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For over a thousand years South American indigenous peoples have chewed the leaves of Erythroxylon coca, a plant that contains vital nutrients as well as numerous alkaloids, including cocaine. The coca leaf was, and still is, chewed almost universally by some indigenous communities. Today, in many countries, cocaine is a popular recreational drug. In the United States, cocaine use is prevalent across all socioeconomic strata, including age, demographics, economic, social, political, religious, and livelihoods. It was reported in October 2010 that the use of cocaine in Australia has doubled since monitoring began in 2003.

Abstract

Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant.The name comes from "coca" and the alkaloid suffix -ine, forming cocaine. It is a stimulant, an appetite suppressant, and a topical anesthetic. Biologically, cocaine acts as a serotonin–norepinephrine–dopamine reuptake inhibitor, also known as a triple reuptake inhibitor (TRI). It is addictive because of its effect on the mesolimbic reward pathway. It is illegal to possess, grow, or distribute cocaine for non-medicinal and non-government-sanctioned purposes in almost all countries.

Street Names

Coke
Snow
Yoyo
Blow

History

For over a thousand years South American indigenous peoples have chewed the leaves of Erythroxylon coca, a plant that contains vital nutrients as well as numerous alkaloids, including cocaine. The coca leaf was, and still is, chewed almost universally by some indigenous communities. The remains of coca leaves have been found with ancient Peruvian mummies, and pottery from the time period depicts humans with bulged cheeks, indicating the presence of something on which they are chewing.There is also evidence that these cultures used a mixture of coca leaves and saliva as an anesthetic for the performance of trepanation. Cocaine was used for medicinal purposes right from 1879. With the discovery of this new alkaloid, Western medicine was quick to exploit the possible uses of this plant.It was then used as a remedy for dental pain in children.

Today, in many countries, cocaine is a popular recreational drug. In the United States, cocaine use is prevalent across all socioeconomic strata, including age, demographics, economic, social, political, religious, and livelihoods. It was reported in October 2010 that the use of cocaine in Australia has doubled since monitoring began in 2003.

Pharmacology

The chemical name of cocaine is: benzoylmethylecgonine. Cocaine in its purest form is a white, pearly product. Cocaine appearing in powder form is a salt, typically cocaine hydrochloride (CAS 53-21-4). Street market cocaine is frequently adulterated or “cut” with various powdery fillers to increase its weight; the substances most commonly used in this process are baking soda; sugars, such as lactose, dextrose, inositol, and mannitol; and local anesthetics, such as lidocaine or benzocaine, which mimic or add to cocaine's numbing effect on mucous membranes. Cocaine may also be "cut" with other stimulants such as methamphetamine.Adulterated cocaine is often a white, off-white or pinkish powder.

The color of “crack” cocaine depends upon several factors including the origin of the cocaine used, the method of preparation – with ammonia or baking soda – and the presence of impurities, but will generally range from white to a yellowish cream to a light brown. Its texture will also depend on the adulterants, origin and processing of the powdered cocaine, and the method of converting the base. It ranges from a crumbly texture, sometimes extremely oily, to a hard, almost crystalline nature.

Uses

Cocaine has a number of legitimate medical uses. It is used as a topical anesthetic for eye and ear surgery. It is an anesthetic that works quickly to numb the area about 1-2 minutes after application. Cocaine also causes blood vessels to narrow, an effect that can decrease bleeding and swelling from the procedure.

However, most users of cocaine treat it as a recreational drug. In spite of some positive effects such as helping against fatigue, the side effects, both long term and short term are overwhelming. 

Scheduling

Today, cocaine is a Schedule II drug under the Controlled Substances Act of 1970, meaning that it has high potential for abuse, but can be administered by a doctor for legitimate medical uses, such as local anesthesia for some eye, ear, and throat surgeries.

Psychological and physical addiction liability

Cocaine addiction is psychological dependency on the regular use of cocaine. Cocaine dependency may result in physiological damage, lethargy, psychosis, depression, akathisia, and fatal overdose.

Withdrawal Effects

If a person who is addicted to coacaine tries to discontinue using it, the user will experience what has come to be known as a "crash" along with a number of other cocaine withdrawal symptoms, including paranoia, depression, exhaustion, anxiety, itching, mood swings, irritability, fatigue, insomnia, an intense craving for more cocaine, and in some cases nausea and vomiting. Some cocaine users also report having similar symptoms to schizophrenia patients and feel that their mind is lost. Some users also report formication: a feeling of a crawling sensation on the skin also known as "coke bugs". These symptoms can last for weeks or, in some cases, months. Even after most withdrawal symptoms dissipate most users feel the need to continue using the drug; this feeling can last for years and may peak during times of stress. About 30-40% of cocaine addicted patients will turn to other substances such as medication and alcohol after giving up cocaine. There are various medications on the market to ease cocaine withdrawal symptoms.

