Cathinones
Cathinones is a narcotic substance that can be obtained from an evergreen plant of the Berescletaceae family.
Kata leaves are grown mainly in the Arabian Peninsula and in the Northeastern part of Africa.
The narcotic effect is achieved by chewing fresh shoots or drinking their decoction.
The narcotic effect of cathinone lasts for several hours.
The feeling after consumption is a moderate feeling of elation, excitement, and a surge of energy. In parallel, there is a decrease in appetite and a dulling of pain.
Is it possible to become addicted to cathinones?
Cat is a plant that contains substances with an amphetamine-like effect, but weaker and less lasting. Its intoxicating effect is achieved by chewing the leaves of a plant or shrub of the Catha edulis family. They are also brewed and drunk as a decoction of tea.
In natural conditions, the plant reaches a height of 5-8 meters, a length of 5-10 cm and a width of 1-4 cm. These varieties of trees and shrubs are mainly native to the Arabian Peninsula and Northeast Africa.
Kata chewing is especially common in Yemen, Somalia, Ethiopia, Kenya, Madagascar, Tanzania, and Sudan. According to statistics, men are addicted to the use of cathinones three times more often than women.
In Russia, khat is equated with drugs. Due to the fact that the plant contains euphoric substances cathinone, katine and norephedrine, its import and use in the territory of the Russian Federation for non-medical purposes is prohibited by law.
Is it a drug or a relaxant?
This topic is still being actively discussed in the scientific world. In many countries, kata leaves and stems are still an inexpensive and legal commodity. There, chewing natural raw materials is equivalent to drinking coffee. Its use is an essential attribute of friendly meetings. The substance is also actively marketed as a weight loss product.
In many more progressive countries, this raw material is equated to amphetamine and is prohibited for use. The abuse of the hard hat is becoming an economic and social problem in these States, especially among immigrants from the aforementioned areas.
How are cathinones used?
Fresh leaves and young shoots of the plant are consumed by chewing them for several hours. At this time, only the juice is swallowed, and the coarse fibers are spat out. The absorption of cathinone and cathine from the plant occurs mainly through the oral mucosa, the rest through the intestines. A typical dose of intoxication is usually 100-200 g of kata leaves.1 g of fresh and young leaves contains on average 1 mg of cathinone, 0.9 mg of cathine and 0.5 mg of norephedrine. But such data is quite approximate because the leaves have a different effect depending on how they are stored and how fresh they are.
What are the consequences of using kata?
The main effect is a moderate feeling of elation, increased awareness and pleasant excitement. A person feels more energetic, gains a sense of well-being, and becomes talkative and sociable. There is also an effect of increased self-esteem, increased self-confidence and a sense of emotional uplift.
Chewing kata gives a false sense of abundance and grandeur. The feeling of time and space is distorted. There is an improvement in mood and a feeling of lightness. It is due to such sensations that the substance is addictive.
High doses of cathinone provoke:
Hyperactivity and, in some cases, manic behavior.
Psychoses (mental illnesses) that include manic behavior.
Paranoid thoughts and aggression.
Most of the patients with these reactions were foreigners from the United Kingdom and the United States who had tried the drug in their homeland.
What side effects does the use of cathinones cause?
Increased activation of the nervous system causes rapid heartbeat and increased blood pressure.
Large pupils, bloodshot eyes, and a distant look are signs of an overdose.
People who abuse cat have an increased risk of thrombosis.
There are problems with the work of the heart.
Cathinone addicts are often thin-looking or even physically exhausted people. This is because the substance significantly reduces appetite.
Studies show that cat affects reproductive function in men and gets into breast milk of a nursing woman.
Cata users often have gum and esophageal inflammation, dental diseases, and constipation.
A brownish discoloration of the oral cavity is a sign of chronic kata use.
Withdrawal symptoms after prolonged use of kata are often mild. It can be lethargy, trembling, anxiety and depression.
The effect of the substance on the ability to drive a car has not been thoroughly studied.
Designer drugs: synthetic cathinones.
The cathinones extracted from the cat plant (Catha edulis) have been used by humans for recreational purposes for many centuries. Chewing the leaves and green shoots of this plant causes a euphoric effect similar to that of amphetamines. In 2006, there were 10 million consumers of kata in the world.
The list of synthetic cathinones is quite large: These include butylone, dimethylclathinone, etcathinone, ethylene, 3- and 4-fluromethcathinone, mephedrone, methedrone, methylenedioxypyrovaleron (MDPV), methylone and pyrovaleron.
