Prozerin

Prozerin – the synthetic inhibitor of cholinesterase recovering neuromuscular conductivity, urezhayushchiya heart rate, increasing secretion of glands (salivary, digestive tract, stalemate and bronchial), increasing acidity of a gastric juice, narrowing the pupil causing the accommodation spasm reducing intraocular pressure, strengthening a tone of smooth muscles and bladder, the defiant spasm of bronchial tubes toning skeletal muscles.

Form of release and structure

• Tablets: a ploskotsilindrichesky form, white color, with a facet (on 10 pieces in blister strip packagings, 2 packagings in a pack cardboard);
• Solution for injections: colourless transparent liquid (on 1 ml in ampoules of neutral glass, on 10 ampoules with an ampoule knife or the scarificator in a cardboard pack or on 5 ili10 ampoules in a blister strip packaging, 1 or 2 packagings with an ampoule knife or the scarificator in a pack cardboard; if ampoules with a point of a break or a ring of a break are used the ampoule knife / scarificator does not invest in packaging);
• Solution for intravenous (in/in) and hypodermic (п / to) introductions: colourless transparent liquid (on 1 ml in ampoules, on 10 ampoules with the ampoule scarificator in a pack cardboard or on 5 ampoules in blister strip packagings, on 2 packagings with the ampoule scarificator in a pack cardboard).

Active agent – a neostigmina methyl sulfate (прозерин):

• 1 tablet – 15 mg;
• 1 ml of solution for injections – 0,5 mg;
• 1 ml of solution for in/in and п / to introduction – 0,5 mg.

Auxiliary components of tablets: potato starch, calcium stearate monohydrate, sucrose (sugar).

Additional substance of injection solutions: water for injections.

Indications to use

For all dosage forms of Prozerin:

• gravis myasthenia;
• Paralyzes;
• Motive disturbances after a brain injury;
• The recovery period after the postponed encephalitis, poliomyelitis, meningitis.

In addition for injection solutions:

• Atony of digestive tract and bladder (prevention and treatment);
• Neuritis;
• Weakness of patrimonial activity (for stimulation);
• Muscular weakness and respiratory depression (as an antidote after anesthesia with use of not depolarizing muscle relaxants);
• Atrophy of an optic nerve.

Contraindications

For all dosage forms:

• Epilepsy;
• Arrhythmias;
• Bradycardia;
• Stenocardia;
• Coronary heart disease;
• Vagisection;
• The expressed atherosclerosis;
• Hyperkinesias;
• Thyrotoxicosis;
• Bronchial asthma;
• Infectious diseases in the acute period;
• Prostate hyperplasia;
• Mechanical obstruction of digestive tract and urinary tract;
• Peritonitis;
• Peptic ulcer of a stomach and 12-perstny gut;
• Pregnancy;
• Lactation;
• Hypersensitivity to drug components.

In addition for tablets:

• Deficit of invertase/isomaltase, glyukozo-galaktozny malabsorption, intolerance of fructose;
• Age up to 18 years.

Route of administration and dosage

In the tableted form Prozerin appoint inside (for half an hour to food), in the form of solution for injections – enter subcutaneously, intramusculary or intravenously, in the form of solution for in/in and п / to introduction – intravenously or subcutaneously.

The recommended schemes of use for adults depending on indications:

• Myasthenia: a single dose inside – 15 mg, daily – 50 mg. Treatment of a disease long (25-30 days) with change of ways of use of drug, the most part of a daily dose in the form of tablets is appointed in the afternoon when the patient is most fatigue. At myasthenic crisis at adults Prozerin enter intravenously (with solution of sodium of chloride of 0,9%) in a dose of 0,25-0,5 mg, further – subcutaneously in usual doses with small breaks. For strengthening of effect of drug if necessary in addition enter п / to solution of ephedrine of 5% (1 ml);
• Motive disturbances owing to injuries of the central nervous system, encephalitis and meningitis, at paralyzes of a facial nerve: inside on 15 mg 1-2 times a day within 2-3 weeks;
• Motive disturbances owing to poliomyelitis (in a complex with physical therapy, remedial gymnastics, balneological treatment and other actions): inside on 15 mg of 1 times a day daily or every other day. The course of treatment consists of 15-20 doses. Bucketed 2-3 months conduct repeated courses;
• Stimulation of childbirth: п / to in a dose of 0,5 mg, if necessary in 1 hour introduction is repeated. With the first dose once enter 1 mg of 0,1% of solution of atropine п / to;
• Stopping of action of not depolarizing muscle relaxants: at first enter atropine in/in in a dose of 0,5-0,7 mg, in 1-2 minutes (when pulse becomes frequent) enter into 1,5 mg of Prozerin. At insufficiency of effect enter repeated doses, but no more than 5-6 mg of a neostigmin of methyl sulfate within 20-30 minutes. During the procedure provide adequate ventilation of the lungs;
• Prevention of a postoperative atony of intestines and bladder (including postoperative ischuria): п / to or in oil 0,25 mg in a dose as soon as possible after operation, further – each 4-6 hours in the same dose within 3 days;
• Treatment of an ischuria: п / to or in oil 0,5 mg in a dose. If within 1 hour the diuresis is not recovered, do catheterization for bladder emptying. Further the drug is administered by each 3 hours, all – 5 injections.

