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1

Quaternary ammonium salt derivatives of allylphenols with peripheral analgesic effect  

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Full Text Available Ammonium salt derivatives of natural allylphenols were synthesized with the purpose of obtaining potential peripheral analgesics. These drugs, by virtue of their physicochemical properties, would not be able to cross the blood brain barrier. Their inability to enter into the central nervous system (CNS) should prevent several adverse effects observed with classical opiate analgesics (Ferreira et al., 1984). Eugenol (1) O-methyleugenol (5) and safrole (9) were submitted to nitration, reduction and permethylation, leading to the ammonium salts 4, 8 and 12. Another strategy applied to eugenol (1), consisting in its conversion to a glycidic ether (13), opening the epoxide ring with secondary amines and methylation, led to the ammonium salts 16 and 17. All these ammonium salts showed significant peripheral analgesic action, in modified version of the Randall-Sellito test (Ferreira et al. 1978), at non-lethal doses. The ammonium salt 8 showed an activity comparable to that of methylnalorphinium, the prototype of an ideal peripheral analgesic (Ferreira et al., 1984).

A. B de Oliveira; T. H. A. Silva; S. H. Ferreira; B. B. Lorenzetti

1991-01-01

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Peripheral analgesic effects of ketamine in acute inflammatory pain.  

DEFF Research Database (Denmark)

BACKGROUND. This study examined the analgesic effect of local ketamine infiltration, compared with placebo and systemic ketamine, in a human model of inflammatory pain. METHODS: Inflammatory pain was induced by a burn (at 47 degrees C for 7 min; wound size, 2.5 x 5 cm) on the calf in 15 volunteers on 3 separate days with 7-day intervals. They received either (1) subcutaneous infiltration with ketamine in the burn area (local treatment) and contralateral placebo injections, or (2) subcutaneous ketamine contralateral to the burn (systemic treatment) and placebo in the burn area, or (3) placebo on both sides. The study was double-blinded and the order of the treatments was randomized. Hyperalgesia to mechanical and heat stimuli was examined by von Frey hairs and contact thermodes (3.75 and 12.5 cm2), and pain was rated using a visual analog scale (0-100). RESULTS: The burns produced significant hyperalgesia. Local ketamine infiltration reduced pain during the burn injury compared with systemic treatment and placebo (P < 0.01). Heat pain thresholds were increased by local ketamine treatment compared with placebo immediately after injection (P < 0.03), and so were the mechanical pain thresholds (P = 0.02). Secondary hyperalgesia and suprathreshold pain responses to heat and mechanical stimuli were not significantly affected by local ketamine. No difference between local ketamine and placebo could be detected 1 h and 2 h after the burn. CONCLUSIONS: Ketamine infiltration had brief local analgesic effects, but several measures of pain and hyperalgesia were unaffected. Therefore, a clinically relevant effect of peripheral ketamine in acute pain seems unlikely.

Pedersen, J L; Galle, T S

1998-01-01

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Topical and peripherally acting analgesics.  

UK PubMed Central (United Kingdom)

Acute nociceptive, inflammatory, and neuropathic pain all depend to some degree on the peripheral activation of primary sensory afferent neurons. The localized peripheral administration of drugs, such as by topical application, can potentially optimize drug concentrations at the site of origin of the pain, while leading to lower systemic levels and fewer adverse systemic effects, fewer drug interactions, and no need to titrate doses into a therapeutic range compared with systemic administration. Primary sensory afferent neurons can be activated by a range of inflammatory mediators such as prostanoids, bradykinin, ATP, histamine, and serotonin, and inhibiting their actions represents a strategy for the development of analgesics. Peripheral nerve endings also express a variety of inhibitory neuroreceptors such as opioid, alpha-adrenergic, cholinergic, adenosine and cannabinoid receptors, and agonists for these receptors also represent viable targets for drug development. At present, topical and other forms of peripheral administration of nonsteroidal anti-inflammatory drugs, opioids, capsaicin, local anesthetics, and alpha-adrenoceptor agonists are being used in a variety of clinical states. There also are some clinical data on the use of topical antidepressants and glutamate receptor antagonists. There are preclinical data supporting the potential for development of local formulations of adenosine agonists, cannabinoid agonists, cholinergic ligands, cytokine antagonists, bradykinin antagonists, ATP antagonists, biogenic amine antagonists, neuropeptide antagonists, and agents that alter the availability of nerve growth factor. Given that activation of sensory neurons involves multiple mediators, combinations of agents targeting different mechanisms may be particularly useful. Topical analgesics represent a promising area for future drug development.

Sawynok J

2003-03-01

4

Topical and peripherally acting analgesics.  

Science.gov (United States)

Acute nociceptive, inflammatory, and neuropathic pain all depend to some degree on the peripheral activation of primary sensory afferent neurons. The localized peripheral administration of drugs, such as by topical application, can potentially optimize drug concentrations at the site of origin of the pain, while leading to lower systemic levels and fewer adverse systemic effects, fewer drug interactions, and no need to titrate doses into a therapeutic range compared with systemic administration. Primary sensory afferent neurons can be activated by a range of inflammatory mediators such as prostanoids, bradykinin, ATP, histamine, and serotonin, and inhibiting their actions represents a strategy for the development of analgesics. Peripheral nerve endings also express a variety of inhibitory neuroreceptors such as opioid, alpha-adrenergic, cholinergic, adenosine and cannabinoid receptors, and agonists for these receptors also represent viable targets for drug development. At present, topical and other forms of peripheral administration of nonsteroidal anti-inflammatory drugs, opioids, capsaicin, local anesthetics, and alpha-adrenoceptor agonists are being used in a variety of clinical states. There also are some clinical data on the use of topical antidepressants and glutamate receptor antagonists. There are preclinical data supporting the potential for development of local formulations of adenosine agonists, cannabinoid agonists, cholinergic ligands, cytokine antagonists, bradykinin antagonists, ATP antagonists, biogenic amine antagonists, neuropeptide antagonists, and agents that alter the availability of nerve growth factor. Given that activation of sensory neurons involves multiple mediators, combinations of agents targeting different mechanisms may be particularly useful. Topical analgesics represent a promising area for future drug development. PMID:12615951

Sawynok, Jana

2003-03-01

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Effectiveness of the association between carbamazepine and peripheral analgesic block with ropivacaine for the treatment of trigeminal neuralgia  

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Treatment of trigeminal neuralgia (TN) is achieved by using adjuvant analgesics like antiepileptics, with carbamazepine (CBZ) being the first-line approach for TN patients, although side effects may be present. Other approaches using gabapentin, namely when associated with peripheral analgesic block...

Lemos, L; Fontes, R; Flores, S; Oliveira, P; Almeida, A

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Analgesic effects of preoperative peripheral nerve block in patients with trigeminal neuralgia undergoing radiofrequency thermocoagulation of gasserian ganglion.  

UK PubMed Central (United Kingdom)

Trigeminal neuralgia is the worst pain that human beings have ever experienced. Surgery might be the only solution for some patients because no other way can relieve their severe pain. They experience intolerable pain before operation and during radiofrequency thermocoagulation of the gasserian ganglion. The aim of the current study was to prospectively evaluate the preoperative and perioperative analgesic effects of preoperative single peripheral nerve block. Sixty patients with classic trigeminal neuralgia who were scheduled to undergo radiofrequency thermocoagulation of the gasserian ganglion were randomly divided into a control group (n = 30) and a nerve block group (n = 30). Patients in the nerve block group were treated with single peripheral nerve block using 1% lidocaine and betamethasone on the day of admission. Average pain, worst pain, quality of sleep, and analgesia satisfaction were evaluated before surgery. The incidence and intensity of perioperative episodic pain were determined before the needle reached the gasserian ganglion. Compared with the control group, a single peripheral nerve block significantly attenuated average pain (P < 0.01) and worst pain (P < 0.01), ameliorated the quality of sleep (P < 0.01), and increased analgesia satisfaction (P < 0.01). Moreover, patients in the nerve block group experienced a decrease in incidence (P < 0.01) and intensity (P < 0.01) of episodic pain during surgery as compared with the participants in the control group. These results demonstrate that a single peripheral nerve block may be an effective way to relieve preoperative and perioperative intolerable pain of trigeminal neuralgia.

Weng Z; Halawa MA; Liu X; Zhou X; Yao S

2013-03-01

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Effectiveness of the association between carbamazepine and peripheral analgesic block with ropivacaine for the treatment of trigeminal neuralgia  

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Full Text Available Laurinda Lemos1,2, Ramalho Fontes3, Sara Flores2, Pedro Oliveira4, Armando Almeida11Life and Health Sciences Research Institute (ICVS), School of Health Sciences, Campus de Gualtar, University of Minho, Braga, Portugal; 2Hospital Center of Alto Ave, Unit of Fafe, Fafe, Portugal; 3Department of Neurology, Hospital Săo Marcos, Braga, Portugal; 4Products and Systems Engineering, Campus de Azurém, University of Minho, Guimarăes, PortugalAbstract: Treatment of trigeminal neuralgia (TN) is achieved by using adjuvant analgesics like antiepileptics, with carbamazepine (CBZ) being the first-line approach for TN patients, although side effects may be present. Other approaches using gabapentin, namely when associated with peripheral analgesic block of TN trigger points with the local anesthetic ropivacaine (ROP), resulted in decreased pain and daily drug intake (reduced side effects). This study evaluates if the association between CBZ and the peripheral block with ROP reinforces the clinical value of CBZ. In this parallel, double-blinded study, idiopathic TN patients were randomized to receive during 4 weeks either CBZ (CBZ; n = 21) or CBZ associated with the peripheral analgesic block using ROP (CBZ + ROP; n = 24). The primary outcome measures were the following: i) pain intensity, evaluated by the numerical rating scale; ii) number of pain crises; and iii) number needed to treat. Evaluation points were at the beginning (day 1) and end (day 29) of treatment and after a follow-up of 5 months (month 6). Both protocols resulted in a decrease of pain intensity and number of pain crises, but only the association CBZ + ROP showed i) a significant stronger reduction in pain intensity at month 6 and ii) a significant decrease in the daily dose of CBZ given to patients (both at day 29 and month 6). In contrast, the daily dose in CBZ-only patients remained constant or even increased. The number needed to treat for the association CBZ + ROP over the CBZ protocol reduced from 5 at the end of the 4-week treatment to 3 after the 5-month follow-up. Data reinforce the use of CBZ as a primary tool to control pain in TN patients, as the association CBZ + ROP i) improves the clinical qualities of CBZ, ii) strongly reduces the daily dose of CBZ, and iii) reduces the potential side effects attributed to high doses of CBZ.Keywords: trigeminal neuralgia, carbamazepine, ropivacaine, therapeutical association, pain intensity, daily dose

Laurinda Lemos; Ramalho Fontes; Sara Flores; et al

2010-01-01

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Application of a peripheral nerve block technique in laser treatment of the entire facial skin and evaluation of its analgesic effect.  

UK PubMed Central (United Kingdom)

Background: The aim was to develop a technique for peripheral nerve block anesthesia (PNB) for the skin of the entire face and neck, considering the nerves anesthetized, injection sites, use of an injection method assisted by computer-controlled local anesthetic delivery (CCLAD), and to evaluate the analgesic effects of the PNB technique. Methods: 50 patients who suffered from large nevus of Ota lesions or port-wine stains on their facial and neck skin and who required laser treatment were included. This study was designed as a non-randomized self-control trial. All the patients received the laser treatment under topical anesthesia in the first phase and three to six months later, they received the same treatment under the PNB using CCLAD. The differences in scores from the visual analogue scale of pain for the two phases were analyzed by the t-test. P values <0.05 were considered to be statistically significant. Results: The peripheral nerve block technique was simple to execute and easy to learn, the anesthetic injection site was generally located at a subcutaneous depth of 0.5-1.0 cm. The analgesic effect of PNB was significant, the mean pain score (2.8 ± 2.2) was significantly lower than that with topical anesthesia (P<0.0001). Patients during the PNB phase did not experience injection pain following CCLAD. Conclusion: The peripheral nerve block technique can greatly ease the pain that occurs during laser treatment, especially for patients with larger lesions. CCLAD will allow PNB to be broadly applied in laser treatments.

Wan K; Jing Q; Sun QN; Wang HW; Zhao JZ; Ma L; Kong LJ

2013-06-01

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Evaluation of the analgesic efficacy and psychoactive effects of AZD1940, a novel peripherally acting cannabinoid agonist, in human capsaicin-induced pain and hyperalgesia.  

Science.gov (United States)

The aim of the present study was to investigate the effects of AZD1940, a novel peripherally acting cannabinoid CB(1) /CB(2) receptor agonist, on capsaicin-induced pain and hyperalgesia, as well as on biomarkers of cannabinoid central nervous system (CNS) effects. The present study was a randomized, double-blind, placebo-controlled, four-sequence, two-period, cross-over study in 44 male healthy volunteers aged 20-45 years. The effects of two single oral doses of AZD1940 (400 and 800 ?g) were compared with placebo. Pain intensity after intradermal capsaicin injections in the forearm was assessed on a continuous visual analogue scale (VAS; 0-100 mm). Primary and secondary hyperalgesia induced by application of capsaicin cream on the calf were assessed by measuring heat pain thresholds and the area of mechanical allodynia, respectively. The CNS effects were assessed at baseline and up to 24 h after dosing using a visual analogue mood scales (VAMS) for feeling 'stimulated', 'high', 'anxious', 'sedated' or 'down'. AZD1940 did not significantly attenuate ongoing pain or primary or secondary hyperalgesia compared with placebo. Mild CNS effects for AZD1940were observed on the VAMS for 'high' and 'sedated'. Dose-dependent mild-to-moderate CNS-related and gastrointestinal adverse events were reported following treatment with AZD1940. No evidence of analgesic efficacy was found for a peripherally acting CB(1)/CB(2) receptor agonist in the human capsaicin pain model. The emergence of mild dose-dependent CNS effects suggests that the dose range predicted from preclinical data had been attained. PMID:23324098

Kalliomäki, Jarkko; Annas, Peter; Huizar, Karin; Clarke, Cyril; Zettergren, Annika; Karlsten, Rolf; Segerdahl, Märta

2013-03-01

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The selective neuronal nitric oxide synthase inhibitor 7-nitroindazole has acute analgesic but not cumulative effects in a rat model of peripheral neuropathy  

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Full Text Available Liliane J Dableh, James L HenryDepartment of Psychiatry and Behavioural Neurosciences, McMaster University, Hamilton, Ontario, CanadaAbstract: Chronic neuropathic pain that may arise from various nerve injuries or insults remains notoriously difficult to manage. The neuronal isoform of the enzyme nitric oxide synthase (nNOS) has been shown to be involved in the spinal transmission of nociception in animal models of chronic pain. The aim of this study is to evaluate the effect of single dose and repeated administration of a selective nNOS inhibitor. Rats were unilaterally implanted with a 2-mm polyethylene cuff around the sciatic nerve. Paw withdrawal thresholds were measured using von Frey filament stimulation. Rats were given 10, 20, or 30 mg/kg of 7-nitroindazole (7-NI), or vehicle, on days 2, 5, and 7 after model induction, respectively. Paw withdrawal thresholds were measured before and at 30 and 60 min after injection. 7-NI significantly increased paw withdrawal thresholds at 60 min at the 20 and 30 mg/kg dosages. In the second part of this study, rats were given 20 mg/kg 7-NI daily for five days starting immediately after cuff implantation (days 0 to 4), and the cuff was removed on day 4. Withdrawal thresholds were measured intermittently over a 24-day observation period. No differences in withdrawal thresholds were observed between drug and vehicle-treated rats. Therefore, early and repeated administration of 7-NI did not affect the development or progression of the model. In conclusion, inhibition of nNOS had an analgesic but not a pre-emptive effect in this model of peripheral neuropathic pain.Keywords: neuronal nitric oxide synthase, nitric oxide, 7-nitroindazole, neuropathic pain, peripheral nerve injury, nociception 

Henry JL; Dableh LJ

2011-01-01

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Targeting peripheral opioid receptors to promote analgesic and anti-inflammatory actions  

Science.gov (United States)

Mechanisms of endogenous pain control are significant. Increasing studies have clearly produced evidence for the clinical usefulness of opioids in peripheral analgesia. The immune system uses mechanisms of cell migration not only to fight pathogens but also to control pain and inflammation within injured tissue. It has been demonstrated that peripheral inflammatory pain can be effectively controlled by an interaction of immune cell-derived opioid peptides with opioid receptors on peripheral sensory nerve terminals. Experimental and clinical studies have clearly shown that activation of peripheral opioid receptors with exogenous opioid agonists and endogenous opioid peptides are able to produce significant analgesic and anti-inflammatory effects, without central opioid mediated side effects (e.g., respiratory depression, sedation, tolerance, dependence). This article will focus on the role of opioids in peripheral inflammatory conditions and the clinical implications of targeting peripheral opioid receptors.

Iwaszkiewicz, Katerina S.; Schneider, Jennifer J.; Hua, Susan

2013-01-01

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Cardiovascular effects of common analgesics.  

UK PubMed Central (United Kingdom)

The clycoxygenase (COX) enzyme forms locally active prostaglandins responsible for producing inflammation and pain. Classical non-steroidal anti-inflammatory drugs (NSAID) inhibit the COX-2 enzyme that produces inflammatory prostaglandins as well as the COX-1 enzyme that produces gastric mucosa protecting prostaglandins. By specifically inhibiting only the COX-2 enzyme, coxibs thus reduce pain but do not damage the gastric mucosa. However, COX-2 at the vascular endothelium produces antithrombotic prostaglandins, and so by inhibiting COX-2 enzyme, the coxibs promote thrombosis. Rofecoxib and valdecoxib have been withdrawn because of the adverse cardiovascular events they induce. Amongst presently available coxibs cardiovascular risk is highest with enterocoxib and lowest with celecoxib. NSAIDS also increase cardiovascular events, the risk is highest with diclofenac and lowest with naproxen. Paracetamol and corticosteroids induce hypertension, while steroids also adversely affect the heart from metabolic change as well as fluid retention. Aspirin is an anti-thrombotic agent because of its ability to inhibit the COX-1 enzyme that produces the pro-aggregatory thromboxane. However, it increases gastrointestinal bleeding, can promote fluid retention and is nephrotoxic, all of which may lead to adverse cardiovascular outcomes. Patients at especially high risk of cardiovascular events from analgesic use include the elderly, and those with heart failure, hypertension, rheumatoid arthritis, chronic renal disease, chronic obstructive airway disease and previous myocardial infarction, cerebrovascular disease or peripheral vascular disease. Adverse cardiovascular events can occur within a week of initiation of analgesic treatment.

Ong HT; Ong LM; Tan TE; Chean KY

2013-04-01

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Peripheral antihyperalgesic and analgesic actions of ketamine and amitriptyline in a model of mild thermal injury in the rat.  

UK PubMed Central (United Kingdom)

UNLABELLED: In this study, we examined antihyperalgesic and analgesic actions after local peripheral administration of ketamine and amitriptyline in a rat model of mild thermal injury. Exposure of the hindpaw to 52 degrees C for 45 s under anesthesia produced a subsequent thermal hyperalgesia lasting at least 2 h. The local peripheral administration of ketamine (100-1000 nmol) 15 min before the thermal injury produced an antihyperalgesic effect when injected into the ipsilateral paw, whereas amitriptyline produced both antihyperalgesic (300 nmol) and analgesic (1000 nmol) effects. Administered after the thermal injury, ketamine had no effect, whereas amitriptyline retained its analgesic but not its antihyperalgesic effect. Amitriptyline (300 and 1000 nmol) produced an analgesic action when administered into the normal nonsensitized hindpaw. Both drugs increase paw volume, particularly at larger doses; biogenic amines are not involved in the action of amitriptyline, as was shown previously for ketamine. These results indicate that (a) ketamine produces antihyperalgesia, but not analgesia, when administered locally with a mild thermal injury model; (b) amitriptyline produces both antihyperalgesia and analgesia when administered locally; and (c) the increase in paw volume produced by these drugs occurs by different mechanisms. IMPLICATIONS: This study examines the pain-relieving properties of the local peripheral administration of ketamine and amitriptyline, two drugs in current clinical use, in a thermal injury model of hyperalgesia and demonstrates both antihyperalgesic and analgesic properties. These observations provide support for their potential use as local (e.g., topical) analgesics.

Oatway M; Reid A; Sawynok J

2003-07-01

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Peripheral opioids act as analgesics in bone cancer pain in mice.  

UK PubMed Central (United Kingdom)

Previous reports have shown that systemic administration of morphine can prevent the thermal hyperalgesia induced by the development of an osteosarcoma in C3H/HeJ mice after the implantation of NCTC 2472 cells. We show here that this type of hyperalgesia is also abolished by the local administration of morphine given at low doses (10 nmol), or the peripheral acting opioid receptor agonist loperamide (146 nmol). The analgesic effect of loperamide is prevented by the administration of the opioid receptor antagonist naloxone methiodide (10 mg/kg, i.p.), which is unable to cross the blood-brain barrier. These results provide evidence which supports the fact that peripheral opioids could be useful tools in the management of some types of cancer pain.

