Caffeine benzoate solution for intravenous administration. Instructions for use and dosage. Instructions for use of Caffeine: method and dosage

Name:

Caffeine (Cofleinum)

Pharmacological
action:

Psychostimulant and analeptic agent, a methylxanthine derivative.
Competitively blocks central and peripheral A1 and A2 adenosine receptors.
Inhibits the activity of PDE in the central nervous system, heart, smooth muscle organs, skeletal muscles ah, adipose tissue, promotes the accumulation of cAMP and cGMP in them ( this effect observed when used only in high doses). Stimulates the centers medulla oblongata(respiratory and vasomotor), as well as the n.vagus center, has a direct stimulating effect on the cerebral cortex.

In high doses it facilitates interneuronal conduction in spinal cord , enhancing spinal reflexes.
Increases mental and physical performance, stimulates mental activity, motor activity, shortens reaction time, temporarily reduces fatigue and drowsiness.

In small doses, the stimulation effect predominates, and in large cases - the effect of depression of the nervous system.
Speeds up and deepens breathing. Usually it has a positive ino-, chrono-, bathmo- and dromotropic effect (since the effect on the cardiovascular system consists of a direct stimulating effect on the myocardium and a simultaneous stimulating effect on the n.vagus centers, the resulting effect depends on the predominance of one or another action).
Stimulates the vasomotor center and has a direct relaxing effect on vascular wall, which leads to dilation of the blood vessels of the heart, skeletal muscles and kidneys, while tone cerebral arteries increases (causes cerebral vasoconstriction, 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's influence: with normal initial blood pressure, caffeine does not change or slightly increases it, with arterial hypotension normalizes it.

Has an antispasmodic effect on smooth muscles (including a bronchodilator effect), on striated muscles - stimulating.
Increases the secretory activity of the stomach.
Has a moderate diuretic effect, which is due to a decrease in the reabsorption of sodium and water ions in the proximal and distal renal tubules, as well as dilation of the renal vessels and increased filtration in the renal glomeruli.
Reduces platelet aggregation and histamine release from mast cells.
Increases basal metabolism: increases glycogenolysis, increases lipolysis.

Indications for
application:

Diseases accompanied by depression of the central nervous system, cardiovascular and respiratory systems(including poisoning with opioid analgesics, infectious diseases);
- spasms of cerebral vessels;
- decreased mental and physical performance;
- drowsiness.

Mode of application:

Administered subcutaneously or taken orally.
For adults- 100-200 mg 2-3 times/day; children- 25-100 mg 2-3 times/day.

Side effects:

From the side of the central nervous system: sleep disturbance, agitation, anxiety; With prolonged use, addiction is possible.
From the outside of cardio-vascular system : tachycardia, increased blood pressure, arrhythmias.
From the outside digestive system : nausea, vomiting.

Contraindications:

Arterial hypertension;
- organic diseases cardiovascular system (including severe atherosclerosis);
- glaucoma;
- increased excitability;
- sleep disorders;
- old age;
- children under 12 years old.

Interaction
other medicinal
by other means:

At simultaneous use effect decreases sleeping pills and drugs for anesthesia.
With simultaneous use, it is possible to enhance the effect of analgesics-antipyretics, salicylamide, naproxen.
With simultaneous use of estrogens ( hormonal contraceptives, drugs for HRT) it is possible to increase the intensity and duration of action of caffeine due to the inhibition of the CYP1A2 isoenzyme by estrogens.

With simultaneous use of adenosine caffeine reduces the increased heart rate and blood pressure changes caused by adenosine infusion; reduces vasodilation caused by the action of adenosine.
With simultaneous use, it is possible to increase bioavailability, absorption rate and plasma concentration acetylsalicylic acid.

With simultaneous use of mexiletine reduces the clearance of caffeine and increases its plasma concentrations, apparently due to mexiletine inhibition of caffeine metabolism in the liver.
Methoxsalen reduces caffeine excretion from the body with possible strengthening its effect and the development of toxic effects.

Due to the induction of microsomal liver enzymes under the influence of phenytoin, its simultaneous use accelerates the metabolism and excretion of caffeine.
Fluconazole and terbinafine cause a moderate increase in plasma caffeine concentrations, ketoconazole – less pronounced.