To children drug is appointed only at a myasthenia гравис, treatment is carried out only in the conditions of a hospital. The drug is administered п / to or in oil 0,05 mg in a dose for 1 year of life a day, but by no more than 0,375 mg for 1 injection. As a rule, the daily dose is entered once, but if necessary can be divided into 2-3 injections.

Side effects

• From cardiovascular system and blood (a hemopoiesis, a hemostasis): bradycardia, arrhythmia, tachycardia, a nodal rhythm, an atrioventricular block, a syncope, nonspecific changes on the electrocardiogram, a lowering of arterial pressure (it is preferential at parenteral administration), a cardiac standstill;
• From a nervous system and sense bodys: weakness, drowsiness, loss of consciousness, headache, вертиго, dysarthtia, vision disorder, miosis, spasms;
• From respiratory system: an asthma, strengthening of bronchial and pharyngeal secretion, a bronchospasm (it is preferential at parenteral administration), respiratory depression up to a stop;
• From the alimentary system: meteorism, nausea, vomiting, diarrhea, spastic reduction and strengthening of a vermicular movement of intestines, hypersalivation;
• Allergic reactions: rash, itch, hyperemia of the person, anaphylaxis;
• Others: spasms and twitchings of skeletal muscles (including fastsikulyation of muscles of language), tremor, arthralgia, spasms, plentiful sweating, increase of an urination.

To remove side effects, reduce Prozerin's dose or stop its use. If there is a need, enter a metotsiniya iodide, 0,1% solution of atropine or other holinoblokator.

Special instructions

During treatment it is necessary to be careful at the driving of the car and performance of work demanding the speed of reactions and special attention.

If during therapy there is myasthenic or cholinergic crisis (owing to an insufficient therapeutic dose or overdose respectively), it is necessary to carry out careful differential diagnosis because of similarity of symptomatology.

Medicinal interaction

At a myasthenia Prozerin appoint in a combination with anabolic hormones and glucocorticosteroids.

Novokainamid, quinidine, local anesthetics, ganglioblokator (Pachycarpinum hydroiodide), m-holinoblokatory (including homatropine hydrobromide, a metotsiniya iodide, Platyphyllinum and atropine) weaken m - cholinomimetic effects of drug (are his pharmacological antagonists) that is shown by strengthening of motility of digestive tract, hypersalivation, narrowing of a pupil, bradycardia, etc.

With care Prozerin it is necessary to apply along with cholineblockers, at patients with a myasthenia – along with Kanamycinum, Neomycinum, streptomycin and other antibiotics which have the anti-depolarizing effect, and also with antiarrhytmic drugs, local anesthetics, means for the general anesthesia and other medicines breaking cholinergic transfer.

Neostigmina methyl sulfate – the antagonist of not depolarizing muscle relaxants (including Tubocurarini chloridum, a bromide rokuroniya, an atrakuriya of a bezilat) recovering neuromuscular conductivity. When after the termination of anesthesia using not depolarizing muscle relaxants muscular weakness and respiratory depression remain, Prozerin use as an antidote of these means.

Prozerin pharmacological is incompatible with the depolarizing muscular relaxants (for example, succinylcholine iodide).

The cyanocobalamine applied in high doses weakens action of a neostigmin of methyl sulfate.

Prozerin reduces activity of a pyridoxine.

As well as all inhibitors of cholinesterase, Prozerin in a combination to laxatives strengthens their action, with strychnine – considerably raises a tone of a vagus nerve.

Antiarrhythmic drugs (β-adrenoblockers)))))))))) and a neostigmina methyl sulfate are synergists (bradycardia is aggravated).

Prozerin is well combined: at cardiovascular frustration – with Nikethamidum, at neuritis – with thiamin, at muscular dystrophies – from calcium a gluconate and adenosinetriphosphate.

Ephedrine exponentiates action of a neostigmin of methyl sulfate therefore it is entered together with Prozerin at myasthenic crises.

Terms and storage conditions

To store in the place, dry, dark, unavailable to children.

Period of validity:

• Tablets – 5 years at a temperature up to 25 °C;
• Solution for injections – 4 years at a temperature of 15-25 ºС;
• Solution for in/in and п / to introduction – 4 years at a temperature of 18-25 ºС.