Buy Efavirenz
Efavirenz

3.87
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of antiretroviral therapy (ART) to manage HIV-1 infection. It works by blocking the enzyme the virus needs to replicate, helping to decrease the viral load in the body and support the immune system's long-term health.


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
Sustiva
Manufacturer
Bristol-Myers Squibb
Product Form
Tablet, Capsule
Regulatory Classification
Rx
Primary Category
Antivirals
Product Category
Anti-infectives for systemic use, Antivirals for systemic use, Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Pharmacological Class
NNRTIs
Clinical Indications
Manufacturer Description
An antiretroviral medication used as part of HIV combination therapy to control the viral load and support the immune system.
Mechanism of Action
Efavirenz is a non-nucleoside reverse transcriptase inhibitor. It works by blocking a specific enzyme (reverse transcriptase) that the HIV virus needs to copy its genetic material, thereby stopping the virus from replicating in the body.
Route of Administration
Oral
Onset Time
Variable
Duration
24-52 hours
Contraindications
Severe liver impairment, Concurrent use of St John's Wort, History of certain heart rhythm conditions
Severe Adverse Events
Severe depression, Psychosis, Liver failure, Pancreatitis, Severe skin reactions
Common Side Effects
Nausea, Fatigue, Fat redistribution
Uncommon Side Effects
Dizziness, Insomnia, Skin rash, Concentration problems, Abnormal dreams
Drug Interactions
Statins, Midazolam, Oral contraceptives, St John's Wort
Pregnancy Safety Warnings
Avoid during the first trimester; breastfeeding not recommended for HIV+ mothers.
Age Restrictions
Adults and children over 3 years.
Storage Guidelines
Keep at room temperature.
Related Products
Nevirapine, Etravirine, Rilpivirine

Efavirenz FAQ

How should I take efavirenz if I have trouble sleeping at night?

Efavirenz is commonly taken in the evening because CNS side effects, such as vivid dreams, often diminish when the drug is taken before sleep. If insomnia persists, discuss timing adjustments or alternative regimens with your prescriber.

Can efavirenz affect my results on a drug test for employment?

Efavirenz is not a controlled substance and is not screened for in standard workplace drug tests. However, some occupational health programs may request a medication list; disclose efavirenz to avoid misunderstandings.

What does the imprint on an efavirenz tablet look like?

In the UK, 600 mg efavirenz tablets typically carry the imprint “EFA 600” while 200 mg tablets may be imprinted “EFA 200”. Imprints help verify authenticity when pharmacy staff check the medication.

Is efavirenz safe for travelers visiting countries with limited medical facilities?

Efavirenz has a long half-life, allowing once-daily dosing, which is convenient for travel. Carry a sufficient supply, keep tablets in original packaging, and have a copy of your prescription in case you need to refill abroad.

How does efavirenz compare with other NNRTIs like nevirapine?

Both drugs inhibit reverse transcriptase, but efavirenz generally has a higher genetic barrier to resistance and is once-daily, whereas nevirapine is dosed twice daily and has a higher risk of hepatotoxicity in certain populations. Choice depends on individual clinical factors.

Will efavirenz interact with hormonal contraceptives?

Efavirenz can reduce plasma concentrations of some hormonal contraceptives (e.g., levonorgestrel) by inducing CYP enzymes, potentially decreasing contraceptive effectiveness. Using a non-hormonal method or a higher-dose contraceptive may be advised.

What should I know about efavirenz storage while traveling abroad?

Keep the medication in a cool, dry place away from direct sunlight. If you expect extreme temperatures, store the tablets in a sealed bag with a desiccant packet and avoid leaving them in a car.

Are there any cost-saving options for efavirenz in the UK?

Efavirenz is available as a generic medication, which can be prescribed through the NHS at a lower cost than brand-name products. Discuss generic options with your prescriber to optimise affordability.

Can efavirenz be taken with antacids or mineral supplements?

Antacids containing aluminium or magnesium do not significantly affect efavirenz absorption. However, high-dose calcium or iron supplements may modestly reduce plasma levels; spacing them several hours apart is prudent.

What is the patent status of efavirenz in the UK?

Efavirenz’s original patents have expired, allowing multiple manufacturers to produce generic versions. This facilitates broader access and competitive pricing.

Efavirenz: Generic Medication Overview

Efavirenz is an antiretroviral medication classified as a non-nucleoside reverse transcriptase inhibitor (NNRTI). It is prescribed for the management of HIV-1 infection and is available in oral pill form in strengths of 200 mg and 600 mg. In the United Kingdom the drug is prescription-only (POM) and regulated by the Medicines and Healthcare products Regulatory Agency (MHRA).

How Efavirenz Works in the Body

Efavirenz binds directly to the reverse transcriptase enzyme of HIV-1, blocking the enzyme’s ability to copy viral RNA into DNA. This inhibition stops the virus from replicating inside host cells. The drug is well absorbed after oral administration, reaches peak plasma concentrations in about 3-5 hours, and has a long half-life of 40-55 hours, allowing once-daily dosing. Efavirenz is metabolised mainly by the liver enzyme CYP2B6 and, to a lesser extent, by CYP3A4.

