Caffeine-benzoate sodium - instructions for use, dose, side effects, contraindications

Competitively blocks central and peripheral AT and A2 adenosine receptors. It inhibits the activity of phosphodiesterase in the central nervous system, heart, smooth and striated muscle tissue, adipose tissue, contributes to the accumulation of penicidal adenosine monophosphate and cyclic guanosine monophosphate in them (this effect occurs only with high doses of caffeine).Stimulates the centers of the medulla oblongata (respiratory and vasomotor), as well as the center of the vagus nerve, exerts a direct stimulating effect on the cortex, the brain. In high doses, "facilitates." Neuronal conduction in the spinal cord, reinforcing the reflexes.

Increases mental and physical performance, stimulates mental activity, motor activity, shortens the reaction time, temporarily reduces fatigue and drowsiness. In low doses, the effect of stimulation prevails, and in large doses the effect of inhibition of the nervous system prevails.

Takes and deepens breathing, usually has a positive foreign, chrono-, batmo- and droplet effect (since the effect on the cardiovascular system consists of direct stimulating action on the myocardium and a simultaneous exciting effect on the center of the vagus nerve, the resulting effect depends on the prevalence of a particular action).

Stimulates the vasomotor center and has a direct relaxing action on the vascular wall, which leads to the expansion of the vessels of the heart, skeletal muscles and kidneys, while the tone of the cerebral arteries rises (causes narrowing of the vessels of the headwhich is accompanied by a decrease in cerebral blood flow). Arterial pressure changes under the influence of vascular and cardiac mechanisms of caffeine influence:low initial arterial pressure caffeine does not change or slightly improves it, with arterial hypotension increases it.

Has spasmolytic effect on smooth muscles (including bronchodilator effect), on cross-striped - stimulating. Increases secretory activity sameand diuresis (reduced reabsorption of sodium and water in the proximal and distaltubular tubules, as well as enlargement of renal vessels and increased filtration in renal glomeruli).

Reduces platelet aggregation and histamine release from mast cells. Increases the basal metabolism: increases glycogenolysis, increases lipolysis.

Pharmacokinetics:

When taken orally, absorption is good; occurs throughout the intestine. Rapidly distributed in all organs and tissues of the body, penetrates through the blood-brain barrier and the placenta. The maximum concentration in blood plasma is achieved through 50-75 min; the half-life is 3.9-5.3 hours (sometimes up to 10 hours). Connection with protein blood (albumins) - 15 %. Metabolism in the liver is more than 90%, in children of the first years of life up to 10-15%. Caffeine is metabolized in the liver (the main part is dimethylated and oxidized) to form 5 metabolites. The excretion of caffeine and its metabolites is carried out by the kidneys (10% in unchanged form).

Indications:

Reduction of mental and physical performance, drowsiness, headache of the vascular systemstogo genesis (including migraine), moderate arterial hypotension.

Contraindications:

Hypersensitivity to the components of the drug (including other xanthines), anxiety disorders (agoraphobia, panic disorders), organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis), paroxysmal tahikardia, ventricular extrasystole, arterial hypertension, sleep disorders, children's age up to 12 years.

Carefully:

Glaucoma, increased excitability, elderly age, epilepsy and addiction to crampseizures.

Pregnancy and lactation:

Use is only possible after consultation with the doctor, if the expected benefit for the mother exceeds the potential risk to the fetus.

Dosing and Administration:

Assign inside regardless of food intake. Do not take before bedtime.

With a decrease in mental and physical performance, drowsiness - adults and children over 12 years - 50-100 mg 2-3 times a day. The course of treatment from several weeks to nothow many months depending on the condition of the patient.

With headache of vascular genesis (including migraine) - adults and children over 12 years of age - by 50-100 mg 2-3 times a day for several days.

With moderate arterial hypotension - adults and children over 12 years - 50 - 100 mg 2-3 times a day. The course of treatment is several weeks.

