A.4 COCAINE

INTRODUCTION

Cocaine is obtained from the leaves of Erythroxylon coca, a bush which is found in abundance in parts of South America. For more than a thousand years, the mountain Indians of Peru and Bolivia have chewed coca leaves for medical, non-medical and religious purposes. It is said that this practice provides renewed energy, endurance, and strength, reduces the need for food and water, improves the spirits, and helps the user withstand the discomforts of cold, illness, and fatigue. In the centuries before the Spanish invaded and conquered South America, coca played an important role in religious customs and ceremonies among the Incas.6, 7, 34' 54' 57

The coca leaf was brought to Europe from the New World by adventurers and tradesmen and it gained a considerable degree of popularity in certain areas. In Paris, in the latter part of the last century, coca elixirs, lozenges and tea were commonly taken. Mariani's famous Vin Coca Mariani, made from an infusion of coca leaf and wine, was used and acclaimed by thousands, including Gounod, Pope Leo XIII and other European notables.6• 35. 54 In the 1850s, cocaine, the principal active alkaloid in the coca plant, was isolated.7, 27, 54 The natural leaf typically contains about one per cent of this material.

Among the first to inquire into the medical usefulness of cocaine was Sigmund Freud, later to become the father of psychoanalysis. In addition to his own extensive personal use of the drug, Freud recommended cocaine for the treatment of morphine and alcohol dependence, asthma, digestive dis- orders, and for the relief of depression and fatigue.19, 27, 43 Freud's associate Carl Kroller demonstrated the powerful local anesthetic properties of cocaine in 1884. In the same year William Halsted, an American surgeon, discovered its nerve-blocking effects. Cocaine was soon hailed in many circles as a medical wonder drug.

Soon after cocaine was introduced, certain undesirable effects of the isolated and potent material began to appear. Dependence problems were frequently reported, even among the medical pioneers in the area, including Halsted.8, 43 However, little difficulty seemed to stem from the use of natural coca leaf or such products as coca tea and wine.

One of the more famous cocaine users was the fictitious prototype of detectives, Sherlock Holmes. In later books, Holmes gave up his use of cocaine and switched to the tobacco pipe.43

In the United States, one of the most popular 'soft' drinks of all time, Coca-Cola®, was developed in 1888 using extracts of coca leaf (containing cocaine) and Kola nut (containing caffeine). Originally, Coca-Cola® was sold as a home remedy rather than a recreational drink. By 1906, when coca came under strict control in the United States, the natural cocaine had been removed from the drink. Large quantities of `decocainized' coca extract are still used for flavouring purposes in the preparation of Coca-Cola®.28, 54

Cocaine has mixed effects, but is generally considered a stimulant and is, in many respects, pharmacologically similar to the amphetamines.4, 26 The patterns and problems of chronic cocaine use, which began to appear soon after the drug was introduced, bear a marked resemblance to the more recently evolved conditions of amphetamine dependence. Although cocaine was often used a few decades ago by heroin users and others in some of the big cities in North America, it had, for a number of years, largely disappeared from the drug scene. Cocaine is back, however, and can no longer be considered rare in Canada. The use of cocaine is presently severely restricted by its high price and very limited availability. The drug is usually referred to as 'coke', 'snow', or 'flake', and occasionally as 'C', 'girl', 'fly', `happy dust', 'lady', or 'rock'.

Cocaine is legally classified with the opiates, as a narcotic, although pharmacologically it has little in common with the opiate narcotics.

MEDICAL USE

The main medical use of cocaine today is as a local anesthetic or pain blocker, particularly in operations involving the eye. This use arises from the fact that low concentrations of cocaine block terminal sensory nerve fibres, and higher concentrations produce anesthesia by direct contact with mucous membranes and the cornea in the eye. Cocaine has also been used to treat asthma and colic, and for symptomatic relief in tuberculosis. The exploratory use of cocaine in the treatment of drug dependence at the turn of the century has been abandoned. Today numerous synthetic cocaine-like compounds have replaced cocaine in most of its former medical applications. For example, procaine (Novocaine()) and lidocaine (Xylocaine®) are widely used medically to block pain in local areas for surgical and dental work, and to reduce the pain from burns, earaches, etc.", 55

