FIZOSTIGMIN (Physostigminum).

     Physostigmine, or ezerin, is the main alkaloidom so-called kalabarskih beans, seeds of West African plants Physostigma venenosum, herewith. pulses (Leguminosae).

     On chemical structure Physostigmine is a product of indole, a uretanovuyu group.

     In medical practice used fizostigmina BUN (Physostigmini salicylas).

     Synonyms: Ezerina BUN, Eserini salicylas, Physostigmine salicylate, Physostigminum salicylicum.

     Yield prizmaticheskie brilliant crystals. It is difficult to dissolve in water (1: 100), soluble in alcohol (1: 12). From the action of light and air powder and solutions painted in red and become inactive. Solutions to prepare ex tempere asepticheski or subjected tindalizatsii.

     Fiziostigmin is one of the main representatives antiholinesteraznyh substances reversible action. In high doses, together with the impact of cholinesterase can provide (as well as other drugs antiholinesteraznye) direct effect on holinoretseptory.

     Fiziostigmina BUN used mainly in the eye practice to narrow pupil and downward pressure vnutriglaznogo with glaucoma. Enter in konyunktivalny bag for 1 to 2 drops of 0.25 to 1% solution of 1 to 6 times a day. Declining pupil is usually after 5 to 15 minutes and kept 2 to 3 hours or more. In keratitah applied ointment to salitsilatom fizostigmina (0.2 - 0.25%).

     When glaucoma Physostigmine is a stronger decline vnutriglaznogo pressure than pilocarpine, but it is often about pain in the eyes and nadbrovnoy area because a strong reduction iris. For this reason Physostigmine often used in acute glaucoma and when pilocarpine not effective. A good combination gives effect fizostigmina (0.25%) with pilokarpinom (1%).

     Physostigmine is also sometimes used in the clinic for nervous diseases nervnomyshechnyh diseases, as well as paresis bowel (0.5 ml -1 0.1% solution under the skin). Increased use for these purposes are Galantamine, oksazil, Neostigmine, as paresis bowel and bladder-Aceclidine.

     In recent years, trying to use Physostigmine (subcutaneously) for the improvement of the patients with Alzheimer disease. It was found that when the disease reduced the content of crust-holinatsetiltransferazy large brain enzyme involved in pain acetylcholine. What if this violation holinergicheskoy innervation accompanied by characteristic of the disease, clinical symptoms (less memory, etc.). Found that Physostigmine improves condition of patients suffering from Alzheimer disease. But quite resistant therapeutic effect Physostigmine not. However, there are undesirable side effects that limit the use of this drug. For better holinergicheskih funds available for the integrated treatment of Alzheimer's, being sought specific agonists M1- muskarinovyh postsynaptical receptor antagonists and presinaptichesnih M2- receptors can increase the release of acetylcholine holinergicheskimi nerve end.

     Higher doses fizostigmina salitsilata for adults under the skin: single 0.0005 g daily 0,001 city

     In applying fizostigmina, as well as other antiholinesteraznyh drugs, especially in high doses, can be observed side effects associated with hyperactivity holinergicheskih processes, increasing salivatsii, bronhiolospazm, muscle spasm bowel and bladder, slowing heart reductions and violation heart rhythm, spasmodic reaction et al.

     Fizostigmina pharmacological antagonists are atropine, metatsin holinoliticheskie and other drugs.

     Solutions are released in orange glass bottle.

     Storage: A. In a list ukuporennyh banks orange glass in sheltered from the world scene.

     Rp. : Pilocarpini hydrochloridi 0.1

     Physostigmini salicylatis 0,025

     Aq. destill. 10 ml

     M. D. in vitro nigro

     S. Eye drops. On 1 - 2 drops of 4 to 6 times a day

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