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

Caffeine is methylxanthine, which has a psycho-stimulating and analeptic effect. Competitively blocks the central and peripheral Ai and A2 adenosine receptors. It inhibits the activity of phosphodiesterase in the central nervous system, heart, smooth muscle organs, skeletal muscles, adipose tissue. Stimulates the centers of the medulla oblongata (respiratory and vasomotor), 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.

It increases and deepens the breathing, 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 a narrowing of the cerebral vessels, which is accompanied by a decrease in the cerebral cortexflow and pressure of oxygen 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 ions in the proximal and distal renal tubules, as well as expansion of renal 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:

It is quickly distributed in all organs and tissues of the body: it easily penetrates the blood-brain barrier 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 - 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 monomethylxanthates, and then into methylated uric acids. The half-life in adults is 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 adults are withdrawn 1-2%, in newborns - up to 85%).

Indications:

Decrease in mental and physical working capacity, 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 asphyxiated infants) , restoration of pulmonary ventilation after the use of general anesthesia.

Cyliochoroidal detachment in adults.

Contraindications:

Hypersensitivity (including other xanthines), anxiety disorders, severe arterial hypertension, organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis), paroxysmal tachycardia, frequent ventricular extrasystole, sleep disorders, children under 18 (for subconjunctival administration).

Carefully:

Use with caution in glaucoma, increased excitability, in old age, with epilepsy and a tendency to convulsive seizures.

Pregnancy and lactation:

Excessive use of the drug during pregnancy can lead to spontaneous abortion, slowing fetal development,arrhythmias 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.

The drug penetrates into breast milk in small amounts, but accumulates in infants and can cause hyperactivity and insomnia. For the duration of treatment, stop breastfeeding.

Dosing and Administration:

Caffeine-benzoate sodium is used subcutaneously and subconjunctivally.

Doses of the drug are selected individually. Higher doses for adults (under the skin): single 0.4 g, daily 1 g. Adults 1 ml 10-20% solution (100-200 mg); children (depending on age) - 0.25-1.0 ml 10% solution (25-100 mg).

In ophthalmic practice, subconjunctival 10% solution is administered at 0.3 ml once a day (30 mg). The number of injections depends on the intraocular pressure and the depth of the anterior chamber.

Side effects:

From the nervous system: agitation, anxiety, tremor, anxiety, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, ringing in the ears, 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; with subconjunctival injection - a short-term pain, a small local edema with the possible emergence of individual petechiae.

Overdose:

Symptoms: gastralgia, agitation, anxiety, agitation, motor anxiety, confusion, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, tremor, or muscle twitching; nausea and vomiting; ringing in the ears, epileptic fits.

In newborns (including prematurity) at a concentration of caffeine in plasma of 50 mg / ml toxic effects are possible: anxiety, tachypnea, tachycardia, tremor, painful swollen abdomen or vomiting, increase in Moro reflex, at higher concentrations - convulsions.

Treatment: maintenance of ventilation and oxygenation; with epileptic seizures - intravenously diazepam, phenobarbital or phenothoin; maintaining the balance of liquid and salts.Hemodialysis, in newborns if necessary - exchange blood transfusion.

Interaction:

Reduces the effect of hypnotics and drugs, increases (improving the bioavailability) - acetylsalicylic acid, paracetamol and other non-narcotic analgesics, increases the excretion of lithium drugs with urine. Joint use of the drug with beta-adrenoblockers can lead to mutual suppression of therapeutic effects. Accelerates absorption and enhances the action of cardiac glycosides, increases their toxicity.

Special instructions:

It should be borne in mind that a sudden discontinuation of medication 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.

The connection with 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), applied caffeine or caffeine citrate, but not caffeine - sodium benzoate.

Do not take before bedtime.

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

Given the side effect of the drug during the period of treatment, care must be taken when driving vehicles, taking other potentialsThese are socially dangerous activities requiring an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

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

Packaging:

1 ml or 2 ml into neutral glass ampoules. 10 ampoules together with a vial for opening ampoules or a scarifier ampoule and instructions for use in a cardboard box. 5 ampoules per circuit cell box made of polyvinyl chloride film and foil of aluminum printed lacquered or foil-free. 2 contoured cell packs together with instructions for use and a knife for opening ampoules or a scarifier ampullum in a pack of cardboard. When using ampoules with notches,rings and dots scarifier ampoule or opener for opening ampoules do not invest.

Storage conditions:

At a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000493

Date of registration:05.05.2010 / 27.12.2012

Expiration Date:Unlimited

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

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp21.01.2018

Illustrated instructions

Instructions

Sodium caffeine-benzoate (Coffein-benzoate sodium)