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

Caffeine - methylxanthine, which has psychostimulant and analeptic effect. Competitively blocks central and peripheral A1 and A2 adenosine receptors. It inhibits the activity of phosphodiesterase (PDE) in the central nervous system (CNS), heart, smooth muscle organs, skeletal muscles, adipose tissue, promotes the accumulation in them of a cyclicadenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) (this effect is observed with only high doses of caffeine). Stimulates the centers of the medulla oblongata (respiratory and vasomotor), as well as the center n.vagus, has a direct stimulating effect on the cerebral cortex. In high doses, it facilitates interneuronal conduction in the spinal cord, strengthening spinal reflexes.

Increases mental and physical performance, stimulates mental activity, motor activity, shortens the reaction time, temporarily reduces fatigue and drowsiness. In small 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 dromotropic effect (since the effect on the cardiovascular system consists of direct stimulating action on the myocardium and a simultaneous excitatory effect on the centers n.vagus, the resulting effect depends on the prevalence of an action). Stimulates the vasomotor center and has a direct relaxing effect 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 cerebral vessels, which is accompanied by a decrease in cerebral blood flow and oxygen pressure in the brain). Arterial pressure changes under the influence of vascular and cardiac mechanisms of caffeine influence: at normal initial arterial pressure caffeine does not change or slightly increases it, with arterial hypotension normalizes it.

Has an antispasmodic effect on smooth muscles (including bronchodilating effect), on the striated - stimulating. Increases the secretory activity of the stomach and diuresis (reduced reabsorption of sodium and water in the proximal and distal renal tubules, as well as expansion of the kidney vessels and increased filtration in the renal glomeruli).

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

Pharmacokinetics:

Quickly distributed in all organs and tissues of the body. Stach - 1.58-1.76 mg / l. Easily penetrates the blood-brain barrier and the placenta.

The volume of distribution in adults is 0.4-0.6 l / kg, in newborns it is 0.78-0.92 l / kg. Communication with blood proteins (albumins) is 25-36%.

Metabolism in the liver is more than 90%, in children of the first years of life up to 10-15%.

In adults, about 80% of the dose of caffeine is metabolized to paraxanthin, about 10% to theobromine and about 4% to theophylline. These compounds are subsequently demethylated into monomethylxanthines, and then into methylated uric acids. T1 / 2 in adults - 3.9-5.3 hours (sometimes - up to 10 hours); in newborns - 65-130 hours, to 4-7 months of life decreases to the value as in adults. The excretion of caffeine and its metabolites is carried out by the kidneys (in unchanged form in adults it is deduced 1-2%, in newborns - up to 85%).

Indications:

Decreased mental and physical performance, drowsiness, headache of vascular genesis (including migraine), moderate arterial hypotension, respiratory depression (including with light poisoning with narcotic analgesics and hypnotic drugs, carbon monoxide, with asphyxiation of newborns), restoration of pulmonary ventilation after using general anesthesia. Cyliochoroidal detachment in adults.

Contraindications:

Hypersensitivity (including to other xanthines), anxious disorders (agoraphobia, panic disorders), organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis), paroxysmal tachycardia, frequent ventricular extrasystole, arterial hypertension, sleep disorders, children under 18 years of age (for subconjunctival administration). Pregnancy and lactation.

Carefully:

Glaucoma, increased excitability, elderly age, epilepsy and a tendency to convulsive seizures.

Pregnancy and lactation:

Application during pregnancy is contraindicated. If you need to use the drug during lactation at the time of treatment should stop breastfeeding.

Dosing and Administration:

Subcutaneously for adults 1 ml of solution (100-200 mg). The highest single dose is 0.4 g, the highest daily dose is 1 g.

Subcutaneously to children (depending on age) - to 0.25-1 ml of solution (25-100 mg).

In ophthalmic practice, adults are administered subconjunctively in the form of a solution of 0.3 ml once a day (30 mg).

Side effects:

From the nervous system: agitation, anxiety, tremor, headache, dizziness, epileptic seizures, increased tendon reflexes, tachypnea, insomnia.With a sudden abolition - increased inhibition of the central nervous system, increased fatigue, drowsiness, increased muscle tone.

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

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

Other: nasal congestion, with prolonged use - addiction, drug dependence; with subconjunctivaznom introduction of short-term pain, a small local edema with the possible emergence of individual petechiae.

Overdose:

Symptoms: gastralgia, agitation, anxiety, agitation, motor anxiety, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensation, tremor or muscle twitching; nausea and vomiting, sometimes with blood; ringing in the ears, epileptic seizures (with acute overdose - tonic-clonic). Caffeine in doses of 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, confusion, extrasystole.

In newborns (including prematurity): anxiety, tachypnea, tachycardia, tremor, increased Moro reflex, at higher concentrations - convulsions.

Treatment: symptomatic therapy, maintenance of ventilation and oxygenation, with epileptic seizures - intravenously diazepam, phenobarbital or phenytoin, maintaining a balance of fluid and salts, hemodialysis. In newborns, if necessary, exchange blood transfusion.

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 contraceptive drugs, disulfiram, ciprofloxacin, norfloxacin - decrease metabolism of caffeine in the liver (slowing its excretion and increase in concentration in the blood).

Caffeine-containing beverages and other medicines that stimulate the central nervous system may cause excessive stimulation of the central nervous system.

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

Inhibitors of monoamine oxidase, 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 in the gastrointestinal tract.

Reduces the effect of narcotic and hypnotic drugs. Increases the excretion of lithium drugs with urine.

Accelerates absorption and enhances the action of cardiac glycosides, increases their toxicity.

Joint use of caffeine with beta-blockers can lead to mutual suppression of therapeutic effects; with adrenergic bronchodilator drugs - to additional stimulation of the central nervous system and other additive toxic effects.

Caffeine can reduce the clearance of theophylline and, possibly, other xanthines, increasing the possibility 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 depends on the type of the nervous system and can be manifested both by excitation and inhibition of the higher nervous activities.

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.

Do not take before bedtime.

Effect on the ability to drive transp. cf. and fur:

The drug should not be used during work drivers of vehicles and people,The profession of which requires an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

A solution for subcutaneous and subconjunctival administration of 100 mg / ml or 200 mg / ml.

Packaging:

1 ml or 2 ml into neutral glass ampoules.

For 10 ampoules with instruction for use and a knife for opening ampoules or a scarifier ampullum is placed in a box of cardboard.

5 or 10 ampoules are placed in a contoured cell pack of a polyvinylchloride film or polyethylene terephthalate tape and aluminum foil or paper with a polyethylene coating or without a foil, or without paper.

For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.

When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.

Storage conditions:

At a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

Shelf life 6 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001257 / 01

Date of registration:30.01.2012

Expiration Date:Unlimited

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Information update date: & nbsp21.01.2018

Illustrated instructions

Instructions

Sodium caffeine-benzoate (Coffein-benzoate sodium)