The instruction for use
of medicine for experts
of Coffeinum natrio-benzoicum
A trade name
the International unlicensed name
Is not present
the Dosage form
Solution for injections of 20%
1 ml of solution contains
active agents: caffeine of 0.08 g, Natrium benzoicum of 0.12 g,
excipients: hydroxide 0.1M sodium solution, water for injections.
Transparent colourless or slightly yellowish color liquid.
Psychostimulants and nootropa. Xanthine derivatives.
The code of automatic telephone exchange N06BC01
Pharmacokinetics Later properties of hypodermic introduction absorption happens quickly and fully. Well gets through all gistogematichesky barriers, being distributed on bodies and fabrics. Gets through GEB and a gematoplacentrany barrier. Concentration in liquor and amniotic liquid are comparable to concentration of caffeine in blood plasma. In saliva the concentration of caffeine makes 65-85% of its concentration in plasma.
After introduction is exposed to intensive metabolism in a liver with education dimetil- and monomethylxanthines, dimetil- and monomethyl-uric acid, trimetil- and dimethylallantoin, uridine derivatives. The main way of metabolism education under the influence of an isoform of P450 CYP1A2 cytochrome of the dimethylxantines (theophylline, paraxanthine) having pharmacological activity (72-80% of the entered dose).
The semi-elimination period (T½) caffeine is 2.5-4.5 h, at newborns in connection with low enzymatic activity of microsomal enzymes the elimination of caffeine is slowed down, T½, makes 80 & plusmn, 23 h, at the age of 3-5 months it decreases up to 14.4 h and in 5-6 months becomes to equal indicators of the adult. The general clearance of caffeine at the adult is 155 ml/kg/h, at the newborn child it is equal to 31 ml/kg/h.
At the smoking persons the reduction of the period of semi-elimination of caffeine by 30-50% in comparison with non-smoking persons is observed.
Caffeine mainly with urine in the form of metabolites is emitted. 10% of the entered dose are allocated in not changed look.
Has psychogogic and analeptical properties.
The mechanism of action is connected with ability of caffeine to act as the competitive antagonist of purine A1 and A2A-receptors. As a result of blockade of receptors, processes of braking in central nervous system decrease, secretion of neurotransmitters (serotonin, noradrenaline and dopamine) in motor zones of a cerebral cortex, a hypothalamus and a medulla is facilitated and stabilized. In doses of relatives to toxic caffeine is capable to block activity of phosphodiesterases (mainly III, IV types) and to slow down disintegration of tsAMF and tsGMF that stimulates activity of neurons and accelerates a metabolism in a cell.
Strengthening of dofaminergichesky transfer in synapses of a cerebral cortex makes psychogogic impact. Activation of adrenergic transfer in synapses of a hypothalamus and a medulla activates cortical functions, increases physical activity, causes anorexia, makes tonic impact on a vasomotor center. Strengthening of cholinergic transfer in synapses of bark and a medulla activates cortical functions, increases activity of a respiratory center.
Caffeine has direct exciting impact on central nervous system: stimulates mental activity, increases intellectual and physical effeciency, shortens reaction time, activates positive conditioned reflexes. After administration of caffeine the cheerfulness appears, the exhaustion and drowsiness temporarily decrease or eliminated. At elderly people the influence on a dream is more significant: approach of a dream slows down, the general time of a dream decreases and the frequency of night awakenings increases.
Against the background of oppression of a respiratory center causes increase and deepening of breath. Influences a cardiovascular system: increases the frequency and force of warm reductions, in hypotension raises the ABP (does not influence the AD normal level). At premature children eliminates periodic breathing due to decrease in partial pressure of carbon dioxide in blood, increases ventilation volume, without influencing significantly function of a cardiovascular system.
Relaxes smooth muscles of bronchial tubes, bilious ways, causes dilatation of vessels of skeletal muscles, heart and kidneys, narrows vessels of abdominal organs (especially at their initial dilatation). Has weak diuretic effect due to expansion of renal vessels and braking of a reabsorption of electrolytes in renal tubules.
Reduces aggregation of thrombocytes. Stimulates secretion of glands of a stomach. Increases standard metabolism, strengthens a glycogenolysis, causing a hyperglycemia.
