Analogue of "Proserin" in action. Comparison of analogues and reviews about them. Prozerin analogues and prices Prozerin instructions for use analogues

As part of drugs in tablets contains active ingredient neostigmine methyl sulfate , as well as additional ingredients: potato starch, sucrose, calcium stearate.

Part Prozerin in the form of a solution contains the active ingredient neostigmine (0.5 mg) and water for injection as an additional component.

Release form

Produced Prozerin tablets which are contained in packs of 20 pcs. (two blister packs each). White tablets.
Prozerin in the form of a solution contained in ampoules of 1 ml.

pharmachologic effect

The pharmacological group of the drug is a cholinesterase inhibitor. It is a synthetic anticholinesterase drug that reversibly blocks cholinesterase. As a result of this action, acetylcholine accumulates and its effect on tissues and organs increases. As a result, neuromuscular conduction is restored.

Under the influence of the drug, the heart rate decreases, the secretion of the bronchial, salivary, sweat glands, as well as the glands of the digestive tract increases. In turn, this contributes to the manifestation of bronchorrhea, hypersalivation, and an increase in the level of acidity of gastric juice.

The active substance causes pupillary constriction, lowers , provides stimulation of the tone of the smooth muscles of the intestines and bladder, tones the skeletal muscles, provokes bronchospasm.

Prozerin is an antagonist of antidepolarizing curariform drugs. When taking large doses, the drug can provoke a violation of neuromuscular conduction, which occurs due to the accumulation of acetylcholine. It produces a direct n-cholinomimetic effect. The influence of the agent coincides with the characteristic effects of excitation of the cholinergic nerves. It does not cause central effects, in comparison with it provides more active stimulation of the muscles of the bladder, intestines, uterus. Little effect on the heart.

Pharmacokinetics and pharmacodynamics

After the introduction of neostigmine methyl sulfate parenterally, the substance undergoes hydrolysis . It also occurs in the liver, in which inactive ones are formed. It binds to proteins by 15-25%. It is excreted from the body through the kidneys, while 80% of the substance is excreted within 24 hours, while approximately 50% is excreted as metabolites. It penetrates poorly through the BBB.

Indications for Prozerin's use

There are the following indications for the use of Prozerin:

movement disorders after brain injury;
recovery after , meningitis, ;
open-angle ;
with intestinal atony, atony of the digestive tract as a whole;
atony of the bladder;
neuritis, ;
weak labor activity (in rare cases);
in order to eliminate disorders of neuromuscular transmission with non-depolarizing muscle relaxants.

The use of funds for children is practiced in similar cases.

Contraindications

The medicine can not be used for such diseases and conditions:

hyperkinesis;
arrhythmia, bradycardia;
vagotomy ;
ischemic heart disease (including angina pectoris);
expressed;
stomach and duodenal ulcer;
thyrotoxicosis;
peritonitis;
mechanical obstruction of the urinary tract or digestive tract;
prostate hyperplasia;
acute infectious diseases;
in children weakened by diseases;
high sensitivity to neostigmine methyl sulfate .

Side effects

Injections and taking Prozerin tablets can cause the following side reactions:

digestion: , hypersalivation, vomiting, , nausea, increased peristalsis;
central and peripheral NS: and, blurred vision, weakness, miosis, , convulsions, impaired consciousness, dysarthria, skeletal muscle twitching;
heart and blood vessels: , bradycardia, arrhythmia, AV blockade, junctional rhythm, non-specific ECG changes, decrease;
: rash on the skin, flushing of the face, anaphylactic manifestations;
breath: respiratory depression, increased bronchial tone, increased secretion of bronchial glands, ;
other manifestations: increased urination, increased sweating, arthralgia.

Application instruction of Prozerin (Way and dosage)

Injections with Prozerin, instructions for use

In order to use the drug to stop the effect of muscle relaxants, it is initially administered intravenously atropine sulfate (0.5-0.7 mg), then wait until the pulse quickens and after about 2 minutes, 1.5 mg of Prozerin is administered intravenously. If the effect is insufficient, a similar dose is administered repeatedly. In total, the introduction of 5-6 mg of the drug for about 30 minutes is allowed.

In ophthalmology, it is practiced to introduce 1-2 drops into the conjunctival sac from 1 to 4 times a day.

