Active substanceNeostigmine methyl sulfateNeostigmine methyl sulfate
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  • Proserin
    solution w / m in / in PC 
  • Proserin
    pills inwards 
    DALHIMFARM, OJSC     Russia
  • Proserin
    solution in / in PC 
  • Proserin-Darnitsa
    solution in / in PC 
  • Dosage form: & nbspsolution for intravenous and subcutaneous administration
    Composition:1 liter of solution contains: active substance: Proserine-0.5 g; adjuvant: water for. injections - up to 1 liter.
    Description:clear, colorless liquid.
    Pharmacotherapeutic group:cholinesterase inhibitor
    ATX: & nbsp

    S.01.E.B   Parasympathomimetics

    S.01.E.B.06   Neostigmine

    Pharmacodynamics:

    Synthetic anticholinesterase agent. Reversibly blocks cholinesterase, which leads to the accumulation and intensification of the action of acetylcholine on organs and tissues and the restoration of neuromuscular conduction. It causes a decrease in the heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal tract) and promotes the development of hypersalivation, bronchorrhoea, increased acidity of gastric juice, causes a narrowing of the pupil, a spasm of accommodation, reduces intraocular pressure (in patients with closed-angle glaucoma) , strengthens the tone of the smooth muscles of the intestine and bladder, causes spasm of the bronchi, increases the tone of the skeletal muscles. After intravenous administration, the maximum effect is observed after 5-15 minutes.The duration of the effect is 2.5-4 hours.

    Pharmacokinetics:

    Being a quaternary ammonium base, poorly penetrates the blood-brain barrier and does not have a central effect. Connection with blood plasma proteins - 15-25%. Half-life with intravenous administration - 53 minutes. Metabolized in the liver by microsomal enzymes with the formation of inactive metabolites. Excretion: 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% in unchanged form and 30% in the form of metabolites).

    Indications:

    Myasthenia gravis; motor disorders after brain injuries; paralysis; the recovery period after the meningitis, poliomyelitis, encephalitis; atrophy of the optic nerve; neuritis; prevention and treatment of atony of the intestine and bladder; stimulation of labor.

    As an antidote after anesthesia with antidepolarizing and depolarizing (if they begin to act as an antidepolarizing "double block") muscle relaxants with muscle weakness and respiratory depression.

    Contraindications:

    Hypersensitivity, epilepsy, hyperkinesia, vagotomy, ischemic heart disease, bradycardia, arrhythmias, angina pectoris, bronchial asthma,pronounced atherosclerosis, hyperthyroidism, gastric and duodenal ulcer, peritonitis, mechanical obstruction of the gastrointestinal tract and urinary tract, prostatic hyperplasia, intoxication in severely impaired children, pregnancy, lactation.

    Dosing and Administration:

    Subcutaneously and intravenously.

    Adults are usually prescribed under the skin for 0.5 mg (1 ml of solution) 1-2 times a day.

    In the treatment of myasthenia gravis, prozerin can be administered in combination with aldosterone antagonists. Myasthenia gravis is treated for a long time. With the development of the myasthenic crisis, adults are given intravenously (with 0.9% sodium chloride solution) 0.5-1 ml of the solution, then under the skin in usual doses at small intervals. To enhance the action of Proserin sometimes injected under the skin in addition ephedrine - 1 ml of 5% solution. In other diseases, the duration of treatment is 25-30 days, if necessary, the course of treatment is repeated after 3-4 weeks break.

    To stimulate childbirth, 0.5 mg (1 ml of solution) can be administered 1-2 times at intervals of 1 hour, simultaneously with the first injection, 1 mg (1 ml of 0.1% solution) of atropine is administered once under the skin.

    To stop the effect of muscle relaxants, intravenously, atropine sulfate is administered at a dose of 0.5-0.7 mg (0.5-0.7 ml of 0.1% solution), expect a rapid pulse and after 1.5-2 minutes, intravenously 1, 5 mg (3 ml of solution) of Proserin. If the effect of this dose is insufficient, re-inject the same dose (with the appearance of bradycardia, an additional injection of atropine). In total, you can enter 5-6 mg (10-12 ml of solution) of Proserin for 20-30 minutes. During the procedure, adequate ventilation is provided.

