Method for preventing acute exposure to organophosphates

FIELD: medicine.

SUBSTANCE: what is presented is a method for acute exposure to organophosphates with pronounced non-anticholinesterase mode of toxicity. A method consists in preventive administration of β-oestradiol 100 mg/kg 20-60 min prior to application of the toxic agent organophosphate.

EFFECT: reducing the manifestations of first signs of the exposure, developing convulsions and complete elimination of animals' death experimentally, administering β-oestradiol 5 days or 1 day before the exposure has not been producing such an effect.

3 tbl

 

The present invention may find application in medicine as a prophylactic agent in acute poisoning cholinesterase poisons with nervously-paralytic action.

At present time for emergency aid in cases of poisoning by substances with marked anticholinesterase activity recommended anticholinergics and reaktivatory cholinesterase (e.g. 1-methyl-5-[2'-benzyldimethylammonium)ethyl]carbamoyl-pyridine-2-aldoxime dichloride in the form of a 15% aqueous solution (patent RF №2243770, publ. 10.01.2005, A61K 31/4425, A61K 31/455, A61P 39/02) whose action is directed primarily to the blockade of cholinergic effects of toxicants. However, despite the relief of a number of manifestations of intoxication, their introduction is only partially addresses the development of seizures, masking the true severity of the lesion [Kolbasov S. E. Comparative efficacy pantethine and atropine under experimental simulation of an emergency situation on objects on chemical weapon destruction / S. E. S. Kolbasov, P. Nechiporenko, M. B. Melikhov [et al.] / / Proceedings of Institute of toxicology, dedicated to the 75th anniversary of the Foundation day: Sat. article edited by Professor S. P. Paciorek. - SPb.: ELBI-SPb, 2010. - S. 160-163, Mohort N. And. The modern condition of development of antidotal remedies for the treatment of lesions of the nerve agents / N. And. Mohort, Etc�ula // Modern problems ciï - 2003. - No. 2. - P. 49-55].

At the same time, long-term persistent cramps define high risk of death struck and disability, as well as the formation of neurodegenerative changes in an intoxication distant period [Prozorovsky V. B. New data on not sinaps (distant) effects of organophosphorus cholinesterase inhibitors (Review of literature.) / Prozorovsky V. B., S. V. Chepur // Tox. Vestn. 2001. No. 4. C. 2-7].

Lack of effect of available therapeutic agents allows to make a conclusion about the importance neholinergichesky mechanisms in the pathogenesis of poisoning by organophosphates and emphasizes the necessity of correction that determines the relevance of search for new means of pathogenetic therapy of lesions. Mostly it relates to acute poisoning with compounds with anticholinesterase activity, which has a pronounced pantyhosepictures mechanism of toxic action, such as Malathion, metaphos, etc. In this regard, the search continues for ways to improve the efficiency of emergency treatment of poisoning with organophosphates pronounced pantyhosepictures mechanism of toxic action, one of which is the study of compounds of steroid structure, including estrogenic hormones with FAMK-mimetic and glutamatemediated effect.

The basis for invented�I put the task of creating an effective method of prevention of acute poisonings with organophosphates pronounced pantyhosepictures mechanism of toxic action.

A solution to a technical problem is provided in that prophylactically for 20-60 min before the application of toxic substances used β-estradiol at a dose of 100 mg/kg.

To simulate intoxication as an example used metaphos, which was injected intramuscularly once the rate of 0.1 ml/kg of body weight of the animal.

Working solutions of β-estradiol was prepared in 4% aqueous solution of tween-80 ex tempore and injected intramuscularly once in doses of 25 to 100 mg/kg of body weight of the animal.

Observation of experimental animals was carried out for 15 days. During the period of observation in experimental animals was recorded the time of occurrence of the main symptoms (lockjaw, tremors, convulsions) and time to onset of death.

The findings of the experimental data were subjected to standard statistical analysis with calculation of average value and the average error. A quantitative estimate of the death rate of animals was performed using probit analysis (Finney). The assessment of differences of mean values was performed using t-student criterion. The average value of the indicators and its error were determined using the tables of interest and their errors in Genes V. S. (1967). To assess the significance of intergroup differences of indicators used Fisher's exact test. Evaluation of the protective activity prep�preparations was carried out by examining the latent period of onset of the first symptoms of intoxication, the latent period for the development of seizures, the time until death of animals, the case-fatality rate (LD50).

To determine the effectiveness of β-estradiol on the model of acute poisoning metafoam was an optimal effective dose and the optimal time of drug administration.

Studies to determine the optimal effective dose of β-estradiol was found that the prophylactic use of the drug had an impact on the dynamics of poisoning caused by metafoam at a dose of 1 LD50,and helped reduce the severity of symptoms (table 1).

From the data presented in table 1. it follows that the use of β-estradiol at doses of 75 and 100 mg/kg 20 min before the injection of the poison is in the dose 1-LD50contributed to a significant increase in NO50development of the first signs of intoxication and ET50start convulsing all degrees compared with the control group. At the same time, the use of the drug in the doses of 25 and 50 mg/kg did not significantly affect these indicators. In addition, it was shown that the introduction of high doses of estrogen were associated with decreased frequency of seizures in the acute poisoning metafoam at a dose of 1 LD50. In the control group cramps 1-5 degrees, developed at 100-17% of specimens, and preventive �primenenie β-estradiol at a dose of 100 mg/kg reduced the likelihood of seizures 1-2 and 3-4 degrees to 17±11% (differences from control are significant at p< 0,05). The introduction of the drug in doses of 75 mg/kg and 100 mg/kg prevent the development of seizures 5-th degree in all animals.

