Caffeine in ampoules dosage. Caffeine guide: action, effects, correct and lethal doses

Instructions for use of Caffeine sodium benzoate 20% solution for injection
for stimulation of the central nervous and cardiovascular systems in animals
(manufacturing organization: Nita-Pharm CJSC, Saratov)

I. General information
Caffeine sodium benzoate 20% (Coffeinum-natrii benzoas 20% solution pro injectionibus).
International generic name: Caffeine, sodium benzoate.

The drug is available in the form sterile solution for injection.
1 ml of the drug contains caffeine 75 mg, sodium benzoate 120 mg and excipients.
By appearance the drug is a clear, colorless liquid.

Caffeine sodium benzoate is available packaged in glass bottles of 10, 20, 100 ml, hermetically sealed with rubber stoppers and rolled aluminum caps.

The shelf life, subject to storage conditions, is 2 years from the date of manufacture, after opening the bottle - 28 days.
Do not use Caffeine Sodium Benzoate after the expiration date.

Store the medicinal product with precautions (list B), in the manufacturer’s closed packaging, separately from food and feed, in a dry place, protected from direct sun rays place at a temperature from 0°C to + 25°C.
The bottle is opened using a sterile syringe.
It is recommended to store the opened bottle at a temperature of 0 to + 10 ⁰C in a dry place, protected from direct sunlight.
Caffeine sodium benzoate should be kept out of the reach of children.
No special precautions are required when disposing of unused drug.
Unused medicinal product is disposed of in accordance with legal requirements.

II. Pharmacological properties
Caffeine benzoate sodium 20% solution for injection has a stimulating effect on the central nervous system of animals. It enhances and regulates excitation processes in the cerebral cortex, enhances positive conditioned reflexes and increases motor activity. The stimulating effect of caffeine leads to increased physical performance, reduce fatigue and prevent drowsiness. The effect of the drug depends on the dose, as well as on the type of higher nervous activity animals. Large doses of the drug can lead to depletion of nerve cells.
Under the influence of the drug, cardiac activity increases, with collaptoid and states of shock blood pressure rises, gas exchange increases, water and nitrogen metabolism increases, breathing increases, breathing becomes deep, especially against the background of depression of the respiratory center. The drug has a moderate diuretic effect.

Caffeine benzoate sodium 20% injection solution according to the degree of impact on the human body according to GOST 12.1.007 is classified as low-hazard substances (hazard class 4).

III. Application procedure
Caffeine benzoate sodium 20% solution for injection is prescribed to horses, large cattle, sheep, goats, pigs, dogs. Used to stimulate the central nervous system in case of poisoning with poisons that depress the central nervous, cardiovascular and respiratory systems, overwork, muscle weakness arising from various diseases.
Used to stimulate the cardiovascular system in case of weakness of cardiac activity, decreased excitability and conductivity in the heart muscle, and shock conditions. The drug is used to stimulate the respiratory center when it is depressed and weakened breathing, with a spastic state of the muscles of the gastrointestinal tract, with a maternity cut in cows. Used for chronic myocarditis, myodystrophies, chronic myodegenerations, as a vasodilator for spasms of blood vessels in the brain, kidneys, and heart.

Contraindications to the use of Caffeine sodium benzoate 20% solution for injection are: individual intolerance to the components of the drug, severe arterial hypertension, organic diseases cardiovascular system (including atherosclerosis), increased excitability.

Caffeine benzoate sodium 20% solution for injection is used subcutaneously in the following doses:

Doses and timing of use depend on the weight of the animal and the course of the disease.

In case of overdose or exceeding the duration of the recommended course of treatment, anxiety, agitation, insomnia, tachycardia, arrhythmias, increased blood pressure, nausea, and vomiting are possible. In this case, stop using the drug and prescribe symptomatic treatment.

No peculiarities of action were identified during the first use of the drug and when it was discontinued.

If one or more doses of the drug are missed, use is carried out according to the same scheme in accordance with these instructions. Do not administer a double dose to compensate for a missed dose.

The use of caffeine sodium benzoate 20% solution for injection does not exclude the use of other medicines. The drug is combined with cardiac glycosides atropine, bronchodilators, analgesics, ergot alkaloids, bromides, accelerates their absorption and enhances the effect, reduces the effect of sleeping pills and narcotics.

Meat and milk during and after the use of caffeine sodium benzoate 20% solution for injection are used without limitation.

IV. Personal prevention measures
When using Caffeine benzoate sodium 20% solution for injection, no special precautions are required. Hands should be washed after finishing work warm water with soap.
It is prohibited to smoke, eat or drink during work.
All work with the medicinal product should be carried out in compliance with the rules of personal hygiene and safety precautions provided for when working with veterinary medicinal products.
Bottles of Caffeine benzoate sodium 20% injection solution are prohibited from being used for food purposes.

In case of accidental contact of the drug with the skin or mucous membranes of the eyes, rinse big amount water.
If ingested, consult a doctor.

Manufacturing organization: Nita-Pharm CJSC; 410010, Saratov st. Osipova, 1.
Address of place of production: 410010, Saratov st. Osipova, 1.

The product is produced in the form of tablets in blister packaging. The main substance is caffeine (in the form of sodium benzoate).