The highest single dose for adults is 300 mg, the highest daily dose for adults is 1000 mg;

The highest single dose for children from 12 years is 150 mg, the highest daily dose for children is 500 mg.

Side effects:

From the central nervous system: psychomotor agitation, anxiety, tremor, anxiety, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, insomnia; with sudden withdrawal - increased inhibition of the central nervous system, increased fatigue, drowsiness, muscle tension.

From the side of the cardiovascular system: palpitation, tachycardia, increased blood pressure.

From the digestive system: nausea, vomiting, exacerbation of peptic ulcer.

Other: nasal congestion, with prolonged use - addiction, drug dependence.

Overdose:

Symptoms: gastralgia, agitation, anxiety, agitation, motor anxiety, 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, convulsions (with acute overdose - tonic-clonic).

Caffeine in doses more than 300 mg / day (including against the background of the abuse of coffee - more than 4 cups of natural coffee of 150 ml) can cause anxiety, tremor, headache,annity of consciousness, 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; reception of activated carbon, laxative drugs; with hemorrhagic gastritis - the introduction of antacid drugs and gastric lavage icy 0.9 % solution of sodium chloride; maintenance of ventilation and oxygenation; with convulsions - in / in diazepam, phenobarbital or phenytoin; maintenance of water-electrolyte balance.

Interaction:

Caffeine is an adenosine antagonist (large doses of adenosine may be required).

With the joint use of caffeine and barbiturates, primidone, anticonvulsant drugs (hydantoin derivatives, especially phenytoin) it is possible to increase metabolism and increase caffeine clearance; cimetidine, oral contraceptives, disulphuram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver .. (slowing its elimination and increase in blood concentration).

Caffeine-containing drinks and other medicines that stimulate the centerMr.yy nervous system, - excessive stimulation of the central nervous system is possible.

Mexiletine - reduces caffeine withdrawal by 50 %; nicotine - Increases the speed of caffeine removal.

Inhibitors of monoamine oxidase, furazolidone, procarbazine and selegiline - large doses of kofein (more than 300 mg / day) can cause the development of life-threatening heart arrhythmias or - a pronounced increase in blood pressure.

Caffeine reduces the absorption of calcium in the gastrointestinal tract.

Reduces the effectiveness of narcotic and hypnotic drugs.

Increases the excretion of lithium drugs with urine;

Accelerates absorption and enhances the action of cardiac glycosides, increases their toxicitytion. Joint application with beta-blockers can lead to mutual suppression of therapeutic effects; from β-adrenomimetics - to additional stimulation of the central nervous system and other additive toxic effects.

Caffeine can reduce clearance; theophylline and, possibly, other xanthines, increasingPossibility of additive pharmacodynamic and toxic effects.

Special instructions:

It should be borne in mind that a sudden discontinuation of reception can lead to increased inhibition of the central nervous system (drowsiness, depression).

Influence on the central nervous system depends on the type of nervous system and can be manifested as excitation or inhibition of higher nervous activity.

Due to the fact that the effect of caffeine on blood pressure is composed of vascular and cardiac components, as a result can develop as a stimulation effect of the hearttsa, and oppression (weak) of his activity.

Do not take before bedtime.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and occupying potentially harmful activities that require concentration and speed of psychomotor reactions.

Form release / dosage:Tablets of 100 mg.

Packaging:For 6 or 10 tablets in a contiguous, non-jawed package or 10 tablets in a planar cell package. 1 or 2 contour mesh packages together with the instruction for use are placed in a cardboard pack. Contoured cell packs and contour non-jawed packages with an equal number of instructions for use are placed directly in the group package.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001544

Date of registration:03.08.2011

Expiration Date:Unlimited

The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia

Manufacturer: & nbsp

TATHIMFARMPREPARATY, JSC Russia

Information update date: & nbsp21.01.2018

Illustrated instructions

Instructions

Caffeine-sodium benzoate (Coffein-benzoate sodium)