Last Updated June 10, 2016
HIV protease inhibitor antiretroviral
400 mg capsules (as sulphate)
Indication: treatment of HIV infection in combination with other antiretrovirals.
Mechanism of action*: inhibits HIV-1 protease activity by binding to active site to prevent cleavage of viral polyproteins.
Pharmacokinetics*: rapidly absorbed, metabolized in the liver by CYP3A4. Tmax: 0.8 hours; half-life: ~ 2 hours. Inhibits CYP3A4 enzyme. Weakly inhibits CYP2D6.
Adult Dose: 800 mg every 8 hours, taken orally with water 1 hour before or 2 hours after a meal. Patients should consume 48 ounces of fluid daily to avoid renal calculi.
Use in Renal or Hepatic Insufficiency:
Use in Pregnancy and Breastfeeding*: US Pregnancy Category C. Not recommended for use in pregnant women. It is not known whether indinavir is excreted in human breast milk.
Use in Children: Children 4-17 years (off label): 500 mg/m2 (maximum dose 800 mg) every 8 hours.
See drug–drug interactions for medications that should not be coadministered.
Contraindicated in patients with hypersensitivity to indinavir or any of its components.
Maintain adequate hydration to avoid renal calculi.
Potential for nephrolithiasis/urolithiasis, with increased risk in paediatric patients; acute haemolytic anaemia; hepatitis; and new onset or exacerbation of diabetes mellitus, hyperglycaemia, and/or ketoacidosis.*
HIV cross-resistance with other PIs may occur.
Contraindicated: alfuzosin, amiodarone, dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, lovastatin, simvastatin, pimozide, sildenafil for pulmonary arterial hypertension, oral midazolam, triazolam, alprazolam.*
Increased concentrations of concomitant medication: ritonavir, saquinavir, antiarrhythmic agents (bepridil, systemic lidocaine, quinidine), trazodone, colchicine, quetiapine, dihydropyridine calcium channel blockers (felodipine, nifedipine, nicardipine), clarithromycin, bosentan, atorvastatin, rosuvastatin, immunosuppressants (cyclosporine, tacrolimus, sirolimus), salmeterol, fluticasone, parenteral midazolam, rifabutin, sildenafil, tadalafil, vardenafil.*
Decreased concentrations of indinavir with concomitant medication: St John’s wort, rifampicin, efavirenz, nevirapine, anticonvulsants (carbamezapine, phenobarbital, phenytoin), rifabutin, venlafaxine.*
Drug interactions between indinavir and other antiretrovirals:
Paediatric patients: higher incidence of nephrolithiasis.
Pregnancy: see above.
Nephrolithiasis/urolithiasis, haemolytic anaemia, hepatitis, hyperglycaemia, asymptomatic hyperbilirubinaemia, rash, upper respiratory infection, dry skin, pharyngitis, taste perversion, tubulointerstitial nephritis in patients with asymptomatic severe leucocyturia, fat maldistribution, possible increased bleeding in patients with haemophilia, immune reconstitution syndrome (including autoimmune disease), abdominal pain, fatigue, fever, nausea, diarrhoea, vomiting, headache, dizziness.
*Information from US prescribing information.
†Recommendation of the Southern African HIV Clinicians Society.