scholarly journals Involvement of serotonergic, noradrenergic and gabaergic systems in the antinociceptive effect of a ketamine-magnesium sulfate combination in acute pain

2018 ◽  
Vol 68 (1) ◽  
pp. 108-118 ◽  
Author(s):  
Savić Vujović Katarina ◽  
Vučković Sonja ◽  
Stojanović Radan ◽  
Divac Nevena ◽  
Medić Branislava ◽  
...  
Keyword(s):  
Magnesium Sulfate ◽  
Acute Pain ◽  
Antinociceptive Effect ◽  
Nmda Antagonist ◽  
Anion Channel ◽  
Immersion Test ◽  
Nmda Receptor Antagonist ◽  
Albino Rats ◽  
Dependent Manner ◽  
Tail Immersion

Abstract Ketamine and magnesium can interact in additive, supra-additive and antagonistic manners in analgesia or anesthesia. Ketamine is a non-competitive NMDA receptor antagonist. Magnesium is an endogenous non-competitive NMDA antagonist that causes anion channel blockade in a dose-dependent manner. It has been established that ketamine and magnesium interact synergistically in the tail-immersion test in rats. To determine the role of serotonergic, GABAergic and noradrenergic systems in analgesia induced by the ketamine-magnesium sulfate combination. Experiments were performed on male Wistar albino rats (200-250 g). Antinociception was evaluated by the tail-immersion test. Methysergide (0.5 and 1 mg/kg, sc) administered alone did not affect nociception in rats. Methysergide (0.5 and 1 mg/kg, sc) antagonized the antinociceptive effect of the ketamine (5 mg/kg)-magnesium sulfate (5mg/kg) combination. Bicuculline (0.5 and 1 mg/kg, sc) given alone did not change the threshold to thermal stimuli in rats. Bicuculline (0.5 and 1 mg/kg, sc) antagonized the antinociceptive effect of the ketamine (5 mg/kg)-magnesium sulfate (5 mg/kg) combination. Yohimbine (0.5, 1 and 3 mg/kg, sc) applied alone did not change nociception. Yohimbine at a dose of 0.5 mg/kg did not influence the effect of ketamine (5 mg/kg)-magnesium sulfate (5 mg/kg), while yohimbine at doses of 1 and 3 mg/kg antagonized the antinociceptive effect of this combination. Serotonergic, noradrenergic and GABAergic systems participate, at least in part, in the antinociceptive effect of the ketamine-magnesium sulfate combination in acute pain in rats.

Study of the Interactions Between Magnesium, Ketamine and Morphine on Acute Nociception in Rats

2017 ◽  
Vol 41 (S1) ◽  
pp. S708-S709
Author(s):  
K. Savic Vujovic ◽  
A. Vujovic ◽  
S. Vuckovic ◽  
B. Medic ◽  
M. Prostran
Keyword(s):  
Magnesium Sulfate ◽  
Magnesium Sulphate ◽  
Wistar Rats ◽  
Antinociceptive Effect ◽  
Immersion Test ◽  
Synergistic Interaction ◽  
Tail Immersion ◽  
Male Wistar Rats ◽  
Competing Interest ◽  
First Time

ObjectivesStudy is aimed at evaluating the effects of ketamine and magnesium sulphate on acute nociceptive pain in rats and examination whether magnesium sulfate added to ketamine or morphine-ketamine combination produces higher level of analgesia.MethodsAnalgesic activity was assessed by tail-immersion test in male Wistar rats (200–250 g).ResultsMagnesium sulfate (2.5–60 mg/kg, s.c.) and ketamine (2.5-30 mg/kg, i.p.) given alone did not produce any effect on antinociception. However, there is a synergistic interaction between ketamine (2.5, 5 and 10 mg/kg) and magnesium sulfate (5 mg/kg). Both ketamine and magnesium sulfate, as well as their combination potentiated the antinociceptive effect of morphine (2.6 mg/kg, i.p.).ConclusionThis study revealed potentiation of ketamine and morphine-ketamine combination by magnesium sulphate in tail-immersion test in rats with higher activity when ketamine is given before magnesium sulfate. It is first time to demonstrate the synergistic interaction between magnesium sulphate and ketamine in lowering body temperature and in antinociception with statistical confirmation.Disclosure of interestThe authors have not supplied their declaration of competing interest.

