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 ah, 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 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 stimulation effect predominates, and in large doses, the suppression effect predominates. nervous system.
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 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 of the brain, which is accompanied by a decrease 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 secretory activity of the stomach.
Has a moderate diuretic effect, which is due to a decrease in the reabsorption of sodium ions 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.
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.
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 outside digestive system
: nausea, vomiting.
Contraindications:
Increased excitability;
- insomnia;
- severe hypertension;
- atherosclerosis;
- organic diseases of cardio-vascular system;
- old age;
- glaucoma;
- in the treatment of increased fatigue and drowsiness - childhood up to 12 years old.
Carefully during pregnancy and lactation.
Interaction
other medicinal
by other means:
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 simultaneous use of estrogens ( hormonal contraceptives, funds for HRT) 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 caffeine consumption during pregnancy can lead to spontaneous abortions, delayed intrauterine development fetus, 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.
Overdose:
Symptoms: gastralgia, agitation, anxiety, agitation, motor restlessness, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensitivity, tremors or muscle twitching; nausea and vomiting, sometimes with blood; tinnitus, 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), with a plasma caffeine concentration of 50 mg/ml, toxic effects are possible: anxiety, tachypnea, tachycardia, tremor, painful, bloated belly 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.
Instructions for medical use
medicinalfacilities
Caffeine sodium benzoate
Tradename
Caffeine sodium benzoate
International nonproprietary name
Dosage form
Solution for subcutaneous administration 200 mg/ml
Compound
One ampoule contains:
Description
Transparent colorless or slightly yellowish color liquid.
Pharmacotherapeutic group
Psychostimulants and nootropics. Xanthine derivatives. Caffeine.
ATX code N06B C01
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.
After administration, it undergoes intensive metabolism in the liver with the formation of 7 metabolites. The main route of metabolism is the formation, under the influence of the cytochrome P 450 isoform CYP1A2, of dimethylxanthines (theophylline, paraxanthine), which have pharmacological activity (72-80% of the administered dose).
The half-life of caffeine (T ½) is 2.5-4.5 hours, in newborns the elimination of caffeine is slowed down, T ½ is 80 ± 23 hours, at the age of 3-5 months it decreases to 14.4 hours and at 5-6 months becomes equal to those 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 A 1 and A 2A receptors.
Caffeine has a direct stimulating effect on the central nervous system: it stimulates mental activity, increases mental and physical performance, shortens reaction time, activates positive conditioned reflexes. After the introduction of caffeine, vigor appears, fatigue and drowsiness are temporarily reduced or eliminated. In older people the effect is more pronounced.
Affects the cardiovascular system: increases the frequency and strength of heart contractions, and with hypotension increases blood pressure (by normal level BP has no effect). In premature infants, it eliminates periodic breathing and increases the volume of ventilation without significantly affecting the function of the cardiovascular system.
Relaxes the smooth muscles of the bronchi, biliary tract, causes dilatation of blood vessels in skeletal muscles, heart and kidneys. Has a weak diuretic effect due to expansion 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 depression 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)
Spasms of cerebral vessels
Decreased mental and physical performance during the period of convalescence after severe general somatic and infectious diseases
Narcolepsy
Breathing disorders (periodic breathing, idiopathic apnea) in newborns, incl. premature babies.
Method of application anddoses
Adults are administered subcutaneously 200 mg (1 ml of 20% solution).
Higher single dose- 0.4 g, highest daily dose- 1 year
Intramuscular administration of a solution of caffeine-sodium benzoate is not recommended due to the possibility of developing painful spastic muscle contractions at the injection site.
Side effects
Excitement, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, insomnia
CNS depression, increased fatigue, drowsiness, muscle tension with sudden discontinuation of the drug after long-term use
Palpitations, tachycardia, arrhythmia, increased blood pressure
Nausea, vomiting, exacerbation of peptic ulcer
Nasal congestion
Addiction, drug dependence with long-term use.
Contraindications
Hypersensitivity to xanthine derivatives
Increased excitability, insomnia
Atherosclerosis
Organic diseases of the cardiovascular system, including acute heart attack myocardium, paroxysmal tachycardia, arterial hypertension
Pregnancy, breastfeeding period
Old age over 60 years
Glaucoma
Children under 18 years of age (20% solution for injection).
When used simultaneously, caffeine enhances the effect of antiplatelet drugs.
