Description of the medicine: Proserinum (Proserinum)

PROSERINUM.

N- (meta-Dimethylcarbamoyloxyphenyl) -trimethylammonium methyl sulfate.

Synonyms: Eustigmin, Metastigmin, Miostin, Muastigmine, Neoeserin, Neostigmani Methylsulfas, Neostigmine Methyisulfate, Prostigmin methylsulfate. Stigmosan, Syntostigmin, Vagostigmin, and others.

White crystalline powder odorless, bitter taste. Hygroscopic. In the light acquires a pinkish hue. Very easily soluble in water (1: 10), easily - in alcohol (1: 5). Aqueous solutions (pH 5, 9 - 7, 5) are sterilized at + 100 ° C for 30 minutes.

Proserin is a synthetic anticholinesterase substance. By chemical structure can be considered as a simplified analog of physostigmine containing an N-alkyl substituted carbamoyloxyphenyl moiety. However, the characteristic feature of proserin (as well as oxazyl and pyridostigmine) is the presence in its molecule of a quaternary ammonium group. It differs from the alkaloids of physostigmine and galantamine, which do not contain quaternary nitrogen atoms.

Prozerin has a strong reversible anticholinesterase activity. By peripheral effects is close to physostigmine and galantamine. Like other quaternary ammonium compounds, it has a predominant effect on peripheral systems and hardly penetrates the blood-brain barrier.

Applied with myasthenia gravis, motor disorders after brain injuries, paralysis, in the recovery period after meningitis, polymyelitis, encephalitis, etc., with atrophy of the optic nerve, neuritis, for preventing and treating intestinal atony and bladder. In ophthalmic practice, proserine is sometimes prescribed to narrow the pupil and lower the intraocular pressure in open-angle glaucoma.

Prozerin is an antagonist of antidepolarizing curare-like drugs. However, large doses can themselves cause a breakdown in neuromuscular conduction as a result of the accumulation of acetylcholine and persistent depolarization in the synapse region. As an antidote to muscle relaxants, proserin is used for muscle weakness and respiratory depression after the anesthesia is completed using antidepolarizing, and also in the case of depolarizing muscle relaxants (see Ditilin), if the latter begin to act as antidepolarizing ("double block").

Usually, it is used inside or under the skin.

Inside (30 minutes before meals), adults are prescribed in powder or tablet to adults 0.01 to 0.015 g (10 to 15 mg) 2 to 3 times a day; Children under 10 years of 0,001 g (1 mg) for 1 year of life per day; Children older than 10 years - not more than the total daily dose of 0.01 g (10 mg).

It is convenient for children to prescribe proSerine in the form of granules.

Granulese proserine for children (Granulae Proserini pro infantibus) is pinkish-white or creamy-pink, soluble in water. Produced in 150 ml bottles. Before use, pour freshly boiled warm water into the vial to the mark <100 ml>. The resulting solution corresponds to a 0.02% solution of prosirin and contains 1. 1 teaspoonful (5 ml) of 0.001 g, and in 1 dessert spoon (10 ml) 0.002 g of proserine.