Caffeine sodium benzoate pharmacological group. Medicinal reference book geotar

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, drowsiness disappears, 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 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 antispasmodic effect of the alkaloid on smooth muscles, and stimulating - to striated. Under the influence of caffeine, the secretory activity of the stomach increases and the basal metabolism increases (increased glycogenolysis, accelerated lipolysis). 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 drugs, alcohol and toxins as a result 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 mental and mental decline. physical performance, drowsiness, 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. Wherein mandatory conditions are strict adherence to dosage, doctor’s recommendations and physical exercise. 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 psychostimulant "Caffeine-benzoate" instructions for use do not recommend prescribing to people with arterial hypertension, increased excitability, sleep disorders (insomnia), 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, fatigue, and increased inhibition of the central nervous system reaction may occur.

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. During the 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.

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. Of 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.

Being a psychostimulant and stimulant of the central nervous system, caffeine sodium benzoate is a derivative of methylxanthine. It inhibits the activity of special phosphodiestrases (PDE) enzymes in the heart, nervous system, organs and adipose tissue. IN high doses accumulates in the body in the form of adrenaline derivatives cAMP and cGMP.

This synthetic drug, which is based on caffeine, is obtained from tea leaves and coffee seeds. It is produced in the form of tablets of 0.1 g, and there are 6 pieces in total in the package. There is also a solution in ampoules (20%), with a dosage of 1 ml.

Effects of caffeine tablets:

  • increases mental excitability;
  • helps to concentrate attention;
  • improves ;
  • reduces fatigue and delays its onset;
  • stimulates the release of adrenaline in the blood;
  • activates the fat burning process;
  • during intensive training allows muscles to more actively use triglyceride (a source of nutrition);
  • increases muscle activity in people exercising by force sports: participates in calcium metabolism, maintains the potential of muscle membranes.

In small doses it stimulates the central nervous system, and in large doses, on the contrary, it depresses it. After taking caffeine-sodium benzoate, breathing becomes deep and rapid, blood vessels dilate and tone increases. cerebral arteries.

The decrease is normalized and slightly increases when taking caffeine. In addition, caffeine promotes the production gastric juice, and is also a weak diuretic. Due to this, the vessels of the kidneys dilate, and filtration in the renal glomeruli increases. Caffeine slows down the process of “gluing”, that is, platelet aggregation.

Scheme of use of caffeine-sodium benzoate

Caffeine tablets can be taken throughout the day, regardless of meals. Immediately before going to bed, MirSovetov recommends not taking pills, as it will be difficult to fall asleep. To improve performance and eliminate drowsiness, adolescents and adults take 50-100 mg of the drug up to 3 times a day. The course of treatment usually ranges from several weeks to two months.

To relieve an attack, children over 12 years of age and adults are recommended to take 50-100 mg of caffeine in tablets 2 times a day for 3 days.

For the treatment of hypotension, children over 12 years of age and adults are prescribed similar dose drug 3 times a day. The treatment period usually lasts several weeks.

When consuming caffeine-sodium benzoate, it is important to observe permissible dose. The maximum single dosage is 300 mg, and the daily dosage is 1000 mg.

Application for weight loss

It is believed that the recommended dosage of caffeine to stimulate the nervous system is not at all effective for weight loss, since in order to burn overweight, you need to use other doses. If a person with overweight If he plays sports, then before each workout he needs to take from 9 to 20 mg of the drug in tablets per 1 kg of body weight. Only in this case will it be possible to accelerate the work of the heart and speed up all metabolic processes. You need to drink 30 minutes before the start of training, and reducing the dose, according to athletes, will not have the desired stimulating effect.

Doctors, in turn, advise not to rush and start taking caffeine at 2 mg/kg, gradually increasing the dose.

Side effects of caffeine tablets

Before you start a course of taking sodium benzoate, you need to check how the body reacts to the main component of the drug. If after the first day of treatment the body does not react negatively to caffeine, then you can continue therapy.