CHEMICAL ANALYSIS' OF ILLICIT SAMPLES IN CANADA

Few cocaine samples have been subjected to careful chemical analysis in Canada. No cocaine was found among the 621 'street drug' samples reported in 1970 by Marshman and Gibbins in Toronto." The Commission's national survey of analysis facilities and our own collection of drug samples in 1971-72 provide data on seven items alleged to be cocaine.", [c] Only four of these samples actually contained the drug. In addition, cocaine was found in four other samples where it had not been specified as such. The Health Protection Branch reported the quantitative analysis of 10 police seizures of cocaine in 1971-72.22, Eb] These samples ranged from 0.3%-94.2% cocaine with a median of 53.4%. Procaine and amphetamine are sometimes distributed as cocaine or are used to dilute it. Various sugars are reportedly also common diluents.

ADMINISTRATION, ABSORPTION, DISTRIBUTION AND PHYSIOLOGICAL FATE

Cocaine is a white crystalline powder. In medical practice today, cocaine is rarely applied internally or injected, but is usually administered topically. Epinephrine (adrenalin) is present in official medical preparations of cocaine. In non-medical usage in North America, cocaine is generally sniffed or, less commonly, injected intravenously. The Indians of Peru mix the raw coca leaf with a small amount of lime or vegetable ashes which aid in the extraction of the active alkaloid when the leaf is chewed.

The local vasoconstriction caused by the administration of cocaine limits the rate of its absorption. Nevertheless, cocaine is rapidly absorbed from all sides of application, including the mucous membranes in the nose and mouth, and in the gastrointestinal tract. However, if cocaine is swallowed much of it becomes ineffective before absorption due to chemical alteration in the stomach. Cocaine can be highly toxic because it is absorbed much faster than it is excreted. Cocaine is partially excreted unchanged and may be detected in the urine, but most of a given dose is, rapidly metabolized in the liver.16, 41, 49, 52, 55 A rapid and extremely sensitive immunoassay technique has recently been developed for the detection of cocaine metabolites in body fluids and tissues.33

PSYCHOLOGICAL EFFECTS

In addition to eliminating pain in local areas, cocaine has powerful psychological effects. The general similarities between the effects of cocaine and amphetamine are so striking that some authorities have subsumed both drugs under the same general classification.'' 5, 26 Cocaine is much shorter acting, however, and the main effects of a single dose usually dissipate in less than an hour. In contrast to cocaine, the amphetamines do not have any local analgesic action. Most of the effects of cocaine, which are briefly summarized below, are similar to those of amphetamine described earlier.

Small doses of cocaine and coca leaf have long been reported to provide increased energy, muscle strength and capacity to work; a pleasant psychological lift; an improvement in reaction time and simple mental functions; and relief from the discomforts of hunger, thirst, illness and fatigue.6. 26, 34.54 Most of these claims have not been subjected to rigorous scientific investigation, however.31 As with amphetamines, improvement in function is probably most noticeable when prior performance was low due to fatigue or boredom. There has been little research into the psychological effects of chronic cocaine use. A study in South America suggested slightly poorer intellectual functioning in coca chewers than in non-users, but limitations in the study preclude any simple conclusions.42, 46

There is a considerable resemblance between the patterns of chronic intravenous cocaine use and the 'speed freak' picture discussed earlier in this appendix. The initial 'rush' or 'splash' from intravenous cocaine has been reported to be essentially the same as that associated with the use of amphetamine," although in other respects many stimulant users claim that the two drugs are subjectively different. Users become extremely self-confident in their physical and mental capabilities, may report increased self-insight and, like amphetamine users, often claim to experience more intense and pleasurable sexual orgasms while under the influence of the drug. Cocaine is very short-acting and a period of indescribable euphoria may be followed by considerable psychological depression within an hour after administration. Consequently the dose is often repeated at frequent intervals in patterns which may include several cycles per hour. Some users have been reported to consume several grams a day, although the actual doses of pure cocaine employed are not certain.

