Efavirenz

brand names Sustiva and Stocrin a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as a treatment for HIV type 1-is never used alone and is always given in combination with other drugs. In the 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.- Efavirenz acts allosterically by binding to a distinct site away from the active site known as the NNRTI pocket. 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. As with most HIV treatments, efavirenz is quite expensive. A one month supply of 600 mg tablets cost approximately $550 in April 2008 Efavirenz is chemically described as (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1benzoxazin-2-one. Its empirical formula is C14H9ClF3NO2. Efavirenz is a white to slightly pink crystalline powder with a molecular mass of 315.68 g/mol. It is practically insoluble in water (<10 g/mL). The usual adult dose of efavirenz is 600 mg per day (usually given at bedtime); or 800 mg daily when given concurrently with rifampicin as part of treatment of co-infection with tuberculosis. Efavirenz was approved by the FDA on September 21, 1998, making it the 14th approved antiretroviral drug. Efavirenz is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class. Drug Interactions Efavirenz is metabolized in the liver, and possesses both inhibitory and inducing effects on the 3A4 isoform of the cytochrome P450 system. This means efavirenz may interact with other drugs metabolized in the liver, requiring either increased or decreased dosages Lowers blood levels of most protease inhibitors. Dosages of amprenavir, atazanavir, or indinavir may need to be increased. The blood levels of saquinavir are dramatically lowered, so that the two drugs cannot be used simultaneously. St John's wort and garlic supplements may decrease efavirenz blood levels. Adverse effects Psychiatric symptoms, including insomnia, confusion, memory loss, and depression, are common, and more serious symptoms such as psychosis may occur in patients with compromised liver or kidney function. Rash, nausea, dizziness and headache may occur Efavirenz can cause birth defects and should not be used in women who might become pregnant Safety in children has not been established Use of efavirenz can produce a false positive result in some urine tests for marijuana Abuse of efavirenz by crushing and smoking the tablets for supposed hallucinogenic and dissociative effects has been reported in South Africa