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"Pharmacology of Cocaine Abuse"

Cocaine, Marijuana, Designer Drugs
by Kinfe Redda, Charles Walker, Gene Barnett
CRC Press, Boca Raton, Florida, 1989.

by Roger M. Brown


The earliest documentation of cocaine use goes back at least as far as 500 A.D. A grave in Peru was discovered which contained several bags of cocaine, as well as other things, for the occupant to take into the afterlife. During the 16th century, the Spanish entrepreneurs in South America noted the power of the influence of coca and they used the leaves to recruit Indians for labor. The conquistadors brought reports to Europe of the invigorating properties of coca and how it improved the stamina of the Peruvians working at high altitdues. The Europeans, however, weren't much impressed with coca leaves; this was probably due to an inactivation of the alkaloid during the long boat trip from South America. It wasn't until about 1750 that the plant itself reached the continent.

By the mid-1800s, cocaine was being recommended among other things for toothache, digestive disorders, and even as a "balm for young people suffering from timidity". In 1846, Johan Jakob von Tschudi wrote, "I am clearly of the opinion that moderate use of coca is not merely innocuous, but that it may even be conducive to health.", and in 1859 Paolo Mantegazzi, a neurologist famed at the time, wrote, "I prefer a life of ten years with coca to one hundred thousand without it." The widespread use of coca was facilitated in 1863 by Angelo Mariana's concoction, Vin Mariani, a mixture of Bordeaux wine, a small amount of alkali, and fragments of coca lead sufficient to yield 30 grains per wine glass. Mariana's wine was advertised as a tonic to "aid digestion, strengthen the system, and prevent malaria, influenza, and wasting disease". The tonic received testimonials from popes, kings, and czars; even Thomas Edison appeared among the notables who enthusiastically supported the mixture. Thus, cocaine was available not only to professional and so-called "intellectual" circles, but also to the general public through various nostrums

Another way cocaine became generally available was through the drug store soda fountain. John Styth Pemberton, a pharmacists, formulated a product in 1885 which he called "French Wine of Coca, Ideal Tonic". This mixture was so popular that he sought to improve on it. He combined coca with kola nut, aromatized it, added syrup, and therewith gave birth to Coca-Cola, "the brain tonic and intellectual soda fountain beverage". The soda fountain at Jacobs Pharmacy in Atlanta where Coca-Cola was introduced rapidly became one of the most popular places in the city.

Conaine also received more serious medical considerations. In 1880, an article appeared in the Therapeutic Gazette by W.H. Bentley in which the rationale was set forth for its use in the treatment of opiate and alcohol addition. Cocaine was seen as a means of providing the customary "stimulus" to the opiate or alcohol addict without leaving a feeling of depression. In this way, the victim of drugs could walk away from his vice with little effort. Numerous articles appeared about this time testifying to the treatment of opiate addiction with cocaine. Among them was a statement in the Louisville Medican News: "One feels like trying coca with or without the opium habit. A harmless remedy for the blues is imperial. And so we say." Among the many proponents of the use of cocaine in the treatment of addition was Sigmund Freud, whose experience with cocaine treatment is well-known. Freud was initially so-enthused with cocaine that he spoke of administering an "offering" rather than a dose, and he described all attacks on cocaine as "slander". His enthusiasm greatly diminished, however, after he nursed a close friend through a bout of cocaine psychosis. After that we was very much disenchanted with the drug.

Cocaine was found to have beneficial properties and Karl Koller is given the credit for recommending cocaine as a local anesthetic in 1884. The drug was known to produce numbness, but it took Koller to suggest its use in surgery. Soon it was being recommended for surgery of eye, ear, nose and throat, not to mention its use as a nerve block for hernia operations and amputations.

By the late 1800s, the enthusiasm for cocaine diminished as negative experiences with the drug started to make an impact. There were reports of "substituting one addiction for another", cocaine pyschosis, and other consequences such as "cocaine bugs". Even as early as 1836, Edvard Poppig said that the cocaine user is, "a slave of his passion even more so than the drunk". As a result of excessive use and negative outcome, legislation was initiated to control cocaine. First, the Pure Food and Drug Act of 1906 attempted to limit the import of cocaine to medical purposes only. Later, legislators involved in formulating the Harrison Narcotic Act of 1914 were so enthusiastic that they labeled cocaine as a narcotic. Even today confusion still exists over the legal versus pharmacological definition of a narcotic! Finally, the Controlled Substances Act of 1970 [in the U.S.] was the first act in which illegal posession of cocaine was made a Federal crime.



Cocaine has two major pharmacological actions. It is (1) a local anesthetic and (2) an indirect acting sympathomimetic which potently enhances the effect of neural transmission.

1. Cocaine as a Local Anesthetic

Cocaine prevents conduction of sensory impulses by reacting with the neuron membrane to block ion channels. As a result of this block, the ion exchange which is normally responsible for the electrical signals cannot be propagated along the axon and so sensory messages are not received in the central nervous system. This is the basis for the early application of cocaine in eye surgery. Problems with abuse, however, led to a search for other local anesthetics and, as a result, novocaine (Procaine) was synthesized in 1905 followed by xylocaine (Lidocaine) about 1906. The local anesthetic action is important in and of itself. In addition, the role of a local anesthetic action in the subjective psychotropic response to cocaine is presently debated with respect to its contribution to the abuse liability fo cocaine.

2. Cocaine is a Sympathomimetic

The second major action of cocaine is its ability to potentiate neurotransmission in neurons that use of on the monoamines, norepinephrine, dopamine, or serotonin, as a neurotransmitter. In the periphery this occurs mainly at the noradrenergic terminals of the sympathetic component of the autonomic nervous system, and in the brain at monoaminergic terminals (i.e., those that utilize norepinephrine, dopamine or serotonin), for which there are many fiber networks. ....


2. Routes of Administration

Various routes of administration have been tried by the cocaine user, and each produces its own characteristic absorption pattern and associated problems.

Topical - This route is mentioned only for the sake of completeness. It is the only licit route of administration and is used for local application of anesthetic. There is insufficient absorption from the cutaneous route to cause a psychotropic response.

Oral (chewing leaves) - The natives of South America chew coca leaves by mixing them with alkali (ashes) and then chewing the mixture into a quid which is then placed between the cheek and gum. There is no or little high produced by chewing, probably due to the relatively slow absorption and the low concentration of cocaine in the blood which is only half that obtained by snorting. Cocaine can also be absorbed by the gastrointestinal tract, but the absorption is too slow to produce any profound subjective effect.

Nasal inhalation (snorting) - Cocaine is readily absorbed from the nasal mucosa. ... The high induced by inhaled cocaine may have been first noticed by an allergy sufferer since cocaine was once used as a decongestant and for a time was the official remedy of the Hay Fever Association.

Cocaine is an alkaloid, i.e., a nitrogenous plant base, and it exists in this form in coca leaves. Because cocaine alkaloid is not stable, practically all isolated cocaine is converted to the form of the stable hydrochloride salt.

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