Cocaine
Dr. Joseph E. Graas, Scientific Director
Dr. Edward Moore, Medical Director
Dr. Paul Robandt, Scientific Director
Cocaine is a powerful plant alkaloid obtained from the Erythroxylum plant genus. When ingested it has remarkable stimulant and euphoric qualities. The plant is cultivated largely in South America and southern Mexico, and cocaine comprises 0.25 to 0.77% of the leaves.1 Cocaine is extracted from the leaves of the plant by a solvent process or an acid process, then the extract is treated with dilute sulfuric acid to produce a paste of cocaine sulfate. The paste is then treated with an oxidizing agent and hydrochloric acid to precipitate cocaine hydrochloride from the solution.2
The cocaine alkaloid was first isolated by Fredrich Gaedcke in Germany in 1885. Through the late 1800s cocaine was medicalized due to its anesthetic and euphoric qualities. In 1879 cocaine was even used to treat morphine addiction. Sigmund Freud published his work on cocaine in 1884, initially interested in its medical qualities.3 In 1885, Parke-Davis was selling cocaine in various forms including cigarettes, powder and an injectable form that included a needle. It is also true that the Coca-Cola company included cocaine in their original preparation of the popular soft drink but discontinued its use in 1903.
Cocaine is an effective local anesthetic and a vasoconstrictor, rendering it useful for surgical procedures for the mouth and nose. For this reason, cocaine is a Schedule II narcotic on the Drug Enforcement Agency (DEA) list and sees limited use in the medical community.
Non-medical ingestion of cocaine hydrochloride can be via insufflation, injection or orally. In the mid-1980s, a method to extract the free base of cocaine with baking soda became popular in the US, allowing users to smoke the drug and feel the results almost as rapidly as injecting the hydrochloride. The free-base form was nicknamed “crack” for the crackling sound it made when heated in a smoking apparatus.
Cocaine is the second-most abused illegal drug after marijuana.4 Cocaine acts by inhibiting the reuptake of serotonin, norepinephrine and dopamine. The reward aspect of the euphoria and feeling of well-being it causes can lead to addiction, even after a short period of use. It is also a central nervous system stimulant, causing users to be alert, show more motor activity and have more energy.
Cocaine use increases the risk of stroke, myocardial infarction and sudden cardiac death. Due to its effects on the heart and circulatory system, cocaine is sometimes referred to as the “heart-attack drug”.5 Lung and oral problems may also present in those who smoke crack. Constant pursuit of a cocaine “high” can disrupt the lifestyles and families of cocaine users. Withdrawal from cocaine can leave the user fatigued, depressed, unable to feel pleasure and perhaps with suicidal thoughts or actions.
Cocaine is rapidly and extensively metabolized in the liver and plasma by cholinesterase enzymes. Only about 1% of the dose is excreted unchanged in the urine. The primary metabolites measured in urine are benzoylecgonine (BE) and ecgonine methyl ester. Hydroxylated metabolites are produced in minor amounts and may be of interest from a forensic standpoint, as they are not produced in vitro (as BE can be). BE is generally detectable by most drug tests for approximately 2-4 days after ingestion. Screening immunoassays are remarkably accurate for BE as the plant alkaloid and its metabolites are unique in nature. Confirmation may be performed by GC/MS or LC/MS/MS.
References
- Plowman, T; Rivier L (1983). Cocaine and Cinnamoylcocaine content of thirty-one species of Erythroxylum (Erythroxylaceae). Annals of Botany. London. 51: 641–659.
- Drug Enforcement Administration, Microgram Bulletin Vol. XXXVI, No. 2, February 2003
- “Über Coca” Von Dr. Sigm. Freud, house officer of the General Hospital of Vienna. Centrallblatt für die ges. Therapie. 2, 289-314, July 1884
- Karila, L; Zarmdini, R; Petit, A; Lafaye, G; Lowenstein, W; Reynaud, M (January 2014). Cocaine addiction: current data for the clinician. Presse Médicale. 43 (1): 9–17.
- Figtree, G.A., et. al., PLOS One, (April 2014), Regular Cocaine Use Is Associated with Increased Systolic Blood Pressure, Aortic Stiffness and Left Ventricular Mass in Young Otherwise Healthy Individuals.