Disorders from cocaine use in our society are increasing. Studies have been done that show that 5.9% of people between 15 and 64 have used at some time in their life and 2.7% have used cocaine in the last year.
In our country, cocaine, together with heroin, is the second or third most consumed drug among some drug addicts. Disorders due to cocaine use develop due to their ability to recapture catecholamines and serotonin from the synaptic cleft to the presynaptic termination.
As a consequence of its action, these substances accumulate in the synaptic cleft triggering the corresponding effects.
Although consumption is increasing, acute poisonings are rare. Poisonings usually appear due to a mixture of substances, since consumers prefer to take this drug with other substances, such as alcohol, with the appearance of different disorders due to cocaine use.
What is cocaine?
Cocaine is an active ingredient that is extracted from a plant grown in South America called coca. It has been the popular drug of the 80s and 90s. However, it is not a new drug but it has been known for more than 100 years. Currently, its consumption is illegal.
This drug is a very addictive stimulant that directly affects the brain. As we have already said, it is extracted from the leaves of the coca plant of the genus Erythroxylum. In addition, there are two chemical forms of cocaine that are usually consumed: the hydrochloride salt and the cocaine or base crystals.
The first, salt, is in the form of white and odorless powder and is consumed either injected or inhaled. At first, it was used for medical purposes as a local anesthetic. Afterward, the disorders due to use and its toxicity were observed and it was no longer used in a sanitary way.
As for the drug crystals or “crack”, they are processed with ammonia or sodium bicarbonate and water. Then they are heated to remove the hydrochloride and produce the substance that can be smoked.
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Toxicokinetics of cocaine
To know the toxicity of this drug we must divide it into four processes: absorption, distribution, metabolism, and elimination.
Absorption
The absorption will depend on the route of administration. If it is administered orally / inhalatively, it will present an absorption of 30-40%, being more likely to cause disorders due to use. If smoked cocaine is taken, the absorption decreases up to 10-20%.
After an inhaled dose, the effects are observed after 3 minutes and the maximum peak in blood is reached around 15 minutes. The effects at brain level are very fast, about 5-30 seconds, and last approximately 5-10 minutes.
Distribution
Cocaine is widely distributed throughout the body and can cross the blood-brain barrier, which protects the brain. Due to its high liposolubility, it accumulates in the lipid tissues and in the central nervous system.
It crosses the placenta by simple diffusion (the type of transport in the body that does not require energy). If administered chronically, it can accumulate in the fetus. On the other hand, the half-life depends on the route of administration, the dose, and interindividual variability.
Metabolism
It is mainly metabolized in the liver after having passed 2 hours after administration. There are 3 biotransformation routes. The first is carried out by the cholinesterase enzymes of the liver, plasma, and brain producing metabolites such as benzoylecgonine, ecgonine methyl ester, and ecgonine.
The second route is spontaneous hydrolysis in which no enzyme intervenes. And the last N-demethylation producing the metabolite norcocaine.
Elimination
The metabolites formed in the previous phase are mostly excreted through the urine. From 1 to 9% are eliminated without modification with a higher proportion if the urine is acidic. This is because free cocaine is a weak base and will dissolve better without urine being acidic.
In addition to urine, it can also be eliminated in saliva or through feces. After 4 hours most of the drug has been removed from the plasma. However, certain metabolites may persist up to 144 hours after administration.
Disorders due to cocaine use
Overdoses of this substance cause symptom related to:
- Adrenergic activity: cardiovascular complications, hypertension, tachycardia, and hyperthermia.
- Central activity: euphoria, restlessness, hallucinations.
- Digestive disorders : nausea and vomiting.
- Respiratory disorders : respiratory depression.
In addition, several psychiatric cocaine use disorders have been described, such as major depressive disorder, bipolar disorder type II, cyclothymic disorder, anxiety disorder and antisocial personality disorder.
On the other hand, the long-term effects are similar to those of amphetamines although they tend to be more serious. Highlights the effects on the fetus during pregnancy and high mortality, mainly caused by cerebral hemorrhages or heart failure.
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