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Indinavir

Indinavir is a protease inhibitor used as a component of highly active antiretroviral therapy to treat HIV/AIDS. More

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Description

Indinavir is a protease inhibitor used as a component of highly active antiretroviral therapy to treat HIV/AIDS.

Generic Name

Indinavir

Chemical names

Indinavir; Crixivan; Compound J; MK-639

Brand names

Inbec, Inbed, Ind, Indease, Indivan, Indivir, Virodin

IUPAC name

(2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-4-{[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}butyl]-N-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide

Pharmacokinetics

Oral absorption.

Actions

Indinavir inhibits the HIV viral protease enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Dosage/Dosage form

The recommended dose is 800 mg 8 hourly orally.

Therapeutic uses

Indinavir is an antiretroviral drug prescribed for the treatment of HIV infection.

Adverse effects/Side effects

Flank pain, abdominal pain, nephrolithiasis, malaise, nausea, vomiting, diarrhoea, elevated liver enzymes, hyperbilirubinaemia, raised creatinine phosphokinase and blood lipids, back pain, lipodystrophy, alopecia, acid regurgitation, dyspepsia, dry mouth, dysuria, dry skin, hyperpigmentation, headache, dizziness, somnolence, cough, dyspnoea.

Interaction

  • Increased risk of cardiac arrhythmias with amiodarone, pimozide or cisapride.
  •  Increased sedation and respiratory depression with midazolam, alprazolam and triazolam.
  •  Increased risk of ergotism with ergot derivatives.
  • Increased toxicity of drugs with narrow therapeutic index.
  • Reduced absorption with antacids. Increased concentrations with ketoconazole, delavirdine, nelfinavir and ritonavir.
  • Reduced efficacy with nevirapine, efavirenz or rifampicin.
  • Increased risk of myopathy with statins.
  • Reduced concentrations with grapefruit juice.
  • Reduced antiviral response with St. John's wort.
  • Increased concentrations of phosphodiesterase-5 inhibitors.

Contraindications

Hypersensitivity. Severe hepatic impairment.

Storage

Store at 15-30°C

Information

Molecular weight

613.7895

Molecular formula

C36H47N5O4

CAS number

150378-17-9

Precautions

  • Increased risk of urolithiasis/nephrolithiasis.
  • Ensure adequate hydration.
  • Hyperbilirubinaemia may be exacerbated.
  • Diabetes; haemophilia.
  • Monitor for signs of lipodystrophy.
  • Pregnancy and lactation.