scholarly journals Bioactivities of the ethanol extract from Ageratum fastigiatum branches: antioxidant, antinociceptive and anti-inflammatory

2016 ◽  
Vol 88 (3) ◽  
pp. 1471-1484
Author(s):  
GLAUCIEMAR DEL-VECHIO-VIEIRA ◽  
BRUNA C.S. SANTOS ◽  
MARIA SILVANA ALVES ◽  
AÍLSON L.A. ARAÚJO ◽  
CÉLIA H. YAMAMOTO ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Folk Medicine ◽  
Reducing Power ◽  
Ethanol Extract ◽  
Immersion Test ◽  
Significant Inhibition ◽  
Paw Edema ◽  
Hot Plate ◽  
Tail Immersion ◽  
Anti Inflammatory

ABSTRACT The present study was designed to investigate the antioxidant, antinociceptive and anti-inflammatory activities of the ethanol extract from Ageratum fastigiatum branches. Phytochemical screening and total phenol and flavonoid contents were determined. The antioxidant activity was assessed by 2,2-diphenyl-1-pycrilhydrazin (DPPH) and iron reducing power methods. The antinociceptive effect was evaluated using the acetic acid-induced writhing, formalin, hot plate and tail immersion assays; while the carrageenan-induced paw edema and pleurisy tests were performed to examine the anti-inflammatory activity against acute inflammation. The extract revealed the presence of flavonoids, tannins, coumarins, terpenes, sterols and saponins. Expressive levels of total phenols and flavonoids and a promising antioxidant effect were quantified. At the doses of 50, 100 and 200 mg/kg, the extract inhibited the writhing, reduced both phases of paw licking time and increased the reaction time on the hot plate. In the tail immersion test, the extract (50, 100 and 200 mg/kg) caused a significant inhibition of pain. In these doses, the paw edema, exudate volume and leucocyte mobilization were significantly reduced. These results suggest that A. fastigiatum can be an active source of substances with antioxidant, antinociceptive and anti-inflammatory activities, adding scientific support to the appropriate use in the Brazilian folk medicine.

scholarly journals A comparative study of antinociceptive effect of paroxetine with pethidine in acute pain in albino rats

2017 ◽  
Vol 6 (7) ◽  
pp. 1728
Author(s):  
Manju Gari ◽  
Kumari Ranjeeta ◽  
Lakhan Majhee ◽  
Akhilesh Kumar ◽  
Sumit Kumar Mahato
Keyword(s):  
Acute Pain ◽  
Water Immersion ◽  
Antinociceptive Effect ◽  
Warm Water ◽  
Albino Rats ◽  
Thermal Method ◽  
Average Weight ◽  
Tail Flick ◽  
Immersion Method ◽  
Standard Drug

Background: Pain is the most common reason patients seek medical care. Increased level of monoamines (serotonin and norepinephrine) in synaptic clefts lead to changes in pain threshold and induce antinociception. The study was carried out to evaluate antinociceptive effect of paroxetine in albino rats and to probe into its possible mechanism of action. The study was carried out to evaluate anti-nociceptive effect of paroxetine in albino rats.Methods: Male Albino rats of average weight 150-240gms were used. The drugs used were paroxetine 5mg/Kg, pethidine 5mg/kg (standard drug). Anti-nociceptive effect tested by using thermal method i.e. Tail flick response and Tail warm water immersion method.Results: In this study, Anti-nociceptive effect of respective drugs were measured by using two methods i.e. tail flick test and tail warm water immersion method at 0 min., 30 min., 60 min. and 90min.after administration of drugs. Reaction time started to increase from baseline at 0 min. and peak effect was seen at 60 min. then it started to decrease at 90 min. in almost all the groups except in control group.Conclusions: Paroxetine have significant analgesic effect in acute pain, which may be mediated via central and peripheral mechanisms. Efficacy of Paroxetine is almost equal to that of standard drug pethidine in acute pain management.

