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Caffeine sodium benzoate, 100 mg, tablets, 10 pcs.

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 it has a positive ino-, chrono-, bathmo- 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 of 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; 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 the 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.

Publications in the media

(Coffeinum-natrii benzoas)

Synonyms.

Composition and release form. Powder, tablets of 0.075, 0.1 and 0.2 g; 10% and 20% solutions in ampoules of 1 and 2 ml and in syringe tubes of 1 ml.

Indications. Increased mental and physical performance; infectious and other diseases accompanied by inhibition of the functions of the central nervous system and cardiovascular system; poisoning with narcotic and other drugs that depress the central nervous system; drowsiness; hypotension; enuresis; migraine.

Pharmachologic effect. Caffeine sodium benzoate is a psychostimulant - a purine derivative. The neurochemical mechanism of action of drugs in this group is their ability to compete with adenosine for “purine” or adenosine receptors, which contributes to the development of a psychostimulating effect. Sodium caffeine benzoate in large doses inhibits phosphodiesterase, which leads to the accumulation of intracellular c-AMP, which enhances glycogenolysis, metabolic processes in muscle tissue and the central nervous system. The drug stimulates all parts of the central nervous system. Compared to amphetamine stimulants, the effect on the central nervous system is more “mild”. Sodium caffeine benzoate has a positive inotropic and chronotropic effect, causing an increase in the frequency and strength of heart contractions, and increases cardiac output.

In high doses, caffeine causes severe tachycardia, and in highly sensitive patients arrhythmias (ventricular extrasystoles) may develop. The action of caffeine has central and peripheral components regarding vascular tone. By stimulating the vasomotor center, caffeine increases vascular tone, and with a direct effect on smooth muscles, it reduces vascular tone. Caffeine increases systemic vascular resistance, which leads to increased blood pressure. These effects are associated with the drug's blockade of adenosine vasodilation and activation of the sympathetic division of the autonomic nervous system. The drug has a stimulating effect on skeletal muscles, possibly by inducing the release of acetylcholine, increasing the strength of contractions and relieving muscle fatigue. Caffeine sodium benzoate stimulates the secretion of hydrochloric acid by parietal marks and the activation of pepsin. The drug has a mild diuretic effect by increasing renal blood flow and glomerular filtration rate and reducing the reabsorption of sodium and water in the proximal renal tubules. Inhibits uterine contractility, increases the concentration of catecholamines in the blood plasma and urine, causes a short-term increase in plasma levels due to stimulation of glycogenolysis and lipolysis. The drug stimulates the respiratory center, increasing the breathing rate. In high doses, caffeine has analeptic properties.

Pharmacokinetics. The drug is easily absorbed from the gastrointestinal tract into the blood when taken orally or parenterally. Absorption of methylxanthines occurs mainly due to their lipophilicity rather than water solubility. Caffeine sodium benzoate is quickly distributed in all tissues of the body; easily penetrates the placental and blood-brain barriers; the volume of distribution in adults ranges from 0.4 to 0.6 l/kg. Binds to plasma proteins by 25-36%. The peak concentration of the drug in the blood plasma is observed 50-75 minutes after oral administration. Therapeutic concentrations in blood plasma are 5-25 mcg/ml (25.8-128.8 μmol/l). The drug is metabolized in the liver. About 80% of its dose is converted to paraxanthine (1,7-dimethylxanthine), about 10% to theobromine (3,7-dimethylxanthine), and about 4% to theophylline (1,3-dimethylxanthine). These compounds are further metabolized by demethylation to first form monomethylxanthines and ultimately methylated uric acid derivatives. T 1/2 averages 3-7 hours. The drug is excreted mainly in the form of metabolites by the kidneys, 1-2% is excreted unchanged.

Side effects. Dizziness; cardiopalmus; irritability, nervousness or severe nervous agitation; tremor; sleep disturbance; diarrhea, nausea, vomiting.

Contraindications. Increased excitability, insomnia; severe hypertension and atherosclerosis, organic diseases of the cardiovascular system; glaucoma.