Menéndez L; Lastra A; Hidalgo A; Meana A; García E; Baamonde A

2003-05-01

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The analgesic action of topical diclofenac may be mediated through peripheral NMDA receptor antagonism  

DEFF Research Database (Denmark)

The analgesic mechanism underlying the efficacy of topical diclofenac in the treatment of musculoskeletal pain is incompletely understood. The present study investigated whether intramuscular injection of diclofenac (0.1mg/ml, approximately 340microM) could attenuate jaw-closer muscle nociceptor discharge and mechanical sensitization induced by activation of peripheral 5-hydroxytryptamine (serotonin) or excitatory amino acid receptors in anesthetized Sprague-Dawley rats. Diclofenac inhibited nociceptor discharge evoked by NMDA, but had no effect on nociceptor discharge evoked by 5-hydroxytryptamine or AMPA. Subsequent experiments revealed that diclofenac-mediated inhibition of NMDA-evoked nociceptor discharge was competitive. Intramuscular injection of 5-hydroxytryptamine, NMDA and AMPA also decreased nociceptor mechanical threshold, however, only the mechanical sensitization produced by NMDA was reversed by diclofenac. Co-administration of the proinflammatory prostaglandin PGE(2) did not alter the ability ofdiclofenac to significantly attenuate NMDA-evoked nociceptor discharge or NMDA-induced mechanical sensitization. Intramuscular injection of either diclofenac or the competitive NMDA receptor antagonist DL-2-amino-5-phosphonovalerate (50mM) alone could elevate nociceptor mechanical threshold for a 30min period post-injection. The present study indicates that in vivo, diclofenac can exert a selective, competitive inhibition of peripheral NMDA receptors at muscle concentrations achievable after topical administration of diclofenac containing preparations. This property may contribute to the analgesic effect of topical diclofenac when used for muscle pain.

Dong, Xu-Dong; Svensson, Peter

2009-01-01

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Investigation of the Central and Peripheral Analgesic and Anti-inflammatory Activity of Kutajarishta, an Indian Ayurvedic formulation  

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Full Text Available Kutajarishta (KTJ) is an Ayurvedic formulation approved by the “National formulary of Ayurvedic Medicine 2011”, of Bangladesh. It is widely available in the Bangladeshi market as an effective preparation to treat lumbago, sciatia and arthritic pain of joints. Our present studies make an attempt toward identifying probable anti-nociceptive and anti-inflammatory mechanisms of KTJ. KTJ, at three doses, (10mL/kg, 20mL/kg, and 40mL/kg) showed no involvement of the CNS in anti-nociceptive activity of KTJ. Carrageenan induced paw edema and acetic acid writhing tests both gave significant results (P ? 0.05), indicating possible peripheral analgesic and anti-inflammatory action. Formalin induced paw-licking test showed that KTJ had significant effect in suppressing inflammatory pain (P?0.05) but not neurogenic pain. Hence our study shows anti-inflammatory and peripheral analgesic action for KTJ.

Ashraful Kabir

2012-01-01

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[Do antidepressive agents have analgesic effects?  

UK PubMed Central (United Kingdom)

Patients with chronic pain are often depressed, and antidepressants have been widely used in the treatment of these patients. Well controlled clinical studies have shown that antidepressants have analgesic effects, apparently independent of changes in mood, and in lower doses than used in the treatment of depression. Good results have been reported for several types of chronic pain, especially headache and facial pain, arthritis, fibromyalgia and neuralgias. In addition, antidepressants have also an indirect analgesic action by relieving a depressive condition associated with chronic pain.

Fasmer OB

1990-08-01

18

Topical analgesics.  

UK PubMed Central (United Kingdom)

Historically, analgesics were applied by the topical route of administration. With the advent of oral formulations of drugs, topical application became less popular among physicians, although patients still rated this method of drug delivery as efficacious and practical. We now appreciate that peripheral mechanisms of actions of a variety of preparations rationalizes their topical application and gives further opportunity to target peripheral receptors and neural pathways that previously required systemic administration to achieve therapeutic effect. Therefore, a peripheral effect can be generated by using locally applied drug and, consequently, systemic concentrations of that drug may not reach the level at which systemic side effects can occur.

McCleane G

2007-12-01

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The analgesic effect of the methanolic extract of Acanthus montanus.  

Science.gov (United States)

The analgesic effect of the methanolic leaf extract of Acanthus montanus was studied in rats using the cold water tail flick assay, and in mice using the tail immersion, tail clip, acetic acid induced writhing and formalin pain tests. The results showed dose-dependent and significant (P<0.05) increases in pain threshold, at 60 min post treatment, with doses of 200 and 400 mg/kg of the extract in tail flick, tail immersion and tail clip methods. The effects of the extract were significantly (P<0.05) lower than those produced by morphine (10 mg/kg) in the same tests. The extract (100-400 mg/kg) exhibited a dose-dependent inhibition of writhing and also showed a significant (P<0.001) inhibition of both phases of the formalin pain test, but with a less intense effect on the first than on the second phase. The results indicate that the analgesic effect of Acanthus montanus methanolic extract is both centrally and peripherally mediated. PMID:14698507

Adeyemi, Olufunmilayo O; Okpo, Steve O; Okpaka, Orowo

2004-01-01

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The analgesic effect of the methanolic extract of Acanthus montanus.  

UK PubMed Central (United Kingdom)

The analgesic effect of the methanolic leaf extract of Acanthus montanus was studied in rats using the cold water tail flick assay, and in mice using the tail immersion, tail clip, acetic acid induced writhing and formalin pain tests. The results showed dose-dependent and significant (P<0.05) increases in pain threshold, at 60 min post treatment, with doses of 200 and 400 mg/kg of the extract in tail flick, tail immersion and tail clip methods. The effects of the extract were significantly (P<0.05) lower than those produced by morphine (10 mg/kg) in the same tests. The extract (100-400 mg/kg) exhibited a dose-dependent inhibition of writhing and also showed a significant (P<0.001) inhibition of both phases of the formalin pain test, but with a less intense effect on the first than on the second phase. The results indicate that the analgesic effect of Acanthus montanus methanolic extract is both centrally and peripherally mediated.

Adeyemi OO; Okpo SO; Okpaka O

2004-01-01

 
 
 
 
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Lignocaine is a better analgesic than either ethyl chloride or nitrous oxide for peripheral intravenous cannulation.  

UK PubMed Central (United Kingdom)

BACKGROUND: Peripheral intravenous (i.v.) cannulation is a painful, frequently performed ED procedure. It is common practice in other medical settings to offer analgesia prior to cannulation. OBJECTIVE: The present trial aims to reproduce in the ED studies that found a reduction in the pain of i.v. cannulation after intradermal lignocaine, ethyl chloride topical spray and entonox (50:50 oxygen : nitrous oxide). It also intends to determine which is analgesic most effective and explore the role of entonox for cannulation analgesia. Methods: Three hundred subjects were randomized into four groups: i.v. cannula inserted with (i) no anaesthesia; (ii) entonox; (iii) ethyl chloride; and (iv) 0.1 mL intradermal 1% lignocaine. Pain was recorded on 100 mm visual analogue scales (VAS) after lignocaine injection or ethyl chloride spray and following i.v. cannulation. A clinically significant reduction in VAS pain score was determined to be 13 mm. RESULTS: Patients cannulated without analgesia reported the most pain. Those cannulated after lignocaine had the least pain (median VAS 20 mm, 95% CI 15-25, vs 1 mm 95% CI 0-6, P < or = 0.001). Ethyl chloride (VAS 11 mm, 95% CI 7-15, P = 0.003) and entonox (VAS 13 mm, 95% CI 8-18, P = 0.047) reduced i.v. cannulation pain but did not reach clinical significance. Neither pain from presenting symptoms (P = 0.3), nor size of cannula (P = 0.8) affected pain scores. VAS scores were independent of sex and age (P = 0.1). Cannulation success was not affected by either the choice of analgesia or cannulation site. CONCLUSIONS: The present trial confirms the findings of Harris and colleagues that lignocaine reduces the pain of cannulation in the ED. Lignocaine reduced the pain of i.v. cannulation more effectively than entonox or ethyl chloride.

Robinson PA; Carr S; Pearson S; Frampton C

2007-10-01

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Anti-inflammatory and peripheral analgesic activity of esculetin in vivo.  

UK PubMed Central (United Kingdom)

Esculetin determined a reduction in oedema and granulocyte infiltration in the Croton oil ear test in vivo. The drug was able to inhibit Acethylcholine-writhing test and showed a LD50 of 1450 mg/kg i.p. and greater than 2000 mg/kg by mouth. In our experimental conditions, esculetin has an anti-inflammatory and analgesic effect.

Tubaro A; Del Negro P; Ragazzi E; Zampiron S; Della Loggia R

1988-12-01

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Study of Analgesic Effect of Hydroalcoholic Extract of Cinammom  

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Full Text Available Background and Objective: The side effects due to application of synthetic analgesic drugs in the clinical practice have turned on researchers to focus on development of herbal medicine as more appropriate analgesic agents. The aim of this study was evaluation the analgesic effects of hydroalcholic extract of Cinnamomum Zeylanicum in comparison with morphine and aspirin.Materiales and Methods: For preparing the hydroalcoholic extract of Cinnamomum the maceration method was used. Wistar male rats were divided into eight groups of 6 rats, randomly and treated groups have received 200, 400, 600, 800 mg/kg extract and the two positive control groups received 2.5 mg/kg morphine or 300mg/kg aspirin. Negative control group received normal saline (5ml/kg) and an additional group also received 600 mg/kg extract+1mg/kg naloxan intraperitonealy respectively. 50 µl formalin 2.5% was injected in right hindpaw subcutaneously and analgesic behaviors were scored.Results: The results revealed that the Cinnamomum Zeylanicum extract had analgesic effect as dose-dependent and its analgesic effective dose was 600 mg/kg. Our results showed that the analgesic effect of its best effective dose (600mg/kg) on acute pain was more than aspirin while it was less than morphine. Also the effect of extract on chronic pain was less than morphine and aspirin. There were no significant differences between analgesic effects of Cinnamomum Zeylanicum extract with naloxone or alone.Conclusion: We concluded that the analgesic effect of Cinnamo- mum Zeylanicum extract is dose-dependent and is driven negatively through opioid receptors.Sci Med J 2011; 10(3):271-279

Arzi Ardeshir; Sarkaki Alireza; Aghel Nasrin; Nazari Zahra; Saeidnejad Sara

2011-01-01

24

Effects of melatonin on peripheral nerve regeneration.  

Science.gov (United States)

In the available literature, there are thousands of studies on peripheral nerve regeneration using many nerves of several animals at different ages with various types of lesions and different methods of evaluation at certain time of follow-up. Despite many experimental data and clinical observations, there is still no ideal treatment method enhancing peripheral nerve regeneration. In clinical practice, various types of surgical nerve repair techniques do not frequently result in complete recovery due to neuroma formation, lipid peroxidative damage, ischemia and other factors. Recently, a number of neuroscientists demonstrated that pineal neurohormone melatonin (MLT) has an effect on the morphologic features of the nerve tissue, suggesting its neuroprotective, free radical scavenging, antioxidative, and analgesic effects in degenerative diseases of peripheral nerves. At present, it is widely accepted that MLT has a useful effect on axon length and sprouting after traumatic events to peripheral nerves. Our studies using various experimental injury models clearly suggest positive effects of MLT on the number of axons, thickness of myelin sheath by inhibition of collagen accumulation and neuroma formation following traumatic events to peripheral nerves, myelination of developing peripheral nerve after intrauterine ethanol exposure. Nevertheless, further experimental and randomized controlled clinical studies are vital to identify the clinical use of MLT hormone. This is an overview of recent patents and current literature in terms of the effects of MLT on peripheral nerve regeneration based on a critical analysis of electrophysiological, biochemical and light and electron microscopic findings, in addition to functional observations. PMID:22074585

Turgut, Mehmet; Kaplan, Süleyman

2011-05-01

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Analgesic effect of tianeptine in mice.  

UK PubMed Central (United Kingdom)

The effects of tianeptine, a novel and unusual tricyclic antidepressant drug, on tail-flick and hot-plate tests, which are two thermal analgesia evaluating methods, have been investigated in mice. Tianeptine (5 and 10 mg/kg), para-chlorophenylalanine (pCPA) (100 mg/kg) and a combination of pCPA and tianeptine (10 mg/kg) or saline were injected to mice intraperitoneally. pCPA (100 mg/kg) was injected 24 h before tianeptine or saline treatment when it was combined with tinaeptine (10 mg/kg) or tested alone. The tail-flick latencies and hot-plate reaction times of the mice were measured between 15th and 180th minutes following injections. Tianeptine (10 mg/kg) exhibited a significant antinociceptive activity that could be measured by both tests as compared to groups which were treated with saline or pCPA alone between 15th and 180th min of the observation period. The lower dose of tianeptine (5 mg/kg) or pCPA (100 mg/kg) did not produce any significant changes on tail-flick latency or hot-plate reaction time of the mice. However, pretreatment with pCPA completely blocked the antinociceptive effect induced by tianeptine (10 mg/kg) in both tests used in the present study. Furthermore, tianeptine (10 mg/kg) did not cause any significant impairment effects on rotarod performance of the mice. Our results suggested that tianeptine has a prominent thermal antinociceptive activity in mice and that increased serotonergic activity may be responsible for the analgesic effect of tianeptine.

Uzbay IT; Cinar MG; Aytemir M; Tuglular I

1999-01-01

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Intrathecal administration of epinephrine inhibits and reverses analgesic tolerance to analgesic effect of morphine in rats  

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Full Text Available Introduction: Several researches have reported that stress is able to inhibit the development of morphine tolerance via activating of Hypothalamic-Pituitary-Adrenal (HPA) axis. In the present study we tried to examine the effect of epinephrine, the product of adrenal medulla, on the development of morphine tolerance. Methods: Analgesic tolerance was induced by intrathecal (i.t.) injection of morphine 15 ?g/kg, twice a day for 5 days. To study the effect of epinephrine on morphine tolerance, epinephrine (2, 5, 10 or 20 ?g/kg, i.t.) was administrated 20 minutes before morphine injection. Analgesia was assessed using tail flick test. Results: In animals that received combined treatments of morphine and epinephrine in doses 2, 5, 10 or 20 ?g/ kg for 5 days, at 6th day, morphine produced a more potent analgesia comparing with animals that received saline and morphine during days 1-5. Following tolerance induction during first 5 days, co-administration of epinephrine and morphine during days 6 – 10 reduced the initial tolerance as it induced potent analgesia on day 11th. Conclusion: Our results showed that i.t. administration of epinephrine is able to inhibit and reverse the analgesic tolerance to morphine. It also suggests the possible role of adrenal medulla and epinephrine in mediating the inhibitory effect of stress and HPA activation of the development of analgesic tolerance to morphine.

Leila Satarian; Mohammad Javan; Yagoob Fathollahi

2006-01-01

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A study on anti-inflammatory and peripheral analgesic action of Salvia sclarea oil and its main components.  

UK PubMed Central (United Kingdom)

Activity against the acute inflammatory process induced by carrageenin and histamine in rats and the anti-nociceptive effect in mice were investigated after administration of Salvia sclarea oil and some of its constituents. The oil showed a significant anti-inflammatory effect and moderate analgesic action after subcutaneous injection at a dose of 250 mg/kg. The anti-inflammatory action was more conspicuous in the carrageenin-induced edema, where it produced the equivalent effect of a 5 mg/kg dose of indomethacin, than in the histamine-induced edema. The effect was correlated to the presence of methyl chavicol, linalool, alpha-terpineol and linalyl acetate. The results show that these constituents produce less anti-inflammatory action when administered separately than the oil in toto, and are also less effective than the oxygenated fractions obtained by Flash chromatography of the oil. This indicates that the action of the oil is determined by synergistic action of its constituents. The moderate peripheral analgesia (evaluated by writhing test) produced by S. sclarea oil appears to be mainly attributable to its alcoholic component.

Moretti MDL; Peana AT; Satta M

1997-04-01

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Non-narcotic orally effective, centrally acting analgesic from an Ayurvedic drug.  

UK PubMed Central (United Kingdom)

Embelin, a p-quinone, is derived from Embelia ribes Burm. The analgesic effect of potassium embelate has been studied in rats and mice. The test drug was found to be effective by oral, i.m. and i.c.v. routes and the results compared well with morphine. Although potassium embelate acts centrally to produce analgesia, its effect is not antagonized by naloxone indicating a different central site of action. There is no precipitation of abstinence syndrome as observed with morphine. Peripheral site of action of the drug is ruled out as it lacks any demonstrable anti-inflammatory action. It can be concluded that high oral efficacy and non-narcotic properties of the test drug make it more acceptable than morphine. In addition, lack of any adverse effects, high therapeutic index and absence of abstinence syndrome confers a long term safety on potassium embelate for use as an analgesic.

Atal CK; Siddiqui MA; Zutshi U; Amla V; Johri RK; Rao PG; Kour S

1984-08-01

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Non-narcotic orally effective, centrally acting analgesic from an Ayurvedic drug.  

Science.gov (United States)

Embelin, a p-quinone, is derived from Embelia ribes Burm. The analgesic effect of potassium embelate has been studied in rats and mice. The test drug was found to be effective by oral, i.m. and i.c.v. routes and the results compared well with morphine. Although potassium embelate acts centrally to produce analgesia, its effect is not antagonized by naloxone indicating a different central site of action. There is no precipitation of abstinence syndrome as observed with morphine. Peripheral site of action of the drug is ruled out as it lacks any demonstrable anti-inflammatory action. It can be concluded that high oral efficacy and non-narcotic properties of the test drug make it more acceptable than morphine. In addition, lack of any adverse effects, high therapeutic index and absence of abstinence syndrome confers a long term safety on potassium embelate for use as an analgesic. PMID:6541278

Atal, C K; Siddiqui, M A; Zutshi, U; Amla, V; Johri, R K; Rao, P G; Kour, S

1984-08-01

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Analgesic effect of the aqueous and ethanolic extracts of clove  

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Full Text Available Objective: The beneficial effects of clove on toothache have been well documented. We have also previously shown the analgesic effects of clove essential oil. The present work was done to investigate the analgesic effects of the aqueous extract of clove using hot plate test. The possible role of opioid receptors in the analgesic effects of clove was also investigated using naloxone.Materials and Methods: Ninety male mice were divided into nine groups: (1) Saline, (2-4) Aaqueous (Aq 50, Aq 100, and Aq 200) groups which were treated with 50, 100, and 200 mg/kg of aqueous extract of clove, respectively, (5-7) Ethanolic (Eth 50, Eth 100, and Eth 200) groups which were treated with 50, 100, and 200 mg/kg of ethanolic extract of clove, respectively, and (8-9) Aq 100- Naloxone and Aq 200- Naloxone which were pretreated with 4 mg/kg of naloxone before injection of 100 or 200 mg/kg of the aqueous extract. The hot plate test was performed as a base record 10 min before injection of drugs and consequently repeated every 10 minutes after the injection.Results: The maximal percent effect (MPE) in the animal groups treated with 50, 100, and 200 mg/kg of aqueous extract was significantly higher than the control group. Pretreatment with naloxone reduced the analgesic effects of both 100 and 200 mg/kg of the aqueous extract. Administration of all three doses of the ethanloic extract also non-significantly increased the MPE.Conclusion: The results of the present study showed that aqueous extract of clove has analgesic effect in mice demonstrated by hot plate test which is reversible by naloxone. The role of opioid system in the analgesic effect of clove might be suggested. However, more investigations are needed to elucidate the exact mechanism(s).

Mina Kamkar Asl; Ashraf Nazariborun; Mahmoud Hosseini

2013-01-01

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[Analgesic effects of cannabinoids on central pain syndrome].  

UK PubMed Central (United Kingdom)

It was shown that cannabinoids anandamide, HU210 and WIN 55,212-2 inhibit both spontaneous episodes of pain and mechanical allodynia in rats with central pain syndrome caused by disturbance of inhibitory processes in the dorsal horns of lumbar spinal cord. The analgesic effect is most pronounced in the intrathecal route of administration. The intensity of analgesic actions of cannabinoids on the central pain syndrome in rats, depending on the drug is as follows: HU210 > WIN 55,212-2 > anandamide.

Igon'kina SI; Churiukanov MV; Churiukanov VV; Kukushkin ML

2011-10-01

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[Analgesic effects of cannabinoids on central pain syndrome].  

Science.gov (United States)

It was shown that cannabinoids anandamide, HU210 and WIN 55,212-2 inhibit both spontaneous episodes of pain and mechanical allodynia in rats with central pain syndrome caused by disturbance of inhibitory processes in the dorsal horns of lumbar spinal cord. The analgesic effect is most pronounced in the intrathecal route of administration. The intensity of analgesic actions of cannabinoids on the central pain syndrome in rats, depending on the drug is as follows: HU210 > WIN 55,212-2 > anandamide. PMID:22359935

Igon'kina, S I; Churiukanov, M V; Churiukanov, V V; Kukushkin, M L

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[Analgesic effects of H1 receptor antagonists in the rat model of formalin-induced pain].  

