COCAINE IN BRIEF

This information is provided courtesy of Erowid.



Overview


Cocaine, sometimes known as Coke, Snow, Nose Candy, Dust, White Lady, Toot, and Blow is an alkaloid found in leaves of the South American shrub Erythroxylon coca plant grown primarily in the Andean region of South America. Cocaine is a naturally derived CNS (central nervous system) stimulant.

Cocaine is typically a white-ish powder with a bitter, numbing taste. It is most often insufflated (snorted), though it can also be injected and used orally.

The drug induces a sense of exhilaration in the user primarily by blocking the reuptake of the neurotransmitter dopamine in the midbrain.

History

In pre-Columbian times, the coca leaf was officially reserved for Inca royalty. The natives used coca for mystical, religious, social, nutritional and medicinal purposes. Coqueros exploited its stimulant properties to ward off fatigue and hunger, enhance endurance, and to promote a benign sense of well-being. Coca was initially banned by the Spanish. In 1551 the Bishop of Cuzco outlawed coca use on pain of death because it was "an evil agent of the Devil". The noted 16th century orthodox Catholic artist Don Diego De Robles declared that "coca is a plant that the devil invented for the total destruction of the natives." But the invaders discovered that without the Incan "gift of the gods", the natives could barely work the fields - or mine gold. So it came to be cultivated even by the Catholic Church. Coca leaves were distributed three or four times a day to the workers during brief rest-breaks.

Returning Spanish conquistadores introduced coca to Europe. The plant is perishable and travels poorly. Yet coca was touted as "an elixir of life". In 1814, an editorial in Gentleman's Magazine urged researchers to begin experimentation so that coca could be used as "a substitute for food so that people could live a month, now and then, without eating..."

The active ingredient of the coca plant was first isolated in the West by Albert Niemann around 1860. Sigmund Freud, an early enthusiast, described cocaine as a magical drug. Freud wrote a song of praise in its honour; and he practiced extensive self-experimentation. To Sherlock Holmes, cocaine was "so transcendentally stimulating and clarifying to the mind that its secondary action is a matter of small moment". Robert Louis Stephenson wrote The Strange Case of Dr Jekyll and Mr Hyde during a six-day cocaine-binge.

Doctors dispensed cocaine as an antidote to morphine addiction. Unfortunately, some of their patients made a habit of combining both.

Cocaine was soon sold over-the-counter. Until 1916, one could buy it at Harrods in London. Cocaine was widely used in tonics, toothache cures and patent medicines; in coca cigarettes "guaranteed to lift depression"; and in chocolate cocaine tablets. One fast-selling product, Ryno's Hay Fever and Catarrh Remedy ("for when the nose is stuffed up, red and sore") was 99.9 per cent pure cocaine. Prospective buyers were advised - in the words of pharmaceutical firm Parke-Davis - that cocaine "could make the coward brave, the silent eloquent, and render the sufferer insensitive to pain".

When combined with alcohol, the cocaine alkaloid yields a further potently reinforcing compound, now known to be coca ethylene. Thus cocaine was a popular ingredient in wines, notably Vin Mariani. Coca wine received endorsement from prime-ministers, royalty and even the Pope. Architect Frédérick-Auguste Bartholdi remarked that if only he had used Vin Mariani earlier in his life, then he would have engineered the Statue of Liberty a few hundred meters higher.

Coca-cola was introduced in 1886 as "a valuable brain-tonic and cure for all nervous afflictions". Coca-cola was promoted as a temperance drink "offering the virtues of coca without the vices of alcohol". The new beverage was invigorating and popular. Until 1903, a typical serving contained around 60mg of cocaine. Sold today, it still contains an extract of coca-leaves. The Coca-Cola Company imports eight tons from South America each year. Nowadays the leaves are used only for flavoring since the drug has been removed. Recreational use was banned in the United States in 1914.

The Law

Cocaine is illegal to possess and sell in the United States (schedule II) and in most other countries. It was as one of the first substances to be made illegal in the U.S.

Chemistry



The chemical name for cocaine is benzoylmethyl ecognine (C17H21NO4). It is a bitter, white, odorless, crystalline drug.

Cocaine can be manufactured by converting tropinone into 2 carbomethoxytropinone, reducing this to ecgonine, and then converting the ecgonine to cocaine. This isn't as easy as it sounds.

It is usually exported in the form of the salt, cocaine hydrochloride. This is the powdered cocaine most common, until recently, in the West. Drug testing for cocaine aims to detect the presence of its major metabolite, the inactive benzoylecgonine.

Benzoylecgonine can be detected for up to five days in casual users. In chronic users, urinary detection is possible for as long as three weeks.

When the leaves are soaked and mashed, however, cocaine is then extracted as a coca-paste. After the organic solvent used has evaporated, the coca-paste is 60 to 80 per cent pure. It is usually exported in the form of the salt, cocaine hydrochloride. This is the powdered cocaine most common, until recently, in the West. Drug testing for cocaine aims to detect the presence of its major metabolite, the inactive benzoylecgonine.

Crack Cocaine



To obtain crack-cocaine, ordinary cocaine hydrochloride is concentrated by heating the drug in a solution of baking soda until the water evaporates. This type of base-cocaine makes a cracking sound when heated; hence the name "crack". Base-cocaine vaporizes at a low temperature, so it can be easily inhaled via a heated pipe. Crack is cut or broken into small 'rocks' weighing a few tenths of a gram.