Oral administration is carried out at the rate of 10-15 mg 2-3 times a day for adults and 1 mg per day for 1 year of life for children under 10 years of age. The highest allowable dose for adults is 50 mg per day, for children - 10 mg per day.

Overdose

With an overdose of the drug, symptoms occur that are associated with the process of overexcitation of cholinergic receptors (the so-called cholinergic crisis). Hypersalivation, miosis, bradycardia, nausea, bronchospasm, frequent urination, general weakness, twitching of the muscles of the skeletal muscles and tongue, lowering may develop.

In this case, you need to reduce the dose of the drug or stop taking it completely. If there is such a need, the patient is administered, as well as other drugs with anticholinergic action.

Interaction

It should be borne in mind that neostigmine methyl sulfate is an antagonist of non-depolarizing muscle relaxants, therefore, when taken simultaneously, it activates the effect of depolarizing muscle relaxants.

If applied at the same time ganglioblockers, m-cholinergic blockers, Novocainamide, Quinidine, local action, tricyclic antidepressants , drugs with antiepileptic and antiparkinsonian action, the effect of neostigmine methyl sulfate is reduced.

The effect of neostigmine methyl sulfate is potentiated when taken .

When taking neostigmine methyl sulfate and beta blockers may intensify bradycardia .

Terms of sale

You can buy Prozerin by prescription, the doctor writes out a prescription in Latin.

Storage conditions

Store in a dark and dry place, at t no more than 25 degrees.

Best before date

Prozerin in ampoules is stored for 1.5 years, in tablets - 5 years.

special instructions

Injections and pills are used with caution in people with Addison's disease.

When administered parenterally in large doses, Atropine must be administered simultaneously or preliminarily.

If during treatment a myasthenic crisis develops (due to an insufficient dose) or a cholinergic crisis (due to an overdose), a thorough differential diagnosis should be carried out due to the similarity of signs.

Prozerin's analogs

Coincidence in the ATX code of the 4th level:

An analogue of this medicine is a remedy Neostigmine methyl sulfate . Analogues according to the mechanism of action - drugs Armin , Amiridin , Deoxypeganine hydrochloride , Oksazil .

children

For the treatment of children, it is recommended to use Prozerin in the form of granules, which are previously dissolved in water. Children under 10 years of age are shown taking 1 mg of medication per day for each year of life. Electrophoresis with Prozerin is also practiced for children under the supervision of a doctor.

During pregnancy and lactation

The active substance penetrates the placental barrier, passes in small amounts into breast milk. Therefore, it is possible to use the remedy during the period and at the time only if there are strict indications.

Name:

Prozerin (Proserinum)

Pharmacological
action:

Acetylcholinesterase and pseudocholinesterase inhibitor.
It has an indirect cholinomimetic effect due to reversible inhibition of cholinesterase and potentiation of the action of endogenous acetylcholine.
It improves neuromuscular transmission, enhances gastrointestinal motility, increases the tone of the bladder, bronchi, and secretion of exocrine glands.
Causes bradycardia, lowering blood pressure. Constricts the pupil, lowers intraocular pressure, causes a spasm of accommodation.

Pharmacokinetics
After parenteral administration of neostigmine, methyl sulfate undergoes hydrolysis and is also metabolized in the liver to form inactive metabolites.
Plasma protein binding is 15-25%.
It is excreted in the urine (80% within 24 hours) in the form of unchanged substance (about 50%) and metabolites. Poorly penetrates through the BBB.

Indications for
application:

Myasthenia and myasthenic syndrome;
- movement disorders after brain injury, paralysis;
- recovery period after meningitis, poliomyelitis, encephalitis;
- weakness of labor activity (rarely);
- atrophy of the optic nerve, neuritis;
- atony of the stomach, intestines and bladder;
- elimination of residual disorders of neuromuscular transmission with non-depolarizing muscle relaxants.
- in ophthalmology: to narrow the pupil and lower intraocular pressure in open-angle glaucoma.

Mode of application:

Inside adults- 10-15 mg 2-3 times / day; s / c - 1-2 mg 1-2 times / day.
Inside children under 10 years old- 1 mg/day for 1 year of life; for children over 10 years of age, the maximum dose is 10 mg. S / c dose is calculated at 50 mcg for 1 year of life, but not more than 375 mcg per injection.
In ophthalmology: injected into the conjunctival sac 1-4 times / day.
Maximum doses: for adults, when taken orally, a single dose is 15 mg, daily - 50 mg; with s / c administration, a single dose is 2 mg, a daily dose is 6 mg.

