Active substanceNeostigmine methyl sulfateNeostigmine methyl sulfate
Similar drugsTo uncover
  • 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: & nbspinjection
    Composition:

    Active substance: neostigmine methyl sulfate (proserin) - 0.5 mg. Excipient: water for injection - up to 1 ml.

    Description:Colorless transparent liquid.
    Pharmacotherapeutic group:cholinesterase inhibitor
    ATX: & nbsp

    S.01.E.B   Parasympathomimetics

    S.01.E.B.06   Neostigmine

    Pharmacodynamics:

    Synthetic cholinesterase inhibitor. 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 gastric intestinal tract) and promotes the development of hypersalivation, bronchorrhea, increased acidity of the gastric juice, narrows the pupil, spasm of accommodation, reduces intraocular pressure, strengthens the tone of the smooth muscles of the intestine (enhances peristalsis and relaxes the sphincters) and bladder, causes spasm of the bronchi, increases the tone of the skeletal muscles.

    Pharmacokinetics:

    Being a quaternary ammonium base, poorly penetrates the blood-brain barrier and does not have a central effect. Bioavailability of neostigmine methyl sulfate is 1-2 %. When intramuscular injection, the time to reach the maximum concentration in the blood plasma - 30 minutes.

    Connection with blood plasma proteins - 15-25%. The half-life with intramuscular injection of the drug is 51-90 minutes, with intravenous - 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% is unchanged and 30% in the form of metabolites).

    After intramuscular injection, the maximum effect is observed after 10-30 minutes, and after intravenous - after 5-15 minutes. The duration of the effect is 2.5-4 h.

    Indications:

    Myasthenia gravis; motor disorders after brain injuries; paralysis; the recovery period after the meningitis, poliomyelitis, encephalitis; neuritis; prevention and treatment of atony of the gastrointestinal tract and bladder; weakness of labor activity (rarely). As an antidote after anesthesia with the use of nondepolarizing muscle relaxants with muscle weakness and respiratory depression.

    In children's practice apply only with myasthenia gravis gravis.

    Contraindications:

    Hypersensitivity, epilepsy, hyperkinesia, ischemic heart disease, bradycardia, arrhythmias, angina pectoris, bronchial asthma, severe atherosclerosis, hyperthyroidism, peptic ulcer and duodenal ulcer, peritonitis, mechanical obstruction of the gastrointestinal tract and urinary tract, prostatic hyperplasia.

    The use of the drug is contraindicated in the period of acute infectious diseases, intoxication in severely impaired children.

    Carefully:
    Pregnancy and lactation:The use of the drug is contraindicated in pregnancy and during breastfeeding.
    Dosing and Administration:

    Subcutaneously, intramuscularly, intravenously.

    Adults are usually prescribed skin of 0.5 mg (1 ml of solution) Prozerina 1-2 times a day, the maximum single dose is 2 mg, daily - 6 mg.

    With the development of the myasthenic crisis in adults, the drug is administered

    intravenously (from 0.9 % solution sodium chloride) 0.25-0.5 mg (0.5-1 ml of solution) of Proserin, then under the skin in usual doses with in small intervals.

    Treatment of myasthenia gravis long.

    With other diseases, the course treatment lasts 25-30 days, if necessary treatment course repeat after 3-4 weeks break.

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

    When using the drug for stopping action Nondepolarizing muscle relaxants previously introduced atropine intravenously in a dose of 0.5-0.7 mg (0.5-0.7 ml of a 0.1% solution) are expected increased heart rate and 1.5-2 minutes are administered intravenously 1.5 mg (3 ml of 0.5 mg / ml solution) preparation. If the effect of this dose was inadequate, the same dose of the appearance of bradycardia make an additional injection atropine). In total, you can enter 5-6 mg (10-12 ml of 0.5 mg / ml solution) of the drug for 20-30 minutes.

    With postoperative atony of the intestine, the bladder: for prevention, at t.ch. postoperative urine retention - subcutaneously or intramuscularly at 0.25 mg (0.5 ml) of Prozerin, as soon as possible after surgery, and repeatedly every 4-6 hours for 3 days; Treatment of a delay of urine - subcutaneously or intramuscularly 0.5 mg (1 ml of solution) of Prozerin; if within 1 h diuresis is not restored, conduct catheterization and after emptying the bladder is administered every 3 hours, with only 5 injections. Children are only used with myasthenia gravis gravis (only in a hospital!) subcutaneously or intramuscularly at 0.05 mg (0.1 ml of 0.5 mg / ml solution) for 1 year life per day, but not more than 3.75 mg (0.75 ml 0.5 mg / ml solution) per injection.

