COCAINE

Cocaine is the active alkaloid that is extracted from the leaves of Erythroxylon coca (Lam.), which contain between 0.5 and 1 % cocaine

History

E. coca comes from the high Andes region in South America, where chewing the leaves has been going on since time immemorial.

The word 'coca' comes from the Aymara Indians of Bolivia, who were conquered by the Inca in the tenth century, and means 'plant'. Under the Inca it acquired a religious significance and was used in prophecies and religious rites, marriage ceremonies, funerals, and the initiation ritual for young noblemen ('haruaca'). This religious significance ensured that its use among the population was extremely restricted. The Inca elite controlled the production on state plantations and only allowed it to be used at rituals and as a special royal gift.

When the Inca empire was conquered by the Spaniards, the chewing of coca was legalized for the entire population by an edict of Philip II. The cultural norms regulating its use lapsed and the drug which satisfied hunger became a substitute for food. As a Spanish administrator remarked: 'If there were no coca, there would be no Peru'. Monardes first described the plant in 1580, but cocaine remained confined to South America for a long time.

The plant does not grow in Europe, and the leaves lost their efficacy during the long voyage. The botanist Joseph de Tussie sent the first plants to Europe in 1750.
Coca was praised in publications by travelers for its stimulating effects and its effectiveness in coping with difficulties of breathing at a high altitude.

Wohler and Niemann managed to isolate cocaine between 1844 and 1862. Aschenbrant, a Bavarian military doctor, first used it medically for asthenia and diarrhea on an Alpine regiment. This was followed by Mantegazza's publications on its fantastic properties. (note 50)

This was the time when it became popular: 'Vin Mariani', wine containing 6 mg of cocaine per ounce, was patented by Angelo Mariani and medically used for a variety of ailments; it was also widely used for non-medical purposes (Pope Leo XVIII, King William III and others used large quantities). Another example of the non-medical use is 'Coca cola', created by Pemberton in 1886.

Arthur Conan Doyle, Alexandre Dumas, Jules Verne, Thomas Edison and R.L. Stevenson are among the famous who used it; it was probably under the influence of cocaine that Stevenson wrote Jekyll and Hyde in three days.

In 1878 W.H. Bentley began to praise cocaine in the US as an antidote to opium, morphine and alcohol addiction. Freud published his 'Uber Koka' in 1884.(note 51) He used it to counter depression and morphine addiction. One of his students, Koller, introduced it as a local anesthetic in the same year. Parke Davis sold cocaine in cigarettes, in the form of an alcoholic drink ('Coca Cordial'), in spray and tablet form, and as an injection fluid.

The first signs of a drop in enthusiasm began to appear between 1885 and 1890: more than 400 reports on chronic psychic and physical disturbances appeared in the medical literature before 1890. Most of them were on the effects among people who had been given cocaine as an antidote to morphine addiction. Many of them combined morphine and cocaine. As a result, the two drugs tended more and more to be confused with one another, and despite the fact that they have completely different effects, they were treated as such by international attempts to regulate them.

The use of cocaine, particularly when sniffed (a form of consumption which came into fashion in 1890), retained its popularity in that sector of society which overlapped high society, bohemian society and the lower middle class, but it virtually disappeared in the US in connection with the disappearance of the patent medicine containing opium as a result of the Pure Food and Drug Act of 1904 and the Harrison Narcotic Act of 1914. It was removed from Coca Cola in 1903. (notes 52 53)

The introduction of Novocain also led to a reduction in its use as a local anesthetic. Events followed a different course in Europe, where it was legal until World War I, but for medical purposes (about which a lot more could be said...). It was made illegal after World War I, but it was still widely used medically until it was replaced by amphetamines at the end of the 1930s. It did not resurface until the 1970s, though within a limited circle.

However, the number of users gradually grew, accelerating in the first half of the 1980s. This was partly a result of the repression of amphetamine, but it was due above all to intervention by the CIA in the Colombian cocaine export. (note 54)

While the use of heroin is mainly confined to the characteristic junkie scene, cocaine is used on a much wider scale. While it was initially the drug or choice of the trend groups (advertising, fashion, jet set), its use was adopted by people from other levels of society. The most striking feature is the relatively wide distribution of cocaine use among non-deviants:
people who otherwise lead a normal life and are no different from their neighbors. The number of people who ask for assistance for specifically cocaine related problems is extremely low. Its use among junkies was a phenomenon of the 1980s. To a large extent it took the place of amphetamine.

A new method of application came into fashion in the US in the 1980s: smoking by freebasing or crack. However, this was not really new, as cocaine cigarettes and cigars were used medicinally at the turn of the century.