UK PubMed Central (United Kingdom)

BACKGROUND AND OBJECTIVES: Histamine receptors mediate nociceptive pathways, especially in the central nervous system. Some studies have demonstrated the analgesic effects of histamine receptor antagonists in the peripheral nervous system. It is not clear whether the local analgesic effect is class-specific or drug-specific. METHODS: To answer this question, we used three different H1 receptor antagonists (pyrilamine, promethazine, and cetirizine) administered directly in the paw of the rat, intraperitoneally, or in peripheral nerve blockade in the formalin-induced pain model. The effects of the drugs on the number of paw elevations were observed. RESULTS: In phase I, the local administration of pyrilamine caused a dose-dependent reduction on the number of paw elevations; in the highest dose, the number of paw elevations was reduced by 97.8%. Promethazine decreased it by 92%, while cetirizine decreased by 23.9%. In phase II, pyrilamine decreased the number of paw elevations by 93.5%, promethazine by 78.2%, and cetirizine by 80.1%. Intraperitoneal administration of drugs did not change painful behavior. When used in peripheral nerve block, in phase I pyrilamine reduced the number of paw elevations by 96.7%, promethazine by 73.3%, and cetirizine by 23.9%. In phase II, pyrilamine reduced the number of paw elevations by 86.6%, promethazine by 64.4%, and cetirizine by 19.9%. CONCLUSIONS: The results demonstrate that H1 receptor antagonists have local analgesic effects, different from the systemic effects, one of them an anti-inflammatory and class-specific effect and the other similarly to the local anesthetic effect, specific for promethazine and pyrilamine.

Ashmawi HA; Braun LM; Sousa AM; Posso Ide P

2009-07-01

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Analgesic effects of glycoproteins from Panax ginseng root in mice.  

UK PubMed Central (United Kingdom)

ETHNOPHARMACOLOGICAL RELEVANCE: The root of Panax ginseng C.A. Mey has various beneficial pharmacological effects. The present study aimed to evaluate the analgesic activities of glycoproteins from the root of Panax ginseng C.A. Mey in mice. MATERIALS AND METHODS: Glycoproteins were isolated and purified from the root of Panax ginseng C.A. Mey. Physicochemical properties and molecular mass were determined by chemical assay and HPLC. Acetic acid-induced writhing and hot-plate tests were employed to study the analgesic effect of glycoproteins and compared with that of aspirin or morphine. The locomotor activity was tested in mice by using actophometer. RESULTS: Four glycoproteins were obtained. The glycoproteins which protein content was the highest (73.04%) displayed dose-dependent analgesic effect. In writhing test, the glycoproteins significantly inhibited writhes (P<0.001) at the dose of 20 mg/kg by intraperitoneal injection. In hot-plate test, only at the dose of 20 mg/kg prolong the hot-plate latency (P<0.05, at 30 min). In the locomotor activity test, the glycoproteins were significant decrease of motility counts at the dose of 20 and 40 mg/kg. CONCLUSION: These findings collectively indicate that the glycoproteins from the root of Panax ginseng C.A. Mey exhibited significant analgesic activities and the proteins were the active site, providing evidence for its pharmacal use.

Wang Y; Chen Y; Xu H; Luo H; Jiang R

2013-07-01

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Synthesis and analgesic effects of novel ?(2)-tryptophan hexapeptide analogs.  

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Aiming to develop more potent analgesic substances a new series of hexapeptides containing ?(2)-tryptophan analogues was synthesized. The Trp in position 4 and 5, respectively in Ac-Arg-Phe-Met-Trp-Met-Lys-NH2 (opioid receptor antagonist) and Ac-Arg-Tyr-Tyr-Arg-Trp-Lys-NH2 (highly potent and selective NOP-receptor agonist) was substituted by the (S)-2-(1-methyl-1H-indol-3-yl)propionic residue or the (S)-2-(5-methoxy-1H-indol-3-yl)propionic residue. The analgesic effect of the four newly synthesized compounds has been evaluated in male Wistar rats by PP- and HP tests and compared to the native templates. Further estimation of the mechanisms of action of each compound was achieved using specific antagonists-naloxone for opioid and JTC801 for the NOP receptor. Replacement of Trp with ?(2)-tryptophan analogues in 4th position (Ac-Arg-Phe-Met-Trp-Met-Lys-NH2) led to increased and longer lasting analgesic effect. The results obtained permit us to assume that both opioid and NOP receptors take part in the newly synthesized compounds analgesic effects. PMID:23851698

Bocheva, Adriana; Nocheva, Hristina; Pavlov, Nikola; Todorov, Petar; Calmčs, Monique; Martinez, Jean; Naydenova, Emilia

2013-07-13

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Analgesic, anti-inflammatory and venotonic effects of Cissus quadrangularis Linn.  

UK PubMed Central (United Kingdom)

Cissus quadrangularis, a medicinal plant indigenous to Asia and Africa, is used for many ailments, especially for the treatment of hemorrhoid. The effects associated with hemorrhoid, i.e. analgesic and anti-inflammatory activities as well as the venotonic effect of the methanol extract of C. quadrangularis (CQ) were assessed in comparison with reference drugs. In the analgesic test, CQ provoked a significant reduction of the number of writhes in acetic acid-induced writhing response in mice. CQ also significantly reduced the licking time in both phases of the formalin test. The results suggest peripheral and central analgesic activity of CQ. In acute phase of inflammation CQ elicited the inhibitory effect on the edema formation of the rats' ear induced by ethyl phenylpropiolate as well as on the formation of the paw edema in rats induced by both carrageenin and arachidonic acid. It is likely that CQ is a dual inhibitor of arachidonic acid metabolism. In addition, CQ exerted venotonic effect on isolated human umbilical vein similarly to the mixture of bioflavonoids, i.e. 90% diosmin and 10% hesperidin. The results obtained confirmed the traditional use of C. quadrangularis for the treatment of pain and inflammation associated with hemorrhoid as well as reducing the size of hemorrhoids.

Panthong A; Supraditaporn W; Kanjanapothi D; Taesotikul T; Reutrakul V

2007-03-01

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Analgesic, anti-inflammatory and venotonic effects of Cissus quadrangularis Linn.  

Science.gov (United States)

Cissus quadrangularis, a medicinal plant indigenous to Asia and Africa, is used for many ailments, especially for the treatment of hemorrhoid. The effects associated with hemorrhoid, i.e. analgesic and anti-inflammatory activities as well as the venotonic effect of the methanol extract of C. quadrangularis (CQ) were assessed in comparison with reference drugs. In the analgesic test, CQ provoked a significant reduction of the number of writhes in acetic acid-induced writhing response in mice. CQ also significantly reduced the licking time in both phases of the formalin test. The results suggest peripheral and central analgesic activity of CQ. In acute phase of inflammation CQ elicited the inhibitory effect on the edema formation of the rats' ear induced by ethyl phenylpropiolate as well as on the formation of the paw edema in rats induced by both carrageenin and arachidonic acid. It is likely that CQ is a dual inhibitor of arachidonic acid metabolism. In addition, CQ exerted venotonic effect on isolated human umbilical vein similarly to the mixture of bioflavonoids, i.e. 90% diosmin and 10% hesperidin. The results obtained confirmed the traditional use of C. quadrangularis for the treatment of pain and inflammation associated with hemorrhoid as well as reducing the size of hemorrhoids. PMID:17095173

Panthong, Ampai; Supraditaporn, Wanicha; Kanjanapothi, Duangta; Taesotikul, Tawat; Reutrakul, Vichai

2006-09-26

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Making the decision to stop pain: Probability and magnitude effects of expected pain relief on the choice of analgesics.  

UK PubMed Central (United Kingdom)

BACKGROUND: Pain is a major ailment that motivates individuals to look for treatment. Despite its enormous clinical relevance, very little is known about the factors that influence our preference of an analgesic (or pain-relieving treatment). The current study investigated the influence of the information regarding the probability and the magnitude of the expected analgesic effect on preference of analgesic options. METHODS: Twenty-four healthy volunteers were instructed to imagine pain across different scenarios and choose between two hypothetical analgesics that differed in their probabilities to successfully relieve pain and the magnitude of their expected analgesic effects. The conservative analgesic was more reliable but less potent than the radical analgesic, whereas the radical analgesic was less reliable but more potent than the conservative analgesic. RESULTS: Consistent with the predictions of prospect theory, a larger proportion of the participants chose the radical analgesic when the overall probability of both analgesics decreased, and when the potency of the radical analgesic was expected to be stronger relative to the conservative analgesic. At the individual level, individuals' relative imagined pain relief (radical analgesic/conservative analgesic) predicted their preference for the radical analgesic. CONCLUSIONS: Our findings revealed that preference of analgesic options is mediated by the overall probability of analgesic effect and the relative potency of analgesics. The expected relief one imagines to obtain from analgesics would guide preference. The findings highlight the importance for clinicians to understand how patients subjectively frame the probability and magnitude factors related to decision making in medical context.

Lin C

2013-04-01

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Analgesic effect of clove essential oil in mice  

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Full Text Available Objective: Results obtained from literature reviews and human studies have shown the analgesic effects of clove plant in toothache. The present work was undertaken in order to investigate the possible analgesic effect of clove oil in mice.Materials and Methods: Fifty mice were divided into 5 groups: 1) Saline; 2) Essential oil (Ess) 2%, 3) Ess 5%, 4) Ess10% and 5) Ess 20%. The hot plate test (55±0.2 °C; Cut-off 60 sec) was performed as a base record 15 min before injection of drugs (Saline or 2, 5, 10 and 20% concentrations of Essential oil) and consequently repeated every 15 minutes after injection. Results: Repeated measures ANOVA test showed that maximal percent effect (MPE) in animal groups treated by 5, 10 and 20% essential oil was significantly higher than saline group. Comparison between 4 treated groups showed that MPE in 10% essential group was higher than 2 and 5% groups however; there was no significant difference between 10% and 20% groups.Conclusion: The result of present study showed that clove essential oil has analgesic effect inmice using hot plate test. More investigations are needed to elucidate the exact mechanism (s).

Mahmoud Hosseini; Mina Kamkar Asl; Hassan Rakhshandeh

2011-01-01

40

Hemostatic and analgesic effect of Gonghuan Zhixue Tablet on mice  

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Full Text Available Objective: To explore the hemostatic and analgesic effect of Gonghuan Zhixue Tablet (GHZXT) on mice and to produce experimental evidence for exploiting new drug for endometrorrhagia caused by Cu-intrauterine contraceptive device (Cu-IUD). Methods: Compared with 6-aminocaproic acid and notoginseng, the effects of GHZXT on clotting and bleeding time of mice with capillary method and severed tail were investigated; and compared with aspirin, the analgesic effects of GHZXT on mice were investigated with hot plate and torsive body method. Results: The clotting time of mice was remarkably shortened with a rising of the dosage of GHZXT and the difference between each therapeutic group and distilled water group was remarkable. As compared with distilled water group, the bleeding time of each dosage group of GHZXT was obviously shortened; and each dosage of GHZXT could prolong the time of pain reaction to hot plate and decrease the degree of torsive body of the mice. Conclusion: Pharmacological experiment has proved that GHZXT has evident hemostatic and analgesic function.

FU Ling-Mei

2004-01-01

 
 
 
 
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[Analgesic placebo effect: contribution of the neurosciences].  

Science.gov (United States)

Over the past twenty years, neuroscience has changed our understanding of placebo analgesia. Often perceived by researchers as a response bias adding noise to the assessment of efficacy, in the patients' view, it is associated with charlatanism. The origin of the word, qualifying a patient's response to "please" the doctor, did not help its rightful appreciation. However, today the placebo analgesia is considered as a psychobiological phenomenon. Thanks to pharmacological manipulations and the development of functional brain imaging, the neural circuitry involved in this effect as well as the role of endorphins and dopamine have been identified. This article describes our current knowledge about this fascinating phenomenon: a psychological modulation can lead to a biological effect. PMID:21815494

Berna, C; Cojan, Y; Vuilleumier, P; Desmeules, J

2011-06-29

42

Analgesic effects of gabapentine in tonsillectomy  

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Full Text Available Objectives: To evaluate the preemptive effects of gabapentin on postoperative pain relief and its effect on meperidine consumption in patients undergoing tonsillectomy. Methods: This study took place in King Abdulaziz Naval Base Hospital in the year 2009. Sixty patients ASA I and II were randomly assigned in a prospective randomized double- blind placebo-control clinical trial. Gabapentine 1200 mg or placebo was given orally two hours before induction of anesthesia to patients undergoing tonsillectomy under general anesthesia. Postoperative pain score was recorded on a visual analogue scale at 1, 3, 6, 12, 18 and 24 postoperative hours. Patients received meperidine 1 mg/ kg i.m once every 4 h if pain score 3 or if requested by the patient. Total dose of meperidine consumption was recorded. Results: Thirty patients in the gabapentine group and 30 patients in the placebo group completed the study. Patients in gabapentine group had significantly lower pain score in comparison to placebo group. Total postoperative meperidine consumption in the gabapentin group was (48.8±33.9 VS 93.8 ± 54.6) in the placebo group (P< 0.001). There was higher incidence of nausea, vomiting, and use of antiemetic drugs in the placebo group. Conclusion: Preemptive use of gabapentine decreased pain score and post operative meperidine consumption and reduced meperidine ­related adverse effects in patients undergoing tonsillectomy under general anesthesia.

Waleed Abdelmageed*, Salah Abdelrazik**, Ahmad Nassar

2010-01-01

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ACUTE CENTRAL AND PERIPHERAL ANALGESIC ACTIVITY OF ETHANOLIC EXTRACT OF THE LEAVES OF CLERODENDRUM VISCOSUM (EECV) IN RODENT MODELS  

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Full Text Available Pain, inflammation and pyrexia are the most common disturbing symptom a person experiences in life. Numerous drugs are available in the market for relieving these symptoms and which are sold over the counter. However they have high tendency of having adverse drug reaction from a trivial nausea and vomiting to gastric irritation leading to peptic ulcer, perforation and even death. The aim of the study was to investigate the acute peripheral activity of Ethanolic Extract of the leaves of Clerodendrum viscosum (EECV) by acetic acid induced writhing reflex test in mice and acute central analgesic activity by tail immersion method in rats. Dried powdered leaves of Clerodendrum viscosum were subjected to solvent extraction by using 90 % ethanol. Based on acute oral toxicity study according to Organization for Economic Cooperation and Development (OECD) guidelines No. 423, three doses of the test drug was selected (100, 200 & 400mg/kg for mice)  and (75, 150 & 300 mg/kg for rats), and were subjected to acute analgesic activity. The Ethanolic Extract of the leaves of Clerodendrum viscosum (EECV) showed significant (p

Chandra Shekar

2012-01-01

44

Postoperative analgesic efficacy of peripheral levobupivacaine and ropivacaine: a prospective, randomized double-blind trial in patients after total knee arthroplasty.  

UK PubMed Central (United Kingdom)

BACKGROUND: Several previous trials have characterized the intra- and postoperative effects of the recently introduced local anesthetics, levobupivacaine and ropivacaine, for a variety of continuous peripheral nerve blocks. METHODS: We compared the analgesic efficacy of levobupivacaine 0.125% versus ropivacaine 0.2% via patient-controlled femoral nerve analgesia after total knee arthroplasty. In a double-blind, randomized, prospective design, 60 patients received femoral infusion with either substance. We analyzed postoperative local anesthetic consumption, pain scores, motor block, and opioid requirements over 72 h. RESULTS: Pain scores, motor block incidence, and opioid requirements were low and not different between the groups. Ropivacaine consumption in milligrams was 67% higher than that of levobupivacaine. CONCLUSIONS: Both levobupivacaine 0.125% and ropivacaine 0.2% provide similar analgesia after total knee arthroplasty with the latter being less potent.

Heid F; Müller N; Piepho T; Bäres M; Giesa M; Drees P; Rümelin A; Werner C

2008-05-01

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Dipyrone elicits substantial inhibition of peripheral cyclooxygenases in humans: new insights into the pharmacology of an old analgesic.  

Science.gov (United States)

Dipyrone (INN, metamizol) is a common analgesic used worldwide. Its widespread prescription or over-the-counter use in many countries (e.g., Brazil, Israel, Mexico, Russia, Spain) requires insight into its mode of action. This study therefore addressed the impact of its metabolites 4-methyl-amino-antipyrine (MAA) and 4-amino-antipyrine (AA) on peripheral cyclooxygenases (COX). Pharmacokinetics of metabolites and ex vivo COX inhibition were assessed in five volunteers receiving dipyrone at single oral doses of 500 or 1000 mg. Coagulation-induced thromboxane B2 formation and lipopolysaccharide-induced prostaglandin E2 synthesis were measured in vitro and ex vivo in human whole blood as indices of COX-1 and COX-2 activity. In vitro, metabolites elicited no substantial COX-1/COX-2 selectivity with MAA (IC50=2.55 micromol/L for COX-1; IC50=4.65 micromol/L for COX-2), being approximately 8.2- or 9-fold more potent than AA. After administration of dipyrone, MAA plasma concentrations remained above the IC50 values for each isoform for at least 8 h (500 mg) and 12 h (1000 mg) postdose. COX inhibition correlated with MAA plasma levels (ex vivo IC50 values of 1.03 micromol/L [COX-1] and 0.87 micromol/L [COX-2]). By contrast, plasma peak concentrations of AA after the 1000 mg dose were 2.8- and 6.5-fold below its IC50 values for COX-1 and COX-2, respectively. Maximal inhibitions of COX-1 and COX-2 were 94% and 87% (500 mg), 97% and 94% (1000 mg). Taken together, dipyrone elicits a substantial and virtually equipotent inhibition of COX isoforms via MAA. Given the profound COX-2 suppression by dipyrone, which was considerably above COX-2 inhibition by single analgesic doses of celecoxib and rofecoxib, a significant portion of its analgesic action may be ascribed to peripheral mechanisms. In view of the observed COX-1 suppression, physicochemical factors (lack of acidity) rather than differential COX-1 inhibition may be responsible for dipyrone's favorable gastrointestinal tolerability compared with acidic COX inhibitors. PMID:17435173

Hinz, Burkhard; Cheremina, Olga; Bachmakov, Jouri; Renner, Bertold; Zolk, Oliver; Fromm, Martin F; Brune, Kay

2007-04-13

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Preemptive analgesic effects of intravenous paracetamol in total abdominal hysterectomy.  

UK PubMed Central (United Kingdom)

OBJECTIVES: Paracetamol is primarily thought to be a cyclooxygenase inhibitor acting through the central nervous system. Indirect effects of paracetamol are through the serotoninergic system as a non-opioid analgesic. In this study, total abdominal hysterectomy patients were given intravenous (iv) paracetamol 1 g preoperatively or intraoperatively to assess its postoperative analgesic effects. METHODS: 90 patients undergoing total abdominal hysterectomy were enrolled into the study. Patients were randomized into three groups: in Group I, iv paracetamol 1 g was given 30 minutes prior to induction. In Group II, iv paracetamol 1 g was given prior to skin closure. Group III served as the control group and received saline as placebo. Postoperatively, all patients received morphine via patient-controlled analgesia pump. Postoperatively, rest and activity pain scores, sedation scores, hemodynamic parameters, postoperative morphine consumption, side effects, patient satisfaction, and total hospital stay were recorded. RESULTS: In the control group, at rest and movement pain scores and total morphine consumption via patient-controlled analgesia were higher than in Groups I and II. When Groups I and II were compared, total morphine consumption was much greater in Group II. Intravenous paracetamol intraoperatively and postoperatively did not result in any hemodynamic effects. CONCLUSION: In total abdominal hysterectomy, preemptive iv paracetamol 1 g provided good quality postoperative analgesia, with decreased consumption of morphine and minimal side effects.

Arici S; Gurbet A; Türker G; Yava?cao?lu B; Sahin S

2009-04-01

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Central action of narcotic analgesics. VIII. The effect of dopaminergic stimulants on the action of analgesics in rats.  

UK PubMed Central (United Kingdom)

We investigated the influence of apomorphine, amphetamine, amantadine, dimethylaminoadamantane, nomifensine, ergometrine and beta-phenylethylamine on cataleptogenic and antinociceptive action of analgesics in rats. Nomifensine, apomorphine, beta-phenylethylamine, amantadine and ergometrine antagonized the catalepsy induced by morphine and codeine. Catalepsy induced by fentanyl was depressed only by nomifensine and apomorphine. Amphetamine only slightly antagonized the analgesic-induced catalepsy and the effects were not dose-dependent. Dimethylaminoadamantane did not antagonize catalepsy at all. Antinociceptive action of morphine and codeine was antagonized by apomorphine and amphetamine. Ergometrine counteracted the action of morphine, and beta-phenylethylamine decreased the action of pentazocine. The results suggest that: 1. There are differences in the mechanism of cataleptogenic action of the opiates (morphine and codeine) and fentanyl; 2. Catalepsy after analgesia differs from the catalepsy produced by neuroleptics in respect of interaction with such drugs as amphetamine, apomorphine or dimethylaminoadamantane. Analgesic-induced catalepsy seems to depend on the presynaptic inhibition of dopaminergic neurotransmission; 3. Stimulation of the central dopaminergic system in rat brain either does not change or weakly antagonizes the action of analgesics in the hot plate test.

Malec D; Langwi?ski R

1981-10-01

48

Analgesic effect of high intensity laser therapy in knee osteoarthritis.  

UK PubMed Central (United Kingdom)

Knee osteoarthritis (KOA), the most common type of osteoarthritis (OA), is associated with pain and inflammation of the joint capsule, impaired muscular stabilization, reduced range of motion and functional disability. High-intensity laser therapy (HILT) involves higher-intensity laser radiation and causes minor and slow light absorption by chromophores. Light stimulation of the deep structures, due to high intensity laser therapy, activates cell metabolism through photochemical effect. The transmissions of pain stimulus are slowed down and result in a quick achievement of pain relief. The aim of our research was to investigate the prompt analgesic effect of HILT on patients with KOA. Knee radiographs were performed on all patients and consequently graded using the Kellgren-Lawrence grading scale (K/L). A group of 96 patients (75 female, 21 male, mean age 59.2) with K/L 2 and 3 were submitted to HILT therapy. Pain intensity was evaluated with visual analogue scale (VAS) before and after the treatment. HILT consisted in one daily application, over a period of ten days, using protocol wavelength, frequency and duration. The results showed statistically significant decrease in VAS after the treatment (p < 0.001). Considering these results, HILT enables prompt analgesic effects in KOA treatment. Therefore HILT is a reliable option in KOA physical therapy.

