Efavirenz
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]
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Overview
Efavirenz is {{{aOrAn}}} non-nucleoside reverse transcriptase inhibitor that is FDA approved for the treatment of HIV-1 in adults and children at least 3 months old and weighing at least 3.5 kg. Common adverse reactions include impaired concentration, abnormal dreams, rash, dizziness, nausea, headache, fatigue, insomnia and vomiting..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
HIV Infection
The recommended dosage of Efavirenz is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs). It is recommended that SUSTIVA be taken on an empty stomach, preferably at bedtime. The increased efavirenz concentrations observed following administration of SUSTIVA with food may lead to an increase in frequency of adverse reactions. Dosing at bedtime may improve the tolerability of nervous system symptoms. SUSTIVA capsules or tablets should be swallowed intact with liquid. For patients who cannot swallow capsules or tablets, the capsule sprinkle method of administration is recommended.
Concomitant Antiretroviral Therapy
- SUSTIVA must be given in combination with other antiretroviral medications
DosageAdjustment
- If SUSTIVA is coadministered with voriconazole, the voriconazole maintenance dose should be increased to 400 mg every 12 hours and the SUSTIVA dose should be decreased to 300 mg once daily using the capsule formulation (one 200 mg and two 50 mg capsules or six 50 mg capsules). SUSTIVA tablets should not be broken.
- If SUSTIVA is coadministered with rifampin to patients weighing 50 kg or more, an increase in the dose of SUSTIVA to 800 mg once daily is recommended
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Efavirenz in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Efavirenz in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
HIV Infection
It is recommended that SUSTIVA be taken on an empty stomach, preferably at bedtime. Table 1 describes the recommended dose of SUSTIVA for pediatric patients 3 months of age or older and weighing between 3.5 kg and 40 kg. The recommended dosage of SUSTIVA for pediatric patients weighing 40 kg or greater is 600 mg once daily. For pediatric patients who cannot swallow capsules, the capsule contents can be administered with a small amount of food or infant formula using the capsule sprinkle method of administration.
=Capsule Sprinkle Method of Administration=
For pediatric patients at least 3 months old and weighing at least 3.5 kg and adults who cannot swallow capsules or tablets, the capsule contents may be administered with a small amount (1 to 2 teaspoons) of food. Use of infant formula for mixing should only be considered for those young infants who cannot reliably consume solid foods. Patients and caregivers must be instructed to open the capsule carefully to avoid spillage or dispersion of the capsule contents into the air. The capsule should be held horizontally over a small container and carefully twisted to open. For patients able to tolerate solid foods, the entire capsule contents should be gently mixed with an age-appropriate soft food, such as applesauce, grape jelly, or yogurt, in the small container. For young infants receiving the capsule sprinkle-infant formula mixture, the entire capsule contents should be gently mixed into 2 teaspoons (10 mL) of reconstituted room temperature infant formula in a medicine cup by carefully stirring with a small spoon, and then drawing up the mixture into a 10 mL oral dosing syringe for administration. After administration of the SUSTIVA-food or -formula mixture, an additional small amount (approximately 2 teaspoons) of food or formula must be added to the empty mixing container, stirred to disperse any remaining SUSTIVA residue, and administered to the patient. The SUSTIVA-food or -formula mixture should be administered within 30 minutes of mixing. No additional food should be consumed for 2 hours after administration of SUSTIVA.
Further patient instructions on the capsule sprinkle method of administration are provided in the FDA-approved patient labeling (see Patient Information and Instructions for Use).
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Efavirenz in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Efavirenz in pediatric patients.
Contraindications
There is limited information regarding Efavirenz Contraindications in the drug label.
Warnings
There is limited information regarding Efavirenz Warnings' in the drug label.
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Efavirenz Clinical Trials Experience in the drug label.
Postmarketing Experience
There is limited information regarding Efavirenz Postmarketing Experience in the drug label.
Drug Interactions
There is limited information regarding Efavirenz Drug Interactions in the drug label.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Efavirenz in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Efavirenz in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Efavirenz during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Efavirenz in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Efavirenz in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Efavirenz in geriatric settings.
Gender
There is no FDA guidance on the use of Efavirenz with respect to specific gender populations.
Race
There is no FDA guidance on the use of Efavirenz with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Efavirenz in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Efavirenz in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Efavirenz in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Efavirenz in patients who are immunocompromised.