Cocaine is used in a different form in South America: the first extraction product, produced by adding sulfur and kerosene to the macerated coca leaves, and then neutralizing this mixture with lye after extraction and drying it. The result is coca paste, known as 'basuko' in South America. The cocaine content can be as high as 90%. The paste is smoked. (note 55)

Effects

Cocaine works by extending and strengthening the activity of the neurotransmitters noradrenaline and dopamine by inhibiting the re-uptake. The effect therefore resembles that of amphetamine, though the peripheral effects are milder, it does not create tolerance, and its effects last for a much shorter period (max. one hour).

Cocaine is not physically addictive. However, people with a low level of self-awareness can develop strong psychical dependence, primarily expressed in an increased frequency of use.

Although cocaine is often portrayed as highly addictive, experience indicates that many people can use cocaine without serious symptoms of social dropping out. Besides systematic research, (notes 56, 57, 58) there are numerous anecdotal accounts which indicate that the use of cocaine need not necessarily create problems. (note 59)

Cocaine also inhibits the re-uptake of serotonin, thereby counteracting the dopamine effect. Cocaethylene, which is formed in the liver when alcohol and cocaine are taken together (as they often are) has no influence on the serotonin, so that the cocaine effect is stronger. (note 60)

Cocaine addiction is sometimes treated with desipramine, an antidepressant, 2.5 mg/kg. The dose has to be reduced if methadone is also being used, in connection with the reduced metabolism through hydroxylizating. (note 61)

Crack
The chemical form in which cocaine is sold on the streets is that of hydrochloric salt: cocaine-HCl. This form is very stable (melting point 195 C), but when heated it is broken down into waste products which have no pharmacological effects. As a result, this form of cocaine cannot be smoked.

To transform cocaine into a form that can be smoked, it has to be heated with a base.
This is done using either NaHOC3, better known as baking powder or bicarbonate of soda, or ammonia (NH40H).
The following reaction is produced:
Cocaine-H-Cl + NaHCO3 --- CO2 + NaCl + Cocaine -H-OH In ordinary language, carbon dioxide is released and common salt is formed. If ammonia is used, NH4Cl (sal ammoniac) is formed. The remaining O and H atoms combine with the cocaine-H- to form cocaine-H-OH.
This is cocaine in base form, which is where the term 'freebase' comes from. This mixture is known as crack (*) because the residual baking powder makes a crackling noise when it is heated. This form of cocaine has a melting point of 98 C, which makes it suitable for smoking.

Since the effect of the substance is generally more dependent on the speed with which the concentration of it rises in the body rather than on the level of the concentration itself, smoking has a greater effect. When sniffed, the substance first has to penetrate a relatively thick mucous membrane in the nose, travel in the blood to the heart, and then return from the heart to the lungs before it can be transported to the brain, resulting in a considerable dilution. When smoked, cocaine rapidly penetrates the extremely thin lung tissue, which is constructed to allow gases to pass through, and then proceeds via the heart straight to the brain. The result is a much more rapid rise in the concentration of cocaine than when it is sniffed. The intensification of the resulting effect seems to be almost of a different kind from the effect of sniffing cocaine, though in fact the difference is only one of degree.

In the US, where the quality of street cocaine is low because of the many adulterations and where the price is high, it is more worthwhile to take cocaine in this way. The combination of cocaine and baking powder is marketed there ready for use under the name 'crack'.

In the Netherlands, where cocaine is good and cheap, it is less worthwhile, and crack ready for use is not available on the market. Crack is prepared and used individually, but generally speaking this is not problematical.

For clarity's sake, blood, urine and other tests will reveal the presence of cocaine, but not how it has been taken. Free-base cocaine has been available in the US since the 1970s, but crack only appeared on the scene in Los Angeles and New York in 1985. Crack was first noted in England in 1987.

Although crack is portrayed in the US drug hysteria as 'instantly addictive', this is not substantiated by research. (note 62 63)

Cocaine and pregnancy
Since the first reports (note 64 65) of the possible negative effects of the use of cocaine by the mother on the foetus and on the pregnancy, an impressive flow of publications has appeared, almost all of it from the US, on the course of the pregnancy and the-neonates.
Much of this is the work of Chasnoff , (note 66 -72) who was head of a special program for women addicts in Chicago. His data are thus based on a very select research group. He attributed all kinds of complications during pregnancy to the use of cocaine by the mother. Most of them, however, were suggestive case histories, a type of publication which attracts a good deal of attention but has little scientific value.

In a large number of other studies, no distinction is made between the use of cocaine and the use of other drugs and/or no control groups are used. The popular idea that 'cocaine' - 'crack' is the devil's drug leads to prejudice at all levels, as has clearly been demonstrated by Koren. (note 73)

Recent studies (notes 74 75) reduce the suggested negative effects to inhibition of the growth of the foetus, which is probably not even due to cocaine but to the life-style and social conditions of the women under investigation. Incidentally, this can serve as a warning to be extremely cautious in assessing the existing literature on the negative effects of illegal drugs.