Cathinone, Methcathinone

1. Methcathinone (methcathinone, ephedrone).
2. Cathinone (cathinone, norephedrone, beta-ketoamphetamine).

The khat is a shrub of the celastraceae family, resembling a tea bush in appearance. It has long been cultivated in Abyssinia, Somalia, Arabia, the mountains of Yemen, India and Sri Lanka. The smallest, youngest, still growing leaves from the tops of the shoots are used.

Khat was introduced to the United States and other countries for consumption by emigrants from supplying countries. It contains a certain amount of chemicals, among which are two controlled substances: cathinone and cathine (Schedule I – Psychotropic Substances). Once the leaves mature and dry out, cathinone is converted to cathine, which greatly reduces its stimulant properties.

The main psychoactive constituent of fresh khat leaves is the amphetamine-like alkaloid cathinone: (-)-alpha-aminopropiophenone or in another designation 2-amino-1-phenyl-propanone-1. Unlike phenamine (2-amino-1-phenyl-propanone), cathinone contains a periphenyl ketone radical (C=O) in the alkyl chain. It is the presence of the ketone radical that is thought to attenuate the excitatory, anorectic, and toxic properties of cathinone (norephedrone) compared to phenamine. Fresh khat leaves also contain small amounts of norpseudoephedrine, the content of which increases as the leaves age, usually after 3-4 days. Cathinone was isolated as a previously unknown alkaloid in the late 1970s and caught the attention of neuropharmacologists for a long time.

History

Cathinone was first discovered in the leaves of khat (catha ebulis), which grows and is used as a psychostimulant primarily in East Africa. Cathinone was found to be an unstable compound, found only in freshly harvested khat plants. In 1978, cathinone was synthetically produced. It was noted that cathinone posed a serious danger due to the possibility of such synthesis, but there were no reports of cases of abuse of synthetic cathinone in the literature before the first reports of psychoactive use of the substance made from koldact and effect capsules. It is true that to write, in this case, of “abuse of synthetic cathinone” is at the very least inappropriate. Much closer to the body is the phrase “binge drinking”.

In a number of African and Asian regions, there is a centuries-old tradition of chewing the young shoots of the leaves of the khat plant. This initially localized cultural phenomenon has a dramatically pronounced tendency to increase regular forms of consumption and to spread far beyond the places where the shrub grows and is cultivated. Even episodic and regular use of khat in Europe and the Americas has been documented among individuals from selected Asian and African diasporas.

Action

Simply put: Immediately after the injection, there is a sensation of coming, “hitting in the head”, “a rush of blood to the head”. Often there is a chill, tingling in the hands and feet, a feeling of creeping goosebumps, “hair stands on end”. Almost immediately there is a rapid heartbeat. Mood and activity increase. The flow of thoughts speeds up. You feel a rush of energy and a thirst for activity. After the first drug intake drug intoxication lasts from one to three hours, then it decreases to about half an hour.

During the period of work in the East African region (Addis Ababa, Ethiopia) were studied 58 self-descriptions of the state of khat intoxication in persons who are not addicted and use the leaves only as part of the local tradition, The age of chewers ranged from 12 to 57 years. Male individuals who were able to adequately convey their feelings and experiences were selected. The information obtained was compared with 16 self-descriptions of conditions during the first trials of the aforementioned cathinone-containing solution administered intravenously. The interviewees were inpatients between the ages of 14 and 33:

The effects of the substances compared (khat leaves and homemade solution) revealed a significant affinity, due to the chemical-pharmacological kinship of their main psychoactive constituents. In the generalized picture of acute intoxication with khat leaves and cathinone-containing solution, three groups of effects can be distinguished with a certain convention: physiological, predominantly psychophysiological and predominantly personality-psychological. Physiological reactions include central and peripheral effects. The former are manifested by general and selective excitation of the central nervous system, and the latter – by sympathomimetic actions associated with both alpha-adrenoreceptors (mydriasis, narrowing of blood vessels, relaxation of intestines, etc.) and beta-adrenoreceptors (increased heart rate, relaxation of smooth muscles of bronchi and skeletal muscles, etc.).

Immediately in the acute period of intoxication (intoxication) physiological manifestations occur with the following frequency: dry mouth, mydriasis, anorexia – 100%, increased libido – 83.8%, hyperemia – 70.3%, frequent urination – 62.2%, pulsation of blood vessels in the neck – 56.5%, palpitation – 51.3%, pulsation in the temples – 43.2%, spermatheria – 35.1%, muscle lethargy – 27.0%, feeling of compression in the heart – 24.3%, headache – 16.2%, nausea – 10.8%. After 4-12 hours, the most frequently noted were lack of appetite – 89.2%, general weakness – 70.3%, sleep disturbance – 70.1%, flatulence – 62.2%, tachycardia and increased libido – 51.2% each, weakness of erection – 35.1%, motor restlessness – 29.7%, skin itching – 18.9%, paresthesias – 13.5%.