Administration and Monitoring
Administration
There is limited information regarding Efavirenz Administration in the drug label.
Monitoring
There is limited information regarding Efavirenz Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Efavirenz and IV administrations.
Overdosage
There is limited information regarding Efavirenz overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Efavirenz Pharmacology in the drug label.
Mechanism of Action
There is limited information regarding Efavirenz Mechanism of Action in the drug label.
Structure
There is limited information regarding Efavirenz Structure in the drug label.
Pharmacodynamics
There is limited information regarding Efavirenz Pharmacodynamics in the drug label.
Pharmacokinetics
There is limited information regarding Efavirenz Pharmacokinetics in the drug label.
Nonclinical Toxicology
There is limited information regarding Efavirenz Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Efavirenz Clinical Studies in the drug label.
How Supplied
There is limited information regarding Efavirenz How Supplied in the drug label.
Storage
There is limited information regarding Efavirenz Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Efavirenz Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Efavirenz interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Efavirenz Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Efavirenz Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [3]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [4]
Overview
Efavirenz (EFV, brand names Sustiva, Stocrin, Efavir etc.) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1.
For HIV infection that has not previously been treated, the United States Department of Health and Human Services Panel on Antiretroviral Guidelines currently recommends the use of efavirenz in combination with tenofovir/emtricitabine (Truvada) as one of the preferred NNRTI-based regimens in adults and adolescents.[1]
Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to reduce the risk of HIV infection in people exposed to a significant risk (e.g. needlestick injuries, certain types of unprotected sex etc.).
The usual adult dose is 600 mg once a day. It is usually taken on an empty stomach at bedtime to reduce neurological and psychiatric adverse effects.
Efavirenz was combined with the popular HIV medication Truvada, which consists of tenofovir and emtricitabine, all of which are reverse transcriptase inhibitors. This combination of three medications approved by the U.S. Food and Drug Administration (FDA) in July 2006 under the brand name Atripla, provides HAART in a single tablet taken once a day. It results in a simplified drug regimen for many patients.
Category
Antiretroviral
US Brand Names
SUSTIVA®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Historical Perspective
Efavirenz was approved by the FDA on September 21, 1998, making it the 14th approved antiretroviral drug.
Recreational use
Abuse of efavirenz by crushing and smoking the tablets for supposed hallucinogenic and dissociative effects has been reported in South Africa, where it is used in a mixture known as whoonga.[2][3][4] This is believed to be because of activity at a side target, the 5-HT2A receptor, which is better known as the target of drugs such as LSD.[5]
Pricing information
As with most HIV treatments, efavirenz is quite expensive. A one month supply of 600 mg tablets costed approximately $550 in April 2008.[6] Some emerging countries have opted to purchase Indian generics such as Efavir by Cipla Ltd for a fraction of the cost. In Thailand, one month supply of Efavirenz + Truvada, as of June 2012, costs THB 2900 ($90), there's also a social program for poorer patients who can't afford even this price.[7] In South Africa, a license has been granted to generics giant Aspen Pharmacare to manufacture, and distribute to Sub-Saharan Africa, a cost-effective antiretroviral drug.[8]
Mechanism of Action
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against HIV-1 by binding to reverse transcriptase. It consequently blocks the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication. It does not require intracellular phosphorylation for antiviral activity.
References
- ↑ "Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents". Retrieved 10 May 2013.
- ↑ IOL: Thugs get high on stolen Aids drugs
- ↑ Getting high on HIV drugs in S Africa. BBC News, 8 December 2008.
- ↑ 'No Turning Back': Teens Abuse HIV Drugs. ABC News, April 6, 2009.
- ↑ PMID 23702798 (PMID 23702798)
Citation will be completed automatically in a few minutes. Jump the queue or expand by hand - ↑ Price listed on http://drugstore.com website, 4/20/2008
- ↑ IndiaDaily - A new trend in emerging nations - Brazil opts for Indian generic drug ignoring US pharmaceutical giant Merck’s patent on AIDS drug Efavirenz
- ↑ Patrick Lumumba Osewe; Yvonne Korkoi Nkrumah; Emmanuel K. Sackey (15 June 2008). Improving Access to HIV/AIDS Medicines in Africa: Trade-Related Aspects of Intellectual Property Rights (TRIPS) Flexibilities Utilization. World Bank Publications. pp. 35–39. ISBN 978-0-8213-7544-0. Retrieved 30 June 2012.