scholarly journals Comparison of the Central and Peripheral Components of Action in Comprehensive Analgesic Activity of New Kappa-Agonist

2018 ◽  
pp. 32-35
Author(s):  
Viktor Batrakov ◽  
Darya Shamshina ◽  
Andrey Ivanov
Keyword(s):  
Analgesic Activity ◽  
Experimental Work ◽  
Analgesic Effect ◽  
Pain Syndrome ◽  
Chemical Mixture ◽  
Kappa Agonist ◽  
Urgent Task

Elimination of the pain syndrome is still an urgent task in various fields of medicine. Therefore, the problem of finding new effective and safe analgesics remains today one of the most important. The research is aimed at comparing the central and peripheral analgesic activity of chemical mixture KOR 205 in an experiment in rats. Based on the results of the experimental work, indicators of the maximum possible effect (MVE%) have been determined. The KOR 205 compound has a more pronounced central analgesic effect, compared with peripheral analgesic activity.

scholarly journals Effect of adjuvant drugs on the analgesic activity of opioid morphine analgesics and compound RU-1205

2021 ◽  
Vol 7 (3) ◽  
pp. 41-47
Author(s):  
Alexander A. Spasov ◽  
Olesya Iu. Grechko ◽  
Natalya V. Eliseeva ◽  
Yuliya V. Lifanova ◽  
Angelina N. Aleksandrenkova
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Opioid Analgesics ◽  
Benzodiazepine Receptor ◽  
Tail Flick ◽  
Opioid Agonist ◽  
Tail Flick Test ◽  
Kappa Agonist ◽  
Kappa Opioid Agonist ◽  
Probable Interaction

Introduction: Adjuvant medications can be used to increase the analgesic effect of opioid analgesics, reduce the manifestation of side effects, and also for premedication. This paper provides information on the effect of clonidine, haloperidol, metocloparmide, diazepam, midazolam on opioid analgesics: - morphine and the selective kappa-opioid agonist compound RU-1205. Materials and methods: A probable interaction between RU-1205, morphine and adjuvant drugs in pain behaviors was carried out on the model of somatogenic pain. 95 male mice received either RU-1205 (5 mg/kg, i.p.) and morphine (1 mg/kg, i.p.) separately or in combination with haloperidol (0.45 mg/kg, i.p.); midazolam (0.3 mg/kg, i.p.); diazepam (1 mg/kg, i.p.); metoclopramide (5 mg/kg, i.p.), and clonidine (1 mg/kg, i.p.). The analgesic effect was assessed by tail flick test. Registration of the latent period of the reaction was carried out 30, 60 and 90 minutes after the adjuvant drug administration. Results: When studying the interaction with morphine, it was found that clonidine, haloperidol and metoclopramide enhanced the effects; diazepam offset them, and midazolam had no affect on the analgesic properties. In the course of the studies, RU-1205 showed an increase in analgesic activity when combined with clonidine, a slight increase with midazolam, and a decrease when co-administered with diazepam. Haloperidol had no influence on the effect of RU-1205, while metoclopramide both potentiated and reduced the analgesic effect. Discussion: Pharmacodynamic and pharmacokinetic interactions of RU-1205 with an α2AR agonist, benzodiazepine receptor agonists, D2P antagonist, and σ-receptor blocker were established. Conclusion: The presented data make it possible to more accurately formulate ideas about the localization and action mechanism of the kappa-agonist of opioid receptors, the compound RU-1205.

Pain Syndrome, Markers of Bone Metabolism in Patients with Osteoarthritis, Approaches to Drug Therapy and the Impact of Obesity

2016 ◽  
pp. 26-35
Author(s):  
Oleksandr Kuryata ◽  
Anna Cherkasova
Keyword(s):  
Neuropathic Pain ◽  
Bone Metabolism ◽  
Clinical Efficacy ◽  
Functional Ability ◽  
Analgesic Effect ◽  
Pain Syndrome ◽  
Knee Joints ◽  
Osteocalcin Level ◽  
Positive Effects ◽  
The Impact

