I. General information
1. Name of the medicinal product for veterinary use:
– trade name of the medicinal product – Caffeine-sodium benzoate 20%;
– international nonproprietary names – caffeine, sodium benzoate.
2. Dosage form: solution for injection.
1 ml of the drug contains as active ingredients: caffeine - 75 mg, sodium benzoate - 120 mg, and as excipients: sodium phosphate disubstituted 12-water, citric acid and water for injection.
3. In appearance, sodium caffeine benzoate 20% is a transparent, colorless liquid.
The shelf life of the medicinal product, subject to storage conditions in the manufacturer's closed packaging, is 3 years from the date of production, after opening the bottle - 28 days.
It is prohibited to use the medicinal product after the expiration date.
4. Sodium caffeine benzoate 20% is produced packaged in 10, 20 and 100 ml glass bottles of appropriate capacity, hermetically sealed with rubber stoppers and reinforced with aluminum caps with tamper evident clips. Each consumer package is supplied with instructions for use of the drug.
5. The medicinal product is stored in the manufacturer’s sealed packaging, separate from food and feed, in a place protected from direct sunlight at a temperature of 0°C to 25°C.
6. Sodium caffeine benzoate 20% should be kept out of the reach of children.
7. Unused medicinal product is disposed of in accordance with legal requirements.
8. Sodium caffeine benzoate 20% is available without a veterinarian's prescription.
Caffeine-sodium benzoate solution d/s injection 20% ampoule 1 ml No. 10
Compound
Each ampoule (1 ml) contains: active substances - caffeine - 80 mg; sodium benzoate - 120 mg; excipients - sodium hydroxide, water for injection.
Pharmacokinetics
After subcutaneous administration, it is absorbed 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 isoform CYP1A2, of dimethylxanthines (theophylline, paraxanthine), which have pharmacological activity (72–80% of the administered dose). The half-life of caffeine (T?) is 2.5-4.5 hours; in newborns, due to the low enzymatic activity of microsomal enzymes, the elimination of caffeine is slowed down, T? 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.
Indications for use
An auxiliary agent for respiratory depression (including mild poisoning with narcotic analgesics and hypnotic drugs, carbon monoxide) and restoration of pulmonary ventilation after the use of general anesthesia.
Contraindications
Hypersensitivity (including to other xanthines); anxiety disorders (agoraphobia, panic disorders); organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis); paroxysmal tachycardia, frequent ventricular extrasystole; arterial hypertension; sleep disorders.
With caution: Glaucoma, increased excitability, old age, epilepsy and tendency to seizures, pregnancy, lactation.
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.
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.
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 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.
Description
Transparent colorless or slightly yellowish liquid.
Conditions for dispensing from pharmacies
On prescription.
Dosage form
Solution for injection 200 mg/ml.
Manufacturer and organization accepting consumer complaints
Open Joint Stock Company "Borisov Medical Preparations Plant", Republic of Belarus, Minsk region, Borisov, st. Chapaeva 64/27, tel/fax +375(177)735612.
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.
Side effects
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 system: nausea, vomiting, exacerbation of peptic ulcer. Other: nasal congestion, with prolonged use - addiction, drug dependence.
Use during pregnancy and breastfeeding
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 consumption of caffeine during pregnancy can lead to spontaneous abortions, retardation of intrauterine development of the fetus, and arrhythmias 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 infants in the postoperative period, caffeine or caffeine citrate is used, but not caffeine sodium benzoate. Use in persons with a history of gastric and duodenal ulcers. Caution is required when prescribing caffeine to these groups of patients, due to the increased risk of exacerbation of peptic ulcer disease in them. 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.
Interaction
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 of caffeine can cause the development of dangerous cardiac arrhythmias or a marked increase in blood pressure. Caffeine reduces the absorption of calcium preparations in the gastrointestinal tract. Reduces the effect of narcotic and sleeping pills. Increases the excretion of lithium drugs in urine. Accelerates absorption and enhances the effect of cardiac glycosides, increasing their toxicity. Concomitant use of caffeine with beta-blockers may lead to mutual suppression of therapeutic effects; with adrenergic bronchodilators - to additional stimulation of the central nervous system and other additive toxic effects. When used simultaneously, it increases the bioavailability of 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.
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, and 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. 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).
II. Pharmacological properties
9. Caffeine-sodium benzoate 20% refers to drugs that stimulate the central nervous and cardiovascular systems of animals.
10. The drug enhances and regulates excitation processes in the cerebral cortex, enhances positive conditioned reflexes and increases motor activity. The stimulating effect of caffeine leads to increased physical performance, reduced fatigue and drowsiness. The effect of the drug depends on the dose, as well as on the type of higher nervous activity of animals. Large doses of the drug can lead to depletion of nerve cells.
Under the influence of the drug, cardiac activity and diuresis increase, gas exchange increases, and water and nitrogen metabolism increases.
Caffeine-sodium benzoate 20% in terms of the degree of impact on the body is classified as a low-hazard substance (hazard class 4 according to GOST 12.1.007-76).
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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