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Sustiva

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Sustiva (efavirenz) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection in adults and children. It helps maintain a low viral load by blocking specific enzymes needed for virus replication, supporting long-term immune system function when used as part of a combination therapy regimen.


Ingredient
Category
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Efavirenz
Reference Brand
Efavirenz
Manufacturer
Bristol-Myers Squibb
Product Form
Tablet, Capsule
Regulatory Classification
Rx
Primary Category
Antiviral, HIV Treatment
Product Category
Antivirals for systemic use, Direct acting antivirals, Non-nucleoside reverse transcriptase inhibitors
Pharmacological Class
NNRTI
Clinical Indications
Manufacturer Description
Part of a combination therapy (HAART) used to manage HIV and prevent the progression of the virus.
Mechanism of Action
It prevents the HIV virus from multiplying by blocking the reverse transcriptase enzyme, which the virus needs to create new copies of itself.
Route of Administration
Oral
Onset Time
Within days
Duration
24 hours
Contraindications
Severe liver disease, Concurrent use of St John's Wort, QT interval prolongation
Severe Adverse Events
Severe depression, Psychotic reactions, Liver failure, Severe skin peeling
Common Side Effects
Fatigue, Nausea, Headache
Uncommon Side Effects
Dizziness, Sleep disturbances, Concentration problems, Rash
Drug Interactions
Statins, St John's Wort, Anticonvulsants, Rifampicin
Pregnancy Safety Warnings
Can be used; however, close medical monitoring is required.
Age Restrictions
Adults and children over 3 months
Storage Guidelines
Store at room temperature.
Related Products
Nevirapine, Etravirine, Rilpivirine

Sustiva FAQ

Can Sustiva be taken on an empty stomach?

Yes. Efavirenz may be taken with or without food. A high-fat meal can slightly increase absorption, which might intensify central nervous system effects for some individuals.

What does the imprint on a Sustiva pill look like?

In the UK, the 200 mg tablet typically bears the imprint “EF 200” and the 600 mg tablet “EF 600”. Imprints help verify authenticity when compared with the packaging insert.

Will taking Sustiva affect a drug test for employment?

Efavirenz is not a controlled substance and is not screened for in standard workplace drug testing panels. However, any antiretroviral medication will be listed on a medical questionnaire if required.

Is there a generic version of Sustiva available in the UK?

Yes. Efavirenz is marketed as a generic tablet by multiple manufacturers. The active ingredient and dosage are identical; only the branding differs.

How does Sustiva compare with other NNRTIs like nevirapine?

Both belong to the NNRTI class, but efavirenz has a longer half-life allowing once-daily dosing, whereas nevirapine often requires twice-daily dosing. Efavirenz is more commonly associated with vivid dreams and CNS side effects, while nevirapine has a higher risk of hepatotoxicity.

Can Sustiva be used while traveling internationally?

Yes, but you should carry a copy of the prescription and a letter from your clinician confirming medical necessity, as some countries require documentation for antiretroviral drugs at customs.

Does Sustiva interact with over-the-counter herbal supplements?

St. John’s wort induces CYP enzymes and can reduce efavirenz concentrations, potentially compromising viral suppression. Patients should discuss any herbal products with their healthcare provider.

What should I do if I experience a rash while on Sustiva?

Mild rashes can be monitored, but if the rash spreads, is accompanied by fever, or blisters, stop the medication and seek urgent medical attention as it could signal a serious skin reaction.

Are there any special considerations for pilots or drivers?

Because efavirenz can cause dizziness, visual disturbances, or sleep-related side effects, individuals operating aircraft or heavy machinery should assess their response to the medication before performing safety-critical tasks. In the UK, the Civil Aviation Authority requires reporting of any medication that may impair performance.

How long does it take for viral load to become undetectable after starting Sustiva?

Most patients achieve an undetectable viral load within 12 weeks when efavirenz is part of a fully suppressive HAART regimen, though individual response may vary based on baseline viral load and adherence.