Butylon is the only cathinone derivative that is used for medical reasons in the United States and European countries. The first synthetic cathinone, methcathinone– was created in 1928. Metcathinone was previously used in Russia as an antidepressant. In 1988, the UN listed the cathinones in List 1, and in 1993, the United States did the same. Another type of synthetic cathinone, mephedrone, appeared in the USA in 2009; it came from Europe.
The appearance of so-called “bath salts” has led to an increase in the number of poisoning cases, and in some cases their use has been fatal. For example, in the first six months of 2011, the American centers for poisons and poisoning received more phone calls in connection with the use of narcotic drugs than in the whole of 2010. The number of seizures caused by synthetic cathinones increased from 14 in 2009 to 290 in 2010. In September 2011, the US authorities added three synthetic cathinones to List 1 (mephedrone, methylone and MDPV).
Pharmacology / Pharmacokinetics
Information on the pharmacokinetics and pharmacodynamics of synthetic cathinones is rather limited. As you know, the traditional stimulant contained in kata has undergone changes in order to create many analogues of synthetic cathinones, in which minor biochemical substitutions in the “mother” molecule resulted in a new class of drugs with a wide range of potency. Synthetic cathinones belong to beta-ketophenethylamines, which are structurally similar to amphetamines. However, cathinone derivatives are more hydrophilic, which reduces their ability to cross the blood-brain barrier and makes them less potent than amphetamines. Some authors believe that due to the peculiarities of the chemical structure, cathinones can exhibit cellular toxicity through their incorporation into DNA. Scientific studies also show that cathinone, mephedrone, methcathinone, and methylone strongly inhibit the reuptake of dopamine, serotonin, and norepinephrine. Pyrovaleron suppresses the reuptake of norepinephrine and dopamine, but has little effect on the reuptake of serotonin. Pyrovaleron is 9 times more powerful than cocaine in suppressing dopamine reuptake, and 13 times more powerful than cocaine in suppressing norepinephrine reuptake.
According to consumers, a typical dose of mephedrone and methylone is 100-200 mg orally, with the onset of effect after 30-45 minutes and its duration from 2 to 5 hours. It seems that MDPV (structurally similar to pyrovaleron) has a higher potency: the effect occurs 15-30 minutes after taking a typical oral dose of 10-15 mg. The psychoactive effect can last from 2 to 7 hours.
Clinical effect and toxicity
Consumers note the following effects of synthetic cathinones: euphoria, a state of “high alert”, a surge of energy, talkativeness, increased sexual arousal and a compulsive desire to frequently “refresh” the dose. Some medical descriptions mention extremely aggressive and psychotic behavior, with phenomenal manifestations of physical strength, as with phencyclidine intoxication.
The clinical effects of synthetic cathinones correspond to the descriptions of toxicity characteristic of sympathomimetics: these are high blood pressure, tachycardia, hyperthermia, dehydration and psychomotor agitation. Patients may also complain of palpitations, headaches, chest pain, trismus, bruxism, tremor, insomnia, and paranoia. The long-term effects of synthetic cathinones are still unknown.
Drug detection
Current routine screening methods for detecting amphetamines are not capable of detecting synthetic cathinones, although they may give a false result of the presence of methamphetamine. However, commercial testing kits exist using both gas chromatography/mass spectrophotometry and liquid chromatography/mass spectrometry to detect certain synthetic cathinones, in particular mephedrone, MDPV and methylene.
Cathinones
Conventionally, psychostimulants can be divided into the following groups::
1. “Classic” – amphetamines, MDMA (ecstasy), cocaine.
1. Phenethylamines (methamphetamine, including cathinones, substituted cathinones – mephedrone), methylenedioxyphenethylamines (MDPV, PVF, MDPBF);
Amphetamines are the most numerous group of narcotic and psychotropic substances. To date, more than 100 different derivatives with psychotropic activity have been described. The basis of the chemical structure of amphetamines is phenylethylamine. Many derivatives have a similar chemical formula and are similar in action. Piperazines differ in chemical structure from other psychostimulants, but they have a similar effect [7].
