Prezero instructions for use. Prezero - instructions for use, composition, form of release, readings, side effects, analogues and price

Transparent colorless liquid;

pharmachologic effect

Prezero - synthetic cholinesterase blocker reversible action. It has a high affinity for acetylcholinesterase, which is due to its structural identity with acetylcholine. Like acetylcholine, the prozero initially interacts with the catalytic center of Holinesterase, but in the future, in contrast to acetylcholine, it forms, due to its carbamine group, a stable connection to the enzyme. The enzyme is temporarily (from several minutes to several hours) loses its specific activity. At the end of this time, due to the slow hydrolysis of prozer, cholinesterase is released from the blocker and restores its activity. Such an action leads to accumulation and strengthening of acetylcholine in cholinergic synapses. Prezero has a pronounced muscarinic and nicotine effect, it is capable of directly exciting to influence skeletal muscles.

Causes a reduction in heart rate, increases the secretion of the excretory glands (salivary, bronchial, sweat and gastrointestinal tract) and promotes the development of hypersion, bronchio breeding, increasing the acidity of gastric juice, narrows the pupil, causes an accommodation spasm, reduces intraocular pressure, increases the tone of the intestinal muscles (enhances the peristaltics and relaxes the sphincters) and the bladder, causes the bronchi spasm, tones the skeletal muscles.

Pharmacokinetics

Prezero, being a quaternary ammonium base, penetrates poorly through the hematopoid-encephalotic barrier and does not have a central action. Bioavailability in parenteral administration is high, 0.5 mg of prozermina introduced parenterally, corresponds to 15 mg, taken inside. With an increase in the dose of the drug, bioavailability increases, with intramuscular administration, the time to achieve maximum concentration in the blood is 30 minutes. Communication with proteins (albumin) plasma -15-25%. The half-life (T] #) period with intramuscular administration - 51 - 90 minutes, with intravenous administration - 53 minutes. Metabolized in two ways. Due to hydrolysis at a place of compound with cholinesterase and microsomal liver enzymes. Inactive metabolites are formed in the liver. 80% of the administered dose is derived by the kidneys within 24 hours (of which 50% is unchanged and 30% in the form of metabolites).

Indications for use

Miasthenia, acute miasthenic crisis. Atony of the gastrointestinal tract, atony of the bladder. Elimination of residual phenomena after the blockade of neuromuscular transmission non-polarizing muscle relaxants.

Contraindications

Increased sensitivity to the components of the drug. Epilepsy, hypercines, wagotomy, ischemic heart disease, angina, arrhythmia, bradycardia, bronchial asthma, pronounced atherosclerosis, thyrotoxicosis, ulcerative ulcerative disease of the stomach and duodenum, peritonitis, mechanical obstruction of the gastrointestinal tract and urinary tract, prostate hypertrophy, accompanied by weathered urination , acute period of infectious disease, intoxication in highly weakened children. During pregnancy and breastfeeding. Do not assign simultaneously with antide -olarizing muscle relaxants, for example, succinylcholine.

Pregnancy and lactation period

During pregnancy, the drug is contraindicated.

If necessary, the use of the drug during lactation, breastfeeding must be stopped.

Method of application and dose

Adults prescribe the drug subcutaneously, intramuscularly and intravenously. Subcutaneously adults - 0.5 - 2 mg (1-4 ml) 1 - 2 times a day. Maximum one-time dose for adults - 2 mg, daily - 6 mg. The course of treatment (except for Miasthenia) - 25 - 30 days, if necessary, re-in 3-4 weeks. Most of the total daily dose is prescribed during the day when the patient is largely fatigue.

For miastic, adults subcutaneously or intramuscularly 0.5 mg (1 ml of 0.05% solution) per day. The course of treatment is long, with the change of way of administration.

With a miasthenic crisis (with difficulty breathing and swallowing) - adults 0.5 - 1 ml of 0.05% solution intravenously, in the future subcutaneously, with small intervals.

Under postoperative intestinal atony, bladder: for prophylaxis, including postoperative urine delay, - subcutaneously or intramuscularly, 0.25 mg (0.5 ml of 0.05% solution), as early as possible after the operation, and re-every 4-6 hours for 3-4 days.

As an antidote of the muscle relaxants (after the preliminary administration of atropine sulfate at a dose of 0.6 - 1.2 mg intravenously, to the increase in the pulse up to 80 ° C.) to enter 0.5 - 2 min 0.5 - 2 mg intravenously slowly. If necessary, injection is repeated (including atropine in the case of bradycardia) in a total dose of no more than 5-6mg (10 - 12 ml) for 20-30 minutes; During the procedure, artificial ventilation of the lungs are provided.

Children subcutaneously (in hospital conditions) - 0.05 mg (0.1 ml of 0.05% solution) for 1 year of life, but not more than 0.375 mg (0.75 ml of 0.05% solution) for 1 injection.

Side effect

From the gastrointestinal tract: spastic reduction and strengthening of the peristaltics of the gastrointestinal tract, flatulence, diarrhea, nausea, vomiting.