At independent use or non-compliance with the doctor's recommendations, feelings of anxiety and restlessness may appear. Typically the side effect is headache and general malaise. Sometimes when visiting a doctor, the patient complains of nasal congestion and vomiting, as well as exacerbation and peptic ulcer.

Abrupt withdrawal of the drug can lead to inhibition of reactions and fatigue.

The following symptoms are contraindications to the use of sodium benzoate with caffeine:

Older people, those with eye diseases, and those with a tendency to convulsions and seizures should take the pills with caution. Pregnant and breastfeeding women should take caffeine tablets only as directed by a doctor. At simultaneous administration the drug with oral contraceptives, the activity of caffeine decreases, it is eliminated more slowly by the liver and accumulates in the blood.

To prevent hyperstimulation of the nervous system, it is better to avoid combining sodium benzoate tablets with coffee and other substances containing caffeine. It is also important to consider that caffeine can inhibit the absorption of calcium into gastrointestinal tract. It also reduces efficiency sleeping pills and drugs, promotes active absorption of cardiac glycosides and excretion of lithium in the urine.

Overdose symptoms

Excess daily norm Taking caffeine in tablets (300 mg) is fraught with the following consequences for a person:

  • dizziness;
  • increased heart rate;
  • nausea;
  • confusion;
  • restlessness and tremors.

Having felt it myself Negative consequences drug needed in urgently do a gastric lavage, take a laxative and, which adsorbs toxic substances in the gastrointestinal tract. In people with chronic diseases stomach after an overdose of caffeine, gastritis can be greatly aggravated. In this case, you should contact medical institution, where the doctor can promptly rinse the stomach with a special solution and introduce antacid. When convulsions occur caused by a high concentration of caffeine in the blood, the patient is administered antiepileptic drugs intravenously.

After much research, scientists were able to determine lethal dose tablets of sodium benzoate with caffeine, and this is what we managed to record. Positive effect caffeine on the body is observed when taking from 1 to 5 mg per 1 kg of human body weight. That is, with a weight of 70 kg you can take from 70 to 350 mg of the drug, but no more. For people who do not regularly consume caffeine, the effect of taking it is much greater.

Each time you increase the dose of a medicine, the likelihood of an overdose increases. Shrinks first total time sleep, its quality decreases. Then headaches, insomnia and anxiety appear. Next appointment higher permissible norm is fraught with rapid heartbeat and muscle twitching. A gastrointestinal tract disorder appears.

People addicted to caffeine pills usually suffer from mental disorders. Regularly overdosing caffeine may one day play a role cruel joke against a person. Scientists have proven that a dose of sodium benzoate with caffeine of 100-200 mg per 1 kg of weight is lethal for humans. After a fatal overdose, consciousness turns off, spasms appear and death. It follows: a dose of more than 18 g of caffeine per day is life-threatening.

If you take caffeine tablets every day, you should be aware that abruptly stopping treatment leads to depression of the central nervous system. Each organism is individual, therefore the effect on the central nervous system may be different: one person will notice a surge of vigor and strength, while another will experience depression and drowsiness. The same effect occurs on the heart.

Constant use of sodium benzoate with caffeine during pregnancy can lead to spontaneous heart problems in the fetus and a slowdown in its development. In small quantities, the drug passes into breast milk, and after feeding the baby, he may experience insomnia and excessive activity.

Caffeine sodium benzoate: instructions for use

Compound

Each ampoule (1 ml) contains: active substances- caffeine - 80 mg; sodium benzoate - 120 mg; Excipients- sodium hydroxide, water for injection.

Description

Transparent colorless or slightly yellowish color liquid.

Indications for use

Auxiliary agent for respiratory depression (including mild poisoning narcotic analgesics and hypnotic drugs, carbon monoxide) and restoration of pulmonary ventilation after use general anesthesia.

Contraindications

Carefully

Glaucoma, increased excitability, elderly age, epilepsy and tendency to seizures, pregnancy, lactation period.

Directions for use and doses

Adults are administered subcutaneously 200 mg (1 ml of solution), children 25 - 100 mg (0.1 - 0.5 ml of solution) 2 - 3 times a day.