The most pronounced increase in AUC and decrease in clearance are observed with simultaneous use of caffeine with enoxacin, ciprofloxacin, pipemidic acid; less pronounced changes– with pefloxacin, norfloxacin, fleroxacin.
When used simultaneously, caffeine accelerates the absorption of ergotamine.

Pregnancy:

Carefully the drug should be used during pregnancy and lactation
Excessive consumption during pregnancy may lead to spontaneous abortions, slowdown intrauterine development fetus, arrhythmias in the fetus; There may be disturbances in skeletal development when using large doses and a slowdown in skeletal development when using lower doses.
Penetrates breast milk V small quantity, but accumulates in infants and can cause hyperactivity and insomnia.

Overdose:

Symptoms: abdominal pain, agitation, anxiety, mental and motor agitation, confusion, delirium (dissociative), dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensitivity, tremors or muscle twitching; nausea and vomiting, sometimes with blood; tinnitus, epileptic seizures(in case of acute overdose - tonic-clonic convulsions).
Caffeine in doses of more than 300 mg per day (including against the background of coffee abuse - more than 4 cups of natural coffee, 150 ml each) can cause anxiety, headache, tremor, confusion, extrasystole.

Treatment: gastric lavage, use of laxatives, activated carbon.
If the patient hemorrhagic gastritis, he is administered antacid medications and the stomach is washed with a 0.9% sodium chloride solution, and artificial ventilation is maintained.
If convulsions occur during an overdose, diazepam, phenytoin, phenobarbital are administered intravenously, and water-electrolyte balance is maintained.

Release form:

Caffeine solution for subcutaneous administration 100 mg/1 ml, 200 mg/2 ml, 400 mg/2 ml in ampoules of 10 pcs.
Tablets 100 mg 6 or 10 tablets in a blister pack or 10 tablets in a blister pack. 1 or 2 blister packs along with instructions for use are placed in a cardboard box.

Storage conditions:

At room temperature.
Keep out of the reach of children.

1 ampoule of Caffeine solution for subcutaneous administration contains - caffeine sodium benzoate 200 mg.

1 ml of caffeine-sodium benzoate solution for subconjunctival and subconjunctival administration contains - caffeine sodium benzoate 200 mg.

1 ml of caffeine-sodium benzoate solution for subcutaneous administration contains -caffeine sodium benzoate 200 mg.

1 tabletCaffeine sodium benzoate contains:
- active substance: caffeine sodium benzoate - 100 mg;
- Excipients: potato starch - 15.77 mg, calcium stearate - 0.23 mg.

In general, caffeine is a psychostimulant, and this can be confirmed by everyone. own experience- of course, it does not act as strongly as the psychostimulant amphetamine, acting on other targets.

There was an incident at our university with students who, before an exam in pharmacology, decided to study and not sleep, using caffeine in different forms. They started with instant freeze-dried coffee, switched to powdered coffee for brewing when instant coffee stopped working, and then switched to grain coffee. When these doses of caffeine stopped helping, they switched to caffeine tablets. Conda caffeine in tablets stopped helping, they switched from the above range of oral forms of caffeine to parenteral ones, dug up ampoules of caffeine somewhere and administered them intravenously.

Yes, they managed to read all the textbooks they wanted for the exam. But when they came to the exam, they looked so broken that at first the examiners thought that they were so worried that they would soon faint: their faces were covered cold sweat, his hands were shaking as if he had Parkinsonism, his eyes were cloudy, and his gaze was, as they say, “a thousand miles away,” like that of soldiers after Vietnam experiencing post-traumatic stress. stress disorder. But when the teachers found out the real reason, these students... were given a "fail" without a survey. Why? Because they did it non-pharmacologically.

Psychoactive psychostimulants, which include caffeine and amphetamine, increase energy but reduce concentration. They are suitable for performing creative, varied work, but are not suitable for monotonous routine activities such as reading a textbook. Moreover: even if the shutter speed for continuation of work is found, sleepless nights deplete the reserves of neurotransmitters, which leads not only to motor disorders, but also to the loss of memory functions from memorization to recall.

What does this teach us? Firstly, the toxic and lethal doses of caffeine are quite large, given the fact that its concentrations in medicines are very small. One tablet or one ampoule contains on average about 100 mg of caffeine, while the lethal dose is 200 mg per kg of body weight, that is, the average person needs more than 50 such tablets or ampoules. Secondly, sleeping before an exam will give you more than staying up all night and re-reading textbooks several times.