On the part of the central nervous system and the peripheral nervous system: headache, dizziness, general weakness, loss of consciousness, drowsiness, convulsions, dysrtarium, mios, tremor, spasms and twitching muscles of skeletal muscles and muscles of the language, the increase in urinary, redness of the face, hypersivation.

From the side of the cardiovascular system: arterial hypotension, violation of the heart rate in the form of tachy and bradycardia, an atrioventricular blockade of the nodal rhythm, extrasystole arrhythmia, a sudden stop of the heart.

The side effect of the drug is mainly due to the M-cholinomimetic action of the prozer.

From the side of the respiratory system: the strengthening of the secretion of the Faringent and bronchial glands, shortness of breath, bronchospasm, the oppression of breathing up to his stop.

When using the drug, the development of allergic reactions in the form of a skin, rashes and other manifestations of allergies to anaphylactic shock is possible.

To eliminate side effects, the dose of the drug reduce or stop its use. If necessary, atropine, metacin and other cholinolithic agents are introduced.

From the side of the skin and subcutaneous fiber: hyperhydrosis.

From the side of the muscular, connective tissue: muscle spasms.

From the side of the kidneys and urinary tract: urinary incontinence.

Overdose

Symptoms: associated with the overexcixation of cholinaroreceptors (cholinergic crisis): bradycardia, hypersalization, miosis, bronchospasm, nausea, strengthening of peristaltics, diarrhea, strengthening of urination, twitching muscle muscles and skeletal muscles, gradual development of general weakness, reduction of blood pressure.

Treatment: Dose reduce or cancel the drug. If necessary, atropine is administered (1 ml of 0.1% solution), metacin. Therapy is symptomatic.

Interaction with other medicines

During myasthenia, they are prescribed in combination with aldosterone antagonists, glucocorticosteroids and anabolic hormones. Atropine, metacin and other Mgroblockers weaken M-cholinomimetic effects. Prolongs and strengthens the influence of depolarizing muscle relaxants, is succumbing or eliminating - antide-polarizing. Caution is prescribed simultaneously with neomycin, streptomycin, kanamycin, which have an antihasipeolarizing effect. Sharing with local and some general anesthetics, antiarrhythmic drugs that violate the cholinergic transmission can lead to the weakening of the effects of prozer. Organic nitrates reduce the effectiveness of the prozer.

Ephedrine will potentiate the action of the prozer.

With the simultaneous use of prozero with beta-adrenoblockers, bradycardia is possible.

Prezero should not be prescribed during anesthesia using cyclopropane or halotan, although after the end of the anasthesia it can be used.

Easily destroyed by alkalis and oxidizing agents.

Instructions for use:

Prezero - synthetic cholinesterase inhibitor, regenerating neuromuscular conductivity, reducing heart rate, increases secretion of the glands (salivary, gastrointestinal tract, sweat and bronchial), which increases the acidity of gastric juice, a narrowing pupil, causing accommodation spasmodes that reduces intraocular pressure, enhancing The tone of the smooth muscles and bladder, which causes the spasm of bronchi, tonic skeletal muscles.

Release form and composition

• Tablets: plane-cylindrical shape, white, with a chamfer (10 pcs. In contour cellular packs, 2 packs in a pack of cardboard);
• Injection solution: Colorless transparent liquid (1 ml in ampoules of neutral glass, 10 ampoules with an ampumen knife or scarifier in a cardboard pack or 5 or 10 ampoules in the contour cellular packaging, 1 or 2 packs with an ampumen knife or scarifier in a pack of cardboard; If the ampoules are used with a dummy point or a ring of an ampumen knife / scarifier in the package not invested);
• Solution for intravenous (in / c) and subcutaneous (n / c) administration: colorless transparent liquid (1 ml in ampoules, 10 ampoules with an ampumen scarifier in a pack of cardboard or 5 ampoules in contour cellular packs, 2 packs with ampumen Scarifier in a pack of cardboard).

Active substance - Neostigmin Methylsulfate (prozerne):

• 1 tablet - 15 mg;
• 1 ml of injection solution - 0.5 mg;
• 1 ml of solution for V / B and p / k administration is 0.5 mg.

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

Additional substance of injection solutions: water for injection.

Indications for use

For all dosage forms of Poszero:

• Miastic gravis;
• Paralysis;
• Motor disorders after the injury of the brain;
• Recovery period after transferred encephalitis, polio, meningitis.

Additionally for injection solutions:

• Atony of the gastrointestinal tract and bladder (prevention and treatment);
• Neuritis;
• Weakness of labor activities (for stimulation);
• Muscular weakness and respiratory depression (as an antidote after anesthesia using non-polarizing muscle relaxants);
• Atrophy of the optic nerve.

Contraindications

For all dosage forms:

• Epilepsy;
• Arrhythmias;
• Bradycardia;
• Angina;
• Coronary artery disease;
• Wagotomy;
• Pronounced atherosclerosis;
• Hypercines;
• Thyrotoxicosis;
• Bronchial asthma;
• Infectious diseases in the acute period;
• Prostate hyperplasia;
• Mechanical obstruction of the gastrointestinal tract and urinary tract;
• Peritonitis;
• Ulcerative ulcer of the stomach and a 12-rosewoman;
• Pregnancy;
• Lactation;
• Hypersensitivity to the components of the drug.