Conditions Treated by Efavirenz

  • HIV-1 infection in adults and adolescents (≥ 12 years) as part of combination antiretroviral therapy (cART).
  • The medication is not approved for HIV-2 infection.

Efavirenz is typically combined with two nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) such as tenofovir disoproxil fumarate and emtricitabine, forming a complete treatment regimen.

Off-Label and Investigational Applications

Evidence-Based Off-Label Uses

  • Prevention of mother-to-child transmission (PMTCT): Some guidelines describe efavirenz-containing regimens for pregnant women living with HIV when other options are unsuitable. This use is not formally licensed for pregnancy in the UK; careful risk-benefit assessment is required.

Off-label use requires medical supervision and individualized risk assessment.

Evaluating Efavirenz for Your Health Profile

  • Ideal candidates are adults or adolescents with confirmed HIV-1 infection who can adhere to a once-daily regimen.
  • Absolute contraindications
  • Known hypersensitivity to efavirenz or any tablet excipients.
  • Severe hepatic impairment (Child-Pugh class C).
  • Relative contraindications
  • Moderate hepatic dysfunction (Child-Pugh class A or B).
  • Pregnancy (especially first trimester) due to potential teratogenicity; alternative regimens are preferred when possible.
  • Pre-existing psychiatric illness (e.g., depression, psychosis) because efavirenz may exacerbate symptoms.

Special populations such as the elderly or patients with renal impairment usually do not require dose changes, but clinicians may monitor drug levels in patients with known CYP2B6 polymorphisms.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Dizziness or light-headedness (frequently reported).
  • Insomnia, vivid dreams, or other central nervous system (CNS) disturbances.
  • Rash, often mild and transient.
  • Nausea or mild gastrointestinal upset.

Serious Adverse Events

  • Severe skin reactions, including Stevens-Johnson syndrome or toxic epidermal necrolysis.
  • Hepatotoxicity presenting as jaundice, elevated transaminases, or hepatitis.
  • Neuropsychiatric events such as severe depression, suicidal ideation, or psychosis.
  • Black-box warning: Efavirenz may increase the risk of suicidal thoughts and behaviors. Prompt medical attention is essential if such symptoms arise.

Drug Interactions

  • Major interactions

  • Ritonavir, cobicistat, or other strong CYP3A4 inhibitors increase efavirenz concentrations; dose reduction may be necessary.

  • Carbamazepine, phenobarbital, rifampicin, or St. John’s wort (CYP2B6 inducers) lower efavirenz levels, potentially reducing efficacy.

  • Moderate interactions

  • Protease inhibitors (e.g., atazanavir, lopinavir/ritonavir) can raise efavirenz levels; monitoring for CNS toxicity is advised.

  • Warfarin: Efavirenz may reduce warfarin anticoagulant effect; INR should be checked regularly.

Food and Lifestyle Interactions

  • Efavirenz can be taken with or without food; taking the dose at night may lessen CNS side effects.
  • Moderate alcohol consumption does not significantly alter efavirenz pharmacokinetics, but excessive use can worsen liver toxicity.
  • Patients should avoid operating heavy machinery until they know how efavirenz affects their alertness.

How to Take Efavirenz

  • Standard dosing: One tablet of 600 mg taken once daily, preferably in the evening.
  • Alternative strength: A 200 mg tablet may be prescribed for dose adjustments in patients with known CYP2B6 polymorphisms or for pediatric formulations.
  • Administration: Swallow the tablet whole with a glass of water; no crushing or chewing is required.
  • Missed dose: Take the missed dose as soon as remembered if it is still the same day; otherwise skip and resume the regular schedule. Do not double the dose.
  • Overdose: Symptoms may include severe CNS depression, seizures, or cardiac arrhythmia. Seek emergency medical care; supportive care is the mainstay of treatment.
  • Discontinuation: Efavirenz should not be stopped abruptly without medical advice, as abrupt cessation can lead to viral rebound. Switching to an alternative regimen should be guided by a clinician.

Monitoring and Follow-Up

  • Laboratory tests: Baseline and periodic liver function tests; HIV viral load and CD4+ count every 3-6 months.
  • Mental health: Screen for depression, suicidal thoughts, and other psychiatric symptoms at treatment initiation and during follow-up.
  • Drug levels: Therapeutic drug monitoring may be considered for patients with known CYP2B6 variants or those experiencing toxicity.

Storage and Handling

  • Store tablets at room temperature (below 30 °C) in a dry place, protected from light.
  • Keep out of reach of children and pets.
  • Do not use tablets after the expiry date printed on the packaging.

Medication-Specific Glossary

Non-nucleoside reverse transcriptase inhibitor (NNRTI)
A class of antiretroviral drugs that bind directly to HIV-1 reverse transcriptase at a site distinct from the nucleoside binding pocket, blocking viral DNA synthesis.
CYP2B6
A liver enzyme that metabolises efavirenz; genetic variations can affect drug concentrations and may require dose adjustments.
Stevens-Johnson syndrome
A rare, severe skin reaction characterised by epidermal detachment and mucosal involvement; it requires immediate medical attention.

Medical Disclaimer

This article provides educational information about efavirenz 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 Efavirenz 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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