Caffeine benzoate solution for injection 20%, 1ml No. 10

• Decreased mental and physical performance, muscle weakness, drowsiness, migraine, moderate arterial hypotension, respiratory depression (including with mild poisoning with opioid analgesics and hypnotics, carbon monoxide, with asphyxiation of newborns, restoration of the required level of pulmonary ventilation after using general anesthesia).

• Hypotension of the eyeball (after abdominal eye surgery, ciliochoroidal retinal detachment, hypotonic retinal detachment).

Subcutaneously: adults, 100 mg or 200 mg. The highest single dose for adults is 400 mg, the highest daily dose is 1 g. For children, 25-100 mg, depending on age. In ophthalmology, 30 mg is administered subconjunctivally once a day, every day. The number of injections depends on the intraocular pressure and the depth of the anterior chamber.

1 ml of solution contains 200 mg of sodium caffeine-benzoate as an active substance and excipients - sodium hydroxide 0.1 M solution and water for injection.

• Hypersensitivity

• organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis),

• arterial hypertension,

• glaucoma, sleep disorders,

• increased excitability,

• elderly age,

• paroxysmal tachycardia,

• frequent ventricular premature beats,

• epilepsy and tendency to seizures.

• Pregnancy and lactation.

With care: glaucoma, irritability, old age.

Trade name of the drug: Caffeine-sodium benzoate

International non-proprietary name:

caffeine

Dosage form:

solution for subcutaneous and subconjunctival administration

Composition

1 ml of solution contains 100 mg or 200 mg of sodium caffeine-benzoate as an active substance and excipients - sodium hydroxide 0.1 M solution and water for injection.

Description

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:

psychostimulant

ATX code: [N06BC01]

Pharmacodynamics

It has a psychostimulating and analeptic effect. It has an exciting effect on the central nervous system (CNS), increasing excitation in the cerebral cortex, respiratory and vascular-motor centers, activates conditioned reflexes and physical performance, reduces drowsiness and fatigue, causes deepening and rapid breathing, increases heart rate, increases arterial pressure during hypotension, dilates the bronchi, biliary tract, blood vessels of skeletal muscles, reduces platelet aggregation, has a moderate diuretic effect, stimulates the secretion of gastric juice, increases basal metabolism and enhances glycogenolysis, causing hyperglycemia. The multiple pharmacological effects of the drug are due to the blockade of central and peripheral adenosine receptors. Inhibits phosphodiesterase,which leads to intracellular accumulation of cyclic adenosine monophosphate, under the influence of which the processes of glycogenolysis are enhanced, metabolic processes in organs and tissues are stimulated, including in muscle tissue and the central nervous system.

With subconjunctival administration, it improves microcirculation and activates the metabolic processes of the ciliary epithelium.

Pharmacokinetics

It is quickly distributed in all organs and tissues of the body, penetrates the blood-brain barrier and the placenta. The half-life is 3.9-5.3 hours (sometimes up to 10 hours). Communication with blood proteins (albumin) - 15%. More than 90% undergo metabolism in the liver, in children of the first years of life up to 10-15%. Caffeine is metabolized in the liver (the main part is demethylated and oxidized) to form 5 metabolites. Excretion of caffeine and its metabolites is carried out by the kidneys (10% - unchanged).

Indications for use

• Decreased mental and physical performance, muscle weakness, drowsiness, migraine, moderate arterial hypotension, respiratory depression (including with mild poisoning with opioid analgesics and hypnotics, carbon monoxide, with asphyxiation of newborns, restoration of the required level of pulmonary ventilation after using general anesthesia).

• Hypotension of the eyeball (after abdominal eye surgery, ciliochoroidal retinal detachment, hypotonic retinal detachment).

Contraindicated

• Hypersensitivity

• organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis),

• arterial hypertension,

• glaucoma, sleep disorders,

• increased excitability,

• elderly age,

• paroxysmal tachycardia,

• frequent ventricular premature beats,

• epilepsy and tendency to seizures.

• Pregnancy and lactation.

With care: glaucoma, irritability, old age.

Method of administration and dosage

Subcutaneously: adults, 100 mg or 200 mg. The highest single dose for adults is 400 mg, the highest daily dose is 1 g. For children, 25-100 mg, depending on age. In ophthalmology, 30 mg is administered subconjunctivally once a day, every day. The number of injections depends on the intraocular pressure and the depth of the anterior chamber.

Side effect

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

From the side of the cardiovascular system: tachycardia, heart rhythm disturbances, increased blood pressure.

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

Others: nasal congestion.

With prolonged use, slight addiction is possible (the decrease in action is associated with the formation of new adenosine receptors in the brain cells), drug dependence.

Overdose

Symptoms: increased severity of side effects. In newborns (including premature babies), anxiety, tachypnea, tachycardia, tremor, increased Moro reflex, at higher concentrations - convulsions are possible.

Treatment: symptomatic therapy, oxygen therapy, hemodialysis. In newborns, if necessary, exchange blood transfusion.

Interaction with other medicinal products

With the combined use of caffeine and barbiturates, primidone, antiepileptic drugs (hydantoin derivatives, especially phenytoin), it is possible to increase metabolism and increase the clearance of caffeine.

Simultaneous use with cimetidine, oral contraceptives, disulfiram, ciprofloxacin, norfloxacin leads to a decrease in the metabolism of caffeine in the liver, a slowdown in its excretion and an increase in blood concentration.

When used with caffeine-containing drinks and other drugs that stimulate the central nervous system, overstimulation of the central nervous system is possible. Caffeine is an adenosine antagonist - large doses of adenosine may be required.

Mexiletin - reduces the excretion of caffeine by up to 50%; nicotine - increases the rate of caffeine elimination.

Monoamine oxidase (MAO) inhibitors, furazolidone, procarbazine and selegiline - large doses of caffeine can cause the development of dangerous cardiac arrhythmias or a pronounced increase in blood pressure.

Caffeine reduces the effect of narcotic and sleeping pills. Increases the excretion of lithium (Li +) preparations in the urine.

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

The combined 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 decrease the clearance of theophylline and possibly other xanthines, increasing the potential for additive pharmacodynamic and toxic effects.

special instructions

It should be borne in mind that a sudden cessation of admission can lead to increased inhibition of the central nervous system (drowsiness, depression). The effect on the central nervous system can be manifested both by excitation and inhibition of higher nervous activity.

Release form

Solution for subcutaneous and subconjunctival administration of 100 mg / ml or 200 mg / ml. 1 ml or 2 ml of 10% (100 mg / ml) or 20% (200 mg / ml) solution in neutral glass ampoules. 10 ampoules with instructions for use and a knife for opening ampoules or an ampoule scarifier in a cardboard box or 5 or 10 ampoules in a blister strip made of polyvinyl chloride film, 1 or 2 blister packs with instructions for use and a knife for opening ampoules or ampoule scarifier in a cardboard box. When packing ampoules with a break ring or a break point, do not insert an ampoule opener or ampoule scarifier.

Storage conditions

List B.

At temperatures from + 15 ? — to + 25 ? — Store out of the reach of children.

Shelf life

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

Terms of dispensing from pharmacies:

on prescription.