Cocaine was used in surgery


CocaineDrug groupsLocal anesthetics Cocaine is an alkaloid found in the leaves of the coca bush Erythroxylum coca. It was used primarily as a local anesthetic in the past. At present, there are no longer any drugs containing cocaine on the market in Switzerland; the corresponding preparations must be made in a pharmacy. Because of its stimulating and euphoric effects, cocaine is mainly abused as an intoxicant. As such, it leads to numerous undesirable effects and addiction.

synonymous: Kokain, Cocainum, Cocaini hydrochloridumPhEur, Cocainhydrochlorid

Products

In Switzerland there are currently no more finished medicinal products containing cocaine on the market. However, they can be prepared as a magistral prescription in a pharmacy. Cocaine is subject to the Narcotics Act and requires a more stringent prescription, but is not prohibited as a medicinal product. It is also sold on the black market as an illegal intoxicant, often stretched and contaminated.

In 2020, the nasal solution Numbrino® with cocaine hydrochloride was approved as a local anesthetic for the nasal mucosa in the USA. The drug is intended for diagnostic and surgical uses.

Structure and properties

Cocaine (C.17H21NO4, Mr = 303.4 g / mol), like the alkaloids of the nightshade family, belongs to the tropane alkaloids. Cocaine hydrochloride is a white, crystalline powder or colorless crystals. It is very easily soluble in water and easily soluble in ethanol 96%. It melts at 197 ° C with decomposition.

Parent plant

Cocaine is a natural substance that comes from the → leaves of the coca bushErythroxylum sp. (Family Erythroxylaceae) is obtained. The medicinal drug is called Cocae folium (coca leaf). The coca bush is native to South America. See also under → Coca leaves.

Manufacturing

Cocaine is mainly produced illegally in South America, including Peru, Colombia, Ecuador and Bolivia. To do this, the leaves are extracted with a solvent (kerosene) and hydrochloric acid. The end product is usually the salt cocaine hydrochloride.

Preparations
  • The older pharmacopoeias contain some preparations such as Vinum cocae (CocaweinPH 5) or Extractum Cocae fluidum PH 4, PH 5.
  • Cocaine eye drops
  • Coca-Cola® still contains an extract from coca leaves, from which the cocaine has been removed.
  • Freebase is the deprotonated (alkaline) and smokable form of cocaine. To do this, a base (ammonia) is added to an aqueous solution of cocaine hydrochloride and the mixture is extracted with ether. Disadvantage: residues of ether make it flammable (risk of burns when smoking).
  • Like Freebase, crack is the deprotonated form of cocaine. To this end, soda (sodium hydrogen carbonate) is added to an aqueous solution of cocaine hydrochloride. After drying, a white mass is created that can be smoked or inhaled (film smoking).
Effects

"Some laboratory animals, if given a choice, will ignore food and keep taking cocaine until they starve" (Nestler, 2005)

The effects come on quickly and usually only last for a short time. Cocaine has a short half-life of around 1.5 hours.

Mechanism of action

The dopaminergic effect of cocaine on the nucleus accumbens of the limbic system seems to be of central importance for euphoria and the arousal of addiction. Cocaine induces a high and a strong memory of how it came about (people, places, associated things). This leads to a strong desire and later an obligation to repeat the intake. Cocaine increases the concentration of neurotransmitters in the synaptic cleft by inhibiting their reuptake (e.g. dopamine, norepinephrine, serotonin).

Medical indications

For local anesthesia and vasoconstriction, for example of the nasal mucosa.

abuse

As a stimulant intoxicant, stimulant, party drug and smart drug.

dosage

Cocaine can be snorted, injected or taken orally as an intoxicant. It is well absorbed through the mucous membranes. It can also be smoked, but not as cocaine hydrochloride, as this decomposes when heated. To do this, it must first be converted into the free base by deprotonation (crack or freebase, see above). Due to the short duration of action, the application is often repeated. Cocaine is often combined with other intoxicants, such as alcohol or heroin.

unwanted effects

Acute and chronic adverse effects (abuse):

  • Habituation, strong dependency, addiction, craving
  • Sleep disorders up to absolute insomnia, excitement, compulsion to speak, irritability, fear, exhaustion, aggressiveness, disorientation, hallucinations, convulsions, tremors, depression, hyperactivity, psychoses, obsessive-compulsive disorders, mania, paranoia, paranoia, hyperthermia, delirium, rhabdomyolysis, unconsciousness, death
  • Cognitive disorders (decision making, problem solving, abstract thinking)
  • Cardiovascular toxicity: chest pain, prolongation of the QT interval, arrhythmias, vasoconstriction, rapid pulse, high blood pressure, myocarditis, cardiac ischemia, angina pectoris, myocardial infarction, sudden death
  • Airways: bronchial constriction, worsening asthma, burns, alveolar bleeding, dyspnoea, respiratory depression, respiratory arrest
  • Nose: perforation of the nasal septum
  • Eyes: dilated pupils
  • Gastrointestinal tract: poor appetite, intestinal ischemia, nausea and vomiting
  • Other undesirable effects from impurities and additives, such as local anesthetics, talc, sugar, quinine, strychnine.
see also literature
  • Carrera M.R., Meijler M.M., Janda K.D. Cocaine pharmacology and current pharmacotherapies for its abuse. Bioorg Med Chem. 2004, 12 (19), 5019-30 Pubmed
  • Farrar H.C., Kearns G.L. Cocaine: clinical pharmacology and toxicology. J Pediatr, 1989, 115 (5 Pt 1), 665-75 Pubmed
  • Freud S. On Coca. Centralbl Ges Ther, 1884, 2, 289-314
  • Goldstein R.A., DesLauriers C., Burda A.M. Cocaine: history, social implications, and toxicity - a review. Dis Mon. 2009, 55 (1), 6-38 Pubmed
  • Nestler E.J. The neurobiology of cocaine addiction. Sci Pract Perspect. 2005, 3 (1), 4-10 Pubmed
  • Karch S.B. A brief history of cocaine. Boca Ration: CRC / Taylor & Francis, 2006
  • Pendergrast M. For god, country, and Coca-Cola: the definitive history of the great American soft drink and the company that makes it. New York: Basic Books, 2000
author

Conflicts of Interest: None / Independent. The author has no relationships with the manufacturers and is not involved in the sale of the products mentioned.

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This article was last changed on February 20, 2021.
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