![]() The Department of Health and Human Services, December 2009 guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents indicate non-nucleoside reverse transcriptase inhibitors (NNRTI) for current best practices. The US Center for Disease Control reports the number of people living with HIV continues to increase due, in large part, to highly efficacious antiretroviral medicines. Worldwide almost 1 in 200 people are living with HIV/AIDs and every 12 s someone else becomes infected. This finding correlates, in part, with the subjective experiences in humans who abuse efavirenz and with specific dose-dependent adverse neuropsychiatric events, such as hallucinations and night terrors, reported by HIV patients taking it as a medication. Although its molecular pharmacology is multifarious, efavirenz's prevailing behavioral effect in rodents is consistent with LSD-like activity mediated via the 5-HT 2A receptor. Despite having GABA A-potentiating effects (like benzodiazepines and barbiturates), and interactions with dopamine transporter, serotonin transporter, and vesicular monoamine transporter 2 (like cocaine and methamphetamine), efavirenz fails to maintain responding in rats that self-administer cocaine, and it fails to produce a conditioned place preference. Similar to LSD, efavirenz induces head-twitch responses in wild-type, but not in 5-HT 2A-knockout, mice. Efavirenz occasions drug-lever responding in rats discriminating LSD from saline, and this effect is abolished by selective blockade of the 5-HT 2A receptor. Both LSD and efavirenz reduce ambulation in a novel open-field environment. ![]() In rodents, interaction with the 5-HT 2A receptor, a primary site of action of lysergic acid diethylamine (LSD), appears to dominate efavirenz's behavioral profile. ![]() Molecular profiling of the receptor pharmacology of efavirenz pinpointed interactions with multiple established sites of action for other known drugs of abuse including catecholamine and indolamine transporters, and GABA A and 5-HT 2A receptors. Anecdotal reports have surfaced concerning misuse of the HIV antiretroviral medication efavirenz ((4 S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1 H-3,1-benzoxazin-2-one) by HIV patients and non-infected teens who crush the pills and smoke the powder for its psychoactive effects. ![]()
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