The popularity of cocaine as a drug of misuse

In the late 1970s the use of cocaine by championship athletes associated the drug with manliness and power.  Cocaine became the media’s powdery star with stories of its use by the famous, its increasing expense and its description as the caviar or champagne of drugs.  In July 1981 Time magazine showed a champagne glass full of sparkling white powder with the headline “HIGH ON COCAINE- a drug with status- and menace”.  The net effect of the article was a positive and alluring image of cocaine.  In New York magazine (1978) cocaine was referred to as “the drug of choice” and “every bit as enjoyable as Freud claimed”1. Cocaine is God’s way of telling you that you’ve made too much money.” –Manager of a rock ‘n’ roll band 3.

An Extremely Addictive Drug4

Cocaine is highly addictive - once a person has used cocaine the urge to use it again is almost irresistible, and in this respect it is one of the most insidious 'recreational' drugs around. However, despite the feelings of overwhelming ecstasy it brings, cocaine never produces satisfaction. The user is left with an overwhelming craving to experience the joy of cocaine over and over again, which leads to tolerance and an ever-increasing dose. Laboratory research has shown that given an option, animals prefer cocaine to food, water and even sex. If given free access to it, they continue to take the drug until they overdose and die. The same, unfortunately, is true for humans as well. For this reason cocaine is classified as an illegal substance in most countries of the world.

The combination of cocaine with alcohol is substantially more toxic than either substance on their own

Twelve million Americans combine ethanol with cocaine to produce a pronounced and prolonged euphoria.  However it is known that the combination of these to drugs is substantially toxic.  This may be a result of cocaethylene, detected in the serum of emergency patients.  Cocaethylene is a cocaine metabolite, formed in the liver only in the presence of ethanol.  It is pharmacologically active and depresses the myocardium causing cardiotoxicity8. The cardiovascular effects of cocaine are complex.  These include sympathomimetric and local anesthetic effects.  Low doses of cocaine cause the sympathomimetric effects to predominate, but tolerance develops.  Whereas for high doses the local anesthetic effects predominate causing potential cardiovascular collapse and sudden death.

Strategy for the treatment of cocaine abuse

Improvements in the treatments for drug abuse are continually improving.  For twenty-five years methadone was the only treatment for opiate dependence9.  Now LAAM, buprenorphine and naloxone are being used as treatments9.  Similarly for alcohol dependence, disulfiram, nactrexone and shortly amprosate are prescibed9.  However the treatment of cocaine abuse poses a more difficult challenge for addition pharmacotherapy.  Potential treatments in the future may be based on immunopharmacotherapeutic agents that can suppress the effect of cocaine on behavioral and locomotive actions.  A second-generation vaccine also protects against the psychoactive effects of cocaine10. Similarly a catalytic monoclonal antibody (mAB) is under development to bind and degrade cocaine-by hydrolysing the benzoate ester of cocaine11.

The actual mechanism whereby cocaine produces euphoria is still unknown.  Sigma 1 receptors are unique endoplasmic reticulum proteins that bind certain steroids, neuroleptics and psychotropic drugs.  Sigma 1 receptors form a trimeric complex with ankyrin B and IP2Rtype 3 in NG-108 cells, which regulate Ca2+ signaling and may represent an active site for the binding of cocaine and neurosteroids12.  

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