Stigli?-Rogoznica N; Stamenkovi? D; Frlan-Vrgoc L; Avancini-Dobrovi? V; Vrbani? TS

2011-09-01

49

ANALGESIC EFFECTS OF GLUCOSE AND WATER IN NEONATES  

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Full Text Available Several methods have been used to relieve pain in neonates. The objective of this study was to assess the analgesic effect of 50% glucose and water during hepatitis B vaccination. In this randomized controlled trial, 90 term neonates were studied. Infants were randomly assigned to one of the three equal sized groups. First, heart rates were measured by EKG monitor. Then, 2mL of either 50% glucose or sterile water was administered into the mouths of infants in groups one and two, respectively. No intervention was done for group three. During vaccination until three minutes after, crying of babies was taped. Heart rates were measured during injection until 60 seconds. Mean values of duration of crying for glucose, water, and no intervention groups were 21.1 s, 33.3 s, and 56.9 s, respectively, which were significantly different (P= 0.0003). Post hoc test revealed substantial differences between groups one and three (P= 0.0001) and between groups two and three (P= 0.006). However, groups one and two were not statistically different (P= 0.19). Moreover, heart rate did not rise significantly in any of those groups. Both 50% glucose and water showed analgesic effects in neonates.

M. Golestan; S. Akhavan Karbasi; M. Modares-Mosadegh M. Sadr-Bafghi

2007-01-01

50

Activation of inhibition from the periaqueductal grey matter mediates central analgesic effect of metamizol (dipyrone).  

UK PubMed Central (United Kingdom)

The pyrazolone derivative, metamizol (dipyrone), possesses analgesic, antipyretic, anti-inflammatory and spasmolytic properties. It is often classified as peripherally acting. To test the possibility that a central action of the drug contributes to its antinociceptive and analgesic effects, experiments were carried out in which the tail-flick response to radiant heat, flexor reflex activity in the tibialis anterior muscle and activity in ascending spinal axons evoked by stimulation of afferent C fibres in the sural nerve, and activity of neurones in the periaqueductal grey matter and the substantia nigra were assessed in rats. Metamizol administered by intraperitoneal (i.p.; 10, 20 and 40 mg/kg) or intrathecal (i.t.; 50 to 400 micrograms) injection to intact rats dose-dependently prolonged the tail-flick latency. Administration by i.t. injection to spinal rats was without effect. Intravenous (i.v.) injection of metamizol (140 mg/kg) reduced flexor reflex activity in intact animals, while an i.t. injection to spinal rats was ineffective at a low dose (100 micrograms) or enhanced the reflex activity at a higher dose (400 micrograms). Activity in ascending axons responding to afferent C fibre stimulation was mostly depressed by i.t. injection of metamizol (40, 80 and 140 mg/kg) in rats with an intact spinal cord. Ascending activity was increased by i.t. injection of the drug (100 and 200 micrograms) to spinal rats. Metamizol (140 mg/kg) i.v. increased the activity of neurones in the PAG and reduced that of neurones in the substantia nigra. Metamizol administered by microinjection into the PAG prolonged the tail-flick latency (15-100 micrograms) and depressed C fibre-evoked activity in ascending axons (100 micrograms). The results suggest that a central action is involved in the analgesic effect of metamizol and that this central action manifests itself by an activation of inhibition originating in the PAG.

Carlsson KH; Helmreich J; Jurna I

1986-12-01

51

Analgesic effect of ketamine and morphine after tonsillectomy in children.  

UK PubMed Central (United Kingdom)

A comparative double blind study of Ketamine and Morphine was conducted on eighty children following tonsillectomy to assess the analgesic, respiratory rate depressant and emesis. Children (6-12 years) were divided into two groups randomly (n=40). General anesthesia was induced followed by 0.1mg/kg morphine (I/M) and 0.5mg/kg ketamine (I/M) to Group I and Group II respectively before the initiation of surgical procedure. Pain scores (face score and CHEOPS score) were estimated for children at thirty, sixty, one hundred and twenty and two hundred and forty minutes following surgery. Comparison of CHEOPS score estimation reflected that pain scores were statistically significant (P < 0.05) in Group I receiving Morphine as compared to Group II who received Ketamine. The analgesic effect of ketamine and morphine showed statistically insignificant results (P >0.05) in case of face score. Moreover, respiratory rate in Group I had shown statistical association (p<0.05) as compared to the ketamine at 60 and 120 minutes. Furthermore, incidence of vomiting was more in Group I (0.05) as compared to Group II. It can be concluded from the study that ketamine may be used as a suitable substitute to that of morphine in children undergoing tonsillectomy.

Hasnain F; Janbaz KH; Qureshi MA

2012-07-01

52

Analgesic effect of Lepidium sativum Linn. (Chandrashura) in experimental animals.  

Science.gov (United States)

Lepidium sativum Linn, which is known as "Aselio" locally, is frequently used by the villagers for the treatment of Sandhivata (osteoarthritis), with good therapeutic relief. Here, we have to observe the analgesic activity of the seed of Lepidium sativum Linn in albino rats and Swiss albino mice with different parameters. The analgesic study was performed with acetic acid-induced writhing response in mice, formaldehyde-induced paw licking response in rats and tail flick response in mice. Experiments were carried out in two groups - therapeutic dose group and double dose group - with comparison with the control group. In the acetic acid-induced writhing syndrome, latency of onset was highly significantly increased in the therapeutic dose group and significant increase was found in the double dose group. In the formaldehyde-induced paw licking response, the test drug produced significant inhibition of neurogenic pain in the double dose group and significant inhibition of inflammatory pain in the therapeutic dose group. In the tail flick response, the test drug produced a mild to moderate effect in the therapeutic dose group and also in the double dose group. PMID:22131742

Raval, Nita D; Ravishankar, B

2010-07-01

53

Analgesic effect of Lepidium sativum Linn. (Chandrashura) in experimental animals.  

UK PubMed Central (United Kingdom)

Lepidium sativum Linn, which is known as "Aselio" locally, is frequently used by the villagers for the treatment of Sandhivata (osteoarthritis), with good therapeutic relief. Here, we have to observe the analgesic activity of the seed of Lepidium sativum Linn in albino rats and Swiss albino mice with different parameters. The analgesic study was performed with acetic acid-induced writhing response in mice, formaldehyde-induced paw licking response in rats and tail flick response in mice. Experiments were carried out in two groups - therapeutic dose group and double dose group - with comparison with the control group. In the acetic acid-induced writhing syndrome, latency of onset was highly significantly increased in the therapeutic dose group and significant increase was found in the double dose group. In the formaldehyde-induced paw licking response, the test drug produced significant inhibition of neurogenic pain in the double dose group and significant inhibition of inflammatory pain in the therapeutic dose group. In the tail flick response, the test drug produced a mild to moderate effect in the therapeutic dose group and also in the double dose group.

Raval ND; Ravishankar B

2010-07-01

54

Analgesic effects of various extracts of the root of Abutilon indicum linn  

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Full Text Available Purpose : Abutilon indicum (Linn.) sweet (Malvaceae) commonly called ?Country Mallow? is a perennial plant up to 3 m in height. It is abundantly found as a weed in the sub-Himalayan tract and in the hotter parts of India. The plant is traditionally used for treatment of several diseases like bronchitis, body ache, toothache, jaundice, diabetes, fever, piles, leprosy, ulcers, cystitis, gonorrhea, diarrhea, and so on. Abutilon indicum Linn. is reported to have hepatoprotective, hypoglycemic, antimicrobial, male contraceptive, and antidiarrheal activities. The present study was done to evaluate the analgesic potential of various extracts of the root of Abutilon indicum Linn. Materials and Methods : The powdered root (900 g) was subjected to successive solvent extraction, with solvents in increasing order of polarity, namely, petroleum ether (60 - 80?C), methanol, and ethanol, using the soxhlet apparatus for 72 hours. The marc was extracted by cold maceration for 72 hours, to obtain a water-soluble extract. The peripheral analgesic activity was studied using acetic acid-induced writhing method in Swiss albino mice (20 - 30 g), while the central analgesic activity was evaluated by the tail flick method and the tail immersion method. Results : Results indicated that all the tested extracts, except the methanol extract, exhibited significant analgesic activity in both animals? models. Petroleum ether extract showed higher analgesic activity. The activity may be related to the central mechanism or may be due to the peripheral analgesic mechanisms. Conclusion : The present study authenticates the traditional use.

Goyal Naveen; Singh Sumitra; Sharma Surendra

2009-01-01

55

Analgesic Effects and Side Effects of Combinations of Morphine and Dextroamphetamine.  

Science.gov (United States)

To evaluate the feasibility of combination drug therapy for postoperative pain, analgesic and other effects of morphine and dextroamphetamine administered together were measured in 450 surgical patients in five Veterans Administration Hospitals using a ra...

D. L. Mahler G. Teutsch R. Defalque P. Shroff H. E. Gordon

1976-01-01

56

The Effect of Saliva Officinalis Hydroalcoholic Extract on Analgesic Effect of Morphine in Rat  

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Full Text Available Background and Objective: There are some reports in Iranian traditional medicine concerning the anti-inflammatory effect of Saliva Officinalis (SO). In the present study with the aim of decreasing analgesic dose of morphine, analgesic effect of different doses of SO hydroalcoholic extract alone and associated with morphine were evaluated by tail flick in rats. Subjects and Methods: Analgesic effects of SO hydroalcholic extract at doses of 200, 400, 600, 800 and 1000 mg/kg, i.p. were investigated. Then the influence of these doses associated with analgesic dose of morphine (2.5 mg/kg) was evaluated. Rats were placed into restrainer and then transferred into the tail flick apparatus with the intensity 55 Cş and cut off time= 10 sec. In order to verify the role of opioid receptors on analgesic effect of SO extract, naloxone (1mg/kg, i.p.) was administered to one group of rats 15 min before receiving 800 mg/kg extract. Then, the data were analyzed by two-way ANOVA followed by LSD post hoc test and significant difference between groups was accepted with P<0.05. Results: The Data have shown that, the SO extract relieved pain in tail-flick test dose dependently and the most effective dose was 800 mg/kg. The maximum analgesic effect of the extract combined with morphine was observed at time point 45 min. Naloxane, opioid receptor antagonist could reduce analgesic effect of the extract. Conclusion: On the basis the results obtained in this study, it could be suggested that the SO extract potentiates morphine anti-nociceptive effect and this means that the opioid system may be involved in the analgesic effect of this plant extract. Sci Med J 2011;10(5):505-13

A Arzi; A Sarkaki; N Aghel; Z Nazari; M Zarei Naserabadi

2011-01-01

57

The analgesically effective peptide deprolorphin exhibits cross-tolerance to morphine in rats.  

UK PubMed Central (United Kingdom)

The potent analgesically active beta-casomorphin derivative, D-Pro4-beta-casomorphin 1-5 (= Deprolorphin), was tested for its capacity to induce tolerance. In animals tolerant to morphine, a previously analgesically effective test dose of the peptide was without any antinocipetive effect, demonstrating a cross-tolerance between morphine and deprolorphin.

Grecksch G; Rüthrich HL

1985-01-01

58

Topical analgesics.  

UK PubMed Central (United Kingdom)

BACKGROUND AND OBJECTIVES: Pain treatment involves the usage of common and opioid analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs) and adjuvant analgesics. Traditionally, these drugs are administered systemically or into the neuraxis. However, when analgesics are applied through these pathways, they are associated with significant side effects, which can hinder its use. Topical administration of analgesics is an alternative. The objective of this paper is to discuss topical analgesics, the mechanisms of action and clinical efficacy. CONTENT: This is a review paper addressing the usage of the topical local anesthetics: capsaicin, clonidine, tricyclic antidepressants, ketamine, opioids and cannabinoids, discussing mechanism of action and effectiveness. CONCLUSIONS: Topical analgesics are promising as a strategy for pain treatment, as they are associated with lower incidence of side effects. The benefit of local anesthetics, NSAID's and capsaicin is well established. However, the efficacy of clonidine, tricyclic antidepressants, ketamine, opioids and cannabinoids is still questionable. Studies have shown that the multimodal approach is an alternative, but studies are needed to confirm this hypothesis.

Flores MP; Castro AP; Nascimento Jdos S

2012-03-01

59

Analgesic activity and pharmacological characterization of N-[1-phenylpyrazol-3-yl]-N-[1-(2-phenethyl)-4-piperidyl] propenamide, a new opioid agonist acting peripherally.  

Science.gov (United States)

We previously reported the synthesis of three new opioid agonists as well as their in vitro and in vivo activity [Girón, R., Abalo, R., Goicoechea, C., Martín, M.I., Callado, L.F., Cano, C., Goya, P., Jagerovic, N. 2002. Synthesis and opioid activity of new fentanyl analogs. Life Sci. 71, 1023-1034]. One of them, N-[1-phenylpyrazol-3-yl]-N-[1-(2-phenethyl)-4-piperidyl)] propenamide (IQMF-4), showed an interesting antinociceptive activity. Intraperitoneally (i.p.) administered, it was as effective as fentanyl or morphine, being less potent than fentanyl but more so than morphine. The aim of the present work was to evaluate its antinociceptive effect by different routes of administration, using the hot plate test, and to investigate possible side effects, such as tolerance and withdrawal, in vitro, using the myenteric plexus-longitudinal muscle strip preparation from guinea pig ileum, and in vivo, using the hot plate test. IQMF-4 was more potent than morphine when administered per os (p.o.), but less potent when administered intracerebroventricularly (i.c.v.). By both routes, fentanyl is more potent that IQMF-4. When IQMF-4 was administered i.p., naloxone methiodide, a peripherally acting antagonist, was able to completely block its antinociceptive effect, whereas, after i.c.v. administration, the blockade was only partial. An interesting feature of the new compound is that it induces tolerance in vitro but not in vivo. Moreover, though in vitro withdrawal was not different from fentanyl or morphine, in vivo withdrawal symptoms were significantly less frequent in mice treated with IQMF-4 than in those treated with morphine or fentanyl. Although more assays are required, these results show that IQMF-4 appears to be a potent analgesic compound with an interesting peripheral component, and reduced ability to induce dependence. PMID:18706410

Goicoechea, Carlos; Sánchez, Eva; Cano, Carolina; Jagerovic, Nadine; Martín, Maria Isabel

2008-07-31

60

An in vitro investigation of the effect of some analgesics on human enamel.  

UK PubMed Central (United Kingdom)

The sale of over-the-counter pain relief medication has increased dramatically in recent years, and typically amounts to several hundred thousands of pounds per year in the UK. Many soluble analgesic preparations contain citric acid, and it has been suggested that these formulations may cause dental erosion. The aim of this study was to investigate the effect of some over-the-counter analgesics on tooth surface loss from human enamel. Six commonly available analgesics were chosen for this study and the effect of immersing unerupted human enamel was examined using non-contact optical profilometry. Two of the six analgesics investigated caused no detectable erosion (Boots soluble aspirin and Anadin Extra). Three caused statistically significant enamel erosion, but this was very slight and is thought to be clinically insignificant (Alka Seltzer, Panadol and Solpadeine). Only one analgesic caused possible potentially clinical significant enamel erosion. Further studies are needed to determine whether Aspro causes clinically significant enamel erosion.

McNally LM; Barbour ME; O'Sullivan DJ; Jagger DC

2006-07-01

 
 
 
 
61

Chronopharmacology of analgesic effect and its tolerance induced by morphine in mice.  

UK PubMed Central (United Kingdom)

The influence of morphine dosing time on analgesic effect after acute or chronic treatment, recovery of analgesic effect after once developed tolerance, and their pharmacological mechanisms were investigated in ICR male mice under a 12-h light/dark cycle (light on from 7:00 AM to 7:00 PM). There was a significant 24-h rhythm in the latency of thermal response at 30 min after morphine injection. The analgesic effect was significantly greater at the dark phase than at the light phase. The rhythmic pattern resembled overall the rhythm occurring in the latency of thermal response under non-drugged state. The absolute value of morphine analgesic effect (the real time spent on the hot-plate) on days 1 and 2 after morphine daily injection was significantly larger after morphine injection at 9:00 PM than after saline injection at 9:00 PM or after morphine injection at 9:00 AM. The recovery from tolerance of analgesic effect was significantly faster at the dark phase than at the light phase. The time-dependent difference in the analgesic effect after chronic treatment or recovery from tolerance is closely related to that in the expression of mu-opioid receptor. The present study suggests that 24-h rhythm of morphine analgesic effect is consistent with 24-h rhythm of mu-opioid receptor expression.

Yoshida M; Ohdo S; Takane H; Tomiyoshi Y; Matsuo A; Yukawa E; Higuchi S

2003-06-01

62

Contribution of oxycodone and its metabolites to the overall analgesic effect after oxycodone administration.  

UK PubMed Central (United Kingdom)

OBJECTIVE: Oxycodone (OC) is an opioid which exerts its analgesic effect through µ-receptors in the brain. It is metabolized through CYP450 enzymes and some of the metabolites show pharmacological activity. The aim of this investigation is to research the contribution of the metabolites of OC to its overall analgesic effect. A further aim was to elucidate the role of drug-drug interactions and CYP2D6 polymorphism. RESEARCH DESIGN AND METHODS: The authors performed a literature search to identify published information on: blood concentrations of OC and metabolites, protein binding, blood-brain-barrier behavior and opioid receptor affinity. The authors then calculated the contribution of OC and metabolites to the overall analgesic effect. RESULTS: OC itself is responsible for 83.02 and 94.76% of the analgesic effect during p.o. and i.v. administration, respectively. Oxymorphone (OM), which has a much higher affinity for the µ-receptor, only plays a minor role (15.77 and 4.52% for p.o. and i.v., respectively). Although the CYP2D6 genotype modulates OM pharmacokinetics, OC remains the major contributor to the overall analgesic effect. CONCLUSION: This article's calculations demonstrate that OC itself is responsible for the analgesic effect. Although OM and noroxymorphone have much higher µ-receptor affinity than the parent drug, the metabolite concentrations at the site of action are very low. This suggests that there is a minimal analgesic effect from these metabolites.

Klimas R; Witticke D; El Fallah S; Mikus G

2013-05-01

63

Analgesic effect of high intensity laser therapy in knee osteoarthritis.  

Science.gov (United States)

Knee osteoarthritis (KOA), the most common type of osteoarthritis (OA), is associated with pain and inflammation of the joint capsule, impaired muscular stabilization, reduced range of motion and functional disability. High-intensity laser therapy (HILT) involves higher-intensity laser radiation and causes minor and slow light absorption by chromophores. Light stimulation of the deep structures, due to high intensity laser therapy, activates cell metabolism through photochemical effect. The transmissions of pain stimulus are slowed down and result in a quick achievement of pain relief. The aim of our research was to investigate the prompt analgesic effect of HILT on patients with KOA. Knee radiographs were performed on all patients and consequently graded using the Kellgren-Lawrence grading scale (K/L). A group of 96 patients (75 female, 21 male, mean age 59.2) with K/L 2 and 3 were submitted to HILT therapy. Pain intensity was evaluated with visual analogue scale (VAS) before and after the treatment. HILT consisted in one daily application, over a period of ten days, using protocol wavelength, frequency and duration. The results showed statistically significant decrease in VAS after the treatment (p KOA treatment. Therefore HILT is a reliable option in KOA physical therapy. PMID:22220431

Stigli?-Rogoznica, Nives; Stamenkovi?, Doris; Frlan-Vrgoc, Ljubinka; Avancini-Dobrovi?, Viviana; Vrbani?, Tea Schnurrer-Luke

2011-09-01

64

The study of analgesic effect of hydroalcoholic extract of FicuscaricaLeafin rat by formalin test  

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Full Text Available Background and Objective: Whereas the available synthetic analgesic drugs have side effects, it seems tobe logical to using herbal medicines with few side effects. The purpose of this study was the evaluation of analgesic effect of hydroalcoholic extract of ficuscarica leaf and comparing it with morphine and aspirin. Materials and Methods: This study was done on male rats of Wistar species. The animals were divided into nine groups (n= 6 rats). A negative control group received a single intraperitoneal dose of normal saline (5ml/kg). Two positive control groups received morphine (2.5 mg/kg) and aspirin (300 mg/kg) intraperitoneally, respectively. Five treatment groups received a single intraperitoneal dose of 200, 400, 600, 800 and 1000 mg/kg of hydroalcoholic extract of Ficuscarica leaves, and a group received hydroalcoholic extract (800mg/kg) with naloxon (1mg/kg). In this study, the analgesic effects were investigated via formalin test. Results: The results showed that the 600, 800, 1000 mg/kg of extract had analgesic effects significantly different in comparison with negative control group. Our results showed that the analgesic effect (800 mg/kg) was less than aspirin on the second phase of pain and morphine on both pain phases. Naloxone could reduce the analgesic effect of extract on the second phase of pain. Conclusion: The hydroalcoholic extract of Ficuscarica leaf contains analgesic effects in both pain phases. It can be concluded that Ficuscarica leaf extract may induce its effect through opioid receptors activation. ?Please cite this paper as: Arzi A , Aghel N, Nazari Z, Houseini M. The Study of Analgesic Effect of Hydroalcoholic Extract of Ficuscarica Leaf in Rat by Formalin Test. Jundishapur Sci Med J. 2012;11(4):383-392

Ardeshir Arzi; Nasrin Aghel; Zahra Nazari; Mostafa Houseini

2012-01-01

65

Analgesic activity of Heliopsis longipes and its effect on the nervous system.  