What is Sustiva?

Sustiva is a brand-name medication that contains efavirenz as its active ingredient. It belongs to the antiretroviral class of drugs used to treat Human Immunodeficiency Virus (HIV) infection. In the United Kingdom, Sustaina is a prescription-only medicine (POM) regulated by the Medicines and Healthcare products Regulatory Agency (MHRA). It is supplied as a pill in two strengths: 200 mg and 600 mg.

How Sustiva Works in the Body

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It binds directly to the HIV-1 reverse transcriptase enzyme, blocking the enzyme’s ability to copy viral RNA into DNA. This interruption prevents the virus from replicating inside host cells. The drug is absorbed well after oral administration, reaching peak plasma concentrations within 3-5 hours. Its half-life is long (≈40-55 hours), allowing once-daily dosing. By reducing the amount of circulating virus, efavirenz helps to restore and preserve immune function.

Conditions Treated by Sustiva

Sustiva is approved by the MHRA for use in combination with other antiretroviral agents as part of highly active antiretroviral therapy (HAART) for:

  • Adults and adolescents (≥12 years) with HIV-1 infection
  • When used with two nucleoside reverse transcriptase inhibitors (NRTIs) or with a boosted protease inhibitor.

The medication is not approved for HIV-2 infection or for use as a single-agent therapy.

Patient Suitability and Contraindications

Who Should Use Sustiva?

  • Adults and adolescents with confirmed HIV-1 infection who require an NNRTI as part of a combination regimen.
  • Individuals whose viral load and CD4 count indicate the need for HAART according to current UK guidelines.

Absolute Contraindications

  • Known hypersensitivity to efavirenz or any of the pill’s inactive ingredients.
  • Pregnant women (Category D): efavirenz is associated with fetal neural tube defects when exposure occurs in the first trimester. It is contraindicated in pregnancy unless the benefits outweigh the risks and no safer alternatives are available.
  • Severe hepatic impairment (Child-Pugh Class C) because drug clearance is markedly reduced.

Relative Contraindications / Precautions

  • Mild to moderate hepatic impairment (Child-Pugh A or B) - dose adjustment may be required.
  • History of psychiatric illness - efavirenz can cause or worsen depression, anxiety, and vivid dreams.
  • Concurrent use of drugs that strongly induce CYP2B6 (e.g., carbamazepine, phenytoin) - may lower efavirenz concentrations.
  • Renal impairment - no dosage change needed, but monitor for accumulation of co-administered drugs cleared renally.

Special Populations

  • Pregnancy & Lactation: Efavirenz is not recommended during the first trimester. If used later in pregnancy, close obstetric monitoring is essential. Efavirenz is excreted in breast milk; breastfeeding is generally discouraged while on therapy.
  • Elderly patients: May be more prone to central nervous system (CNS) side effects; start at the lowest effective dose and titrate cautiously.
  • Adolescents (≥12 years): Dosing follows adult recommendations, but weight-based considerations may apply.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Dizziness, headache, and fatigue - usually mild and transient.
  • Central nervous system effects (e.g., vivid dreams, insomnia, mood changes) - reported in up to 30 % of users.
  • Rash - mild maculopapular eruptions are common; discontinue if severe or accompanied by fever.
  • Gastro-intestinal discomfort - nausea, abdominal pain, or loss of appetite.

Serious Adverse Events

  • Severe skin reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis) - require immediate medical attention.
  • Hepatotoxicity - elevated liver enzymes; monitor in patients with pre-existing liver disease.
  • Neuropsychiatric toxicity - new or worsening depression, suicidal ideation, or psychosis; discontinue if severe.
  • Birth defects - increased risk of neural tube defects when exposure occurs during the first trimester of pregnancy.

Drug Interactions

  • Major interactions

  • Ritonavir-boosted protease inhibitors - may increase efavirenz levels, risking toxicity.

