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 ml of the solution contains:

    active substance: proserin (neostigmine methyl sulfate) 0.5 mg; auxiliary substance: water for injection up to 1 ml.

    Description:clear, colorless liquid.
    Pharmacotherapeutic group:cholinesterase inhibitors.
    ATX: & nbsp

    S.01.E.B   Parasympathomimetics

    S.01.E.B.06   Neostigmine

    Pharmacodynamics:

    Synthetic cholinesterase inhibitor of reversible action. Has a high relationship to acetylcholinesterase, which is due to its structural identity with acetylcholine. Like acetylcholine, Prozerin-Darnitsa initially interacts with the catalytic center of cholinesterase, but in the future, unlike acetylcholine, it forms, at the expense of its carbamoy group, a stable compound with the enzyme. The enzyme temporarily (from several minutes to several hours) loses its specific activity. After this time, due to the slow hydrolysis of Proserin-Darnitsa, cholinesterase is released from the blocker and restores its activity.This action leads to the accumulation and enhancement of the action of acetylcholine in the cholinergic synapses. Prozerin-Darnitsa has a pronounced muscarinic and nicotine effect, it is able to directly stimulate the skeletal muscles.

    Causes a decrease in heart rate, increases secretion of excretory glands (salivary, bronchial, sweat and gastrointestinal tract) and promotes the development of hypersalivation, bronchorrhoea, increased acidity of the gastric juice, narrows the pupil, causes a spasm of accommodation, reduces intraocular pressure, strengthens the tone of the smooth muscles of the intestine (enhances peristalsis and relaxes the sphincters) and urinary bladder, causes spasm of the bronchi, tones up the skeletal muscles.

    Pharmacokinetics:

    Prozerin-Darnitsa, being a quaternary ammonium base, poorly penetrates the blood-brain barrier and does not have a central effect. Bioavailability for parenteral administration is high, 0.5 mg of Prozerin-Darnitsa administered parenterally corresponds to 15 mg taken internally. With increasing dose of the drug, bioavailability increases.With intramuscular injection, the time to reach the maximum concentration in the blood is 30 minutes. The connection with proteins (albumin) of plasma is 15-25%. The half-life (T1/2) with intramuscular injection - 51-90 min, with intravenous administration - 53 min. Metabolized in two ways. Due to hydrolysis at the junction with cholinesterase and microsomal enzymes of the liver. In the liver, inactive metabolites are formed. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% is unchanged and 30% is metabolites).

    Indications:

    Myasthenia gravis, motor disorders after brain injuries, paralysis, recovery period after meningitis, poliomyelitis, encephalitis; weakness of labor (rarely); prevention and treatment of atony of the gastrointestinal tract and bladder. In children, the drug is used only with myasthenia gravis gravis.

    Elimination of residual disorders of neuromuscular transmission by non-depolarizing muscle relaxants.

    Contraindications:

    Hypersensitivity, epilepsy, hyperkinesia, vagotomy, bronchial asthma, ischemic heart disease, arrhythmias, angina, bradycardia, severe atherosclerosis, thyrotoxicosis, peptic ulcer and duodenal ulcer, peritonitis, mechanical obstruction of the gastrointestinal tract and urinary tract, prostatic hyperplasia, acute infectious diseases, intoxication in weakened children, pregnancy, lactation.

    Dosing and Administration:

    Method of administration: subcutaneously and intravenously.

    Prozerin-Darnitsa should be injected intravenously very slowly. There must always be a ready-made solution of atropine to eliminate the arising severe cholinergic reactions.

    For the treatment of motor disorders after brain injuries, paralysis, during the recovery period after the meningitis, poliomyelitis, encephalitis: Adults - 0.5-1-2 mg (0.5 mg - 1 ml 0.05% solution) 1-2 times a day, the maximum single dose - 2 mg, daily - 6 mg.

    The course of treatment (except for myasthenia gravis) - 25-30 days, if necessary - again, after 3-4 weeks. Most of the total daily dose is administered in the daytime, when the patient is most fatigued.

    With myasthenia gravis subcutaneously 0.5 mg per day; The course of treatment is long, with a change in the way of administration. With myasthenic crisis (with difficulty breathing and swallowing) - adults 0.5-1 ml 0.05% solution intravenously, then subcutaneously, with small intervals.

    With postoperative atony of the intestine, bladder: for prevention, incl.postoperative urinary retention, subcutaneously, 0.25 mg as soon as possible after surgery, and repeatedly every 4 to 6 hours for 3-4 days; treatment of urine retention - subcutaneously 0.5 mg; if the urine does not depart within 1 hour, catheterization is carried out and after the bladder is emptied, injected every 3 hours, with only 5 injections.

    With the weakness of labor: subcutaneously - 1 ml of 0.05% solution 1-2 times with a break of 1 hour (in combination with 1 ml of 0.1% solution of atropine, subcutaneously once, against the background of the first injection).

    To eliminate residual neuromuscular disorders by nondepolarizing muscle relaxants (after the preliminary administration of atropine at a dose of 0.6-1.2 mg intravenously, before the pulse is increased to 80 beats / min), 0.5-2 mg is injected slowly slowly through 1 / 2-2 minutes. If necessary, injections are repeated (including atropine in the case of bradycardia) in a total dose of not more than 5-6 mg (10-12 ml) for 20-30 minutes; During the procedure, good ventilation is provided.