Long term effects

Cocaine is a powerfully addictive drug. Thus, it is unlikely that an individual will be able to reliably predict or control the extent to which he or she will continue to want or use the drug. And, if addiction takes hold, the risk for relapse is high even following long periods of abstinence. Recent studies have shown that during periods of abstinence, the memory of the cocaine experience or exposure to cues associated with drug use can trigger tremendous craving and relapse to drug use.
Users take cocaine in "binges," during which the cocaine is used repeatedly and at increasingly higher doses. This can lead to increased irritability, restlessness, panic attacks, and paranoia—even a full-blown psychosis, in which the individual loses touch with reality and experiences auditory hallucinations. With increasing dosages or frequency of use, the risk of adverse psychological or physiological effects increases.
Different routes of cocaine administration can produce different adverse effects. Regularly snorting cocaine, for example, can lead to loss of sense of smell; nosebleeds; problems with swallowing; hoarseness; and an overall irritation of the nasal septum, which could result in a chronically inflamed, runny nose. Ingested cocaine can cause severe bowel gangrene, due to reduced blood flow. Persons who inject cocaine have puncture marks called "tracks," most commonly in their forearms, and may experience allergic reactions, either to the drug or to some additive in street cocaine, which in severe cases can result in death. Many chronic cocaine users lose their appetite and experience significant weight loss and malnourishment.

Physical effects

Cocaine is bad for the heart. Cocaine increases heart rate and blood pressure while constricting the arteries supplying blood to the heart. The result can be a heart attack, even in young people without heart disease. Cocaine can also trigger a deadly abnormal heart rhythm called arrhythmia. Cocaine can constrict blood vessels in the brain, causing strokes. This can happen even in young people without other risk factors for strokes. Cocaine causes seizures and can lead to bizarre or violent behavior.

Snorting cocaine damages the nose and sinuses. Regular use can cause nasal perforation. Smoking crack cocaine irritates the lungs and, in some people, causes permanent lung damage.
Cocaine constricts blood vessels supplying the gut. The resulting oxygen starvation can cause ulcers, or even perforation of the stomach or intestine. Although cocaine has a reputation as an aphrodisiac, it actually may make you less able to finish what you start. Chronic cocaine use can impair sexual function in men and women. In men, cocaine can cause delayed or impaired ejaculation.

Psychological treatment options

Psychological treatments help patients engage in the treatment process, modify their attitudes and behaviors related to drug abuse, and increase healthy life skills. These treatments can also enhance the effectiveness of medications and help people stay in treatment longer. Treatment for drug abuse and addiction can be delivered in many different settings using a variety of behavioral approaches.

Some programs also offer other forms of behavioral treatment such as:

Cognitive–behavioral therapy, which seeks to help patients recognize, avoid, and cope with the situations in which they are most likely to abuse drugs.

Multidimensional family therapy, which was developed for adolescents with drug abuse problems—as well as their families—addresses a range of influences on their drug abuse patterns and is designed to improve overall family functioning.

Motivational interviewing, which capitalizes on the readiness of individuals to change their behavior and enter treatment.

Medical Treatment options

Currently, there are no FDA-approved medications for treating cocaine addiction; thus, developing a medication to treat cocaine and other forms of addiction remains one of NIDA’s top research priorities. Researchers are seeking to develop medications that help alleviate the severe craving associated with cocaine addiction, as well as medications that counteract cocaine-related relapse triggers, such as stress. Several compounds are currently being investigated for their safety and efficacy, including a vaccine that would sequester cocaine in the bloodstream and prevent it from reaching the brain. Current research suggests that while medications are effective in treating addiction, combining them with a comprehensive behavioral therapy program is the most effective method to reduce drug use in the long term. There are no medications currently available recommended by the FDA. Consequently, NIDA is aggressively pursuing the identification and testing of new cocaine treatment medications. Several newly emerging compounds are being investigated to assess their safety and efficacy in treating cocaine addiction.

In 1999 a promising anti-cocaine drug medications, selegeline, was being taken into multi-site phase III clinical trials . These trials showed two innovative routes of selegeline administration: a transdermal patch and a time-released pill, to determine which is most beneficial. Disulfiram, a medication that has been used to treat alcoholism, has also been shown, in clinical studies, to be effective in reducing cocaine abuse.

