THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY

The development of new antinociceptive agents and new approaches to pain relief based on potent non-narcotic analgesics is one of the most in demand and urgent directions of modern pharmacology. This work substantiates the choice of the clinically most relevant representative of non-narcotic analges...

Full description

Bibliographic Details
Main Authors: O. I. Rudko, E. A. Klimov, V. V. Sobolev, A. V. Sosnov, K. A. Rufanov, F. M. Semchenko
Format: Article
Language:Russian
Published: LLC Center of Pharmaceutical Analytics (LLC «CPHA») 2019-01-01
Series:Разработка и регистрация лекарственных средств
Subjects:
Online Access:https://www.pharmjournal.ru/jour/article/view/435
_version_ 1826569748707540992
author O. I. Rudko
E. A. Klimov
V. V. Sobolev
A. V. Sosnov
K. A. Rufanov
F. M. Semchenko
author_facet O. I. Rudko
E. A. Klimov
V. V. Sobolev
A. V. Sosnov
K. A. Rufanov
F. M. Semchenko
author_sort O. I. Rudko
collection DOAJ
description The development of new antinociceptive agents and new approaches to pain relief based on potent non-narcotic analgesics is one of the most in demand and urgent directions of modern pharmacology. This work substantiates the choice of the clinically most relevant representative of non-narcotic analgesics from the α2-adrenoreceptor agonist class - dexmedetomidine, which acts at low doses and demonstrates high therapeutic index for various modes of administration. An analgesic efficacy of dexmedetomidine in single intranasal administration of the original experimental pharmaceutical formulation was evaluated in models of acute thermal and visceral pain in laboratory animals (female outbred white mice). A pronounced dose-dependent analgesic effect of the dexmedetomidine preparation in the 10 and 50 μg/kg dosage was revealed in the test models of visceral pain. The analgesic effect of dexmedetomidine was accompanied by a dose-dependent sedative (but not anesthetic) effect in mice, with peak at 30 minutes for intranasal administration of 50 μg/kg of drug. In the doses used, dexmedetomidine did not exert any acute toxic effects in mice.
first_indexed 2024-04-10T01:40:15Z
format Article
id doaj.art-62addb1f82ba46c19305f98c809fa3cb
institution Directory Open Access Journal
issn 2305-2066
2658-5049
language Russian
last_indexed 2025-03-14T11:44:16Z
publishDate 2019-01-01
publisher LLC Center of Pharmaceutical Analytics (LLC «CPHA»)
record_format Article
series Разработка и регистрация лекарственных средств
spelling doaj.art-62addb1f82ba46c19305f98c809fa3cb2025-03-02T09:53:20ZrusLLC Center of Pharmaceutical Analytics (LLC «CPHA»)Разработка и регистрация лекарственных средств2305-20662658-50492019-01-0102236241435THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITYO. I. Rudko0E. A. Klimov1V. V. Sobolev2A. V. Sosnov3K. A. Rufanov4F. M. Semchenko5University Diagnostic Laboratory LLC; Lomonosov Moscow State University, Faculty of BiologyUniversity Diagnostic Laboratory LLC; Lomonosov Moscow State University, Faculty of BiologyUniversity Diagnostic Laboratory LLC; Centre of Theoretical Problems of Physico-Chemical Pharmacology, Russian Academy of SciencesFederal State Unitary Enterprise «State Pharmaceutical Plant» (FSUE «GosZMP»)Federal State Unitary Enterprise «State Pharmaceutical Plant» (FSUE «GosZMP»)Federal State Unitary Enterprise «State Pharmaceutical Plant» (FSUE «GosZMP»)The development of new antinociceptive agents and new approaches to pain relief based on potent non-narcotic analgesics is one of the most in demand and urgent directions of modern pharmacology. This work substantiates the choice of the clinically most relevant representative of non-narcotic analgesics from the α2-adrenoreceptor agonist class - dexmedetomidine, which acts at low doses and demonstrates high therapeutic index for various modes of administration. An analgesic efficacy of dexmedetomidine in single intranasal administration of the original experimental pharmaceutical formulation was evaluated in models of acute thermal and visceral pain in laboratory animals (female outbred white mice). A pronounced dose-dependent analgesic effect of the dexmedetomidine preparation in the 10 and 50 μg/kg dosage was revealed in the test models of visceral pain. The analgesic effect of dexmedetomidine was accompanied by a dose-dependent sedative (but not anesthetic) effect in mice, with peak at 30 minutes for intranasal administration of 50 μg/kg of drug. In the doses used, dexmedetomidine did not exert any acute toxic effects in mice.https://www.pharmjournal.ru/jour/article/view/435dexmedetomidinepain sensitivityanalgesiamiceintranasal administrationα₂-adrenomimetics
spellingShingle O. I. Rudko
E. A. Klimov
V. V. Sobolev
A. V. Sosnov
K. A. Rufanov
F. M. Semchenko
THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY
Разработка и регистрация лекарственных средств
dexmedetomidine
pain sensitivity
analgesia
mice
intranasal administration
α₂-adrenomimetics
title THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY
title_full THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY
title_fullStr THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY
title_full_unstemmed THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY
title_short THE STUDY OF EFFECTS OF THE INTRANASAL DEXMEDETOMIDINE ADMINISTRATION ON PAIN SENSITIVITY
title_sort study of effects of the intranasal dexmedetomidine administration on pain sensitivity
topic dexmedetomidine
pain sensitivity
analgesia
mice
intranasal administration
α₂-adrenomimetics
url https://www.pharmjournal.ru/jour/article/view/435
work_keys_str_mv AT oirudko thestudyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT eaklimov thestudyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT vvsobolev thestudyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT avsosnov thestudyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT karufanov thestudyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT fmsemchenko thestudyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT oirudko studyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT eaklimov studyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT vvsobolev studyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT avsosnov studyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT karufanov studyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity
AT fmsemchenko studyofeffectsoftheintranasaldexmedetomidineadministrationonpainsensitivity