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 functions by binding directly to reverse transcriptase, blocking RNA-dependent and DNA-dependent DNA polymerase activities. This mechanism effectively inhibits viral replication, reduces viral load, and supports immune reconstitution in appropriate patient populations. Its once-daily dosing and high barrier to resistance—when used appropriately—make it a clinically valuable option within comprehensive HIV management strategies.
Features
- Active ingredient: Efavirenz 600 mg
- Pharmacologic class: Non-nucleoside reverse transcriptase inhibitor (NNRTI)
- Standard formulation: Film-coated tablet for oral administration
- Dosing frequency: Once daily, preferably at bedtime
- FDA-approved for use in combination therapy for HIV-1 infection
- Available in both brand and generic formulations
Benefits
- Potent viral suppression: Effectively reduces HIV-1 RNA viral load, supporting undetectable status goals.
- Immune system recovery: Contributes to CD4+ T-cell count increases, reducing risk of opportunistic infections.
- Convenient dosing regimen: Once-daily administration improves adherence compared to multi-dose alternatives.
- High genetic barrier to resistance: When used in combination therapy, helps maintain long-term virologic control.
- Extensive clinical experience: Backed by over two decades of efficacy and safety data in diverse patient populations.
- Compatibility with many ART backbones: Can be effectively paired with NRTIs, integrase inhibitors, or other classes.
Common use
Sustiva is indicated for the treatment of HIV-1 infection in adults and pediatric patients aged 3 months and older weighing at least 3.5 kg, in combination with other antiretroviral agents. It is commonly prescribed as part of initial therapy regimens and may be used in treatment-experienced patients with demonstrated susceptibility. Clinical decision-making should consider baseline viral load, CD4+ count, comorbid conditions, potential drug interactions, and patient lifestyle factors. It is particularly valuable in regimens prioritizing once-daily dosing and long-term adherence support.
Dosage and direction
Adults: The recommended dosage is 600 mg orally once daily.
Pediatric patients: Dosing is based on body weight:
- 3.5 kg to <5 kg: 100 mg daily
- 5 kg to <7.5 kg: 150 mg daily
- 7.5 kg to <15 kg: 200 mg daily
- 15 kg to <20 kg: 250 mg daily
- 20 kg to <25 kg: 300 mg daily
- 25 kg to <32.5 kg: 350 mg daily
- 32.5 kg to <40 kg: 400 mg daily
- ≥40 kg: 600 mg daily
Administration should occur on an empty stomach, preferably at bedtime, to improve tolerability of central nervous system effects. Tablets should be swallowed whole with water. For patients unable to swallow tablets, alternative formulations or compounding options should be discussed with a healthcare provider.
Precautions
- Psychiatric symptoms: Monitor for severe depression, suicidal ideation, or aggressive behavior, particularly during initial treatment phases.
- Central nervous system effects: Dizziness, insomnia, impaired concentration, and abnormal dreams are common; caution patients about operating machinery.
- Hepatotoxicity: Monitor liver enzymes before and during treatment; use with caution in patients with hepatic impairment.
- Lipid effects: May increase total cholesterol and triglycerides; monitor lipid profile periodically.
- Rash: Usually mild-to-moderate maculopapular eruptions; discontinue if severe rash or accompanied by systemic symptoms.
- Pregnancy: Not recommended during first trimester due to potential fetal harm; pregnancy testing recommended before initiation.
Contraindications
- Hypersensitivity to efavirenz or any component of the formulation
- Coadministration with elbasvir/grazoprevir, voriconazole, or pimozide
- Patients with severe hepatic impairment (Child-Pugh Class C)
- Concurrent use with other medications highly dependent on CYP3A4 clearance with narrow therapeutic indices
Possible side effects
Very common (>10%):
- Dizziness
- Insomnia
- Abnormal dreams
- Rash
- Fatigue
- Nausea
Common (1-10%):
- Depression
- Anxiety
- Impaired concentration
- Headache
- Diarrhea
- Increased cholesterol/triglycerides
Less common (<1%):
- Severe skin reactions (Stevens-Johnson syndrome)
- Hepatotoxicity
- Suicidal ideation
- Pancreatitis
- Convulsions
Drug interaction
Sustiva is a moderate CYP3A4 inducer and potential inhibitor of CYP2C9/2C19, resulting in numerous clinically significant interactions:
- Contraindicated: Voriconazole, pimozide, elbasvir/grazoprevir
- Requires dosage adjustment: Atorvastatin, rifabutin, bupropion, methadone
- May reduce efficacy of: Oral contraceptives, warfarin, calcium channel blockers, some antifungals
- Concentrations affected by: CYP3A4 inhibitors (e.g., ketoconazole) may increase efavirenz levels
Comprehensive medication review is essential before initiation and when adding new medications.
Missed dose
If a dose is missed, take it as soon as possible unless it is almost time for the next dose. Do not double the next dose. Maintaining consistent timing is important for therapeutic drug levels and resistance prevention. If vomiting occurs within hours of dosing, consult healthcare provider regarding potential redosing.
Overdose
Limited experience exists with efavirenz overdose. Symptoms may include increased nervous system symptoms, involuntary muscle contractions, and hepatic abnormalities. There is no specific antidote; treatment should consist of general supportive measures including monitoring of vital signs and ECG. Charcoal may be administered if presented soon after ingestion. Hemodialysis is unlikely to be effective due to high protein binding.
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 after expiration date printed on packaging.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made in consultation with a qualified healthcare professional familiar with the patient’s complete medical history. Dosage and administration may vary based on individual patient factors. Always refer to the full prescribing information for complete details.
Reviews
“Sustiva has been a mainstay in my HIV practice for years. The once-daily dosing supports excellent adherence, and most patients tolerate the CNS effects which typically diminish after several weeks. Its robust efficacy data and high barrier to resistance make it a reliable choice in appropriate patients.” – Infectious Disease Specialist, 15 years experience
“While the side effect profile requires careful management, particularly regarding neuropsychiatric effects, Sustiva’s potency and convenience make it valuable within combination regimens. Monitoring and patient education are crucial for success.” – HIV Clinical Pharmacist
“Patients who successfully tolerate the initial adjustment period often achieve excellent long-term virologic suppression. The generic availability has improved accessibility while maintaining therapeutic efficacy.” – Clinical Researcher, HIV Therapeutics