxy-N-[(1S,2R)-2-hydroxy-1-indanyl]-4-(3-pyridylmethyl)-1-piperazinevaleramide sulfate (1:1). CAS-157810-81-6 (1995).

Pharmacologic Category

Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE02).

Mechanism of action

Indinavir is a human immunodeficiency virus protease inhibitor. HIV protease is an enzyme required for cleavage of viral polyprotein precursors into individual functional proteins found in infectious HIV. Inhibition prevents cleavage of these polyproteins resulting in formation of immature noninfectious viral particles.

Therapeutic use

Treatment of HIV infection in conjunction with other antiretrovirals.

Pregnancy and lactiation implications

Associated with increased risk of hyperglycemia. Use not recommended in pregnant patients.

Unlabeled use

Contraindications

Hypersensitivity to indinavir or any component of the formulation. Use of alprazolam, amiodarone, cisapride, triazolam, midazolam, pimozide, or ergot alkaloids.

Warnings and precautions

May cause fat redistribution. Hemolytic anemia reported. Immune reconstitution syndrome possible. May cause nephrolithiasis/urolithiasis. May cause tubulointerstitial nephritis (rare). Changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, DKA, and new-onset diabetes mellitus reported. Use with caution in hemophilia A or B (risk of increased bleeding). May cause hepatitis and/or exacerbate pre-existing hepatic dysfunction. High potential for CYP-mediated interactions. Hyperbilirubinemia reported (should not be used in neonates). Use with caution in the elderly.

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