Cocaine
 NAME OF DRUG: Cocaine |
| PHYSICAL CHARACTERISTICS: Cocaine is a white crystalline powder. It is slightly volatile and slightly soluble in water. |
| DOSAGE/OCCURRENCE/USAGE: Cocaine is one of the strongest naturally occurring central nervous system stimulants. It is a alkaloid found in the plant Erythroxylon coca which originated in the northern South American Andes. The leaves are harvested and dried then are converted to coca paste which is eventually used to make cocaine hydrochloride. It takes about 100 kg of coca leaves to produce 800 g of cocaine. Since it was first isolated in 1855, it has been widely used in medicine as a local anesthetic. It is used by drug abusers for its stimulant properties. Its medical use is limited to topical application as a local anesthetic in ear, nose, and throat surgery in 10-20% solutions and in ophthalmological procedures in a 1-4% solution. Abusers commonly administer the hydrochloride by nasal insufflation, intravenous injection, or by smoking the free base in doses of 10-120 mg. |
| BLOOD CONCENTRATIONS VS. DOSAGE: Nine subjects who had each been given an intr-nasal dose of 1.5 mg/kg (equivalent to a surgical dose) had peak plasma cocaine concentrations of 120-470 ng/mL after one hour. Subjects who were given 16 mg of cocaine intravenously produced concentrations of 90-310 ng/mL within 5 minutes. Four subjects who had been given an oral dose of 2 mg/kg produced peak plasma cocaine concentrations of 100-420 ng/mL in 50-90 minutes. The average concentration was 160 ng/mL at one hour. |
| URINE EXCRETION RATE: About 1-9% (depends on urine pH) of a dose is excreted as the unchanged drug, 35-54% as benzoylecgonine, and 32-49% as ecgonine methyl ester. After a 1.5 mg/kg intranasal dose the concentration of cocaine averaged 6700 ng/mL during the first hour then dropped to undetectable levels by 12 hours. The benzoylecgonine concentrations reached an average peak level of 52000 ng/mL during the 4-8 hour period. It dropped slowly to an average of 400 ng/mL for the 48-72 hour collection period. |
| METABOLITES: benzoylecgonine, ecgonine methyl ester |
| TOXICITY: Symptoms of chronic cocaine use include psychiatric disturbances, rhinitis with possible nasal septum perforation, shortness of breath, cold sweats, tremors, violent protective behavior, distorted perception, tachycardia, tachypnea, dyspnea, and hyperkinetic behavior. Signs of cocaine intoxication can include profound CNS stimulation with psychosis and repeated grand mal convulsions, ventricular arrhythmias, respiratory dysfunction with Cheyne-Stokes breathing, respiratory paralysis, hyperthermia, and even coma. Death from cocaine intoxication can occur from doses as low as 30 mg (1-3 lines) in sensitive persons. However, 1.2 g is considered to be the minimum lethal dose. Many addicts can tolerate higher doses, up to 5 g/day, due to physiological tolerance form chronic daily use. Blood concentrations of cocaine after an overdose are variable due to dose, route of administration, period of survival, and instability of the drug. |
| REFERENCES: Baselt, R C. Disposition of Toxic Drugs and Chemicals
in Man, Second Edition. Davis, Calif.: Biomedical Publications, 1982. Clarke, E.G.C. Isolation and Identification of Drugs. London: The Pharmaceutical Press, 1969. Caplan, Yale H. Cocaine Abused Drugs Monograph Series. Ed. Caplan, Yale H. Irving: Abbott Laboratories, 1994. |