Additionally for tablets:

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

Method of application and dosage

In the tablet form, the prozero is prescribed inside (half an hour before meals), in the form of a solution for injections - is administered subcutaneously, intramuscularly or intravenously, in the form of a solution for V / B and n / k administration - intravenously or subcutaneously.

• Miasthenia: one-time dose - 15 mg, daily - 50 mg. Treatment of the disease is long (25-30 days) with the change of ways to use the drug, most of the daily dose in the form of tablets is prescribed during the daytime, when the patient is most of fatigue. In the miasthenic crisis in adults, the prozero is administered intravenously (with a solution of chloride sodium 0.9%) at a dose of 0.25-0.5 mg, then subcutaneously in ordinary doses with minor interruptions. To enhance the effect of the drug, if necessary, additionally introduced a p / to Ephedrine solution 5% (1 ml);
• Motor disorders due to injuries of the central nervous system, encephalitis and meningitis, with paralymps of the facial nerve: inward 15 mg 1-2 times a day for 2-3 weeks;
• Motor disorders due to poliomyelitis (in a complex with physiotherapy, medical gymnastics, balneological treatment and other activities): inward 15 mg 1 time per day daily or every other day. The course of treatment consists of 15-20 doses. At intervals of 2-3 months conduct repeated courses;
• Stimulating delivery: p / k in a dose of 0.5 mg, if necessary, after 1 hour, the introduction repeat. With the first dose, 1 mg of 0.1% of the atropine p / k solution is once again injected;
• The relief of the action of non-polarizing minelaxants: Atopin in / c at a dose of 0.5-0.7 mg, after 1-2 minutes (when the pulse is frequent), 1,5 mg of prozerminas are entered. In case of insufficiency, repeated doses are introduced, but not more than 5-6 mg of neostigmine methyl sulfate for 20-30 minutes. During the procedure, adequate pulmonary ventilation;
• Prevention of postoperative intestinal and bladder atony (including postoperative urine delay): P / C or V / m in a dose of 0.25 mg as early as possible after the operation, then - every 4-6 hours in the same dose for 3 days ;
• Treatment of urine delay: p / k or in / m at a dose of 0.5 mg. If for 1 hour diuresis is not restored, make catheterization for emptying the bladder. The drug is introduced every 3 hours, only 5 injections.

Children are prescribed the drug only during the Miastic gravis, the treatment is carried out exclusively in the hospital. The drug is administered by P / C or V / 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 introduced once, but if necessary, can be divided into 2-3 injections.

Side effects

• From the side of the cardiovascular system and blood (blood formation, hemostasis): bradycardia, arrhythmia, tachycardia, nodal rhythm, atrioventricular blockade, syncope, nonspecific changes in the electrocardiogram, reduced blood pressure (mainly in parenteral administration), stopping the heart;
• From the side of the nervous system and the senses: weakness, drowsiness, loss of consciousness, headache, vertigo, dysarthria, vision, mios, convulsions;
• From the side of the respiratory system: shortness of breath, strengthening of bronchial and pharyget secretion, bronchospasm (mainly under parenteral administration), inhibition of breathing up to the stop;
• From the digestive system: flatulence, nausea, vomiting, diarrhea, spastic abbreviation and enhancement of intestinal peristalsis, hypersalization;
• Allergic reactions: rash, itching, face hyperemia, anaphylaxia;
• Others: Spasms and twitching skeletal muscles (including the muscles of the muscles of the tongue), tremor, arthralgia, convulsions, abundant sweating, the increase in urination.

To remove side effects, reduce the dose of prozerne or stop its use. If there is a need to introduce the iodide metocycy, 0.1% solution of atropine or other cholinoblocators.

special instructions

During treatment, caution should be taken when driving a car and performing work requiring the speed of reactions and increased attention.

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

Medicinal interaction

During myasthenia, prozerne is prescribed in combination with anabolic hormones and glucocorticosteroids.

Novocainamide, County, local anesthetics, gangliplockers (patchicardine hydroeodyid), M-cholinoblocators (including homatropine Hydrobromide, iodide metocycy, platiphyllin and atropine) weaken the M-cholinomimetic effects of the drug (are its pharmacological antagonists), which is manifested by the gain of the gastrointestinal motility tract, hypersalization, narrowing of pupil, bradycardia, etc.

With caution, prozero should be used simultaneously with the cholinblocators, in patients with miastenia - simultaneously with Canamycin, neomycin, streptomycin and other antibiotics, which have an antide-polarizing effect, as well as antiarrhythmic drugs, local anesthetics, means for general anesthesia and other drugs that violate the cholinergic drugs. Transmission.

Neostigmine methyl sulfate is an antagonist of non-polarizing minelaxants (including chloride tubaurine, bromide rocuroneonia, atrakuria flavored), restoring neuromuscular conductivity. In cases where, after the end of the anesthesia, the muscle weakness and oppression of breathing are preserved, the prozero is used as an antidote of these tools.

