Indinavir: Potent Protease Inhibition for Advanced HIV Management
| Product dosage: 400 mg | |||
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Synonyms | |||
Indinavir sulfate is a highly selective protease inhibitor indicated for the treatment of human immunodeficiency virus (HIV-1) infection. It functions by binding to the active site of the HIV-1 protease enzyme, effectively preventing the cleavage of viral polyprotein precursors into functional proteins required for viral maturation and infectivity. This agent is typically prescribed as part of a combination antiretroviral therapy (ART) regimen to reduce viral load, increase CD4+ cell counts, and delay disease progression. Proper adherence to dosing and dietary guidelines is essential to maintain therapeutic drug levels and minimize resistance development.
Features
- Active pharmaceutical ingredient: Indinavir sulfate
- Mechanism: Selective inhibition of HIV-1 protease
- Formulation: Capsules for oral administration
- Bioavailability: Enhanced by acidic conditions; requires administration with water on an empty stomach or with a light, low-fat meal
- Half-life: Approximately 1.5–2 hours in adults
- Metabolism: Hepatic, primarily via CYP3A4 isoenzyme
- Excretion: Renal and fecal
Benefits
- Significantly reduces HIV-1 RNA viral load in treatment-naïve and experienced patients
- Increases CD4+ T lymphocyte counts, supporting immune reconstitution
- Delays progression to AIDS-defining illnesses and mortality
- Provides a well-established option within combination antiretroviral regimens
- Demonstrates high barrier to resistance when used appropriately in combination therapy
- Available in generic formulations, improving accessibility
Common use
Indinavir is indicated for the treatment of HIV-1 infection in adults and pediatric patients aged 4 years and older, in combination with other antiretroviral agents. It is used in both treatment-naïve individuals and those who have previously received antiretroviral therapy. Clinical use is guided by resistance testing where available, and it is often incorporated into regimens including nucleoside reverse transcriptase inhibitors (NRTIs) to maximize viral suppression.
Dosage and direction
The recommended adult dosage is 800 mg (two 400 mg capsules) orally every 8 hours. Must be taken with water on an empty stomach (1 hour before or 2 hours after a meal) or with a light, low-fat snack. Adequate hydration (at least 1.5 L daily) is recommended to reduce risk of nephrolithiasis. Dosage adjustments are required when co-administered with certain CYP3A4 inducers or inhibitors. Pediatric dosing is based on body surface area or weight—consult prescribing information.
Precautions
Monitor liver function tests at baseline and during therapy; use with caution in patients with hepatic impairment. Assess for signs of nephrolithiasis (flank pain, hematuria). May cause hyperglycemia or exacerbate diabetes; monitor glucose levels. Redistribution/accumulation of body fat may occur. Not a cure for HIV; does not reduce risk of transmission. Use effective barrier contraception.
Contraindications
Hypersensitivity to indinavir or any component of the formulation. Concurrent use with drugs highly dependent on CYP3A4 for clearance and with narrow therapeutic indices (e.g., alfuzosin, simvastatin, lovastatin, sildenafil for pulmonary hypertension, triazolam, oral midazolam). Contraindicated with strong CYP3A4 inducers such as rifampin.
Possible side effect
Common: nausea, abdominal pain, headache, asthenia, blurred vision, dizziness, metallic taste, rash, dry skin. Nephrolithiasis/urolithiasis reported in approximately 9% of patients. Less common: hyperbilirubinemia, thrombocytopenia, hepatitis, hyperglycemia, fat redistribution, kidney dysfunction.
Drug interaction
Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) increase indinavir levels—reduce indinavir dose to 600 mg every 8 hours. CYP3A4 inducers (e.g., rifampin, St. John’s wort) decrease levels—avoid concomitant use. May increase levels of CYP3A4 substrates (e.g., calcium channel blockers, ergot derivatives, PDE5 inhibitors). Didanosine should be taken at least 1 hour apart.
Missed dose
If a dose is missed within 2 hours of the scheduled time, take as soon as possible. If more than 2 hours have passed, skip and resume at next scheduled time. Do not double dose.
Overdose
No specific antidote. Treatment is supportive. Hemodialysis unlikely to be effective due to high protein binding and extensive metabolism. Monitor vital signs, hydration, and renal function.
Storage
Store at 15–30°C (59–86°F). Keep in original container; protect from moisture.
Disclaimer
This information is for educational purposes and does not replace professional medical advice. Always consult a healthcare provider for diagnosis, treatment decisions, and personalized medical guidance. Do not initiate or discontinue therapy without physician supervision.
Reviews
Clinical trials and post-marketing experience support the efficacy of indinavir in reducing viral load and increasing CD4+ counts when used in combination regimens. Tolerability is generally acceptable with adherence to hydration and dietary recommendations. Nephrolithiasis remains a notable adverse effect requiring monitoring. Resistance patterns should guide use in treatment-experienced patients.