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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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Dosage and Administration
Solution for adultsProzerin Subcutaneously injected - 1-2 mg 1-2 times / day.
Children enterProzerin subcutaneously, the dose is calculated at 50 mcg for 1 year of life, but not more than 375 mcg per injection.
Hypersalivation, spastic contraction and increased intestinal motility, nausea, vomiting, flatulence, diarrhea; headache, dizziness, weakness, loss of consciousness, drowsiness; miosis, visual impairment, arrhythmia, brady- or tachycardia, atrioventricular block, blockade, nodal rhythm, nonspecific changes on the electrocardiogram, cardiac arrest, shortness of breath, respiratory depression, up to a stop tongue, convulsions, dysarthria, arthalgia; increased urination; excessive sweating; allergic reactions (facial flushing, rash, itching, anaphylaxis).
Against the background of anticholinergic drugs, in children (with myasthenia) on the background of neomycin, streptomycin, kanamycin and other antibiotics with anti-depolarizing effect, local and some general anesthetics, antiarrhythmic and a number of other drugs that violate cholinergic transmission.
When myasthenia gravis is prescribed in combination with aldosterone antagonists, glycocorticosteroids and anabolic hormones. Atropine, metacin and others. M-anticholinergics weaken M-cholinomimetic effects (pupil constriction, bradycardia, increased gastrointestinal motility, hypersalivation, etc.).
Pregnancy and Lactation
Prozerin contraindicated in pregnancy and lactation.
When a myasthenic (with insufficient therapeutic dose) or cholinergic (due to overdose) crisis occurs during treatment, a thorough differential diagnosis is required due to the similarity of symptoms.
Symptoms: associated with overexcitation of cholinergic receptors (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased peristalsis, diarrhea, increased urination, twitching of the muscles of the tongue and skeletal muscles, the gradual development of general weakness, reduction of blood pressure (A)
Treatment: reduce the dose or stop treatment, if necessary, inject atropine (1 ml of 0.1% solution), metacin and other anticholinergic drugs.
- Brand name: Prozerin
- Active ingredient: Neostigmine
- Annulate lamellae-soleplate nuclei associations in skeletal muscle fibers of rats during chronic high-dose exposure to neostigmine
- ChemInform Abstract: Synthesis of Some New Neostigmine Methyl Sulfates and Related Compounds
- Effects of a low-doses treatment with cuprum on neostigmine digestive action in female mice
- Inhibitions by 6-hydroxydopamine and neostigmine singly or together of gastric carcinogenesis induced by N-methyl-N′-nitro-n-nitrosoguanidine in wistar rats
- Effect of neostigmine on the tissue concentration of antibiotic in streptomycin treated rats
- Influence of physostigmine and neostigmine on the responses of goldfish intestine to acetylcholine
- Synthesis and Preliminary Pharmacology of an Internal Standard for Assay of Neostigmine
- Alkali halide-assisted penetration of neostigmine across excised human skin: A combination of structured water disruption and a donnan-like effect
- A note on the acute toxicity of neostigmine methyl bromide in the rat
- Intracerebral injection of neostigmine and eserine in conscious mice
- Prednisone-neostigmine interactions at cholinergic junctions
- Effect of lumbar epidural administration of neostigmine on lower urinary tract function
- Synergism of the toxicity of physostigmine and neostigmine by lithium or by a reserpine-like agent (Ro4-1284)
- Use of low-dose neostigmine intravenously in the treatment of supraventricular tachycardia: An immediate bradycardic effect
- Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine
- Flow injection determination of neostigmine and galanthamine by immobilised acetylcholinesterase inhibition
- Effect of neostigmine on concentration and extraction fraction of acetylcholine using quantitative microdialysis
- Neostigmine for the Treatment of Neurotoxicity Following Envenomation by the Asiatic Cobra
- Reversed-phase, ion-pair liquid chromatography of quaternary ammonium compounds : Determination of pyridostigmine, neostigmine and edrophonium in biological fluids
- Determination of neostigmine in human plasma and cerebrospinal fluid by high-performance liquid chromatography with ultraviolet detection
- Sepsis attenuates the intensity of the neuromuscular blocking effect of d-tubocurarine and the antagonistic actions of neostigmine and edrophonium accompanying depression of muscle contractility of the diaphragm
- Efficacy of intrathecal neostigmine for the relief of postinguinal herniorrhaphy pain