Prezero pharmacologically incompatible with depolarizing muscle relaxants (for example, suucamenia iodide).

The cyanocobalamin applied in large doses weakens the action of the neostigmine methyl sulfate.

Prezero reduces pyridoxine activity.

Like all cholinesterase inhibitors, prozerne in combination with laxatives enhances their action, with strikhnin - significantly increases the tone of the wandering nerve.

Antichardimical preparations (β-adrenoblays) and neostigmine methyl sulfate are synergists (bradycardia aggravated).

Prezero is well combined: with cardiovascular disorders - with nickelamide, with neuritis - with thiamine, with muscle dystrophy - with calcium gluconate and adenosineryphosphate.

The ephedrine potenties the action of the neostigmine of methyl sulfate, therefore it is administered together with the prozero in miasthenic crises.

Analogs

Prezero counterparts are: Prezeroga-Darnitsa, Neostigmin methylsulfate, ulitid, armimine, amyridine, oxazil, deoxypeganine hydrochloride.

Terms and conditions of storage

Store in a dry, dark, inaccessible for children.

Shelf life:

• Tablets - 5 years at temperatures up to 25 ° C;
• A solution for injection - 4 years at a temperature of 15-25 ºС;
• The solution for V / B and P / k administration is 4 years at a temperature of 18-25 ºС.

Content

Prezernum preparation (Proserinum) refers to synthetic cholinesterase inhibitors. He finds use in the treatment of diseases of the nervous system. The active substance of the composition is neostigmine methyl sulfate. The medication is produced by domestic pharmaceutical companies. Check out his application instructions, learn about the analogues.

Composition and form of release

Prezero is a drug that have two forms of release. These are oral tablets and parenteral solution:

Mechanism of action of Poszerne

The active component of the composition is an inhibitor of acetylcholinesterase and pseudocholinesterase. The substance has indirect cholinomimetic effects, the effect of endogenous acetylcholine potentiates. Neostigmin increases the transmission between the cells of the nervous and muscle tissue, enhances the motorcycle of the digestive tract, improves the tone of the smooth muscle muscles of the bronchi and the bladder.

Reception of the drug may cause bradycardia, lowering arterial and intraocular pressure, mydriasis (narrowing of the pupil), the appearance of spasmodation spasmodation. If we take a large dose of the medication, acetylcholine will accumulate, which will lead to a violation of neuromuscular conductivity.

The tool excites the cholinergic nerves, does not have a central action and influence on the heart. After taking inside or administration, parenterally neostigmin is hydrolyzed in the liver, after metabolism, inactive metabolites are formed. The substance is binding to plasma proteins by 20%, is excreted in the kidneys. 80% of the components are excreted from the body per day, 50% of the dose form metabolites. Neostigmin penetrates badly through the brain-shell barrier.

Indications for use of prozer

Prezero is a widely active drug, so the spectrum of its testimony to use is large. The instruction allocates the following:

• miasthenia, Miasthenic syndrome;
• atrophy of the optic nerve;
• disorders of the motor system after brain injury;
• weakness of labor activities;
• paralysis;
• recovery after meningitis, polio, encephalitis;
• neuritis;
• elimination of residual transmission disorders between nerves and muscles nonpolarizing muscle relaxants;
• intestinal atony, stomach or bladder;
• the narrowing of the pupil, an open-hearted glaucoma.

Method of application and dosage

Instructions for use of prozermina has a different appearance for each of the forms of drug release. Tablets are administered orally, the solution can be administered intravenously or subcutaneously. There is also a children's version of the medication - in the form of granules, which are bred by water, the resulting emulsion is accepted inside. The dosage and course of treatment depends on the severity of the disease, appointed by the doctor.

In tablets

Medication in tablet format is taken half an hour before meals. Adults are prescribed for 10-15 mg 2-3 times a day. The maximum single dose is 15 mg, daily - 50 mg of the drug. Children under 10 years old should be 1 mg for the year of life per day, older - 10 mg per day. The course of treatment lasts 25-30 days, after 3-4 weeks it can be continued. The maximum proportion of the dose taken during the day is used at the time of the greatest fatigue.

With weakness of labor, they take 3 mg 4-6 times a day every 40 minutes. With violations of motor activity after injuries of the brain, encephalitis, meningitis, paralysis is taken inside 15 mg 1-2 times a day for 2-3 weeks. If the brain restoration is required after poliomyelitis, take 15 mg every day or every other day 15-20 doses.

In injections

Injections of the solution are administered subcutaneously or intramuscularly. To prevent the atony of the bladder, the intestines caused by surgical interventions, 0.25 mg of the drug is subcutaneously or intramuscularly administered, then the dosage is repeated every 4-6 hours for three days. 0.5 mg of prozerne is introduced for the treatment of urine delay.

If after an hour diuresis does not come back to normal, the instruction advises to make catheterization. Then the prozerne in ampoules is used every 3 hours, five injections are used. For children, the medicine is administered subcutaneously or intramuscularly to treat Miasthenia gravis (GRAVIS) - in a dosage of 0.05 mg per year of life per day, a maximum of 0.375 mg at a time. The daily dose is introduced once or for 2-3 injections. In ophthalmology, the solution can be introduced into the cavity of the eye 1-4 times a day.

