Caffeine sodium benzoate, 100 mg, tablets, 6 pcs.
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.
Caffeine-sodium benzoate 20%/1 ml No. 10 solution d/in.amp.
Instructions for the use of the drug for specialists Caffeine-sodium benzoate (Coffeinum natrio-benzoicum) Trade name Caffeine-sodium benzoate International nonproprietary name No Dosage form Solution for injection 20% Composition 1 ml of solution contains active substances: caffeine - 0.08 g, sodium benzoate – 0.12 g, excipients: sodium hydroxide solution 0.1 M, water for injection. Description Transparent colorless or slightly yellowish liquid. Pharmacotherapeutic group Psychostimulants and nootropics. Xanthine derivatives. ATC code N06BC01 Pharmacological properties Pharmacokinetics After subcutaneous administration, absorption occurs quickly and completely. Penetrates well through all histohematic barriers, distributed throughout organs and tissues. Penetrates the BBB and the hematoplacental barrier. Concentrations in cerebrospinal fluid and amniotic fluid are comparable to caffeine concentrations in blood plasma. The concentration of caffeine in saliva is 65-85% of its concentration in plasma. After administration, it undergoes intensive metabolism in the liver with the formation of dimethyl- and monomethylxanthines, dimethyl- and monomethyluric acid, trimethyl- and dimethylallantoin, uridine derivatives. The main route of metabolism is the formation, under the influence of the cytochrome P450 CYP1A2 isoform, of dimethylxanthines (theophylline, paraxanthine), which have pharmacological activity (72-80% of the administered dose). The half-life of caffeine (T½) is 2.5-4.5 hours; in newborns, due to the low enzymatic activity of microsomal enzymes, the elimination of caffeine is slowed down, T½ is 80 ± 23 hours, at the age of 3-5 months it decreases to 14.4 hours and at 5-6 months it becomes equal to that of an adult. The total clearance of caffeine in an adult is 155 ml/kg/h, in a newborn child it is 31 ml/kg/h. In smokers, there is a decrease in the half-life of caffeine by 30-50% compared to non-smokers. Caffeine is excreted primarily in the urine in the form of metabolites. 10% of the administered dose is excreted unchanged. Pharmacodynamics It has psychostimulating and analeptic properties. The mechanism of action is associated with the ability of caffeine to act as a competitive antagonist of purine A1 and A2A receptors. As a result of receptor blockade, inhibition processes in the central nervous system are reduced, the secretion of neurotransmitters (serotonin, norepinephrine and dopamine) in the motor areas of the cerebral cortex, hypothalamus and medulla oblongata is facilitated and stabilized. In doses close to toxic, caffeine is able to block the activity of phosphodiesterases (mainly types III, IV) and slow down the breakdown of cAMP and cGMP, which stimulates the activity of neurons and accelerates metabolism in the cell. Strengthening dopaminergic transmission in the synapses of the cerebral cortex has a psychostimulating effect. Activation of adrenergic transmission in the synapses of the hypothalamus and medulla oblongata activates cortical functions, increases physical activity, causes anorexia, and has a tonic effect on the vasomotor center. Strengthening cholinergic transmission in the synapses of the cortex and medulla oblongata activates cortical functions and increases the activity of the respiratory center. Caffeine has a direct stimulating effect on the central nervous system: it stimulates mental activity, increases mental and physical performance, shortens reaction time, and activates positive conditioned reflexes. After the introduction of caffeine, vigor appears, fatigue and drowsiness are temporarily reduced or eliminated. In older people, the effect on sleep is more pronounced: sleep onset slows, total sleep time decreases, and the frequency of night awakenings increases. Against the background of depression of the respiratory center, it causes increased and deepening of breathing. Affects the cardiovascular system: increases the frequency and strength of heart contractions, and with hypotension increases blood pressure (does not affect normal blood pressure levels). In premature babies, it eliminates periodic breathing by reducing the partial pressure of carbon dioxide in the blood, increases the volume of ventilation without significantly affecting the function of the cardiovascular system. Relaxes the smooth muscles of the bronchi and bile ducts, causes dilatation of the vessels of skeletal muscles, heart and kidneys, narrows the vessels of the abdominal organs (especially with their initial dilatation). It has a weak diuretic effect due to dilation of renal vessels and inhibition of reabsorption of electrolytes in the renal tubules. Reduces platelet aggregation. Stimulates the secretion of gastric glands. Increases basal metabolism, enhances glycogenolysis, causing hyperglycemia. Indications for use - conditions associated with inhibition of the functions of the central nervous system, respiratory and cardiovascular systems: drug poisoning, severe infectious diseases, conditions after the use of general anesthetics (anesthesia) - cerebral vascular spasms - decreased mental and physical performance during the period of convalescence after suffered severe general somatic and infectious diseases - narcolepsy - breathing disorders (periodic breathing, idiopathic apnea) in newborns, incl. premature babies. Method of administration and dosage Administered subcutaneously at 200 mg (1 ml of 20% solution) for adults, 25-100 mg (0.25 - 1 ml of 10% solution or 0.1 - 0.5 ml of 20% solution) for children 2-3 once a day. To eliminate apnea in newborns, a solution of caffeine-sodium benzoate is administered intravenously or orally. 