DIPIROKSIM (Dipyroximum; synonym: Trimedoximum, Trimedoximi bromidum, TMB 4; joint venture. B) — the antidote applied at poisoning with organophosphorous connections (FOS). 1,1 '-Trimetilen-bis-(4-oksiminometit) - pyridinia a dibromide — monohydrate, C 15 H 18 Br 2 N 4 O 2 - H 2 O:
Yellowish fine-crystalline powder, inodorous, bitter taste. Let's easily dissolve in water, it is slightly soluble in 95% alcohol.
Is one of the most effective specific antagonists organophosphorous connections (see). Its action is based on ability to dephosphorylate inhibited these poisons acetylcholinesterase (see. Cholinesterases ). As a result of reactivation of enzyme the symptoms of poisoning connected with excitement of peripheral cholinergic systems are eliminated or weakened (a bronchospasm, an enterospasm, disturbance of neuromuscular transmission, hypersecretion of salivary and bronchial glands, etc.). Badly gets through a blood-brain barrier and therefore does not influence cholinesterase of a brain and consequently, and on the symptoms caused by impact of FOS on c. N of page.
At parenteral administration of D. it is soaked up quickly enough. The maximum level of drug in blood serum at introduction of a therapeutic dose is (once) observed within 30 min. after an injection, then contents it in blood quickly falls and by the end of the first hour makes a half of the maximum concentration. Is quickly brought out of an organism (within the first hour about a half of the entered dose is removed). Renders the weak irritant action which is shown short-term pain reaction on site of an injection. Drug is used in the presence of symptoms of poisoning of FOS or at suspicion of poisoning. Enter subcutaneously 1 ml of 15% of solution usually into combinations with atropine (2 — 3 ml of 0,1% of solution). If symptoms of poisoning do not disappear, along with atropine enter repeatedly the same dose D. Tselesoobrazney D. to apply in combination with the central cholinolytics (e.g., aprophene) compensating lack of antagonistic action of D. on acetylcholinesterase of c. N of page. After elimination of spasms repeatedly apply atropine in a maintenance dose. In hard cases on a course of treatment use 3 — 4 ml of 15% of solution D. (in especially hard cases to 7 — 10 ml).
Can be applied also to treatment of poisonings with antikholinesterazny connections of other chemical classes. There are data on efficiency of reaktivator of cholinesterase at some bakteriotoksikoza, in particular at tetanus.
Drug usually does not cause by-effects. At introduction of the dose exceeding therapeutic several times moderate falling of the ABP, tachycardia is observed. At D.'s poisoning are noted a vision disorder (diplopia), neuromuscular transmission (kurarepodobny effect) and symptoms of excitement of cholinergic systems. Cholinolytic substances, antagonists of kurarepodobny means and symptomatic means apply to treatment of poisoning.
Form of release: ampoules on 1 ml of 15% of solution. Remains in the cool, protected from light place.
See also Antidotes of OV .
Bibliography: S. N. brooms and 3augolnikov S. D. Reaktivatora of cholinesterases, L., 1970, bibliogr.; Brooms G. N, Shchekoldina V. I. and Simonova I. G. To pharmacology of a dipiroksim, Pharm, and toksikol., t. 35, No. 5, page 589, 1972; Prozorovsky V. B. and Savateev N. V. Neantikho-linesteraznye mechanisms of action of antikholinesterazny means, L., 1976, bibliogr.
S. N. Golikov.