Cat intoxication builds up more slowly and proceeds more mildly. Euphoria prevails over hypomania in a number of hyperthemic changes. The state of animation is more evident in speech activity. A sense of “self-assured wisdom” with a gradual shift from relatively realistic plans to projection dominates later, the relaxation stage is not filled with any specific content, but is experienced as a pleasant state of rest. It may be shortened or lengthened by the mobilization stage, depending on the original or new setting of the chewer.

Periods of asthenization and autonomic-somatic disorders are relatively mild, with sleep and gastrointestinal disorders (burning sensation, constipation, flatulence) being among the most painful. Thus, the milder effect of khat (compared to injection of cathinone-containing solution) is explained by the way of its consumption – chewing, which physically limits the intensity of cathinone intake into the body. As a result, the content of cathinone in the blood plasma is held for a long time within certain, relatively low limits. The course of khat intoxication is also positively colored by the traditional attitude of collective khat chewers toward friendly companionship. Such an atmosphere is noted from the peculiarities of the subcultural environment in which artisanal stimulants are used. Naturally, the intravenous injection of a cathinone-containing solution somewhat modifies the picture of intoxication, at the expense of a one-step entry of high doses of the psychoactive substance directly into the bloodstream. Known (manganese) and unknown substances contained in the final solution also play an indisputable role in the execution of intoxication and its consequences. Their toxic effect becomes more significant in the transition to regular use, so the picture of acute intoxication in chronic khat chewers and individuals with a pronounced dependence on psychostimulant derived from the drugs “Effect” and “Coldact” becomes even more different, as well as the clinic itself of these drug addiction diseases.

Danger

Ephedrone (norephedrone) contains a small amount of manganese, which, nevertheless, can cause severe damage to the central and peripheral nervous systems in a few years – “manganese polyneuroencephalopathy”, manifested by dementia and limb paralysis. Ephedrone (norephedrone) also causes other complications: paranoid psychosis, heart rhythm disorders, inflammation of the mucous membranes of the mouth, caries. An indirect (indirect) complication of ephedrone (norephedrone) abuse is general dystrophy.

More than two years of regular (at least once every couple of days) use, so far, has not withstood anyone with a human body – all as one became disabled. Already on the third-fourth month, speech and gait become disturbed, but as a rule, the addict does not connect it with the effect of cathinone and only a few go to the doctor. This kind of neglect is catastrophic because at that stage it is still possible to correct something. But who will voluntarily go to see a psychiatrist or neurologist? As a result, you get incurable consequences, including: impaired coordination of movements, propulsion and retropulsion, difficulty in changing the body position, almost no spontaneous movements, mask-like facial expressions, dysarthria and hypophonia, sometimes sagging of the soft palate, finger tremors. And also: spasms and twitches of muscles, convulsions, rough handwriting disorder up to complete loss of writing skills and slowed speech or even complete aphasia – absence of ability to speak.

The most frustrating thing is that cathinone is almost not to blame here, although it does contribute to the overall condition. But, by and large, it is the trivial manganese. It is manganese, which is an aggressive chronic neurotropic poison, that causes irreversible severe organic damage to the brain and other fucked up things that fall on the head of the already miserable junkie.

Users of khat, which contains “natural” cathinone, have not been described as having any such disorders. Virtually the only factor capable of causing such early and massive brain damage is manganese compounds. Vinegar, however, also hits the kidneys and liver, but by the time this becomes noticeable, the “effects” of manganese encephalopathy will turn the junkie into an emotionless lunatic, strapped to the bed with some haloperidol.

Characteristically, lovers of the “classic” mulka made from ephedrine, such a gloomy future awaits much later than adherents of pounding the shirevos out of norephedrine, although the recipe and method of administration into the body are almost identical. The effects of intravenous cathinone are comparable to those of ephedrone, the real stuff, but with less duration and strength, and as a rule, a cathinone user will start looking to re-inject after an hour or two. Addicts who were “registered” and interviewed by doctors who meticulously recorded their conversations, said that at the beginning of narcotization the frequency of injection was usually 2-3 times a day and then increased to 6-8 times a day. In some cases, the average daily number of injections could be as many as 25 times a day. And, although it is difficult to establish the exact daily dose of the solution obtained from “Coldact” or “Effect” preparations, it should be noted that it is significantly higher than the daily dose of mulka from preparations containing ephedrine.

When the first clinical manifestations of severe neurological disorders appear, addicts stop them by administering another dose. But after some time (up to three months after the initial symptoms), the injection stops helping, because the cause is not withdrawal (withdrawal), but brain damage. And this reason alone prompts them to go to treatment facilities, although it is often too late.