Adverse reactions when interacting with other drugs. When taken concomitantly in large doses with MAO inhibitors, including procarbazine and selegiline, caffeine sodium benzoate may cause the development of dangerous cardiac arrhythmias or severe hypertension as a result of increased sympathomimetic effects of caffeine; small doses of caffeine-sodium benzoate may lead to a slight increase in blood pressure and tachycardia. With simultaneous use of the drug with other central nervous system stimulants, the development of hyperstimulation of the central nervous system, up to the development of arrhythmias and seizures, is possible. Concomitant use of barbiturates (phenobarbital) and caffeine sodium benzoate may increase caffeine metabolism due to barbiturate-induced induction of liver microsomal enzymes, leading to increased elimination of caffeine sodium benzoate. Cimetidine and OK reduce the metabolism of caffeine in the liver, which leads to an increase in its concentration in the blood and increased side effects of the latter.

Information for the patient. The drug is used orally in tablets of 0.1-0.2 g 2-3 times a day 30-40 minutes before meals. Do not take the drug immediately before bed. Extended-release capsules should be swallowed whole without breaking, crushing or chewing. It is not recommended to drink caffeine sodium benzoate with milk, as it is bound by 30% milk protein, and the release of caffeine from this binding is very slow. Smoking accelerates the metabolism of caffeine-sodium benzoate and reduces its therapeutic effects. Drinking large quantities of coffee with a high caffeine content in the drink (60 mg of caffeine per 100 g of drink), tea (50 mg per 100 g of drink), cola, cocoa and chocolate with preparations containing caffeine or caffeine-sodium benzoate may lead to tachycardia , increased breathing and dizziness. Closely monitor for signs indicating the occurrence of possible side effects, especially such as stimulation of the central nervous system and irritation of the gastrointestinal mucosa, dysfunction of the cardiovascular system.

Missed dose: Take the missed dose as soon as possible; do not take it at all if there is no time left before the next dose; do not take double doses.

Caffeine-sodium benzoate tablets 100 mg 10 pcs. in Magnitogorsk

Latin name

COFFEINE-BENSONATE SODIUM

International nonproprietary name

caffeine

Release form

Pills.

Package

10 pieces. — cellless contour packages. 10 pieces. — contour cellular packaging.

Description

Tablets are white, flat-cylindrical in shape, with a bevel.

pharmachologic effect

Psychostimulant and analeptic drug, a derivative of methylxanthine. 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 of the medulla oblongata (respiratory and vasomotor), as well as the n.vagus center, has a direct stimulating effect on the cerebral cortex. In high doses, it facilitates interneuronal conduction in the 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 it has a positive ino-, chrono-, bathmo- 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 of 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; 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 the 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

Diseases accompanied by depression of the central nervous system, functions of the cardiovascular and respiratory systems (including poisoning with opioid analgesics, infectious diseases), cerebral vascular spasms, decreased mental and physical performance, drowsiness.

Directions for use and doses

Administered subcutaneously or taken orally. Adults - 100-200 mg 2-3 times a day; children - 25-100 mg 2-3 times a day.

Compound

1 tablet contains: active substance: caffeine sodium benzoate 100 mg. Excipients: potato starch, calcium stearate.

Contraindications

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

Use during pregnancy and breastfeeding

Since there have been no adequate and well-controlled studies in women during pregnancy, and 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. Caffeine and its metabolites are excreted into mother's milk in small quantities. If it is necessary to use it during lactation, the benefit/risk ratio for the mother and child should be assessed. Use in neonatology.

special instructions

It should be borne in mind that 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 infants in the postoperative period (prevention), caffeine or 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. Do not take before bedtime.

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.

Drug interactions

When used simultaneously, the effect of sleeping pills and anesthetics is reduced. With simultaneous use, it is possible to enhance the effect of analgesics-antipyretics, salicylamide, naproxen. With the simultaneous use of estrogens (hormonal contraceptives, drugs for HRT), it is possible to increase the intensity and duration of action of caffeine due to inhibition of the CYP1A2 isoenzyme by estrogens. 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 the bioavailability, absorption rate and plasma concentration of acetylsalicylic acid. With simultaneous use, mexiletine reduces the clearance of caffeine and increases its plasma concentrations, apparently due to mexiletine inhibition of caffeine metabolism in the liver. 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, its simultaneous use accelerates the metabolism and excretion of caffeine. 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.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 degrees.