Solution for in / in and p / k administration

In the miasthenic crisis, the prozero is administered intravenously at a dose of 0.2-0.5 mg in combination with a physiological solution of 0.9%, then subcutaneously. If it is required to increase the effect of the drug, 1 ml of 5% ephedrine is additionally injected subcutaneously. 0.5 mg is administered subcutaneously to stimulate birth, each hour is repeated. At the first dose of the prozerne additionally introduced atropine.

If you need to stop the action of Miorolaksanta, it is first intravenously administered 0.5-0.7 mg of atropine, when the pulse is frequent (this is about 1-2 minutes), the intravenously is already used by 1.5 mg of prozer. In the absence of effect, the dose is repeated, but not more than 5-6 mg of the neostigmine in 25 minutes. When performing the procedure, you need to provide ventilation of the lungs.

special instructions

Medication with caution is appointed with Addison's disease. High doses of the solution require a preliminary or simultaneous assignment of atropine. If the dose was insufficient or exceeded, miasthenic and cholinergic crises are developing. During treatment, the prozero instruction advises to refrain from managing transport or hazardous mechanisms.

Neostigmin can pass through the placenta and discovered in breast milk, so it can be used during the baby tooling and with breastfeeding (lactation) only by strict indications. For the treatment of children, it is better to use a granular drug or electrophoresis with a solution for injection. All procedures require a doctor control.

Medicinal interaction

Neostigmin refers to antagonists of nonpolarizing muscle relaxants, therefore, it may increase the action of depolarizing drugs of this group. With the simultaneous use of gangliplockers, Novocainamide, M-cholinoblockers of adenosinerphosphate, local anesthetics, quinidine, tricyclic antidepressants, anti-parkinsonic, anti-epileptic agents, drugs for anesthesia reduce the action of prozero. Its effect can potentiate ephedrine, and when combinations with β-adrenoblockers, bradycardia develops.

Side effects

Reception of prozero may be accompanied by side effects. Instructions for use allocates the following:

• spastic contraction of the muscles of the digestive tract, vomiting, flatulence, diarrhea;
• dysarthria, convulsions, dizziness, muscle twitch, weakness, visual impairment, drowsiness;
• reduction of pressure, arrhythmia, atrioventricular blockade, bradycardia, tachycardia;
• hypersion;
• dystrophy;
• disorders of the exocrine glands;
• hemostasis disorders;
• dyspnea;
• allergic reactions, anaphylaxis, skin rash, face hyperemia, itching;
• arthralgia;
• tremor;
• obstruction of the digestive tract;
• reduction of the secretion of thiamine;
• increase in the acidity of gastric juice;
• student urination;
• increased sweating.

Media overdose is manifested by excitation, bradycardia, bronchospasm, nausea, diarrhea. A person intensifies the intestinal peristalsis, urination is rapidly, a tongue is twisted, the pressure is reduced, the overall weakness develops. For the treatment of overdose, 1 ml of a 0.1% solution of atropine sulfate, metacine or other cholin-blocking preparations (M-cholinblocators) is introduced. Antidote to buy signs no.

Contraindications

The drug cannot be taken to certain groups of patients. The instruction highlights contraindications:

• epilepsy;
• bronchial asthma;
• hyperkines;
• wagotomy;
• ischemic heart disease, angina, arrhythmia, bradycardia;
• thyrotoxicosis;
• pronounced atherosclerosis;
• mechanical obstruction of the digestive tract;
• prostate hyperplasia;
• ulcer of the stomach, duodenum;
• peritonitis;
• acute infectious diseases;
• intoxication, the weakening of the state;
• increased sensitivity to composition components.

The preparation with caution is used in miastic in children, in the syndrome of Malabsorption isomaltase, against the background of taking anticholinergic drugs, neomycin, streptomycin, kanamycin, antibiotics with antide-polarizing effect, local and general anesthetics. Accuracy should be observed while simultaneously use of prozero with antiarrhythmic drugs, glucocorticosteroids, homochopine hormopic and drugs that violate the cholinergic transmission.

Terms for sale and storage

Poszerne is released by recipe, stored at temperatures up to 25 degrees. The shelf life of ampoules - 1.5 years, tablets can be used for five years from the date of manufacture.

Analogs

Replace the medicine can preparations based on the same current component or the other, but with a similar therapeutic effect. These include:

• Neostigmine methyl sulfate - direct analogue of the medicine, is its generic (cheaper at a price);
• Ulitid - anticholinesterase agent in the form of tablets and a solution based on a distigmine bromide or iodide;
• Armin - cholinomimetics for the treatment of glaucoma;
• Amyridine - tableted cholinomimetic, eliminating myasthenia;
• Oxazyl is a reversible cholinesterase inhibitor containing ambenonium chloride;
• Deoxipian hydrochloride or hydrobromide, sodium nichetamide is a reversible cholinesterase inhibitor.

