According to modern concepts, Atropine, Ipratropia bromide are an exogenous antagonists of cholinergic receptors. The ability of ipratropium bromide to bind to holinoreceptors is explained by the presence in its structure of a fragment that is related to the molecule of an endogenous agonist-acetylcholine .
The main pharmacological feature of ipratropium bromide is its ability to block m-cholinergic receptors; it also acts (although much weaker) on n-holinoretseptors. Atropine is thus a non-selective blocker of m-cholinergic receptors. By blocking m-cholinergic receptors, it makes them insensitive to acetylcholine in the region of the endings of postganglionic parasympathetic (cholinergic) nerves. The effects of ipratropium bromide are opposite to the effects observed when the parasympathetic nerves are excited. The ipratropium of bromide the body is accompanied by a decrease in the secretion of salivary, gastric, bronchial, sweat glands (the latter receive sympathetic cholinergic innervation), pancreas, increased heart rate (due to reduced inhibitory action on the heart vagus nerve), a decrease in tone of smooth muscle organs (bronchi, abdominal organs, etc.) .
The effect of ipratropium bromide is more pronounced with increased vagus nerve tone. Apply M- holinoblokers for peptic ulcer of the stomach and duodenum, pylorospasm, cholecystitis, cholelithiasis, intestinal spasms and urinary tract, bronchial asthma, to reduce the secretion of salivary, gastric and bronchial glands, with bradycardia, developed as a result of increased vagus nerve tone. For pain associated with smooth muscle spasms, M-cholinoblockers are often administered together with analgesics (analgin, promedol, morphine, etc.). Due to the effect of atropine on the cholinergic systems of the brain, it has been proposed to use it in psychiatric practice for the treatment of psychoses (affective, paranoid, catatonic and other conditions) [1, 2]. The so-called atropunctata therapy involves the use of high doses of ipratropium bromide. However, the anti-inflammatory properties of M- holinoblokers not been studied.
The purpose of the study: to study the effect of M-holinoblokers on the phase of inflammation.
Materials and methods: the Antiexudative activity of Ipratropium bromide was determined by the difference in the volume of exudate in control and experimental animals. The drug was administered 1 hour before the experiment. To study the effect of the drug on the proliferative phase of inflammation, the “cotton pellet“ method proposed by Mejeg and co-authors was used (282). 1 hour after the drug was administered, sterile cotton balls weighing 5 mg were implanted into the subcutaneous tissue of the interscapular region of the back of rats under ether anesthesia. The drug was administered daily for 7 days. On day 8, the animals were slaughtered, cotton balls with the resulting granulation tissue were removed,their mass was determined in wet form , and then, dried to a constant weight at a temperature of 70° C, in dry form. The mass of the formed granulation tissue was determined by the mass difference between the dried granuloma and the implanted cotton ball (303). To simultaneously study the antiexudative and antiproliferative effects of the drug, the “pocket granuloma” method was used according to Selye ( 74, 80,131).
To do this, the rats ' hair was cut in the interscapular area and 20 ml of air was injected subcutaneously. Then 0.5 ml of 10% Croton oil was injected through the same needle. On day 8, the granuloma SAC was separated to determine the amount of exudate. The exudate was sucked out with a syringe, and then the mass of the granuloma bag was determined in a wet state, and after drying to a constant weight, in a dry state. Next, the amount of exudate was determined.
Results: This series of experiments was performed to determine the effect of ipratropium bromide on the formation of granulation tissue around a foreign object. By day 8 of the experiments, granulation tissue was formed around the cotton balls. The weight of wet swabs in control animals was 231.5±5.11 mg, in animals receiving the studied drug at a dose of 40 mg / kg 133.5±3.13 mg; respectively, and the antiproliferative effect was 42.3%.
Comparison drugs also inhibited the formation of granulation tissue, but only voltaren showed a pronounced antiproliferative effect.
When using the drug, the weight gain of the dry implant also decreased by 43.8%, respectively. In voltaren, these indicators are equal to 41.8%, respectively.
These data indicate that the studied drug has a pronounced antiproliferative activity.
Thanks to this series of experiments, it was possible to study both the antiexudative and antiproliferative effects of the studied drug.
The results showed that in animals of the control group, the amount of exudate in the granuloma SAC was on average 5.5±0.1 ml, in animals receiving the studied drug 3.3 ±0.076 ml, respectively). In voltaren, these data are equal to 3.7±0.084 ml, respectively. The wet weight of the granuloma bag was 1.585±0.02 g in the control group, and 1.05 ±0.03 g in the ipratropium bromide group, i.e. the decrease in the wet weight gain of the granuloma bag was 33.7%, respectively . For voltaren, this data was 41.9%.
The drug also significantly reduced the mass of the dry granuloma bag. So, if in the control group the indicator was equal to an average of 0.45 ±0.03 g, then in the M-holinoblokator group 0.31 ± 0.03 g.
Conclusions: Thus, we can conclude that M-holinoblokator has a pronounced anti-inflammatory effect, affecting both the exudative and proliferative phases of inflammation.
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- Tiganov A.S. Abuse of anticholinergics // Exogenous mental disorders., 2012.