The objective: to assess the nature of pain in patients with osteoarthritis, the impact of obesity on the clinical efficacy of treatment of osteoarthritis (OA) and dynamics of bone metabolism markers. Patients and methods. The research included 150 patients with OA, who were divided into two groups, according to the receiving therapy. Patients of the main group – received diacerein (drug «Flexirin» PC «Kyiv Vitamin Factory») and patients of control group – received only nonsteroidal anti1inflammatory drugs (NSAIDs). Results. The prevalence of neuropathic pain component in patients with OA was 64,7%, among which 80,7% use NSAIDs as an analgesic therapy. Obesity in patients with OA was associated with significantly higher levels of pain from the side of knee joints and higher degree of stiffness according to WOMAC index. The results of the study demonstrated a direct moderate correlation (R = 0,49; p = 0,04) between PICP level and the severity of pain at physical load from the side of hands and hip joints. The therapy by diacerein within 3 months resulted in a reliable decrease of pain syndrome intensity from the side of all articular zones, unlike to isolated NSAIDs use, where a reliable analgesic effect was demonstrated only from the side of knee joints. Obesity in patients with OA led to a significant decrease in clinical efficacy of therapy in point of functional status of the joints. Conclusions. Neuropathic pain is quite common among patients with OA, which at the same time is associated with the lack of patient’s awareness about possible risks during NSAID’s use. Medical treatment by diacerein (drug “Flexirin”) causes stability of osteocalcin level, in contrast to the isolated NSAIDs use, where priority changes have been demonstrated against osteocalcin level decrease. The use of diacerein also resulted to additional positive effects from the side of zonal prevalence of analgesic effect and improving of functional ability of joints. Obesity in patients with OA was associated with a reliable increase of pain level intensity from the side of knee joints and the higher degree of functional limitation, causing at the same time, reduction of clinical efficacy of therapy in point of achieving analgesic effect and improving functional ability of joints.

scholarly journals EVALUATION OF ANALGESIC ACTIVITY OF MURRAYA KOENIGII AND CORIANDRUM SATIVUM LEAVES EXTRACT IN ANIMAL MODEL.

2018 ◽  
Vol 11 (1) ◽  
pp. 328
Author(s):  
Kartik Salwe J ◽  
Mirunalini R ◽  
Jervin Mano ◽  
Manimekalai K
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Coriandrum Sativum ◽  
Control Group ◽  
Tail Flick ◽  
Murraya Koenigii ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Soxhlet Apparatus

 Objective: The objective of the study was to investigate the analgesic activity of hydroalcoholic extract of Murraya koenigii and Coriandrum sativum leaves and compared it with standard drug in an animal model.Methods: Hydroalcoholic extracts of M. koenigii and C. sativum leaves were obtained using Soxhlet apparatus. The central analgesic property was screened by hot plate method in mice and tail flick method in rats. The pain reaction time (PRT) was measured at 30, 60, and 120 min. The peripheral analgesic activity was evaluated by acetic acid induced writhing in mice.Results: In hot plate method M. koenigii leaves extract at both doses and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. C. sativum leaves extract showed significant increase in PRT only at 60 and 120 min compared to control group. In tail flick method M. koenigii leaves extract at both doses, higher dose of C. sativum leaves extract and tramadol showed significant increase in PRT at 30, 60, and 120 min compared with control group. Higher dose of M. koenigii leaves extract (200 mg/kg) was comparable with standard drug tramadol in both the methods. M. koenigii leaves extract at both dose showed significant reduction in the number of writhing but C. sativum leaves extract failed to show any significant reduction in the number of writhing compared with control. Higher dose of M. koenigii leaves extract was comparable with standard drug tramadol.Conclusion: M. koenigii leaves extract showed both peripheral and central analgesic effect while C. sativum leaves extract showed only peripheral analgesic effect.

scholarly journals Analgesic Activity of the Kappa Opioid Receptor Agonist RU-1205 in Rats