scholarly journals Quercetin action on pain modulation/ Ação da quercetina sobre a modulação da dor

2021 ◽  
Vol 7 (4) ◽  
pp. 43616-43634
Author(s):  
Maria Elvira Ribeiro Cordeiro ◽  
Flávio Klinpovous Kerppers ◽  
Luiza Ferreira Cunha ◽  
Ketllin Bragnholo ◽  
Luana Rodrigues Vasconcelos ◽  
...  
Keyword(s):  
Antinociceptive Effect ◽  
Immersion Test ◽  
Positive Control ◽  
Pain Modulation ◽  
Antinociceptive Activity ◽  
Formalin Injection ◽  
Immersion Method ◽  
Cholinergic Pathways ◽  
Cholinergic Pathway ◽  
Tail Immersion

Background: Quercetin is a flavonoid widely found in plant kingdom and target of studies in pharmacological area due to its potent antinociceptive effect compared to analgesics used in conventional therapies. The aim was to evaluate its antinociceptive activity and antinociception mechanism. Methods: For this, 40 Norvegicus Wistar rats were used, divided into 4 groups: Q50 (treated with quercetin 50 mg/Kg), Q100 (treated with quercetin 100 mg/Kg), Q500 (treated with quercetin 500 mg/Kg) and Positive control (PC) without quercetin treatment), who were submitted through the pain induction methods by tail immersion and formalin in the first step to assess antinociceptive action and in the second step, tail immersion method receiving antagonists from opioid, cholinergic and nitric oxide - L-arginine to evaluate the action mechanism. Results: Quercetin antinociceptive activity was verified at the dose of 50 mg/kg and 100 mg/kg in tail immersion test after formalin injection, with better performance at the dose of 50 mg/kg. There were no statistically significant results in paw opening and capsaicin tests. Quercetin demonstrated a possible influence on opioid and cholinergic pathway, which was not observed on the nitric acid - L-arginine pathway in view of parameters tested. Conclusion: Quercetin performed the best antinociceptive activity at a dose 50 mg/kg and there was a possible influence on opioid and cholinergic pathways.

scholarly journals Antinociceptive Effect of the Ethanol Leaf Extract of Balanites aegyptiaca Linn in Albino Rats

2020 ◽  
Vol 27 (2) ◽  
pp. 39-46
Author(s):  
O.A. Sodipo ◽  
J. Yakubu ◽  
A.M. Dungus ◽  
B. Wampana
Keyword(s):  
Acute Toxicity ◽  
Chemical Constituents ◽  
Antinociceptive Effect ◽  
Ethanol Extract ◽  
Albino Rats ◽  
Balanites Aegyptiaca ◽  
Hot Plate ◽  
Tail Immersion ◽  
Anti Inflammatory ◽  
Dose Dependent

Balanites aegyptiaca is a medicinal plant that has been used in a variety of folk medicines in India and Africa for the treatment of different ailments such as syphilis, jaundice, liver and spleen problems, epilepsy, yellow fever. This research aimed at investigating the phyt ochemical constituents, acute toxicity, anti inflammatory and antinociceptive activities of the ethanol extract of Balanites aegyptiaca (EEBA) leaves. The plant material was extracted using ethanol as solvent. The dried ethanol extract was screened for the presence of phytochemicals; Acute toxicity (LD50) was  determined using Lorke’s method while anti inflammatory and antinociceptive activities were evaluated using hot plate and tail immersion methods in albino rats. Results of the study revealed that phyto chemical constituents such as flavonoids, carbohydrates, saponins and glycosides were found in the EEBA, intraperitoneal LD 50 of 2154 mg/kg shows the substance is non toxic. The EEBA produced significant (p <0.05) and dose dependent anti inflammatory and a ntinociceptive activities at all test doses (200, 400 and 600 mg/kg). The presence of the phytochemicals detected might be responsible for the demonstrated anti inflammatory and antinociceptive activities in the plant extract. Keywords: Phytochemical, Anti inflammatory, Antinociceptive , Balanites aegyptiaca

The Analgesic Efficacy of Ketamine-Magnesium Combination is Influenced by the Order of Medication Administration