More recently, in 2011, a team of researchers Xiaoyun Shen, Frank M. Orson, and Thomas R. Kosten were able to successfully develop and anti-addiction vaccine and conduct some clinical trials as well. As per them, "Anti-addiction vaccines can produce the antibodies to block the effects of these drugs on the brain, and have great potential to ameliorate the morbidity and mortality associated with illicit drug intoxications" However there were some challenges that were experienced during the course of this development. Clinical trials of cocaine and nicotine vaccines so far have reported modest efficacy. The abstinence rates among those vaccinated against nicotine have been no better than placebo overall, but the rates have been superior to placebo in the third who achieved therapeutic antibody levels.

Pychological Treament

Many behavioral treatments have been found effective for cocaine addiction, including both residential and outpatient approaches. Indeed, behavioral therapies are often the only available effective treatment for many drug problems, including cocaine addiction. However, integration of both pharmacological and behavioral treatments may ultimately prove to be the most effective approach. Disulfiram (a medication that has been used to treat alcoholism), in combination with behavioral treatment, is effective in reducing cocaine abuse. It is important that patients receive services that match all of their treatment needs. For example, if a patient is unemployed, it may be helpful to provide vocational rehabilitation or career counseling. Similarly, if a patient has marital problems, it may be important to offer couples counseling. A behavioral therapy component that may be particularly useful for helping patients achieve initial abstinence from cocaine is contingency management. Some contingency management programs use a voucher-based system to give positive rewards for staying in treatment and remaining cocaine-free.

Cognitive-behavioral treatment is a focused approach to helping cocaine-addicted individuals abstain—and remain abstinent—from cocaine and other substances. The underlying assumption is that learning processes play an important role in the development and continuation of cocaine abuse and dependence. The same learning processes can be employed to help individuals reduce drug use and successfully cope with relapse. This approach attempts to help patients recognize the situations in which they are most likely to use cocaine, avoid these situations when appropriate, and cope more effectively with a range of problems associated with drug abuse. This therapy is also noteworthy because of its compatibility with a range of other treatments patients may receive, such as pharmacotherapy.

Therapeutic communities (TCs), or residential programs with stays of 6 to 12 months, offer another alternative to those in need of treatment for cocaine addiction. TCs focus on resocialization of the individual, and can include on-site vocational rehabilitation and other supportive services. Of course, there is variation in the types of therapeutic processes offered in TCs.

Related drugs

Cocaine acts as a stimulant, so various amphetamines are closely related.

Related synthetics

A number of synthetic derivatives of cocaine have been investigated as potential pharmaceutical agents (e.g. 4-fluorococaine and 2-hydroxycocaine), but only two have been reported as potential substances of misuse, namely 3-(p-fluorobenzoyloxy) tropane, pFBT and dimethocaine. Both are available as ‘research chemicals’ from retail websites or have been identified in ‘legal highs’ products.

The structure of pFBT is closely related to that of cocaine, however dimethocaine lacks a tropane ring and more closely resembles the structure of procaine, a local anaesthetic drug without psychoactive properties. There is therefore some doubt as to whether dimethocaine itself has psychoactive effects in humans. Neither substance is under international control, and apart from Denmark (pFBT) and Romania (dimethocaine) there are no national controls in the European Union.

References

[1] http://www.drugabuse.gov/drugs-abuse/cocaine
[2] http://www.sciencedirect.com/science/article/pii/0378874181900635
[3] http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(07)60464-4/fulltext
[4] http://www.webmd.com/drugs/drug-1383-cocaine+top.aspx?drugid=1383&drugname=cocaine
[5] http://www.justice.gov/dea/concern/cocaine.html
[6] http://www.cedro-uva.org/lib/cohen.cocaine.html
[7] http://www.webmd.com/mental-health/cocaine-use-and-its-effects
[8] http://www.emcdda.europa.eu/publications/drug-profiles/synthetic-cocaine-derivatives
[9] http://www.tdpf.org.uk/WHOleaked.pdf
[10] http://www.scienceblog.com/community/older/1999/A/199900322.html
[11] http://www.emcdda.europa.eu/topics/cocaine
[12] http://www.cocainewithdrawalsymptoms.net/
[13] Anti-addiction vaccines by Thomas R. Kosten et al
[14] http://www.psychologytoday.com/conditions/cocaine?tab=Treatments