Prozerin injections (neostigmine methyl sulfate) 0.05% 1ml. №10

Description

Prozerin Composition
active substance: neostigmine methylsulphate;
1 ml of solution contains 0.5 mg prozerin;
excipient: water for injection.

Dosage form
Injection.

Pharmacological properties
Neurin is a reversible synthetic cholinesterase blocker. It has a high affinity for acetylcholinesterase due to its structural identity with acetylcholine. Like acetylcholine, prozerin first interacts with the catalytic center of cholinesterase, but later, unlike acetylcholine, it forms, due to its carbamine group, a stable connection with the enzyme. The enzyme temporarily (from several minutes to several hours) loses its specific activity. At the end of this time, due to the slow hydrolysis of prozerin, cholinesterase is released from the blocker and restores its activity. This action leads to the accumulation and enhancement of the action of acetylcholine in the cholenergic synapses. Neurin has a pronounced muscarinic and nicotinic effect, has a direct stimulating effect on skeletal muscles.
It causes a decrease in heart rate, increases the secretion of excretory glands (salivary, bronchial, sweat and digestive tract) and promotes the development of hypersalivation, bronchorhea, increased acidity of gastric juice, constricts the pupil, causes a spasm of accommodation, reduces intraocular pressure, enhances the tone of smooth muscles of the intestine ( peristalsis and relaxes the sphincters) and the bladder, causes bronchospasm, tones up the skeletal muscles.

Indications
Myasthenia gravis, acute myasthenic crisis; movement disorders after brain injury; paralysis; the recovery period after suffering from meningitis, poliomyelitis, encephalitis; neuritis, optic nerve atrophy; intestinal atony, bladder atony; elimination of residual effects after blockade of neuromuscular transmission by non-depolarizing muscle relaxants.

Contraindications
Hypersensitivity to the active substance or to other components of the drug; epilepsy; hyperkinesis; vagotomy; coronary heart disease; angina pectoris; arrhythmias; bradycardia; bronchial asthma; severe atherosclerosis; thyrotoxicosis; peptic ulcer of the stomach and duodenum; peritonitis; mechanical obstruction of the gastrointestinal tract and urinary tract; hypertrophy of the prostate gland, proceeding with dysuria; acute period of an infectious disease; intoxication in severely weakened children, simultaneous use with depolarizing muscle relaxants.

Method of administration and dosage
Adults.
The drug prozerin is prescribed subcutaneously at a dose of 0.5-2 mg (1-4 ml) 1-2 times a day. The maximum single dose for adults is 2 mg, the daily dose is 6 mg. The duration of the course of treatment (except for myasthenia gravis, myasthenic crisis, postoperative bowel and bladder atony, muscle relaxant overdose) is 25-30 days. If necessary, prescribe a second course – in 3-4 weeks. Most of the total daily dose is administered in the daytime when the patient is most tired.
Myasthenia gravis: the drug is prescribed subcutaneously or intramuscularly at a dose of 0.5 mg (1 ml) per day. The course of treatment is long, with a change in the route of administration.
Myasthenic crisis (with difficulty breathing and swallowing): the drug should be administered intravenously at a dose of 0.25-0.5 mg (0.5-1 ml), then subcutaneously, at short intervals.
Postoperative bowel and bladder atony, prevention, including postoperative urinary retention: the drug is administered subcutaneously or intramuscularly, at a dose of 0.25 mg (0.5 ml), as early as possible after the operation, and again – every 4 6 hours for 3-4 days.
As an antidote for an overdose of muscle relaxants (after the previous administration of atropine sulfate at a dose of 0.6-1.2 mg intravenously, until the pulse rate increases to 80 beats / min): the drug is administered slowly intravenously at a dose of 0.5-2 mg through 0, 5-2 minutes. If necessary, repeat injections (including atropine in case of bradycardia) with a total dose of no more than 5-6 mg (10-12 ml) for 20-30 minutes. During the procedure, artificial ventilation of the lungs should be provided.

Children (only in a hospital setting).
Myasthenia gravis:
Newborns: at the initial stage, the drug is prescribed in a dose of 0.1 mg in the form of intramuscular injections. Thereafter, the dose is selected individually, usually 0.05-0.25 mg or 0.03 mg / kg of the drug intramuscularly every 2-4 hours. Due to the special nature of the disease in newborns, the daily dose of the drug can be reduced up to complete cancellation.
Children under 12 years of age: the drug should be prescribed in a dose of 0.2-0.5 mg in the form of injections as needed. The dosage of the drug should be adjusted according to the patient’s response.
As an antidote for an overdose of muscle relaxants (after preliminary administration of atropine sulfate at a dose of 0.02-0.03 mg / kg intravenously, until the pulse rate increases to 80 beats / min): the drug should be administered intravenously slowly at a dose of 0.05-0.07 mg / kg for 1 minute. The maximum recommended dose for children is 2.5 mg.
Other indications: the drug should be prescribed in a dose of 0.125-1 mg in the form of injections. Doses can be changed according to the individual needs of the patient.

Children
The drug prozerin can be used for children only in a hospital setting.

Overdose
Symptoms: associated with overexcitation of cholinergic receptors (cholinergic crisis): tachycardia, bradycardia, hypersalivation, difficulty swallowing, miosis, bronchospasm, shortness of breath, nausea, vomiting, increased peristalsis, diarrhea, increased urination, lack of coordination and muscle twitching, muscle twitching sweat, the gradual development of general weakness, paralysis, lowering blood pressure, anxiety, panic. Very high doses can cause agitation, impatience. Death can occur due to cardiac arrest or respiratory paralysis, pulmonary edema. In patients with myasthenia gravis, in whom overdose is more likely, muscle twitching and parasympathomimetic effects may be absent or mild, which complicates the differential diagnosis of an overdose with a myasthenic crisis.
Treatment: dose reduction or discontinuation of drug administration. If necessary, you should enter atropine (1 ml of 0.1% solution), metacin. Further treatment is symptomatic.

Side effects:

• From the side of the organs of vision: miosis, visual impairment.
• From the respiratory system, chest and mediastinal organs: shortness of breath, respiratory depression, up to a stop, bronchospasm, increased bronchial secretion.
• From the gastrointestinal tract: hypersalivation, spastic contraction and increased intestinal peristalsis, nausea, vomiting, flatulence, diarrhea, involuntary emptying.
• On the part of the kidneys and urinary tract: increased frequency of urination, involuntary urination.
• From the nervous system: headache, dizziness, loss of consciousness, weakness, drowsiness, tremors, convulsions, spasms and twitching of skeletal muscles, including the muscles of the tongue and larynx, leg numbness, dysarthria.
• From the side of the cardiovascular system: arrhythmia, brady- or tachycardia, atrioventricular block, atrioventricular junctional rhythm, nonspecific ECG changes, cardiac arrest, lowering blood pressure (mainly with parenteral administration).
• From the immune system: rashes, itching, flushing, urticaria, allergic reactions, including anaphylactic shock.
• General disorders and reactions at the injection site: increased sweating, sensation of heat, lacrimation, arthralgia, disorders at the injection site, including hyperemia, itching, skin edema.

Shelf life
4 years.
Do not use the medicinal product after the expiry date indicated on the package.

Storage conditions
Store in its original packaging at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of the reach of children.

Incompatibility
Neserin should not be mixed in the same syringe with alkaline solutions and oxidizing agents, as this leads to its destruction.