Reduces the effect of sleeping pills, narcotics and other drugs that depress the central nervous system.
When used simultaneously, it increases the bioavailability of acetylsalicylic acid, paracetamol and ergotamine, thereby enhancing their effect.
When used simultaneously with b2-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 concentration is lower than in non-smoking patients.
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 arterial pressure consists of vascular and cardiac components, both the effect of stimulating the heart and a slight inhibition of its activity can develop.
Use in persons with peptic ulcer stomach 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.
Features of influence medicine on the ability to drive vehicles and potentially dangerous mechanisms
Reduces neuromuscular reaction time and is not contraindicated for vehicle drivers and persons working with potentially dangerous mechanisms.
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.
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; taking 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.
Release form and packaging
1 ml in glass ampoules.
The text is applied to each ampoule using intaglio printing with quick-fixing ink or a label made of paper for multicolor printing or offset paper, or a self-adhesive label is affixed.
10 ampoules, together with a knife for opening ampoules or an ampoule scarifier, are placed in a cardboard box with a corrugated liner made of corrugated paper.
The box is covered with a label-parcel made from paper for multicolor printing or offset paper.
The boxes, along with instructions for medical use in the state and Russian languages, are placed in group containers. The number of instructions for medical use in the state and Russian languages must correspond to the number of packages.
Or 10 ampoules are placed in a polyvinyl chloride film insert. 1 insert with ampoules, along with a knife for opening ampoules or an ampoule scarifier and instructions for medical use in the state and Russian languages, is placed in a pack of chrome-ersatz cardboard.
Injection.
Basic physical and chemical properties: colorless transparent liquid.
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Pharmacological group
Psychostimulants, drugs for use in attention deficit hyperactivity disorder (ADHD) and nootropics. Xanthine derivatives. ATX code N06B C01.
Pharmacological properties
Pharmacological.
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 is associated with its antagonism of adenosine in the mechanism of action 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 increases mental activity, mental and physical performance. 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 sodium caffeine benzoate is associated with its effect on the respiratory and hemodynamic centers of the medulla oblongata. As a result, there is an increase in the frequency and volume of inhalation.
The peripheral effects of the drug are ambiguous and related to its dose and level of influence on vascular bed and myocardium. Coronary blood flow first increases and then decreases, renal blood flow increases, blood vessels constrict abdominal cavity, skin. Under the influence of the drug, central blood circulation is suppressed and cerebrospinal fluid pressure is reduced, which explains its effectiveness in migraines. The effect of the drug on the heart is ambiguous. In small doses it causes a positive inotropic effect, in higher doses it causes a positive chronotropic effect. In some people it can cause tachycardia and even arrhythmia.
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. Penetrates 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% of the taken dose of the drug is metabolized in the liver, in children of the first year 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 combinations are demethylated into monomethylxanthines, and then into methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10:00), in newborns (up to 4-7 months of age) - 65-130 hours. Caffeine and its metabolites are excreted by the kidneys (1-2% is excreted unchanged in adults, and up to 85% in newborns).
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Indications
Infectious and other diseases 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.
Contraindications
Increased sensitivity increased excitability to xanthine derivatives and other components of the drug; insomnia, marked increase in blood pressure; atherosclerosis; organic diseases of the cardiovascular system, including acute myocardial infarction, paroxysmal tachycardia, arterial hypertension; glaucoma age over 60 years.
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Special Security Measures
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, both the effect of stimulating the heart and a slight inhibition of its activity can develop.
Use with caution in patients with a history of gastric and duodenal ulcers.
For apnea in newborns and children infancy V postoperative period(prevention) use caffeine or caffeine citrate, but not caffeine sodium benzoate.