Science.gov (United States)

Heliopsis longipes S.F. Blake (Asteraceae: Heliantheae) (chilcuague) is used in Mexican traditional medicine against parasites and to alleviate tooth and muscle pains. Its biocide effect has already been experimentally demonstrated; however, its analgesic action and its action on the nervous system (NS) have not been investigated yet. The objectives of this study were to evaluate the analgesic action of affinin and the H. longipes root ethanol extract, as well as their effects on the NS using an animal model. The ethanol extract was obtained by maceration, and affinin was purified from it through chromatographic techniques. Chemical and thermal analgesia were used to assess their analgesic proprieties. Irwin's test was used to evaluate their stimulating or depressing effects. The ethanol extract and affinin displayed analgesic action similar to ketorolac and stimulating effect comparable to caffeine on the nervous system of adult mice. PMID:20645840

Cilia-López, V G; Juárez-Flores, B I; Aguirre-Rivera, J R; Reyes-Agüero, J A

2010-02-01

66

ANALGESIC (VERSIONS)  

UK PubMed Central (United Kingdom)

FIELD: medicine. ^ SUBSTANCE: analgesic contains alcoholic extract of elevated bloom of poison hemlock (Conium maculatum L) in the component ratio as follows, wt %: dry elevated bloom of poison hemlock -10, 40% ethanol - 90 fresh elevated bloom of poison hemlock - 2, 40% ethanol - 98 ethyl acetate fraction from elevated bloom of poison hemlock. ^ EFFECT: absence of side effects. ^ 4 cl, 3 ex, 1 tbl

POPOVA ELENA VLADISLAVOVNA; POVET EVA TAT JANA NIKOLAEVNA; NESTEROVA JULIJA VLADIMIROVNA; ANDREEVA TAMARA IVANOVNA; SUSLOV NIKOLAJ INNOKENT EVICH; PASHINSKIJ VITALIJ GLEBOVICH; PROVALOVA NADEZHDA VALER EVNA; ZELENSKAJA KRISTINA LEONIDOVNA; AKSINENKO SVETLANA GENNAD EVNA; NAGORNJAK JULIJA GENNAD EVNA; GAJDAMOVICH NATAL JA NIKOLAEVNA; PUSHKARSKIJ SERGEJ VITAL EVICH

67

Analgesic effect of Lepidium sativum Linn. (Chandrashura) in experimental animals  

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Lepidium sativum Linn, which is known as “Aselio” locally, is frequently used by the villagers for the treatment of Sandhivata (osteoarthritis), with good therapeutic relief. Here, we have to observe the analgesic activity of the seed of Lepidium sativum Linn in albino rats and Swiss albino mice wit...

Raval, Nita D.; Ravishankar, B.

68

ANALGESIC AND ANTIINFLAMMATORY EFFECTS OF TOTAL EXTRACT, FLAVONOID FRACTION AND VOLATILE OIL OF SALVIA HYDRANGEA  

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Full Text Available Background. Gol-e-arvaneh with the scientific name of salvia hydrangea (Labiatea) belongs to Salvia genus. In traditional medicine it has been used as analgesic, relieving headache, cold remedy, antipyretic and diuretic. Since until now this plant has not been investigated pharacologically. This study was aimed to find any anti-inflammatory or analgesic activity of the plant. Methods. At first, total extract, flavonoid fraction and volatile oil was prepared. Analgesic effect was assessed using light tail flick and acetic acid writhing test. Male wistar rats (180-220g) and mice (25±2g) were used in these tests. Carrageen in test was used for assessing anti-inflammatory activity. Results. Total extract and flavonoid fraction could not produce analgesic effect in light tail flick test, while morphine as a standard drug 15 and 30 min. after administration produced 35% and 90% of MPE respectively. In writhing test, total extract and flavonoid fraction had considerable analgesic effect which was comparable to that of indomethacin. Results of Carageenin test showed that both total extract and flavonoid fraction had marked anti-inflammatory activity and volatile oil had only a slight effect. Discussion. Since potent drugs (such as opioids) show positive response to light tail flick test, it seems that the plant lacks such compounds. Considerable analgesic activity of total extract and flavonoid fraction in writhing test and also their anti-inflammatory activity indicate that this plant is probably useful for relieving pains, particularly with inflammatory origin.

V.A HAJ HASHEMI; A GHANADI; D MOSAVI

2000-01-01

69

The Study of Analgesic Effect of Hydroalcoholic Extract of Ficuscarica Leaf in Rat by Formalin Test  

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Full Text Available Background and Objective: Whereas the available synthetic analgesic drugs have side effects, it seems tobe logical to using herbal medicines with few side effects. The purpose of this study was the evaluation of analgesic effect of hydroalcoholic extract of ficuscarica leaf and comparing it with morphine and aspirin.Materials and Methods: This study was done on male rats of Wistar species. The animals were divided into nine groups (n= 6 rats). A negative control group received a single intraperitoneal dose of normal saline (5ml/kg). Two positive control groups received morphine (2.5 mg/kg) and aspirin (300 mg/kg) intraperitoneally, respectively. Five treatment groups received a single intraperitoneal dose of 200, 400, 600, 800 and 1000 mg/kg of hydroalcoholic extract of Ficuscarica leaves, and a group received hydroalcoholic extract (800mg/kg) with naloxon (1mg/kg). In this study, the analgesic effects were investigated via formalin test.Results: The results showed that the 600, 800, 1000 mg/kg of extract had analgesic effects significantly different in comparison with negative control group. Our results showed that the analgesic effect (800 mg/kg) was less than aspirin on the second phase of pain and morphine on both pain phases. Naloxone could reduce the analgesic effect of extract on the second phase of pain. Conclusion: The hydroalcoholic extract of Ficuscarica leaf contains analgesic effects in both pain phases. It can be concluded that Ficuscarica leaf extract may induce its effect through opioid receptors activation.

Ardeshir Arzi; Nasrin Aghel; Zahra Nazari; Mostafa Houseini

2012-01-01

70

Analgesic effects of adenosine during exercise-provoked myocardial ischaemia.  

UK PubMed Central (United Kingdom)

The analgesic potential of adenosine during myocardial ischaemia was studied in patients with coronary artery disease and exercise-limiting angina pectoris. Patients were given a low dose of adenosine or placebo in a double-blind cross-over fashion by continuous i.v. infusion before and during two exercise tests. Adenosine decreased chest pain by 45 +/- 13% (p < 0.02) while heart rate-blood pressure product and electrocardiographic signs of myocardial ischaemia did not change. Ten healthy volunteers received increasing doses of adenosine by continuous i.v. infusion. The heat pain threshold increased in skin covering the chest (p < 0.03) and also tended to increase at the left thenar eminence (p < 0.07). In conclusion, the neuromodulator adenosine can therefore act as an analgesic in myocardial ischaemia.

Sylvén C; Eriksson B; Jensen J; Geigant E; Hallin RG

1996-06-01

71

Preliminary evaluation on anti-inflammatory and analgesic effects of Sideritis syriaca L. herba extracts.  

Science.gov (United States)

We studied the anti-inflammatory and analgesic activity of extracts of Sideritis syriaca L. herba. Samples were collected from the wild plant, dried, powdered, and extracted with hexane and methanol. The extracts were evaporated to dryness and then suspended in suitable solvent. They were then tested for anti-inflammatory activity in the carrageenin rat paw edema test and for analgesic activity in the Randall and Selitto test and in the tail-flick test. At 24 hours after the treatment, the gastric mucosa of each rat was observed macroscopically. Based on these results the hexane extract was fractionated by column chromatography, and the fractions were obtained tested in the same way. Results showed interesting anti-inflammatory activity only for the hexane extract and all the fractions obtained from it. All the extracts and all the other fractions showed both peripheral and central analgesic activity. In rats treated with the tested compounds hyperemia and ulcers were absent. The data from this preliminary study reveal interesting pharmacological properties of S. syriaca L. herba extracts related to the marked analgesic activity and the absence of gastric ulcerogenic activity. The same is for anti-inflammatory activity, but in this case it seems to be related only to the apolar fraction. PMID:16117615

Menghini, Luigi; Massarelli, Paola; Bruni, Giancarlo; Menghini, Alessandro

2005-01-01

72

Analgesic Effect of Aqueous and Hydroalcoholic Extracts of Three Congolese Medicinal Plants: Hyptis suavolens, Nauclea latifolia and Ocimum gratissimum  

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Full Text Available Analgesic effect of aqueous and hydroalcoholic extracts of aeral parts of Hyptis suavolens, Nauclea latifolia and Ocimum gratissimum, three plants used in congolese folk medicine in pain, were tested on acetic acid and hot plate tests. All extracts manifest analgesic effect on the two models used. The more active was the hydroalcoholic extract of Ocimum gratissimum which is not antagonized by naloxone and could potentiate analgesic effect of paracetamol.

N. Okiemy-Andissa; M.L. Miguel; A.W. Etou; J.M.Ouamba; M. Gbeassor; A.A. Abena

2004-01-01

73

Evidence for anti-inflammatory and putative analgesic effects of a monoclonal antibody to calcitonin gene-related peptide.  

UK PubMed Central (United Kingdom)

BACKGROUND: Calcitonin gene-related peptide (CGRP) is a powerful pro-inflammatory mediator thought to play a significant role in the development of inflammation and pain. We investigated the role of CGRP in trigeminal inflammatory pain by determining the ability of a monoclonal antibody to CGRP to modify central Fos expression in response to stimulation of the inflamed ferret tooth pulp. We also assessed the effect of the antibody on pulpal inflammation. METHODS: Ten adult ferrets were prepared under anaesthesia to allow stimulation of the upper and lower left canine pulps, recording from the digastric muscle and intravenous injections at subsequent experiments. In all animals, pulpal inflammation was induced by introducing human caries into a deep buccal cavity. Four days later animals were treated intravenously with either CGRP antibody (n=5) or vehicle (n=5). After a further 2 days animals were re-anaesthetised and the tooth pulps stimulated at 10 times jaw-opening reflex threshold. Brainstems and tooth pulps were processed immunohistochemically for Fos and the common leucocyte marker CD45, respectively. RESULTS: Fos was expressed in ipsilateral trigeminal subnuclei caudalis (Vc) and oralis (Vo). Significantly fewer Fos-positive nuclei were present within Vc of CGRP antibody-treated animals (p=0.003 vs vehicle-treated). Mean percentage area of staining for CD45 was significantly less in antibody-treated animals (p=0.04 vs vehicle-treated). CONCLUSIONS: This is the first direct evidence that sequestration of CGRP has anti-inflammatory and putative analgesic effects. Previous studies using this Fos model have demonstrated that it is able to predict clinical analgesic efficacy. Thus these data indicate that this antibody may have analgesic effects in dental pain and other types of inflammatory-mediated transmission, and suggest that this is in part due to peripheral anti-inflammatory effects.

Bowler KE; Worsley MA; Broad L; Sher E; Benschop R; Johnson K; Yates JM; Robinson PP; Boissonade FM

2013-01-01

74

Effects of Papaver rhoeas Extract on the Tolerance Development to Analgesic Effects of Morphine in Mice  

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Full Text Available Previous studies have shown that the extract of Papaver rhoeas reduces morphine dependence, locomotor activity and reward. In present study, the effects of hydro-alcohol extract of Papaver Rhoeas on the tolerance to analgesic effects of morphine in mice have been investigated using tail flick method. Subcutaneous (s.c.) administration of morphine (1, 2, 5 and 10 mg/kg) induced analgesia. However, intrapretoneal administration of the hydro-alcohol extract of Papaver rhoeas (25, 50 and 100 mg/kg) had not an effects on analgesia. Reduction of analgesic in mice pretreated with morphine (50 mg/kg, twice daily; for 3 days), alone, indicated that tolerance has been developed. Hydro-alcohol extract of Papaver rhoeas (25, 50 and 100 mg/kg, i.p.) administration, 30 min before each of three daily doses of morphine, attenuated the morphine tolerance dose-independently,indicating that administration of the extract reduces morphine tolerance in mice.

Jamal Shams; Hedayat Sahraei; Zohreh Faghih-Monzavi; Seyed Hossein Salimi; Seyedeh Maedeh Fatemi; Ali Pourmatabbed; Hassan Ghoshooni; Mohammad Kamalinejad

2008-01-01

75

[Assessment of ropivacaine postoperative analgesic effect after periapical maxillary incisors surgery].  

UK PubMed Central (United Kingdom)

BACKGROUND/AIM: Ropivacaine is a relatively new long-acting local anesthetic. The aim of this study was to compare the postoperative analgesic effect of topical anesthetics ropivacaine 0.75% and lidocaine 2% with adrenaline in the postoperative treatment of periapical lesions in the maxilla. METHODS: The study was conducted on 60 subjects, divided into two groups. The study-group received 0.75% ropivacaine without a vasoconstrictor, while the control group was treated with 2% lidocaine with adrenaline (1 : 80.000). Block anesthesia for n. infraorbitalis was used and local anesthetics were applied also on the palatine side for the end branches of n. nasopalatinus. The following parameters were observed: time elapsed from the application of an anesthetic until the first occurrence of pain after the surgery and first intake of an analgesic, the intensity of initial pain, pain intensity 6 h after the application of anesthetics and the total number of analgesics taken within 24 h after the completion of surgery. RESULTS: The pain appeared statistically significantly earlier in the patients who had been given lidocaine with adrenaline (p < 0.001), while statistically significantly higher mean values of initial postoperative pain (p < 0.05) and pain intensity 6 h after the intervention (p < 0.01) were also registered in the same group of patients. In the period of 24 h upon the intervention, the study-group patients were taking less analgesics as compared to the control-group subjects (46.6% vs 73.3%), who were given analgesics earlier, although no statistically significant differences were observed related to the number of analgesic doses taken. CONCLUSION: The results of our study indicate a better postoperative analgesic effect of ropivacaine as compared to lidocaine with adrenaline.

Tijani? M; Buri? N; Jovanovi? G; Stojanovi? S; Spasi? M

2012-05-01

76

The analgesic effect and mechanism of the combination of sodium ferulate and oxymatrine.  

UK PubMed Central (United Kingdom)

Sodium ferulate (SF) and Oxymatrine (OMT) were compounds extracted from Chinese herbs, and have been used in clinical treatment of heart and hepatic diseases, respectively, in China for many years. The objective of this study was to examine the analgesic effect and the mechanism of the combined treatment of SF and OMT. Using the animal pain models by applying Acetic Acid Writhing Test and Formalin Test, the combination of SF and OMT showed significant analgesic effect in dose-dependent manner. In vitro, the combined treatment inhibited the increase in intracellular calcium concentration evoked by capsaicin in the dorsal root ganglion neurons. Importantly, a synergistic inhibitory effect of SF and OMT on the capsaicin-induced currents was demonstrated by whole-cell patch-clamp. Our results suggest that SF and OMT cause significant analgesic effect which maybe related to the synergistic inhibition of transient receptor potential vanilloid-1.

Liu H; Sun Y; Gao Y; Chen F; Xu M; Liu Z

2010-09-01

77

The analgesic effect and mechanism of the combination of sodium ferulate and oxymatrine.  

Science.gov (United States)

Sodium ferulate (SF) and Oxymatrine (OMT) were compounds extracted from Chinese herbs, and have been used in clinical treatment of heart and hepatic diseases, respectively, in China for many years. The objective of this study was to examine the analgesic effect and the mechanism of the combined treatment of SF and OMT. Using the animal pain models by applying Acetic Acid Writhing Test and Formalin Test, the combination of SF and OMT showed significant analgesic effect in dose-dependent manner. In vitro, the combined treatment inhibited the increase in intracellular calcium concentration evoked by capsaicin in the dorsal root ganglion neurons. Importantly, a synergistic inhibitory effect of SF and OMT on the capsaicin-induced currents was demonstrated by whole-cell patch-clamp. Our results suggest that SF and OMT cause significant analgesic effect which maybe related to the synergistic inhibition of transient receptor potential vanilloid-1. PMID:20521101

Liu, Hanqing; Sun, Yan; Gao, Yan; Chen, Fangfang; Xu, MingBo; Liu, Zhifeng

2010-06-03

78

Analgesic activity of piracetam: effect on cytokine production and oxidative stress.  

Science.gov (United States)

Piracetam is a prototype of nootropic drugs used to improve cognitive impairment. However, recent studies suggest that piracetam can have analgesic and anti-inflammatory effects. Inflammatory pain is the result of a process that depends on neutrophil migration, cytokines and prostanoids release and oxidative stress. We analyze whether piracetam has anti-nociceptive effects and its mechanisms. Per oral pretreatment with piracetam reduced in a dose-dependent manner the overt pain-like behavior induced by acetic acid, phenyl-p-benzoquinone, formalin and complete Freund's adjuvant. Piracetam also diminished carrageenin-induced mechanical and thermal hyperalgesia, myeloperoxidase activity, and TNF-?-induced mechanical hyperalgesia. Piracetam presented analgesic effects as post-treatment and local paw treatment. The analgesic mechanisms of piracetam were related to inhibition of carrageenin- and TNF-?-induced production of IL-1? as well as prevention of carrageenin-induced decrease of reduced glutathione, ferric reducing ability and free radical scavenging ability in the paw. These results demonstrate that piracetam presents analgesic activity upon a variety of inflammatory stimuli by a mechanism dependent on inhibition of cytokine production and oxidative stress. Considering its safety and clinical use for cognitive function, it is possible that piracetam represents a novel perspective of analgesic. PMID:23474372

Navarro, Suelen A; Serafim, Karla G G; Mizokami, Sandra S; Hohmann, Miriam S N; Casagrande, Rubia; Verri, Waldiceu A

2013-03-06

79

Analgesic activity of piracetam: effect on cytokine production and oxidative stress.  

UK PubMed Central (United Kingdom)

Piracetam is a prototype of nootropic drugs used to improve cognitive impairment. However, recent studies suggest that piracetam can have analgesic and anti-inflammatory effects. Inflammatory pain is the result of a process that depends on neutrophil migration, cytokines and prostanoids release and oxidative stress. We analyze whether piracetam has anti-nociceptive effects and its mechanisms. Per oral pretreatment with piracetam reduced in a dose-dependent manner the overt pain-like behavior induced by acetic acid, phenyl-p-benzoquinone, formalin and complete Freund's adjuvant. Piracetam also diminished carrageenin-induced mechanical and thermal hyperalgesia, myeloperoxidase activity, and TNF-?-induced mechanical hyperalgesia. Piracetam presented analgesic effects as post-treatment and local paw treatment. The analgesic mechanisms of piracetam were related to inhibition of carrageenin- and TNF-?-induced production of IL-1? as well as prevention of carrageenin-induced decrease of reduced glutathione, ferric reducing ability and free radical scavenging ability in the paw. These results demonstrate that piracetam presents analgesic activity upon a variety of inflammatory stimuli by a mechanism dependent on inhibition of cytokine production and oxidative stress. Considering its safety and clinical use for cognitive function, it is possible that piracetam represents a novel perspective of analgesic.

Navarro SA; Serafim KG; Mizokami SS; Hohmann MS; Casagrande R; Verri WA Jr

2013-04-01

80

Immunomodulatory, analgesic and antipyretic effects of violacein isolated from Chromobacterium violaceum.  

Science.gov (United States)

Violacein was isolated from Chromobacterium violaceum, a soil Gram negative bacterium collected from the forest water body soil sample of Kolli Hills; Tamil Nadu, India. In the present study the immunomodulatory, analgesic and antipyretic activities of violacein were investigated in wistar rats and mice. Analgesic effect was evaluated by acetic acid- induced writhing, formalin induced paw licking and hotplate tests. Immunomodulatory effect was investigated by using ovalbumin- induced active paw anaphylaxis and sheep red blood cells (SRBC)-induced DTH tests. Antipyretic activity was evaluated by yeast- induced hyperpyrexia in rats. The anti- oedema effect was compared with indomethacin. Violacein inhibited 42.9% of ovalbumin- induced edema. Further we found that violacein (40mg/kg b.w.) reduced the edema induced by sheep red blood cells. Violacein also produced significant (pviolacein showed a significant (pviolacein possesses potent immunomodulatory, analgesic and antipyretic activities. PMID:19576742

Antonisamy, P; Ignacimuthu, S

2009-07-02

 
 
 
 
81

[Does iv paracetamol have preemptive analgesic effect on lumber disc surgeries?].  

UK PubMed Central (United Kingdom)

In this study, postoperative analgesic effects of intravenous paracetamol administration in lumbar discectomy patients were evaluated. After the approval of ethic committee, 90 patients undergoing lumbar disc hernia operation randomly divided into 3 groups. After standart general anesthesia, patients in group I received 1 gr i.v. paracetamol infusion 15 minutes before the induction, patients in group II received i.v. Paracetamol infusion started 15 minutes before the end of surgery. i.v morphine via PCA is used for postoperative analgesia maintenance and patients pain scores were assessed with VAS at 0., 1., 2., 3., 6., 12. and 24. hours. First analgesic requirement time, total morphine consumption and side effects were recorded. In group I and II, VAS scores, 24 h morphine consumption and first morphine requirement times were significantly different comparing to group III. As a result, we think that in lumbar discectomy cases preoperative administration of 1 gr paracetamol has no preemptive analgesic effect.

