Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
Pharmacodynamics:Antagonism against central adenosine receptors, stimulation of the centers of the medulla oblongata (vagal, vasomotor and respiratory).
Stimulates the central nervous system, breathing, skeletal muscles, secretion of pepsin and hydrochloric acid in the digestive tract, glycogenolysis. Increases the sensitivity of the respiratory center to the stimulating effect of carbon dioxide, increasing the alveolar ventilation.
Increases the strength and heart rate, the minute volume of the heart (a positive inotropic effect on the myocardium and a positive chronotropic effect on the sinus-atrial node).
Has hypertensive and diuretic effects, stimulates the narrowing of the vessels of the brain and reduces the contractility of the uterus.
Pharmacokinetics:The connection with plasma proteins is 25-36%. The biotransformation in the liver, adult 80% of the caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% - theobromine (3,7-dimethylxanthine) and 4% - a theophylline (1,3-dimethylxanthine), the compounds are demethylated in monomethylxanthines, and then into methylated derivatives of uric acid. Preterm infants theophylline turns into caffeine. The half-life is 3-7 hours, in newborns - 65-130 hours, decrease to the level of adults in 4-7 months. Maximum concentration through 50-75 minutes. It is excreted by the kidneys (in the form of metabolites, 1-2% unchanged), in newborns by the kidneys (85% unchanged).
Indications:Diseases accompanied by depression of the cardiovascular and respiratory systems (including poisoning with drugs, infectious diseases).
Oppression of the central nervous system.
Spasms of cerebral vessels (including migraine).
Decreased mental and physical performance.
Enuresis in children.
Drowsiness.
Respiratory disorders (periodic respiration, idiopathic apnea) in newborns.
V.F50-F59.F51.1 Drowsiness [hypersomnia] inorganic etiology
IX.I70-I79.I73 Other peripheral vascular diseases
VI.G40-G47.G43 Migraine
XVIII.R30-R39.R32 Urinary incontinence, unspecified
XVIII.R50-R69.R53 Malaise and fatigue
XIX.T36-T50.T40 Poisoning and Drug psychodysleptics [hallucinogens]
XXI.Z70-Z76.Z73.6 Limitations of activities caused by a decrease or loss of ability to work
Contraindications:Individual intolerance, including other xanthines.
Anxiety disorders (agoraphobia, panic disorder).
Organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis).
Paroxysmal tachycardia, frequent ventricular extrasystole.
Arterial hypertension.
Sleep disorders in the therapy of increased fatigue and drowsiness.
Children under 12 years.
Carefully:Glaucoma.
Increased excitability.
Elderly age.
Epilepsy and a tendency to seizures.
Pregnancy and lactation.
Pregnancy and lactation:FDA recommendations in category C. Increased risk of developing spontaneous abortions, intrauterine growth retardation, arrhythmia in the fetus (high doses). Experiments on animals: a violation of the development of the skeleton (fingers and individual phalanges) with doses equivalent to caffeine in 12-24 cups of coffee per day,during the entire pregnancy or with single administration of large doses (50-100 mg / kg); in smaller doses - slowing the development of the skeleton.
Penetrates into breast milk (1% of its concentration in the blood plasma of the mother). If a nursing mother consumes 6-8 cups of caffeine-containing drinks per day, the child may develop hyperactivity and insomnia.
Dosing and Administration:Inside (regardless of food intake): adults - 0,05-0,1 g per dose 2-3 times a day (maximum daily dose - 1 g), children over 2 years old - 0,03-0,075 g per day reception.
PIn migraine (often combined with non-narcotic analgesics and ergot alkaloids) - 1-2 tablets during a pain attack, then - 1 tablet 2-3 times a day for several days (up to 1 month).
In the form of sodium caffeine-benzoate, subcutaneously: adults - 1 ml 10% or 20% solution, children - 0.25-1 ml 10% solution. For the removal of apnea in newborns - enter through the mouth or intravenously (in the form of caffeine-citrate), creating a concentration of caffeine-base in blood plasma from 3 to 10 mg / ml.
Side effects:Nervous system: dizziness, headache, anxiety, irritability, nervousness, marked neural excitation in newborns; tremor, sleep disturbance, muscle tension.
The cardiovascular system: cardiopalmus.
Digestive system: diarrhea, nausea, vomiting, necrotizing enterocolitis.
Blood: hypoglycemia, hyperglycemia.
Overdose:In case of an overdose, pain in the abdomen or stomach is observed; agitation, anxiety, agitation or motor anxiety; confusion or delirium; dehydration; tachycardia, arrhythmia; frequent urination; headache; increased tactile or pain sensitivity; irritability; tremor or muscle twitching; nausea and vomiting, sometimes with blood; painful, swollen abdomen or vomiting in newborns; ringing in the ears or sensation of other sounds; photopsy; epileptic seizures, usually clonic-tonic convulsions in acute overdose; sleep disturbance; whole body trembling in newborns.
Treatment is symptomatic - 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; Activated carbon, laxatives; with hemorrhagic gastritis - the introduction of antacid drugs and washing the stomach with an ice 0.9% solution of sodium chloride; maintenance of ventilation and oxygenation; atepileptic seizures - intravenously diazepam, phenobarbital or phenytoin; maintaining the balance of liquid and salts. Hemodialysis, in newborns if necessary - exchange blood transfusion.
Interaction:Caffeine-containing drinks (coffee, tea, soft drinks) or other caffeine-containing drugs or other means that cause CNS stimulation, - CNS stimulation, with nervousness, irritability, insomnia, convulsions, cardiac arrhythmias.
Inhibitors of monoamine oxidase (MAO), furazolidone, procarbazine and selegiline - arrhythmias or severe hypertension (large doses); increased blood pressure and tachycardia (small doses).
Special instructions:Sudden discontinuation may lead to increased inhibition of the central nervous system (drowsiness, depression).
The effect on the CNS depends on the type of nervous system and can be manifested both by excitation and inhibition of higher nervous activity.
Due to the fact that the effect of caffeine on blood pressure is made up of the vascular and cardiac components, as a result, both the effect of heart stimulation and the oppression (weak) of its activity can develop.
In apnea in newborns and in infants in the postoperative period (prevention) is applied caffeine or caffeine citrate, but not caffeine-sodium benzoate. Excessive use during pregnancy can lead to spontaneous abortion, slowing fetal development, arrhythmia in the fetus; there may be a developmental disability of the skeleton when using large doses and slowing the development of the skeleton against a background of smaller doses. It penetrates into breast milk in small amounts, but accumulates in infants and can cause hyperactivity and insomnia.