Proserin

Prozerin - a drug designed to treat disorders of the nervous system. It goes on sale as a colorless solution for intramuscular injection.

It is a synthetic inhibitor of cholinesterase, restoring neuromuscular conduction, decreasing heart rate, increasing secretion of glands (salivary, gastrointestinal tract, sweat and bronchial), strengthening the tone of smooth muscles and bladder, causing bronchospasm, tonic skeletal musculature, increasing the acidity of gastric juice, narrowing pupil, causing a spasm of accommodation, reducing intraocular pressure.

Clinical and pharmacological group

Inhibitor of acetylcholinesterase and pseudocholinesterase.

Conditions of leave from pharmacies

It is released on prescription.

Price list

How much is Proserin in pharmacies? The average price is at the level of100 rubles.

Form of issue and composition

The drug Proserin is available in a dosage form for parenteral administration, which is clear and colorless. Also available in tablet form.

Composition of 1 tablet:

• Active substance: neostigmine methylsulfate (proserin) - 15 mg;
• Additional components: sugar (sucrose) - 64 mg, potato starch - 20 mg, calcium stearate monohydrate - 1 mg.

Composition 1 ml solution for subcutaneous and intravenous administration and for injection:

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

Solution for parenteral administration Proserin is in glass ampoules with a volume of 10 ml, which are packaged in a planar cell package. The carton contains one contoured package with ampoules and an instruction.

Pharmacological effect

The active substance of Proserin is neostigmine methyl sulfate. Getting into the body, this substance temporarily blocks cholinesterase - the main enzyme, which is contained in the nervous tissue and skeletal muscles. This leads to an increase in the activity of acetylcholine - a neurotransmitter, which is responsible for neuromuscular transmission.

Its accumulation helps to achieve the following therapeutic effects:

• narrowing of the pupil;
• the tone of the skeletal musculature;
• activation and toning of the muscles responsible for supporting the skeleton;
• strengthening the glands involved in the development of sweat and saliva;
• decrease in heart rate;
• increased mobility of the intestine (peristalsis).

When administered in therapeutic doses, it stimulates the smooth transfer of nerves to the muscles. In excessive doses leads to disorders of neuromuscular conduction. It falls into the right substance in the liver. Decomposition products that do not have any effect on the body are 80% excreted along with urine.

Indications for use

Application of tablets and injections of a medicine Proserinum subcutaneously appoint or nominate at such pathologies:

• atony of the bladder, organs of the digestive tract;
• neuritis of the facial or optic nerve;
• atrophy of the optic nerve, neuritis;
• motor disorders due to brain trauma;
• myasthenia gravis;
• recovery from encephalitis, poliomyelitis, meningitis;
• open-angle glaucoma;
• weak labor activity;
• decrease or absence of tonus in the walls of the bladder, intestines, stomach
• disorders of neuromuscular transmission;
• paralysis.

Contraindications

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

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

Use in pregnancy and lactation

Proserin penetrates through the placental barrier, in very small quantities excreted in breast milk.

During pregnancy and during lactation apply only on strict indications.

Dosage and route of administration

The instructions for use indicate that the solution for parenteral use of Proserin is intended for subcutaneous, intramuscular or intravenous administration in the conditions of a medical institution in compliance with the rules of antiseptics and asepsis aimed at excluding the possibility of infection of the patient's body. For adults, the mode of application and dosage of the drug depend on the pathological process:

• Atony of the intestine or bladder, including postoperative - the drug is used in a dose of 0.25 or 0.5 mg, depending on the severity of atony, it is administered subcutaneously or intramuscularly.
• Myasthenia gravis - dosage is 0.5 mg (1 ampoule) 1 time per day subcutaneously and intramuscularly, the course of treatment is prolonged with alternation of methods of drug administration.
• Overdose with muscle relaxants - the drug is administered intravenously drip in a dose of 0.5 mg for 2 minutes. If necessary, the injection is repeated, with the dosage administered within 20-30 minutes, may be 5-6 mg of proserin.
• Pronounced myasthenia gravis with difficulty swallowing and breathing (myasthenic crisis) - the drug is administered intravenously at a dosage of 0.25 or 0.5 mg, followed by subcutaneous injection.
• Stimulation of childbirth: subcutaneously, 1 ml of a solution (0.5 mg) of Prozerin 1-2 times (at intervals of 1 hour), simultaneously with the first injection, one mg (1 ml of 0.1% solution) of atropine must be administered once per subcutaneously;

Usually the dosage and mode of application of the drug the doctor sets individually, which depends on the type of pathological process, the severity of its course, as well as the age and sex of the patient.

Pills

Proserin is taken orally, preferably 30 minutes before a meal.