Toygar P; Akkaya T; Ozkan D; Ozel O; Uslu E; Gümü? H

2008-04-01

82

[Does iv paracetamol have preemptive analgesic effect on lumber disc surgeries?].  

Science.gov (United States)

In this study, postoperative analgesic effects of intravenous paracetamol administration in lumbar discectomy patients were evaluated. After the approval of ethic committee, 90 patients undergoing lumbar disc hernia operation randomly divided into 3 groups. After standart general anesthesia, patients in group I received 1 gr i.v. paracetamol infusion 15 minutes before the induction, patients in group II received i.v. Paracetamol infusion started 15 minutes before the end of surgery. i.v morphine via PCA is used for postoperative analgesia maintenance and patients pain scores were assessed with VAS at 0., 1., 2., 3., 6., 12. and 24. hours. First analgesic requirement time, total morphine consumption and side effects were recorded. In group I and II, VAS scores, 24 h morphine consumption and first morphine requirement times were significantly different comparing to group III. As a result, we think that in lumbar discectomy cases preoperative administration of 1 gr paracetamol has no preemptive analgesic effect. PMID:19021006

Toygar, Pinar; Akkaya, Taylan; Ozkan, Derya; Ozel, Ozgür; Uslu, Ebru; Gümü?, Haluk

2008-04-01

83

Perspective of nurses on effective factors on their decisions to administer PRN analgesics to children after surgery  

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Full Text Available Post-surgery pain is usually controlled by PRN drugs administered by nurses. According to the decision-making theories, this clinical decision-making depends on three factors: nurse-related factors; child-related factors; and hospital-related factors. This study deals with the first and second factors mentioned. This descriptive-analytic study aims at determining the perspective of nurses on factors which affect their decisions to administer the analgesic PRN to children after surgery in several chosen hospitals of Tehran. The study used a standardized questionnaire to collect data from 57 nurses in pediatric surgery wards. The questionnaire consisted of three parts: 1) nurses demographic data 2) 20 clinical scenario for nurses to make a decision for prescribing either analgesic medication, non-analgesic medication or no medication where necessary and 3) 12 factors which affect clinical decision-making in using analgesics.(in prioritizing among the above mentioned). The results show that factors such as age, nursing experience, pediatric nursing experience and motherhood were significantly related to choosing to use analgesics. Education and personal experience of extreme pain was also related to the type of analgesic chosen. Concerning the specifics of the children there was a significant difference between the choice to use analgesics and the type of analgesic used according to the various ages of the children. There was also a significant relationship between the type of surgery and the time of surgery and with the choice to use analgesics and the type of analgesics used, such that medication and analgesics were administered more frequently for complicated surgeries and in first 24 hours after surgery. Type of surgery, severity of pain, time of surgery and uneasy behaviors were selected respectively as the most effective in the administration of PRN analgesic drugs. Nurse and child related factors strongly influence nurses in making decisions to administer PRN analgesics postoperatively.

Karimi; R. Parsa-Yekta; Z. Mehran; A. Nik-Farid; L.

2002-01-01

84

Translational pain research: Evaluating analgesic effect in experimental visceral pain models  

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Full Text Available Deep visceral pain is frequent and presents major challenges in pain management, since its pathophysiology is still poorly understood. One way to optimize treatment of visceral pain is to improve knowledge of the mechanisms behind the pain and the mode of action of analgesic substances. This can be achieved through standardized experimental human pain models. Experimental pain models in healthy volunteers are advantageous for evaluation of analgesic action, as this is often difficult to assess in the clinic because of confounding factors such as sedation, nausea and general malaise. These pain models facilitate minimizing the gap between knowledge gained in animal and human clinical studies. Combining experimental pain studies and pharmacokinetic studies can improve understanding of the pharmacokinetic-pharmacodynamic relationship of analgesics and, thus, provide valuable insight into optimal clinical treatment of visceral pain. To improve treatment of visceral pain, it is important to study the underlying mechanisms of pain and the action of analgesics used for its treatment. An experimental pain model activates different modalities and can be used to investigate the mechanism of action of different analgesics in detail. In combination with pharmacokinetic studies and objective assessment such as electroencephalography, new information regarding a given drug substance and its effects can be obtained. Results from experimental human visceral pain research can bridge the gap in knowledge between animal studies and clinical condition in patients suffering from visceral pain, and thus constitute the missing link in translational pain research.

Anne Estrup Olesen, Trine Andresen, Lona Louring Christrup, Richard N Upton

2009-01-01

85

Analgesic Effect of the Methanol Extract of Erica Arborea (L.) in Mice Using Formalin Test  

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Background and the purpose of the study: Erica arborea L. (Ericaceae) has been used in Turkey folk medicine as a diuretic, urinary antiseptic and laxative. However, its other pharmacological effects have not been yet elucidated clearly. The aim of this study was to investigate analgesic effects of i...

A Mohajjel Nayebi; H Nazemiyeh; R Omidbakhsh; S Çobanoglu

86

Influence of serotonin on the analgesic effect of granisetron on temporomandibular joint arthritis  

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Full Text Available THE influence of circulating serotonin (5-HT) on the effects of intra-articular administration of granisetron on temporomandibular joint (TMJ) pain was investigated in 11 patients with chronic polyarthritides. An analgesic effect superior to placebo has been shown previously.

Ülle Voog; Per Alstergren; Edvitar Leibur; Riina Kallikorm; Sigvard Kopp

1992-01-01

87

Tramadol Safer and Effective Analgesic to Treat Chronic Pain: A Review  

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Full Text Available pain is defined by the International Association for the Study of Pain (IASP) as "an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage".Pain has now been equated to a “fifth vital sign” highlighting the significance of pain management in patient care. Tramadol is a centrally acting analgesic, structurally related to codeine and morphine .It is effectively used to treat moderate-to-severe acute and chronic pain in diverse conditions. Tramadol is placed on the second step of WHO analgesic ladder and in contrast to traditional opioids, exerts its analgesic activity, a dual mechanism of action inhibiting transmission as well as perception of pain. Tramadol is more suitable than NSAIDs and coxibs for patient with GI, renal and cardiovascular problems. Combined with low dependence/abuse potential, it has proven to be of significant advantage over other agents, especially in the elderly.

Gulshan Pandey

2012-01-01

88

The effect of topical analgesics on ex vivo skin growth and human keratinocyte and fibroblast behavior.  

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The application of topical analgesics to the donor site of split thickness skin grafts has been proven to be an effective method of pain management but little is known about their effects on wound reepithelialization. This study compares the effect of four analgesics on human keratinocytes and fibroblasts and whole skin explants in vitro to determine whether epithelial cell behavior is affected by topical analgesics. The effect of diclofenac, bupivacaine, lidocaine, and ketorolac was studied at concentrations between 10 mM and 1 nM. The effect on epithelial growth was measured using an ex vivo skin explant model. In addition, cell proliferation, and cytotoxicity were measured in cultured primary human keratinocytes and fibroblasts. Epithelial growth from the explant model was most inhibited by diclofenac with a significant reduction at 100 microM (p=>0.001). Diclofenac also exhibited the strongest inhibitory effect on cell proliferation especially in keratinocytes. Ketorolac was the most cytotoxic. Bupivacaine showed cytotoxicity in a dose-dependent manner with only the very highest concentrations having a significant inhibitory effect. Lidocaine showed no evidence of cytotoxicity at the concentrations tested in either the in vitro cell studies or the ex vivo explant model. Topical analgesics alter keratinocyte and fibroblast behavior and such inhibition may affect wound healing. PMID:19660041

Harris, Kathryn L; Bainbridge, Natalie J; Jordan, Nigel R; Sharpe, Justin R

89

The effect of topical analgesics on ex vivo skin growth and human keratinocyte and fibroblast behavior.  

UK PubMed Central (United Kingdom)

The application of topical analgesics to the donor site of split thickness skin grafts has been proven to be an effective method of pain management but little is known about their effects on wound reepithelialization. This study compares the effect of four analgesics on human keratinocytes and fibroblasts and whole skin explants in vitro to determine whether epithelial cell behavior is affected by topical analgesics. The effect of diclofenac, bupivacaine, lidocaine, and ketorolac was studied at concentrations between 10 mM and 1 nM. The effect on epithelial growth was measured using an ex vivo skin explant model. In addition, cell proliferation, and cytotoxicity were measured in cultured primary human keratinocytes and fibroblasts. Epithelial growth from the explant model was most inhibited by diclofenac with a significant reduction at 100 microM (p=>0.001). Diclofenac also exhibited the strongest inhibitory effect on cell proliferation especially in keratinocytes. Ketorolac was the most cytotoxic. Bupivacaine showed cytotoxicity in a dose-dependent manner with only the very highest concentrations having a significant inhibitory effect. Lidocaine showed no evidence of cytotoxicity at the concentrations tested in either the in vitro cell studies or the ex vivo explant model. Topical analgesics alter keratinocyte and fibroblast behavior and such inhibition may affect wound healing.

Harris KL; Bainbridge NJ; Jordan NR; Sharpe JR

2009-05-01

90

Analgesic and anti-inflammatory effects of ethyl acetate fraction of Polygonum cuspidatum in experimental animals.  

UK PubMed Central (United Kingdom)

Polygonum cuspidatum (PC) has been used for the treatment of arthritis and urinary diseases in traditional medicine. Despite recent evidence that PC has anti-oxidant, anti-tumoral, and anti-inflammatory effects, analgesic and anti-inflammatory effects of PC have not been elucidated yet in vivo. Thus, in the present study, analgesic and anti-inflammatory effects of ethyl acetate extract of PC (EAPC) were investigated in vivo for the first time. Hot plate test and tail-flick test revealed that EAPC at 200?mg/kg exerts analgesic effect (p?analgesic effect in acetic acid-induced writhing test. Serotonin-induced paw edema model and Freund's complete adjuvant (FCA)-induced adjuvant arthritis model were used to examine anti-inflammatory effect of EAPC in vivo. In serotonin-induced paw edema model, EAPC suppressed swelling inflammatory response within 12?min after serotonin injection, at both 100- and 200-mg/kg dose (p?effectively inhibited positive responses of c-reactive protein and rheumatoid factor compared to untreated control. Taken together, our findings suggest that EAPC can be a potent candidate for rheumatoid arthritis treatment.

Han JH; Koh W; Lee HJ; Lee HJ; Lee EO; Lee SJ; Khil JH; Kim JT; Jeong SJ; Kim SH

2012-04-01

91

[Study on analgesic and accompanying toxic and side effects of euodiae fructus based on clinical efficacy dose].  

UK PubMed Central (United Kingdom)

CONCLUSION: Continuous oral administration of certain dose of water extracts from Euodiae Fructus to mice can generate the toxic and side effects in liver accompanying with the analgesic effect, and show dose-dependence relationship to some extent. Its analgesic mechanism is related to the reduction of PGE, content in blood, while its toxic mechanism is related to oxidative injury to some extent.

Huang W; Sun R

2013-07-01

92

Analgesic and anti-inflammatory effects of ethanol extracted leaves of selected medicinal plants in animal model  

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Aim: The research was carried out to investigate the analgesic and anti-inflammatory effects of ethanol extract of Desmodium pauciflorum, Mangifera indica and Andrographis paniculata leaves. Materials and Methods: In order to assess the analgesic and anti-inflammatory effects acetic acid induced wri...

Mohammad M. Hassan; Shahneaz A. Khan; Amir H. Shaikat; Md. Emran Hossain; Md. Ahasanul Hoque; Md Hasmat Ullah; Saiful Islam

93

Analgesic Effect of Aqueous and Hydroalcoholic Extracts of Three Congolese Medicinal Plants: Hyptis suavolens, Nauclea latifolia and Ocimum gratissimum  

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Analgesic effect of aqueous and hydroalcoholic extracts of aeral parts of Hyptis suavolens, Nauclea latifolia and Ocimum gratissimum, three plants used in congolese folk medicine in pain, were tested on acetic acid and hot plate tests. All extracts manifest analgesic effect on ...

N. Okiemy-Andissa; M.L. Miguel; A.W. Etou; J.M.Ouamba; M. Gbeassor; A.A. Abena

94

Role of matrix metalloproteinase II on analgesic effect of nitric oxide inhibition in rat  

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Full Text Available Abstract Introduction: Matrix metalloproteinase 2 is one of the inflammatory mediators that is involved in nociceptive processing and its production is regulated by many inflammatory factors such as nitric oxide. We studied the role of MMP-2 on the analgesic effects of nNOS inhibitor. Methods: Considering that nitric oxide has many roles in pain processing, we studied the CSF levels of MMP-2 after hind paw formalin injection (50µl, 2.5%) and neuronal nitric oxide synthase inhibition intrathecally. We also studied the effect of MMP-2 inhibitor on pain behavior and its role on analgesic effect of neuronal nitric oxide synthase (nNOS) inhibitor. Results: Rats that received MMP-2 inhibitor (30mM) showed severe responses to the formalin injection. Pain was reduced after nNOS inhibition. Prior to nNOS inhibitor injection, MMP-2 inhibition reduced the analgesic effects of nNOS inhibitor. Immunological study showed that MMP-2 increased in rats that received nNOS inhibitor. Conclusion: These data suggest the possible roles for MMP-2 in analgesic effect of nNOS inhibitor.

Fatemeh Khojasteh; Majid Hasanpour-Ezati; Seyed Javad Mirnajafi-Zadeh; Saeed Semnanian

2009-01-01

95

Analgesic effects of minodronate on formalin-induced acute inflammatory pain in rats.  

Science.gov (United States)

Minodronate is expected to produce greater analgesic effects than other bisphosphonates. However, there are no studies comparing bisphosphonate analgesic effects on formalin-induced acute inflammatory pain in rats. The purpose of the present study was to evaluate the analgesic effects of minodronate, morphine, and placebo. Four-month-old female Wistar rats were administered minodronate (50 mg/kg), morphine (10 mg/kg), or vehicle (n = 10 each) injections. Thirty minutes later, all rats were injected with formalin (right hind paw) to induce acute inflammatory pain. Paw licking and lifting as indicators of nociceptive pain responses were monitored from 0 to 5 min (phase 1; chemical-stimulation state) and then from 10 to 30 min (phase 2; spinal-sensitized state) after injection. The percentage of limb usage of the formalin-injected and the non-injected sides were measured in phases 1 and 2 by counting foot stamps. Minodronate significantly decreased nociceptive responses and increased limb usage compared with vehicle in phase 2 only (P < 0.05). Morphine significantly decreased nociceptive responses and increased limb usage compared with minodronate and vehicle in both phase 1 and 2 (P < 0.05). In conclusion, minodronate showed significant analgesic effects for formalin-induced acute pain in the spinal-sensitized state. PMID:23782747

Segawa, Toyohito; Miyakoshi, Naohisa; Kasukawa, Yuji; Aonuma, Hiroshi; Tsuchie, Hiroyuki; Shimada, Yoichi

2013-06-01

96

Pharmacokinetic-Pharmacodynamic modeling of the analgesic effect of bupredermTM, in mice  

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Purpose: BupredermTM?Buprenorphine transdermal delivery system (BTDS) was developed for the treatment of post-operative and chronic pains. This study examined the relationship between the plasma concentration of buprenorphine and its analgesic effect (tail flick test) in order to assess the usefulne...

Min-Hyuk Yun; Seung-Wei Jeong; Chaul-Min Pai; Sun-Ok Kim

97

Evaluation of Analgesic Effects of Hydroalcoholic Extract of Marrubium parviflorum by Formalin Test in Mice  

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In this research, hydroalcoholic extract obtained from the aerial parts of Marrubium parviflorum (Lamiaceae) was subjected to evaluation of analgesic effects using formalin test at the doses of 50, 100 and 200 mg kg-1 in mice. Duration of licking and biting time (min) of the inject...

Mahnaz Khanavi; Mohammad-reza Delnavazi; Vahid Nikoui; Sattar Ostadhadi; Azam Bakhtiarian

98

Immunomodulatory, analgesic and antipyretic effects of violacein isolated from Chromobacterium violaceum.  

UK PubMed Central (United Kingdom)

Violacein was isolated from Chromobacterium violaceum, a soil Gram negative bacterium collected from the forest water body soil sample of Kolli Hills; Tamil Nadu, India. In the present study the immunomodulatory, analgesic and antipyretic activities of violacein were investigated in wistar rats and mice. Analgesic effect was evaluated by acetic acid- induced writhing, formalin induced paw licking and hotplate tests. Immunomodulatory effect was investigated by using ovalbumin- induced active paw anaphylaxis and sheep red blood cells (SRBC)-induced DTH tests. Antipyretic activity was evaluated by yeast- induced hyperpyrexia in rats. The anti- oedema effect was compared with indomethacin. Violacein inhibited 42.9% of ovalbumin- induced edema. Further we found that violacein (40mg/kg b.w.) reduced the edema induced by sheep red blood cells. Violacein also produced significant (p<0.05) analgesic activity in acetic acid induced writhing response, formalin induced paw licking response and hot plate analysis. Treatment with violacein showed a significant (p<0.05) dose-dependent reduction in pyrexia in rats. The results suggest that violacein possesses potent immunomodulatory, analgesic and antipyretic activities.

Antonisamy P; Ignacimuthu S

2010-03-01

99

Preemptive Analgesic Effect of Ketamine in Children with Lower Abdominal Surgery  

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Full Text Available Objective: Preemptive analgesic effect of low dose ketamine has been supported by clinical studies in adults. The aim of this study was to evaluate the analgesic effect of ketamine applied at different times in children who underwent lower abdominal surgery.Material and Methods: A total of 90 children having ASAI-II physical status between 3 and 12 was randomly divided into three groups as pre, int and post groups. Ketamine were given to these groups in the following manner respectively; 1mg/kg intravenous ketamine before incision (pre-incisional); the same dose ketamine 10 minutes following the first incision (intraoperative); and ketamine at the end of the surgical operation (postoperative). The pain of patients was assessed by postoperative pain scale (CHIPPS) in children and infants; the sedation status of children was assessed by Ramsey’s sedation scale. The first analgesic requirement time was recorded.Results: No significant difference was found in demographic characteristics of the three groups (p>0.05). Lower CHIPPS scores were found in Group Post throughout all measurement periods (p<0.05). Group Post was found to have significantly higher sedation levels compared with the other two groups (p=0.003). Conclusion: No analgesic effect was obtained using by pre-incisional and intraoperative i.v.1mg/kg ketamine, during lower abdominal surgery in children. Further studies with different drugs are needed to clarify this topic.

Serbülent Gökhan Beyaz

2011-01-01

100

Obestatin prevents analgesic tolerance to morphine and reverses the effects of mild morphine withdrawal in mice.  

UK PubMed Central (United Kingdom)

Obestatin is a 23-amino acid gut-derived neuropeptide, encoded by the same gene with ghrelin. The goal of this study was to examine the effects of obestatin on the acute and chronic analgesic actions of morphine and on mild morphine withdrawal. Open-field (OF) and elevated plus maze (EPM) tests were used to assess mild morphine withdrawal-induced behavior changes and the heat-radiant tail-flick assay was used to investigate analgesic actions of morphine. CFLP male mice were treated twice a day with graded doses of morphine in EPM and OF experiments and once a day in tail-flick studies. Obestatin (1.5?g/2?l) was administrated once a day in all experiments. Furthermore, 0.2mg/kg naloxone or saline was administered after the final injection of morphine at a dose of 20mg/kg in EPM and OF. These behavioral parameters were monitored in the OF: the percentage of center ambulation time and distance; whereas in the EPM: the time spent in open arms and the entries into open arms compared to the total time (%OAT) and entries (%OAE). In the OF, obestatin significantly decreased the percentage of time spent in the center in mice undergoing naloxone-precipitated mild morphine withdrawal. EPM results were similar to open field, but obestatin had no significant effect on parameters mentioned above. Besides, obestatin maintained the analgesic effect of morphine 90 and 120min after morphine injection in mice treated with morphine receiving obestatin compared to mice treated with morphine. In tolerance studies, obestatin diminished the analgesic tolerance to morphine on the 5th day. In this study we confirmed that obestatin reversed the effect of mild morphine withdrawal and enhances the analgesic effect of morphine. These data suggest that obestatin may have a role in opioid-induced analgesia and in behavioral responses induced by opioid withdrawal.

Lipták N; Dochnal R; Csabafi K; Szakács J; Szabó G

2013-07-01

 
 
 
 
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Persistent peripheral inflammation attenuates morphine-induced periaqueductal gray glial cell activation and analgesic tolerance in the male rat.  