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 effects - anxiety, agitation, insomnia - tachycardia, arrhythmia, increased blood pressure - nausea, vomiting - development of weak psychological dependence and tolerance with long-term use in high doses - with sudden cessation of use, the development of reactive fatigue, drowsiness and depression is possible. Contraindications - arterial hypertension of the third degree - organic diseases of the cardiovascular system (including atherosclerosis) - increased excitability, sleep disorders - glaucoma - old age. Drug interactions When used simultaneously, caffeine enhances the effect of antiplatelet drugs. Reduces the effect of sleeping pills, narcotics and other central nervous system depressants. When used simultaneously, it increases the bioavailability of acetylsalicylic acid, paracetamol and ergotamine, thereby enhancing their effect. When used simultaneously with β2-adrenergic agonists in high doses (salmeterol, salbutamol, fenoterol), it increases the risk of developing hypokalemia. When used simultaneously with methylxanthines (theophylline, aminophylline), there is an increase in the concentration of theophylline in the blood plasma and an increase in the risk of its toxic effect. Anticonvulsants (carbamazepine, diphenin), barbiturates accelerate the metabolism of caffeine and reduce its concentration in plasma. Combined oral contraceptives, macrolide antibiotics (clarithromycin, erythromycin), interferon preparations and antifungals (ketoconazole, fluconazole) slow down the metabolism of caffeine and increase its concentration in plasma. When caffeine sodium benzoate is used in smokers, its plasma concentrations are lower than in non-smoking patients. Special instructions Pregnancy and lactation Since adequate and well-controlled studies have not been conducted in women during pregnancy, and also 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 Caffeine can be used during the neonatal period, as well as in premature infants. In this case, the concentration of caffeine in plasma should be monitored and maintained within therapeutic limits (3-10 mcg/ml). Use in persons with a history of gastric and duodenal ulcers Caution must be exercised when prescribing caffeine to these groups of patients, due to the increased risk of exacerbation of their peptic ulcer. Effect on the ability to perform work that requires concentration. When taken orally in high doses, caffeine makes it difficult to concentrate and increases the number of operator errors when performing work that requires concentration. Overdose Symptoms of intoxication occur when consuming caffeine in a dose of more than 300 mg/day (although cases of consuming more than 1000 mg/day of caffeine have been described). 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, pathological strengthening of reflexes and the appearance of a convulsive syndrome are possible. There is no specific antidote. Assistance measures include discontinuation of the drug, supportive and symptomatic therapy aimed at eliminating the disorders that have arisen, monitoring blood pressure levels and stopping seizures with the administration of benzodiazepine tranquilizers (diazepam). Release form and packaging Ampoules of 1 ml. 10 ampoules with a knife for opening ampoules in a cardboard box. Storage conditions: Protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children! Shelf life: 5 years Do not use after expiration date. Conditions for dispensing from pharmacies By prescription, Republic of Belarus. Minsk region, Borisov, st. Chapaeva, 64/27
Buy Caffeine-sodium benzoate injection solution 20% 1ml No. 10 in pharmacies
Instructions for use Caffeine-sodium benzoate solution d/in. 20% 1ml No. 10
Dosage forms injection solution 20% 1 ml Group Psychomotor stimulants - purine and imidazole derivatives International nonproprietary name Caffeine Composition Caffeine. Manufacturers : Belmedpreparaty (Belarus), Biokhimik OJSC (Russia), Borisov Medical Preparations Plant (Belarus), Dalkhimfarm (Russia), Darnitsa Pharmaceutical Company (Ukraine), Moscow Endocrine Plant (Russia), Moskhimfarmpreparaty im. ON THE. Semashko (Russia), Chelyabinsk Chemical Pharmaceutical Plant (Russia) Pharmacological action Analeptic, psychostimulating, cardiotonic. It has a stimulating effect on the central nervous system, increases reflex excitability of the spinal cord, stimulates the respiratory and vasomotor centers, regulates and enhances excitation processes in the cerebral cortex. Increases mental and physical performance, reduces fatigue and drowsiness. Increases the strength and frequency of heart contractions (especially in large doses), increases blood pressure during hypotension (does not change normal). Dilates the blood vessels of skeletal muscles, heart, kidneys, bronchi, narrows the abdominal organs. Increases the secretory activity of the stomach. Reduces platelet aggregation. Has a moderate diuretic effect. Blocks central and peripheral adenosine receptors. Stabilizes transmission at dopaminergic synapses, beta-adrenergic synapses of the hypothalamus and medulla oblongata, cholinergic synapses of the cortex and medulla oblongata, noradrenergic synapses. The effect of caffeine largely depends on the type of nervous system in the patient, so dosing of caffeine should take into account the individual characteristics of nervous activity. 