Interaction with other drugs and other types of interactions
When used simultaneously with other drugs, it is possible:
with alpha- and beta-adrenergic agonists, analgesics-antipyretics, clozapine, xanthine derivatives, psychostimulants, cardiac glycosides, thyroid-stimulating drugs - enhancing the effects of the above-mentioned drugs;
with anxiolytics, opioid analgesics, hypnotics and sedatives- weakening of the effects of the above-mentioned medications;
With antiarrhythmic drugs(mexiletine), hormonal oral contraceptives, disulfiram, enoxacin, erythromycin, isoniazid, methoxalen, norfloxacin, ofloxacin, cimetidine, ciprofloxacin - increased effects of caffeine
with antidepressants, barbiturates, beta-blockers, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin), cholestyramine, anticholinergics, - weakening the effects of caffeine
with medications that stimulate the central nervous system, drinks containing caffeine - excessive stimulation of the central nervous system;
with MAO inhibitors, procarbazine, furazolidone - dangerous arrhythmias or a pronounced increase in blood pressure;
with ergotamine - increased absorption of the latter from the digestive tract
with calcium supplements - weakening of absorption of the latter gastrointestinal tract
with lithium preparations - increased excretion of the latter in the urine;
with nicotine - increased excretion of caffeine in the urine.
The drug slightly increases the concentration of 5-hydroxyindoleacetic acid when determined in urine.
The drug slightly increases the concentration of catecholamines and vanillylmygdalic acid, which can lead to false-positive test results when diagnosing pheochromocytoma and neuroblastoma. The drug should not be used during tests.
The drug may lead to erroneous results when determining serum urate concentration using the Bittner method.
Features of application
Use during pregnancy or breastfeeding.
The drug should not be used during pregnancy and breastfeeding.
The ability to influence the reaction rate when driving a vehicle or working with other mechanisms.
During treatment, care should be taken when driving vehicles and operating machinery, and in case of side effects on the part of the nervous system, refrain from potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
Directions for use and doses
For adults, the drug is administered subcutaneously in a dose of 1-2 ml of a 10% solution (100-200 mg). The highest single dose is 400 mg, the maximum daily dose is 1 g.
For children over 12 years of age, the drug should be administered subcutaneously at a dose (depending on age) of 0.25-1 ml of a 10% solution (25-100 mg).
Children
The drug should not be used in children under 12 years of age.
Overdose
Symptoms: anxiety, agitation, motor restlessness, agitation, tremors or muscle twitching, epileptic seizures (in case of acute overdose - tonic-clonic seizures), hyperesthesia, atrial scotoma, ringing in the ears, headache, insomnia, confusion, delirium, delirium, tachycardia, arrhythmia, hyperthermia, frequent urination, dehydration, nausea, vomiting, sometimes with blood.
Treatment: support of pulmonary ventilation, oxygenation, maintenance of fluid and salt balance, hemodialysis, for epileptic seizures - intravenous diazepam, phenobarbital or phenytoin.
Caffeine is medicinal product, which has a stimulating effect on the nervous system. Available in the form of tablets and solution for subconjunctival and subcutaneous administration.
Pharmacological action of Caffeine
Caffeine Sodium Benzoate is a psychostimulant drug, the active ingredient of which in all forms of release is caffeine.
Caffeine has a stimulating effect on the cerebral cortex, stimulates the work of the vasomotor and respiratory centers of the medulla oblongata, and stimulates reflex activity. Caffeine Sodium Benzoate promotes interneuronal conduction spinal cord, increases motor activity and mental activity, prevents drowsiness and helps overcome symptoms of fatigue.
When using small doses of the drug, stimulation of the functions of the nervous system is noted. The use of Caffeine Sodium Benzoate in large doses leads to inhibition of the functions of the central nervous system.
The active component of the drug affects the cardiac and vascular mechanisms of the body, which leads to changes in blood pressure: due to caffeine, low or slightly increased normal pressure occurs.
Caffeine in ampoules and tablets can increase physical and mental performance humans, has an antispasmodic effect on smooth muscles and a stimulating effect on striated muscles. Medicinal substance increases diuresis and gastric secretory activity, and also reduces platelet aggregation and the release of histamine from mast cells.
Thanks to Caffeine, the body's basal metabolism increases: glycolysis increases and lipolysis increases.
The use of caffeine by older people slows down the onset of sleep, significantly reduces its duration and increases the frequency of night awakenings.
In premature infants, when using Caffeine Sodium Benzoate, there is an elimination of periodic breathing, a decrease in the partial pressure of carbon dioxide, and an increase in the volume of ventilation without changes in heart rate.
A mixture of Caffeine and Capsicam is effectively used in cosmetology.
Indications for use of Caffeine
In ampoules and tablets, Caffeine is prescribed for decreased mental and physical performance, for headaches of vascular origin, migraines, and infectious diseases.
