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.
Cocaine and methamphetamine abuse is a major problem in the U.S.,
although accurate assessment of prevalence is limited.
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.
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
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
181-1 Pharmacokinetics of Cocaine
| Save Table
181-1 Pharmacokinetics of Cocaine
|Route of Exposure||Onset of Action||Peak Action||Duration of Action|
|IV||<1 min||3–5 min||30–60 min|
|Nasal insufflation (snorting)||1–5 min||20–30 min||60–120 min|
|Inhalation (smoking)||<1 min||3–5 ...|
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