UK PubMed Central (United Kingdom)

UNLABELLED: Morphine is among the most prevalent analgesics prescribed for chronic pain. However, prolonged morphine treatment results in the development of analgesic tolerance. An abundance of evidence has accumulated indicating that central nervous system glial cell activity facilitates pain transmission and opposes morphine analgesia. While the midbrain ventrolateral periaqueductal gray (vlPAG) is an important neural substrate mediating pain modulation and the development of morphine tolerance, no studies have directly assessed the role of PAG glia. Here we test the hypothesis that morphine-induced increases in vlPAG glial cell activity contribute to the development of morphine tolerance. As morphine is primarily consumed for the alleviation of severe pain, the influence of persistent inflammatory pain was also assessed. Administration of morphine, in the absence of persistent inflammatory pain, resulted in the rapid development of morphine tolerance and was accompanied by a significant increase in vlPAG glial activation. In contrast, persistent inflammatory hyperalgesia, induced by intraplantar administration of complete Freund's adjuvant (CFA), significantly attenuated the development of morphine tolerance. No significant differences were noted in vlPAG glial cell activation for CFA-treated animals versus controls. These results indicate that vlPAG glia are modulated by a persistent pain state, and implicate vlPAG glial cells as possible regulators of morphine tolerance. PERSPECTIVE: The development of morphine tolerance represents a significant impediment to its use in the management of chronic pain. We report that morphine tolerance is accompanied by increased glial cell activation within the vlPAG, and that the presence of a persistent pain state prevented vlPAG glial activation and attenuated morphine tolerance.

Eidson LN; Murphy AZ

2013-04-01

102

Effect of Celecoxib on the Peripheral NO Production  

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Full Text Available Objective(s)Celecoxib acts through both COX-2-dependent and -independent pathways. According to the paradoxical effect of NO on the inflammatory and nociceptive signal processing, the present study designed to evaluate the probable contribution of NO in the analgesic and anti-inflammatory properties of celecoxib. Materials and MethodsDifferent intensities of inflammatory pain were induced by acute and chronic sc administration of 1%, 2.5%, or 5% formalin and spectrophotometrical analysis of the serum nitrite was performed. Then, in the pretreatment process, the effect of celecoxib (10, 20, or 40 mg/kg/ip) was evaluated on the inflammatory pain induced-nitrite. Also, the effect of celecoxib alone (under non-inflammatory condition) was evaluated on the peripheral NO production and the results compared with that of the vehicle. ResultsFormalin-induced inflammatory pain led to an enhancement of the serum nitrite in intensity- and time-dependent manners. Celecoxib (40 mg/kg/ip), except its ineffectiveness on the nitrite level, induced 1.5 hr after 5% formalin, reduced production of formalin-induced nitrite in other cases. Meanwhile, under non-inflammatory condition, 1.5 hr after the administration of celecoxib (40 mg/kg/ip), a considerable elevation of nitrite was observed. Celecoxib 10 or 20 mg/kg/ip did not show a significant effect on either inhibition or stimulation of the peripheral NO.ConclusionNO is involved both in the inflammatory and non-inflammatory conditions. It seems that celecoxib exerts a dual effect on the peripheral NO production; it prevents overproduction of NO due to the induction of inflammatory pain, while, it stimulates NO synthesis at the early stage of its action.

Parichehr Hassanzadeh

2009-01-01

103

Pharmacodynamic analysis of analgesic clinical trials: nonlinear mixed-effects logistic models.  

UK PubMed Central (United Kingdom)

In the development of an analgesic product, placebo-controlled clinical trials in patients with defined pain are used to study the dose-time-response relationship of the drug. In such trials, the response is usually an ordered categorical variable with longitudinal and subject-specific repeated measurements. The primary causal variables are time and analgesic concentration. The response may be informative right-hand censored because remedication with a known analgesic may be given if a patient has inadequate pain relief. Mixed-effects logistic models are used to estimate the probabilities of having certain pain relief or pain severity scores. A jackknife method is proposed to estimate the standard errors of parameter estimates. Posterior estimates of these probabilities, or of the scores themselves, allow the evaluation of efficacy for an analgesic. In this evaluation, therapeutic as well as statistical significance is assessed. Two case studies, one focusing on pain relief and the other on pain severity, are used to demonstrate the approach. The level of baseline pain appears to be a determinant of the pattern of response.

Liu CY; Sambol NC

1999-05-01

104

Effect of the peripherally selective ?-opioid agonist, asimadoline, on adjuvant arthritis  

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Opioids, though widely used as analgesics, have not been seriously considered as therapy for rheumatoid arthritis. The present study evaluated the dose-effect and time-dependence relationships of a new peripherally selective ? agonist, asimadoline, in rats with adjuvant arthritis.The arthritis was assessed by a pooled severity index combining the comprehensive criteria of oedema, radiography and histological changes, in the hind limbs. Asimadoline was extremely effective in attenuating joint damage (by up to 80%) when administered parenterally (0.5 to 10?mg?kg?1?day?1, i.p.) throughout the disease or during its early phase; treatment was less successful if confined to the latter stages. Ten fold higher doses were effective orally.Equimolar doses of a peripherally-selective antagonist, naloxone methiodide, and the ?-selective antagonist, MR2266, fully reversed the peripheral anti-arthritic effects of asimadoline (5?mg?kg?1?day?1), indicating that asimadoline acts through peripheral ?-opioid receptors. However, an equivalent dose of MR2266 did not fully reverse the anti-arthritic effects of the highest dose of asimadoline (40?mg?kg?1?day?1), suggesting a loss of ?-selectivity at this dose.Asimadoline also exhibited analgesic effects (mechanical nociceptive thresholds) in arthritic but not non-arthritic rats, indicating that inflammation is necessary for asimadoline-induced analgesia.These data confirm our previous findings that ?-opioids possess anti-arthritic properties and that these effects are mediated via peripheral ?-receptors. The present results are new in showing that the peripherally acting ?-opioid agonist, asimadoline, is a potent anti-arthritic agent. Such novel drugs, essentially lacking central side effects, herald new treatments for rheumatoid arthritis.

Binder, Waltraud; Walker, Judith S

1998-01-01

105

Analgesic effects of the non-nitrogen-containing bisphosphonates etidronate and clodronate, independent of anti-resorptive effects on bone.  

UK PubMed Central (United Kingdom)

Nitrogen-containing bisphosphonates (NBPs) have greater anti-bone-resorptive effects than non-nitrogen-containing bisphosphonates (non-NBPs). Hence, NBPs are the current first-choice drug for osteoporosis. However, NBPs carry a risk of osteonecrosis of jaws. Some animal and human studies suggest that non-NBPs may have anti-bone-resorptive effect-independent analgesic effects, but there has been no detailed comparison between NBPs and non-NBPs. Here, we compared the analgesic effects of several non-NBPs and NBPs, using (a) writhing responses induced in mice by intraperitoneal injection of 1% acetic acid, (b) acetic acid-induced neuronal expression of c-Fos, (c) acetic acid-induced elevation of blood corticosterone, and (d) hindpaw-licking/biting responses induced by intraplantar injection of capsaicin. Among the NBPs and non-NBPs tested, only etidronate and clodronate displayed clear analgesic effects, with various routes of administration (including the oral one) being effective. However, they were ineffective when intraperitoneally injected simultaneously with acetic acid. Intracerebroventricular administration of etidronate or clodronate, but not of minodronate (an NBP), was also effective. The effective doses of etidronate and clodronate were much lower in writhing-high-responder strains of mice. Etidronate and clodronate reduced acetic acid-induced c-Fos expression in the brain and spinal cord, and also the acetic acid-induced corticosterone increase in the blood. Etidronate and clodronate each displayed an analgesic effect in the capsaicin test. Etidronate and clodronate displayed their analgesic effects at doses lower than those inducing anti-bone-resorptive effects. These results suggest that etidronate and clodronate exert potent, anti-bone-resorptive effect-independent analgesic effects, possibly via an interaction with neurons, and that they warrant reappraisal as safe drugs for osteoporosis.

Kim S; Seiryu M; Okada S; Kuroishi T; Takano-Yamamoto T; Sugawara S; Endo Y

2013-01-01

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Evaluation of analgesic effect of local administration of morphine after iliac crest bone graft harvesting: A double blind study.  

UK PubMed Central (United Kingdom)

BACKGROUND AND OBJECTIVE: Pain is a complex process influenced by both physiological and psychological factors. In spite of an armamentarium of analgesic drugs and techniques available to combat post-operative pain, appropriate selection, and effective management for relief of post-operative pain still poses unique challenges. The discovery of peripheral opioid receptors has led to growing interest in the use of locally applied opioids (intra-articular, intra-pleural, intra-peritoneal, and perineural) for managing acute pain. As bone graft harvesting is associated with significant post-operative pain and there is a paucity of literature on the use of peripheral opioids at the iliac crest bone harvesting site, the present study was planned to evaluate the analgesic efficacy of local administration of morphine after iliac crest bone graft harvesting. MATERIALS AND METHODS: A total of 60 patients, 20-50 years of age scheduled to undergo elective surgery for delayed and non-union fracture both bone leg with bone grafting under general anaesthesia (GA) were randomly assigned to one of the four groups of 15 patients each: group 1: 2.5 ml normal saline (NS) +2.5 ml NS infiltrated into the harvest site at 2 sites + 1 ml NS intramuscularly (i/m); Group 2: 2.5 ml NS + 2.5 ml NS infiltrated into the harvest site at 2 sites + 5 mg morphine in 1 ml i/m.; Group 3: 2.5 mg (2.5 ml) morphine + 2.5 mg (2.5 ml) morphine infiltrated into the harvest site at 2 sites + 1 ml NS i/m; Group 4: 0.5 mg naloxone (2.5 ml) +5 mg (2.5 ml) morphine infiltrated into the harvest site at 2 sites + 1 ml NS i/m. Pain from the bone graft site and operative site was assessed for 24 h post-operatively. RESULTS: The patients who had received morphine infiltration (Group 3) had significantly less pain scores at the graft site at 4, 6, and 10 post-operative hours. They also had significantly less morphine consumption and overall better pain relief as compared to the other groups. CONCLUSIONS: Morphine administered peripherally provided better analgesia as compared to that given systemically and this effect was noticeable after 4 h post-operatively.

Singh D; Gombar KK; Bhatia N; Gombar S; Garg S

2013-07-01

107

Analgesic Effect of the Methanol Extract of Erica Arborea (L.) in Mice Using Formalin Test  

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Full Text Available Background and the purpose of the study: Erica arborea L. (Ericaceae) has been used in Turkey folk medicine as a diuretic, urinary antiseptic and laxative. However, its other pharmacological effects have not been yet elucidated clearly. The aim of this study was to investigate analgesic effects of its methanolic (MeOH) extract in mice using formalin test, as a model of tonic inflammatory pain. Methods: The MeOH extract of aerial parts and its fractions (20, 40, 60, 80 and 100% MeOH in water) were prepared by maceration and solid phase extraction method respectively. Effects of the MeOH extract (10, 20 and 30 mg/kg, i.p.) and different fractions (5 mg/kg, i.p.) were compared with analgesic effects of the morphine (10 mg/kg, i.p.) and indomethacine (5 mg/kg, i.p.) as standard analgesic drugs. Results and major conclusion: Results showed that the MeOH extract of E. arborea (10 mg/kg, i.p.) similar to the morphine (10 mg/kg, i.p.) and indomethacen (5 mg/kg, i.p.) decreased formalin-induced paw licking time,. Among the prepared-fractions of the MeOH extract, only fraction of 20% (5 mg/kg, i.p.) caused significant decrease in paw licking behavior. Moreover, the MeOH extract (10 mg/kg, i.p.) did not produce any motor deficit effects in rotarod test. From the results it may be concluded that the MeOH extract and faction of 20% of E. arborea have a good analgesic effects in formalin test.

A Mohajjel Nayebi; H Nazemiyeh; R Omidbakhsh; S Çobanoglu

2008-01-01

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5. Anti inflammatory and analgesic effect of methanolic extract of Anogeissus acuminata leaf  

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Full Text Available In the present study, the anti-inflammatory and analgesic effect of the methanol extract of Anogeissus acuminata leaf was investigated. The methanolic extracts of Anogeissus acuminata leaf were ingested orally (p.o.) in the form of suspension in 0.5% Tween 80 in two different doses, 200 and 400 mg/kg body weight). The anti-inflammatory effect of Anogeissus acuminata was tested in: carrageenin-induced paw oedema in wistar albino rats and formalin-induced paw oedema in Swiss albino mice and compared with the standard, indomethacin (5 mg/kg body weight). The analgesic effect was evaluated in Swiss albino mice by Eddy’s hot plate method and compared with the standard, aspirin (25 mg/kg body weight). The results showed that Anogeissus acuminata has significant reduction (p?0.01) in inflammation i.e. 66.67 % (200 mg/kg body weight) and 77.78% (400 mg/kg body weight) as compared to the standard drug, indomethacin, which was 88.89%. In assessing analgesic effects, there is a significant (p<0.01) reduction in the paw licking and paw jumping response for Anogeissus acuminata (400 mg/kg) and aspirin (25 mg/kg) when compared to control. These results indicate that the extracts could possess analgesic and anti-inflammatory properties. All these effects and the changes in the behavioural activities could be suggested as contributory effects to the use of Anogeissus acuminata leaf in the management of inflammation and painful conditions.

K. Hemamalini; K. Om Prasad Naik; P. Ashok

2010-01-01

109

Side-effects of analgesic kyotorphin derivatives: advantages over clinical opioid drugs.  

UK PubMed Central (United Kingdom)

The adverse side-effects associated with opioid administration restrain their use as analgesic drugs and call for new solutions to treat pain. Two kyotorphin derivatives, kyotorphin-amide (KTP-NH?) and ibuprofen-KTP-NH? (IbKTP-NH?) are promising alternatives to opioids: they trigger analgesia via an indirect opioid mechanism and are highly effective in several pain models following systemic delivery. In vivo side-effects of KTP-NH? and IbKTP-NH? are, however, unknown and were evaluated in the present study using male adult Wistar rats. For comparison purposes, morphine and tramadol, two clinically relevant opioids, were also studied. Results showed that KTP-derivatives do not cause constipation after systemic administration, in contrast to morphine. Also, no alterations were observed in blood pressure or in food and water intake, which were only affected by tramadol. A reduction in micturition was detected after KTP-NH? or tramadol administrations. A moderate locomotion decline was detected after IbKTP-NH?-treatment. The side-effect profile of KTP-NH? and IbKTP-NH? support the existence of opioid-based mechanisms in their analgesic actions. The conjugation of a strong analgesic activity with the absence of the major side-effects associated to opioids highlights the potential of both KTP-NH? and IbKTP-NH? as advantageous alternatives over current opioids.

Ribeiro MM; Santos SS; Sousa DS; Oliveira M; Santos SM; Heras M; Bardaji E; Tavares I; Castanho MA

2013-07-01

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Blockades of ATP-sensitive potassium channels and L-type calcium channels improve analgesic effect of morphine in alloxan-induced diabetic mice.  

UK PubMed Central (United Kingdom)

In the present study interactions between analgesic effect of morphine with blockade of ATP-sensitive potassium channels and L-type calcium channels were investigated in alloxan-induced diabetic mice. A hot plate test was used to assess analgesic effect of drugs in adult male NMRI mice. All drugs were injected through an intraperitoneal route. A diabetic mouse model was established by injections of alloxan for three consecutive days. Seventy-two hours after the final injection, mice with a blood glucose level higher than 11.1mmol/l were considered as diabetic. The results showed that morphine at doses of 10 and 15mg/kg induced analgesia in both non-diabetic and diabetic mice, but the analgesic effect of morphine at dose of 7.5mg/kg was decreased in diabetic mice. Injections of an ATP-sensitive potassium channel blocker, glibenclamide (4, 8, 12, 20mg/kg) had no effect in non-diabetic mice, while at doses of 12 and 20mg/kg induced analgesia in diabetic mice. Blockade of L-type calcium channels with nimodipine at different doses (2.5, 5, 10 and 20mg/kg) was ineffective in non-diabetic mice, but at dose of 20mg/kg induced analgesia in diabetic mice. Co-administrations of glibenclamide (20mg/kg) or nimodipine (20mg/kg) along with different doses of morphine (5, 7.5 and 10mg/kg) improved the analgesic effect of the later drug in diabetic mice. According to the present results, it is possible that diabetes via affecting the potassium and calcium channels in the pain pathways may alter processing of pain in the peripheral and central nervous system.

Ahmadi S; Ebrahimi SS; Oryan S; Rafieenia F

2012-06-01

111

Blockades of ATP-sensitive potassium channels and L-type calcium channels improve analgesic effect of morphine in alloxan-induced diabetic mice.  

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In the present study interactions between analgesic effect of morphine with blockade of ATP-sensitive potassium channels and L-type calcium channels were investigated in alloxan-induced diabetic mice. A hot plate test was used to assess analgesic effect of drugs in adult male NMRI mice. All drugs were injected through an intraperitoneal route. A diabetic mouse model was established by injections of alloxan for three consecutive days. Seventy-two hours after the final injection, mice with a blood glucose level higher than 11.1mmol/l were considered as diabetic. The results showed that morphine at doses of 10 and 15mg/kg induced analgesia in both non-diabetic and diabetic mice, but the analgesic effect of morphine at dose of 7.5mg/kg was decreased in diabetic mice. Injections of an ATP-sensitive potassium channel blocker, glibenclamide (4, 8, 12, 20mg/kg) had no effect in non-diabetic mice, while at doses of 12 and 20mg/kg induced analgesia in diabetic mice. Blockade of L-type calcium channels with nimodipine at different doses (2.5, 5, 10 and 20mg/kg) was ineffective in non-diabetic mice, but at dose of 20mg/kg induced analgesia in diabetic mice. Co-administrations of glibenclamide (20mg/kg) or nimodipine (20mg/kg) along with different doses of morphine (5, 7.5 and 10mg/kg) improved the analgesic effect of the later drug in diabetic mice. According to the present results, it is possible that diabetes via affecting the potassium and calcium channels in the pain pathways may alter processing of pain in the peripheral and central nervous system. PMID:22743153

Ahmadi, Shamseddin; Ebrahimi, Sayede Shohre; Oryan, Shahrbanoo; Rafieenia, Fatemeh

2012-06-27

112

Curative effect of Dingqi analgesic patch on cancer pain: a single-blind randomized controlled trail.  

UK PubMed Central (United Kingdom)

OBJECTIVE: To observe the curative effect of an acupoint application with a Dingqi analgesic patch on moderate to severe pain caused by liver cancer. METHODS: Forty patients with moderate to severe pain caused by liver cancer were randomly divided into a treatment group (TG) and a control group (CG). Patients with moderate pain were given 100 mg qd of a sustainably released tablet of tramadol hydrochloride; patients with severe pain were given 4.2 mg q3d of the fentanyl transdermal system. The ashi points Ganshu (BL 18), Danshu (BL 19) and Qimen (LR 14) were chosen for the acupoint application intervention. CG patients were given a sham patch and TG patients were given a Dingqi analgesic patch. A visual analogue scale (VAS) was used before treatment and after 1, 3, 6, 9 and 12 days of treatment. The Karnofsky score was measured before treatment and after 12 days of treatment. Any main adverse reactions (e.g. nausea, constipation, dizziness and headache) were recorded after 6 and 12 days of treatment. Any skin side effects (i.e. skin irritation and allergic reactions) were recorded. RESULTS: The VAS in TG was significantly lower than that in CG after 3, 6, 9 and 12 days of treatment (P < 0.05). There was no significant difference in the Karnofsky score before treatment and after 12 days of treatment between CG and TG. There were also no significant differences in the main adverse reactions or skin side effects after 6 and 12 days of treatment between CG and TG (P > 0.05). CONCLUSION: The Dingqi analgesic patch can enhance the analgesic effect of tramadol and fentanyl.

Wang C; Tan W; Huang X; Fu T; Lin J; Bu J; Wei G; Du Y

2013-04-01

113

Analgesic effect of fendosal, ibuprofen and aspirin in postoperative oral surgery pain.  

UK PubMed Central (United Kingdom)

The analgesic efficacy of a single 200-mg dose of fendosal, a nonnarcotic, nonsteroidal antiinflammatory analgesic, was compared, in a double-blind study, with aspirin 650 mg, ibuprofen 400 mg and placebo in outpatients who had moderate or severe pain after the surgical removal of impacted third molars. Using a self-rating record, patients rated their pain and its relief hourly for up to 12 hours after medicating. Each active medication was significantly superior to placebo. The peak analgesic effect of fendosal 200 mg was similar to that of the aspirin 650-mg standard. Although fendosal's onset of action was slow (3 hours), its effect persisted for 8 hours, substantially longer than that of aspirin. Ibuprofen 400 mg was statistically significantly superior to aspirin 650 mg and fendosal 200 mg for most measures of peak and total analgesia, and its effect persisted for 8 hours. The results of this study raise some questions concerning the comparability of data from studies that employ different criteria for remedication and/or different criteria for the inclusion of data in the analyses of efficacy.

Forbes JA; Barkaszi BA; Ragland RN; Hankle JJ

1984-11-01

114

Analgesic effect of simultaneous exposure to infrared laser radiation and ?T magnetic field in rats  

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The aim of the experiment was to estimate the effect of repeated simultaneous exposures to infrared laser radiation and ?T variable magnetic field used in magnetostimulation on pain perception in rats, as well as the involvement of endogenous opioid system in the mechanism of this effect. In experimental group clean-shaven scull of male Wistar rats placed individually in a specially designed plastic chamber were simultaneously exposed to infrared laser radiation (wavelength - 855 nm, mean power - 4,1 mW, energy density - 30 J/cm2) and variable magnetic field of saw-like shape of impulse, at a frequency of basic impulse 180-195 Hz and mean induction value of 120 ?T generated by magneto-laser applicator of device for magnetostimulation Viofor JPS (Med & Life, Poland) 12 minutes daily for 2 periods of 5 consecutive days, with 2 days-lasting break between them, while control animals were sham-exposed. The pain perception was determined by means of "hot plate" test on the basis of calculated analgesic index. As a result of repeated exposures a significant increase in analgesic index persisting also till 14th day after the end of a cycle of exposures was observed. This analgesic effect was inhibited by prior i.p. injection of opioid antagonist - Naloxone.