2018 ◽  
Vol 3 (2) ◽  
pp. 13 ◽  
Author(s):  
AA Spasov ◽  
OY Grechko ◽  
DM Shtareva ◽  
AI Raschenko ◽  
Natalia Eliseeva ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Analgesic Activity ◽  
Analgesic Effect ◽  
Physical Dependence ◽  
Receptor Activation ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test

Introduction: Opioid analgesics are the most efficient and widely used drugs for the management of moderate to severe pain. However, side effects associated with mu receptor activation, such as respiratory depression, tolerance and physical dependence severely limit their clinical application. Currently, the kappa-opioid system is the most attractive in terms of the clinical problem of pain, because kappa-agonists do not cause euphoria and physical dependence. The purpose of this study was to evaluate the antinociceptive effect of the novel compound - RU-1205. Methods: The analgesic activity of RU-1205 was studied on nociceptive models that characterize the central and peripheral pathways of pain sensitivity (hot plate test, electrically induced vocalisation, formalin test, writhing test). Results: RU-1205 exhibited highly potent antinociceptive effects in rodent models of acute pain with ED50 values of 0.002 - 0.49 mg /kg. Pretreatment with the κ-opioid receptor antagonist norBinaltorphimine significantly attenuated the analgesic activity of investigated substance in a hot plate test. Conclusions: It was established that the compound shows a significant dose-dependent central and peripheral analgesic effect. It was assumed kappa-opioidergic mechanism of analgesic effect of RU-1205.

STUDY OF SPECIFIC PHARMACOLOGICAL ACTIVITY OF SODIUM SALT (4-О-Β-GLUCOPYRANOSYLOXY)-BENZOIC ACID

2016 ◽  
Vol 78 (6-8) ◽  
Author(s):  
Smirnov Ivan ◽  
Murashko Tatyana ◽  
Ivanov Alex ◽  
Bondarev Alex ◽  
Udut Vladimir
Keyword(s):  
Benzoic Acid ◽  
Analgesic Activity ◽  
Sodium Salt ◽  
Analgesic Effect ◽  
Inflammatory Diseases ◽  
Peptic Ulcers ◽  
Chronic Inflammatory Diseases ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Chronic inflammatory diseases of various genesis are prevalent today. Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used to treat pain and inflammation, but their long-term use is associated with complications in the gastrointestinal tract, including peptic ulcers. We synthesized a molecule of sodium salt (4-О-β-glucopyranosyloxy)-benzoic acid. This substance has diuretic and anti-inflammatory activities. It should be noted that most of NSAIDs has analgesic effect. In this connection, the aim of this study was to evaluate the analgesic activity of sodium salt (4-О-β-glucopyranosyloxy)-benzoic acid. We studied analgesic effect in the test “acetic writhing”. Sodium salt (4-О-β-glucopyranosyloxy)-benzoic acid significantly reduces the number of writhing by 14 units during the experiment, as an alternative criterion percent of animals with analgesia was 42.6%. Thus, in the test "acetic writhing" revealed the presence of the analgesic activity have developed drug average severity. 

scholarly journals ASSESSMENT OF ANALGESIC ACTIVITY OF NELUMBO NUCIFERA FRUIT ETHANOL EXTRACT

2019 ◽  
pp. 1-5
Author(s):  
MUHAMMAD ALI RAJPUT ◽  
TABASSUM ZEHRA ◽  
FIZZAH ALI ◽  
GUNESH KUMAR
Keyword(s):  
Analgesic Activity ◽  
Analgesic Effect ◽  
Research Work ◽  
Ethanol Extract ◽  
Nelumbo Nucifera ◽  
Herbal Remedies ◽  
Tail Flick ◽  
Traditional Use ◽  
Tail Flick Test ◽  
Pathway Inhibition

