Products
In many countries, finished medicines containing cocaine are currently no longer commercially available. However, they can be prepared as an extemporaneous prescription in a pharmacy. Cocaine is subject to the Narcotics Act and requires an aggravated prescription, but it is not banned as a drug. It is also sold as an illegal narcotic on the black market, often cut and contaminated. In 2020, Numbrino nasal solution containing cocaine hydrochloride was approved in the U.S. as a local anesthetic for the nasal mucosa. The drug is intended for diagnostic and surgical applications.
Structure and properties
Cocaine (C17H21NO4, Mr = 303.4 g/mol) belongs to the tropane alkaloids, as do the alkaloids of the nightshade family. Cocaine hydrochloride is a white crystalline powder or colorless crystals. It is very soluble in water and slightly soluble in ethanol 96%. It melts at 197 °C with decomposition.
Stem plant
Cocaine is a natural substance extracted from the leaves of the coca bush sp. (family Erythroxylaceae). The medicinal drug is called cocae folium (coca leaf). The coca shrub is native to South America. See also under coca leaves.
Production
Cocaine is mainly produced illegally in South America, including Peru, Colombia, Ecuador, and Bolivia. This is done by extracting the leaves 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 (coca wine PH 5) or Extractum cocae fluidum PH 4, PH 5.
- Cocaine eye drops
- Coca-Cola still contains an extract of coca leaves, but the cocaine has been removed.
- Freebase is the deprotonated (alkaline) and smokable form of cocaine. For this purpose, an aqueous solution of cocaine hydrochloride is mixed with a base (ammonia) and extracted with ether. Disadvantage: residues of ether make it flammable (risk of burns when smoking).
- Crack is like Freebase the deprotonated form of cocaine. For this purpose, sodium bicarbonate (sodium hydrogen carbonate) is added to an aqueous solution of cocaine hydrochloride. After drying, a white mass is formed, which can be smoked or inhaled (foil smoking).
Effects
“Some laboratory animals, if given a choice, will ignore food and keep taking cocaine until they starve” (Nestler, 2005).
- Stimulant (stimulating, performance-enhancing).
- Euphoric, dysphorizing
- Local anesthetic (analgesic)
- Vasoconstrictive (vasoconstrictive)
- Sympathomimetic
- Dopaminergic
- Serotoninerg
- Appeitite inhibitory
- Psychotropic
- Aphrodisiac
- Highly addictive, especially when smoked
- Teratogenic
Effects occur rapidly and usually last only a short time. Cocaine has a short half-life of about 1.5 hours.
Mechanism of action
The dopaminergic action of cocaine at the nucleus accumbens of the limbic system appears to be central to the euphoria and arousal of addiction. Cocaine leads to a high and a strong memory of how it came to be (people, places, associated things). This develops into a strong desire and later a compulsion to repeat the ingestion. 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 perorally as an intoxicant. It is well absorbed through mucous membranes. It can also be smoked, but not as cocaine hydrochloride because it decomposes when heated. It must first be converted to the free base by deprotonation (crack or freebase, see above). Because of the short duration of action, the application is frequently repeated. Cocaine is often combined with other narcotics, such as alcohol or heroin.
Adverse effects
Acute and chronic adverse effects (abuse):
- Habituation, severe dependence, addiction, craving.
- Sleep disturbances to absolute insomnia, agitation, compulsive talking, irritability, anxiety, exhaustion, aggressiveness, disorientation, hallucinations, convulsions, tremors, depression, hyperactivity, psychosis, obsessive-compulsive disorder, mania, paranoia, paranoia, hyperthermia, delirium, rhabdomyolysis, unconsciousness, death
- Cognitive disorders (decision making, problem solving, abstract thinking).
- Cardiovascular toxicity: chest pain, QT interval prolongation, arrhythmias, vasoconstriction, rapid pulse, hypertension, myocarditis, cardiac ischemia, angina, myocardial infarction, sudden death
- Respiratory: bronchoconstriction, worsening of asthma, burns, alveolar hemorrhage, respiratory distress, respiratory depression, respiratory failure
- Nose: perforation of the nasal septum.
- Eyes: pupil dilation
- Gastrointestinal tract: lack of appetite, intestinal ischemia, nausea and vomiting.
- Other adverse effects due to impurities and additives, such as local anesthetics, talc, sugar, quinine, strychnine.
