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Efavirenz

3.87
An antiretroviral medication used as part of HIV combination therapy to control the viral load and support the immune system.


Ingredient
Availability
In Stock
Delivery
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

Alternative/Local Brand
Sustiva
Active Ingredient(s)
Efavirenz
Primary Category
Antivirals
Therapeutic Class
Anti-infectives for systemic use, Antivirals for systemic use, Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Pharmacological Class
NNRTIs
Indications
HIV-1 infection
Contraindications
Severe liver impairment, Concurrent use of St John's Wort, History of certain heart rhythm conditions
Minor Side Effects
Nausea, Fatigue, Fat redistribution
Moderate Side Effects
Dizziness, Insomnia, Skin rash, Concentration problems, Abnormal dreams
Serious Side Effects
Severe depression, Psychosis, Liver failure, Pancreatitis, Severe skin reactions
Dosage Forms
Tablet, Capsule
Administration Route
Oral
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.
Prescription Status
Rx
Manufacturer
Bristol-Myers Squibb
Patient Summary
An antiretroviral medication used as part of HIV combination therapy to control the viral load and support the immune system.
Onset Time
Variable
Duration
24-52 hours
Storage Instructions
Keep at room temperature.
Drug Interactions
Statins, Midazolam, Oral contraceptives, St John's Wort
Age Restrictions
Adults and children over 3 years.
Pregnancy Use
Avoid during the first trimester; breastfeeding not recommended for HIV+ mothers.
Alternative Drugs
Nevirapine, Etravirine, Rilpivirine

Efavirenz: Generic Medication Overview

Efavirenz is an antiretroviral medication classified as a non-nucleoside reverse transcriptase inhibitor (NNRTI). It is used to treat infection with human immunodeficiency virus (HIV). The drug is available in pill form at strengths of 200 mg and 600 mg. In Hong Kong, efavirenz is a prescription-only medication and is regulated by the Department of Health in line with international standards such as those set by the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA).

Pharmacology: Efavirenz's Therapeutic Action

Efavirenz works by binding directly to the HIV-1 reverse transcriptase enzyme. This binding blocks the enzyme’s ability to convert viral RNA into DNA, a critical step in the HIV replication cycle. By stopping this conversion, efavirenz reduces the amount of virus that can infect new cells, helping to lower viral load and preserve immune function.

Key pharmacologic characteristics include:

  • Onset of action: Antiviral effects are observed within days of initiating therapy.
  • Peak plasma concentration: Typically reached 3-5 hours after oral intake.
  • Half-life: Approximately 40-55 hours, allowing once-daily dosing.
  • Metabolism: Primarily metabolised by the liver enzyme CYP2B6, with contributions from CYP3A4. This metabolism contributes to drug-drug interaction potential.

Conditions Treated by Efavirenz

Efavirenz is approved for use in combination with other antiretroviral agents to treat HIV-1 infection in adults and adolescents. In Hong Kong, the approved indications align with those of the FDA and EMA:

  • Initial therapy for HIV-1-infected individuals who have no prior exposure to antiretroviral drugs.
  • Switch therapy when a patient requires a regimen change due to toxicity, resistance, or simplification, provided the new regimen includes appropriate companion drugs.

Efavirenz is not indicated for prevention of HIV infection (pre-exposure prophylaxis) or for use in patients with documented hypersensitivity to the drug.

Evaluating Efavirenz for Your Health Profile

Who Should Use Efavirenz?

  • Adults and adolescents (≥ 12 years) with confirmed HIV-1 infection who require a NNRTI-based regimen.
  • Patients with adequate hepatic function, as efavirenz is processed by the liver.

Absolute Contraindications

  • Known hypersensitivity to efavirenz or any of its excipients.
  • Severe hepatic impairment (Child-Pugh C).

Relative Contraindications

  • Moderate hepatic impairment (Child-Pugh B) - dose adjustment or alternative therapy may be needed.
  • Pregnancy (Category D): Efavirenz is associated with potential fetal neural tube defects, especially when exposure occurs during the first trimester.
  • Concomitant use of potent CYP2B6 or CYP3A4 inducers (e.g., rifampicin, carbamazepine) may reduce efavirenz levels.

Special Populations

  • Pregnancy/Lactation: Efavirenz is generally avoided during the first trimester. If used later in pregnancy, benefits and risks should be discussed with a specialist. Efavirenz is excreted in breast milk; breastfeeding while on efavirenz is not recommended.
  • Elderly: No specific dosage reduction is required solely based on age, but clinicians should monitor for central nervous system (CNS) side effects, which may be more pronounced.
  • Renal Impairment: No dose adjustment is required for patients with reduced renal function, as renal clearance is minimal.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Central nervous system effects: dizziness, insomnia, vivid dreams, and mood changes (reported in > 10 % of patients).
  • Gastrointestinal symptoms: nausea, vomiting, and abdominal pain.
  • Skin reactions: mild rash or pruritus.

Serious Adverse Events

  • Severe rash or Stevens-Johnson syndrome: requires immediate medical attention.
  • Hepatotoxicity: elevations in liver enzymes; monitor regularly.
  • Neuropsychiatric toxicity: depression, suicidal ideation, or psychosis - rare but serious.

Drug Interactions

Efavirenz induces several CYP enzymes, notably CYP3A4, CYP2B6, and CYP2C9, which can lower plasma concentrations of co-administered drugs.

