Proserine, 0.5 mg/ml 1 ml 10 pcs

Pharmacological action

Acetylcholinesterase and pseudocholinesterase inhibitor. It has indirect cholinomimetic effect due to reversible inhibition of cholinesterase and potentiation of endogenous acetylcholine action.

It improves neuromuscular transmission, increases gastrointestinal motility, increases tone of the bladder, bronchi, secretion of exocrine glands. Causes bradycardia and lowering of blood pressure. Narrows the pupil, lowers intraocular pressure, causes spasm of accommodation.

Pharmacokinetics

After parenteral administration, neostigmine methylsulfate undergoes hydrolysis and is also metabolized in the liver to form inactive metabolites. Binding to plasma proteins is 15-25%.

It is excreted in the urine (80% within 24 hours) as unchanged substance (about 50%) and metabolites. It poorly penetrates through the HEB.

Indications

• myasthenia gravis (muscle weakness)
• polio
• glaucoma
• decreased tone of the stomach, bowel and bladder.

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Active ingredient

Neostigmine methyl sulfate

Composition

1 ml of the solution contains:

Active ingredient:

neostigmine methyl sulfate – 500 µg

How to take, the dosage

The solution for adults is administered Proserine subcutaneously – 1-2 mg 1-2 times a day.

In children, Prozerin is administered subcutaneously, the dose is calculated at 50 micrograms per 1 year of life, but not more than 375 micrograms per injection.

Interaction

Neostigmine methyl sulfate is an antagonist of nondepolarizing myorelaxants, while concomitant use increases the effect of depolarizing myorelaxants.

Concomitant use of m-cholinoblockers, ganglioblockers, quinidine, novocainamide, local anesthetics, tricyclic antidepressants, antiepileptic and anti-parkinsonian drugs decrease the effect of neostigmine methylsulfate.

Ephedrine potentiates the effect of neostigmine methylsulfate.

The concomitant use of neostigmine methylsulfate with beta-adrenoblockers may increase bradycardia.

Special Instructions

With caution is used in Addison’s disease.

Parenteral administration at high doses requires prior or concomitant administration of atropine.

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

Impact on driving and operating machinery

At the time of treatment, it is necessary to refrain from driving and other potentially dangerous activities in which concentration and high speed of psychomotor reactions are required.

Contraindications

• Epilepsy,
• bronchial asthma,
• sthenocardia,
• atherosclerosis,
• adenomatology,
• gastric and duodenal ulcer,
• high sensitivity to the drug.

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Side effects

• nausea,
• vomiting,
• diarrhea
• slow heart rate,
• .decrease in BP
• twitching of the muscles of the tongue and skeletal muscles
• allergic reactions.

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Overdose

Symptoms: associated with overexcitation of cholinoreceptors (cholinergic crisis): bradycardia, hypersalivation, miosis, bronchospasm, nausea, increased peristalsis, diarrhea, increased frequency of urination, twitching of the tongue and skeletal muscles, gradual development of general weakness, decrease of blood pressure (BP).

Treatment: reduce the dose or discontinue treatment, if necessary administer atropine (1 ml of 0.1% solution), methacin or other choline-blocking drugs.