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Synthetic anticholinesterase agent. Reversibly blocks cholinesterase, which leads to the accumulation and enhancement of the action of acetylcholine on organs and tissues and the restoration of neuromuscular conduction.
Causes a decrease in heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal tract (GIT)) and contributes to the development of hypersalivation, bronchorea, increase the acidity of gastric juice, narrows the pupil, causes a spasm of accommodation, reduces intraocular pressure, increases the tone of the smooth the muscles of the intestine (increases peristalsis and relaxes the sphincters) and the bladder, causes bronchospasm, tones the skeletal muscles.
Prozerin is an antagonist of anti-depolarizing curare-like drugs. At the same time, in high doses, prozerin itself can cause a neuromuscular conduction disorder as a result of acetylcholine accumulation and persistent depolarization in the synapse region. Gives a direct H-cholinomimetic effect.
The action of the drug coincides with the characteristic effects of excitation of cholinergic nerves. Unlike physostigmine, it more stimulates the muscles of the intestines, bladder and uterus, has little effect on the heart and does not cause central effects. When administered in therapeutic doses, skeletal muscle N-cholinergic receptors are largely excited, and neuromuscular transmission is enhanced.
Being a quaternary ammonium base, it does not penetrate through the blood-brain barrier and has no central action. Bioavailability - 1-2%. Communication with plasma proteins - 15-25%. The oral half-life is 52 minutes. Metabolism - in the liver with the formation of inactive metabolites. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% is in an unchanged form and 30% is in the form of metabolites).
Myasthenia gravis, motor impairment after brain injury, paralysis, recovery period after suffering meningitis, polio, encephalitis, weakness of labor activity (rarely), open-angle glaucoma, optic atrophy, neuritis; atony of the digestive tract, atony of the bladder.
Elimination of residual disorders of the neuromuscular transmission of non-depolarizing muscle relaxants.
In pediatric practice: myasthenia gravis, motor disorders after brain injury, paralysis, recovery period after suffering meningitis, polio, encephalitis, optic nerve atrophy, neuritis; atony of the digestive tract, atony of the bladder. Elimination of residual disorders of the neuromuscular transmission of non-depolarizing muscle relaxants.
1 ml of solution contains:
Active substance:neostigmine methyl sulfate - 500 mcg
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