Meperidine And Its Analogues

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Meperidine (Figure 7.4) was introduced in the 1930s as an alternative to morphine for relieving pain. Its advantage over morphine was that its duration of action was shorter and it had fewer unwanted side effects such as sedation and constipation.

However, meperidine turned out to be less potent than morphine as a painkiller. This inspired underground chemists to try to synthesize more potent analogues of meperidine, with hopes that increasing the potency might give heroin addicts another way to get high. One such analogue was developed in 1977 by a college student in Bethesda, Maryland, who also had a drug habit. (Ironically, he started making meperidine analogues with a home chemistry kit that his parents gave him.) The analogue he synthesized was 1-methyl-4-phenyl-propionoxypiperidine, or MPPP for short. MPPP was sometimes referred to as New Heroin.

Synthesis Meperidine

Figure 7.4 The chemical structure of meperidine, its analogue MPPP, and the closely related neurotoxin MPTP, are all shown here. Meperidine, an anesthetic, was also used as an alternative to morphine. It proved advantageous because it has a shorter length of duration and fewer side effects than morphine.

Figure 7.4 The chemical structure of meperidine, its analogue MPPP, and the closely related neurotoxin MPTP, are all shown here. Meperidine, an anesthetic, was also used as an alternative to morphine. It proved advantageous because it has a shorter length of duration and fewer side effects than morphine.

This college student was able to successfully make MPPP from meperidine for months for his own use. However, one day while cooking up some MPPP, he was in a hurry and skipped a step or two in the synthesis process. Later, when he decided to inject himself with this latest batch of MPPP, he immediately knew something was wrong when his whole arm began to burn. Within a few days, his arms and legs became completely paralyzed, and he was unable to move or speak. His parents took him to several psychiatrists and neurologists who eventually diagnosed him with Parkinson's disease, a disease that primarily occurs in people over 65 years old and is largely incurable. The college student's life was forever changed.

Unaware of it at the time, the college student's "sloppy chemistry" had, in addition to synthesizing MPPP, inadvertently created some additional by-products that were very toxic. It turns out that one of the by-products, called 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), is very toxic to neurons in

PARKINSON'S DISEASE — NATURAL AND EXPERIMENTAL

Parkinson's disease is a devastating brain disorder that occurs in approximately one out of every 100 people. The disease is marked by extreme muscle stiffness, slowness or inability to walk, difficulty initiating movements of the arms and legs, and occasionally tremors. Although the disease usually strikes elderly people over the age of 65, it can also occur in younger people. Notable celebrities that have this "early onset" form of Parkinson's disease include boxer Muhammad Ali (who was in his early 40s when diagnosed) and actor Michael J. Fox (who was actually 30 when he was originally diagnosed, but did not go public about the disease for another seven years).

The cause of Parkinson's disease is still unknown. However, researchers have pinpointed the brain regions and neurotransmitters involved in the disease. For some reason, neurons containing the neurotransmitter dopamine that are located in a brain region called the substantia nigra (literally, "black substance") start to die in patients with Parkinson's disease. These neurons send their dopamine-releasing axon fibers to the striatum (also known as the caudate nucleus and putamen), a brain region involved in voluntary control of movements. When neurons in the substantia nigra die, a shortage of dopamine in the striatum results, and the patient begins to lose control over muscle movements, walking, etc. Drugs that the brain that use the neurotransmitter dopamine. Circuits in the brain that use dopamine are primarily involved in the control of motor skills such as movements of the arms, legs, and face. This MPTP-laced heroin explained why this young man showed signs of Parkinson's disease.

In 1982, many more cases of drug addicts becoming "frozen" after injecting themselves with (what they thought to be) heroin were reported by various emergency rooms in the San Francisco Bay area. Neurologists, psychiatrists, and mimic the action of dopamine, or are converted to dopamine once taken, such as L-dopa, are currently used to treat Parkinson's disease, but with limited success.

When heroin laced with toxic MPTP enters the body, it is metabolized to form MPP+, which is very toxic to neurons containing dopamine, such as those in the substantia nigra. In addition, it is a relatively selective toxin, so it does not destroy neurons containing other types of neurotransmitters. When heroin addicts injected that bad batch of heroin containing the meperidine analogue MPTP, it was converted to MPP+ and destroyed many neurons in their substantia nigra, resulting in a dopamine shortage in their striatum and subsequently causing symptoms resembling Parkinson's disease.

