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Historical records document stimulant use since ancient times by indigenous cultures in the region of South America, whose members chewed Erythroxylum coca leaves. Cocaine was first used therapeutically in 1884 for ophthalmologic procedures. Amphetamines were first synthesized in 1887, and in 1932 they were first marketed medicinally in an inhaler form for the treatment of congestion. Therapeutic use of methamphetamine to enhance physical and intellectual performance began in the 1930s. Currently these drugs have limited therapeutic roles, but are widely used as drugs of abuse. All of these substances cause their effects and toxicity by stimulation of the sympathetic nervous system.

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Cocaine and methamphetamine abuse is a major problem in the U.S., although accurate assessment of prevalence is limited.

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The 2008 National Household Survey on Drug Abuse reported that an estimated 5.3 million Americans had used cocaine within the past year and 1.9 million had used cocaine within the past month.1 This report estimates that during 2008 there are over 700,000 new cocaine users in the U.S., averaging about 2000 new initiates per day.1 One third of drug-related ED visits in the U.S. are related to cocaine use.2 Fatal injuries (homicides, suicides, falls, and overdoses) after cocaine use are a leading cause of death among young adults in New York City, and probably in many other urban locations as well.3 Statistics from the United Nations show that methamphetamine is the second most commonly abused drug worldwide, following cannabis, and is used by 0.6% of the global population.4 In both Australia and the U.S., methamphetamine was involved in a significant percentage of drug-related ED visits.5–7 The incidence of methamphetamine use is highest in the western U.S., but is increasing in other regions.

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During 2008, the American Association of Poison Control Centers received reports of 32,476 exposures to cocaine, methamphetamine, and related amphetamines, with 30 deaths identified.8

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Cocaine

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Cocaine is the naturally occurring alkaloidal extract of E. coca, a plant indigenous to South America. The water-soluble hydrochloride salt is absorbed across all mucosal surfaces, including the oral, nasal, GI, and vaginal epithelium; thus, cocaine can be topically applied, swallowed, or injected IV. The hydrochloride (salt) form is most often insufflated (snorted) or injected IV. The freebase form of cocaine can be prepared in several ways. A common method uses an alkali, such as sodium bicarbonate, to produce “crack cocaine,” a freebase form that is stable to pyrolysis and can be smoked, producing the popping sound that characterizes its name. The onset and duration of action vary with the route of administration (Table 181-1).

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Table Graphic Jump Location
Table 181-1 Pharmacokinetics of Cocaine 

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