Side effects:

From the digestive system: nausea, vomiting, diarrhea, hypersalivation, flatulence, spastic contraction and increased peristalsis.
From the side of the central nervous system and peripheral nervous system: headache, dizziness, weakness, loss of consciousness, drowsiness, miosis, visual disturbances, twitching of skeletal muscles (including the muscles of the tongue), convulsions, dysarthria.
From the side of the cardiovascular system: arrhythmias, brady- or tachycardia, AV blockade, junctional rhythm, nonspecific ECG changes, lowering blood pressure.
From the respiratory system: shortness of breath, respiratory depression, increased secretion of bronchial glands, increased bronchial tone.
allergic reactions: possible skin rash, itching, flushing of the face, anaphylactic reactions.
Other: arthralgia, increased urination, increased sweating.

Contraindications:

Epilepsy, hyperkinesis;
- vagotomy, bronchial asthma;
- IHD (including angina pectoris);
- arrhythmias, bradycardia;
- severe atherosclerosis;
- thyrotoxicosis;
- peptic ulcer of the stomach and duodenum;
- peritonitis, mechanical obstruction of the gastrointestinal tract or urinary tract;
- prostatic hyperplasia;
- acute infectious diseases;
- intoxication in debilitated children;
- hypersensitivity to neostigmine methyl sulfate.

Carefully used in Addison's disease.
With parenteral administration in high doses, preliminary or simultaneous administration of atropine is necessary.
If a myasthenic (due to insufficient therapeutic dose) or cholinergic (due to overdose) crisis occurs during therapy, careful differential diagnosis is required due to the similarity of symptoms.
Influence on the ability to drive vehicles and control mechanisms
During the period of treatment, one should refrain from driving vehicles and other potentially hazardous activities that require concentration of attention and a high speed of psychomotor reactions.

Interaction
other medicinal
by other means:

Drug interaction P roserin is not described.

Pregnancy:

Neostigmine methyl sulfate crosses the placental barrier and is excreted in breast milk in very small amounts.
During pregnancy and lactation, use only according to strict indications.

pharmachologic effect

Synthetic anticholinesterase agent. It reversibly blocks cholinesterase, which leads to the accumulation and enhancement of the action of acetylcholine on organs and tissues, and the restoration of neuromuscular conduction. Causes a decrease in heart rate, increases the secretion of glands (salivary, bronchial, sweat and gastrointestinal tract) and contributes to the development of hypersalivation, bronchorrhea, increased acidity of gastric juice, constricts the pupil, causes a spasm of accommodation, reduces intraocular pressure, increases the tone of intestinal smooth muscles (increases peristalsis and relaxes sphincters ) and bladder, causes bronchospasm, tones skeletal muscles.

Pharmacokinetics

Being a quaternary ammonium base, it penetrates poorly through the BBB and does not have a central effect. Bioavailability - 1-2%. With the / m administration of TCmax - 30 minutes. Communication with plasma proteins - 15-25%. T1 / 2 when taken orally - 52 minutes, intramuscularly - 51-90 minutes, intravenously - 53 minutes. Metabolism - in the liver with the formation of inactive metabolites. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% are unchanged and 30% are in the form of metabolites).

Indications

Myasthenia gravis, movement disorders after brain injury, paralysis, recovery period after meningitis, poliomyelitis, encephalitis, weakness of labor activity (rarely), open-angle glaucoma, optic nerve atrophy, neuritis; atony of the gastrointestinal tract, atony of the bladder. Elimination of residual disorders of neuromuscular transmission with non-depolarizing muscle relaxants.

Dosing regimen

Prozerin accept inside, 30 minutes before meals, adults - 10-15 mg 2-3 times a day, the maximum single dose - 15 mg, daily - 50 mg; children - preferably in the form of granules (before use, dissolve in warm boiled water to the mark "100 ml", obtaining a solution of 0.02% concentration with a content of 5 ml of solution - 1 mg), up to 10 years - 1 mg per 1 year of life per day , older than 10 years - up to 10 mg / day (no more).