Results analysis of the dynamics and frequency of death of the animals suggests that the prophylactic use of β-estradiol for 20 min to acute poisoning metafoam at a dose of 1 LD50was accompanied by dose-dependent change of the pattern of intoxication, reducing its severity and reduce the frequency of death. The maximum protective effect was observed against the background of preventive applications of the drug in a dose of 100 mg/kg, which completely prevented the death of poisoned animals (p<0,05).

To determine the optimal time for application of β-estradiol was administered at a dose of 100 mg/kg for 5 days, 1 day, 1 hour, 20 mins to poisoning and in the development of the first signs of intoxication, caused by the introduction of metaphase in doses of 1 LD50, 1,25 LD50and 1.5 LD50. Obtained in the course of this experiment the data presented in table 2.

Found that prophylactic use of the drug intramuscularly single dose of 100 mg/kg for 5 days or 1 day before the injection of metaphase in all tested doses had no effect on the dynamics of signs of intoxication and death of animals.

The introduction of the drug for 20 minutes before application of the poison to animals at a dose of 1 LD50increased NO50development of the first signs of into�ikali and seizures, warned the convulsions 1-4 degrees at 83,3±17% of the individuals of the group (differences from control are significant at p<0,05), and completely prevented the development of seizures 5 degrees (p<0.01) and mortality (p<0,05). In rats, which metaphos was introduced in doses of 1.25 LD50or 1.5 LD50increased NO50development of the first signs of poisoning, ET50the development of seizures and the occurrence of death (all differences were significant when compared with the control group).

The use of β-estradiol for 1 h to defeat metafoam at a dose of 1 LD50contributed to the increase of ET50development of the first signs of intoxication (significantly difference at p<0.05) and ET50of seizures 1-2 and 3-4 degrees and completely prevented the appearance of seizures 5 degrees and the death of animals. In rats, which metaphos was introduced in doses of 1.25 LD50or 1.5 LD50increased NO50development of the first signs of intoxication, ET50the development of seizures and ET50the occurrence of death (all differences were significant when compared with the control group), however, the complete prevention of seizures 5 degrees and deaths were noted.

The introduction of β-estradiol in the development of the first symptoms of intoxication with poison in the dose of 1 LD50contributed to the reduction in the frequency of death, but were not warned of convulsions Shin�Roma. Increasing the dose of toxicant completely neutralized the protective effect of the drug.

When assessing the frequency of death is established that the introduction of the drug for 5 days and 1 day before the poisoning metafoam not affect the value of this index compared with the control group animals. Prophylactic use of the drug for 1 h before the injection of metaphase at a dose of 1 LD50completely prevented the death of animals. When you increase the dose of toxicant to 1.25 LD50registered a reduction in the frequency of death in the early period after exposure (up to 1 day), however further significant differences in this indicator from the control group were noted. With the introduction of metaphase in the dose of 1.5 LD50the prophylactic use of β-estradiol for 1 h before toxicity had no effect on the frequency of death of the experimental animals.

The introduction of β-estradiol for 20 min to poisoning metafoam at a dose of 1 LD50contributed to the prevention of destruction of animals throughout the observation period (15 days), at a dose of 1.25 LD50the probability of death was 17±17%, in the dose of 1.5 LD50- 83,3+17% (the differences with the control group are not significant).

The introduction of the drug when the first signs of intoxication warned the death of animals after poisoning metafoam at a dose of 1 LD50but when you increase the dose of toxicant killed all the ex�erimentale animals. It should be noted that only by the use of β-estradiol for 1 h and 20 min before the application of toxicant death of animals occurred significantly later than individuals in the control group.

Similar data were obtained when assessing the effectiveness of the prophylactic use of β-estradiol on the model of acute poisoning by other organophosphate - Malathion (table 3).

It is established that the introduction of the drug for 20 minutes before application of the poison to animals at a dose of 1 LD50increased NO50development of the first signs of intoxication, convulsions, warned the convulsions 1-4 degrees at 83,3±17% of the individuals of the group (differences from control are significant at p<0,05), and completely prevented the development of seizures 5 degrees (p<0.05) and mortality (p<0,05). In rats, which Malathion was introduced in doses of 1.25 LD50or 1.5 LD50increased NO50development of the first signs of poisoning, ET50the development of seizures and the occurrence of death (all differences were significant when compared with the control group). It should be noted that the introduction of β-estradiol for 20 min to poisoning by Malathion at a dose of 1.25 LD50almost completely prevented the development of seizures 5 degrees and significantly (p<0,05) reduced the frequency of death. When assessing the frequency and dynamics of death of the animals shown, �the introduction of β-estradiol in a dose of 100 mg/kg 20 min before poisoning Malathion significantly influenced the rate of mortality, reducing it only in the groups of animals that received the poison in doses of 1 LD50and 1.25 LD50(all differences were significant, p<0,05, when compared with the control group).

Thus, prophylactic administration of β-estradiol in a dose of 100 mg/kg for 20 min and 1 hour before poisoning metafoam and Malathion in the dose range up to 1,0-1,5 LD50helped reduce the severity of intoxication and frequency of death.

The data indicate that prophylactic administration of β-estradiol to acute poisoning by organophosphates contributed to a significant reduction in the severity of intoxication, severity of seizures and probability of death of the experimental animals.

Method of prevention of acute poisoning with organophosphates, wherein the prophylactically for 20-60 min to acute poisoning used β-estradiol.



 

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