Designer Drugs

DESIGNER DRUGS

Designer drugs are synthesized chemical analogues of known, dangerous drugs; they are designed to produce pharmacological effects similar to the drugs they mimic. In the pharmaceutical industry, the development of new drugs often utilizes principles of basic chemistry, so that the structure of a drug molecule may be slightly altered to change its pharmacological activity. For therapeutic purposes, these strategies have had a long and successful history; for medical pharmaceutics, many useful new drugs or modifications of older drugs have resulted in improved health care. The principle of structure-activity relationships has been applied to many medically approved drugs in the marketplace, especially in the search for painkillers—nonaddicting opioid analgesics.

The clandestine production of new street drugs is, however, intended to avoid federal regulation and control. This practice can often result in the appearance of unknown substances, with wide-ranging degrees of purity, which have the potential to cause dangerous toxicity and serious health consequences for the unwitting drug user (the quality of personnel involved in clandestine drug synthesis can range from cookbook amateurs to highly skilled chemists). The most publicized case regarding the tragic consequences associated with the manufacture and use of designer drugs on the street involves MPTP (1-methyl, 4-phenyl, 1, 2, 3, 6-tetra-hydropyridine), a substance that was later found to cause a Parkinsonian syndrome in humans.

A controlled substance that has served as a template for the design of new look-alike Opioid drugs is Meperidine (Demerol). A slight change in its chemical structure yields the drug known as MPPP (1-methyl-4-propionoxy-4-phenylpyridine), a meperidine look-alike drug, which is known on the streets as synthetic heroin. In California in 1982, four young drug abusers developed Parkinsonian symptoms after the illicit intravenous use of street Heroin. The analysis of their remaining drug samples revealed the presence of both MPPP and MPTP. The dealer involved in this illicit synthesis and sale of MPPP was a bad chemist, since MPTP represents a side product formed through the inadequate control of the temperature and/or acidity of the chemical reaction.

Another opioid that has resulted in serious health hazards on the street is fentanyl (Sublimaze), a potent and extremely fast-acting Nar-Cotic Analgesic (painkiller) with a high Abuse Liability. This drug has also served as a template for many look-alike drugs that come out of clandestine chemical laboratories. Very slight modifications in the chemical structure of fentanyl can result in analogues such as para-flouro-, 3-methyl-, or alpha-methyl-fentanyl—with, respectively relative potencies 100,900, and 1,100 times that of Morphine. During the 1980s, the Drug Enforcement Administration (DEA) has reported a steady increase in deaths from drug overdoses associated with fentanyl-like designer drugs. Not every "de-signer" drug is actually thought up by chemists in illegal labs; some were actually synthesized for legitimate medical uses but were never marketed. Hallucinogenic drugs, such as LSD or Mescaline, rarely cause death—except as Acci-Dents related to drug-induced mental aberrations. Adverse reactions to typical hallucinogens are usually treated by support, reassurance, and a quiet environment. Hallucinogenic designer drugs, however, include such substituted Amphetamine ("speed") analogues as methylenedioxyamphetamine (MDA), methylenedioxymethamphetamine (MDMA or "Ecstasy"), and methylenedioxyethamphetamine (MDEA or "Eve"). Both acute and chronic toxicity have been reported following the administration of these drugs. Acute toxicity is usually manifested as restlessness, agitation, sweating, high blood pressure, tachycardia, and other cardiovascular effects, all of which are suggestive of excessive central nervous system stimulation. Following chronic administration in animals, MDA has been demonstrated to produce a degeneration of serotonergic nerve terminals in rats, implying that MDA might induce chronic neurological damage in humans as well. This also suggests that extreme caution should be exercised regarding the manufacture and use of MDA, MDMA, and related drugs—although a few psychotherapists claim that MDMA is a useful adjunct in the treatment of some patients.

The widespread illicit manufacture and use of designer drugs with unknown chronic toxicity could result in millions of people experimenting with the drug before the toxic effect was recognized; this could potentially produce an epidemic of neurodegenerative disorders.

(See also: Complications ; Controlled Substances Act of 1970 ; MDMA ; MPTP )

BIBLIOGRAPHY

Barnett, G., & Rapaka, R. S. (1989). Designer drugs: An overview. In K. K. Redda, C. A. Walker, & G. Barnett (Eds.), Cocaine, marijuana, designer drugs: Chemistry, pharmacology, and behavior (pp. 163-174). Boca Raton, FL: CRC Press.

Dowling, G. P., Mc Donough, E. T., III. & Bost, R.O. (1987). "Eve" and "ecstasy": A report of five deaths associated with the use of MDEA and MDMA. Journal of the American Medical Association, 257, 1615.

Nichols, D. E. (1989). Substituted amphetamine controlled substance analogues. In K. K. Redda, C. A. Walker, & G. Barnett (Eds.), Cocaine, marijuana, designer drugs: Chemistry, pharmacology, and behavior (pp. 175-185). Boca Raton, FL: CRC Press.

Nick E. Goeders