    Children under the skin appoint 0.05 mg (0.1 ml of solution) for 1 year of life, but not more than 0.75 ml of 0.05% solution per injection. Usually, the children of Prozerin are prescribed once a day, however, if necessary, the daily dose of the drug can be divided into 2-3 doses. Side effect

    Hypersalivation; spastic reduction and strengthening of intestinal motility; nausea; vomiting; flatulence; diarrhea; headache; dizziness; weakness; loss of consciousness; drowsiness; miosis; visual impairment; arrhythmias; brady or tachycardia; atrioventricular block; nodal rhythm; nonspecific changes on the electrocardiogram; heart failure; lowering blood pressure; dyspnea; respiratory depression until the stop; bronchospasm; tremor; spasms and twitching of the skeletal musculature,including the fasciculation of the muscles of the tongue, convulsions; dysarthria; arthralgia; increased frequency of urination; profuse sweating; allergic reactions (redness of the face, rash, itching, anaphylaxis).

    For the removal of side effects reduce the dose or stop the use of the drug, if necessary, introduce atropine (1 ml of a 0.1% solution), metocinium iodide or other anticholinergic drugs.

    Overdose:

    In case of an overdose, a cholinergic crisis occurs (bradycardia, hypersalivation, miosis, bronchospasm, nausea, abdominal pain, increased peristalsis of the gastrointestinal tract, diarrhea, frequent urination, heavy sweat, difficulty breathing, cyanosis, fibrillation of skeletal muscles and tongue, general weakness, decrease in blood pressure). Treatment: the drug should be discontinued and immediately enter atropine sulfate (1 ml 0.1% solution under the skin) or other anticholinergics. In cases of severe poisoning with Prozerin, atropine sulfate is administered at intervals of 10 minutes up to 3 times (before occurrence dry mouth). When there is a seizure, amobarbital is prescribed - intramuscularly
    (5-10 ml of 10% solution) or hexobarbital (10 ml of 10% solution), or chloral hydrate rectally.

    Interaction:

    Proserin and depolarizing muscle relaxants (suxamethonium iodide and others) are pharmacologically incompatible, since in the direct interaction the effect of suxamethonium iodide is enhanced. However, in the case of depolarizing muscle relaxants in large doses, after depolarizing action, an antidepolarizing effect ("double block") develops, therefore it is expedient to prescribe Proserin.

    M-holinoblokatory (atropine, gomatropine hydrobromide, platyphylline and others), ganglion blockers (pahikarpine hydroiodide), quinidine, novocainamide, local anesthetics are pharmacological antagonists of Prozerin.

    There is relative antagonism between tricyclic antidepressants, antiepileptic and antiparkinsonian agents. Cyanocobalamin in large doses weakens the action of Proserin.

    Reduces the activity of pyridoxine.

    Proserin combines well with adenosine triphosphate and calcium gluconate in muscular dystrophies; with thiamine - with neuritis; with niketamidom - with cardiovascular disorders.

    Anticholinesterase substances in combination with strychnine significantly increase the tone of the vagus nerve; with laxatives - strengthen themact; with antiarrhythmic drugs (padrenoblockers) are synergists (aggravation of bradycardia).

    Ephedrine enhances the action of Proserin, so when myasthenic crises they are administered together.

    With myasthenia it is advisable to combine with aldosterone antagonists.

    Special instructions:
    Form release / dosage:

    A solution for intravenous and subcutaneous administration of 0.5 mg / ml per 1 ml in ampoules, 10 ampoules together with a scarifier and instructions for use in a box; or 5 ampoules per contour cell package, 2 contour packs along with a scarifier and instructions for use in a pack.

    Packaging:

    ampoules (10) / complete with scarifier / - carton boxes
    ampoules (5) / complete with scarifier / - packs, cellular contour-packs, cardboard

    Storage conditions:

    AT protected from light at a temperature of 18 to 25 ° C. Keep out of the reach of children.

    Shelf life:

    4 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000262
    Date of registration:05.03.2010
    The owner of the registration certificate:MIKFARM, LLCMIKFARM, LLC
    Manufacturer: & nbsp
    Information update date: & nbsp07.08.2015
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