Zaychenko G. V., Stakhorskaya M. A., Faizullin A. V.

CLINICAL AND EXPERIMENTAL MEDICINE

Scentific article

Objective – study of topical anaesthetic action of combined rectal cream under spontaneous and inflammatory hyperalgesia models in rats. Object and methods. The investigated drug contains as active components diltiazem, lidocaine and methyluracil, and is proposed for the treatment of anal fissures. As a reference drug, a monocomponent rectal ointment containing lidocaine in an equivalent amount and having an identical ointment base was used. Topical anaesthetic action of investigated drugs under spontaneous and induced pain reactions was estimated on the pain threshold. Pain threshold was determined using the algesimeter Plantar test Ugo Basile 7370 (2002) when the infrared ray was focused on a foot of rats. Inflammatory hyperalgesia was caused by subplantation of a 2% aqueous solution of phormalin in a volume of 0.1 ml. Results. It has been established that under spontaneous hyperalgesia hyperalgesia models, the combined rectal cream shows a pronounced analgesic (topical anaesthetic) activity. A high anaesthetic effect was detected after 5 minutes after application of combined rectal cream and monocomponent rectal ointment containing lidocaine to the hind limb in rats, while the pain threshold increased by 37% and 32% respectively. A comparative analysis of the values of pain threshold showed that the combined rectal cream and monocomponent rectal ointment containing lidocaine were equivalent to analgesic (topical anaesthetic) action. Similar results were recorded by the rate of development of anesthetic effect. Further research of the topical anaesthetic effect of combined rectal cream and monocomponent rectal ointment containing lidocaine was carried out under the model of inflammatory hyperalgesia. It was established that in the application of combined rectal cream, after 30 minutes after administration of formalin (20 minutes after application of cream), pain threshold increased by 91.5% and remained significantly higher (by 19-118%) compared with animals in the control group. Monocomponent rectal ointment containing lidocaine also significantly increased pain threshold (by 67.3%) in 30 minutes after the introduction of formalin (20 minutes after application of the ointment). In animals treated with monocomponent rectal ointment containing lidocaine, pain threshold was significantly higher for all other observation periods – by 19-118% compared to control animals. Consequently, monocomponent rectal ointment containing lidocaine has a long analgesic effect – more than 5 years. Thus, the combined rectal cream is characterized by a significant long-lasting analgesic (topical anaesthetic) effect – more than 5 hours. By analgesic activity, the combined rectal cream has some advantage over a monocomponent rectal ointment containing lidocaine within the first 30 minutes after the induction of hyperalgesia with formalin. In addition, under spontaneous and inflammatory hyperalgesia models, it is established that a combined rectal cream does not actually differ from a reference drug – a monocomponent rectal ointment containing lidocaine, neither in strength nor in duration and in the rate of onset of topical anesthetic action. Conclusions. The results of the carried out researches can serve as an experimental substantiation of the composition of the investigated agent and testify to the expediency of its further study.

chronic anal fissure, rectal cream, topical anesthetic action

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«Bulletin of problems biology and medicine» Issue 4 Part 3 (141), 2017 year, 133-136 pages, index UDK 615.24:616.352

10.29254/2077–4214–2017–4–3–141–133-136