  • Major interactions:

  • Decreases concentrations of protease inhibitors (e.g., atazanavir, lopinavir/ritonavir).

  • Reduces effectiveness of hormonal contraceptives - alternative non-hormonal methods should be considered.

  • Moderate interactions:

  • May lower levels of certain antiepileptics (e.g., phenytoin) and anticoagulants (warfarin).

  • May increase concentrations of drugs metabolised by CYP2C19 (e.g., clopidogrel).

Patients should provide a complete medication list, including over-the-counter products and herbal supplements, before starting efavirenz.

Food and Lifestyle Interactions

  • Efavirenz can be taken with or without food, but a high-fat meal may delay absorption and slightly increase peak concentration.
  • Alcohol may exacerbate CNS side effects; patients are advised to limit intake.
  • Efavirenz does not impair driving ability for most patients, but those experiencing dizziness or severe insomnia should avoid operating heavy machinery.

How to Take Efavirenz

  • Standard adult dosing: 600 mg (one 600 mg pill) taken once daily, preferably at bedtime to reduce CNS side effects.
  • Pediatric or dose-adjusted regimen: 200 mg (one 200 mg pill) may be used in adolescents weighing less than 50 kg, under specialist guidance.

Administration Instructions

  • Swallow the pill whole with a full glass of water.
  • Do not split, chew, or crush the tablet, as this may affect absorption.
  • Store at room temperature, away from moisture and direct sunlight.

Missed Dose

If a dose is missed, take it as soon as remembered unless it is close to the time of the next scheduled dose. Do not double the dose.

Overdose

Symptoms may include severe CNS depression, seizures, or respiratory compromise. Seek emergency medical care immediately; supportive measures and monitoring are the primary treatment.

Discontinuation

Efavirenz does not require tapering. However, abrupt cessation can lead to viral rebound and resistance. Any change in therapy should be supervised by a qualified healthcare professional.

Monitoring and Follow-Up

  • Baseline labs: HIV viral load, CD4 count, liver function tests (ALT, AST, bilirubin).
  • Follow-up labs: Liver enzymes every 3-6 months, or sooner if symptoms develop.
  • Clinical assessments: Viral load measurement at 4-8 weeks after initiation, then every 3-6 months to ensure suppression.
  • Neuropsychiatric monitoring: Routine screening for mood changes, especially during the first weeks of therapy.

Storage and Handling

  • Keep the pills in their original packaging until use.
  • Store at 15-30 °C (59-86 °F) in a dry place.
  • Do not use the medication past its expiration date.
  • Dispose of unused tablets according to local pharmacy or hazardous waste guidelines to keep them out of reach of children.

Medication-Specific Glossary

Reverse Transcriptase Inhibitor
A class of antiretroviral drugs that block the activity of reverse transcriptase, an enzyme HIV uses to replicate its genetic material.
CYP2B6 Induction
The process by which a substance increases the activity of the liver enzyme CYP2B6, leading to faster metabolism of drugs that are CYP2B6 substrates.
Neuropsychiatric Toxicity
Adverse effects affecting mood, cognition, or perception, such as insomnia, vivid dreams, depression, or anxiety.

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.

Efavirenz FAQ

Can efavirenz be taken with other antiretroviral drugs?

Efavirenz is intended to be part of a combination regimen that typically includes two nucleoside reverse transcriptase inhibitors (NRTIs). This combination maximises viral suppression and reduces the chance of resistance. Always follow the prescriber's specific regimen plan.

Why is efavirenz usually taken at bedtime?

Taking efavirenz at night can lessen the impact of its common central nervous system side effects, such as vivid dreams and insomnia, because sleep may mask these symptoms.

Does efavirenz affect hormone-based contraception?

Yes. Efavirenz induces enzymes that lower the effectiveness of hormonal contraceptives (pills, patches, rings). Women using efavirenz should discuss alternative or additional non-hormonal birth control methods with their provider.

What should I do if I experience severe rash while on efavirenz?

A severe or spreading rash may indicate a serious allergic reaction (e.g., Stevens-Johnson syndrome). Seek immediate medical attention, as discontinuation of the drug may be required.

Is efavirenz safe for patients with mild liver disease?

Patients with mild to moderate hepatic impairment can often use efavirenz, but clinicians usually monitor liver enzymes closely and may adjust the regimen if abnormalities develop.

Can I travel internationally while on efavirenz?

Yes, but keep medication in its original labelled container, carry a copy of your prescription, and be aware of any country-specific import restrictions for antiretroviral drugs. Always have a supply that covers the entire trip plus extra days.

Does efavirenz interact with common over-the-counter pain relievers?

Acetaminophen generally does not interact with efavirenz. Non-steroidal anti-inflammatory drugs (NSAIDs) are also safe, but patients with liver disease should use caution with high-dose acetaminophen.

Why do some patients report vivid dreams while taking efavirenz?

Efavirenz penetrates the central nervous system and can alter neurotransmitter activity, leading to changes in sleep architecture and vivid dreaming. These effects usually lessen after several weeks of therapy.

Is there a generic version of efavirenz available in Hong Kong?

Yes. Several manufacturers produce generic efavirenz tablets that meet the same quality standards as the branded product. Availability may vary by pharmacy.

How does efavirenz compare with newer NNRTIs like doravirine?

Both belong to the NNRTI class, but newer agents may have fewer central nervous system side effects and a different resistance profile. Choice of therapy depends on individual patient factors, resistance testing, and physician judgment.

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