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. This action inhibits viral replication, reduces viral load, and supports immune reconstitution in appropriate patient populations. Clinical studies have demonstrated its efficacy in both treatment-naïve and experienced individuals when used as part of a comprehensive therapeutic strategy.
Features
- Contains efavirenz as the active pharmaceutical ingredient
- Available in 600 mg film-coated tablets for oral administration
- Formulated for once-daily dosing to support adherence
- Demonstrated high barrier to resistance among NNRTI class agents
- Compatible with many backbone nucleoside reverse transcriptase inhibitors (NRTIs)
- Standardized manufacturing under current Good Manufacturing Practices (cGMP)
Benefits
- Potent viral suppression – achieves and maintains undetectable viral loads in compliant patients
- Convenient dosing schedule – once-daily regimen supports long-term treatment adherence
- Established efficacy profile – backed by extensive clinical trial data and real-world experience
- Improved CD4 cell recovery – supports immune system restoration when used in combination therapy
- Reduced transmission risk – viral suppression decreases likelihood of HIV transmission to others
- Flexible combination options – can be paired with various antiretroviral agents per treatment guidelines
Common use
Sustiva is primarily prescribed as part of combination antiretroviral therapy for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 40 kg. It is commonly used in both initial treatment regimens and as a component of simplified maintenance therapy following virologic suppression. The medication may be particularly suitable for patients who require once-daily dosing convenience and have demonstrated tolerance to its side effect profile. Healthcare providers typically consider Sustiva within the context of current treatment guidelines, patient comorbidities, potential drug interactions, and resistance testing results when designing individualized therapeutic regimens.
Dosage and direction
The recommended adult dosage is 600 mg orally once daily. Administration should occur on an empty stomach, preferably at bedtime, to improve tolerability of nervous system symptoms that may occur during initial treatment. Tablets should be swallowed whole with water and not crushed, chewed, or broken. For pediatric patients weighing 40 kg or more, the adult dosage applies. Dosage adjustment may be necessary when coadministered with certain medications that affect efavirenz metabolism, particularly rifampin, where an increase to 800 mg daily may be considered. Hepatic impairment requires careful consideration and potential dosage modification based on severity.
Precautions
Patients should be informed about potential central nervous system symptoms including dizziness, insomnia, impaired concentration, and abnormal dreams, which typically diminish within 2-4 weeks of initiation. Psychiatric symptoms such as severe depression, suicidal ideation, and aggressive behavior have been reported and require immediate medical attention. Liver function should be monitored regularly due to risk of hepatic toxicity. Pregnancy testing should be performed before initiation in women of childbearing potential due to potential fetal harm. Lipid profiles should be monitored as treatment may increase cholesterol and triglyceride levels. Patients should avoid becoming pregnant during therapy and use effective contraception.
Contraindications
Sustiva is contraindicated in patients with known hypersensitivity to efavirenz or any component of the formulation. Coadministration with elbasvir/grazoprevir, glecaprevir/pibrentasvir, or voriconazole is contraindicated due to potentially dangerous interactions. Concomitant use with St. John’s wort is prohibited due to reduced efavirenz concentrations and potential loss virologic response. Patients with severe hepatic impairment should not use Sustiva without careful risk-benefit assessment and possible dosage adjustment under specialist supervision.
Possible side effects
Very common (>10%): dizziness, headache, insomnia, abnormal dreams, fatigue, rash, nausea Common (1-10%): depression, anxiety, impaired concentration, somnolence, vomiting, diarrhea, increased triglycerides, increased cholesterol Uncommon (0.1-1%): suicidal ideation, psychosis, hepatitis, pancreatitis, Stevens-Johnson syndrome Rare (<0.1%): hepatic failure, erythema multiforme, convulsions Most adverse reactions are mild to moderate and often resolve with continued therapy. Nervous system symptoms typically improve within the first month of treatment. Severe skin reactions or psychiatric symptoms require immediate medical evaluation and possible discontinuation.
Drug interaction
Sustiva is both a substrate and inducer of CYP3A4 and CYP2B6 enzymes, resulting in numerous potential interactions. It reduces concentrations of methadone, bupropion, voriconazole, and certain anticonvulsants. Concentrations are increased by CYP3A4 inhibitors like ketoconazole and decreased by inducers like rifampin. Coadministration with other NNRTIs is generally not recommended. Significant interactions occur with certain antiretroviral agents, particularly protease inhibitors, requiring dosage adjustments or alternative selections. Healthcare providers should conduct comprehensive medication reviews before initiation and during therapy.
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 regularly scheduled time. Patients should not double the dose to make up for a missed dose. Consistent adherence is critical to maintain virologic suppression and prevent resistance development. Healthcare providers should reinforce adherence counseling at each follow-up visit.
Overdose
Experience with efavirenz overdose is limited. Reported symptoms may include increased nervous system symptoms, involuntary muscle contractions, and altered mental status. 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. Gastric lavage may be considered if performed soon after ingestion. Administration of activated charcoal may help reduce drug absorption. Due to high protein binding, dialysis is unlikely to provide benefit. Healthcare providers should contact a poison control center for current management recommendations.
Storage
Store at 25°C (77°F); excursions permitted to 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 after the expiration date printed on the packaging. Avoid exposure to excessive heat or humidity. Do not transfer tablets to other containers as this may affect stability. Proper disposal of unused medication should follow local regulations for antiretroviral agents.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient circumstances. Always follow the prescribing information provided with the medication and consult appropriate clinical guidelines. Patients should not alter their treatment regimen without consulting their healthcare provider. The manufacturer and distributors are not liable for any damages resulting from the use or misuse of this information.
Reviews
Clinical trials demonstrate Sustiva-containing regimens achieve virologic suppression in 60-80% of treatment-naïve patients at 48 weeks. Real-world evidence supports sustained efficacy with appropriate adherence, though nervous system side effects lead to discontinuation in approximately 5% of patients. Many clinicians appreciate its once-daily dosing and high genetic barrier to resistance compared to other NNRTIs. Patient satisfaction surveys indicate high adherence rates despite initial side effects, with most reporting improved quality of life following viral suppression. Long-term follow-up studies show maintained efficacy through 5 years in compliant patients with regular monitoring.