Navigation Links
Recreational use of HIV antiretroviral drug linked to its psychoactivity
Date:4/21/2013

BOSTON More than 1 in 270 people in the US are living with HIV and every 9.5 minutes someone is else is infected. The economic cost estimates associated with HIV/AIDS exceed 36 billion dollars a year. The development of effective drug treatments have allowed people with HIV to live longer with federal health officials now predicting that by 2015 one-half of the population with HIV in the US will be older than 50.

Efavirenz (tradenames: Sustiva, Stocrin) is an antiretroviral (ARV) drug commonly used to treat HIV. Its popularity as a medication, alone or more commonly in combination with other HIV medications (tradename: Atripla), is due to its superior effectiveness in suppressing replication of the virus that causes AIDS. Though highly effective, a standard dose of efavirenz is known to carry a risk of side effects that include adverse neuropsychiatric complications such as depression, anxiety, sleep disturbances, impaired concentration, aggressive behavior, night terrors, hallucinations, paranoia, psychosis and delusions. However the question remains as to why these side effects occur. Recent anecdotal reports of the recreational use of efavirenz provided some clues.

Dr. John A. Schetz at the University of North Texas Health Science Center in Fort Worth, Texas, utilizes a mechanistic approach to solving problems and answering questions of importance to society. As a neuropharmacologist working to discover and develop new drugs for the treatment of neurological and psychiatric disorders, his experience and intuition helped solve the mystery as to why efavirenz, when taken as prescribed, can cause adverse psychiatric events, as well as why there are reports of efavirenz being diverted for recreational use. The later practice could encourage the emergence of ARV-resistant HIV strains by educating the HIV virus.

Dr. Schetz's interest was sparked by a network news report covering the topic of ARV abuse in South Africa. The report described how pills used to treat HIV were being crushed and the powder smoked for its psychoactive effects. Though there were no scientific studies on the topic, Dr. Schetz was aware of studies describing neuropsychiatric side effects in HIV patients taking the medication as prescribed, as well as case reports of sudden onset adverse psychiatric events in patients with no history of mental illness. However, research study results suggested that the later patient population were genetically predisposed because they have less effective variants of the enzyme primarily responsible for metabolizing efavirenz, leading to much slower than expected breakdown of efavirenz, and consequently higher than expected levels of drug in the body. Dr. Schetz initiated his investigation with molecular profiling of the receptor pharmacology of efavirenz which lead to the pinpointing of interactions with multiple established sites of action for other known drugs of abuse. He and a number of his colleagues worked together to achieve a pre-clinical understanding of the psychoactivity induced by efavirenz that may help explain reports both of its adverse neuropsychiatric side effects in HIV patients and of its diversion for recreational use.

Dr. Schetz's work is the first ever study of the mechanisms of efavirenz's psychopharmacology and these new findings will help stimulate interest to support additional research related to the mechanism of ARV side effects and abuse potential. This would help translate the pre-clinical findings into preventative measures addressing HIV medication-induced adverse side effects in patients living with HIV. Additionally, preventative strategies would improve patient adherence and quality of life, reduce the potential risk for the emergence of HIV drug resistant strains, and could prevent diversion of HIV medication for illicit use."

His findings will be presented April 21, 2012 during Experimental Biology 2013 in Boston, MA.


'/>"/>

Contact: Jim Bernstein
jbernstein@aspet.org
301-646-3259
Federation of American Societies for Experimental Biology
Source:Eurekalert

Related biology news :

1. Early antiretroviral treatment reduces viral reservoirs in HIV-infected teens
2. Scientists find ethnicity linked to antibodies
3. A proteins well-known cousin sheds light on its gout-linked relative
4. Microorganisms detected via breath test linked to body mass, fat accumulation
5. Genetic alterations linked with bladder cancer risk, recurrence, progression, and patient survival
6. Global nitrogen availability consistent for past 500 years, linked to carbon levels
7. Reward linked to image is enough to activate brains visual cortex
8. Kids consumption of sugared beverages linked to higher caloric intake of food
9. Prenatal exposure to pesticide DDT linked to adult high blood pressure
10. 2 new genes linked to amyotrophic lateral sclerosis and related disorders
11. MBL scientists find genes linked to human neurological disorders in sea lamprey genome
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:3/2/2017)... , March 2, 2017 Summary ... better understand Merck KGaA and its partnering interests and ... https://www.reportbuyer.com/product/3605601/ Description The Partnering Deals and Alliance ... partnering activity of one of the world,s leading life ... prepared upon purchase to ensure inclusion of the most ...
(Date:3/2/2017)... , March 2, 2017 Australian stem ... (ASX: CYP), has signed an agreement with the ... the Monash Biomedicine Discovery Institute and Department of Pharmacology ... conduct a further preclinical study to support the use ... of asthma.  Asthma is a chronic, ...
(Date:2/28/2017)... --  Acuant , a leading provider of data capture ... new and core technologies building upon the acquisition of ... desktop Acuant FRM TM facial recognition and match ... manual review of identity documents by accredited professionals. ... most accurate capture software to streamline workflows by securely ...
Breaking Biology News(10 mins):
(Date:3/28/2017)... Durham, NC (PRWEB) , ... March 28, 2017 ... ... unwanted side effects and diminished effectiveness over time. A recent study published in ... treat PD by stimulating subventricular zone (SVZ) stem cells to produce more neural ...
(Date:3/28/2017)... VANCOUVER , March 28, 2017 /PRNewswire/ -RepliCel Life Sciences ... is pleased to report compelling safety and clinical data from ... RepliCel,s type 1 collagen-expressing, hair follicle-derived fibroblasts (RCT-01) as a ... ... of establishing a complete safety profile at 6 months and ...
(Date:3/27/2017)... March 27, 2017 Roka Bioscience, Inc. (NASDAQ: ROKA), ... for the detection of foodborne pathogens,  today announced that ... Company Spring 2017 Convention on March 29 at 9:50am ET. ... Marquis. About Roka Bioscience ... Roka Bioscience is ...
(Date:3/27/2017)... Linda, Ca (PRWEB) , ... March 27, 2017 ... ... metastatic colorectal cancer (mCRC) generally produce small, heterogeneous samples with limited tumor content ... analytical challenges remain to be resolved, such as the need for reliable detection ...
Breaking Biology Technology: