Caffeine indications. Medicinal reference book geotar. Pharmacological group of the substance Caffeine

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 a synthetic drug derived 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 may also increase arterial pressure, but this happens more often in states of shock or collapse. In small doses, caffeine provides a stimulating effect; in large doses, depression often occurs. nervous system. 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. At 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 an infectious process), asphyxia, asthenia, enuresis (including in children), migraines, to relieve cerebral vascular spasms. 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 stable trend recent years has become an application 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 to be an effective 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 of the psychostimulant "Caffeine Benzoate" do not recommend prescribing it 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 for children under 12 years of age and elderly people. and 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 of the 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. With long-term use, addiction and 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 of 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, slowing of intrauterine development, inhibition or disturbances in skeletal development, and arrhythmia in the fetus. During the lactation period, caffeine penetrates into breast milk and, accumulating, threatens insomnia in the baby and its 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.

Analogs

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.

Name:

Caffeine sodium benzoate (Coneinum natrii-benzoas)

Pharmacological
action:

Psychostimulant and analeptic agent, a methylxanthine derivative.
Competitively blocks central and peripheral A1 and A2 adenosine receptors.
Inhibits the activity of PDE in the central nervous system, heart, smooth muscle organs, skeletal muscles, adipose tissue, promotes the accumulation of cAMP and cGMP in them (this effect is observed when used only in high doses).
Stimulates the centers medulla oblongata(respiratory and vasomotor), as well as the n.vagus center, has a direct stimulating effect on the cerebral cortex.
In high doses facilitates interneuronal conduction in spinal cord , enhancing spinal reflexes.
Increases mental and physical performance, stimulates mental activity, motor activity, shortens reaction time, temporarily reduces fatigue and drowsiness.
In small doses, the stimulating effect predominates, and in large doses, the effect of depression of the nervous system predominates.
Speeds up and deepens breathing.
Usually has a positive foreign-, chrono-, batmo- and dromotropic effect(since the effect on the cardiovascular system consists of a direct stimulating effect on the myocardium and a simultaneous stimulating effect on the n.vagus centers, the resulting effect depends on the predominance of one or another action).

Stimulates the vasomotor center and has a direct relaxing effect on the vascular wall, which leads to dilation of the vessels of the heart, skeletal muscles and kidneys, while the tone of the cerebral arteries increases (causes a narrowing of the blood vessels in the brain, which is accompanied by a decrease in cerebral blood flow and oxygen pressure in the brain).
Blood pressure changes under the influence of vascular and cardiac mechanisms of caffeine's influence: with normal initial blood pressure, caffeine does not change or slightly increases it, and with arterial hypotension it normalizes it.
It has an antispasmodic effect on smooth muscles (including a bronchodilator effect), and a stimulating effect on striated muscles.
Increases secretory activity of the stomach.
It has a moderate diuretic effect, which is due to a decrease in the reabsorption of sodium and water ions in the proximal and distal renal tubules, as well as dilation of renal vessels and increased filtration in the renal glomeruli.
Reduces platelet aggregation and histamine release from mast cells.
Increases basal metabolism: increases glycogenolysis, increases lipolysis.

Indications for
application:

Infectious and other diseases accompanied by depression of the central nervous system and of cardio-vascular system(acute heart failure);
- respiratory depression;
- asphyxia;
- poisoning with drugs and other poisons that depress the central nervous system;
- asthenic syndrome;
- spasms of cerebral vessels;
- to increase mental and physical performance, eliminate drowsiness;
- used in children for enuresis.

Mode of application:

Inside And PC.
Doses are set individually, frequency of administration is no more than 2–3 times a day.
A single dose for adults is usually 1 ml of 10 or 20% solution; children are prescribed (depending on age) 0.25–0.1 ml of 10% solution.
Higher doses for adults for parenteral use: single - 0.4 g, daily - 1 g; when taken orally: single dose - 0.5 g, daily - 1.5 g.
It can be used as mono- or as part of combination therapy.

Side effects:

From the side of the central nervous system: sleep disturbance, agitation, anxiety; With prolonged use, addiction is possible.
From the cardiovascular system: tachycardia, increased blood pressure, arrhythmias.
From the digestive system: nausea, vomiting.

Contraindications:

Increased excitability;
- insomnia;
- severe hypertension;
- atherosclerosis;
- organic diseases of cardio-vascular system;
- old age;
- glaucoma;
- during therapy increased fatigue and drowsiness - children under 12 years of age.
Carefully during pregnancy and lactation.

Interaction
other medicinal
by other means:

When used simultaneously, the effect decreases sleeping pills and drugs for anesthesia.
With simultaneous use, it is possible to enhance the effect of analgesics-antipyretics, salicylamide, naproxen.
With the simultaneous use of estrogens (hormonal contraceptives, HRT agents) possible increase in intensity and duration of caffeine action due to inhibition of the CYP1A2 isoenzyme by estrogen.
When administered concomitantly with adenosine, caffeine reduces the increased heart rate and blood pressure changes caused by adenosine infusion; reduces vasodilation caused by the action of adenosine.
With simultaneous use, it is possible to increase bioavailability, absorption rate and plasma concentration acetylsalicylic acid.

With simultaneous use of mexiletine reduces caffeine clearance and increases its plasma concentrations, apparently due to the inhibition of caffeine metabolism in the liver by mexiletine.
Methoxsalen reduces the excretion of caffeine from the body with a possible increase in its effect and the development of toxic effects.
Due to the induction of microsomal liver enzymes under the influence of phenytoin during its simultaneous use Metabolism and elimination of caffeine are accelerated.
Fluconazole and terbinafine cause a moderate increase in the concentration of caffeine in the blood plasma, ketoconazole - less pronounced.
The most pronounced increase in AUC and decrease in clearance are observed with simultaneous use of caffeine with enoxacin, ciprofloxacin, pipemidic acid; less pronounced changes - with pefloxacin, norfloxacin, fleroxacin.
When used simultaneously, caffeine accelerates the absorption of ergotamine.

Pregnancy:

Given the slow elimination of caffeine from the fetus, its use during pregnancy is possible only after assessing the benefit/risk ratio for the mother and fetus.
Excessive use caffeine during pregnancy can lead to spontaneous abortions, slowing of intrauterine development of the fetus, arrhythmia in the fetus; There may be disturbances in skeletal development when using large doses and a slowdown in skeletal development when using lower doses.
Caffeine and its metabolites pass into mother's milk in small quantities, but accumulate in infants and can cause hyperactivity and insomnia.
If it is necessary to use it during lactation, the benefit/risk ratio for the mother and child should be assessed.

Overdose:

Symptoms: gastralgia, agitation, anxiety, agitation, restlessness, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensitivity, tremor or muscle twitching; nausea and vomiting, sometimes with blood; ringing in the ears, epileptic seizures (in case of acute overdose - tonic-clonic).
Caffeine in doses of more than 300 mg/day (including against the background of coffee abuse - more than 4 cups of natural coffee, 150 ml each) can cause anxiety, tremor, headache, confusion, extrasystole.
In newborns (including premature infants), at a plasma caffeine concentration of 50 mg/ml, toxic effects are possible: anxiety, tachypnea, tachycardia, tremor, painful, bloated abdomen or vomiting, increased Moro reflex, and at higher concentrations - convulsions.
Treatment: gastric lavage if caffeine was taken in the last 4 hours at a dose of more than 15 mg/kg and there was no vomiting caused by caffeine; reception activated carbon, laxatives; for hemorrhagic gastritis - administration of antacid drugs and gastric lavage with an ice-cold 0.9% NaCl solution; maintaining pulmonary ventilation and oxygenation; for epileptic seizures - intravenous diazepam, phenobarbital or phenytoin; maintaining fluid and salt balance.
Hemodialysis, in newborns, if necessary, exchange blood transfusion.

Included in the preparations

Included in the list (Order of the Government of the Russian Federation No. 2782-r dated December 30, 2014):

VED

ATX:

N.06.B.C.01 Caffeine

Pharmacodynamics:

Antagonism of central adenosine receptors, stimulation of the medulla oblongata centers (vagal, vasomotor and respiratory).

Stimulates the central nervous system, respiration, skeletal muscles, secretion of pepsin and hydrochloric acid in the gastrointestinal tract, glycogenolysis. Increases sensitivity respiratory center to the stimulating effect of carbon dioxide, increasing alveolar ventilation.

Increases the strength and frequency of heart contractions, cardiac output (positive inotropic effect on the myocardium and positive chronotropic effect to the sinoatrial node).

It has hypertensive and diuretic effects, stimulates cerebral vasoconstriction and reduces uterine contractility.

Pharmacokinetics:

The binding to plasma proteins is 25-36%. Biotransformation in the liver, in adults 80% of caffeine is metabolized into paraxanthine (1,7-dimethylxanthine), 10% into theobromine (3,7-dimethylxanthine) and 4% into (1,3-dimethylxanthine), compounds are demethylated into monomethylxanthines, and then into methylated derivatives uric acid. In premature babies it turns into. The half-life is 3-7 hours, in newborns - 65-130 hours, decreasing to adult levels at 4-7 months. Maximum concentration after 50-75 minutes. Excreted by the kidneys (in the form of metabolites, 1-2% unchanged), in newborns by the kidneys (85% unchanged).

Indications:

Diseases accompanied by depression of the cardiovascular and respiratory systems (including drug poisoning, infectious diseases).

CNS depression.

Spasms of cerebral vessels (including migraine).

Decreased mental and physical performance.

Enuresis in children.

Drowsiness.

Respiratory disorders (periodic breathing, idiopathic apnea) in newborns.

V.F50-F59.F51.1 Drowsiness [hypersomnia] of non-organic etiology

IX.I70-I79.I73 Other peripheral vascular diseases

VI.G40-G47.G43 Migraine

XVIII.R30-R39.R32 Urinary incontinence, unspecified

XVIII.R50-R69.R53 Malaise and fatigue

XIX.T36-T50.T40 Poisoning with drugs and psychodysleptics [hallucinogens]

XXI.Z70-Z76.Z73.6 Restrictions in activity caused by reduction or loss of ability to work

Contraindications:

Individual intolerance, including to other xanthines.

Anxiety disorders(agoraphobia, panic disorder).

Organic diseases of the cardiovascular system (including acute heart attack myocardium, atherosclerosis).

Paroxysmal tachycardia, frequent ventricular extrasystole.

Arterial hypertension.

Sleep disturbances in the treatment of increased fatigue and drowsiness.

Childhood up to 12 years old.

Carefully:

Glaucoma.

Increased excitability.

Elderly age.

Epilepsy and tendency to seizures.

Pregnancy and breastfeeding.

Pregnancy and lactation:

FDA category C recommendations. Increased risk of spontaneous abortion, intrauterine growth retardation, fetal arrhythmia (high doses). Animal experiments: disturbance of skeletal development (fingers and individual phalanges) when using doses equivalent to the caffeine content of 12-24 cups of coffee per day, throughout pregnancy or with a single administration of large doses (50-100 mg/kg); in smaller doses - slowing down skeletal development.

Penetrates into breast milk (1% of its concentration in the mother's blood plasma). If a nursing mother drinks 6-8 cups of caffeine-containing drinks per day, the baby may develop hyperactivity and insomnia.

Directions for use and dosage:

Inside (regardless of food intake): adults - 0.05-0.1 g per dose 2-3 times a day (maximum daily dose- 1 g), children over 2 years old - 0.03-0.075 g per dose.

P for migraines (often in combination with non-narcotic analgesics and ergot alkaloids) - 1-2 tablets during an attack of pain, then 1 tablet 2-3 times a day for several days (up to 1 month).

It is administered in the form of caffeine sodium benzoate subcutaneously: adults - 1 ml of 10% or 20% solution, children - 0.25-1 ml of 10% solution. To eliminate apnea in newborns - administered orally or intravenously(in the form of caffeine citrate), creating a concentration of caffeine base in the blood plasma from 3 to 10 mg/ml.

Side effects:

Nervous system: dizziness, headache, anxiety, irritability, nervousness, severe nervous excitement in newborns; tremor, sleep disturbance, muscle tension.

The cardiovascular system: cardiopalmus.

Digestive system: diarrhea, nausea, vomiting, necrotizing enterocolitis.

Blood: hypoglycemia, hyperglycemia.

Overdose:

In case of overdose, pain in the abdomen or stomach is observed; agitation, anxiety, agitation or restlessness; confusion or delirium; dehydration; tachycardia, arrhythmia; frequent urination; headache; increased tactile or pain sensitivity; irritability; tremors or muscle twitching; nausea and vomiting, sometimes with blood; a painful, swollen belly or vomiting in newborns; ringing in the ears or sensation of other sounds; photopsia; epileptic seizures, usually clonic-tonic convulsions in acute overdose; sleep disturbance; trembling of the whole body in newborns.

Treatment is symptomatic - gastric lavage, if taken in the last 4 hours at a dose of more than 15 mg/kg and there was no vomiting caused by caffeine; , laxatives; for hemorrhagic gastritis - administration of antacids medicines and gastric lavage with ice-cold 0.9% sodium chloride solution; maintaining pulmonary ventilation and oxygenation; for epileptic seizures - intravenously, - arrhythmias or severe hypertension (large doses); increased blood pressure and tachycardia (small doses).

Special instructions:

Sudden cessation of use may lead to increased inhibition of the central nervous system (drowsiness, depression).

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

Due to the fact that the effect of caffeine on blood pressure consists of vascular and cardiac components, as a result, both the effect of stimulating the heart and inhibition (weak) of its activity can develop.

For apnea in newborns and children infancy V postoperative period(prevention) either caffeine citrate is used, but not caffeine sodium benzoate. Excessive consumption during pregnancy can lead to spontaneous abortions, slowing of intrauterine development of the fetus, arrhythmia in the fetus; There may be disturbances in skeletal development when using large doses and a slowdown in skeletal development when using lower doses. Passes into breast milk in small quantities, but accumulates in infants and can cause hyperactivity and insomnia.

Instructions


Caffeine is probably the most well-known remedy for helping fight fatigue. It is a strong psychostimulant that excites the nervous system. Caffeine is found in many medications, energy drinks and tonic drinks. Sodium caffeine benzoate is a methylxanthine derivative. When it enters the body, it acts as a kind of brake on the activity of PDE enzymes - phosphodiesterases in adipose tissues, major organs, the central nervous system, and the heart. Also, in high doses it accumulates in the form of cAMP and cGMP, special derivatives of adrenaline. The synthetic drug we are considering, available in tablets, is made from coffee seeds and tea leaves.

What is caffeine used for?


When using the product, you should remember that small doses stimulate the nervous system, and large doses depress it. It is taken to:
  • increase mental excitability;
  • improve mood;
  • reduce fatigue and delay its occurrence;
  • concentrate attention;
  • activate the fat burning process;
  • stimulate the release of more adrenaline;
  • increase muscle activity, maintain muscle membrane potential, accelerate calcium metabolism;
  • allow muscles to more actively use such a food source as triglyceride during particularly intense training.
Usually, after consuming it, breathing quickens, becomes deeper, arterial tone increases and blood vessels dilate. The low pressure in the arteries returns to normal and may even increase slightly. The medication promotes the production of gastric juice, has a weak diuretic effect, dilates blood vessels in the kidneys, which increases filtration and slows down the process of platelet aggregation.

Instructions for using caffeine tablets


According to the instructions from the manufacturer and according to experts, you can drink this product throughout the day. The only exception is the evening for highly excitable people and the time before bed. Since after using this medicine it will be difficult to fall asleep. As for the dosage:
  1. Adults and adolescents can take the drug three times a day, 50–100 mg. A course of treatment from two weeks to three months will help improve performance and eliminate drowsiness.
  2. If you need to fix sudden attack headache and prevent its recurrence, then children over twelve years of age and adult patients are advised to drink 50–100 mg of the drug twice a day for three days.
  3. In the case of use of the drug for the treatment of hypertension, it is recommended to take 50-100 mg for 2-3 weeks a day three times.
In order to avoid the unpleasant consequences that usually accompany an overdose, it is imperative not to exceed the maximum permissible daily norm. Maximum dose, which can be taken at a time is 300 mg; you can drink no more than 1000 mg per day.

Caffeine for weight loss


This drug is quite popular in the fight against excess weight, people speak positively about it. It allows you to achieve quite good results, especially if you take it while following a certain diet and exercising. It is known that the dose recommended for stimulating the nervous system will not be very effective for weight loss. To make the extra pounds go away, it is increased. In order for the heart to work faster and metabolic processes to become more intense, you should take the medication no more than once a day before training. When using, follow these rules:
  1. Before every regular physical activity drink 9–20 mg per kilogram of weight.
  2. For greatest effectiveness, take the product half an hour before classes.
To avoid undesirable consequences, but also to see the result, before starting the course you should consult a doctor or professional nutritionist. Today, doctors generally advise starting a course with 2-3 milligrams of sodium caffeine benzoate per kilogram of body weight, gradually increasing the norm and monitoring your well-being.

Side effects and contraindications of caffeine tablets


Before starting the full course, you should carefully monitor your reaction to the first use. If no negative consequences occur, then you do not have hypersensitivity or allergies to the components and you can continue therapy. TO side effects include:
  • feeling of anxiety, groundless worry;
  • headache;
  • dizziness;
  • sleep disturbances, nightmares, general insomnia;
  • fatigue and feeling unwell;
  • nausea and vomiting;
  • nasal congestion;
  • exacerbation of gastritis.
If you are in the middle of a course, abruptly canceling it can lead to fatigue, depression, and slow reactions.

This medicine should not be used if:

  • diseases of an acute and chronic nature in the heart and blood vessels;
  • problems with sleep and excessive excitability;
  • anxiety, regular stress;
  • high blood pressure;
  • allergies and caffeine intolerance;
  • paroxysmal tachycardia.
It is not recommended for children under 12 years of age and is advised to be used with caution by older people who have eye diseases, signs of epilepsy, or a tendency to seizures or convulsions. Nursing mothers and pregnant women at any stage can drink this product only with medical prescription.

Combination of caffeine with other drugs and substances


In general, these tablets combine well with various medications, without affecting their properties in any way and maintaining their own, but there are some exceptions:
  • Together with oral contraceptives, the activity of contraceptives remains the same, but caffeine decreases. It accumulates in the blood and is eliminated by the liver much more slowly.
  • It should not be consumed with coffee or other substances that excite the central nervous system. This can lead to overstimulation.
  • Calcium with a simultaneous course, it is less absorbed in the stomach, which reduces its effectiveness.
  • Sleeping pills and narcotic substances in combination with caffeine-sodium benzoate give less effect. Thanks to it, cardiac glycosides are more actively absorbed, and lithium is excreted in the urine.
If for any reason you have an overdose or notice unpleasant consequences from use, doctors advise urgently flushing your stomach, drinking a laxative, then a large number of activated carbon, it will help remove the drug from the body.

The price of caffeine in tablets in Russia is 70 rubles, and in Ukraine on average 20 hryvnia. More information about the stimulator in the video below:

Breathing stimulants Psychostimulants General tonics and adaptogens

Pharmacological properties

psychostimulant, analeptic, cardiotonic.

It has a direct stimulating effect on the central nervous system: it regulates and enhances excitation processes in the cerebral cortex, respiratory and vasomotor centers, activates positive conditioned reflexes and motor activity. Stimulates mental activity, increases mental and physical performance, shortens reaction time. After administration, vigor appears, fatigue and drowsiness are temporarily eliminated or reduced. Causes increased and deepening of breathing, especially against the background of depression of the respiratory center. Affects the cardiovascular system: increases strength and heart rate (especially in large doses), increases blood pressure during hypotension (does not change normal). Dilates the bronchi, biliary tract, blood vessels skeletal muscles, heart, kidneys, constricts - organs abdominal cavity(especially when they are dilated). Reduces platelet aggregation. It has a moderate diuretic effect, mainly due to a decrease in the reabsorption of electrolytes in the renal tubules. Stimulates the secretion of gastric glands. Increases basal metabolism, enhances glycogenolysis, causing hyperglycemia.