PRICE POSORNA

You can purchase prozeros via online pharmacies or usual networks. The cost depends on the type of release, the volume of packaging and the level of trading charge. Approximate Moscow prices will be.

Medical Instructions

drug

Prezero

Tradename

Prezero

International non-proprietary title

Dosage form

Solution for injections, 0.5 mg / ml, 1 ml

Structure

1 ml of solution contains

active substance: Prezero in terms of 100% substance 0.5 mg;

auxiliary: water for injections

Description

Transparent colorless liquid

Pharmacotherapeutic group

Parasympathomimetics. Anticholinesterase preparations. Neostigmin. ATH code N07A A01

Pharmacological properties

Pharmacokinetics

Prezero, being a quaternary ammonium base, hesitantly penetrates through the hematorecephalic barrier and does not have a central action. Bioavailability in parenteral administration is high: 0.5 mg of prozermina, entered parenterally, corresponds to 15 mg, taken inside. With an increase in the dose of the drug, bioavailability increases. With intramuscular administration, the time to achieve maximum concentration in the blood is 30 minutes. Communication with proteins (albumin) plasma - 15 - 25%. The half-life (T 1/2) during intramuscular administration is 51 - 90 minutes, with intravenous administration - 53 minutes. Metabolized in two ways: due to hydrolysis at a place of compound with cholinesterase and microsomal liver enzymes. Inactive metabolites are formed in the liver. 80% of the administered dose is excreted by the kidneys within 24 hours (of which 50% are unchanged and 30% in the form of metabolites).

Pharmacodynamics

Prezero - synthetic cholinesterase blocker reversible action. It has a high affinity for acetylcholinesterase, which is due to its structural identity with acetylcholine. Like acetylcholine, prozerne interacts at the beginning with the catalytic center of cholinesterase, but in the future, unlike acetylcholine, it forms a stable connection with the enzyme due to its carbamine group. The enzyme is temporarily (from several minutes to several hours) loses its specific activity. At the end of this time, due to the slow hydrolysis of prozer, cholinesterase is released from the blocker and restores its activity. Such an action leads to accumulation and strengthening of acetylcholine in cholinergic synapses. Prezero has a pronounced muscarinic and nicotine effect, it is capable of directly exciting to influence skeletal muscles.

Causes a reduction in heart rate, increases the secretion of the excretory glands (salivary, bronchial, sweat and gastrointestinal tract) and contributes to the development of hypersion, bronchio breeding, increase the acidity of gastric juice, narrows the pupil, causes an accommodation spasm, reduces intraocular pressure, enhances the tone of the intestinal muscles (enhances the peristaltics and relaxes the sphincters) and the bladder, causes the bronchi spasm, tones the skeletal muscles.

Indications for use

• miasthenia
• acute miasthenic crisis
• motor disorders after brain injury
• palace
• recovery period after transferred meningitis, poliomyelitis, encephalitis
• neuritis
• atrophy of the optic nerve
• athony of the gastrointestinal tract
• bladder Atonia
• elimination of residual phenomena after the blockade of neuromuscular transmission non-polarizing muscle relaxants

Method of application and dose

Adults prescribe the drug subcutaneously, intramuscularly and intravenously. Subcutaneously adults - 0.5 - 2 mg (1-4 ml) 1 - 2 times a day. Maximum one-time dose for adults - 2 mg, daily - 6 mg. The course of treatment (other than miasthenia) - 25 - 30 days, if necessary, again, after 3 to 4 weeks. Most of the total daily dose is prescribed during the day when the patient is largely fatigue.

For miastic, adults subcutaneously or intramuscularly 0.5 mg (1 ml of 0.05% solution) per day. The course of treatment is long, with the change of ways of administration.

With a miasthenic crisis (with difficulty breathing and swallowing) - adults 0.5 - 1 ml of 0.05% solution intravenously, in the future subcutaneously, with small intervals.

With postoperative intestinal atony, bladder: for prophylaxis, including postoperative urine delay - subcutaneously or intramuscularly 0.25 mg (0.5 ml of 0.05% solution), as early as possible, and re-every 4 - 6 hours within 3 - 4 days.

As an antidote of the muscle relaxants (after the preliminary administration of atropine sulfate at a dose of 0.6 - 1.2 mg intravenously, to the increase in the pulse up to 80 ° C.) are injected after 0.5 - 2 min 0.5 - 2 mg intravenously slowly. If necessary, injection is repeated (including atropine sulfate in the case of bradycardia) in a total dose of no more than 5 - 6 mg (10 - 12 ml) for 20 to 30 minutes; During the procedure, artificial ventilation of the lungs are provided.

Children are subcutaneously (under hospital) - 0.05 mg (0.1 ml of 0.05% solution) for 1 year of life, but not more than 3.75 mg (0.75 ml of 0.05% solution) by 1 injection.