PC: adults - 0.5-1-2 mg (0.5 mg - 1 ml of a 0.05% solution) 1-2 times a day, the maximum single dose is 2 mg, daily - 6 mg; children (only in a hospital setting) - 0.05 mg (0.1 ml of a 0.05% solution) for 1 year of life per day, but not more than 3.75 mg (0.75 ml of a 0.05% solution) per 1 injection. 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 during the daytime, when the patient is most fatigued. With myasthenia gravis, 15 mg orally and s / c or 0.5 mg / m per day are prescribed; the course of treatment is long, with a change in the route of administration. With myasthenic crisis (with difficulty breathing and swallowing) - adults 0.5-1 ml of a 0.05% solution in / in, then s / c, at short intervals. With postoperative atony of the intestines, bladder: for prevention, incl. postoperative urinary retention, - s / c or / m, 0.25 mg, as soon as possible after surgery, and again - every 4-6 hours for 3-4 days; treatment of urinary retention - s / c or / m 0.5 mg; if urine does not pass within 1 hour, catheterization is performed and after emptying the bladder, it is administered every 3 hours, a total of 5 injections. To reduce intraocular pressure, 1-2 drops of a 0.5% solution are instilled into the conjunctival sac 1-4 times a day. With weakness of labor activity - inside 3 mg 4-6 times a day with an interval of 40 minutes or s / c - 1 ml of a 0.05% solution 1-2 times with an interval of 1 hour (in combination with 1 ml of a 0.1% solution of atropine sulfate, p /k once, against the background of the first injection). As an antidote for muscle relaxants (after the preliminary administration of atropine sulfate at a dose of 0.6-1.2 mg IV, until the pulse increases to 80 beats / min), 0.5-2 mg IV is slowly administered after 1/2-2 minutes. If necessary, injections are repeated (including atropine in case of bradycardia) in a total dose of not more than 5-6 mg (10-12 ml) for 20-30 minutes; during the procedure provide good ventilation of the lungs.

Contraindications

Hypersensitivity, epilepsy, hyperkinesis, vagotomy, ischemic heart disease, bradycardia, arrhythmias, angina pectoris, bronchial asthma, severe atherosclerosis, hyperthyroidism, peptic ulcer of the stomach and duodenum, peritonitis, mechanical obstruction of the gastrointestinal tract and urinary tract, prostate adenoma, period of acute illness, intoxication in sharply weakened children, pregnancy, lactation.

Side effects

Hypersalivation, spastic contraction and increased intestinal motility, nausea, vomiting, flatulence, diarrhea; headache, dizziness, weakness, loss of consciousness, drowsiness; miosis, visual disturbances, arrhythmias, bradycardia or tachycardia, AV blockade, junctional rhythm, nonspecific ECG changes, cardiac arrest, decrease in blood pressure (mainly with parenteral administration), shortness of breath, respiratory depression up to stop, bronchospasm, tremor, spasms and twitching skeletal muscles, including fasciculations of the muscles of the tongue, convulsions, dysarthria, arthralgia; increased urination; profuse sweating; allergic reactions (facial redness, rash, itching, anaphylaxis). Overdose. Symptoms: associated with overexcitation of cholinergic receptors (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased peristalsis, diarrhea, frequent urination, twitching of the muscles of the tongue and skeletal muscles, gradual development of general weakness, decrease in blood pressure. Treatment: reduce the dose or stop treatment, if necessary, introduce atropine (1 ml of a 0.1% solution), metacin and other anticholinergic drugs.

special instructions

With parenteral administration of large doses, it is necessary (preliminary or simultaneous) administration of atropine. If a myasthenic (with insufficient therapeutic dose) or cholinergic (due to overdose) crisis occurs during treatment, careful differential diagnosis is required due to the similarity of symptoms.

drug interaction

When myasthenia gravis is prescribed in combination with aldosterone antagonists, corticosteroids and anabolic hormones. Atropine, metacin, etc. M-anticholinergics weaken M-cholinomimetic effects (pupil constriction, bradycardia, increased gastrointestinal motility, hypersalivation, etc.). Lengthens and enhances (with parenteral administration) the effect of depolarizing muscle relaxants (ditilin, etc.); weakens or eliminates - antidepolarizing. It is prescribed with caution against the background of anticholinergics, in children (with myasthenia gravis) against the background of neomycin, streptomycin, kanamycin and other antibiotics that have an antidepolarizing effect, local and some general anesthetics, antiarrhythmics and a number of other drugs that disrupt cholinergic transmission.

Terms and conditions of storage

List A .: In a dry, dark place, at a temperature of 15-25 ° C. Shelf life 2 years.

