Recreational Use of HIV Antiretroviral Drug Linked to its Psychoactivity

EMBARGOED UNTIL12:30 PMET April21, 2013ONSITENEWSROOMBoston Convention CenterApril 20-24, 2013Phone: 617-954-3976Media@ @faseb.orgPRIMARY CONTACTJim Bernsteinjbernstein@aspet.orgCell/text: 301-646-3259Recreational Use of HIV Antiretroviral Drugg Linked ToIts PsychoactivityBOSTON— More than 1 in 270people in the US are living with HIV and every9.5 minutessomeone is else is infected. The economic cost estimatess associated with HIV/AIDS exceed 36billion dollars a year. The development of effective drugg treatments have allowed people withHIV to live longer with federal health officials now predicting that by 2015 one-half of thepopulation with HIVin the US will be older than 50.Efavirenz(tradenames: Sustiva® ®, Stocrin®) is an antiretroviral (ARV) drug commonly usedtotreat HIV. Its popularity as a medication, alone or more commonly incombination with otherHIV medications (tradename: Atripla®), is due to its superior effectiveness in suppressingreplication of the virus that causes AIDS. Though highlyy effective, a standard dose of efavirenzis knownn to carry a risk of side effects that include adverse neuropsychiatric complications suchas depression, anxiety, sleep disturbances, impaired concentration, aggressive behavior, nightterrors, hallucinationns, paranoia, psychosis and delusions. However the question remains as towhy these side effects occur. Recent anecdotal reports off the recreational use of efavirenzprovidedd some clues.Dr. John A. Schetz atthe University of NorthTexas Health Science Center in Fort Worth, Texas,utilizes a mechanisticc approach to solving problems and answering questions of importance tosociety. As a neuropharmacologist working to discover and developnew drugs for the treatmentof neurological and psychiatric disorders, hisexperience and intuition helped solve the mysteryas to whyefavirenz, when taken as prescribed, can causee adverse psychiatric events, as well aswhy there are reportsof efavirenz being diverted for recreational use. The later practice couldencourage the emergence of ARV-resistant HIV strains by educatingthe HIV virus.Dr. Schetz’s interest was sparkedby a network news report coveringthe topic ofARV abuseinSouth Africa. The report described how pills used to treat HIV weree being crushed and thepowder smoked for its psychoactive effects. Though there were no scientific studies on thetopic, Dr. Schetz wasaware of studies describing neuropsychiatric side effects inHIV patientstaking the medicationas prescribed, as well as case reports of suddenonset adverse psychiatric

events in patients with no history of mental illness. However, research study results suggestedthat the later patient population were genetically predisposed because they have less effectivevariants of the enzyme primarily responsible for metabolizing efavirenz, leading to much slowerthan expected breakdown of efavirenz, and consequently higher than expected levels of drug inthe body. Dr. Schetz initiated his investigation with molecular profiling of the receptorpharmacology of efavirenz which lead to the pinpointing of interactions with multipleestablished sites of action for other known drugs of abuse. He and a number of his colleaguesworked together to achieve a pre-clinical understanding of the psychoactivity induced byefavirenz that may help explain reports both of its adverse neuropsychiatric side effects in HIVpatients and of its diversion for recreational use.Dr. Schetz’s work is the first ever study of the mechanisms of efavirenz’s psychopharmacologyand these new findings will help stimulate interest to support additional research related to themechanism of ARV side effects and abuse potential. This would help translate the pre-clinicalfindings into preventative measures addressing HIV medication-induced adverse side effects inpatients living with HIV. Additionally, preventative strategies would improve patient adherenceand quality of life, reduce the potential risk for the emergence of HIV drug resistant strains, andcould prevent diversion of HIV medication for illicit use.”His findings will be presented April 21, 2012 during Experimental Biology 2013 in Boston, MA.To request an interview with Dr. Schetz, please contact Jim Bernstein at the contact informationlisted above.###About Experimental Biology 2013Experimental Biology’s mission is to share the newest scientific concepts and research findingsshaping future and current clinical advances – and to give scientists and clinicians anunparalleled opportunity to hear from colleagues working on similar biomedical problems usingdifferent disciplines. With six sponsoring societies and another 20 U.S. and international guestsocieties, the annual meeting brings together scientists from throughout the United States and theworld, representing dozens of scientific areas, from laboratory to translational to clinicalresearch. The meeting also offers a wide spectrum of professional development sessions.About the American Society for Pharmacology and Experimental TherapeuticsASPET is a 5,100 member scientific society whose members conduct basic and clinicalpharmacological research within the academic, industrial and government sectors. Our membersdiscover and develop new medicines and therapeutic agents that fight existing and emergingdiseases, as well as increase our knowledge regarding how therapeutics affects humans.