From: [C upi] at [clari.net] (UPI) Newsgroups: clari.biz.industry.health.pharma,clari.news.alcohol+drugs Subject: Ritalin fails to wean cocaine addicts Keywords: health, social issues, substance abuse, pharmaceutical Organization: Copyright 1996 by United Press International Date: Mon, 16 Sep 1996 14:30:14 PDT UPI Science News WASHINGTON, Sept. 16 (UPI) -- A brain imaging study has given new insight into why some cocaine substitutes intended to help addicts kick the habit may actually give a higher high, said researchers Monday. These drugs are designed to bind to a brain mechanism known as the dopamine transporter (DAT), which regulates the mood-lifting substance dopamine. By binding to the DAT, the drugs in theory should neutralize the high from cocaine. But in a new study using brain imaging techniques, investigators found that injections of one of these drugs, methylphenidate (MP), blocks only about eight tenths of the DAT, which is not enough to have a therapeutic effect. Methylphenidate is the scientific name for the controversial drug Ritalin, which, in its oral form, is used to treat attention-deficit disorder (ADD) in children. ``Clearly, without any interpretation or anything, these strategies are not going to work unless a very significant amount of the transporter is occupied,'' said Nora D. Volkow, chairman of the medical department and director of nuclear medicine at Brookhaven National Laboratory, in Upton, N.Y. MP would have to be administered at dangerously high doses to work in treating cocaine, said Volkow. She led the team of researchers whose work on cocaine and Ritalin appears in the Proceedings of the National Academy of Sciences. High doses of drugs that bind to DAT could also damage the heart and cause seizures, she said. ``Based on our results, I don't think we will ever be able to use methylphenidate to treat cocaine abusers,'' said Volkow. In previous studies, addiction researchers tried but failed to wean cocaine abusers with DAT binding drugs, she said. Volkow believes that the drugs might have worked, but only at the higher, possibly toxic, doses. ``They were giving doses, based on our results, that are not going to be effective,'' she said. ``In fact, what we are postulating is: by giving them, they are going to make cocaine more efficient.'' In the study, eight men between the ages of 25 and 35 with no history of drug abuse, were given two injections of MP, spaced one hour apart, about the time it would take for the high from the first dose to subside. The second dose produced a high similar to the first, even though 80 percent of the drug remained in the brains. The researchers found that ``in contrast to the predictions of the 'cocaine substitute' concept, in this study we were unable to block the high by prior DAT blockade.'' Some of the subjects also reported feeling no high after either dose, despite high levels of MP in their brains. This suggests that DAT occupancy alone is not enough to explain the cocaine high. The researchers also said: ``Inducing partial occupancy of DAT with a 'therapeutic' medication might even enhance the high experienced after self-administration of cocaine.'' The use of MP to treat cocaine abusers actually increased cocaine craving and consumption in earlier studies. Researchers estimate about 2 million Americans are addicted to cocaine. Many laboratories are seeking a solution, including vaccines, cocaine analogs and drugs that interfere with the three major brain mechanisms that come into play in cocaine abuse, said Dr. Herbert Kleber, a professor of psychiatry at New York City's Columbia University Medical School. At first, scientists thought that they would be able to use MP in the same way methadone is used to treat heroine addiction, he said. But in Kleber's own experiments using MP to treat cocaine addiction about ten years ago, he found the drug ineffective. Volkow's research, Kleber said, ``provides a rationale for why our studies didn't work.'' He is, however, now testing the drug in one group of patients, cocaine addicts who also have attention-deficit disorder. He estimates about 15 percent to 20 percent of people hooked on cocaine have ADD. (Written from New York by Mara Bovsun)