Description
Caffeine sodium benzoate Pharmacodynamics
Caffeine is a methylxanthine which has psychostimulant and analeptic effects. It competitively blocks central and peripheral A1 and A2 adenosine receptors. Inhibits phosphodiesterase activity in the central nervous system, heart, smooth and transverse striated muscle tissue, adipose tissue, promotes the accumulation of cyclic adenosine monophosphate and cyclic guanosine monophosphate in them (this effect is observed with high doses of caffeine only). Stimulates the medulla oblongata centers (respiratory and vasomotor), as well as the vagus nerve center, has a direct excitatory effect on the cerebral cortex. At high doses it facilitates inter-neuronal conduction in the spinal cord, increasing reflexes.
Increases mental and physical performance, stimulates mental activity, motor activity, shortens reaction time, temporarily reduces fatigue and sleepiness. In low doses the stimulating effect predominates, while in high doses it has a depressing effect on the nervous system.
It makes breathing faster and deeper, usually has positive in-, chrono-, batmo- and dromotropic effects (since the effect on the cardiovascular system consists of a direct stimulating effect on the myocardium and a simultaneous excitatory effect on the vagus nerve center, the resulting effect depends on the predominance of one or the other action).
It stimulates the vasomotor center and has a direct relaxing effect on the vascular wall, which leads to dilation of heart, skeletal muscle and kidney vessels, while the tone of cerebral arteries increases (causes narrowing of cerebral vessels, which is accompanied by a decrease in cerebral blood flow). Blood pressure changes under the influence of vascular and cardiac mechanisms of caffeine influence: under normal baseline blood pressure caffeine does not change or slightly increases it, under arterial hypotension it increases.
It has antispasmodic effect on smooth muscles (including bronchodilator effect), stimulating effect on transverse striated muscles. Increases secretory activity of the stomach and diuresis (decreases sodium and water reabsorption in the proximal and distal renal tubules, as well as renal vasodilation and increased filtration in the renal glomerules).
Reduces platelet aggregation and histamine release from mast cells. Increases basic metabolism: increases glycogenolysis, increases lipolysis.
Indications
Decreased mental and physical performance, drowsiness, vascular headaches (including migraine), moderate arterial hypotension.
Contraindications .
Hypersensitivity to the components of the drug (including other xanthines), anxiety disorders (agoraphobia, panic disorder), organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis), paroxysmal tachycardia, ventricular extrasystole, arterial hypertension, sleep disorders, children under 12 years of age.
Caution
Glaucoma, hyperexcitability, advanced age, epilepsy and proneness to seizures.
Usage during pregnancy and lactation
Usage is possible only after consultation with the physician, if the expected benefits to the mother exceed the potential risk to the fetus and child.
Dosage and administration
- Appoint orally, regardless of meals. Do not take before bedtime.
- In reducing mental and physical performance, sleepiness – adults and children over 12 years – 50 – 100 mg 2-3 times a day. The course of treatment from a few weeks to several months, depending on the patient’s condition.
- In headache of vascular genesis (including migraine) for adults and children over 12 years old – 50-100 mg 2-3 times a day for a few days.
- In moderate arterial hypotension, adults and children over 12 years of age take 50-100 mg 2-3 times a day. The course of treatment is several weeks.
- The highest single dose for adults is 300 mg, the highest daily dose for adults is 1000 mg.
- The highest single dose for children from 12 years of age is 150 mg, the highest daily dose for children is 500 mg.
