CAFFEINE (Coffeinum; synonym: Cafeine, Caffeine, Coffan, Guaranin, Kaffein, Koffein, Kofka, Theinum; GFH, joint venture. B) — psychogogic and analeptical means. The alkaloid of a purine row which is contained in seeds of coffee, leaves of tea, fruits South American paulinin (gaurana), nuts of the West African plant of a stake, beans of cocoa and bulbs of a squill.
1,3,7-Trimetilksantin; With 8 H 10 N 4 O 2 - H 2 O:
White silky acicular crystals or inodorous white crystal powder, bitterish taste. On air disappears, during the heating it is sublimated. Let's slowly dissolve in water (1: 60), we will easily dissolve in hot water and chloroform, it is difficult alcohol-soluble, very little ether-soluble.
A source of industrial receiving To. from vegetable raw materials waste products of tea (tea dust, scraps of bushes on tea plantations, etc.) or grains of coffee serve. In the semi-synthetic and synthetic way To. receive from cyan-acetic to - you or its ethers in the way of condensation with urea (with receiving theophylline); as a feed stock for receiving To. use also uric to - that.
To. it is well soaked up at different ways of introduction and quite evenly distributed in body tissues. Duration of action To. after single introduction makes apprx. 6 — 7 hour. Biotransformation To. occurs preferential by demethylation. From an organism To. it is allocated with urine of hl. obr. in the form of metabolites (mono - and dimethyl of xanthines, urea); apprx. 8% of drug it is allocated in not changed look.
Basic pharmakol, property K. the stimulating influence on c is. N of page, especially on function of its highest departments. To. facilitates perception, accelerates the course of associative processes, improves functions of sense bodys, increases physical activity, intellectual and physical. working capacity, reduces fatigue and drowsiness. In I. P. Pavlov's laboratory it was for the first time established that To. strengthens and regulates processes of excitement in a cerebral cortex. Under influence To. excitability of a spinal cord, the respiratory and vasomotor centers increases. On action on c. N of page. To. is an antagonist of hypnagogues and anesthetics. It is supposed that the stimulating effect To. concerning c. the N of page is carried out generally due to sensitization of the central katekholaminergichesky receptors. It is established also that To. inhibits phosphodiesterase and by that promotes increase in cells of level of cyclic AMF, edges are stimulated by an ionic yield of calcium from a sarcoplasmic reticulum that is followed by increase in excitability of cells. Action To. at exhaustion of skeletal muscles connect not only with release of ions of intracellular Ca2+, but also their sensitization to potassium ions and a cholinergic mediator.
Action To. on blood circulation it is not unambiguous. At a collapse and shock To. raises the ABP due to stimulation of a vasomotor center and the vasoconstriction of internals connected with it. At the normal ABP does not cause essential changes of his level since at the same time at the same time with stimulation of a vasomotor center To. has direct vasodilating effect on vessels of skeletal muscles, brain, heart and kidneys. Action of the heart To. strengthens. Like other methylxanthines K. increases a diuresis due to reduction of a canalicular reabsorption of electrolytes a little, and also exerts the stimulating impact on gastric secretion.
Apply To. as excitant at intellectual and physical. exhaustion. As a part of drinks (tea, coffee) To. gained distribution as a «household» stimulator of c. N of page. As an analeptic To. apply at insufficiency of cardiovascular system, respiratory depression, and also at poisoning with anesthetics and other substances, the oppressing c. N of page Besides, To. use for treatment of neurosises (often in combination with bromides) and at migraine.
Appoint To. inside on 0,05 — 0,1 g 2 — 3 times a day. The highest doses for adults: one-time 0,3 g, daily 1 g. To children up to 2 years To. do not appoint. To children 2 years depending on age are more senior appoint 0,03 — 0,075 g to reception.
To. it is contraindicated at a hyperexcitability, sleeplessness, the expressed hypertension and atherosclerosis, organic diseases of cardiovascular system, at senile age, at glaucoma.
At acute poisoning To. excitement, a tremor of extremities, dizziness, vomiting, increase of pulse and breath are observed; in hard cases tetanic spasms and a coma develop. As antagonists at acute poisonings To. use means, the oppressing c. N of page (e.g., hypnotic drugs, anesthetics).
Abuse To. and the drinks supporting him can lead to development of a syndrome of medicinal dependence and accustoming.
Form of release: powder. To. is also a part of the combined tablets — askofen, Coffetaminum, Novomigrophenum, novotsefalgin, Pyrameinum, Citramonum, etc. To. and its drugs keep in well corked container.
In addition to To., in medical practice are used also caffeine-sodium benzoate (Coffeinum-natrii benzoas; synonym Coffeinum natrio-benzoicum; GFH, joint venture. B), which on pharmakol, is similar to properties and use To., but differs in bigger water solubility and it is quicker allocated from an organism.
Caffeine-sodium benzoate is appointed inside on 0,1 — 0,2 g by 2 — 3 times a day and under skin on 1 ml of 10 or 20% of solution. To children depending on age appoint inside 0,025 — 0,1 g to reception, under skin — on 0,25 — 1 ml of 10% of solution. The highest doses for adults inside: one-time 0,5 g, daily 1,5 g; under skin: one-time 0,4 g, daily 1 g.
