Sustiva: Advanced NNRTI Therapy for Effective HIV-1 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 binding directly to reverse transcriptase, blocking RNA- and DNA-dependent DNA polymerase activities. Clinically proven to reduce viral load and increase CD4 cell counts, Sustiva offers a well-established option for both treatment-naïve and experienced patients, supported by extensive clinical data and long-term safety profiles. Its once-daily dosing supports adherence, a critical factor in achieving and maintaining virologic suppression.
Features
- Contains efavirenz as the active pharmaceutical ingredient
- Available in 600 mg film-coated tablets
- Once-daily oral administration, simplifying regimen adherence
- Demonstrated high barrier to resistance within the NNRTI class
- Compatible with many other antiretroviral agents for combination therapy
- Manufactured under strict quality control standards ensuring potency and purity
Benefits
- Achieves rapid and sustained virologic suppression in treatment-naïve patients
- Supports immune reconstitution through reliable CD4+ T-cell count increases
- Reduces risk of HIV transmission by lowering viral load to undetectable levels
- Minimizes dosing frequency with a convenient once-daily regimen
- Backed by long-term clinical data demonstrating durability of response
- Provides a cost-effective option within many HAART strategies
Common use
Sustiva is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 3 months of age and older weighing at least 3.5 kg. It is commonly prescribed as part of initial therapy regimens and may be used in treatment-experienced patients with demonstrated susceptibility to efavirenz. The medication is particularly valuable in regimens where once-daily dosing is preferred to support patient adherence, and it has been extensively studied in diverse patient populations across multiple clinical trials.
Dosage and direction
The recommended adult dosage is 600 mg orally once daily. For pediatric patients, dosing is based on body weight: 100 mg for 3.5 to <5 kg, 150 mg for 5 to <7.5 kg, 200 mg for 7.5 to <15 kg, 250 mg for 15 to <20 kg, 300 mg for 20 to <25 kg, 350 mg for 25 to <32.5 kg, 400 mg for 32.5 to <40 kg, and 600 mg for ≥40 kg. Administration should occur on an empty stomach, preferably at bedtime, to minimize central nervous system effects. Tablets should be swallowed whole with water and not crushed, chewed, or broken.
Precautions
Patients should be monitored for severe psychiatric symptoms including severe depression, suicidal ideation, and non-fatal suicidal attempts. Neurological symptoms such as dizziness, insomnia, impaired concentration, and abnormal dreams are common, particularly during the first weeks of therapy. Rash may occur, with rare cases progressing to Stevens-Johnson syndrome. Hepatic function should be monitored, especially in patients with underlying hepatic disease or co-infection with hepatitis B or C. Lipid elevations may occur, requiring monitoring and management. Pregnancy should be avoided due to risk of neural tube defects; women of childbearing potential must use effective contraception.
Contraindications
Sustiva is contraindicated in patients with previously demonstrated hypersensitivity to efavirenz or any component of the formulation. Coadministration with elbasvir/grazoprevir, voriconazole, cisapride, midazolam, pimozide, triazolam, or ergot derivatives is contraindicated due to potential for serious and/or life-threatening reactions. Concomitant use with St. John’s wort is contraindicated due to reduced efavirenz concentrations and potential loss of virologic response.
Possible side effect
Common adverse reactions (≥5%) include: dizziness, insomnia, impaired concentration, somnolence, abnormal dreams, rash, nausea, fatigue, headache, and vomiting. Serious side effects may include: severe psychiatric symptoms (depression, suicidal ideation), severe skin reactions (Stevens-Johnson syndrome), hepatic failure, seizures, and immune reconstitution syndrome. Laboratory abnormalities may include elevated AST, ALT, total cholesterol, and triglycerides. Most central nervous system symptoms improve within 2-4 weeks of continued therapy.
Drug interaction
Sustiva is a moderate CYP3A4 inducer and may decrease concentrations of many drugs metabolized by this pathway. Significant interactions include reduced concentrations of: atazanavir, boceprevir, clarithromycin, itraconazole, ketoconazole, posaconazole, voriconazole, maraviroc, rifabutin, and warfarin. Coadministration with other CYP3A4 inducers may decrease efavirenz concentrations. Drugs that increase gastric pH may reduce efavirenz absorption. Comprehensive medication review is essential before initiation and during therapy.
Missed dose
If a dose is missed, patients should take it as soon as possible unless it is almost time for the next dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the next dose. Consistent adherence is critical to maintain virologic suppression and prevent development of resistance.
Overdose
Experience with efavirenz overdose is limited. Symptoms may include increased nervous system symptoms, involuntary muscle contractions, and psychosis. There is no specific antidote for efavirenz overdose. Treatment should consist of general supportive measures, including monitoring of vital signs and observation of clinical status. Since efavirenz is highly protein-bound, dialysis is unlikely to significantly remove the drug from blood.
Storage
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F). Keep in original container with tightly closed cap to protect from moisture. Keep out of reach of children and pets. Do not use after expiration date printed on packaging.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient characteristics. Patients should not alter or discontinue medication without consulting their healthcare provider. Full prescribing information including boxed warnings should be reviewed before initiation of therapy.
Reviews
Clinical trials demonstrate Sustiva-containing regimens achieve virologic suppression (<50 copies/mL) in 60-70% of treatment-naïve patients at 48 weeks. Long-term studies show maintained efficacy through 3 years of therapy. Real-world evidence supports its effectiveness in diverse populations, though neurological side effects lead to discontinuation in approximately 5% of patients. Most clinicians report favorable experience with sustained virologic control and acceptable tolerability profile when properly managed.