And caffeine is administered intravenously as a stimulant of breathing when it stops, because it is not only a psychoactive psychostimulant, but also respiratory analeptic, activating the respiratory center of the medulla oblongata. If you administer it off-label, the usual effect of caffeine will appear, but it will be more pronounced and occur faster. Why? This way, its bioavailability is higher - so it travels faster through the bloodstream to its targets in the nervous system, without wasting time on absorption from the gastrointestinal tract.

How does caffeine actually work? In short and as clearly as possible, it prevents the action of the “fatigue molecule” (which is a derivative of ATP - our internal energy carrier; something like a used battery), thus delaying the onset of fatigue - it is precisely because of the delaying effect that the fatigue that occurs later is increased effect because it accumulates imperceptibly while caffeine circulates through us.

Do it pharmacologically.

Did you dig it up somewhere? Yes, in any pharmacy! The article is fictitious, because... The coffee itself, even the powdered one, delivers better and longer lasting results than ampoules or tablet dispensers. The only way they could come in feeling overwhelmed was if they didn't take caffeine, otherwise the caffeine would block the uptake of adenosine and they would simply not feel tired in any way. It’s just like schoolchildren telling each other fairy tales in the fifth grade and here...

Caffeine sodium benzoate: instructions for use

Compound

Description

Indications for use

Contraindications

• hypersensitivity (including to other xanthines);
• anxiety disorders (agoraphobia, panic disorders);
• organic diseases of the cardiovascular system (incl. acute heart attack myocardium, atherosclerosis);
• paroxysmal tachycardia, frequent ventricular extrasystole;
• arterial hypertension;
• sleep disorders.

Carefully

Glaucoma, increased excitability, elderly age, epilepsy and tendency to seizures, pregnancy, lactation period.

Directions for use and doses

Adults are administered subcutaneously 200 mg (1 ml of solution), children 25 - 100 mg (0.1 - 0.5 ml of solution) 2 - 3 times a day.

Intramuscular administration of a caffeine-sodium benzoate solution is not recommended due to the possibility of developing painful spastic muscle contractions at the injection site.

Side effect

From the nervous system: agitation, anxiety, tremor, restlessness, headache, dizziness, epileptic seizures, increased reflexes, tachypnea, insomnia.

From the cardiovascular system: palpitations, tachycardia, arrhythmias, increased blood pressure.

From the digestive side systems: nausea, vomiting, exacerbation of peptic ulcer.

Others: nasal congestion, with prolonged use - addiction, drug dependence.

Overdose

Symptoms of intoxication occur when caffeine is consumed in a dose of more than 300 mg/day. Anxiety, restlessness, tremor, headache, confusion, and tachyarrhythmia may occur. In newborns with a blood concentration of more than 50 mcg/ml of caffeine, in addition to the above-described picture, a pathological increase in reflexes, the appearance of convulsive syndrome.

There is no specific antidote. Assistance measures include discontinuation of the drug, supportive and symptomatic therapy aimed at eliminating the disorders that have arisen, monitoring blood pressure levels and stopping seizures with the administration of benzodiazepine tranquilizers (diazepam).

Interaction with other drugs

Caffeine is an adenosine antagonist.

At joint use caffeine and barbiturates, primidone, anticonvulsants (hydantoin derivatives, especially phenytoin) may increase metabolism and increase caffeine clearance.

With the combined use of caffeine and cimetidine, oral contraceptive drugs, disulfiram, ciprofloxacin, norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increasing its concentration in the blood).

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

MAO inhibitors, 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 preparations in the gastrointestinal tract.

Reduces the effect of narcotic and sleeping pills medicines.

Increases the excretion of lithium drugs in urine.

Accelerates absorption and enhances the effect of cardiac glycosides, increasing their toxicity.

Concomitant use of caffeine with beta-blockers may result in mutual suppression therapeutic effects; with adrenergic bronchodilators - to additional stimulation of the central nervous system and other additive toxic effects.

When used simultaneously, it increases the bioavailability of acetylsalicylic acid, paracetamol and ergotamine, thereby enhancing their effect.

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

Antifungal drugs (ketoconazole, fluconazole) slow down the metabolism of caffeine and increase its concentration in plasma.

Features of application

Impact on the central nervous system depends on the type of nervous system and can manifest itself as both excitation and inhibition of higher nervous activity.