Forms of release: powder, tablets on 0,1 and 0,2 g (for adults) and on 0,075 g (for children); in ampoules on 1 ml of 10 and 20% of solution and in the syringe tubes on 1 ml. Is also a part of the combined tablets — ankofen, Diapheinum, Cofalginum, etc. Caffeine-sodium benzoate is kept in well corked container.
Caffeine in the medicolegal relation
is Defined To. in cases of suspicion of artificial reproduction of a disease, at assessment of effects hron, its influences at court. - medical surveys and researches of a corpse. Fatal poisonings To. meet seldom and can be connected with self-treatment or with suicide attempts.
At poisoning To. on opening the phenomena of an acute hypoxia are noted: diffuse blue-crimson livors mortis, cyanosis of mucous membranes, a venous plethora of internals, dark liquid blood, punctulate hemorrhages on mucous membranes and under serous covers; the phenomena of irritation of a mucous membrane of a stomach are possible. At gistol, a research signs of a plethora of internals, hypostasis and emphysema of lungs, hypostasis of a brain are found.
For judicial chemical detection in internals To. extract chloroform from acid solution, process a chlorine water and evaporate solution on the water bath. The red or red-brown rest giving purple-violet coloring in the presence of ammonia turns out. Quantity To. determine by the weight of the rest.
Abuse of caffeine
Expressiveness mental, nevrol, and the somatic frustration arising at abuse To., depends on a dose and extent of accustoming to it.
At a single dose of high doses To. inability to concentration, excess mental mobility and initiative, acceleration of associations is observed that is shown by fussiness and garrulity against the background of emotional revival. Depending on type of the personality emergence of fear, alarm, the unstable crazy ideas of prosecution and the special (bad) relation is possible.
Besides, there are various somatic and nevrol, frustration: moderate expansion of pupils, pallor of integuments, tachycardia, increase in the ABP, increase in a diuresis, tremor, loss of appetite, sleeplessness. Also increase in tendon jerks, a sharpening of sight, hearing and sense of smell, increase of a muscle strength, speed and ease of movements is observed (without lack of coordination). Subjectively unpleasant somatonevrol. the disturbances (tachycardia, etc.) arising at overdose To., interfere with conscious abuse of it for the purpose of achievement of euphoria. Therefore abuse To. develops, as a rule, at its systematic reception for increase in intellectual working capacity and fight against overfatigue. Abuse To. most often develops at the persons hardly changing a rhythm of a dream and wakefulness and accepting To. for increase in productivity of mental work at night.
Long abuse To. in high doses leads to development of caffeine toxicomania, edges can arise during the use To. in the form of various medicines and coffee (a so-called caffeinism), and also tea (so-called theism). Both forms of caffeine toxicomania (caffeinism and theism) are characterized by the changed reactivity of an organism on action To., mental and physical. dependence, and also increase in tolerance (accustoming) to To.
Reception of high doses To. at caffeine toxicomania is not followed by disorganization of mental activity (owing to increase in tolerance). In these cases strengthening of an intellectual and physical activity, emergence of sociability with feeling of a maksimalization of opportunities is observed. At cancellation To. the state physical develops. and mental weakness: feeling of exhaustion, an aspontannost, lack of motivation to activity, apathy, an inclination to reception To. Such polar fluctuations of a state (a giperfreniya and a hypophrenia) are within a day characteristic throughout all course of toxicomania. However in process of its development the condition of excitement caused To., qualitatively changes: intellectual activity and associative activity are weakened, and excitement gains properties of irritability; patients easily have an irascibility, sometimes aggression. Out of receptions To. state psychophysical. weaknesses it is made heavier. Abstinence syndrome (with a general duration up to 2 weeks) it is expressed slightly and it is shown by weakness, an adynamia, sad mood, depressive thinking, the ideas of self-accusation and quite often suicide thoughts. Abstinent psychoses and epileptiform attacks are not observed.
The course of caffeine toxicomania long with progressive decrease in working capacity, gradual development of intellectual weakness, alarming and hypochiondrial states, dysphorias and depressions. Somatonevrol. effects hron, abuses To. weight loss, dryness and pallor of skin and mucous membranes, a Crocq's disease, signs of a dizregulyation of activity of cardiovascular system are and went. - kish. path. Death is caused psychophysical. exhaustions; weakness of cordial activity, a collapse are a proximate cause of death. Treatment comes down to single-step an otnyatiya To. and to purpose of high doses of biostimulators, vitamins, antidepressants from group of MAO inhibitors and fenotiazin with the subsequent gradual decrease in their doses.
Bibliography: Harmful substances in the industry, under the editorship of N. V. Lazarev and E. N. Levina, t. 2, page 557, L., 1976; Melentyeva G. A. Pharmaceutical chemistry, t. 2, page 561, etc., M., 1976; Stolyarov G. V. Medicinal psychoses and psychotomimetic means, page 133, M., 1964; Shvaykova M. D. Toxicological chemistry, M., 1975; Bridges-WebbC. Grounds M. Analgesic use and abuse, role of caffeine, Med. J. Aust., v. 2, p. 805, 1976; G r e d e n J. F. Anxiety of caffei-nism, Amer. J. Psychiat., v. 131, p. 1089, 1974; Karacan J. o. Dose-related sleep disturbances induced by coffee and caffeine, Clin. Pharmacol. Ther., v. 20, p. 682, 1976; The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, L., 1975.
I. I. Baryshnikov; E. 3. Bronstein (court. medical), I. N. Pyatnitskaya (psikhiat.).