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12was reached and the full epithelization of the cornea. Exophthalmos reduced on average by 3,1 ± 0,23mm, the eyesight keenness improved by 0,1 on average. Later in all cases because of absence of the full compensation process after 3 and 6 months anti relapse treatment was done: parabulbar injections, dexamethasone in combination with physiotherapy, diuretics and stimulating medicines.
Thus, performing of inner decompression of the patients at the stage of EOP decompensation on the background of a complex therapy with the use of physiotherapy allows obtaining significant reduction of exophthalmos and steady remission of the disease in prevailing number of cases.
Conclusions
1. Doing inner decompression of the orbit on the background of the complex therapy of EOP at the decompensation stage allows reducing exophthalmos by 6,6 ± 0,76 mm that twice exceeds the results of the pulse therapy with glucocorticosteroids.
2. The steady effect of the inner orbit decompression is preserved for a long time of most patients.
REFERENCES
1. Бровкина А.Ф. Внутренняя декомпрессия - реконструктивная операция при эндокринном экзофтальме.//Сборник научных трудов 3 Всероссийской школы офтальмологов, Москва 2004.- С 164-169.
2. Olivari N. Endocrine ophthalmopathy (surgical theatment). - Kaden Vergal. Heidelberg.-2001. - 120 p.
3. Бровкина А.Ф., Гусев Г.А. Способ хирургического лечения больных с эндокринной офтальмопатией в стадии декомпенсации, з. №2001108869/14 от 04.04.01; публ. 20.11.02.
STUDY OF LOCAL ANESTHETIC ACTIVITY OF NEW PYRIDINE DERIVATIVES
Kadirova. D. M., Smagulova G. S., Amirkulova М. K., students: Nagashibai A. K., Seitkamalova A. A
KazNMU named by S. D.Asfendiyarov, Almaty, Kazakhstan
Abstract. Despite certain achievements of domestic and foreign pharmacologists, chemists and clinicians in the field of creating of local anesthetics, one of the major problems of modern pharmacology are still searching and exploring new, more effective and less toxic substances with locally anesthetic properties. This is largely due to the fact that many of the traditional and modern local anesthetics are not without side effects, the phenomena of intolerance and often of low activity. Modern medicine highly requires such local anesthetics, which could ensure a sufficient depth of local anesthesia for a relatively long time. In connection with this the search for new compounds having advantages over the widely used anesthetics still remains relevant.
The purpose of this work. The search for compounds having certain advantages over existing local anesthetics in terms of duration of action, potency and toxicity on the model of conduction anesthesia.
Materials and methods of research. In the laboratory of chemistry of synthetic and natural medicinal substances JSC "Institute of Chemical Sciences" named A.B. Bekturov new compounds of piperidine derivatives under laboratory code MAV (local anesthetic substance): MAV-177, MAV-179, MAV-181, were synthesized. Experiments to study the conduction anesthesia been tested on rats by the modified method «tail flick». Determined: duration of total anesthesia and the total duration of the action. The activity of compounds and reference drugs was studied in a 1% solution. Each series of experiments carried out on animals. As a reference preparations were used novocaine, lidocaine and trimecaine.
The modified method of "tail-flick" of rats.
Tail flick method has been developed at the Department of Pharmacology of the St. Petersburg Medical University named after academician I.P. Pavlov. It allows to determine the speed of the onset of anesthesia, its depth, duration of complete anesthesia and the total duration of the anesthetic action of preparation.
The activity of compounds and reference preparations was studied in a 0.1% solution. Research was conducted on mongrel white male rats, weighing 200-250 grams.
The principle of the method is to record the latent period of tail-flick in the thermal impact on the middle part focused beam of light from the optoelectronic analgesimeter TF - 003 before and after anesthesia. Intensity of thermal nociceptive exposure has been adjusted so that the initial tail withdrawal response occurred with a latency period in the range 3-6 seconds. First the pain threshold was measured. Then made uniform injection root of the rats tail with four sides with a solution of the test compounds and reference drug in a volume of 1 ml. Control animals the same manner and in the same volume of physiological saline were administered. Irritation deposited on 1 cm distal to the injection site. After the introduction of the test substances and reference preparations tested again with a certain interval of time. Increased latency of the tail flick reflex in 2 times assessed as complete anesthesia. The compounds and reference preparations (procaine, lidocaine, trimecaine) were compared at the time of occurrence of anesthesia, duration of complete anesthesia and the total duration of the anesthetic action of preparation.
Results and discussion.
Of the data in the table it can be seen that all of the compounds have shown in varying degrees of activity in conduction anesthesia. Full anesthesia of highest duration of action provided MAV-181.
Duration of full anesthesia MAV-177 and MAV-179 is shorter than MAV-181.
In comparison the activity of the compounds in 1% solutions and preparations of comparison is shown that MAV-181 is slightly inferior to that trimecaine, MAV-177 and MAV-179 act shorter than it about 4.5.
On the ability to cause full anesthesia MAV-181 acts somewhat weaker than lidocaine. The activity of compounds MAV-177 and MAV-179 is lower than that of lidocaine approximately 6 and 6,5 times respectively.
In the analysis the dependence of studied compounds on the parameter of the total duration of action, they were divided into 2 groups.
MAV- 181, the representative of the first group, showed the most activity in this series of experiments.
The second group included the MAV-177 and MAV-179 operating less than last. Results of research testify that the MAV-181 operates more strongly than trimecaine, but this difference was not statistically significant. MAV-177, the compound of the second group concedes to trimecaine for the total duration of action, and MAV-179 is somewhat weaker than it.
In the 1% solutions MAV-181 is slightly inferior to lidocaine, activity MAB-177 and MAB-179 statistically significantly lower than that of lidocaine.
Indicator of total duration of action MAV-181 is higher than that of novocaine, however this difference was not statistically significant. In comparison the activity of the MAV-177 and MAV-179 with novocaine we see that they act somewhat weaker than the last.
Table 1. Activity and duration of action of 1% concentration of the compounds in conduction anesthesia
Compound, preparation 1 %
The duration of complete anesthesia, min. Duration of action, min.
MAV-177 11,6±2,11 p1 <0,001 p 2 <0,01 p, <0,01 20,0 ±3,17 p2 <0,02 p2 < 0,002 p, >0,05
MAV-179 10,8±2,72 p 1 <0,001 p2 <0,02 p, <0,002 32,8±2,4 p-1 >0,05 p2 <0,01 p, >0,05
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MAV-181 35,0±7,4 ^>0,05 p2>0,05 p^>0,05 67,5±6,4 ^>0,05 p2>0,05 p^>0,05
Trimecaine 47,3±8,4 56,9±12,8
Lidocaine 65,0±18,4 90,0±18,4
Novocaine 35,2±7,1 42,3±13,6
Notes: pi- correlation coefficient compared to trimecaine; p2 - compared to lidocaine; p3 -compared to novocaine.
Analyzing the results of the experiments can be concluded that the tested compounds have anesthetic effect. The most active compound of them is MAV-181, which has advantages over the others and can be recommended for further study.
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