Due to the fact that the effect of caffeine on arterial pressure consists of vascular and cardiac components, as a result, both the effect of stimulation of the heart and inhibition (weak) of its activity can develop.

Pregnancy and lactation. Given the slow elimination of caffeine from the fetus, its use during pregnancy is possible only after assessing the benefit/risk ratio for the mother and fetus. Excessive consumption of caffeine during pregnancy can lead to spontaneous abortions, retardation of intrauterine development of the fetus, and arrhythmias in the fetus; There may be disturbances in skeletal development when using large doses and a slowdown in skeletal development when using lower doses.

Caffeine and its metabolites pass into mother's milk in small quantities, but accumulate in infants and can cause hyperactivity and insomnia. If it is necessary to use it during lactation, the benefit/risk ratio for the mother and child should be assessed.

Use in neonatology. For the treatment and prevention of apnea in newborns and infants in postoperative period Caffeine or caffeine citrate is used, but not caffeine sodium benzoate.

Use in persons with peptic ulcer stomach and duodenum in the anamnesis. Caution is required when prescribing caffeine to these groups of patients due to increased risk exacerbation of their peptic ulcer.

Impact on the ability to perform work that requires concentration. When used in high doses, caffeine makes it difficult to concentrate and increases the number of operator errors when performing work that requires concentration.

Release form

Storage conditions

Best before date

Conditions for dispensing from pharmacies

Caffeine-sodium benzoate analogues, synonyms and group drugs

Self-medication can be harmful to your health.
You should consult your doctor and read the instructions before use.

Trade name of the drug: Caffeine sodium benzoate

International nonproprietary name:

Dosage form:

Compound

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

Description

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:

ATX code:

Pharmacodynamics

It has a psychostimulating and analeptic effect. It has a stimulating 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 blood pressure pressure during hypotension, dilates the bronchi, biliary tract, blood vessels skeletal muscles, reduces platelet aggregation, has moderate diuretic effect, stimulates secretion gastric juice, increases basal metabolism and enhances glycogenolysis, causing hyperglycemia. Multiple pharmacological effects the drug is caused by blockade of central and peripheral adenosine receptors. Inhibits phosphodiesterase, which leads to intracellular accumulation of cyclic adenosine monophosphate, under the influence of which glycogenolysis processes are enhanced, metabolic processes in organs and tissues are stimulated, including muscle tissue and the central nervous system.

When administered subconjunctivally, 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% is metabolized 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) with the formation of 5 metabolites. Caffeine and its metabolites are excreted by the kidneys (10% unchanged).

Indications for use

• Decreased mental and physical performance, muscle weakness, drowsiness, migraine, moderate arterial hypotension, respiratory depression (including mild poisoning with opioid analgesics and hypnotics, carbon monoxide, asphyxia of newborns, restoration of the required level of pulmonary ventilation after the use of general anesthesia).
• Hypotension eyeball(after abdominal eye surgeries, 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, old age, paroxysmal tachycardia, frequent ventricular extrasystole, epilepsy and a tendency to seizures. Pregnancy and lactation period.

Carefully: glaucoma, increased excitability, old age.

Directions for use and doses

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, daily. The number of injections depends on intraocular pressure and depth of the anterior chamber.

Side effect

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

From the cardiovascular system: tachycardia, cardiac arrhythmia, increased blood pressure.

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

Others: nasal congestion.

With long-term use, mild addiction is possible (a decrease in effect is associated with the formation of new adenosine receptors in brain cells), drug dependence.

Overdose

Symptoms: increased severity side effects. In newborns (including premature infants) the following are possible: anxiety, tachypnea, tachycardia, tremor, increased Moro reflex, with more high concentrations- convulsions.

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

Interaction with other drugs

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.

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

When used with caffeinated beverages and other drugs that stimulate the central nervous system, excessive stimulation of the central nervous system is possible. Caffeine is an adenosine antagonist - large doses of adenosine may be required.

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

Monoamine oxidase inhibitors (MAOIs), 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 effect of narcotic and sleeping pills. Increases the excretion of lithium preparations (Li +) in the urine.

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

Concomitant use of caffeine with beta-blockers may lead to mutual suppression of therapeutic effects; with adrenergic bronchodilators - to additional stimulation of the central nervous system and other additive toxic effects.

Caffeine may 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 sudden cessation of use may lead to increased inhibition of the central nervous system (drowsiness, depression). The effect on the central nervous system can be manifested by both excitation and inhibition of higher nervous activity.

