Efavirenz
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]
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.