Intramuscular administration of a caffeine-sodium benzoate solution is not recommended due to the possibility of developing painful spastic muscle contractions at the injection site.

Side effect

From the nervous system: agitation, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, insomnia.

From the cardiovascular system: palpitations, tachycardia, arrhythmias, increased blood pressure.

From the digestive side systems: nausea, vomiting, exacerbation of peptic ulcer.

Others: nasal congestion, with long-term use- addiction, drug addiction.

Overdose

Symptoms of intoxication occur when caffeine is consumed in a dose of more than 300 mg/day. Anxiety, restlessness, tremor, headache, confusion, and tachyarrhythmia may occur. In newborns with a blood concentration of more than 50 mcg/ml of caffeine, in addition to the above-described picture, a pathological increase in reflexes, the appearance of convulsive syndrome.

There is no specific antidote. Help includes drug withdrawal, supportive care and symptomatic therapy, aimed at eliminating the violations that have arisen, controlling blood pressure levels and relieving convulsive syndrome by administering benzodiazepine tranquilizers (diazepam).

Interaction with other drugs

Caffeine is an adenosine antagonist.

With the combined use of caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin), it is possible to enhance metabolism and increase the clearance of caffeine.

With the combined use of caffeine and cimetidine, oral contraceptive drugs, disulfiram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increasing its concentration in the blood).

Mexiletine - reduces caffeine excretion by up to 50%; nicotine - increases the rate of caffeine elimination.

MAO inhibitors, furazolidone, procarbazine and selegiline - large doses caffeine may cause the development of dangerous cardiac arrhythmias or a significant increase in blood pressure.

Caffeine reduces the absorption of calcium preparations in the gastrointestinal tract.

Reduces the effect of narcotic and sleeping pills medicines.

Increases the excretion of lithium drugs in urine.

Accelerates absorption and enhances the effect of cardiac glycosides, increasing their toxicity.

Concomitant use caffeine with beta-blockers may cause mutual suppression therapeutic effects; with adrenergic bronchodilators - to additional stimulation of the central nervous system and other additive toxic effects.

At simultaneous use increases bioavailability acetylsalicylic acid, paracetamol and ergotamine, thereby enhancing their effect.

Caffeine may decrease the clearance of theophylline and possibly other xanthines, increasing the potential for additive pharmacodynamic and toxic effects.

Antifungal drugs (ketoconazole, fluconazole) slow down the metabolism of caffeine and increase its concentration in plasma.

Features of application

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 stimulation of the heart and inhibition (weak) of its activity can develop.

Pregnancy and lactation. 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.

Use in neonatology. For the treatment and prevention of apnea in newborns and children infancy V postoperative period Caffeine or caffeine citrate is used, but not caffeine sodium benzoate.

Use in persons with gastric ulcers and duodenum in the anamnesis. Caution is required when prescribing caffeine to these groups of patients due to increased risk exacerbation of their peptic ulcer.

Impact on the ability to perform work that requires concentration. When used in high doses, caffeine makes it difficult to concentrate and increases the number of operator errors when performing work that requires concentration.

Release form

1 ml in ampoules. 10 ampoules per package No. 10, No. 10 x 1.

Storage conditions

In a place protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Best before date

5 years. Do not use the medicine after the expiration date.

Conditions for dispensing from pharmacies

On prescription.

Caffeine-sodium benzoate analogues, synonyms and group drugs

Self-medication can be harmful to your health.
You should consult your doctor and read the instructions before use.

Transparent colorless or slightly yellowish liquid.

Pharmacotherapeutic group

Psychostimulants and nootropics. Xanthine derivatives.

ATX code N06BC01

Pharmacological properties"type="checkbox">

Pharmacological properties

Pharmacokinetics

The drug is quickly distributed in all organs and tissues of the body. Communication with blood proteins (albumin) – 25-36%. Easily penetrates the blood-brain barrier and placenta. Passes into breast milk. The volume of distribution in adults is 0.4-0.6 l/kg, in newborns – 0.78-0.92 l/kg.