    Usually the children are prescribed once a day, however, if necessary, the daily dose can be divided into two or three doses, once a day, but with The need for a daily dose can be divided into two or three admission.

    Side effects:

    From the nervous system and sensory organs: headache, dizziness, convulsions, weakness, loss of consciousness, drowsiness, miosis, impaired vision, dysarthria.

    From the cardiovascular system and blood (hematopoiesis, hemostasis): arrhythmia, brady- or tachycardia, atrioventricular block, nodal rhythm, nonspecific changes on the electrocardiogram, syncope, cardiac arrest, lowering of arterial pressure (mainly with parenteral administration).

    On the part of the respiratory system: strengthening pharyngeal and bronchial secretion, dyspnea; respiratory depression up to a stop, bronchospasm (mainly with parenteral administration).

    On the part of the organs of the gastrointestinal tract: hypersalivation, spastic reduction and increase in intestinal peristalsis, nausea, vomiting, flatulence, diarrhea.

    Other: tremor, spasms and twitching of skeletal muscles, including fasciculation of the muscles of the tongue, convulsions, dysarthria, arthralgia; increased frequency of urination; profuse sweating; allergic reactions (face hyperemia, 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 holinoblokatory.

    Overdose:

    In case of overdose (hypersalivation, heavy sweat, abdominal pain, diarrhea, difficulty breathing, bradycardia, cyanosis, miosis, skeletal muscle twitching, muscle weakness), stop taking the drug and immediately enter atropine (1 ml 0.1% solution under the skin) or other holinoblokatory. In cases of severe poisoning with proserin, atropine sulfate is administered at intervals of 10 minutes up to 3 times (until dry mouth appears). If there is a seizure, intravenous injection of sodium thiopental under the supervision of a doctor.

    Interaction:

    Neostigmine methyl sulfate is an antagonist of nondepolarizing muscle relaxants, restores impaired neuromuscular conduction.Therefore, if after the termination of anesthesia with nondepolarizing muscle relaxants muscle weakness and respiratory depression remain, neostigmine methylsulfate are used as an antidote for this group of muscle relaxants (atracurium bezylate, rocuronium bromide, tubocurarine chloride, etc.).

    Neostigmine methyl sulfate and depolarizing muscle relaxants (suxamethonium iodide and others) are pharmacologically incompatible, since in the direct interaction the effect of suxamethonium iodide is enhanced.

    M-holinoblokatory (atropine, gomatropine hydrobromide, platyphylline and etc.), ganglion blockers (pahikarpine hydroiodide), quinidine, novocainamide, Local anesthetics are pharmacological antagonists of neostigmine methyl sulfate.

    There is relative antagonism between tricyclic antidepressants, antiepileptic and antiparkinsonian agents.

    Cyanocobalamin in large doses weakens the effect of neostigmine methyl sulfate. The interaction of neostigmine methyl sulfate with pyridoxine decreases the activity of the latter.

    Cholinesterase inhibitors in combination with strychnine significantly increase the tone of the vagus nerve; with laxatives - strengthen them act; with antiarrhythmic drugs (β-adrenoblockers) are synergists (aggravation of bradycardia).

    Ephedrine potentiates the action of neostigmine methyl sulfate, so with myasthenic crises it is administered together with neostigmine methyl sulfate.
    Special instructions:


    Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from driving and other potentially hazardous species The activities that require special attention and speed of reactions.
    Form release / dosage:

    Solution for injection 0.5 mg / ml.

    1 ml per ampoule of neutral glass.

    For 10 ampoules with instructions for application and knife for opening ampoules or scarifier The ampoule is placed in a box of cardboard.

    For 5 or 10 ampoules are placed in contour cell packaging from films of polyvinylchloride or polyethylene terephthalate and aluminum foil or paper with polyethylene coating, or without foil, or without paper.

    1 or 2 contour spinal packages with instructions for application and knife for opening ampoules or scarifier The ampoule is placed in a pack of cardboard.

    When packing ampoules with a ring fracture or break point knife for ampoule opening or scarifier ampoule does not invest.

    Packaging:ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - cardboard boxes
    ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cell outlines without cover-packs cardboard
    ampoules (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cellular contour-packs cardboard
    ampoules (5) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cell outlines without cover-packs cardboard
    ampoules (5) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packaging, cellular contour-packs cardboard
    Storage conditions:

    In the dark place at a temperature of 15 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001354
    Date of registration:28.09.2011
    The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp07.08.2015
    Illustrated instructions
      Instructions
      Up