    Children (only in a hospital with myasthenia gravis gravis) 0.05 mg (0.1 ml 0.05% solution) subcutaneously for 1 year of life per day, but not more than 3.75 mg (0.75 ml 0.05% solution) per injection.

    Carefully prescribe against the background of m-holinoblokatorov, in children (with myasthenia) against neomycin, streptomycin,kanamycin and other antibiotics with antidepolarizing effect, local and some common anesthetics, antiarrhythmic drugs and a number of other drugs that disrupt the cholinergic transmission.

    Application in pregnancy and lactation

    Strictly controlled studies on the use of Prozerin-Darnitsa in pregnant women have not been conducted. The application is only possible if the benefit to the mother exceeds the risk to the fetus.

    If you need to use Prozerin-Darnitsa during lactation, breast-feeding should be stopped.

    Children

    Children are used for myasthenia gravis gravis subcutaneously (only in a hospital setting) at the doses specified in the "Method of administration and dose" section.

    Side effects:

    From the digestive system: hypersalivation, spastic reduction and enhancement of peristalsis, nausea, vomiting, flatulence, diarrhea.

    From the side of the ventral and peripheral nervous system: headache, dizziness, weakness, loss of consciousness, drowsiness, miosis, visual impairment, spasms, twitching of skeletal muscles (including muscles of the tongue), convulsions, dysarthria.

    From the cardiovascular system: arrhythmias in the form of brady or tachycardia, AUBlocade, nodal rhythm, nonspecific changes on the ECG, arterial hypotension, extrasystolic arrhythmia, sudden cardiac arrest.

    From the respiratory system: shortness of breath, respiratory depression, up to a stop, bronchospasm, increased secretion of pharyngeal and bronchial glands, increased bronchial tonus.

    Allergic Reagents: possible skin rash, itching, face hyperemia, anaphylactic reactions.

    Other: arthralgia, increased frequency of urination, excessive sweating.

    Overdose:

    Symptoms: (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased intestinal peristalsis, diarrhea, increased urination, difficulty breathing, cyanosis, muscle twitching of the tongue and skeletal muscles, gradual development of muscle weakness, lowering of blood pressure.

    Treatment: reduce the dose or stop the administration of the drug. If necessary, enter atropine (1 ml of 0.1% solution under the skin), metocinium iodide and other anticholinergic drugs. Further treatment is symptomatic.

    Interaction:

    Prozerin-Darnitsa 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 designate Proserin-Darnitsa.

    Prozerin-Darnitsa weakens or eliminates the effect of nondepolarizing muscle relaxants (atracurium bezylate, rocuronium bromide etc.).

    Caution is prescribed against the background of m-holinoblokatorov, in children (with myasthenia gravis) against neomycin, streptomycin, kanamycin and other antibiotics with antidepolarizing effect, local and some general anesthetics, antiarrhythmic drugs and a number of other drugs that disrupt the cholinergic transmission.

    M-holinoblokatory (atropine, metocinia iodide, gomatropine hydrobromide,

    platifillin, etc.), ganglion blockers (pahikarpine hydroiodide), quinidine, procainamide, local anesthetics are pharmacological antagonists of Prozerin-Darnitsa.

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

    Reduces the activity of pyridoxine.

    Cholinesterase inhibitors in combination with strychnine significantly increase the tone of the vagus nerve; with laxatives - strengthen their action; with antiarrhythmic drugs ((3-adrenoblockers) are synergists (aggravation of bradycardia).

    Ephedrine enhances the action of Proserin-Darnitsa, therefore, with myasthenic crises, they are administered together.

    Incompatibility

    Easily destroyed by alkalis and oxidants.

    Special instructions:

    When parenteral administration in high doses, a preliminary or simultaneous administration of atropine is necessary.

    When a myasthenic (due to an insufficient therapeutic dose) or cholinergic (due to an overdose) crisis occurs during therapy, careful differential diagnosis is required because of the similarity of the symptoms.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, one should refrain from driving vehicles and other potentially hazardous activities,which require attention concentration and high speed psychomotor reactions.
    Form release / dosage:

    Solution for intravenous and subcutaneous administration.

    1 ml per ampoule of transparent glass.

    It is allowed to paste on the ampoule paper label with self-adhesive coating.

    5 ampoules with an autopsy knife ampoules or scarifier ampoule into the contour mesh packing (cassette).

    Two contoured cell packs with instruction on medical application in a pack.

    10 ampoules together with the instructions for medical use and knife for opening ampoules or by ampoule scapegrator box with corrugated liner. Boxes pasted with a label-parcel. When packaging ampoules with a color ring or break point, knives for opening ampoules or ampoule scalers are not included.

    Packaging:the ampoule (10) / complete with ampoule knife or lancet, if necessary for this type ampoules / - boxes
    the ampoule (5) / complete with ampoule knife or lancet, if necessary for this type ampoules / - packings Valium planimetric cassette-pack
    Storage conditions:

    Keep out of reach of children, at a temperature of 5 ° C to 25 ° C.

    Shelf life:

    4 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N010604
    Date of registration:17.05.2010
    The owner of the registration certificate:DARNITSA PHARMACEUTICAL FIRM, CJSCDARNITSA PHARMACEUTICAL FIRM, CJSC Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp07.08.2015
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