Cocaine

Cocaine is a white powder. It can be snorted up the nose or mixed with water and injected with a needle. Cocaine can also be made into small white rocks, called crack. Crack is smoked in a small glass pipe.

Indication

For the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

Pharmacodynamics

Cocaine is a local anesthetic indicated for the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

Mechanism of action

Cocaine produces anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. This is achieved by reversibly binding to and inactivating sodium channels. Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. Cocaine is the only local anesthetic with nonconstructive properties. This is a result of its blockade of nor epinephrine re uptake in the autonomic nervous system. Cocaine binds differentially to the dopamine, serotonin, and nor epinephrine transport proteins and directly prevents the re-uptake of dopamine, serotonin, and nor epinephrine into pre-synaptic neurons. Its effect on dopamine levels is most responsible for the addictive property of cocaine.

Absorption

Cocaine is absorbed from all sites of application, including mucous membranes and gastrointestinal mucosa. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed

Metabolism

Hepatic. Cocaine is metabolized to benzoylecgonine and ecgonine methyl ester, which are both excreted in the urine. In the presence of alcohol, a further active metabolite, coca ethylene is formed, and is more toxic then cocaine itself.

• Cocaine  norcocaine
• Cocaine  Benzoylecgonine
• Cocaine Cocaethylene