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

Caffeine is methylxanthine, which has a psychostimulating 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 cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) (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 cortex of the brain. 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 (CVS) 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). 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 increases (causes a narrowing of the cerebral vessels, which is accompanied by a decrease in cerebral blood flow and oxygen pressure in the brain). Arterial pressure (BP) varies under the influence of vascular and cardiac mechanisms of caffeine influence: with normal initial BP caffeine does not change or slightly increases it, with arterial hypotension normalizes it.

Has a spasmolytic effect on smooth muscles (including bronchodilator 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:

After the subcutaneous injection is absorbed quickly and completely. It penetrates well through all the histohematological barriers, spreading over organs and tissues. Penetrates through the BBB and the hematoplacental barrier.Concentrations in liquor and amniotic fluid are comparable with the concentrations of caffeine in the blood plasma. In saliva, the concentration of caffeine is 65-85% of its concentration in the plasma.

After the introduction, it undergoes intensive metabolism in the liver with the formation of dimethyl- and monomethylxanthines, dimethyl- and monomethyl-uric acid, trimethyl- and dimethylallantoin, derivatives of uridine. The main pathway of metabolism is the formation under the influence of the cytochrome P isoform₄₅₀ CYP1A2 dimethylxanthines (theophylline, paraxanthin), having pharmacological activity (72-80% of the administered dose).

The half-eligation period (T1 /₂) of caffeine is 2.5-4.5 h, in newborns due to low enzymatic activity of microsomal enzymes, the elimination of caffeine is slowed down, T1_/2 is 80 ± 23 hours, at the age of 3-5 months it decreases to 14.4 hours and in 5-6 months it becomes equal to the indicators of an adult. The total clearance of caffeine in an adult is 155 ml / kg / h, in a newborn baby it is 31 ml / kg / h.

Smokers have a decrease in the half-eligination period of caffeine by 30-50 % compared with non-smokers.

Is allocated caffeine mainly with urine in the form of metabolites. 10 % The administered dose is released unchanged.

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 asphyxiated infants), restoration of pulmonary ventilation after using a common anesthesia.

Cyliochoroidal detachment in adults.

Contraindications:

Hypersensitivity (including to other xanthines), anxiety disorders (agoraphobia, panic disorders), organic diseases of the cardiovascular system (CCC) (including acute myocardial infarction, atherosclerosis), paroxysmal tachycardia, frequent ventricular extrasystole, arterial hypertension, sleep disorders, children under 12 years (for oral LF), children under 18 (for subconjunctival administration).

Carefully:Glaucoma, increased excitability, elderly age, epilepsy and propensity to convulsive seizures, pregnancy, lactation.

Pregnancy and lactation:

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.

Dosing and Administration:

S / o: adults with 1 ml 10 - 20 % solution (100-200 mg); children (depending on age) - 0.25 - 1 ml 10 % solution (25-100 mg).

The highest single dose is 0.4 g, the highest daily dose is 1 g.

In ophthalmic practice, adults are administered subconjunctivally in the form of a 10% solution of 0.3 ml once a day (30 mg).

Side effects:

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

On the part of the CAS: 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 - short-term pain, a small local swelling with the possible appearance of single petechiae.

Overdose:

Symptoms: Gastralgia, agitation, anxiety, agitation, restlessness, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, tactile or pain sensitivity, tremors or muscle twitching; nausea and vomiting, sometimes with blood; ringing in the ears, epileptic seizures (with acute overdose - tonic-clonic).

Caffeine in doses of 300 mg / day (including amid abuse coffee - a cup natural coffee 4 150 ml) can cause anxiety, tremor, headache, confusion, extrasystole.

In newborn (including premature) at plasma concentrations of caffeine 50 mg / ml may be toxic effects include restlessness, tachypnea, tachycardia, tremors, painful, swollen stomach or vomiting, increased Moro reflex, at higher concentrations - seizures.

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 (LS); with hemorrhagic gastritis - the introduction of antacids and gastric lavage with ice 0.9% solution of sodium chloride; maintenance of ventilation and oxygenation; with epileptic seizures - in / in diazepam, phenobarbital or phenytoin; maintaining the balance of liquid 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 - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increase in blood concentration).

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

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

Inhibitors of monoamine oxidase (MAO), 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 bronchodilating drugs - to additional stimulation of the CNS, 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.

In apnea in newborns and in infants in the postoperative period (prevention) is 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:

When ingestion in high doses caffeine complicates the concentration of attention and increases the number of operator errors in the performance of works associated with the need for concentration.

Form release / dosage:

Solution for subcutaneous administration, 200 mg / ml.

Packaging:

In ampoules of 1 ml. For 10 ampoules with a knife for opening ampoules and instructions for use in a cardboard box.

10 ampoules in a blister pack. 1 blister pack with a knife for opening ampoules and instructions for use are put in a pack of cardboard.

10 ampoules together with a knife for opening ampoules and instructions for medical use are placed in a pack with a cardboard insert for fixing the ampoules.

In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

Storage conditions:

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 time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N010971

Date of registration:24.06.2010 / 29.04.2015

Expiration Date:Unlimited

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp21.01.2018

Illustrated instructions

Instructions

Sodium caffeine-benzoate (Coffein-benzoate sodium)