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

Caffeine is methylxanthine, which has a psycho-stimulating and analeptic effect. Competitively blocks central and peripheral A1 and A2 adenosine receptors. It inhibits the activity of phosphodiesterase in the central nervous system, heart, smooth muscle organs, skeletal muscles,adipose tissue, promotes the accumulation of cAMP and cGMP in them (this effect is observed when only high doses of caffeine are used). 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 stimulating effect on the centers n.vagus, the resulting effect depends on the prevalence of an action). It stimulates the vasomotor center and has a direct relaxant effect on the vascular wall, which leads to an expansion of the blood vessels of the heart,skeletal muscles and kidneys, while the tone of the cerebral arteries increases (causes a narrowing of the cerebral vessels, which is accompanied by a decrease in cerebral blood flow and oxygen pressure in the brain). Blood 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 cations in the proximal and distal renal tubules, as well as enlargement 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. Cmax -1.58-1.76 mg / l. Easily penetrates through the BBB and the placenta. The volume of distribution in adults is 0,4-0,6 l / kg, in newborns - 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%.

Adults around 80 % doses of caffeine are 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 (up to 4-7 months of life) - 65-130 hours. The excretion of caffeine and its metabolites is carried out by the kidneys (in unchanged form in adults it is excreted 1-2 %, in newborns - up to 85%).

Indications:

Decreased mental and physical working capacity, drowsiness, headache of vascular genesis (including migraine), mild arterial hypotension, respiratory depression (including with light poisoning with opioid analgesics and hypnotic drugs, carbon monoxide), restoration of the required level of pulmonary ventilation after the use of general anesthesia. Cyliochoroidal detachment in adults.

Contraindications:

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

Carefully:

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

Dosing and Administration:

Subcutaneously for adults 1 ml 100-200 mg / ml solution. The highest single dose is 0.4 g. The highest daily dose is 1 g.

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

In ophthalmic practice, adults are administered subconjunctivally in the form of 100 mg / ml of a solution of 0.3 ml once a day (30 mg).

Side effects:

From the central nervous system (CNS): 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, arrhythmia, increased blood pressure.

From the digestive system: nausea, vomiting, exacerbation of peptic ulcer. Other: nasal congestion, with prolonged use - addiction, drug dependence.

The administration of the drug subconjunctively causes short-term pain and small local edema with the possible emergence of single petechial hemorrhages.

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, 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.

Treatment: maintenance of ventilation and oxygenation; with epileptic seizures - intravenously diazepam, phenobarbital or phenytoin; maintaining the balance of liquid and salts.Hemodialysis.

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, ciprofloxacia, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increasing blood concentrations). Caffeine-containing drinks and other drugs that stimulate the central nervous system - excessive stimulation of the central nervous system is possible. Mexiletin - reduces caffeine withdrawal to 50%; nicotine - Increases the speed of caffeine removal. The monoamine oxidase inhibitors, furazolidone, procarbazine and selegiline - large doses of caffeine can cause the development of dangerous cardiac arrhythmias or a marked increase in blood pressure. 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 bronchodilating 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). 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. 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.

Form release / dosage:

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

Packaging:

1 ml per ampoule of neutral glass.

10 ampoules are placed in a box of cardboard and paper bundle. Each box is loaded with an ampoule knife or ampoule scarifier and instructions for use. A box is pasted with a label - a parcel post.

At packing ampoules with notches, rings and points of a knife ampoules and scarifiers do not put.

Storage conditions:

In the dark place at a pacefrom 0 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001182 / 01

Date of registration:13.04.2009

Expiration Date:Unlimited

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp21.01.2018

Illustrated instructions

Instructions

Caffeine-Benzoate Sodium Solution for Injection (Coffein-benzoate sodium solution for injections)