Release form

Solution for subcutaneous and subconjunctival administration 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 pack made of polyvinyl chloride film, 1 or 2 blister packs with instructions for use and a knife for opening ampoules or with an ampoule scarifier in a cardboard pack. When packaging ampoules with a break ring or break point, a knife for opening ampoules or an ampoule scarifier is not included.

Storage conditions

List B.

At temperatures from +15°C to +25°C Store out of the reach of children.

Best before date

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

Conditions for dispensing from pharmacies:

The manufacturer accepts claims from buyers:

OJSC "Novosibkhimpharm", 630028, Russia, Novosibirsk, st. Dekabristov, 275

Caffeine is a psychostimulant drug.

pharmachologic effect

Caffeine sodium benzoate is a drug that reduces drowsiness, fatigue, and stimulates a person’s mental activity, physical and mental performance.

Caffeine tends to have a stimulating effect on the vasomotor, respiratory centers, increase cardiac activity, dilate blood vessels of the muscles, kidneys, heart, brain, constrict the blood vessels of organs located in the abdominal cavity.

Caffeine used by older people has a pronounced effect on their sleep: it slows down its onset, reduces the overall duration, and increases the frequency of awakenings.

In premature babies, the drug eliminates periodic breathing, reduces the partial pressure of carbon dioxide, increases the volume of ventilation, without affecting the heart rate.

Release form

Caffeine is produced in tablets and ampoules (solutions for subconjunctival, subcutaneous administration).

Indications for use of Caffeine

Caffeine benzoate is used to treat decreased physical, mental performance, for headaches vascular nature, with drowsiness, moderate arterial hypotension, respiratory depression (including asphyxia of newborns, poisoning with sleeping pills, opioid analgesics, carbon monoxide), enuresis. An effective remedy for restoring a sufficient level of pulmonary ventilation after anesthesia.

In ophthalmology, caffeine is used to treat decreased tone after eye surgery and retinal detachment.

In cosmetology, a mixture of Caffeine and Capsicam is used for anti-cellulite wraps.

Mode of application

Adults take caffeine tablets 50-100 mg orally two or three times a day. Children are given 30-75 mg two or three times a day. It is not recommended to take the drug before bedtime.

Caffeine in ampoules is administered subcutaneously, 1 ml of solution. The permissible single dose is 0.4 g, the daily dose is 1 g. Children are injected with 0.25-1 ml of 10% caffeine solution in ampoules.

In ophthalmology, it is practiced to administer a 10% solution in the form of injections under the conjunctiva - 0.3 ml once a day. The frequency of injections depends on the depth of the anterior ocular chamber and intraocular pressure.

Anti-cellulite wrap “Caffeine Capsicum” is carried out as follows: prepare a mixture of four ampoules of Caffeine, Capsicam ointment (approximately 2cm), baby cream (about 4cm). Apply it to “problem” areas, cover with cling film and leave the application on for three hours. One hour before the procedure, during it and another two hours after it, it is not recommended to eat or drink. The course consists of 10 procedures.

Side effects

Caffeine can cause anxiety, restlessness, headaches, agitation, tremors, epileptic seizures, dizziness, tachypnea, insomnia, fatigue, muscle tension, arrhythmia, tachycardia, palpitations, increased blood pressure, exacerbation of ulcers, nasal congestion. Long-term use Caffeine benzoate can be addictive and addictive.

Anti-cellulite wrap using Caffeine, Capsicam causes a hot burning sensation on the skin throughout the entire procedure. The wrap does not lead to negative changes on the skin (except in cases of individual intolerance to the products used).

Contraindications to the use of Caffeine

You cannot take Caffeine in tablets or inject Caffeine in ampoules if: anxiety disorders, diseases of cardio-vascular system organic nature, hypersensitivity, paroxysmal tachycardia, frequent ventricular extrasystole, arterial hypertension, sleep disorders.

The drug should not be prescribed to children under 12 years of age.

The drug is prescribed with caution to elderly patients, patients with glaucoma, epilepsy, patients with a tendency to seizures, in old age, during breastfeeding, and pregnancy.

During treatment, it should be taken into account that caffeine benzoate enhances the effect of narcotic drugs, sleeping pills, paracetamol, aspirin, other non-narcotic analgesics.

Sincerely,