Side effects

Hypersion, nausea, vomiting, diarrhea

Spasms and twitching skeletal muscles, including twitching muscles of the language, dysarthria, convulsions

Headache, dizziness, general weakness, loss of consciousness, drowsiness, tremor

Frequent urination

Bradycardia or Tachycardia, AV Blockade, Heart Stop

Reduced arterial pressure

Strengthening the secretion of bronchial glands, increase the tone of the bronchi

Allergic reactions: skin rash, itching, face hyperemia, anaphylactic shock

Shortness of breath, the oppression of breathing down to the stop

Myiosis vision

Arthralgia

Abundant sweating

Contraindications

• increased sensitivity to the components of the drug
• epilepsy
• hyperkinesia
• vagotomy
• coronary artery disease
• angina, arrhythmia, bradycardia
• bronchial asthma
• expressed atherosclerosis
• thyrotoxicosis
• gastric ulcer and duodenal ulcer
• peritonitis
• mechanical obstruction of the gastrointestinal tract and urinary tract
• prostate hypertrophy accompanied by difficult urination
• acute period of infectious disease
• intoxication in highly weakened children
• during pregnancy and breastfeeding

Medicinal interactions

During myasthenia, they are prescribed in combination with aldosterone antagonists, glucocorticosteroids and anabolic hormones. Atropine, metacin and other M-cholinoblocators weaken M-cholinomimetic effects. Prolongs and strengthens the influence of depolarizing muscle relaxants, weakens or eliminates - antidehaming. Caution is prescribed simultaneously with neomycin, streptomycin, kanamycin, which have an antihasipeolarizing effect. Co-use with local and some common anesthetics, antiarrhythmic drugs that violate the cholinergic transmission may result in weakening the effects of prozer. Organic nitrates reduce the effectiveness of the prozer.

Ephedrine will potentiate the action of the prozer.

With the simultaneous use of prozero with beta-adrenoblockers, bradycardia is possible.

special instructions

It should be selected with caution to select the dose of prozerne, taking into account the possible high individual sensitivity to it.

Caution is used in arterial hypotension, heart rate impaired, especially in bradycardia, with a predominance of tone n.Vagus., hyperthyroidism, addison disease, ulcerative ulcer of the stomach and duodenal intestine, when using anticholinergic agents, children who are sick of miastenia and use antibacterial drugs having an antidehauting effect (neomycin, streptomycin, kanamycin, etc.), local and common anesthetics, antiarrhythmic drugs, Violating cholinergic transmission.

When using large doses of the prozermin, it is necessary to pre-or simultaneously assign atropine sulfate.

Due to the coincidence of the clinical symptoms of a miasthenic crisis (with an insufficient therapeutic dose of the drug) and a cholinergic crisis (as a result of the overdose of prozermin), a thorough differentiated diagnosis is necessary.

With caution, the drug is used by the elderly patient.

During the period of treatment, it is prohibited from the management of motor transport and occupation by other potentially hazardous activities that require increased concentrations of attention and the velocity of psychomotor reactions.

Children use subcutaneously (only in conditions of the hospital) in doses established in the "Method of Application and Dose" section.

Overdose

Symptoms: Associated with the overexecision of cholinoreceptors (cholinergic crisis): Bradycardia, hypercitution, mios, bronchospasm, nausea, strengthening of peristalsis, diarrhea, strengthening of urination, twitching muscles of the language and skeletal muscles, gradual development of general weakness, decrease in blood pressure.

Treatment: Dose reduce or cancel the drug. If necessary, atropine sulfate is administered (1 ml of 0.1% solution), metacin. Therapy is symptomatic.

Prezero (name in Latin Proserinum) is a drug that blocks the activity of the enzyme acetylcholynestsee. Increases the content of acetylcholine in nervous endings. Used in miastic, atonic constipation, sclerosis, other neurological disorders.

Structure

Active substance: Neostigmin methylsulfate.

Prezer release form

The drug is produced in several dosage forms.

Pills

1 Tablet contains 0.015 g (15 mg) of neostigmine methyl sulfate, sucrose, starch, calcium stearate.

In ampoules

1 ampoule Contains 1 ml of 0.0005 g / ml of a neostigmine of methyl sulfate medicinal drug. Packing 10 ampoules 0.05%. Used subcutaneously and intramuscularly.

pharmachologic effect

The drug is characterized by the features of the impact.

Pharmacokinetics and Pharmacodynamics Prezero

The tool reversibly blocks the cholinesterase enzyme, leading to a delay of the decay and accumulation of the neurotiator of acetylcholine, which transmits in neuromuscular synapse. Due to this action, it enhances neuromuscular transmission, contractile activity of the smooth muscles of internal organs: bronchi, stomach, intestines, bladder, uterus.

Neostigmin causes an increase in the acidity of the stomach, the release of pepsin, pancreatic enzymes. Enhances the peristalsis of the stomach, reducing the gallbladder, muscles of the intestines, bladder. Tits the muscles of the uterus.

Acetylcholine accumulating in the nerve endings causes the extension of vessels, reduces pressure. It has a negative bathemol, the dromo, inotropic effect on the heart - reduces the frequency, heart force, the excitability of myocardium.

Neostigmin methylsulfate has all the effects of the parasympathetic system - narrows the pupil, causes an accumulation of accommodation, a decrease in intraocular pressure, stimulates the secretion of mucus with bronchial glands, increases the tone of the bronchi. With its action, salivation is enhanced, sweating. Relaxing intestines, bladder sphincters.