The drug Caffeine in tablets has a psychostimulating, analeptic, cardiotonic effect. The stimulating effect on the central nervous system exhibited by the drug Caffeine in tablets excites the vasomotor and respiratory centers, causes an increase in reflex excitability of the spinal cord, enhances and regulates excitation processes in the cerebral cortex.

As a result, physical and mental performance increases, drowsiness and fatigue decrease, strength and heart rate increase, which is especially noticeable in large doses. For hypotension, without changing normal pressure the drug is able to increase blood pressure. In addition, they are expanding blood vessels skeletal muscles, kidneys, heart, bronchi and narrowing of the abdominal organs. Secretory function At the same time, the stomach level increases, platelet aggregation decreases. The drug blocks peripheral and central adenosine receptors and exhibits a moderate diuretic effect, stabilizes transmission at beta-adrenergic synapses medulla oblongata and hypothalamus, dopaminergic synapses, noradrenergic synapses, cholinergic synapses of the medulla oblongata and cortex.

The effectiveness of koeyin tablets significantly depends on the type of nervous system of the patient, and therefore should be prescribed taking into account individual characteristics human nervous activity.

Indications for the use of caffeine tablets

The drug is prescribed for the treatment of diseases in which the functions of the central nervous system are inhibited, respiratory systems s, cardiovascular system, including drug poisoning, infectious diseases and others.

Caffeine is also used for cerebral vascular spasms, to increase physical and mental performance, for breathing problems, to eliminate drowsiness, and enuresis in children.

Contraindications

The drug is not prescribed for organic diseases of the cardiovascular system, including atherosclerosis, severe arterial hypertension, increased excitability, sleep disorders, glaucoma, and old age.

Side effects

When using the drug, manifestations of agitation, anxiety, increased blood pressure, tachycardia, insomnia, arrhythmia, nausea and vomiting are possible. Long-term use of the product is fraught with possible mild addiction. At the same time, it decreases, which is due to the formation of new adenosine receptors in brain cells. If you suddenly stop drinking caffeine, there may be increased inhibition of the central nervous system, resulting in fatigue, depression and drowsiness.

Use of caffeine tablets and doses

The drug is prescribed orally at a dose of 25-100 milligrams up to three times a day.

For adults, the maximum single dose is 0.4 grams, and the daily dose is 1 gram.

The drug reduces the effectiveness of narcotic and sleeping pills, but increases, due to improved bioavailability, paracetamol, acetylsalicylic acid, and other non-narcotic analgesics. The drug improves the absorption of ergotamine in the gastrointestinal tract.

Overdose

When overuse caffeine (more than 0.3 grams per day, which corresponds to four 150 ml) may cause restlessness, anxiety, confusion, tremor, headache, cardiac extrasystoles.

active substance: caffeine sodium benzoate;

1 tablet contains caffeine-sodium benzoate (in terms of 100% dry matter) – 200 mg;

Excipients: lactose monohydrate, microcrystalline cellulose, corn starch, povidone, calcium stearate.

Dosage form. Pills.

Basic physicochemical characteristics: round tablets, white, with a flat surface with beveled edges and a notch.

Pharmacotherapeutic group.

Psychostimulants, drugs for use in attention disorder and hyperactivity disorder (ADHD), and nootropics. Xanthine derivatives. ATX code N06B C01.

Pharmacological properties

Pharmacodynamics.

Sodium caffeine benzoate is used primarily as a central nervous system stimulant.

The mechanism of action of the drug is based on the inhibition of the phosphodiesterase enzyme by caffeine, leading to the accumulation of cyclic adenosine monophosphate inside the cells. The latter enhances glycogenolysis, stimulates metabolism in organs and tissues, including the central nervous system and muscles. An important link in the mechanism of the stimulating effect of the drug is the binding of caffeine to purine receptors in the brain.

Caffeine enhances and regulates excitation processes in the cerebral cortex, enhances positive reflexes, and increases motor activity. These effects are dose-dependent and help improve mental and physical performance, reduce fatigue and drowsiness. In very large doses, caffeine can cause nerve cell depletion.

The drug weakens the effect of sleeping pills and narcotics, increases reflex excitability of the spinal cord, and stimulates the respiratory and vasomotor centers. Under the influence of the drug, cardiac activity increases and the heart rate increases.

Under the influence of caffeine-sodium benzoate, diuresis increases slightly (mainly

due to decreased reabsorption of electrolytes in the renal tubules).

Pharmacokinetics.

The drug is well absorbed from digestive tract. Evenly distributed in the body. Easily penetrates the blood-brain barrier. Penetrates the placenta and is excreted into breast milk. During the biotransformation process, it undergoes demethylation and oxidation. The half-life is 3-7 hours. It is excreted from the body in urine and feces in the form of metabolites, a small part (about 8%) is unchanged.

Clinical characteristics.

Indications

• Infectious and other diseases accompanied by depression of the central nervous and cardiovascular systems;
• arterial hypotension;
• asthenic syndrome;
• spasms of cerebral vessels;
• drowsiness;
• increasing mental and physical performance.

Contraindications

• Hypersensitivity to caffeine, other xanthine derivatives (theophylline, theobromine) or to any of the components of the drug;
• increased excitability;
• insomnia;
• marked increase in blood pressure, arterial hypertension;
• organic diseases of the cardiovascular system (incl. acute heart attack myocardium, paroxysmal tachycardia, atherosclerosis);
• glaucoma;
• age over 60 years.

Interaction with other drugs and other types of interactions.

Concomitant use of caffeine sodium benzoate with:

• ;MAO inhibitors, furazolidone, procarbazine and selegiline– may cause the development of dangerous cardiac arrhythmias or a marked increase in blood pressure;
• ;barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin)– increased metabolism and increased clearance of caffeine;
• ;ketoconazole, disulfiram, ciprofloxacin, norfloxacin, enoxacin, pipemidic acid– may cause a slower elimination of caffeine and an increase in its concentration in the blood;
• ;cimetidine, hormonal contraceptives , isoniazid– increased effect of caffeine;
• ;fluvoxamine– increased caffeine levels in blood plasma;
• ;mexiletine– reduction in caffeine excretion by 50%;
• ;nicotine– increasing the rate of caffeine elimination;
• ;methoxsalen– reducing the excretion of caffeine from the body with a possible increase in its effect and the development of toxic effects;
• ;clozapine– increased concentration of clozapine in the blood;
• ;theophylline and others xanthines– decreased clearance of these drugs, increased risk of additive pharmacodynamic and toxic effects;
• ;β-blockers– may lead to mutual suppression of therapeutic

effects;

• ;thyroid-stimulating drugs– increased thyroid effect;
• ;opioid analgesics, anxiolytics, sleeping pills And sedatives – reduction of the effect of these drugs;
• drugs lithium– increased excretion of lithium in urine;
• drugs calcium– decreased absorption of these drugs;
• ;cardiac glycosides– accelerated absorption, enhanced action and increased toxicity of cardiac glycosides;
• ;analgesics-antipyretics– strengthening their effect;
• ;ergotamine– improved absorption of ergotamine in the digestive tract;
• ;xanthine derivatives, α- and β-adrenergic agonists, psychostimulants– potentiation of their effects.

Caffeine is an antagonist drugs for anesthesia and others drugs that depress the central nervous system, a competitive antagonist of drugs adenosine, ATP.

Drinks and medications containing caffeine, when used together with the drug, may cause excessive stimulation of the central nervous system. High doses of caffeine can cause tremors and palpitations. Patients should avoid excessive consumption coffee or tea.

Features of application

When using the drug, you should avoid excessive consumption of coffee, strong tea, other tonic drinks, alcohol and medications containing caffeine.

In case of prolonged use of the drug, the development of mental dependence is possible. Abrupt cessation of treatment leads to increased inhibition of the central nervous system (drowsiness, depression).

The effect of the drug largely depends on the type of nervous system and can manifest itself as both excitation and inhibition of higher nervous activity.

Caffeine may cause a false increase uric acid in blood determined by the Bittner method.

Caffeine may increase urinary levels of 5-hydroxyindoleacetic acid (5-HIAA), vanillylmandelic acid (VMA), and catecholamines, which may lead to false-positive diagnoses of pheochromocytoma and neuroblastoma.

Use the drug with caution in patients with peptic ulcer stomach and duodenum in the anamnesis.

The drug contains lactose. For patients with rare hereditary forms Galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use this drug.

Use during pregnancy or breastfeeding.

The drug is contraindicated for use during pregnancy or breastfeeding.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Until the patient's individual reaction to the drug is clarified, you should refrain from driving vehicles or other mechanisms, given that during treatment you may experience adverse reactions from the central nervous system.

Directions for use and doses

Use internally 2-3 times a day. A single dose for adults is 100-200 mg.

The highest single dose is 500 mg, highest daily dose– 1 year

Children over 12 years of age are prescribed at a dose of 100 mg 2-3 times a day.

The highest daily dose for children is 500 mg.

The dose of the drug and the course of treatment are determined by the doctor individually, depending on the severity of the disease and the effectiveness of therapy.

Children.

Sodium caffeine benzoate in tablet form is not recommended for use in children under 12 years of age.

Overdose

Symptoms: gastralgia, agitation, anxiety, motor restlessness, confusion, delirium, dehydration, tachycardia, arrhythmias, hyperthermia, increased frequency of urination, headache, increased tactile or pain sensitivity, tremors or muscle twitching; nausea and vomiting, sometimes mixed with blood; ringing in the ears, convulsive seizures (in case of acute overdose - tonic-clonic seizures).

Treatment: gastric lavage, administration of enterosorbents, maintenance of pulmonary ventilation and oxygenation; for convulsive seizures - intravenous diazepam, phenobarbital or phenytoin; maintaining fluid and salt balance; hemodialysis. There is no specific antidote.

Adverse reactions

Nervous system: agitation, anxiety, tremor, restlessness, headache, dizziness, muscle twitching, seizures, increased reflexes, tachypnea, insomnia; with sudden withdrawal - increased inhibition of the central nervous system with the appearance of a feeling of increased fatigue, drowsiness, muscle tension, depression.

The cardiovascular system: a feeling of constriction in the chest, a feeling of palpitations, tachycardia, arrhythmias, increased blood pressure.

Digestive tract: nausea, vomiting, diarrhea, exacerbation of peptic ulcer.

Urinary system: increased frequency of urination, increased creatinine clearance, increased excretion of sodium and calcium.

The immune system: manifestations of hypersensitivity reactions are possible, incl. skin rashes, itching, urticaria, angioedema, bronchospasm, anaphylactic shock, Stevens-Johnson syndrome.

Laboratory indicators: Maybe false promotion uric acid in the blood, determined by the Bittner method, hypoglycemia/hyperglycemia, slight increase

5-hydroxyindoleacetic acid (5-HIAA), vanillylmandelic acid (VMA) and catecholamines in urine.

Other: nasal congestion, with long-term use– decreased effect of caffeine, which is associated with the formation of new adenosine receptors in brain cells, drug dependence.

Best before date

Storage conditions

In original packaging at a temperature not exceeding 25 ºС.

Keep out of the reach of children.

Package

10 tablets in a blister, 1 blister in a pack; 10 tablets in a blister.

Manufacturer

Public Joint-Stock Company"Research and Production Center "Borshchagovsky Chemical and Pharmaceutical Plant".

Society with limited liability"Agrofarm".

The location of the manufacturer and its address of place of business.

Ukraine, 03134, Kyiv, st. Mira, 17.

Ukraine, 08200, Kiev region, Irpen, st. Central, 113-A.

The modern rhythm of life requires a person to be completely involved in its whirlpool, which is why so many people desperately lack rest. How to overcome the resulting drowsiness? A cup of aromatic coffee often helps to disperse drowsiness and get into active mode. But this method doesn't always work. Therefore, many people choose an alternative - a drug called “Caffeine”. The instructions for use characterize it as a psychostimulant drug, the effectiveness of which is associated with the alkaloid it contains, produced from tea leaves (2% caffeine), coffee beans (1-2 percent) and cola nuts.

"Caffeine sodium benzoate", which can be found in pharmacies, is synthetic drug, obtained from these compounds.

Pharmacological properties (application)

A methylxanthine derivative, caffeine, has a psychostimulating and analeptic effect on the body. Its main property is the ability to improve motor activity, stimulate positive reflexes and various processes excitations occurring in the cerebral cortex. Thanks to this effect on the body, mental and physical activity increases, drowsiness disappears, and the feeling of fatigue decreases.

Caffeine can also increase blood pressure, but this occurs more often in states of shock or collapse. In small doses, caffeine provides a stimulating effect; in large doses, depression of the nervous system often occurs. What other effects does caffeine have? Instructions for use warn about increased and deepening of breathing when taking the drug, narrowing of blood vessels in the brain and a decrease in oxygen pressure in it. In cases of arterial hypotension, caffeine often normalizes blood pressure. The alkaloid has an antispasmodic effect on smooth muscles and a stimulating effect on striated muscles. Under the influence of caffeine, the secretory activity of the stomach increases and the basal metabolism increases (increased glycogenolysis, accelerated lipolysis). A moderate diuretic effect is also a consequence of caffeine consumption.

"Caffeine": indications for use

The drug is prescribed for diseases accompanied by a depressed state of the central nervous system, for disturbances in the functioning of the cardiovascular and respiratory systems (including poisoning with drugs, alcohol and toxins as a result of infectious process), asphyxia, asthenia, enuresis (including in children), migraine, to relieve spasms of cerebral vessels. In ophthalmology, caffeine is used after eye surgery to reduce tone and retinal detachment.

This medicine is also indicated for decreased mental and physical performance, drowsiness, and to restore the optimal level of activity. A steady trend in recent years has been the use this drug as a catalyst for the weight loss process. In this case, the obligatory conditions are strict adherence to the dosage, doctor’s recommendations and physical activity. In cosmetology, the mixture of “Caffeine-sodium benzoate” and “Capsicam” has proven itself well as effective remedy for anti-cellulite wrap.

Release form

“Caffeine sodium benzonate” (containing up to 40% caffeine) is available in the form of injection solution, tablets and powder (capsules).

Directions for use and dosage

How to take Caffeine correctly? Tablets, the instructions for use of which advise their use orally no more than 2-3 times a day, are prescribed for adults in a single dose of 100-200 mg (no more than 0.4 g) and a daily dose of no more than one gram, for children - according to 25-100 mg. Caffeine ampoules (1 ml) are intended for subcutaneous and subconjunctival administration.

Children are injected subcutaneously with a ten percent caffeine solution of 0.25-1 ml. In ophthalmology, a 10% solution of caffeine in ampoules is also used: no more than 0.3 ml of the drug is dripped under the conjunctiva once a day. The dosage and duration of treatment are prescribed by the doctor and depend on the patient’s condition, as well as the nature of the disease. Caffeine sodium benzoate should not be taken before bed.

Contraindications

The instructions for use do not recommend prescribing the psychostimulant “Caffeine Benzoate” to people with arterial hypertension, increased excitability, sleep disorders (insomnia), those suffering from atherosclerosis, tachycardia, epilepsy, convulsions, increased intraocular pressure (glaucoma). The drug is also contraindicated in children under 12 years of age and people old age. Anti-cellulite masks should not be applied to affected areas of the skin.

Side effects

When taking a drug containing caffeine, the instructions for use advise paying attention to possible negative reactions body: from the central nervous system - anxiety, agitation, tremor, headache, anxiety, convulsions, dizziness, increased muscle tone, increased reflexes, insomnia, tachypnea. If the drug is abruptly discontinued, lethargy, drowsiness, fast fatiguability, strengthening the processes of inhibition of the central nervous system reaction.

From the cardiovascular system, arrhythmia, tachycardia, and increased blood pressure are possible. From the gastrointestinal tract - nausea, exacerbation of peptic ulcers, vomiting, colic. At long-term use addiction, dependence on the drug is possible due to the formation of new adenosine receptors in the brain cells.

Overdose

What symptoms can excess caffeine cause? Instructions for use warn in such cases about increased severity side effects: anxiety, confusion, mental and motor agitation, tremors or muscle twitching, epileptic seizures; dehydration, tachycardia, arrhythmia, headache, ringing in the ears, hyperthermia, frequent urination, nausea and vomiting.

The same conditions can occur after taking 300-600 mg (4 cups) of coffee per day, especially if combined with taking Caffeine Sodium Benzoate tablets.

special instructions

During pregnancy and while breastfeeding, caffeine is taken only in cases of extreme necessity and under the supervision of a doctor! Abuse of the drug and drink threatens possible spontaneous abortion, delay intrauterine development, inhibition or disturbances in skeletal development, arrhythmia in the fetus. IN lactation period caffeine penetrates into breast milk and, accumulating, threatens the baby’s insomnia and hyperactivity.

"Caffeine": instructions for use, price, storage conditions and expiration date

The drug must be stored away from children, out of reach of them, at temperatures up to 25 degrees, for no more than 5 years.

The cost of “Caffeine-sodium benzoate” tablets (6 pieces) in pharmacies today is approximately 32-40 rubles, a package of 10 ampoules (1 ml) of 20% solution is sold for 40-64 rubles.

Analogues

In addition to tablets produced in blisters of 6 or 10 pieces, as well as a solution for injection in ampoules, in pharmacies you can find drugs with various combinations of substances, which include caffeine. What other medications containing caffeine are listed in the instructions for use of medications? Expert reviews call the following analogues: “Askofen” (40 mg) and “Coficil Plus” (50 mg of the substance in question), “Migrenol” and “Solpadeine Fast” - 65 mg each, “Aquacitramon” (45 mg), as well as “Citramon” "and regular "Solpadeine" - 30 mg each. Among the drinks containing this common psychostimulant, reviews on forums mention coffee, tea, hot chocolate and soda (cola). The weight loss product Liquid Chestnut, which contains guaranine (an analogue of caffeine and theine), has a double concentration of caffeine.

Caffeine- one of the most widely and regularly used natural biologically active compounds, known since ancient times. Caffeine gets its name from one of its main sources - coffee beans (coffee contains over 1000 components that can affect human health). Other names for caffeine still in use (theine, mateine, guaranine) come from other plant sources (tea leaves, yerba mate, guarana fruit). From the point of view of chemistry, pharmacognosy and pharmacology, caffeine is a purine alkaloid, 1,3,7-trimethylxanthine, found in tea leaves (about 2%), coffee seeds (1–2%), cola nuts and belongs simultaneously to two pharmacological groups: “Psychostimulants” and “Analeptics”.

There are different points of view on the benefits of caffeine consumption, each of which is supported by medical observations, from claims of "infinite variety beneficial effects for mind, body and spirit" to warnings about the dangers of consuming caffeine, which acts like classic drugs.

Caffeine, nicotine and alcohol make up the “legal triad” of psychoactive substances (PAS). Their use, with certain restrictions on the availability of the last two substances for certain groups of the population, is not punishable by law in Russia, Europe, the USA and other developed countries.

Caffeine is found in many food products and drinks: coffee, tea, cocoa-containing products (cocoa, dark and milk chocolate, chocolate milk, yogurt, cakes, candies, etc.), mate, soda water (7-Up, Fanta, Tonic Water, Cola-containing drinks : Coca-Cola, Pepsi Cola, Afri Cola, Coke Zero, etc.), some alcoholic drinks, dietary supplements, frozen desserts, chips, chewing gum etc. B Lately Caffeine-containing products are rapidly gaining popularity among young people. energetic drinks(Red Bull, Adrenaline Rush, etc.) - “energy drinks”, “energy drinks”, “energy tonics”) and “energy shots” (“energy charges”).

As a medicine, caffeine is included in the List of Vital and Essential Medicines Russian Federation(RF). The instructions for medical use of the drug caffeine sodium benzoate (international nonproprietary name - caffeine) list the following readings: decreased mental and physical performance, drowsiness, headache of vascular origin (including migraine), moderate arterial hypotension, respiratory depression (including in mild poisoning with narcotic analgesics and hypnotics, carbon monoxide, with asphyxia of newborns), restoration of pulmonary ventilation after use general anesthesia, ciliochoroidal detachment in adults.

The State Register of Medicines of the Russian Federation contains 127 records of medicines (mostly combined) containing caffeine for the treatment of acute respiratory diseases, influenza, cough, migraine, convulsions, vomiting, and to improve cerebral and peripheral circulation.

Found caffeine in cosmetology wide application as active component for the treatment of cellulite, mesotherapy, in makeup products, to stimulate blood circulation in the skin and hair growth (shampoos, creams, biologically active additives). In addition, caffeine is used in sports medicine for weight loss and as a doping agent. 74% of elite level athletes report consuming caffeine before competition. During competitions, the International Olympic Committee limits the use of caffeine by athletes, fixing it to the limit permissible level in urine - 12 mcg/ml.

Contraindications for the medical use of caffeine sodium benzoate include: hypersensitivity (including to other xanthines), anxiety disorders(agoraphobia, panic disorders), organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis), paroxysmal tachycardia, frequent ventricular extrasystole, arterial hypertension, sleep disorders, childhood up to 12 years of age (for the treatment of fatigue, drowsiness), children up to 18 years of age (for subconjunctival administration); with caution: glaucoma, increased excitability, elderly age, epilepsy and tendency to seizures, pregnancy and lactation.

Main effect of caffeine- stimulation of the central nervous system (CNS). Let us consider the mechanism of this effect of caffeine in a simplified form. The main target of the action of caffeine in physiologically significant concentrations is adenosine receptors - caffeine, showing affinity for the latter, blocks them for interaction with adenosine (it is generally accepted that caffeine is a competitive antagonist of adenosine, interacting with the A1 and A2a receptors). The effect of adenosine itself in relation to the central nervous system is manifested through interaction with adenosine receptors of neurons and consists in slowing down (“inhibiting”) the release of mediators that transmit nerve impulses from one nerve cell to another. This is the calming (“inhibiting”) effect of adenosine on the body (without the calming and controlling effects of adenosine nerve cells continue to get excited quickly). Thus, caffeine, by blocking the effect of adenosine, has a stimulating effect on the central nervous system.

You can learn more about the mechanisms and effects of adenosine on the central nervous system by reading:

1. article “Adenosine and P1-purinergic receptors of the central nervous system” Yu.V. Kiselevsky, N.A. Oganesyan, Grodno State Medical University (Journal of the State Medical University No. 1 - 2003) [read];

2. patent for invention (Medicinal product intended for the treatment or prevention of diseases associated with adenosine receptors associated with the adenosine A2a receptor) [read].

In addition to the above, caffeine also stabilizes transmission at dopaminergic synapses (psycho-stimulant properties), in beta-adrenergic synapses of the hypothalamus and medulla oblongata (increased tone of the vasomotor center), in cholinergic synapses of the cortex (activation of cortical functions) and medulla oblongata (excitation of the respiratory center) , in noradrenergic synapses (increased physical activity, anorexia).

Note! With prolonged use of caffeine, “new” adenosine receptors are formed in neurons and the effect of caffeine gradually decreases (as an adaptation to the decrease in adenosine receptors not blocked by caffeine). However, with a sudden cessation of caffeine administration, adenosine occupies all available receptors (including newly formed ones), which can lead to increased inhibition with symptoms of fatigue, drowsiness, depression, etc.

results epidemiological studies, obtained primarily from healthy adults, indicate a wide range of sensitivity to caffeine in the population, which may be associated with polymorphisms of genes (see below) involved in the pharmacodynamics and pharmacokinetics of caffeine. Caffeine and especially its water-soluble salts, after ingestion, are quickly and almost completely (99%) absorbed from the gastrointestinal tract (mainly in the intestines). The rate of absorption of caffeine increases with increasing dose, and no significant effect first pass. Caffeine absorption is not affected by either gender differences or genetic features, no liver disease, no food intake, no medications, including alcohol. After administration of a single oral dose of caffeine (4 mg/kg), the maximum concentration (Cmax) of caffeine is determined in the blood plasma after 15 - 45 minutes and persists for about 2 hours. When caffeine is consumed in doses of 1 to 2 mg/kg, its concentration in a person’s blood reaches values ​​from 1 to 2 μg/ml; when doses of 3 to 5 mg/kg are consumed, the concentration of caffeine in the serum becomes 5 μg/ml. Achievement and retention of Cmax of caffeine after oral and intravenous administration of the drug are approximately the same.

It is believed that most regular caffeine users titrate their intake to maintain plasma caffeine levels that maximize the beneficial effects (increased mental performance, faster reaction time, increased motor activity, reduction of fatigue and drowsiness) and minimize the negative ones, opposite to those that caffeine initially causes (feeling tired, drowsiness, headache, nausea, rarely vomiting, etc.), that is, associated with withdrawal symptoms. Behavioral effects of caffeine (eg, increased cognition, alertness, reaction time) have been observed in some subjects as early as 10 mg.

Depending on the variety and degree of processing of the coffee beans, one cup of natural coffee contains from 60 to 120 mg of caffeine, and the same cup of instant coffee contains from 40 to 80 mg. The lethal dose of caffeine is 10 g. This amount is contained in 100 cups of coffee.

Caffeine content in various products:

Type of coffee - mg caffeine:

■ European - 115 - 175;
■ black - 80 - 135;
■ soluble - 65 - 100;
■ black, decaffeinated - 3 - 4;
■ instant, decaffeinated - 2 - 3.

■ cold - 70;
■ black - 60;
■ black, U.S. - 40;
■ soluble - 30.

Product – weight (g) - mg of caffeine:

■ chocolate with filling - 28g - 15;
■ 3 teaspoons (“topped”) of chocolate powder ~225g - 8;
■ 2 tablespoons of chocolate syrup ~225g - 5;
■ 1 package (serving) cocoa ~225g - 5.

■ Mountain Dew - 54.0;
■ Canada Mountain Dew - 0;
■ Coca-Cola - 45.6;
■ Diet Cola - 45.6;
■ Shasta Cherry Cola - 44.4;
■Dr. Pepper - 39.6;
■ Pepsi Cola - 38.4;
■ Diet Pepsi - 36.0;
■ RC Cola - 36.0;
■ Diet RC - 36.0;
■ 7 Up - 0.

98% of caffeine undergoes biotransformation in the liver (demethylated, oxidized) with the formation of metabolites (paraxanthine, theobromine, theophylline, 1,3,7-trimethyluric acid, 1-methylxanthine, 1-methyluric acid, 5-acetylamino-6-formylamino-3- methyluracil, 1,7-dimethyluric acid). The main metabolite of caffeine in the human body (70 - 80%) is paraxanthine (1,7-dimethylxanthine).

The half-life (T1/2) of caffeine in healthy adult non-smokers is on average 4 - 5 hours, in pregnant women 10 - 20 hours, in full-term newborns - about 80 hours, in premature infants - 97.5 hours, in a child of 7 months of age reaches the values ​​of an adult, in children 6 - 13 years old - 2.3 hours. Compared to caffeine, paraxanthine, theobromine and theophylline have a longer T1/2. Caffeine and its metabolites are excreted primarily by the kidneys, unchanged in adults - about 1 - 3%, in newborns - about 85%.

The major caffeine-metabolizing enzymes include cytochrome P450 isoenzyme 1A2 (CYP1A2), N-acetyltransferase 2 (NAT2), and xanthine oxidase (XO), the activity of which can be determined by measuring levels of caffeine metabolites in urine. In humans, the CYP1A2 enzyme is encoded by the CYP1A2 gene. The CYP1A2 gene is located on chromosome 15, locus 15q24.1. The expression and activity of CYP1A2 (and, accordingly, sensitivity to caffeine and the volume of its consumption) can differ significantly (10 - 200 times) in different people, which reflects genetically determined differences in constitutive and/or inducible expression of the CYP1A2 gene. About 10% of the general population are carriers of a gene with increased enzymatic activity, or "rapid" caffeine metabolizers, who are likely to consume more than 400 mg of caffeine per day, while people with the CYP1A2 gene, which encodes normal activity, are "slow" caffeine metabolizers, and who typically consume less than 100 mg of caffeine per day.

Under the influence of various factors, the genetically determined activity of CYP1A2 can change, slowing or accelerating the metabolism of caffeine. Induction of CYP1A2 activity has been described due to exposure to tobacco smoking, dietary factors (polyaromatic hydrocarbons produced by grilling meats), certain drugs (rifampicin, inhibitors proton pump) etc. It was shown that daily consumption three cups of coffee increases CYP1A2 activity, and therefore heavy coffee drinkers have higher CYP1A2 activity compared to light coffee drinkers. In diseases associated with chronic hepatitis, an increase in the activity of CYP1A2 was observed, and in cirrhosis, its decrease was observed. Quinolone antibiotics, carbamazepine, isoniazid, alcohol, fluvoxamine, sertraline, paroxetine, grapefruit juice, ginger, cruciferous vegetables are inhibitors of CYP1A2 activity; as a result of their use, the metabolism of caffeine is slowed down, and the half-life of caffeine is prolonged. A decrease in the clearance (removal from the body) of caffeine was noted in women using oral contraceptives, in contrast to women who do not take oral contraceptives.

Caffeine and pain. Caffeine, as an adjuvant, is widely used in combination painkillers, for example, Caffetin, Coldrex, Plivalgin, Solpadeine, Pentalgin, Sedalgin, Trimol, Citramon, Citropak, etc. (a drug that is added to a medicine to improve its action is called an adjuvant [auxiliary]). It has been established that caffeine contains combination drug, affecting the lipoxygenase pathway arachidonic acid, promotes a moderate increase in anti-inflammatory activity (and therefore helps reduce the severity of pain). Besides, therapeutic effect caffeine is due to inhibition of phosphodiesterase, which inactivates the secondary messenger - cAMP. As a result, the concentration of calcium ions in smooth muscles changes, which is accompanied by dilation of cerebral vessels.

Caffeine is often used in over-the-counter combination pain relievers. It is believed that the addition of caffeine to commonly used analgesics such as paracetamol, ibuprofen, acetylsalicylic acid helps to increase the analgesic effect. However, evidence to support this is limited and often based on inadequate comparative studies. However, evidence to support this is limited and often based on inadequate comparative studies. In this regard, the authors of a new systematic review of the Cochrane Collaboration, “Caffeine for enhancing the effect of analgesics in acute pain in adults” (Derry C.J. et al., 2012), assessed the analgesic effect of an analgesic + caffeine combination compared with that of an analgesic at the same dose in acute pain. pain syndrome. Through a comprehensive search of published and unpublished results of relevant clinical trials, the authors identified and included data from 19 randomized, double-blind trials in the systematic review. clinical trials(7238 participants) of adequate methodological quality. Most studies used paracetamol or ibuprofen, and the caffeine dose was 100 - 130 mg. The studies involved patients with tension-type headaches and migraines, pain syndrome after dental surgery, episiotomy and childbirth, as well as with algodismenorrhea, acute pain in the throat (tosillopharyngitis). As the main assessments of the analgesic effectiveness of interventions, the review authors used the number of patients who achieved a reduction in the severity of pain by at least 50% of the maximum possible within 4 - 6 hours, or assessed the effectiveness of treatment as good or excellent, or noted the absence of headache after 2 hours A pooled analysis of the data found a small but statistically significant increase in the analgesic effect of analgesics when caffeine was added at a dose of ≥100 mg (approximately the amount found in a cup of coffee). This effect was independent of the pathological condition causing the pain syndrome or the analgesic used. As a result of adding caffeine to the analgesic, a good level of analgesia (at least 50% of the maximum possible) was achieved in an additional 5 - 10% of participants; resulting in an NNT of around 15. In context this review NNT (Number Needed to Treat) is the number of patients with acute pain syndrome who must be treated with an analgesic + caffeine combination to achieve a good level of analgesia in 1 patient. Thus, the use of caffeine (≥100 mg) in combination with commonly used analgesics (paracetamol or ibuprofen) provides a small (5-10%) but significant increase in the proportion of patients with acute pain syndrome who can achieve a good level of analgesia (Derry C.J. , Derry S., Moore R. A. (2012) Caffeine as an analgesic adjuvant for acute pain in adults. Cochrane Database of Systematic Reviews 2012, Issue 3. Art. No.: CD009281. DOI: 10.1002/14651858.CD009281.pub2).

It should be noted that caffeine has complex, often opposing effects on cardiovascular system. By stimulating the vasomotor center, caffeine increases vascular tone, and with a direct effect on vascular smooth muscles, it reduces their tone, which should lead to a decrease in blood pressure (BP). Thus, caffeine has ambiguous effects on different vascular regions and on blood pressure, since they depend on the cardiotropic, central and direct vascular effects of the drug. For example, coronary vessels most often expand due to a direct antispasmodic effect. At the same time, the cerebral vessels are somewhat toned. The latter seems to explain beneficial influence caffeine for migraines. Currently there are only a few completed clinical researches who studied the relationship between coffee consumption and changes in cerebral circulation. Yu.V. Bardik, E.A. Seredenko (1985) showed that with normal blood pressure caffeine causes dilation of blood vessels in the brain. Intravenous administration caffeine as a vasodilator has been successfully used for cerebral circulatory disorders such as vasospasms, thrombosis, and cerebrovascular insufficiency. However, some authors classify caffeine as a drug that has a vasoconstrictor effect on cerebral vessels, which largely explains the beneficial effect of caffeine on migraine.

more details in the article “The influence of caffeine on cerebral circulation” by I.V. Kozachuk, magazine “Bulletin of Tambov University. Series: natural and technical sciences", vol. 15, issue 1, 2010 [read]

Caffeine as a neuroprotector. It is well known that coffee temporarily speeds up thought processes. There are studies showing the long-term effects of coffee on mental activity. A study published in the Journal of Alzheimer's Disease found that patients with mild cognitive impairment and plasma caffeine levels >1200 ng/mL (allowed 3 to 5 cups of coffee per day) did not progress to dementia over the next 2 to 4 years. Related studies in mice show that caffeine inhibits enzymes involved in the formation of beta-amyloid, while coffee consumption increases levels of granulocyte colony-stimulating factor, interleukin-10 and interleukin-6, and cytokines also contribute to the above-described properties. Caffeinated coffee has long been considered a neuroprotective agent for the treatment of Parkinson's disease, and modern research suggest that changes in the GRIN2A gene, which encodes glutamate receptors, influence the risk of developing Parkinson's disease in people who drink coffee. Additionally, data presented this year at the annual meeting of the American Academy of Neurology showed that drinking 3 cups of coffee per day prevents the formation of preclinical Lewy bodies. pathological changes in Parkinson's disease. Despite promising results in neurodegenerative diseases, caffeine intake has also been associated with a decreased age at onset of Huntington's disease.

Coffee as an antidepressant. A 2011 study shows that increasing coffee consumption may also benefit our health. mental health: Women who drank 2 to 3 cups of coffee per day had a 15% lower risk of developing depression compared to those who drank less than 1 cup per week. A 20% reduction in risk was observed among those who drank 4 cups or more of coffee per day. Coffee's short-term effects on mood may be due to changes in serotonin and dopamine activity, although the mechanisms underlying its possible long-term effects on mood are likely related to its antioxidant and anti-inflammatory properties, which play a role in the development of depressive disorders. .

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