Indinavir: Potent Protease Inhibition for HIV Management
| Product dosage: 400 mg | |||
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Synonyms | |||
Indinavir is a protease inhibitor antiretroviral medication indicated for the treatment of human immunodeficiency virus (HIV-1) infection. It functions by selectively binding to the active site of the HIV-1 protease enzyme, thereby inhibiting the cleavage of viral polyprotein precursors into functional proteins required for viral replication. This agent is typically administered in combination with other antiretroviral agents as part of a highly active antiretroviral therapy (HAART) regimen, which is critical for suppressing viral load, increasing CD4 cell counts, and delaying the progression to acquired immunodeficiency syndrome (AIDS). Proper adherence to the prescribed regimen is essential to maintain efficacy and reduce the risk of developing drug-resistant viral strains.
Features
- Active pharmaceutical ingredient: Indinavir sulfate
- Standard formulation: 200 mg, 400 mg capsules
- Mechanism: Selective inhibition of HIV-1 protease
- Bioavailability: Approximately 65% under fasting conditions
- Half-life: 1.5–2 hours in adults
- Metabolism: Hepatic, primarily via CYP3A4
- Excretion: Renal (<20%) and fecal
Benefits
- Effectively reduces HIV viral load in plasma when used as part of combination therapy
- Helps restore and preserve immune function by increasing CD4+ T-cell counts
- Delays disease progression and reduces the incidence of opportunistic infections
- Contributes to improved long-term survival rates among HIV-positive individuals
- May be used in certain post-exposure prophylaxis protocols following potential HIV exposure
- Supports adherence through well-characterized dosing schedules when combined with pharmacokinetic boosters
Common use
Indinavir is primarily used in the management of HIV-1 infection in adults and pediatric patients over 4 years of age. It is always prescribed as part of a combination antiretroviral regimen, never as monotherapy, to maximize viral suppression and minimize resistance development. Common companion agents include nucleoside reverse transcriptase inhibitors such as zidovudine or lamivudine. Its use requires careful consideration of the patient’s clinical history, concomitant medications, and baseline renal and hepatic function.
Dosage and direction
The recommended adult dosage of indinavir is 800 mg orally every 8 hours. To ensure optimal absorption, it should be taken 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 liters of fluid daily) is recommended to reduce the risk of nephrolithiasis. Dosage adjustments are necessary when co-administered with certain drugs that affect CYP3A4 activity, such as rifampin or ketoconazole. Pediatric dosing is based on body surface area or weight and must be determined by a specialist.
Precautions
Patients should be monitored for signs of nephrolithiasis, including flank pain and hematuria. Liver function tests are recommended at baseline and periodically during treatment, as transaminase elevations may occur. Use with caution in patients with hepatic impairment, hemophilia, or diabetes mellitus. Indinavir may exacerbate hyperglycemia and should be used cautiously in patients with pre-existing glucose intolerance. Sun exposure should be limited due to potential photosensitivity reactions.
Contraindications
Indinavir is contraindicated in patients with known hypersensitivity to indinavir or any component of the formulation. Concomitant use with drugs highly dependent on CYP3A4 for clearance (e.g., alfuzosin, simvastatin, lovastatin, sildenafil for pulmonary arterial hypertension) is contraindicated due to the risk of serious adverse reactions. It is also contraindicated with drugs that strongly induce CYP3A4, such as St. John’s wort, due to reduced indinavir concentrations and potential loss of virologic response.
Possible side effect
Common adverse reactions include nephrolithiasis (≥12%), nausea, abdominal pain, headache, asthenia, blurred vision, dizziness, and rash. Laboratory abnormalities may include hyperbilirubinemia (14%), asymptomatic hyperglycemia, elevated ALT/AST, and lipid abnormalities. Less frequently, patients may experience thrombocytopenia, hemolytic anemia, or acute hepatitis. Lipodystrophy and metabolic changes have been associated with protease inhibitor class effects.
Drug interaction
Indinavir is a substrate and inhibitor of CYP3A4 and may interact with numerous medications. Concurrent use with other CYP3A4 inhibitors (e.g., clarithromycin, itraconazole) may increase indinavir levels. Inducers of CYP3A4 (e.g., rifampin, carbamazepine) may decrease indinavir concentrations. Caution is advised with drugs that prolong the QT interval, antiarrhythmics, ergot derivatives, and phosphodiesterase-5 inhibitors. Dose adjustments or alternative therapies may be required.
Missed dose
If a dose is missed within 2 hours of the scheduled time, it should be taken as soon as possible. If more than 2 hours have passed, skip the missed dose and resume the regular dosing schedule. Do not double the next dose. Consistent adherence is critical to maintain therapeutic drug levels and prevent viral resistance.
Overdose
There is no specific antidote for indinavir overdose. Management includes supportive measures and monitoring of vital signs. Hemodialysis is unlikely to be effective due to high protein binding and extensive metabolism. Reported acute toxicity may include nephrolithiasis, nausea, vomiting, and diarrhea. Symptomatic treatment and adequate hydration are recommended.
Storage
Store at controlled room temperature (20–25°C or 68–77°F). Keep in the original container, tightly closed, and protect from moisture and light. Do not use beyond the expiration date printed on the packaging. Keep out of reach of children and pets.
Disclaimer
This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting or changing any medication regimen. Dosage, indications, and safety profiles may vary based on individual patient factors and regional prescribing guidelines.
Reviews
Clinical trials and post-marketing studies have demonstrated that indinavir, as part of combination antiretroviral therapy, significantly reduces viral load and improves immunologic markers in treatment-naïve and experienced patients. However, its use has declined in many regions due to the advent of better-tolerated agents with fewer dosing restrictions and side effects. Specialist consultation is recommended to determine its current role in individualized HIV treatment strategies.