Medication

Physostigmine

Structure

0.25-1% solutions physostigmine salicylate.

Release form

Solution in bottles of dark orange glass or in ampoules.

Pharmachologic effect

Inhibitory cholinesterase.

Anticholinesteraseagent with a reversible effect.

Pharmacodynamics and pharmacokinetics

Physostigmineis an parasympathomimetic alkaloid, reversible cholinesterase inhibitorcontained in "Calabar beans" - seeds physostigma of the poisonous Physostigma venenosum. As a quaternary ammonium derivative has lipophilicproperties that can easily penetrate BBBand exert not only central, but also peripheral effects acetylcholineon m- and n-cholinergic receptors, wherein:

  • there is a decrease Heart rate;
  • the tone of the smooth muscles of the bronchi, gastrointestinal tract, uterus, bile and urinary tract increases;
  • there is a reduction in the circular muscle of the iris;
  • the pupil narrows (miosis occurs after 5-15 minutes for about 2-3 hours);
  • the outflow of chamber moisture from the eye improves and the increased intraocular pressure;
  • increased tone of the ciliary muscle and is disturbed accommodation(distant vision);
  • there is a stimulation of secretion of glands of external secretion;
  • neuromuscular conduction improves.

Glaucoma Effects

  • stronger drop intraocular pressure, (for example, than when applying Pilocarpine);
  • due to the strong contraction of the iris, unpleasant pain in the superciliary region or eye may occur;
  • in / m and in / in the introduction causes an effect after 20-30 minutes and 5 minutes, respectively, the duration of action ranges from 30-60 minutes.

Physostigmineis exposed metabolism in the human body, however, a small amount of unchanged substance is excreted in the urine. In trace amounts physostigminecan be found in bile and saliva.

Indications for use

  • acute attacks angle-closure glaucoma;
  • for diagnostic purposes in ophthalmology;
  • with intestinal atony or urine;
  • with various neuromuscular diseases.

With Alzheimer's

Modern practice suggests the use of physostigmine (sc administration) in order to improve the condition of patients with Alzheimer's. Since this disease is accompanied by a decrease in the content of the cerebral hemispheres in the cortex enzyme choline acetyltransferasewhich is involved in biosynthetic processes acetylcholine. Violation of cholinergic innervation and causes clinical symptoms characteristic of the disease, for example, memory impairment.

Contraindications

  • epilepsy;
  • dyskinesia;
  • bradycardia;
  • CHF;
  • arterial hypertension;
  • angina pectoris;
  • known hypersensitivity;
  • bronchial asthma;
  • mechanical obstruction of the intestines or urinary tract.

Side effects

  • increased sweatingand salivation;
  • nausea and vomiting;
  • development bradycardia;
  • dizziness;
  • cramps
  • bronchospasm and spasm of intestinal muscles, urea.

Physostigmine, instructions for use (method and dosage)

Administration Methods

Intravenous, intramuscular, ophthalmic.

Introduction to the conjunctival sac

For narrowing of the pupil to occur, 1-2 drops of a 0.25% solution are needed. You can apply from 1 to 6 times a day.

With various neuromuscular diseases and with intestinal atony

Enter should be s / c 0.5-1 ml of a 0.1% solution. Maximum doses for an adult: single - not more than 0.5 mg, daily - up to 1 mg.

As part of combination therapy

  • at keratitis prescribe an ointment containing 0.20-0.25% physostigmineor physostigmine salicylate in conjunction with Pilocarpine;
  • with atrophy, weakness of labor, intestinal atony, myasthenia enter 0.3-1.0 ml of a 0.1% solution physostigminesubcutaneously supplementing with therapy Pituitrin.

Overdose

Causes poisoning, accompanied by vomiting, diarrhea, significant salting (salivation) and excessive sweating, myosis, collapse, respiratory paralysis.

An effective treatment is Atropine - 0.1 percent solution atropine sulfate administered subcutaneously in a dose of 0.5-1.0 ml.

Interaction

Known pharmacological antagonists Physostigmine: Atropine, Metacin and others anticholinergic drugs.

Terms of sale

Strictly according to the recipe.

Storage conditions

Store in a place protected from light rays.

Shelf life

5 years.

Synonyms

Eserin salicylate.

Analogs

Matches for ATX Level 4 code:Pilocarpine

To obtain a resorptive action, a synthetic substitute is administered Physostigmine- Prozerin, more resistant and better tolerated.

Reviews

Reviews about the drug are few, but thanks to it anticholinesterase actionPhysostigmine is widely used not only in ophthalmology, but also in the treatment of various neuromuscular diseases, for example, at Alzheimer.

Price, where to buy

At the moment, do not produce drugs under such a trade name.

There is an American version of the drug - Physostigmine Salicylate 1 mg / ml 2 ml, the minimum price is $ 39.99.

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