Universal reference book for medicines
Product name: COFFEIN (COFFEIN)

Active substance: caffeine

Type: Psychostimulant and analeptic

Manufacturer: BORISOVSKIY ZAVOD MEDPREPARATOV (Republic of Belarus)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Psychostimulating and analeptic agent, methylxanthine derivative.
Competitively blocks central and peripheral A1 and A2 adenosine receptors. It inhibits the activity of PDE 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 applied only in high doses). Stimulates the centers of the medulla oblongata (respiratory and vasomotor), as well as the center of n.vagus, exerts 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.
Achieves and deepens the breath.
Usually has a positive foreign, chrono-, batmo- and dromotropic effect (since the effect on SSS consists of direct stimulating action on the myocardium and simultaneous stimulating effect on n.vagus centers, 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 rises (causes narrowing of the cerebral vessels, which is accompanied by a decrease in cerebral blood flow and oxygen pressure in the brain).
BP changes under the influence of vascular and cardiac mechanisms of caffeine influence: at normal initial AD, 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.

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 the 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.

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

Enter the SC or taken internally.
Adults-100-200 mg 2-3 times / day; children - 25-100 mg 2-3 times / day.
From the side of the central nervous system: sleep disturbance, agitation, anxiety;
with prolonged use is possible.
From the cardiovascular system: tachycardia, increased blood pressure, arrhythmia.

From the digestive system: nausea, vomiting.

Arterial hypertension, organic diseases of the cardiovascular system (including pronounced atherosclerosis), glaucoma, increased excitability, sleep disorders, senile age.

Contraindicated in senile age.

Possible application in the form of mono- or as part of a combination therapy.

With simultaneous use, the effect of hypnotics and anesthetics is reduced.

With simultaneous use, it is possible to intensify the action of analgesics-antipyretics, salicylamide, naproxen.

With the simultaneous use of estrogens (hormonal contraceptives, agents for HRT), the intensity and duration of action of caffeine can be increased by inhibiting the isoenzyme CYP1A2 by estrogen.

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

With simultaneous use, mexiletine reduces caffeine clearance and increases its plasma concentration, apparently due to mexiletine inhibition of caffeine metabolism in the liver.

Metoxalen reduces the excretion of caffeine from the body with the possible enhancement of its effect and the development of toxic effects.

Due to the induction of microsomal enzymes of the liver under the influence of phenytoin, it simultaneously accelerates the metabolism and elimination of caffeine.

Fluconazole and terbinafine cause a moderate increase in the concentration of caffeine in the blood plasma, ketoconazole - less pronounced.

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

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