The traditional method of taking cocaine involves snorting the hydrochloride salt. But absorption through the nasal mucosa is relatively modest. This is because their surface-area is small and cocaine is vasoconstrictive. Crack, on the other hand, is smoked and inhaled directly into the lungs. Therefore much higher doses are possible. Inhalation is followed by an intense euphoric rush that comes within a few seconds- even faster than from intravenous cocaine hydrochloride.

Initially, the user may experience a profound sense of power, mastery, cleverness and uninhibited desire. Crack-cocaine delivers an intensity of pleasure completely outside the normal range of human experience. It offers the most wonderful state of consciousness, and the most intense sense of being alive the user will ever enjoy. Groping for adequate words, crack-takers sometimes speak of the rush in terms of a "whole-body orgasm". The exhilaration usually starts to fade within a few minutes. Cocaine is rapidly metabolized in the blood and liver. Its typical half-life is 30-90 minutes.

The euphoria doesn't last long. A "crash" inevitably follows; and a profound melancholy. The user becomes irritable and craves more of the drug. Thus crack-cocaine is not a wise choice of long-term mood-brightener.

Onset and Duration

Onset varies depending on method of ingestion. Snorting cocaine will produce effects within a minute. Smoking freebase cocaine produces effects almost immediately...often before exhaling. Injected cocaine also produces effects within a few seconds.

The effects of snorted cocaine are quite short with the primary high lasting only 20-40 minutes. This is one of the reasons leading to problems with addiction. As the effects wear off, more is often snorted. This pattern of repeated use can quickly move in the direction of addiction. A hit of smoked Crack (freebase cocaine) will typically produce effects lasting 5-15 minutes.

Effects

As with many substances, the effects of cocaine depend greatly on the person and the dose. Possible effects include feelings of well-being, decreased appetite, stimulation, sexual arousal, and increased focus. Negative effects can include increased body temperature and heart rate, agitation and anxiety, paranoia, dizziness, nausea/vomiting, violent behavior, kidney failure, seizure, stroke, and heart attack.

Problems from using Cocaine

Street cocaine is quite often impure. The more direct the route of administration, the more dangerous this can be. Injecting impure cocaine can be deadly. Repeated snorting can cause severe damage to the nose. Smoking of freebase cocaine can cause breathing difficulties.

As a rule of thumb, it is profoundly unwise to use crack-cocaine. The brain has evolved a truly vicious set of negative feedback mechanisms. Their functional effect is to stop us from being truly happy for long. Nature is cruelly parsimonious with pleasure. The initial short-lived euphoria of a reinforcer as powerful as crack will be followed by a "crash".

The neural after effects of chronic cocaine use include changes in monoamine metabolites and uptake transporters. There is down-regulation of dopamine D2 receptors to compensate for their drug-induced over stimulation. Thus the brain's capacity to experience pleasure is diminished.

To obtain more, crack-addicts will often lie, cheat, steal and commit crimes of violence. Whole communities can be disrupted by crack-abuse. Whereas "empathogens" such as Ecstasy - which trigger the release of more serotonin than dopamine - will typically promote empathy, trust, compassionate love and sociability, "dopaminergic" drugs such as cocaine or amphetamines, if taken on their own and to excess, can easily have the reverse effect. There are complications - cocaine's affinity for the serotonin transporter is actually greater than for the dopamine transporter. But simplistically, cocaine tends to be a "selfish" drug.

Negative effects of Cocaine include:
  • Increased heart rate, blood pressure body temperature and respiration
  • Decreased sleep
  • Increased risk of heart attacks, strokes, brain seizure and respiratory failure
  • Reduction of the body's ability to resist and combat infection
  • Confusion, anxiety and depression,
  • Loss of interest in food or sex
  • Erratic behavior

Potential problems from chronic and high dosages:
  • Paranoid behavior
  • Cocaine psychosis"--losing touch with reality,
  • Hallucinations and "coke bugs"--a sensation of imaginary insects crawling over the skin
  • Loss of interest in friends, family, hobbies, and other activities
  • Hyperthermia
  • Violent and hostile behavior
  • Convulsions
  • Damaging the nose eventually leading to a hole in the septum
Withdrawal symptoms from long-term usage of cocaine:

Discontinuing regular use of cocaine can lead to a wide range of unpleasant withdrawal and craving symptoms. They include intense cravings for more cocaine, hunger, irritability, apathy, depression, paranoia, suicidal ideation, loss of sex drive, insomnia or excessive sleep.

Addiction Potential

One of the most problematic aspects of cocaine is its addictive qualities. While cocaine is not believed to be physically addicting, it is, without a doubt, psychologically addicting. Those who use cocaine heavily or regularly frequently encounter great difficulty ceasing use.

Many people find themselves drawn to overusing both crack and powder cocaine. Initial tolerance develops rapidly, especially with heavy use; though tolerance appears to level off relatively quickly (users do not generally require more and more material over time, once they have reached heavy use).

After chronic exposure to cocaine, the number of post-synaptic dopamine receptors in the CNS is reduced. The amount of dopamine transporter protein is increased. Tolerance to cocaine's effects does exist over prolonged use; but the extent of this physiological adaptation is relatively modest. The cocaine-user still gets high; but in the absence of cocaine, his pre-synaptic neurons sequester dopamine in the synaptic cleft with greater efficiency. This may induce depression, and sometimes profound despair.



No one ever feels contented after taking cocaine. They just want more.


Contraindications
  • Research shows that cocaine use during pregnancy may increase chances of miscarriage, premature labor, and stillbirth.
  • Cocaine is likely to be passed to a child during breast-feeding, resulting in irritability and lack of appetite in the baby.


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