Instructions for use:

Prozerin is a synthetic cholinesterase inhibitor that restores neuromuscular conduction, slows down the heart rate, increases the secretion of glands (salivary, gastrointestinal tract, sweat and bronchial), increases the acidity of gastric juice, constricts the pupil, causing spasm of accommodation, reducing intraocular pressure, increasing smooth muscle tone and bladder, causing bronchospasm, toning skeletal muscles.

Release form and composition

Tablets: flat-cylindrical, white, with a chamfer (10 pieces in blister packs, 2 packs in a carton pack);
Solution for injection: a colorless transparent liquid (1 ml in neutral glass ampoules, 10 ampoules with an ampoule knife or a scarifier in a carton pack, or 5 or 10 ampoules in a blister pack, 1 or 2 packs with an ampoule knife or a scarifier in a carton pack; if ampoules with a break point or a break ring are used, the ampoule knife / scarifier is not included in the package);
Solution for intravenous (in / in) and subcutaneous (s / c) administration: colorless transparent liquid (1 ml in ampoules, 10 ampoules with an ampoule scarifier in a carton pack or 5 ampoules in blister packs, 2 packs with an ampoule scarifier in a cardboard pack).

The active substance is neostigmine methyl sulfate (prozerin):

1 tablet - 15 mg;
1 ml solution for injection - 0.5 mg;
1 ml solution for intravenous and s / c administration - 0.5 mg.

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

Additional substance of injection solutions: water for injections.

Indications for use

For all dosage forms of Prozerin:

Myasthenia gravis;
Paralysis;
Movement disorders after brain injury;
The recovery period after suffering encephalitis, poliomyelitis, meningitis.

Additionally for injection solutions:

Atony of the gastrointestinal tract and bladder (prevention and treatment);
Neuritis;
Weakness of labor activity (for stimulation);
Muscle weakness and respiratory depression (as an antidote after anesthesia with non-depolarizing muscle relaxants);
Atrophy of the optic nerve.

Contraindications

For all dosage forms:

Epilepsy;
arrhythmias;
bradycardia;
angina;
Cardiac ischemia;
Vagotomy;
Severe atherosclerosis;
Hyperkinesis;
thyrotoxicosis;
Bronchial asthma;
Infectious diseases in the acute period;
Hyperplasia of the prostate;
Mechanical obstruction of the gastrointestinal tract and urinary tract;
Peritonitis;
Peptic ulcer of the stomach and duodenum;
Pregnancy;
Lactation;
Hypersensitivity to the components of the drug.

Additionally for tablets:

Sucrase / isomaltase deficiency, glucose-galactose malabsorption, fructose intolerance;
Age up to 18 years.

Method of application and dosage

In tablet form, Prozerin is prescribed orally (half an hour before meals), in the form of a solution for injection - administered subcutaneously, intramuscularly or intravenously, in the form of a solution for intravenous and s / c administration - intravenously or subcutaneously.

Myasthenia gravis: a single dose inside - 15 mg, daily - 50 mg. The treatment of the disease is long (25-30 days) with a change in the ways of using the drug, most of the daily dose in the form of tablets is prescribed in the daytime, when the patient is most tired. In myasthenic crisis in adults, Prozerin is administered intravenously (with a solution of sodium chloride 0.9%) at a dose of 0.25-0.5 mg, then subcutaneously in normal doses with short interruptions. To enhance the effect of the drug, if necessary, additionally injected s / c solution of ephedrine 5% (1 ml);
Movement disorders due to injuries of the central nervous system, encephalitis and meningitis, with paralysis of the facial nerve: inside 15 mg 1-2 times a day for 2-3 weeks;
Movement disorders due to poliomyelitis (in combination with physiotherapy, therapeutic exercises, balneological treatment and other measures): inside, 15 mg 1 time per day, daily or every other day. The course of treatment consists of 15-20 doses. Repeated courses are carried out at intervals of 2-3 months;
Stimulation of labor: s / c at a dose of 0.5 mg, if necessary, after 1 hour, the introduction is repeated. With the first dose, 1 mg of a 0.1% solution of atropine s / c is administered once;
Stopping the action of non-depolarizing muscle relaxants: first, atropine is administered intravenously at a dose of 0.5-0.7 mg, after 1-2 minutes (when the pulse becomes more frequent), 1.5 mg Prozerin is administered intravenously. If the effect is insufficient, repeated doses are administered, but not more than 5-6 mg of neostigmine methyl sulfate for 20-30 minutes. During the procedure, ensure adequate ventilation of the lungs;
Prevention of postoperative atony of the intestines and bladder (including postoperative urinary retention): s / c or / m at a dose of 0.25 mg as soon as possible after surgery, then every 4-6 hours at the same dose for 3 days ;
Treatment of urinary retention: s / c or / m at a dose of 0.5 mg. If diuresis is not restored within 1 hour, catheterization is performed to empty the bladder. Further, the drug is administered every 3 hours, in total - 5 injections.