The most well-known substances from the “new” psychostimulants are mephedrone (4-methylmethcathinone, 4-MMC), its analogues – methedrone, 4-methylethcathinone (4-MEC), fluoromethcathinones, etc.; methylene analogues – ethylene (MDEC, bk-MDEA), butylone (bk-MBDB), pentylone; analogues Pyrovalerone – MDPV (3,4-methyldioxypyrovaleron, MDPV), MDPBP (3,4-methyldioxypyrrolidinobuthiophenone), O-2482 (naphiron, naphthylpyrovaleron), etc.
The routes of administration of amphetamines are oral, inhalation (smoking), parenteral, mainly intravenous.
Amphetamines are completely absorbed in the gastrointestinal tract and spread throughout the body. Intravenous administration allows amphetamines to reach the brain in seconds, the inhaled vapors of the substance first condense in the lungs, and then it is quickly absorbed into the blood. For many amphetamines, Cmax is reached after 1-3 hours, while for smoking methamphetamine, it is reached within 7 minutes. The maximum psychostimulating effect of amphetamines is different. Within four days, 90% of amphetamines are eliminated.
The LD of amphetamine for adults is 120-200 mg (significantly higher when used). Serum concentrations: therapeutic 0.02 – 0.15 mcg/ml; toxic 0.2 – 1.0 mcg/ml; lethal 0.5 – 41 mcg/ml. Concentrations in urine: therapeutic 1 – 5 mcg/ml; toxic 25 mcg/ml; lethal 25 – 700 mcg/ml.
LD of methamphetamine is about 5-20 mg/kg. Serum concentrations: therapeutic 0.01 – 0.2 mcg/ml; toxic 0.2 – 1.0 mcg/ml; lethal 10 – 40 mcg/ml. Concentrations in urine: therapeutic 0.5 – 4 mcg/ml; toxic 25 mcg/ml; lethal 10 – 28 mcg/ml.
The amount of amphetamine used by drug addicts varies between 2.5 – 15 g/dose, which is at least 3 times higher than the amount of intravenously administered drug by drug addicts who use large doses of amphetamine [8, 9, 10]. The toxic concentration of ephedrine in blood plasma exceeds 1 mg/l.
– Pathogenesis of amphetamine poisoning [8, 9, 10].
The release and blockade of catecholamine reuptake in nerve endings mainly contribute to the release of norepinephrine and dopamine, in addition, catecholamine receptors are directly stimulated. In high doses, amphetamines promote the release of serotonin and act on the central seratonin receptors. MDMA acts 10 times more strongly in the area of serotonin nerve endings than in the area of noradrenergic and dopaminergic, therefore the seratonergic effect is more pronounced.
Benzylpiperazines, mephedrone, and diphenylprolinol inhibit the presynaptic reuptake of monoamines, especially dopamine; phenylpiperazines and methylone promote the release of serotonin from nerve endings, and some new hallucinogens stimulate seratonin receptors.
Phenethylamines inhibit monoamine oxidase and increase serotonin release in various ways. Tryptamines inhibit reuptake and promote the release of dopamine, norepinephrine, and serotonin.
Stimulation of central and peripheral adrenergic receptors leads to cardiovascular manifestations – tachycardia and hypertension, as well as changes in the nervous system (mood swings, anxiety, agitation, aggressiveness, visual and tactile hallucinations, clonic-tonic seizures). Agitation with increased muscle activity leads to the development of hyperthermia, in some cases, rhabdomyolysis.
The routes of entry of cocaine are inhalation (smoking, inhalation through the nose), intravenous, oral, rapidly absorbed, but due to the vasoconstrictive effect, further absorption and the onset of maximum concentration in the blood are delayed. The onset of action of cocaine depends on the route of entry into the body: when inhaled for 1-3 minutes, when smoked or administered intravenously for how many seconds, and the peak of action occurs after 3-5 minutes. With nasal use, the peak of action occurs after 20-30 minutes, and when swallowed, the activity reaches its peak after 60-90 minutes.
LD when ingested is 500 mg, but there are observations of a fatal outcome at an intranasal dose of 20 mg.
The half-life of cocaine is about 1 hour. Cocaine is excreted in the urine within 24 hours, 80% in the form of metabolites of benzoylecgonine and ecgonine.
– Pathogenesis of cocaine poisoning .
Reducing the rate of reuptake of adrenaline, norepinephrine, serotonin, and dopamine by presynaptic endings and, thus, increasing the release of these catecholamines from adrenergic nerve endings. Cocaine also increases the synthesis of norepinephrine. Stimulation of peripheral alpha-adrenergic receptors and action at the hypothalamic level contribute to the formation of hypertension and tachycardia.
