Sustiva: Advanced Antiretroviral Therapy for HIV Management
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| Product dosage: 600mg | |||
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Synonyms | |||
Sustiva (efavirenz) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in combination with other antiretroviral agents. As a cornerstone of many highly active antiretroviral therapy (HAART) regimens, it works by inhibiting the reverse transcriptase enzyme, a critical component in the HIV replication cycle. Its once-daily dosing and high barrier to resistance make it a preferred option for both treatment-naïve and experienced patients under appropriate clinical guidance. Healthcare providers value its established efficacy profile and role in suppressing viral load to undetectable levels.
Features
- Contains efavirenz as the active pharmaceutical ingredient
- Available in 600 mg film-coated tablets for oral administration
- Formulated for once-daily dosing to enhance adherence
- Demonstrated high genetic barrier to resistance among NNRTIs
- Compatible with many other antiretroviral medications in combination therapy
- Manufactured under strict quality control standards for consistency and purity
Benefits
- Achieves and maintains viral suppression below detectable limits in plasma
- Supports immune reconstitution through sustained CD4+ cell count increases
- Reduces risk of HIV-related complications and disease progression
- Offers convenient dosing schedule to support long-term treatment adherence
- Provides well-characterized safety and efficacy profile from extensive clinical use
- Enables flexible combination with other antiretroviral agents per treatment guidelines
Common use
Sustiva is primarily prescribed as part of combination antiretroviral therapy for HIV-1 infection in adults and pediatric patients weighing at least 40 kg. It is commonly used in first-line treatment regimens according to established guidelines from health authorities such as the WHO and CDC. The medication may be used in both treatment-naïve patients and those switching regimens due to tolerability or adherence issues with other agents, provided there is no documented resistance to efavirenz. Clinical decisions should always consider individual patient factors, including viral load, CD4 count, comorbid conditions, and potential drug interactions.
Dosage and direction
The recommended adult dosage is 600 mg orally once daily. Administration should occur on an empty stomach, preferably at bedtime, to minimize potential nervous system symptoms. For pediatric patients weighing 40 kg or more, the adult dosage applies. The tablet should be swallowed whole with water and not crushed, chewed, or broken. Dosage adjustments may be necessary when coadministered with certain medications that affect CYP3A4 metabolism. Treatment should be initiated and monitored by healthcare providers experienced in HIV management.
Precautions
Patients should be informed that Sustiva may cause dizziness, insomnia, impaired concentration, or abnormal dreams, particularly during the first weeks of therapy. Psychiatric symptoms such as severe depression, suicidal ideation, or aggressive behavior have been reported and require immediate medical attention. Rash occurs in approximately 26% of patients, with rare cases of Stevens-Johnson syndrome. Liver function should be monitored regularly, as hepatic events including hepatic failure have occurred. Use during pregnancy requires careful risk-benefit assessment due to potential neural tube defects.
Contraindications
Sustiva is contraindicated in patients with known hypersensitivity to efavirenz or any component of the formulation. Coadministration with elbasvir/grazoprevir, voriconazole, or certain ergot derivatives is contraindicated due to potentially serious interactions. The medication should not be used as monotherapy or with other NNRTIs. Patients with severe hepatic impairment should not receive Sustiva without careful consideration of alternatives. Concomitant use with St. John’s wort is contraindicated due to reduced efavirenz concentrations.
Possible side effects
Common adverse reactions (≥10%) include rash, dizziness, nausea, headache, fatigue, insomnia, and abnormal dreams. Psychiatric symptoms such as depression, anxiety, and suicidal ideation may occur. Laboratory abnormalities may include elevated liver enzymes, increased cholesterol and triglycerides. Less frequent but serious side effects include severe skin reactions, hepatic failure, convulsions, and pancreatitis. Immune reconstitution inflammatory syndrome (IRIS) may occur during initial treatment.
Drug interaction
Efavirenz is a moderate inducer of CYP3A4 and CYP2B6, potentially decreasing concentrations of coadministered drugs metabolized by these enzymes. Significant interactions occur with: anticonvulsants (carbamazepine, phenobarbital), antifungals (voriconazole), hepatitis C antivirals, methadone (may require dosage adjustment), and hormonal contraceptives (alternative methods recommended). Protease inhibitors generally require dosage adjustments when combined with efavirenz. Comprehensive medication review is essential before initiation.
Missed dose
If a dose is missed within 6 hours of the regular dosing time, the patient should take the missed dose immediately then resume the normal schedule. If more than 6 hours have passed, the missed dose should be skipped and the next dose taken at the regular time. Patients should not double the dose to make up for a missed dose. Consistent adherence is critical to maintain viral suppression and prevent resistance development.
Overdose
Limited experience exists with efavirenz overdose. Reported events include increased nervous system symptoms, involuntary muscle contractions, and psychosis. Management should include supportive measures with monitoring of vital signs and ECG. Since efavirenz is highly protein-bound, dialysis is unlikely to be beneficial. Activated charcoal may be administered if presented soon after ingestion. Medical toxicology consultation is recommended for significant overdose.
Storage
Store at 25°C (77°F); excursions permitted between 15-30°C (59-86°F). Keep in original container with tight closure to protect from moisture. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Protect from light and excessive humidity. Do not store in bathroom or near kitchen sink.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient circumstances. The prescribing physician should be consulted for complete information regarding indications, dosage, warnings, and precautions. Patients should not alter or discontinue medication without medical supervision.
Reviews
Clinical studies demonstrate sustained virologic response rates of 60-70% at 48 weeks in treatment-naïve patients when combined with two NRTIs. Many clinicians report satisfactory long-term outcomes with appropriate management of side effects. Patient satisfaction surveys indicate appreciation for once-daily dosing despite initial CNS effects that typically diminish over time. The drug maintains its position in treatment guidelines despite newer alternatives, particularly in resource-limited settings due to its cost-effectiveness and extensive experience base.