Objective: Utilization of herbal remedies rich in flavonoids and vitamins have increased significantly these days to treat various disorders, thus existing research work encircled to appraise the analgesic effect of Nelumbo nucifera fruit (NNF) for evaluating its traditional use pharmacologically in disorders which are associated with pain and inflammation. Methods: Central analgesic activity in mice was assessed by tail flick test and the latency time i.e. the removal of tail from the stimulus was recorded. Similarly acetic acid induced writhing test was also conducted for the assessment of peripheral analgesic effect in mice and number of writhes was counted along with percent inhibition of writhes. Results: In tail flick test the peek anti-nociceptive effect at all doses of fruit was observed at 90 min. However, the percentage of tail elongation time was highest at a dose of 200 mg/kg i.e. 82% at 90 min. Number of writhes was highly significantly reduced at all doses of NNF but maximum effects were observed at dose 200 mg/kg as compared to control, indicating 48.41 % inhibition of writhes. Conclusion: NNF have exhibited strong analgesic effect in both animal models, which may be connected with the synergistic actions of flavonoids, saponins and tannins on arachidonic acid pathway inhibition. Hence NNF seems to have a great potential in disorders associated with pain but more experimental trials in this field are required to confirm these findings.

Evaluation of the Analgesic Effect of Combination Therapy on Chronic Plantar Pain Through the Myofascial Trigger Points Approach

2018 ◽  
Vol 108 (1) ◽  
pp. 27-32 ◽  
Author(s):  
Rocío Melero-Suárez ◽  
José Antonio Sánchez-Santos ◽  
Gabriel Domínguez-Maldonado
Keyword(s):  
Combination Therapy ◽  
Analgesic Effect ◽  
Myofascial Pain ◽  
Pressure Pain Threshold ◽  
Pain Syndrome ◽  
Myofascial Pain Syndrome ◽  
Trigger Points ◽  
Adductor Muscle ◽  
Rank Test ◽  
Myofascial Trigger Points

Background: Closely related pathologic disorders sometimes manifest with the same symptoms, making for a complex differential diagnosis. This is the situation in plantar fasciitis (PF) and myofascial pain syndrome (MPS) with myofascial trigger points (MTPs) in the sole of the foot. This research assessed the analgesic effect on plantar pain of combination therapy with interferential current stimulation therapy (ICST), treating MTPs in the great toe adductor muscle and the short flexor muscles of the toes in patients whose diagnosis was compatible with PF or MPS. Methods: This study included 22 feet of 17 patients with a diagnosis compatible with PF or MPS with MTP. Participants received combination therapy with ICST for 15 sessions, and the decrease in pain was measured with an algometer and the visual analog scale. Both measurements were taken before and after every fifth session. The pressure pain threshold (PPT) results obtained with the Student t test and the pain intensity perception (PIP) results obtained with the Wilcoxon signed rank test were analyzed by comparing the measurements taken before the treatment and after the fifth, tenth, and 15th sessions. Results: The decrease in PIP was significant after the fifth, tenth, and 15th sessions (P < .001). The increase in PPT was also significant after the fifth (P = .010), tenth (P = .023), and 15th (P = .001) sessions (P < .05). Conclusions: The suggested combination therapy of ultrasound with ICST is clinically significant for reducing plantar pain after 15 treatment sessions, with a 6.5-point reduction in mean PIP and a 4.6-point increase in PPT.

scholarly journals Pharmacokinetic and analgesic properties of the injectable dosage form of a new imidazobenzimidazole derivative RU-1205 with kappa agonist activity

2015 ◽  
Vol 61 (5) ◽  
pp. 636-639 ◽  
Author(s):  
A.A. Spasov ◽  
L.A. Smirnova ◽  
O.U. Grechko ◽  
A.I. Raschenko ◽  
D.M. Shtareva ◽  
...  
Keyword(s):  
Analgesic Effect ◽  
Dosage Form ◽  
Subcutaneous Administration ◽  
Relative Bioavailability ◽  
Agonist Activity ◽  
Hot Plate ◽  
Kappa Agonist ◽  
Pharmacokinetic Properties ◽  
Injectable Dosage

Pharmacokinetic properties of imidazobenzimidazole derivative compound RU-1205 were investigated after subcutaneous administration to rabbits as a substance and a dosage form (lyophilisates for injection) at a dose of 25 mg/kg. The lyophilisate was characterized by high values of the relative bioavailability. In tests, the “hot plate” and “vinegar cramps” the dosage form and the substance exhibited the same analgesic effect.

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