– the states connected with oppression of the central nervous system functions, respiratory and cardiovascular systems: poisonings with drugs, serious infectious diseases, states after use of the general anesthetics (anesthesia)
– brain angiospasms
– decrease in intellectual and physical effeciency in the period of a convalescence after the postponed serious somatic and infectious diseases
– a narcolepsy
– breath disturbances (periodic breathing, idiopathic an apnoea) at newborns, including premature children.
The route of administration and doses
Is entered by the adult subcutaneously on 200 mg (1 ml of 20% of solution), children on 25-100 mg (0.25 – 1 ml of 10% of solution or 0.1 – 0.5 ml of 20% of solution) 2-3 times a day. For elimination of an apnoea at newborns solution of caffeine Natrium benzoicum is entered intravenously or through a mouth.
Intramuscular administration of solution of caffeine Natrium benzoicum is not recommended in connection with a possibility of development of painful spastic reduction of muscles in the place of an injection.
– concern, excitement, insomnia
– tachycardia, arrhythmia, increase arterial blood pressure
– nausea, vomiting
– development of weak psychological dependence and tolerance at prolonged use in high doses
– at sudden phase-out is possible development reactive exhaustions, drowsiness and a depression.
– arterial hypertension of the III degree
– organic diseases of a cardiovascular system (including atherosclerosis)
– hyperexcitability, sleep disorders
– senile age.
At simultaneous use caffeine strengthens action of antiagregantny means.
Reduces effect of the sleeping, narcotic and other medicines oppressing central nervous system.
At simultaneous use increases bioavailability of acetylsalicylic acid, paracetamol and ergotamine enhancing that their effect.
At simultaneous use from b2-adrenomimetika in high doses (salmeterol, salbutamol, Fenoterolum) risk of development of a hypopotassemia increases.
At simultaneous use with drugs of methylxanthines (theophylline, Aminophyllinum) the increase in concentration of theophylline in blood plasma and increase of risk of its toxic action is observed.
Anticonvulsants (carbamazepine, dipheninum), barbituric drugs accelerate metabolism of caffeine and reduce its concentration in plasma.
The combined oral contraceptives, makrolidny antibiotics (klaritromitsin, erythromycin), drugs of interferon and antifungal means (ketokonazol, flukonazol) slow down metabolism of caffeine and increase its concentration in plasma.
When using caffeine-sodium benzoate at the smoking persons of its concentration in blood plasma below, than at non-smoking patients.
instructions Pregnancy and a lactation
As adequate and well controlled researches at women during pregnancy were not conducted and also considering slow elimination of caffeine from a fruit organism the use it during pregnancy is possible only after ratio assessment advantage/risk for mother and a fruit. Caffeine and its metabolites are excreted in mother’s milk in insignificant quantities. In need of its use in the period of a lactation it is necessary to estimate a ratio advantage/risk for mother and the child.
Use in a neonatology
Kofein can be applied in the period of a neonatality and also at premature children. At the same time it is necessary to monitorirovat concentration of caffeine in plasma and to support her within therapeutic borders (3-10 mkg/ml).
Use for persons in the anamnesis
Is required to be careful with a peptic ulcer of a stomach and duodenum when prescribing caffeine to these groups of patients, in connection with the increased risk of aggravation at them a peptic ulcer.
Influence on ability to performance of work, connected with need of concentration of attention
At intake in high doses caffeine complicates concentration of attention and increases number of the operator mistakes when working interfaced to need of concentration of attention.
Symptoms of intoxication arise at the use of caffeine in a dose more than 300 mg/days (though use cases more than 1000 mg/days of caffeine are described). Emergence of alarm, concern, a tremor, a headache, confusion of consciousness, a tachyarrhythmia is possible. At newborn children at concentration in blood more than 50 mkg/ml of caffeine perhaps except the above picture pathological strengthening of reflexes, emergence of a convulsive syndrome.
Specific antidote does not exist. Measures of the help include the drug withdrawal supporting and the symptomatic therapy directed to elimination of the arisen disturbances, control of level of arterial blood pressure and stopping of a convulsive syndrome by administration of tranquilizers of a benzodiazepine row (diazepam).
A form of release and packing
of the Ampoule on 1 ml. On 10 ampoules with a knife for opening of ampoules in a box of cardboard.
In the place protected from light, at
a temperature not higher than 25 S. Hranit out of children’s reach!
Not to use an expiration date of 5 years after expiry date.
RUP Producer the Borisovsky plant of medications,
Republic of Belarus. Minsk Region, Borisov, Chapayev St., 64/27
To develop prescription status According to the prescription