HIV Antiretroviral Drug Has Psychoactive Effects
April 22, 2013

New Study Examines Psychoactivity, Recreational Use Of Popular HIV Drug

redOrbit Staff & Wire Reports - Your Universe Online

The psychoactivity of an antiretroviral (ARV) drug commonly used to treat HIV has been linked to its recreational use, according to research presented during the Experimental Biology 2013 conference in Boston, Massachusetts on Sunday.

The medication efavirenz (which is also known under the brand names Sustiva and Stocrin) has become popular as a treatment for the virus that causes AIDS due to its ability to suppress replication of the HIV virus.

Despite its effectiveness, efavirenz has been linked to neuropsychiatric side effects including depression, anxiety, sleep disturbances, impaired concentration, aggressive behavior, hallucinations, night terrors, paranoia, psychosis and delusions. The reasons why those side effects occur remain unclear, the researchers said, though recent anecdotal reports of recreational use of the drugs have provided some new light on the matter.

Dr. John A. Schetz, an associate professor of pharmacology and neuroscience at the University of North Texas Health Science Center in Fort Worth, has used his past experience discovering and developing new drugs for the treatment of neurological and psychiatric disorders to figure out why efavirenz can lead to psychiatric events.

Furthermore, his work could explain why the antiretroviral has been used by some as a recreational substance, which might lead to the mutation of the HIV virus into ARV-resistant strains, the researchers explained.

The Texas-based neuropharmacologist reportedly first became interested in the topic after seeing news reports of ARV abuse in South Africa. Those stories detailed how pills intended to treat HIV were being crushed into powder, and then smoked for their psychoactive side effects.

Despite the lack of scientific studies covering the issue, Dr. Schetz was familiar with HIV patients who had experienced neuropsychiatric side effects while taking the drug as prescribed, as well as reports of individuals experiencing psychiatric events without a history of mental illness.

Research had suggested that the later patient population had a genetic predisposition because they had less effective variants of the enzyme which is primarily responsible for metabolizing efavirenz. That would lead to far slower breakdown of the ARV drug, and consequently higher-than-expected levels of the substance in the patients´ bodies. Dr. Schetz began his research with molecular profiling of the receptor pharmacology of efavirenz, leading to the identifications of interactions with established sites of action for other drugs of abuse.

He and his colleagues were able to achieve a pre-clinical understanding of the psychoactivity induced by the substance. Their work, which is said to be the first study to ever analyze the mechanisms of efavirenz's psychopharmacology, could help explain both reports of the drug´s adverse neuropsychiatric side effects in HIV patients and of its diversion for recreational use. Dr. Schetz hopes that their findings will help generate interest in further research into the mechanisms of ARV side effects and abuse potential.