Included in the formulation
АТХ:S.01.E.B Parasympathomimetics
S.01.E.B.06 Neostigmine
Pharmacodynamics:Carbamic acid ester binds to the anionic and esterase centers of acetylcholinesterase, hydrolyses in such a way that it appears to be a covalently bound carbamyl group with acetylcholinesterase. The bond is stronger than with the acetyl group, so the restoration of cholinesterase activity slows down from 30 minutes to several hours.
Strengthens and lengthens the action of acetylcholine, mostly in peripheral cholinergic synapses. Has effects associated with parasympathetic nervous excitation system. Due to the contraction of the circular muscle, the iris causes miosis, which entails opening the anterior chamber of the eye and reducing the intraocular pressure due to the outflow of intraocular fluid through the fountain spaces into the helmet canal. By reducing the ciliary muscle causes a spasm of accommodation. It causes a slowing of atrioventricular conduction and bradycardia, increases the bronchial tone, gastrointestinal motility,contractile activity of the bladder and uterus, stimulates the secretion of exocrine glands.
It alleviates neuromuscular transmission.
Pharmacokinetics:After oral administration, an empty stomach is absorbed up to 1-2% in the gastrointestinal tract. When intramuscular introduction is rapidly absorbed and output. The maximum concentration in the blood plasma is reached after 30 minutes. The connection with plasma proteins is up to 25%. Poorly penetrates the blood-brain barrier.
The therapeutic effect develops in 20-30 minutes after administration. Metabolism in the liver.
Half-life is 40-60 minutes with oral administration; 50-90 min - with parenteral administration.
Elimination of the kidneys in the form of metabolites, about 50% unchanged.
Indications:It is used to treat myasthenia gravis, postoperative intestinal atony, rarely - with weakness of labor and glaucoma. It is a means of choice for overdose of muscle relaxants of peripheral action (curare-like remedies).
VI.G00-G09.G04 Encephalitis, myelitis and encephalomyelitis
VI.G70-G73.G70.2 Congenital or acquired myasthenia gravis
VII.H46-H48.H47.2 Atrophy of the optic nerve
VII.H40-H42.H40.1 Primary open angle glaucoma
XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified
XV.O60-O75.O62.2 Other types of weakness in labor
Contraindications:Epilepsy, bradycardia, bronchial asthma, stenocardia, severe atherosclerosis, peptic ulcer of the stomach and duodenum.
Individual intolerance.
Carefully:The disease of Adisson.
Pregnancy and lactation:Recommendations for FDA - Category C. It is used during pregnancy according to vital indications. Contraindicated during lactation.
Dosing and Administration:Children
Newborns: 1-5 mg every 4 hours 30 minutes before meals;
1 month - 6 years: 7.5 mg as required several times a day, total daily dose: 15-90 mg;
12-18 years: 15-30 mg per dose several times a day, total dose not more than 300 mg.
Adults
Inside for 10-15 mg 2-3 times / day; subcutaneously - 1-2 mg 1-2 times / day.
The highest daily dose: 15 mg orally, 2 mg subcutaneously.
The highest single dose: 50 mg orally, 6 mg subcutaneously.
Side effects:Central and peripheral nervous system: dizziness, headache, drowsiness, miosis, convulsions, dysarthria.
Respiratory system: shortness of breath, respiratory depression, increased bronchial tone, increased secretion of bronchial glands.
The cardiovascular system: arrhythmia, arterial hypotension.
Digestive system: nausea, vomiting, hypersalivation, flatulence, diarrhea, increased peristalsis.
Musculoskeletal system: arthralgia.
Allergic reactions.
Overdose:Symtomas: holenergichesky crisis (miosis, spasm of accommodation, lacrimation, hyperhidrosis, involuntary defecation and urination, hypotension, arrhythmia, muscle spasms, ataxia, coma).
Treatment: atropine 2-4 mg intravenously, then 2 mg every 5-10 minutes. until the elimination of muscarinic effects. Allowable daily dose of atropine to 200 mg.
Interaction:Simultaneous use with β-adrenoblockers increases the risk of arterial hypotension. Weaken the anti-myasthenic action with simultaneous use with aminoglycosides, inhalation anesthetics, local anesthetics, propafenone, verapamil, quinine, chloroquine, polymyxins A and B, linkomycin.
Special instructions:When parenteral administration of large doses, a preliminary administration of atropine is recommended.