Despite the misfortunes of these addicts, MPTP has proved an invaluable tool for studying the biology of Parkinson's disease. When MPTP is injected into experimental rats, mice, or monkeys, neurons in the substantia nigra of these animals start to die, and the animals develop motor problems that closely resemble the symptoms of Parkinson's disease. Researchers hope to use MPTP in animals to unravel the mystery of what causes Parkinson's disease in humans, in the hope that they can develop a cure for this devastating disease.

scientists were able to trace contaminants found in the victims' bodies to a bad batch of heroin that was being sold in the area. These unfortunate heroin addicts also developed a form of Parkinson's disease.

Statistics on the patterns of use of fentanyl and meperidine analogues are relatively scarce. Although abuse of prescription painkillers is on the rise, the use of fentanyl and meperi-dine analogues is not. Law enforcement agencies believe the use of painkiller analogues is not nearly as prevalent today as it was in the 1970s and 1980s because of increased law enforcement efforts to shut down illegal underground laboratories and tighter restrictions and documentation of fentanyl and meperidine prescriptions and shipments. In addition, heroin addicts tend to shy away from fentanyl and meperidine analogues because of the frightening reports that they cause frequent overdoses and degeneration of neurons in the brain.

Bibliography and Further Reading

Chapter 1: Designer Drugs and the Brain

Buchanan, J.F., and C.R. Brown. "'Designer drugs.' A problem in clinical toxicology." Medical Toxicology and Adverse Drug Experience 3, 1988. 1-17.

Henderson, G.L. "Designer Drugs: Past History and Future Prospects." Journal of Forensic Science 33 (1988): 569-575.

Morgan, J.P. "Designer Drugs." In: Substance Abuse—A Comprehensive Textbook (Lowinson JH, Ruiz P, Millman RB, Langrod JG, eds). 3rd ed. Baltimore: Williams & Wilkins, 1997, 264-269.

Ziporyn, T. "A growing industry and menace: makeshift laboratory's designer drugs." Journal of the American Medical Association 256 (1986): 3061-3063.

Chapter 2: Methamphetamine

The DAWN Report. Rockville, Md.: Drug Abuse Warning Network, Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), December 2000.

Emergency Department Trends from the Drug Abuse Warning Network: Final Estimates 1994-2001, Rockville, Md.: Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), August 2002.

Fact Sheet: Methamphetamine. Rockville, Md.: Office of National Drug Control Policy Information Clearinghouse, May 1999.

Monitoring the Future 2002—Data from In-School Surveys on 8th, 10th and 12th Grade Students, Rockville, Md.: National Institute on Drug Abuse and the University of Michigan, December 2002.

Research Report: Methamphetamine Abuse and Addiction, Bethesda, Md.: National Institute on Drug Abuse, NIH Publication 98-4210, April 1998.

Chapter 3: Ecstasy

Cole, J.C., and H.R. Sumnall. "Altered States: the Clinical Effects of Ecstasy." Pharmacology and Therapeutics 98 (2003) 35-58.

The DAWN Report. Rockville, Md.: Drug Abuse Warning Network, Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), December 2000.

Emergency Department Trends from the Drug Abuse Warning Network: Final Estimates 1994-2001, Rockville, Md.: Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), August 2002.

Fact Sheet: MDMA (Ecstasy). Rockville, Md.: Office of National Drug Control Policy Information Clearinghouse, May 1999.

| Bibliography and Further Reading

Monitoring the Future 2002—Data from In-School Surveys on 8th, 10th and 12th Grade Students, Bethesda, Md.: National Institute on Drug Abuse and the University of Michigan, December 2002.

Chapter 4: GHB

The DAWN Report. Rockville, Md.: Drug Abuse Warning Network, Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), December 2000.

Emergency Department Trends from the Drug Abuse Warning Network: Final Estimates 1994—2001, Rockville, Md.: Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), August 2002.

Fact Sheet: Gamma Hydroxybutyrate. Rockville, Md.: Office of National Drug Control Policy Information Clearinghouse, November 2002.

Monitoring the Future 2002—Data from In-School Surveys on 8th, 10th and 12th Grade Students, Bethedsa, Md.: National Institute on Drug Abuse and the University of Michigan, December 2002.