Neostigmine methylsulfate - antagonist antide -olarizing muscle relaxants. However, in doses exceeding therapeutic, can cause resistant depolarization. Stimulates muscarinic and nicotine cholinoreceptors.

Unlike physostigmine, neostigmin acts less on the cross-striped muscles of the heart, to a greater degree affects the smooth muscles of the uterus, the bladder, the intestine, as well as the skeletal muscles.

Quaternary nitrogen base. Practically does not penetrate the hematorecephalic barrier. Bioavailability - 1-2%. Binds to plasma proteins by 15-25%. Half-life - about 50 minutes. Metabolized liver in inactive connections. 80% is excreted by the kidneys during the day: 30% of them are inactive metabolites, 50% unchanged substance.

For what is prescribed prozerne

Neostigmine methylsulfate is prescribed with neurological problems associated with the impaired functioning of the peripheral nervous system. The use of the drug is shown in miastic, multiple sclerosis - diseases of the nervous system, in which paralysis of skeletal muscles are observed.

Disorders of motor functions (paresis) arise also after transferred meningitis, encephalitis, polio, stroke, cranial injuries.

The drug reduces intraocular pressure with an open-angle glaucoma. It is used in atrophy of the optic nerve, neuruts of motor nerves, stomach hypotension, atonic constipation, urine delay in the elderly, as well as after the spine injury, osteochondrosis (electrophoresis).

Neostigmin is used to eliminate side effects and symptoms of the overdose of cholinolithics, non-polarizing muscle relaxants, performing the prozer-sample to identify the excessive lack of pancreatic gland.

Neostigmin - a means of first aid from the paralysis of the respiratory muscles in botulusme (canned matter poisoning), to resolve childbirth, with a miasthenic crisis.

With hemorrhoids

Contraindications

It is impossible to use neostigmine methyl sulfate in hyperkinosis of various genesis (autosis, chorea), epilepsy, blockades of a conductive system of heart, bradycardia, wagotomy, ulcerative lesions of the stomach and duodenum. Among the contraindications - mechanical obstruction of the intestines, a benign hyperplasia of prostate, atherosclerosis, thyrotoxicosis, acute infections, allergic to the drug, bronchial asthma, obstructive bronchitis.

Side effects

The most common side effects:

1. From the head of the gastrointestinal tract: nausea, vomiting, increasing salivation, violation of articulation, tongue shake, meteorism, diarrhea, abdominal pain.
2. Nervous system: reduction of blood pressure, dizziness, twitching skeletal muscles, drowsiness, weakness, loss of consciousness, darkness in the eyes due to the narrowing of the pupil.
3. Cardiovascular system: bradycardia, conductive system blockade, nodal rhythm, hypotension.
4. Respiratory system: bronchospasm, secretion of mucus, shortness of breath, inhibition of breathing.
5. Allergy: rash on the skin, swelling of quinque, anaphylactic shock.
6. Strengthening urination, sweating, joint pain.

Overdose

The excess of the required dose causes the cholinergic crisis - redness of the face, salivation, swelling of the lungs, convulsions. Perhaps the condition of the resistant depolarization is paralysis of the muscles. To remove these symptoms, cholinolics (atropine), cholinesterase reactivators (dipiroxim, isonitrosin) are used.

How and how much to take

Adults - on one tablet 15 mg 2-3 times a day. Attachment injections - 1-2 times a day. Children under 10 years old - 1 mg per day for the year of life. Maximum dose for children over 10 years old - 10 mg. Subcutaneous administration - 50 μg / year of life, but not more than 375 μg per injection.

With an open-angle glaucoma, dripped in a conjunctival bag 1-4 times a day.

The maximum one-time dose is 15 mg, daily-50 mg. Subcutaneously: one-time - 2 mg, daily - 6 mg.

With the neuro of the facial nerve combined with the reception of vitamins, the anesthesia of the local (but not at the same time).

special instructions

When introducing large doses, an atropine is required. In case of Asson's disease, caution is needed. In patients with miastenia in cholinergic and miasthenic cries, the dosage is corrected.

Childcare

Treatment of children, baby is desirable to conduct in the hospital under the supervision of doctors.

During pregnancy and lactation

Interaction

Neostigmine sulfate is an antagonist of antide -olarizing muscle relaxants, but at the same time agonist depolarizing, therefore enhances the effect of the latter.

Gangley, M-cholinoblocators, local anesthetics, tricyclic antidepressants, drugs from epilepsy, Parkinsonism reduce the effect of the medication. Ephedrine causes an increase in action.

Sharing with beta-adrenoblockers enhance bradycardia.

Analogs

Ipidakrin, neuromidine, physostigmine - cholinesterase inhibitors.

Terms of sale

Released strictly by recipe.

Storage conditions and shelf life

Store in a dry, inaccessible place at a temperature at a temperature of no more than 25 ° C.

Price

In Russian pharmacies, the cost of packaging 10 ampoules is 70-100 rubles. Tablets 15 mg 20 pcs. - 60-100 rubles.