Blocks central and peripheral adenosine receptors. Promotes the accumulation of cAMP and cGMP by inhibiting the activity of phosphodiesterases involved in their inactivation. IN to a greater extent inhibits cAMP phosphodiesterase (not only in the central nervous system, but also in the heart, smooth muscle organs, adipose tissue, skeletal muscles). Stabilizes transmission in dopaminergic synapses (psychostimulating properties), beta-adrenergic synapses of the hypothalamus and medulla oblongata (increased tone of the vasomotor center), cholinergic synapses of the cortex (activation of cortical functions) and medulla oblongata (excitation of the respiratory center), noradrenergic synapses (increased physical activity, anorexia).

Caffeine and its water-soluble salts are well absorbed in the intestine (including the colon). T1/2 is about 5 hours, in some individuals - up to 10 hours. The main part is demethylated and oxidized. About 10% is excreted unchanged by the kidneys. In the body of full-term newborns and infants (1.5–2 months) it is eliminated more slowly (T1/2 - from 80 to 26.3 hours, respectively).

The effect on higher nervous activity largely depends on the dose and type of the patient’s nervous system. In small doses the stimulating effect predominates, in large doses the depressing effect predominates. In older people, the effect on sleep is more pronounced: its onset slows down, the total time of sleep decreases, and the frequency of awakenings increases (possibly due to faster metabolism of catecholamines in the central nervous system). In premature infants, when eliminating periodic breathing, caffeine reduces the partial pressure of carbon dioxide, the concentration of H+ in the blood and at the same time increases the volume of ventilation without changing heart rate.

Caffeine - indications for use

Diseases accompanied by depression of the central nervous system, functions of the cardiovascular and respiratory systems (including drug poisoning, infectious diseases), cerebral vascular spasms (including migraine), decreased mental and physical performance, drowsiness, enuresis children, breathing disorders (periodic breathing, idiopathic apnea) in newborns (including premature infants).

Contraindications

Expressed arterial hypertension, organic diseases of the cardiovascular system (including atherosclerosis), increased excitability, glaucoma, sleep disorders, old age.

Interactions with drugs

Reduces the effect of sleeping pills and narcotic drugs, increases (improving bioavailability) - acetylsalicylic acid, paracetamol and other non-narcotic analgesics. Improves the absorption of ergotamine in the gastrointestinal tract.

Caffeine - method of application and dosage

Inside (regardless of food intake). Adults - 0.05-0.1 g per dose 2-3 times a day (no more than 1 g per day), children over 2 years old - 0.03-0.075 g per dose; for migraine (often in combination with non-narcotic analgesics and ergot alkaloids) - 1–2 tablets. during an attack of pain, then - 1 tablet. 2–3 times a day for several days (up to 1 month). In the form of caffeine-sodium benzoate, it is administered subcutaneously: adults - 1 ml of 10% or 20% solution, children - 0.25–1 ml of 10% solution. To eliminate apnea in newborns, it is administered orally or intravenously (in the form of caffeine citrate), creating a concentration of caffeine base in the blood plasma from 3 to 10 mg/ml.

Side effects

Anxiety, agitation, insomnia, tachycardia, arrhythmias, increased blood pressure, nausea, vomiting. With long-term use, slight addiction is possible (a decrease in the effect of caffeine is associated with the formation of new adenosine receptors in brain cells). Sudden cessation of caffeine administration may lead to increased central nervous system inhibition with symptoms of fatigue, drowsiness and depression.

Overdose

When abused, caffeine (more than 300 mg per day, i.e. four 150 ml cups of natural coffee) can cause anxiety, restlessness, tremors, headache, confusion, and cardiac extrasystoles. In newborns (including premature infants), at a blood plasma concentration of 50 mg/ml, toxic effects are possible: anxiety, tachypnea, tachycardia, tremor, increased Moro reflex, and at higher concentrations - convulsions.