Recommended dosing regimen:

• Motor disorders resulting from encephalitis, meningitis, trauma, and against paralysis of the facial nerve: 15 mg 1-2 times a day (the dose is determined by the effectiveness and tolerability of therapy). The average course duration is 2-3 weeks;
• Myasthenia gravis: long-term therapy is shown with a change in the route of administration. Single dose - 15 mg, daily - 50 mg (most of it must be taken during the day when the greatest degree of fatigue is observed). The course duration is 25-30 days, after 3-4 weeks a repeated course can be appointed;
• Motor disorders resulting from poliomyelitis (concomitantly with other activities - therapeutic gymnastics, physiotherapy, balneotherapy, etc.) - 15 mg once a day, every day or every other day (determined by the effectiveness and tolerability of therapy). The course of therapy is 15-20 receptions. Repeated courses are conducted after 2-3 months.

Side effects

Injections and taking of tablets of Proserin can cause the following side reactions:

• digestion: diarrhea, hypersalivation, vomiting, flatulence, nausea, increased peristalsis;
• breathing: respiratory depression, increased bronchial tonus, increased secretion of bronchial glands, dyspnea;
• allergic manifestations: itching, rash on the skin, face hyperemia, anaphylactic manifestations;
• heart and blood vessels: tachycardia, bradycardia, arrhythmia, AV-blockade, nodal rhythm, changes in ECG of a non-specific nature, lowering of blood pressure;
• central and peripheral NA: dizziness and headache, blurred vision, weakness, miosis, drowsiness, convulsions, impaired consciousness, dysarthria, twitching of skeletal muscles;
• other manifestations: increased frequency of urination, increased sweating, arthralgia.

Overdose

According to the instructions, the drug may cause side effects due to an overdose. For the first undesirable symptoms, treatment with Proserinum should be discontinued and consult a doctor for symptomatic therapy.

Symptoms of overdose are associated with a cholinergic crisis: diarrhea, bradycardia, frequent urination, lowering blood pressure, general weakness.

special instructions

Before you start using the drug, read the special instructions:

1. Use with caution in Addison's disease.
2. When parenteral administration in high doses, a preliminary or simultaneous administration of atropine is necessary.
3. If a myasthenic (due to an insufficient therapeutic dose) or cholinergic (due to an overdose) a crisis requires careful differential diagnosis due to the similarity of the symptoms.

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

Drug Interactions

When using the drug, it is necessary to take into account the interaction with other drugs:

1. Ephedrine potentiates the action of neostigmine methyl sulfate.
2. With the simultaneous use of m-holinoblokatory, ganglioblokatory, quinidine, novocainamide, local anesthetics, tricyclic antidepressants, antiepileptic and anti-Parkinsonian drugs reduce the effect of neostigmine methyl sulfate.
3. Neostigmine methyl sulfate is an antagonist of nondepolarizing muscle relaxants and, with simultaneous application, enhances the effect of depolarizing muscle relaxants.
4. With the simultaneous use of neostigmine methyl sulfate with beta-adrenoblockers, bradycardia may increase.

Reviews

We picked up some reviews of people who used the drug, Proserin:

1. Vladimir. I can not do without Proserinum. Atony of the bladder with all the ensuing consequences makes it necessary to periodically drink a monthly course of tablets. The disease always recedes for a long period. As for the side effects, I can note that at 3-4 weeks of use I feel drowsiness and general weakness of the body.
2. Elena. In general, I became very ill, pressure increased, my tongue did not turn, my breath, shorter horror. I called the doctor, she denied everything, she can not speak. I called an ambulance. People are more careful who have tachycardia and weak blood vessels.
3. Alexandra. My husband was diagnosed with neuritis. Symptoms of the disease are similar to the clinical manifestations of the brain tumor, so when it was ruled out, we were immensely pleased. Among others, tablets Proserinum have been prescribed. Her husband drank them by a course of 30 days, as the doctor appointed. There were no side effects. They got rid of neuritis with the help of complex therapy.

Analogues

The prodrug does not have structural analogs for the active substance. Analogues on the pharmacological group (stimulators of the motility of the gastrointestinal tract):

• Ganaton;
• Oregano grass;
• Itomed;
• Kalimin 60 N;
• Coordination;
• Juniper fruits;
• Montana home drops;
• Peristil;
• Prozerin Darnitsa;
• Prozerin solution for injection 0.05%.

Before using analogues, consult your doctor.

Storage conditions and shelf life

The shelf life of the solution for parenteral administration of Proserin is 3 years. The drug should be stored in a dark, dry place inaccessible to children at an air temperature of no higher than 25 ° C.

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