2016 ◽  
Vol 33 (S1) ◽  
pp. S503-S503
Author(s):  
K. Savic Vujovic ◽  
S. Vuckovic ◽  
A. Vujovic ◽  
M. Prostran
Keyword(s):  
Nmda Receptor ◽  
Magnesium Sulphate ◽  
Analgesic Efficacy ◽  
Medication Administration ◽  
Immersion Test ◽  
Nmda Receptor Antagonist ◽  
Nociceptive Pain ◽  
Tail Immersion ◽  
Male Wistar Rats ◽  
Competing Interest

IntroductionMagnesium is an endogenous voltage-dependent NMDA receptor channel blocker and ketamine is a non-competitive NMDA receptor antagonist. Magnesium may potentiate the effect of ketamine in analgesia and anaesthesia, but may also interact in an opposing manner. This study aimed at evaluating type of the interaction between magnesium sulphate and ketamine administered systemically in rats with an acute nociceptive pain (tail-immersion test).Materials and methodsAnalgesic activity was assessed by tail-immersion test in male Wistar rats (200-250 g). The distal 5 cm of the tail was immersed in a warm water bath (55 ± 0.5 °C) and the time for tail-withdrawal was measured as response latency.ResultsMagnesium sulphate (2.5–30 mg/kg, s.c.) and ketamine (2.5-30 mg/kg, i.p.) administered alone did not produce any effect. However, significant antinociception (synergistic interaction) was revealed at the following doses of ketamine: magnesium sulphate of 5:5 mg/kg, 2.5:5 mg/kg and 10:5 mg/kg. The effect was not dose-dependent, and a greater response was obtained when ketamine was administered before magnesium sulphate.ConclusionsThis study revealed that (1) magnesium sulphate and ketamine given alone were not effective against acute nociceptive pain in rats, but (2) a combination of both drugs resulted in synergistically inhibited nociception, (3) which occurred only at selected low doses and proportions of the medications in a combination and (4) suggested the importance of the order of drug administration.Disclosure of interestThe authors have not supplied their declaration of competing interest.

scholarly journals Excitatory postsynaptic potentials in rat neocortical neurons in vitro. III. Effects of a quinoxalinedione non-NMDA receptor antagonist

1990 ◽  
Vol 64 (4) ◽  
pp. 1282-1290 ◽  
Author(s):  
J. J. Hablitz ◽  
B. Sutor
Keyword(s):  
Nmda Receptor ◽  
Action Potentials ◽  
Nmda Antagonist ◽  
Nmda Receptor Antagonist ◽  
Cortical Layer ◽  
Bipolar Electrode ◽  
Dependent Manner ◽  
Excitatory Postsynaptic Potentials ◽  
Postsynaptic Potentials

1. Intracellular microelectrodes were used to obtain recordings from neurons in layer II/III of rat frontal cortex. A bipolar electrode positioned in layer IV of the neocortex was used to evoke postsynaptic potentials. Graded series of stimulation were employed to selectively activate different classes of postsynaptic responses. The sensitivity of postsynaptic potentials and iontophoretically applied neurotransmitters to the non-N-methyl-D-asparate (NMDA) antagonist 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) was examined. 2. As reported previously, low-intensity electrical stimulation of cortical layer IV evoked short-latency early excitatory postsynaptic potentials (eEPSPs) in layer II/III neurons. CNQX reversibly antagonized eEPSPs in a dose-dependent manner. Stimulation at intensities just subthreshold for activation of inhibitory postsynaptic potentials (IPSPs) produced long-latency (10 to 40-ms) EPSPs (late EPSPs or 1EPSPs). CNQX was effective in blocking 1EPSPs. 3. With the use of stimulus intensities at or just below threshold for evoking an action potential, complex synaptic potentials consisting of EPSP-IPSP sequences were observed. Both early, Cl(-)-dependent and late, K(+)-dependent IPSPs were reduced by CNQX. This effect was reversible on washing. This disinhibition could lead to enhanced excitability in the presence of CNQX. 4. Iontophoretic application of quisqualate produced a membrane depolarization with superimposed action potentials, whereas NMDA depolarized the membrane potential and evoked bursts of action potentials. At concentrations up to 5 microM, CNQX selectively antagonized quisqualate responses. NMDA responses were reduced by 10 microM CNQX. D-Serine (0.5-2 mM), an agonist at the glycine regulatory site on the NMDA receptor, reversed the CNQX depression of NMDA responses.(ABSTRACT TRUNCATED AT 250 WORDS)

scholarly journals Antinociceptive evaluation of conventional anticonvulsant with conventional analgesics on pain model of albino rats and mice

