Indinavir: Potent Protease Inhibition for HIV Management
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Synonyms | |||
Indinavir is an antiretroviral medication classified as a protease inhibitor, specifically formulated for the treatment of Human Immunodeficiency Virus (HIV-1) infection. It operates by selectively inhibiting the viral protease enzyme, a critical component in the replication cycle of HIV, thereby reducing viral load and supporting immune reconstitution. This agent is typically administered in combination with other antiretroviral drugs as part of a highly active antiretroviral therapy (HAART) regimen, aligning with current clinical guidelines to optimize therapeutic outcomes and delay disease progression.
Features
- Active pharmaceutical ingredient: Indinavir sulfate
- Standard dosage form: Capsules, 200 mg, 333 mg, and 400 mg strengths
- Pharmacologic class: Protease inhibitor (antiretroviral)
- Mechanism: Selective inhibition of HIV-1 protease
- Bioavailability: Approximately 65% under fasting conditions
- Half-life: About 1.8 hours in adults
- Metabolism: Hepatic, primarily via CYP3A4
- Excretion: Renal and fecal
Benefits
- Effectively reduces HIV viral load, supporting undetectable levels when used in combination therapy
- Contributes to increased CD4+ T-cell counts, enhancing immune function
- Helps delay the progression to AIDS and reduces HIV-related morbidity and mortality
- May lower the risk of opportunistic infections due to improved immune status
- Supports long-term viral suppression with adherence to prescribed regimen
- Can be part of individualized treatment plans tailored to patient-specific factors and resistance profiles
Common use
Indinavir is indicated for the treatment of HIV-1 infection in adults and pediatric patients older than 4 years, in combination with other antiretroviral agents. It is used as a component of combination therapy to suppress viral replication, improve immunologic parameters, and reduce the risk of HIV transmission. Its use is guided by resistance testing and treatment history, and it is often reserved for scenarios where preferred first-line options are not suitable or have failed.
Dosage and direction
The recommended adult dosage of indinavir is 800 mg orally every 8 hours. It must be administered on an empty stomach, either 1 hour before or 2 hours after a meal, or with a light, low-fat snack to enhance absorption. Adequate hydration (at least 1.5 liters of fluid daily) is essential to reduce the risk of nephrolithiasis. Dosage adjustments are necessary in patients with hepatic impairment, and concomitant use with certain drugs may require modification. Pediatric dosing is based on body surface area or weight, per prescribing guidelines.
Precautions
- Monitor renal function (e.g., serum creatinine, urinalysis) regularly due to risk of nephrolithiasis and crystalluria.
- Assess liver enzymes periodically; use with caution in patients with hepatic impairment.
- Ensure adequate hydration to minimize renal complications.
- May cause hyperglycemia or exacerbate diabetes; monitor blood glucose.
- Fat redistribution and lipid abnormalities have been reported.
- Not a cure for HIV; does not reduce the risk of transmitting HIV to others.
- Use with caution in patients with hemophilia due to increased bleeding risk.
Contraindications
- Hypersensitivity to indinavir or any component of the formulation.
- Concurrent administration with drugs highly dependent on CYP3A4 for clearance and with narrow therapeutic indices, such as alfuzosin, amiodarone, cisapride, ergot derivatives, lovastatin, simvastatin, pimozide, sildenafil (for pulmonary arterial hypertension), triazolam, and oral midazolam.
- Severe hepatic impairment.
- Concomitant use with St. John’s wort, which reduces indinavir levels.
Possible side effect
Common adverse reactions include:
- Nephrolithiasis/urolithiasis
- Nausea, abdominal pain, vomiting
- Headache, dizziness, insomnia
- Asthenia/fatigue
- Diarrhea
- Rash
- Hyperbilirubinemia
- Lipodystrophy
- Increased triglycerides and cholesterol
Less frequently, acute hemolytic anemia, hepatitis, and hyperglycemia may occur.
Drug interaction
Indinavir is a potent inhibitor of CYP3A4 and is also metabolized by this enzyme. Significant interactions include:
- Rifampin, rifabutin, carbamazepine, phenobarbital, phenytoin: Decrease indinavir concentrations.
- Ketoconazole, itraconazole: Increase indinavir levels.
- Didanosine: Administer at least 1 hour apart on an empty stomach.
- Atorvastatin, other statins: Increased risk of myopathy.
- Sildenafil (for erectile dysfunction): Increased sildenafil levels; dose reduction needed.
- Oral contraceptives: Potential decreased efficacy.
Missed dose
If a dose is missed, it should be taken as soon as possible. However, if it is almost time for the next dose, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed one. Consistent adherence is critical to maintain viral suppression and prevent resistance.
Overdose
There is limited experience with indinavir overdose. Reported events include nephrolithiasis and gastrointestinal symptoms. Treatment is supportive and symptomatic; maintain hydration and monitor renal function. Hemodialysis is unlikely to be beneficial due to high protein binding and extensive metabolism.
Storage
Store at controlled room temperature, 20–25°C (68–77°F), in a tightly closed container. Protect from moisture and light. Keep out of reach of children and pets. Do not use after the expiration date.
Disclaimer
This information is for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider for personalized recommendations and to address any health concerns or before starting any new medication. Do not disregard or delay seeking professional advice based on content herein.
Reviews
Clinical studies and post-marketing reports indicate that indinavir, as part of combination therapy, effectively suppresses viral load and improves CD4 counts in many patients. However, its use has declined with the advent of better-tolerated agents with improved dosing convenience. Adherence challenges due to the strict fasting requirements and side effect profile are noted in patient-reported outcomes. Healthcare professionals emphasize the importance of regimen adherence and monitoring for renal and metabolic effects.