More than 90% is metabolized in the liver dose taken of the drug, in children of the first years of life up to 10-15%. In adults, about 80% of a caffeine dose is metabolized to paraxanthine, about 10% to theobromine, and about 4% to

theophylline. These compounds are subsequently demethylated into monomethylxanthines and then into methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10 hours), in newborns (up to 4-7 months of age) - 65-130 hours. Caffeine and its metabolites are excreted by the kidneys (1-2% are excreted unchanged in adults, and up to 85% in newborns).

Pharmacodynamics

Caffeine is an alkaloid found in tea leaves and coffee beans. The pharmacological properties of the drug are divided into central and peripheral.

The central effects, in turn, are divided into psychostimulating and analeptic. The psychostimulant effect of Caffeine-sodium benzoate-Darnitsa is associated with its antagonism to the action of adenosine on purinergic (adenosine) A-1 and A-2 receptors in the central nervous system (CNS). Adenosine is known to suppress central nervous system functions. Under the influence of the drug, mental activity, mental and physical performance increase. The psychostimulating effect is directly dependent on the dose. Small doses stimulate the functions of the central nervous system, large doses inhibit them (due to depletion of nerve cells).

The analeptic effect of Caffeine-sodium benzoate-Darnitsa is associated with its effect on the respiratory and hemodynamic centers medulla oblongata. As a result, an increase in the frequency and volume of inhalation is observed.

The peripheral effects of the drug are not clear and are related to its dose and level of influence on the vascular bed and myocardium. Coronary blood flow first increases and then decreases, renal blood flow increases, blood vessels narrow abdominal cavity, skin. Under the influence of the drug, central blood circulation worsens and cerebrospinal fluid pressure decreases, which explains its effectiveness for migraines. The effect of the drug on the heart is ambiguous. In small doses it causes positive inotropic effect, in higher doses – positive chronotropic effect. In some people it can cause tachycardia and even arrhythmia.

Indications for use

Infectious and other diseases that are accompanied by depression of the central nervous and cardiovascular systems

Respiratory depression, asphyxia

Poisoning with drugs and other substances that depress the central nervous system

Asthenic syndrome

Spasms of cerebral vessels

Directions for use and doses

For adults, administer the drug subcutaneously in a dose of 1-2 ml of a 10% solution (100-200 mg). Higher single dose– 400 mg, maximum daily dose– 1 year

For children over 12 years of age, the drug should be administered subcutaneously in a dose (depending on

age) 0.25-1 ml of 10% solution (25-100 mg).

Side effects"type="checkbox">

Side effects

Excitement, anxiety, tremor, restlessness, insomnia, headache, dizziness, epileptic seizures, increased reflexes, tachypnea. If the drug is suddenly discontinued after long-term use, the effect on the central nervous system increases, increased fatigue,

drowsiness, muscle tension, depression

Palpitations, chest tightness, tachycardia, arrhythmias, increased blood pressure

Nausea, vomiting, diarrhea, exacerbation of peptic ulcer

Hypersensitivity reactions, including rash, itching, urticaria, angioedema, bronchospasm

Hypo- or hyperglycemia, increased creatinine clearance, increased

excretion of sodium and calcium, false promotion urinary concentration

acids in blood plasma determined by the Bittner method, slight increase concentrations of 5-hydroxyindoleacetic acid, vanillylmandelic acid and catecholamines in urine

Other: increased frequency of urination, nasal congestion,

long-term use – addiction, drug dependence

Contraindications

Increased sensitivity to xanthine derivatives and other components of the drug

Increased excitability

Insomnia

Atherosclerosis

Organic diseases of the cardiovascular system, including acute

myocardial infarction

Paroxysmal tachycardia

Arterial hypertension

Glaucoma

Age over 60 years

Pregnancy, lactation period

Children's age up to 12 years

Drug interactions"type="checkbox">

Drug interactions

When used simultaneously with other drugs

Maybe:

with alpha and beta-agonists, analgesics-antipyretics,

clozapine, xanthine derivatives, psychostimulants,

cardiac glycosides, thyroid-stimulatingmimeans– enhancing the effects of the above-mentioned drugs;

with anxiolytics, opioid analgesics, hypnotics and sedatives – weakening of the effects of the above-mentioned drugs;