  • CYP2B6 inducers (e.g., carbamazepine, phenobarbital) - can reduce efavirenz concentrations, potentially compromising viral suppression.

  • Moderate interactions

  • Azole antifungals (e.g., fluconazole) - may raise efavirenz levels modestly.

  • Warfarin - efavirenz may alter INR; more frequent monitoring is advised.

  • Mechanism - most interactions involve the cytochrome P450 enzyme system, particularly CYP2B6 and CYP3A4.

Food and Lifestyle Interactions

  • Food: Efavirenz can be taken with or without food, but a high-fat meal may slightly increase absorption and lead to higher peak concentrations, occasionally intensifying CNS effects.
  • Alcohol: No direct contraindication, but excessive intake may exacerbate dizziness or liver stress.
  • Driving: Because of possible dizziness or sleep disturbances, patients should assess their own response before operating machinery.

How to Take Sustiva

Standard Dosing (Based on Available Strengths)

  • Initial/maintenance dose: 600 mg once daily (one 600 mg pill) is the standard regimen for most adults.
  • Reduced dose option: 200 mg once daily may be used in patients who are known CYP2B6 “slow metabolizers” or who experience intolerable CNS side effects at 600 mg. Dose adjustments should be guided by therapeutic drug monitoring when available.

All dosing must be individualized by a qualified healthcare professional.

Special Population Adjustments

  • Mild to moderate hepatic impairment: Consider starting at 200 mg daily and titrating upward based on tolerance and viral load response.
  • Pregnancy (after first trimester): Continue the lowest effective dose that maintains viral suppression, with close obstetric review.
  • Elderly patients: Begin with 200 mg daily if CNS side effects are prominent, then assess need for escalation.

Administration Instructions

  • Swallow the pill whole with a glass of water.
  • If difficulty swallowing, the tablet may be broken and the halves taken separately, but do not crush the whole tablet.
  • Store at room temperature (15-30 °C), protected from moisture and light. Keep out of reach of children.

Missed Dose

  • If you remember within 12 hours of the scheduled time, take the missed dose.
  • If more than 12 hours have passed, skip the missed dose and resume the regular schedule. Do not double-dose.

Overdose

  • Symptoms may include severe CNS depression, seizures, or respiratory compromise.
  • Seek emergency medical assistance immediately. Activated charcoal may be considered if presentation is early. No specific antidote exists; treatment is supportive.

Discontinuation

  • Efavirenz does not require tapering, but abrupt cessation can lead to viral rebound.
  • Switching to another antiretroviral regimen should be done under specialist supervision to maintain continuous viral suppression.

Monitoring and Follow-Up

  • Baseline and periodic liver function tests (ALT, AST, bilirubin) - especially in patients with pre-existing liver disease.
  • HIV viral load - checked 4-8 weeks after initiation, then every 3-6 months.
  • CD4+ T-cell count - monitored alongside viral load to assess immune recovery.
  • Mental health assessment - screen for depression or suicidal thoughts at baseline and during follow-up.
  • Therapeutic drug monitoring (optional) - may be useful for patients with suspected CYP2B6 polymorphisms or drug interactions.

Storage and Handling

  • Keep the bottle tightly closed.
  • Store at 15-30 °C, away from direct sunlight and humidity.
  • Do not use after the expiry date printed on the label.
  • Dispose of unused tablets according to local pharmacy take-back programmes or NHS guidelines for hazardous waste.

Medication-Specific Glossary

Reverse Transcriptase Inhibitor (RTI)
A class of drugs that block the HIV enzyme reverse transcriptase, preventing viral replication.
CYP2B6
A liver enzyme that metabolises efavirenz; genetic variations can affect drug levels.
Neural Tube Defect
A serious birth defect of the brain and spine occurring early in fetal development, associated with first-trimester exposure to efavirenz.
Therapeutic Drug Monitoring (TDM)
Measurement of drug concentrations in the blood to guide dosage adjustments.

Medical Disclaimer

This article provides educational information about Sustiva and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Sustiva is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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