With repeated administration of large doses, a toxic psychosis can develop which is similar to the amphetamine psychosis previously described. As with 'speed', some chronic intravenous users have described the sensation of animals or bugs burrowing under the skin. Several cases have been reported of individuals who have injured themselves while attempting to dig out imaginary 'crank bugs'. In a few instances, acute psychotic reactions with hallucinations and severely excited behaviour have occurred after a single injection. Some adverse reactions to topical application have also been noted in medical use. Severe paranoia and violence are not uncommon after long cocaine binges. Many observers attribute the classic popular picture of the 'crazed dope fiend' to the chronic user of cocaine—not the heroin user, as is often assumed.4, 26, 80

In part because of its very limited use at the present time, significant adverse psychological reactions to cocaine are rare in Canada. None of the surveys of treatment facilities conducted by or reported to the Commission have specifically noted cocaine problems.23, 24, 38, 45, 47, 50 The national mental health data collected by Statistics Canada indicated only two psychiatric admissions attributed to cocaine dependence in the country in 1970.14,48' [e] (Poison Control Program Statistics are discussed below.)

PHYSIOLOGICAL EFFECTS

Cocaine's general CNS arousal or stimulant effects are similar to those produced by the amphetamines Administration of cocaine causes an increased rate of respiration resulting in a rapid but shallow breathing pattern, raises body temperature and produces a marked widening of the pupils. Drying of the mouth and nasal passages occurs when cocaine is sniffed. With higher doses, tremors and convulsive movements result from cocaine's effects on motor systems in the brain and spinal cord. Small doses of cocaine cause a slowing of heart rate, but higher doses result in acceleration. The vasoconstrictive properties of the drug produce an initial rise in blood pressure, but this later reserves and pressure drops to subnormal levels. As noted earlier, cocaine blocks nerve transmission in local application.4, 37' 43' 55

As a result of its powerful blood vessel constricting effects, cocaine can damage tissues locally if injected, sometimes leaving small 'pock marks' at the site of injection. Long-term chronic sniffing of large amounts of cocaine can likewise destroy tissue in the nose. Holes in the nasal septum have been reported in some heavy users. Intravenous use of cocaine commonly involves the same problems of unsterile and shared syringes, contaminated drugs, etc., that cause difficulties in the injection of 'speed' and heroin.

There is little evidence of a significant incidence of adverse physiological reactions to cocaine in Canada. We have found no evidence of cocaine deaths in Canada in either our survey of provincial coroner's records or in the reports of Statistics Canada for 1969-71.11, 12, 13, 33 The Federal Poison Control Program has records of one cocaine adverse reaction in 1970 and six for 1971. None were recorded in 1969. No fatal cocaine poisonings were reported.io, 44, [f]

TOLERANCE AND DEPENDENCE

In contrast to the amphetamines, it appears that significant tolerance does not develop to most of the effects of cocaine.4, 18, 31, 34' 53 In fact, increased sensitivity or 'reverse tolerance' with repeated use has been noted by some authors. It has been reported that individuals have self-administered several grams of cocaine in a single day, but that after a period of withdrawal they were still capable of accepting the same amount of drug without ill effects. Although chronic users often increase the frequency of administration and may take the drug several times an hour, there is little general tendency to increase the individual dose to obtain a 'high'.

There seems little question that cocaine can produce, in some individuals, psychological dependence in the sense that there is often a preoccupation with obtaining the drug, compulsive and repeated self-administration, and craving for the drug upon withdrawal in heavy users. The question of physical dependence is less clear. Most authorities feel that no significant physical dependence develops with cocaine use.4, 18 But here again the picture is quite similar to that of chronic 'speed' use. There does appear to be a disruptive syndrome which occurs upon the withdrawal of cocaine, characterized by overeating, prolonged sleep, and emotional depression. It has been suggested that this syndrome cannot be completely accounted for by the appetite suppression and sleep deprivation that occurs during the intake phase of cocaine use.26 Thus cocaine, like the amphetamines, may be capable of producing some subtle kind of physical dependence, albeit in a form different from that produced by the sedatives and opiate narcotics.

COCAINE AND OTHER DRUGS

In spite of the similarity in effects of cocaine and amphetamine, there have been no reports of cross-tolerance between the two. Some of the effects of cocaine are blocked by reserpine, a major tranquilizer 56 Some intravenous heroin users have been known to administer a mixture of cocaine and opiates, known as a 'speed ball'. An alternating pattern between the use of cocaine and opiate narcotics, similar to that noted earlier in the section on amphetamines, has also been described. The occasional sniffing of cocaine by users of marijuana and other psychedelic drugs has been reported, and cocaine and cannabis are sometimes used together. (See also Appendix C Extent and Patterns of Drug Use.)