Psychomotor agitation, the effect on the thermoregulatory centers in the hypothalamus and the decrease in heat transfer caused by vasoconstriction lead to the development of hyperthermia. Seizures, cardiac arrhythmias, and myocardial ischemia are more common in cocaine poisoning than in amphetamine poisoning due to the blockade of rapid sodium channels by cocaine and its thrombogenic effect.
Cathinone in narcology
Drug use causes irreparable harm to health and poses a danger to life!
Phenylalkylamines are of natural and synthetic origin. Despite the centuries-old history of the use of narcotic plants, the use of new psychoactive substances is increasing every year. The main consumer category is young people aged 15-25. The popularity of cathinones is associated with the ability to cause certain toxic effects that exacerbate feelings and increase emotional freedom.
History and distribution
The first detailed description of the Catha edulis plant dates back to 1775 (Peter Formkal). However, the 13th century is considered to be the time of the kata’s discovery, when the Arab healer Naguib al-Din realized that the leaves help eliminate fatigue in soldiers. It was from them that for the first time it was possible to isolate natural cathinones (norephedrone), which are alkaloids with psychoactive properties.
Kata Leaves
Kata shrubs (kath, chat), which have the appearance of a tea bush, have been grown in African countries and Asia since ancient times. These regions still observe the tradition of chewing the young shoots of the plant, which in their fresh form contain the largest amount of narcotic alkaloids. Among them, cathinone and katine, which are included in the List I of psychotropic substances, have the most pronounced effect.
In addition to the ritual chewing of the leaves, they are brewed and drunk instead of tea. This method does not provide a strong effect and is practically non-addictive. However, in regions of traditional use, there is a pronounced trend towards regular forms of consumption.
The substance was first isolated by chemical synthesis in 1978. The pharmaceutical preparations “Koldact” and “Effect” contain phenylpropanolamine hydrochloride, from which cathinones are obtained, and antihistamine components. Since the same time, they have been used in artisanal conditions to create narcotic solutions with complex and not fully understood composition.
Cathinone – alpha-aminopropiophenone is the main psychoactive component of fresh kata leaves. It is distinguished from phenamine by the presence of a ketone radical (C=O), which somewhat reduces the severity of its stimulating and toxic properties. Synthetic analogues are derivatives of beta-keto-amphetamine.
New psychoactive substances are illegally developed drugs that copy the effects of “classic” drugs (marijuana, amphetamines). At the same time, they have a completely modified chemical formula, which makes it possible to circumvent current legal restrictions. In the shadow market, synthetic cathinones combine an extensive group of designer products, such as the following:
MDMA (3,4-methylenedioxypyrovaleron);
Methylethcathinone (4-MEC);
mephedrone (4-methylmethcathinone);
methedrone (4-methoxymethcathinone);
methylene (3,4-methylenedioxymethcathinone);
They are created in a variety of forms – powders, crystals, capsules, tablets. Street names are specific to each sales region. In European countries, “salts” have such slang designations with mandatory labeling “not for human consumption”: “meow”, “bubbles”, “4-MMC”, “NewEcstasy”. In practice, a “pure” product is rarely found; most are mixtures of psychoactive compounds.They are often part of “ecstasy”, in addition to MDMA.
Mechanism of action
The effects of kata leaves, homemade solutions, and designer drugs have similar features due to their chemical structure. However, given the completely different complete composition of the end products, it is very difficult to predict the clinical manifestations of a particular drug. Synthetic cathinones work by inhibiting the reuptake of neurotransmitters, but the selectivity varies as follows:
Similar to methamphetamine are (meth) cathinone and flephedrone. These compounds selectively inhibit the breakdown of norepinephrine and dopamine, while stimulating their release into the synaptic cleft. The release of catecholamines by the adrenal glands is indirectly enhanced.
Similar to cocaine – MDMA, mephedrone, methylone, nafiron. Preventing the reuptake of dopamine is 5 times stronger than serotonin.
The pyrovaleron-like pathway is MDPV. Selective inhibition of catecholamine reuptake occurs, but the release of monoamines is not stimulated.
Thus, in the global understanding, designer drugs can be classified into the group of psychostimulants. But at the same time, they have too many differences in the mechanism of action, which allows them to be considered a separate class. Unfortunately, large-scale clinical trials are still insufficient for a complete assessment of pharmacodynamics, as more and more varieties of “salts” appear on the market every year.
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