It is recommended to take Caffeine Sodium Benzoate for moderate arterial hypotension, drowsiness, enuresis, respiratory depression in newborns resulting from asphyxia, poisoning with opioid analgesics, hypnotics, carbon monoxide.
In surgical practice, the drug is used to restore required level pulmonary ventilation.
Caffeine is used in ophthalmology for decreased tone after surgery on the organs of vision, as well as for retinal detachment.
In cosmetology practice, a mixture of Caffeine and Capsicam is effectively used for wrapping procedures.
Directions for use and dosage
Caffeine tablets for adults are prescribed 50-100 mg 2-3 times a day, regardless of meals. The dose of the drug for children is 30-75 mg 2-3 times a day.
In ampoules, Caffeine is intended for subcutaneous administration. The permissible single dose of the drug is 100-200 mg, the maximum daily dose is 600 mg. For children over 12 years of age, it is recommended to administer 25-100 mg of solution 2-3 times a day.
In ophthalmology, Caffeine Sodium Benzoate is also used in ampoules - the solution is injected into the area under the conjunctiva, 0.3 ml once a day. The frequency of administration of the drug is prescribed and adjusted by the attending physician and depends on intraocular pressure and depth of the anterior eye chamber.
To prepare an anti-cellulite mixture for wrapping, mix 4 ampoules of Caffeine, Capsicam ointment (the size of 2 peas) and baby cream (4 peas). The resulting substance should be applied to problem areas and covered with cling film. You need to keep the application for 3 hours. It is not recommended to take food or any liquids during and for two hours after the wrap. The course is equal to 10 procedures.
Side effects of Caffeine
Both solution and Caffeine tablets can cause the following undesirable effects:
- feeling of restlessness, anxiety and agitation;
- muscle tension;
- increased fatigue;
- insomnia;
- cardiopalmus;
- headache;
- tremor;
- tachypnea;
- epileptic seizures.
Also, the body may experience tachycardia, arrhythmia, high blood pressure, nasal congestion.
Caffeine affects peptic ulcers, causing them to worsen.
With prolonged use of tablets and solution in ampoules, caffeine is addictive and addictive.
When wrapping with a mixture of Caffeine and Capsicam, a hot burning sensation may occur in the area of the procedure.
Contraindications for use
Caffeine is not prescribed for diseases of the cardiovascular system, anxiety disorders, tachycardia, arterial hypertension, extrasystole of the ventricular part, as well as in acute sleep disorders.
The drug is contraindicated in children under 12 years of age, elderly people with epilepsy, glaucoma, seizures, as well as women during pregnancy and lactation.
The anti-cellulite mixture of Caffeine and Capsicam should not be applied to the affected areas of the skin.
Overdose
An overdose of Caffeine and Sodium Benzoate may cause acute conditions anxiety, tremors, restlessness, headaches, cardiac extrasystoles, confusion.
Additional Information
During therapy, it should be taken into account that the drug enhances the effect of hypnotics and narcotic drugs, aspirin, paracetamol and other non-narcotic analgesics.
With the simultaneous use of caffeine with drugs that contain mexiletine, there is a deterioration in the process of removing caffeine from the body. The simultaneous use of this medication with nicotine increases and accelerates its elimination.
Caffeine in all forms must be stored in a dark, cool place out of the reach of children. The shelf life of the drug is 60 months.
Transparent colorless or slightly yellowish liquid.
Pharmacotherapeutic group
Psychostimulants and nootropics. Xanthine derivatives.
ATX code N06BC01
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% of the taken dose of the drug is metabolized in the liver, 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 of the 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, and the vessels of the abdominal cavity and skin narrow. 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 a positive inotropic effect, in higher doses it causes a 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). The highest single dose is 400 mg, the maximum daily dose is 1 g.
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
Excitement, anxiety, tremor, restlessness, insomnia, headache, dizziness, epileptic seizures, increased reflexes, tachypnea. If the drug is suddenly discontinued after long-term use, there will be increased effects on the central nervous system, 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 increase in urinary concentration
acid in blood plasma determined by the Bittner method, a slight increase in the concentration of 5-hydroxyindoleacetic acid, vanillylmandelic acid and catecholamines in the urine
Other: increased frequency of urination, nasal congestion,
long-term use – addiction, drug dependence
Contraindications
Hypersensitivity 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
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 determination of urate concentration in blood serum using the Bittner method.
Caffeine is an adenosine antagonist.
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.