With antiarrhythmic drugs(mexiletine), hormonal oral contraceptives, disulfiram, enoxacin, erythromycin,

isoniazid, methoxsalen, norfloxacin, ofloxacin, cimetidine,

ciprofloxacin– increased effects of caffeine;

with antidepressants, barbiturates,beta-adrenoblockers, primidone, anticonvulsants(hydantoin derivatives, especially phenytoin), cholestyramine, anticholinergics– weakening the effects of caffeine;

with medications, stimulantsmicentral nervous

system, drinks containing caffeine– overstimulation

central nervous system;

with MAO inhibitors, procarbazine, furazolidone– dangerous arrhythmias or severe increases in blood pressure;

with ergotamine– increased absorption of the latter from the gastrointestinal tract;

with calcium supplements– weakening of absorption of the latter from the gastrointestinal tract;

with drugamilithium– increased excretion of the latter in urine;

with nicotine– increased excretion of caffeine in urine.

The drug slightly increases the concentration of 5-hydroxyindoleacetic acid when determined in urine.

The drug slightly increases the concentration of catecholamines and

vanillylmandelic acid, which can lead to false positive

test results for diagnosing pheochromocytoma and neuroblastoma.

The drug should not be used during tests.

The drug may lead to false results in determining serum urate concentration using the Bittner method.

Caffeine is an adenosine antagonist.

special instructions"type="checkbox">

special instructions

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

activities.

Due to the fact that the effect of caffeine on blood pressure consists of vascular and cardiac components, it can develop as an effect

stimulation of the heart and slight inhibition of its activity.

Use with caution in patients with a history of gastric and duodenal ulcers, or with epilepsy.

For apnea in newborns and infants in the postoperative period (prevention), caffeine or caffeine citrate is used, but not

caffeine sodium benzoate.

Children

The drug should not be used in children under 12 years of age.

Pregnancy and lactation

The drug should not be used during pregnancy or breastfeeding.

Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms

During treatment, care should be taken when driving vehicles and working with other mechanisms, and if side effects from the nervous system occur, refrain from working with potential dangerous species activities that require increased concentration and speed of psychomotor reactions.

ABON BIOPHARM (Hangzhou) Co., LTD BELMEDPREPRATY, RUP Boehringer Ingelheim Pharma GmbH and Co.KG Biokhimik, OJSC Borisov Plant medical supplies, OJSC Borisov Medical Preparations Plant, RUE Dalkhimfarm OJSC Moscow Endocrine Plant, Federal State Unitary Enterprise Moskhimfarmpreparaty Federal State Unitary Enterprise named after. Semashko Moskhimfarmpreparaty named after N.A. Semashko, OJSC POLIPHARM ICN POLIPHARM, LLC Tatkhimfarmpreparaty OJSC THFZ ICN Usolye-Sibirsky chemical farm plant, OJSC Pharmstandard-Tomskkhimpharm, OJSC

Country of origin

Republic of Belarus Russia

Product group

Nervous system

Psychostimulant and analeptic.

Release forms

  • 1 ml - ampoules (10) - cardboard packs. 6 - cell-free contour packages. 6 - cell-free contour packages. tablets ao 100.0 mg ---10 pieces in a blister pack

Description of the dosage form

  • Solution for subcutaneous and subconjunctival administration Tablets Tablets white flat-cylindrical shape with a chamfer and a notch.

