Stimulant Abuse: Pharmacology, Cocaine, Methamphetamine, Treatment, Attempts at Pharmacotherapy

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Recent History

Stimulants, including cocaine and amphetamines, are among the most widely used and abused illegal substances in the United States. Coca chewing has a long history of indigenous use in South America.1 Widespread use of cocaine followed its isolation from coca in 1859 and a medical publication purporting its benefits in 1884. The subsequent incorporation of cocaine into patent medicines and popular beverages, for example, Vin Mariani and Coca-Cola, contributed to its profligate use.2 Rising

Cocaine

Cocaine is a naturally occurring alkaloid in the leaves of the coca plant, Erythroxylon coca, which is indigenous to the Andean region of South America. The area of coca under cultivation in Colombia, Peru and Bolivia peaked in 2000 at 221,300 hectares, subsequently declining to 167,600 hectares in 2008. Most of the cocaine derived from this harvest is for export. Estimates of potential cocaine production for the region have varied little since 1994; in that year, the estimated production was

Effects on neurotransmitter systems

Stimulants facilitate the activity of the monoamine neurotransmitters, that is, dopamine, norepinephrine, and serotonin, in the CNS and peripheral nervous system.35, 36 Both cocaine and amphetamines act on presynaptic monoamine reuptake transporters but each in unique ways. Cocaine is a reuptake inhibitor, that is, it blocks the action of the reuptake transporter, thus allowing more neurotransmitters to stay active in the synapse. Amphetamines are releasers, that is, they are taken up by the

Short-Term Use: Intoxication and Overdose

The clinical effects of stimulant use, including psychological, behavioral and physiologic effects, vary by short-term versus long-term use, potency of drug, route of administration, and dosage.

Short-term use of stimulants leads to rapid neurotransmitter release, resulting in euphoria, increased energy and libido, reduced fatigue and appetite, and behavioral responses, for example, increased self-confidence and alertness.47 Acute adrenergic effects include dose-responsive tachycardia and

Screening

In the primary care setting, substance use concerns lie in a continuum of risk, and many patients with low to moderate substance use disorders present subclinically. Screening for at-risk levels of alcohol use in the primary care setting has been given a B rating (recommended based on fair evidence) by the United States Preventive Services Task Force (USPSTF).112 However, according to the USPSTF, the benefit and clinical utility of screening asymptomatic patients for illicit substance use

Summary

The high prevalence of stimulant abuse and its harmful consequences make the screening, diagnosis, and referral for treatment of persons with stimulant abuse a top concern for primary care providers. Having a working knowledge of use patterns, clinical symptomatology, end-organ effects, and advances in treatment of stimulant abuse is essential.

Although cocaine and amphetamine have different use patterns, duration of action, and so forth, the consequences of use are remarkably similar. Effective

Acknowledgments

The author gratefully acknowledges the contributions of Nathan Sackett, RN in researching and editing sections of this article.

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    This work was supported by Grant DA16165, from the National Institutes of Health, National Institute on Drug Abuse.

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