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. Indications for use Diseases accompanied by depression of the functions of the central nervous system, cardiovascular system, respiratory system (drug poisoning, infectious diseases, etc.). For cerebral vascular spasms, to increase mental and physical performance, to eliminate drowsiness, breathing problems, enuresis in children. Contraindications Severe arterial hypertension, organic diseases of the cardiovascular system (including atherosclerosis), increased excitability, glaucoma, sleep disorders, old age. Method of administration and dosage: Adults, 1 ml of 10% or 20% solution subcutaneously. Higher doses for adults under the skin: single dose 0.4 g, daily dose 1 g. Children: 0.25 - 1 ml of a 10% solution subcutaneously, depending on age. Doses must be selected individually. Overdose If abused, caffeine (more than 300 mg per day, i.e. four cups of natural coffee, 150 ml each) 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. Interaction Reduces the effect of sleeping pills and narcotics, increases (improving bioavailability) - acetylsalicylic acid, paracetamol and other non-narcotic analgesics. Improves the absorption of ergotamine in the gastrointestinal tract. Special instructions No data available. Storage conditions List B. In a place protected from light, at room temperature.
Symptoms of caffeine overdose
Unfortunately, drinking coffee has become a habitual ritual for many. In an attempt to get themselves into working condition as quickly as possible, people turn to coffee almost immediately after sleep. However, the negative consequences of such a habit will not be long in coming.
Often the symptoms of a caffeine overdose are perceived by people as negative consequences of daily stress, anxiety and an unsettled lifestyle:
- insomnia;
- depression;
- nervousness and irritability;
- increased anxiety.
To a lesser extent, symptoms of caffeine overdose include frequent urination (enuresis), fluctuations in blood pressure, increased body temperature, heartburn, nausea, diarrhea, deterioration of the skin (caused by dehydration), vision problems and dizziness.
Caffeine-containing drinks are recommended to be consumed with caution by people with increased nervous excitability, cardiac arrhythmia, peptic ulcer, gastritis, atherosclerosis and glaucoma.
Rice. 1. Caffeine content in coffee and tea.
Effect of caffeine on the body
Adenosine receptors in the brain are responsible for suppressing excitation. The ability to block adenosine receptors is the main property of caffeine (the caffeine molecule is similar to adenosine), which determines its invigorating effect. In turn, the breakdown of glycogen under the influence of caffeine molecules helps to release additional energy by raising blood sugar levels. In addition, caffeine also increases the concentration of leptin in the blood, which reduces appetite and increases energy expenditure.
The invigorating effect of caffeine directly depends on its amount. Small doses of caffeine are found in tea (up to 45 mg per cup) and instant coffee (up to 70 mg per serving); roasted beans are more saturated with caffeine (up to 115 mg per serving). Separately, it is worth noting energy drinks, the caffeine content of which can reach 250 mg per can. Thus, excessive consumption of energy drinks poses an increased risk of developing cardiovascular diseases, gastrointestinal diseases, and in some cases leads to premature death (cardiac arrest).
Relatively safe dosage of caffeine
Russian regulatory authorities have established a recommendation for daily caffeine consumption. A relatively safe dosage in our country is considered to be the total number of caffeine-containing drinks consumed, not exceeding a total daily dosage of 150–300 mg of caffeine: in terms of cups of tea - no more than 5, per serving of coffee - no more than 3. In the European Union, the EFSA has established a maximum The permissible daily dosage of caffeine is 400 mg, and the maximum single dose is 200 mg.
The effect of caffeine on the female body
The female body is most sensitive to caffeine overdose. Against the background of coffee and energy drink abuse, women have an increased risk of developing breast cancer and osteoporosis, and during pregnancy, a decrease in blood flow to the placenta, increased heart rate in the fetus, premature birth and miscarriage.
Regularly exceeding the recommended dosage inevitably leads to caffeine overdose, the risk of somatic and mental illnesses, and in some cases, psychological dependence on caffeine.
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