pharmachologic effect

Caffeine is a methylxanthine that has a psychostimulant and analeptic effect. Competitively blocks central and peripheral AT and A2 adenosine receptors. Inhibits the activity of phosphodiesterase in the central nervous system, heart, smooth and striated muscle tissue, adipose tissue, promotes the accumulation of cyclic adenosine monophosphate and cyclic guanosine monophosphate ( this effect observed with only high doses of caffeine). Stimulates the centers of the medulla oblongata (respiratory and vasomotor), as well as the center vagus nerve, has a direct stimulating effect on the cerebral cortex. In high doses, it facilitates interneuronal conduction in spinal cord, strengthening reflexes. Increases mental and physical performance, stimulates mental activity, physical activity, shortens reaction time, temporarily reduces fatigue and drowsiness. In low doses, the stimulating effect predominates, and in large doses, the effect of depression of the nervous system predominates. It quickens and deepens breathing, usually has a positive ino-, 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 center of the vagus nerve, the resulting effect depends on the predominance one action or another). Stimulates the vasomotor center and has a direct relaxing effect on vascular wall, which leads to dilation of the blood 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 cerebral blood flow). 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, but with arterial hypotension it increases it. It has an antispasmodic effect on smooth muscles (including a bronchodilator effect), and a stimulating effect on striated muscles. Increases gastric secretory activity and diuresis (decreased reabsorption of sodium and water 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.

Pharmacokinetics

When taken orally, absorption is good; occurs throughout the intestine. It is quickly distributed in all organs and tissues of the body, penetrates the blood-brain barrier and the placenta. The maximum concentration in blood plasma is achieved after 50-75 minutes; the half-life is 3.9-5.3 hours (sometimes up to 10 hours). Communication with blood proteins (albumin) - 15%. More than 90% is metabolized in the liver, in children of the first years of life up to 10-15%. Caffeine is metabolized in the liver (the main part is dimethylated and oxidized) with the formation of 5 metabolites. Caffeine and its metabolites are excreted by the kidneys (10% unchanged).

Special conditions

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. Do not take before bedtime. Impact on the ability to drive vehicles. Wed and mechanisms During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require concentration and speed of psychomotor reactions.

Compound

  • 1 ml caffeine sodium benzoate 200 mg caffeine 0.1 g; Auxiliary ingredients: potato starch, calcium stearate

Caffeine sodium benzoate indications for use

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

Caffeine-sodium benzoate contraindications

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

Caffeine-sodium benzoate dosage

  • 0.1 g 100 mg 200 mg/ml

Caffeine sodium benzoate side effects

  • From the central nervous system: psychomotor agitation, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, insomnia; with sudden withdrawal - increased inhibition of the central nervous system, increased fatigue, drowsiness, muscle tension. From the cardiovascular system: palpitations, tachycardia, increased blood pressure. From the outside digestive system: nausea, vomiting, exacerbation of peptic ulcer. Other: nasal congestion, with prolonged use - addiction, drug dependence.

Drug interactions

Caffeine is an adenosine antagonist (larger doses of adenosine may be required). With the combined use of caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin), it is possible to enhance metabolism and increase the clearance of caffeine; cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin - decreased metabolism of caffeine in the liver.. (slowing its excretion and increasing its concentration in the blood). Caffeine-containing drinks and other drugs that stimulate the central nervous system - excessive stimulation of the central nervous system is possible. - Mexiletine - reduces caffeine excretion by 50%; nicotine - increases the rate of caffeine elimination. Monoamine oxidase inhibitors, furazolidone, procarbazine and selegiline - large doses of caffeine (more than 300 mg / day) can cause the development of life-threatening cardiac arrhythmias or a pronounced increase in blood pressure. Caffeine reduces the absorption of calcium preparations in the gastrointestinal tract. Reduces the effectiveness of narcotic and sleeping pills. Increases the excretion of lithium drugs in the urine; Accelerates absorption and enhances the effect of cardiac glycosides, increasing their toxicity. Concomitant use with beta-blockers may lead to mutual suppression of therapeutic effects; with β-adrenergic agonists - to additional stimulation of the central nervous system and other additive toxic effects. Caffeine may decrease clearance; theophylline and possibly other xanthines, increasing the potential for additive pharmacodynamic and toxic effects.

Storage conditions

  • store in a dry place
  • store at room temperature 15-25 degrees
  • keep away from children
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