Chapter 5: Rohypnol

The DAWN Report. Rockville, Md.: Drug Abuse Warning Network, Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), December 2000.

Emergency Department Trends from the Drug Abuse Warning Network: Final Estimates 1994—2001, Rockville, Md.: Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), August 2002.

Fact Sheet: Rohypnol. Rockville, Md.: Office of National Drug Control Policy Information Clearinghouse, February 2003.

Monitoring the Future 2001—Data from In-School Surveys on 8th, 10th and 12th Grade Students, Bethesda, Md.: National Institute on Drug Abuse and the University of Michigan, 2002.

Chapter 6: Ketamine

Curran, H.V., and C. Morgan. "Cognitive, Dissociative and Psychotogenic Effects of Ketamine in Recreational Users on the Night of Drug Use and 3 Days Later." Addiction 95 (2000): 575-590.

The DAWN Report. Rockville, Md.: Drug Abuse Warning Network, Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), December 2000.

Dillon, P. Copel, and J.K. Jansen. "Patterns of Use and Harms Associated with Non-Medical Ketamine Use." Drug and Alcohol Dependence 69 (2003): 23-28.

Emergency Department Trends from the Drug Abuse Warning Network: Final Estimates 1994-2001, Rockville, Md.: Office of Applied Studies, Substance Abuse and Mental Health Services Administration (SAMHSA), August 2002.

Monitoring the Future 2002—Data from In-School Surveys on 8th, 10th and 12th Grade Students, Bethesda, Md.: National Institute on Drug Abuse and the University of Michigan, December 2002.

Research Report: Hallucinogens and Dissociative Drugs, Bethesda, Md.: National Institute on Drug Abuse, NIH Publication No. 01-4209, March 2001.

Wenker, C.J. "Anesthesia Of Exotic Animals." The Internet Journal of Anesthesiology. Volume 2, Number 3, 1998.

Chapter 7: Painkiller Analogues

Langston, J.W., and J. Palfreman. The Case of the Frozen Addicts. New York: Pantheon Books, 1995.

Morgan, J.P. "Designer Drugs." Substance Abuse-A Comprehensive Textbook. 3rd ed., eds. J.H. Lowinson, P. Ruiz, R.B. Millman, and J.G. Langrod. Baltimore, Md.: Williams & Wilkins, 1997, 264-269.

Research Report: Prescription Drugs: Abuse and Addiction, Bethesda, Md.: National Institute on Drug Abuse, NIH Publication No. 01-4881, July 2001.

| Websites_

U.S. Department of Health and Human Services and the Substance Abuse and Mental Health Services Administration (SAMHSA)'s National Clearinghouse for Alcohol and Drug Information. Provides information about prevention, treatment, and recovery.

www.whitehousedrugpolicy.gov

The U.S. government's Office of National Drug Control Policy. Legal issues and fact sheets.

www.drugabuse.gov

The National Institute on Drug Abuse's Website. An extensive Website containing information for children and parents, teachers and students, and researchers and health professionals.

Website of the U.S. Drug Enforcement Administration. Contains legal information about drug use and abuse.

www.clubdrugs.org

A Website targeted toward teenagers, part of the National Institute on Drug Abuse. Focuses on club drugs such as Ecstasy, GHB, Rohypnol, ketamine, methamphetamine, and LSD.

www.streetdrugs.org

Extensive Website devoted to education about many drugs, current trends, and law enforcement policies.

www.methamphetamineaddiction.com

Contains information about methamphetamine addiction, treatment options, and personal stories of recovery. Sponsored by the Narconon Arrowhead treatment program.

www.ecstasyaddiction.com

Information about Ecstasy (MDMA) addiction, treatment options, and personal stories of recovery. Sponsored by the Narconon Arrowhead treatment program.

www.projectghb.org

Information about GHB, the effects of the chemical, and date rape, as well as personal accounts.

www.designer-drugs.com

Personal Website of Donald A. Cooper, Drug Enforcement Administration, McLean, Virginia. Contains information about various synthetic, or "designer," drugs.

| Additional Resources_

If you would like more information about drug use and abuse, or to speak to someone confidentially, please call the following hotlines:

American Council for Drug Education

800-488-DRUG (800-488-3784)

National Institute of Drug Abuse

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