For children, the drug is prescribed only for myasthenia gravis, treatment is carried out exclusively in a hospital. The drug is administered s / c or / m at a dose of 0.05 mg per 1 year of life per day, but not more than 0.375 mg per 1 injection. As a rule, the daily dose is administered once, but if necessary, it can be divided into 2-3 injections.

Side effects

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): bradycardia, arrhythmia, tachycardia, junctional rhythm, atrioventricular blockade, syncope, nonspecific changes in the electrocardiogram, lowering blood pressure (mainly with parenteral administration), cardiac arrest;
From the nervous system and sensory organs: weakness, drowsiness, loss of consciousness, headache, vertigo, dysarthria, blurred vision, miosis, convulsions;
From the respiratory system: shortness of breath, increased bronchial and pharyngeal secretion, bronchospasm (mainly with parenteral administration), respiratory depression until it stops;
From the digestive system: flatulence, nausea, vomiting, diarrhea, spastic contraction and increased intestinal motility, hypersalivation;
Allergic reactions: rash, itching, flushing of the face, anaphylaxis;
Other: spasms and twitches of skeletal muscles (including fasciculations of the muscles of the tongue), tremor, arthralgia, convulsions, profuse sweating, increased urination.

To remove side effects, reduce the dose of Prozerin or stop its use. If the need arises, methocinium iodide, a 0.1% solution of atropine or other anticholinergics are administered.

special instructions

During treatment, care should be taken when driving a car and performing work that requires speed of reactions and increased attention.

If during therapy a myasthenic or cholinergic crisis occurs (due to insufficient therapeutic dose or overdose, respectively), a thorough differential diagnosis should be carried out due to the similarity of symptoms.

drug interaction

With myasthenia, Prozerin is prescribed in combination with anabolic hormones and glucocorticosteroids.

Novocainamide, quinidine, local anesthetics, ganglioblockers (pachycarpine hydroiodide), m-anticholinergics (including homatropine hydrobromide, metocinium iodide, platifillin and atropine) weaken the m-cholinomimetic effects of the drug (they are its pharmacological antagonists), which is manifested by increased gastrointestinal motility tract, hypersalivation, pupillary constriction, bradycardia, etc.

With caution, Prozerin should be used simultaneously with cholinergic blockers, in patients with myasthenia gravis - simultaneously with kanamycin, neomycin, streptomycin and other antibiotics that have an antidepolarizing effect, as well as with antiarrhythmic drugs, local anesthetics, general anesthesia and other drugs that disrupt cholinergic transmission.

Neostigmine methyl sulfate is an antagonist of non-depolarizing muscle relaxants (including tubocurarine chloride, rocuronium bromide, atracurium besylate), restoring neuromuscular conduction. In those cases when, after the end of anesthesia with the use of non-depolarizing muscle relaxants, muscle weakness and respiratory depression persist, Prozerin is used as an antidote for these agents.

Prozerin is pharmacologically incompatible with depolarizing muscle relaxants (for example, suxamethonium iodide).

Used in large doses, cyanocobalamin weakens the effect of neostigmine methyl sulfate.

Prozerin reduces the activity of pyridoxine.

Like all cholinesterase inhibitors, Prozerin in combination with laxatives enhances their effect, with strychnine - significantly increases the tone of the vagus nerve.

Antiarrhythmic drugs (β-blockers) and neostigmine methyl sulfate are synergists (bradycardia worsens).

Prozerin goes well: with cardiovascular disorders - with nikethamide, with neuritis - with thiamine, with muscular dystrophies - with calcium gluconate and adenosine triphosphate.

Ephedrine potentiates the action of neostigmine methyl sulfate, so it is administered together with Prozerin in myasthenic crises.