2018 ◽  
Vol 6 (3) ◽  
pp. 790
Author(s):  
Ruchika Agarwal ◽  
Saurabh Kansal
Keyword(s):  
Chronic Pain ◽  
Acute Pain ◽  
Formalin Test ◽  
Visceral Pain ◽  
Diclofenac Sodium ◽  
Antinociceptive Effect ◽  
Albino Rats ◽  
Second Phase ◽  
Writhing Test ◽  
Rats And Mice

Background: Pain is one of the most common presentations of any disorder and needs immediate and appropriate attention of the treating physician. As pain syndrome involves a variety of etiopathogenesis and temporal domains, management of pain as such requires consideration of many factors that may dictate appropriate therapeutic management. Carabmazepine is an established drug for trigeminal neuralgia while Gabapentin has been tried in postoperative pain but its effectiveness per se and when compared to conventional analgesics needs to be evaluated.Methods: The present study was planned to study the analgesic effects of Gabapentin in various pain models like writhing and formalin test and to compare it with conventional analgesics like Diclofenac sodium and Tramadol in various acute pain models.Results: This study has been carried out in department of Pharmacology, HIMS, Dehradun, for evaluation of Gabapentin for its antinociceptive effect in rats and mice. In the writhing test, a reduction in number of writhes, though insignificant, was found in the Gabapentin pre-treatment group. However, in the first phase of Formalin test which is characterized by licking and biting, Gabapentin produced no significant effect in comparison to control values. In the second phase of leg raising (LR), all three drugs, i.e. Gabapentin and the two positive controls i.e. diclofenac and tramadol produced significant decrease (p< 0.05) in episodes when compared to the control group.Conclusions: Hence the result conclude that Gabapentin could be an effective analgesic drug in visceral and chronic pain in humans but not in acute pain as first phase of formalin test is model of acute and second phase denote chronic pain while writhing test is a model of visceral pain.

Hexagonal boron nitride nanoparticles trigger oxidative stress by modulating thiol/disulfide homeostasis

2021 ◽  
pp. 096032712110028
Author(s):  
F Kar ◽  
İ Söğüt ◽  
C Hacıoğlu ◽  
Y Göncü ◽  
H Şenturk ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Boron Nitride ◽  
Hexagonal Boron Nitride ◽  
Chemical Properties ◽  
Heart Tissue ◽  
Albino Rats ◽  
Dependent Manner ◽  
Tissue Samples ◽  
Boron Nitride Nanoparticles

Background: Hexagonal boron nitride nanoparticles (hBN NPs) are encouraging nanomaterials with unique chemical properties in medicine and biomedical fields. Until now, the optimal hBN NP’s dosage and biochemical mechanism that can be used for in vivo systems has not been fully revealed. The main aim of this article is to reveal characteristics, serum and tissue interactions and any acute cytotoxic effect of different dose of hBN NPs for the first time. Methods: hBN NPs at concentrations varying between 50–3200 µg/kg was administered by intravenous injection to Wistar albino rats (n = 80) divided into seven dosage and control groups. Blood and tissue samples were taken after 24 hours. Results: Our findings suggested that higher doses hBN NPs caused oxidative stress on the serum of rats dose-dependently. However, hBN NPs did not affect thiol/disulfide homeostasis on kidney, liver, spleen, pancreas and heart tissue of rats. Furthermore, hBN NPs increased serum disulfide formation by disrupting the thiol/disulfide balance in rats. Also, LOOH and MPO levels increased at high doses, while CAT levels decreased statistically. Conclusion: The results revealed that hBN NPs induce oxidative stress in a dose-dependent manner by modulating thiol/disulfide homeostasis in rats at higher concentrations

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