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Efavirenz (brand names Sustiva and Stocrin) 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 lamivudine/zidovudine (Combivir) or tenofovir/emtricitabine (Truvada) as the preferred NNRTI-based regimens in adults
and adolescents.
Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those
exposed to materials associated with a high risk for HIV transmission.
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 FDA in July 2006 under the brand name Atripla, provides highly active antiretroviral therapy (HAART) in a single tablet
taken once a day. It results in a simplified drug regimen for many patients.
History
Efavirenz was approved by the Food and Drug Administration (FDA) on September 21, 1998, making it the 14th approved antiretroviral drug.
Indications
Efavirenz is used to treat HIV infection. It is never used alone and is always given in combination with other drugs. The decision on when to start treatment should take
into account CD4 count, HIV viral load, treatment history, resistance profiles and patient preference.
Since the preliminary publication of the results of the ACTG 5142 trial in 2006 which compared efavirenz against lopinavir, efavirenz has been used as first line treatment
in preference to the protease inhibitors. The ACTG 5095 trial showed that the potency of efavirenz is maintained at all CD4 counts and HIV viral loads.
Mode of action
Efavirenz falls in the non-nucleoside reverse transcriptase inhibitor (NNRTI) class of antiretrovirals. Both nucleoside and non-nucleoside RTIs inhibit the same target, the
reverse transcriptase enzyme, an essential viral enzyme which transcribes viral RNA into DNA. Unlike nucleoside RTIs, which bind at the enzyme's active site, NNRTIs
bind within a pocket termed the NNRTI pocket.
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