Analogues

Analogues of Prozerin are: Prozerin-Darnitsa, Neostigmine methyl sulfate, Ubretide, Armin, Amiridin, Oksazil, Deoxypeganine hydrochloride.

Terms and conditions of storage

Store in a dry, dark place out of the reach of children.

Best before date:

Tablets - 5 years at temperatures up to 25 ° C;
Solution for injection - 4 years at a temperature of 15-25 ºС;
Solution for intravenous and s / c administration - 4 years at a temperature of 18-25 ºС.

pharmachologic effect

Acetylcholinesterase and pseudocholinesterase inhibitor. It has an indirect cholinomimetic effect due to reversible inhibition of cholinesterase and potentiation of the action of endogenous acetylcholine. It improves neuromuscular transmission, enhances gastrointestinal motility, increases the tone of the bladder, bronchi, and secretion of exocrine glands. Causes bradycardia, lowering blood pressure. Constricts the pupil, lowers intraocular pressure, causes a spasm of accommodation.

Pharmacokinetics

After parenteral administration of neostigmine, methyl sulfate undergoes hydrolysis and is also metabolized in the liver to form inactive metabolites. Plasma protein binding is 15-25%. It is excreted in the urine (80% within 24 hours) in the form of unchanged substance (about 50%) and metabolites. Poorly penetrates through the BBB.

Indications

Myasthenia gravis and myasthenic syndrome, movement disorders after brain injury, paralysis, recovery period after meningitis, poliomyelitis, encephalitis; weakness of labor activity (rarely); atrophy of the optic nerve, neuritis; atony of the stomach, intestines and bladder.

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

In ophthalmology: to narrow the pupil and lower intraocular pressure in open-angle glaucoma.

Dosing regimen

Inside adults - 10-15 mg 2-3 times / day; s / c - 1-2 mg 1-2 times / day.

Inside children under 10 years old - 1 mg / day for 1 year of life; for children over 10 years of age, the maximum dose is 10 mg. S / c dose is calculated at 50 mcg for 1 year of life, but not more than 375 mcg per injection.

In ophthalmology: injected into the conjunctival sac 1-4 times / day.

Maximum doses: for adults, when taken orally, a single dose is 15 mg, daily - 50 mg; with s / c administration, a single dose is 2 mg, a daily dose is 6 mg.

Side effect

From the digestive system: nausea, vomiting, diarrhea, hypersalivation, flatulence, spastic contraction and increased peristalsis.

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

From the side of the cardiovascular system: arrhythmias, brady- or tachycardia, AV blockade, junctional rhythm, non-specific ECG changes, lowering blood pressure.

From the respiratory system: shortness of breath, respiratory depression, increased secretion of bronchial glands, increased bronchial tone.

Allergic reactions: possible skin rash, itching, flushing of the face, anaphylactic reactions.

Others: arthralgia, increased urination, increased sweating.

Contraindications for use

Epilepsy, hyperkinesis, vagotomy, bronchial asthma, ischemic heart disease (including angina pectoris), arrhythmias, bradycardia, severe atherosclerosis, thyrotoxicosis, peptic ulcer of the stomach and duodenum, peritonitis, mechanical obstruction of the gastrointestinal tract or urinary tract, prostatic hyperplasia, acute infectious diseases, intoxication in debilitated children, hypersensitivity to neostigmine methyl sulfate.

Use during pregnancy and lactation

Neostigmine methyl sulfate crosses the placental barrier and is excreted in breast milk in very small amounts.

During pregnancy and lactation, use only according to strict indications.

Use in children

Application is possible according to the dosing regimen.

drug interaction

Neostigmine methyl sulfate is an antagonist of non-depolarizing muscle relaxants and, when used simultaneously, enhances the effect of depolarizing muscle relaxants.

With the simultaneous use of m-anticholinergics, ganglioblockers, quinidine, novocainamide, local anesthetics, tricyclic antidepressants, antiepileptic and antiparkinsonian drugs reduce the effect of neostigmine methyl sulfate.

Ephedrine potentiates the action of neostigmine methyl sulfate.

With the simultaneous use of neostigmine methyl sulfate with beta-blockers, bradycardia may increase.

special instructions

Use with caution in Addison's disease.

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

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

Influence on the ability to drive vehicles and control mechanisms

During the period of treatment, one should refrain from driving vehicles and other potentially hazardous activities that require concentration of attention and a high speed of psychomotor reactions.