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It is an inhibitor of the enzyme human immunodeficiency virus protease which is required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV.
Indinavir is a peptide analogue. It reversibly binds to the HIV encoded aspartyl protease enzyme which is involved in the degradation of poly protein into structural protein and subsequent maturation of virus particle. Binding of Indinavir to the enzyme results in immature noninfectious viral progeny.
Pharmacokinetics
Absorption: It is rapidly absorbed after oral administration. Distribution: About half of the drug is distributed as protein bound form. Metabolism: It undergoes metabolism in the liver. Excretion: The metabolites are excreted through faeces and the parent drug through urine.
On Set of Action
60 minute
Half Life
90 - 120 minute
Adverse Effects
1. Nausea
2. Vomiting
3. Diarrhoea
4. Abdominal pain
5. Crystalluria
6. Nephrolithiasis
7. Headache
8. Dizziness
9. Hyperpigmentation
10. Anaemia
11. Hyperbilirubinaemia
ContraIndications
Hypersensitivity to Indinavir
Special Precautions
1.Renal impairment
2.Hepatic dysfunction
Pregnancy
Use with caution
Breast Feeding
Contraindicated
Elderly
Use with caution
Children
Contraindicated
Neonates
Contraindicated
Interactions
HMG-CoA reductase inhibitors: Risk of myopathy including rhabdomyolysis.
Rifampin: AUC of indinavir decreased by 89%±9%.
Rifabutin: Efficacy of indinavir reduced.
Ketoconazole: Efficacy of indinavir enhanced.
Grapefruit Juice: Efficacy of indinavir decreased.
Nevirapine: Efficacy of indinavir decreased.
Indications
HIV infection
Dosage
Adult: 2.4 g / day in 3 equal divided dose; given along with other antiretroviral drugs.
Storage
Store at 15 - 30 degree C.Protect away from heat and light. Keep out of the reach of Children.
Missed Dose
Take the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.
Over Dose
Give supportive measures and treatment. |
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