Cieslar, Grzegorz; Mrowiec, Janina; Kasperczyk, Slawomir; Sieron-Stoltny, Karolina; Sieron, Aleksander

2008-03-01

115

The effect of acupressure at SP6 point on analgesic taking in women during labor  

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Full Text Available Background: According to the potential side effects of analgesics and anaesthetic drugs to control the labour pains, it is possible to replace non-medical method for palliative treatment. The purpose of this research is to assess the effect of acupressure in spleen point 6 (SP6) on the amount of analgesic drug taking during labour. Materials and Method: We conducted one sided blind randomized clinical trial in 2008. 131 term pregnant women randomly selected and divided into three groups; including one experimental group (pressure on SP6:41 persons) and two control groups (SP6 touch: 41 cases and common care: 49 persons). The data has been analyzed by using the descriptive and inferential statistics by SPSS-16 software.Results: Comparing the average amounts of the consumed drug between three groups showed a significant decrease in the experimental group more than the other two control groups (p=0.006). The average amount of consumed pethidine in the experimental group showed a significant decrease (p=0.02).Conclusion: The findings of our study showed that the pressure on SP6 is an effective method to decrease the amount of analgesic consumption in labor specially pethidine

Parisa Samad; Minoor Lamiyan; Reza Heshmat; Soghrat Faghihzade

2011-01-01

116

Evaluation of Analgesic Effects of Hydroalcoholic Extract of Marrubium parviflorum by Formalin Test in Mice  

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Full Text Available In this research, hydroalcoholic extract obtained from the aerial parts of Marrubium parviflorum (Lamiaceae) was subjected to evaluation of analgesic effects using formalin test at the doses of 50, 100 and 200 mg kg-1 in mice. Duration of licking and biting time (min) of the injected paw was recorded at 5 min intervals for 40 min after formalin injection as a pain index. Results of study showed that the dose of 100 mg kg-1 of the extract decreased duration of licking and biting time between 15 and 40 min, but this effect was not statistically significant (p>0.05), while the dose of 200 mg kg-1 of extract showed significant analgesic effects (pM. parviflorum as a valuable analgesic herbal medicine that can be used in treatment of inflammatory painful disease. It is possible to assume that phytochemical contents of M. parviflorum reduce inflammatory pain by inhibiting the formation of inflammatory mediators such as prostaglandins followed by inhibiting COX-II enzyme.

Mahnaz Khanavi; Mohammad-reza Delnavazi; Vahid Nikoui; Sattar Ostadhadi; Azam Bakhtiarian

2012-01-01

117

Heel lance in newborn during breastfeeding: an evaluation of analgesic effect of this procedure  

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Full Text Available Abstract Objectives The reduction of pain due to routine invasive procedures (capillary heel stick blood sampling for neonatal metabolic screening) in the newborn is an important objective for the so-called "Hospital with no pain". Practices such as skin to skin contact, or breastfeeding, in healthy newborn, may represent an alternative to the use of analgesic drugs. The aim of our work is to evaluate the analgesic effect of breastfeeding during heel puncture in full term healthy newborn. Methods We studied 200 healthy full term newborns (100 cases and 100 controls), proposing the puncture to mothers during breastfeeding, and explaining to them all the advantages of this practice. Pain assessment was evaluated by DAN scale (Douleur Aigue Nouveau ne scale). Results The difference in score of pain according to the DAN scale was significant in the two groups of patients (p = 0.000); the medium score was 5.15 for controls and 2.65 for cases (newborns sampled during breastfeeding). Conclusion Our results confirmed the evidence of analgesic effect of breastfeeding during heel puncture. This procedure could easily be adopted routinely in maternity wards.

Uga Elena; Candriella Manuela; Perino Antonella; Alloni Viviana; Angilella Giuseppina; Trada Michela; Ziliotto Anna; Rossi Maura; Tozzini Danila; Tripaldi Clelia; Vaglio Michela; Grossi Luigina; Allen Michaela; Provera Sandro

2008-01-01

118

Analgesic effect of leaf extract from Ageratina glabrata in the hot plate test  

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Full Text Available Ageratina glabrata (Kunth) R.M. King & H. Rob., Asteraceae (syn. Eupatorium glabratum Kunth) is widely distributed throughout Mexico and popularly known as "chamizo blanco" and "hierba del golpe" for its traditional use as external analgesic remedy. Though glabrata species has been chemically studied, there are no experimentally asserted reports about possible analgesic effects which can be inferred from its genus Ageratina. To fill the gap, we evaluated A. glabrata extracts in an animal model of nociception exploiting thermal stimuli. NMR and mass analyses identified a new thymol derivative, 10-benzoiloxy-6,8,9-trihydroxy-thymol isobutyrate (1), which was computationally converted into a ring-closed structure to explain interaction with the COX-2 enzyme in a ligand-receptor docking study. The resulting docked pose is in line with reported crystal complexes of COX-2 with chromene ligands. Based on the present results of dichloromethane extracts from its dried leaves, it is safe to utter that the plant possesses analgesic effects in animal tests which are mediated through inhibition of COX-2 enzyme.

Guadalupe García P; Edgar García S; Isabel Martínez G; Thomas R. F. Scior; José L Salvador; Mauro M Martínez P; Rosa E. del Río

2011-01-01

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Heel lance in newborn during breastfeeding: an evaluation of analgesic effect of this procedure.  

UK PubMed Central (United Kingdom)

OBJECTIVES: The reduction of pain due to routine invasive procedures (capillary heel stick blood sampling for neonatal metabolic screening) in the newborn is an important objective for the so-called "Hospital with no pain". Practices such as skin to skin contact, or breastfeeding, in healthy newborn, may represent an alternative to the use of analgesic drugs. The aim of our work is to evaluate the analgesic effect of breastfeeding during heel puncture in full term healthy newborn. METHODS: We studied 200 healthy full term newborns (100 cases and 100 controls), proposing the puncture to mothers during breastfeeding, and explaining to them all the advantages of this practice. Pain assessment was evaluated by DAN scale (Douleur Aigue Nouveau ne scale). RESULTS: The difference in score of pain according to the DAN scale was significant in the two groups of patients (p = 0.000); the medium score was 5.15 for controls and 2.65 for cases (newborns sampled during breastfeeding). CONCLUSION: Our results confirmed the evidence of analgesic effect of breastfeeding during heel puncture. This procedure could easily be adopted routinely in maternity wards.

Uga E; Candriella M; Perino A; Alloni V; Angilella G; Trada M; Ziliotto AM; Rossi MB; Tozzini D; Tripaldi C; Vaglio M; Grossi L; Allen M; Provera S

2008-01-01

120

Analgesic effect of leaf extract from Ageratina glabrata in the hot plate test  

Scientific Electronic Library Online (English)

Full Text Available Abstract in english Ageratina glabrata (Kunth) R.M. King & H. Rob., Asteraceae (syn. Eupatorium glabratum Kunth) is widely distributed throughout Mexico and popularly known as "chamizo blanco" and "hierba del golpe" for its traditional use as external analgesic remedy. Though glabrata species has been chemically studied, there are no experimentally asserted reports about possible analgesic effects which can be inferred from its genus Ageratina. To fill the gap, we evaluated A. glabrata extra (more) cts in an animal model of nociception exploiting thermal stimuli. NMR and mass analyses identified a new thymol derivative, 10-benzoiloxy-6,8,9-trihydroxy-thymol isobutyrate (1), which was computationally converted into a ring-closed structure to explain interaction with the COX-2 enzyme in a ligand-receptor docking study. The resulting docked pose is in line with reported crystal complexes of COX-2 with chromene ligands. Based on the present results of dichloromethane extracts from its dried leaves, it is safe to utter that the plant possesses analgesic effects in animal tests which are mediated through inhibition of COX-2 enzyme.

García P, Guadalupe; García S, Edgar; Martínez G, Isabel; Scior, Thomas R. F.; Salvador, José L; Martínez P, Mauro M; Río, Rosa E. del

2011-10-01

 
 
 
 
121

Bak Foong Pills induce an analgesic effect by inhibiting nociception via the somatostatin pathway in mice.  

Science.gov (United States)

Dysmenorrhoea, defined as cramping pain in the lower abdomen occurring before or during menstruation, affects, to varying degrees, up to 90% of women of child-bearing age. We investigated whether BFP (Bak Foong Pills), a traditional Chinese medicine treatment for dysmenorrhoea, possesses analgesic properties. Results showed that BFP was able to significantly reduce pain responses following subchronic treatment for 3 days, but not following acute (1 h) treatment in response to acetic acid-induced writhing in C57/B6 mice. The analgesic effect was not due to inhibition of COX (cyclo-oxygenase) activity, evidenced by the lack of inhibition of prostacyclin and PGE2 (prostaglandin E2) production. Molecular analysis revealed that BFP treatment modulated the expression of a number of genes in the spinal cord of mice subjected to acetic acid writhing. RT-PCR (reverse transcription-PCR) analysis of spinal cord samples showed that both sst4 (somatostatin receptor 4) and sst2 receptor mRNA, but not ?OR (?-opiate receptor) and NK1 (neurokinin-1) receptor mRNA, were down-regulated following BFP treatment, thus implicating somatostatin involvement in BFP-induced analgesia. Administration of c-som (cyclo-somatostatin), a somatostatin antagonist, prior to acetic acid-induced writhing inhibited the analgesic effect. Thus subchronic treatment with BFP has anti-nociceptive qualities mediated via the somatostatin pathway. PMID:21980955

Rowlands, Dewi Kenneth; Cui, Yu Gui; So, Siu Cheung; Tsang, Lai Ling; Chung, Yiu Wa; Chan, Hsiao Chang

2012-01-01

122

Bak Foong Pills induce an analgesic effect by inhibiting nociception via the somatostatin pathway in mice.  

UK PubMed Central (United Kingdom)

Dysmenorrhoea, defined as cramping pain in the lower abdomen occurring before or during menstruation, affects, to varying degrees, up to 90% of women of child-bearing age. We investigated whether BFP (Bak Foong Pills), a traditional Chinese medicine treatment for dysmenorrhoea, possesses analgesic properties. Results showed that BFP was able to significantly reduce pain responses following subchronic treatment for 3 days, but not following acute (1 h) treatment in response to acetic acid-induced writhing in C57/B6 mice. The analgesic effect was not due to inhibition of COX (cyclo-oxygenase) activity, evidenced by the lack of inhibition of prostacyclin and PGE2 (prostaglandin E2) production. Molecular analysis revealed that BFP treatment modulated the expression of a number of genes in the spinal cord of mice subjected to acetic acid writhing. RT-PCR (reverse transcription-PCR) analysis of spinal cord samples showed that both sst4 (somatostatin receptor 4) and sst2 receptor mRNA, but not ?OR (?-opiate receptor) and NK1 (neurokinin-1) receptor mRNA, were down-regulated following BFP treatment, thus implicating somatostatin involvement in BFP-induced analgesia. Administration of c-som (cyclo-somatostatin), a somatostatin antagonist, prior to acetic acid-induced writhing inhibited the analgesic effect. Thus subchronic treatment with BFP has anti-nociceptive qualities mediated via the somatostatin pathway.

Rowlands DK; Cui YG; So SC; Tsang LL; Chung YW; Chan HC

2012-01-01

123

The analgesic effect of Tribulus terrestris extract and comparison of gastric ulcerogenicity of the extract with indomethacine in animal experiments.  

Science.gov (United States)

Tribulus terrestris has been used in traditional medicine for relieving rheumatic pain and as an analgesic plant for a long time. In this investigation the analgesic effect of methanolic extract of this plant on male albino mice was evaluated by formalin and tail flick test. Extraction of the fruits of the plant was done by two different methods (suxheletion and percolation) with methanol 80%. The percolated extract was injected intraperitoneally in mice at 50, 100, 200, 400, and 800 mg/kg. The results showed that a dose of 100 mg/kg of percolated extract had the highest significant analgesic effect compared to the control group (P < 0.01) in formalin and tail flick test. There is no significant difference in the analgesic effect of suxheleted and percolated extract. The analgesic effect of the extract was lower than morphine, 2.5 mg/kg in both tests, and higher than ASA 300 mg/kg in chronic phase of pain in formalin test (P < 0.05). Pretreatment of animal with naloxone did not change the analgesia induced by the plant extract in both tests, therefore the involvement of opioid receptor in the analgesic effect of this plant was excluded. The results of ulcerogenic studies indicate that the gastric ulcerogenecity of plant extract is lower than the indomethacin in the rat's stomach. It can therefore be concluded that T. terrestris extract has a suitable analgesic effect and further studies are required to produce a more effective product of this plant to substitute for conventional analgesic drugs. PMID:17404054

Heidari, M R; Mehrabani, M; Pardakhty, A; Khazaeli, P; Zahedi, M J; Yakhchali, M; Vahedian, M

2007-01-01

124

The analgesic effect of Tribulus terrestris extract and comparison of gastric ulcerogenicity of the extract with indomethacine in animal experiments.  

UK PubMed Central (United Kingdom)

Tribulus terrestris has been used in traditional medicine for relieving rheumatic pain and as an analgesic plant for a long time. In this investigation the analgesic effect of methanolic extract of this plant on male albino mice was evaluated by formalin and tail flick test. Extraction of the fruits of the plant was done by two different methods (suxheletion and percolation) with methanol 80%. The percolated extract was injected intraperitoneally in mice at 50, 100, 200, 400, and 800 mg/kg. The results showed that a dose of 100 mg/kg of percolated extract had the highest significant analgesic effect compared to the control group (P < 0.01) in formalin and tail flick test. There is no significant difference in the analgesic effect of suxheleted and percolated extract. The analgesic effect of the extract was lower than morphine, 2.5 mg/kg in both tests, and higher than ASA 300 mg/kg in chronic phase of pain in formalin test (P < 0.05). Pretreatment of animal with naloxone did not change the analgesia induced by the plant extract in both tests, therefore the involvement of opioid receptor in the analgesic effect of this plant was excluded. The results of ulcerogenic studies indicate that the gastric ulcerogenecity of plant extract is lower than the indomethacin in the rat's stomach. It can therefore be concluded that T. terrestris extract has a suitable analgesic effect and further studies are required to produce a more effective product of this plant to substitute for conventional analgesic drugs.

Heidari MR; Mehrabani M; Pardakhty A; Khazaeli P; Zahedi MJ; Yakhchali M; Vahedian M

2007-01-01

125

[Immediate analgesic effect of wrist-ankle acupuncture for acute lumbago: a randomized controlled trial].  

UK PubMed Central (United Kingdom)

OBJECTIVE: To assess the immediate analgesic effect of wrist-ankle acupuncture on acute lumbago and the relationship between the analgesic effect and the expectation of patients. METHODS: A randomized, single-blind, sham-controlled trial was designed. Sixty cases of acute lumbago were randomly divided into two groups, 30 cases in each one. In observation group, wrist-ankle acupuncture was adopted to the Lower 5 and Lower 6 bilaterally, no requirement of Deqi (arrival of qi). In control group, sham acupuncture was adopted. The treatment was applied once in either group, with the needles retained for 30 min. The Short-form McGill Pain Questionnaire (SF-MPQ) and the Modified-Modified Schober (MMS) test were used to assess the motion related pain and the situation of spinal flexion in 3 min before treatment and 5 min, 10 min, 15 min, during treatment and 30 min (needle removed), respectively. The Expectation and Treatment Credibility Scale (ETCS) was applied to analyze the relationship between the expectation of patients and the analgesic effect. The adverse reaction was recorded. RESULTS: There were no statistically significant differences in SF-MPQ, MMS and ETCS before treatment between two groups (all P>0.05). In 5 min after needles insertion, the scores of the items in SF-MPQ in observation group were lower than those in control group (P<0.05, P<0.01). In 10 min after needles insertion, the scores of SF-MPQ in observation group were lower than those in control group and the scores of MMS were higher than those in control group (P<0.05). In 15 min after needles insertion, except the sensory pain rating index, the scores of the rest items in SF-MPQ in observation group were all lower than those in control group (P<0.05, P<0.01). In 30 min (needles removed), the scores of affective pain rating index of SF-MPQ and Visual Analogue Scale (VAS) in observation group were lower than those in control group (P<0.05, P<0.01). The expectation before treatment was negatively correlated with VAS scores in 5 min, 10 min, 15 min and 30 min after needle insertion separately in observation group (P<0.05), while the correlation was not found in control group (P>0.05). No adverse reaction was reported. CONCLUSION: Wrist-ankle acupuncture can reduce acute lumbago immediately and significantly. The higher the expectation on the analgesic effect of wrist-ankle acupuncture the patients have, the better the analgesic effect will be. This therapy is highly safe in the treatment.

Su JT; Zhou QH; Li R; Zhang J; Li WH; Wang Q

2010-08-01

126

Topical analgesics.  

UK PubMed Central (United Kingdom)

Our knowledge and understanding of the pathophysiology and treatment of pain is increasing; however, we should not lose sight of the simple opportunities that exist for intercepting pain at peripheral targets. Although systemic medication often has peripheral and central modes of action, the appeal for provision of medication close to where these peripheral targets exist should be high. If these sites can be attacked with relatively high concentrations of active drug while keeping systemic levels of that drug below the level at which systemic side effects become apparent, then this should lead to desirable outcomes. Even though the number of true topical agents with an indication for this use is small, a number of other topical agents are available that evidence suggests have the possibility of being effective. Given the increased understanding of pain, the likelihood of further topical agents becoming available is high.

McCleane G

2007-01-01

127

Analgesic effects of intra-articular fentanyl, pethidine and dexamethasone after knee arthroscopic surgery  

Directory of Open Access Journals (Sweden)

Full Text Available BACKGROUND: Many different methods have been used in an effort to provide adequate analgesia after knee arthroscopic surgery. In this study analgesic effect of intra-articular fentanyl, pethidine and dexamethasone was compared. METHODS: In a double blind randomized study 48 male patients undergoing knee arthroscopic meniscectomy were allocated to groups receiving intra-articular fentanyl 50 µg or pethidine 20 mg or dexamethasone 8 mg at the end of arthroscopy during general aesthesia. Postoperative pain scores using visual analogue scale were measured and also analgesic requirements and the time of ability to walk were recorded. RESULTS: Pain scores at one, two, six and 24 h after intra-articular injection were not significantly different for fentanyl and pethidine but were higher significantly for dexamethasone at all four mentioned times. The mean average time of ability to walk was significantly longer for dexamethasone. The analgesic requirements during the first 24 h after intraarticular injection were significantly greater only for dexamethasone too. CONCLUSION: Better postoperative analgesia, less pain score and shorter time to walk were achieved by fentanyl and pethidine in comparison to dexamethasone but the results were not significantly different between fentanyl group and pethidine. KEYWORDS: Arthroscopy, opioid, pain.

H Saryazd; P Kashefi; M Heydari; A Kiani

2006-01-01

128

Effect of some analgesics on paraoxonase-1 purified from human serum.  

Science.gov (United States)

The in vitro effects of the analgesic drugs, lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine, on the activity of purified human serum paraoxonase (hPON1) (EC 3.1.8.1.) were evaluated. hPON1 was purified from human serum with a final specific activity of 3840 U mg(-1) and a purity of 25.3 % using simple chromatographic methods, including DEAE-Sephadex anion exchange and Sepharose 4B-L-tyrozine-1-napthylamine hydrophobic interaction chromatography. SDS-polyacrylamide gel electrophoresis indicated a single protein band corresponding to hPON1. The six analgesics dose-dependently decreased in vitro hPON1 activity, with IC(50) values for lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine of 0.136, 0.195, 0.340, 1.639, 6.23 and 9.638 mM, respectively. K(i) constants were 0.009, 0.097, 0.306, 0.805, 13.010 and 11.116 mM, respectively. Analgesics showed different inhibition mechanisms: lornoxicam, diclofenac sodium and lincomycine were uncompetitive, indomethacin and tenoxicam were competitive, ketoprofen was noncompetitive. According to the results, inhibition potency was lornoxicam>indomethacin>tenoxicam> diclofenac sodium>ketoprofen> lincomycine. PMID:19548782

Ekinci, Deniz; Beydemir, Sükrü

2009-08-01

129

Effect of some analgesics on paraoxonase-1 purified from human serum.  

UK PubMed Central (United Kingdom)

The in vitro effects of the analgesic drugs, lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine, on the activity of purified human serum paraoxonase (hPON1) (EC 3.1.8.1.) were evaluated. hPON1 was purified from human serum with a final specific activity of 3840 U mg(-1) and a purity of 25.3 % using simple chromatographic methods, including DEAE-Sephadex anion exchange and Sepharose 4B-L-tyrozine-1-napthylamine hydrophobic interaction chromatography. SDS-polyacrylamide gel electrophoresis indicated a single protein band corresponding to hPON1. The six analgesics dose-dependently decreased in vitro hPON1 activity, with IC(50) values for lornoxicam, indomethacin, tenoxicam, diclofenac sodium, ketoprofen and lincomycine of 0.136, 0.195, 0.340, 1.639, 6.23 and 9.638 mM, respectively. K(i) constants were 0.009, 0.097, 0.306, 0.805, 13.010 and 11.116 mM, respectively. Analgesics showed different inhibition mechanisms: lornoxicam, diclofenac sodium and lincomycine were uncompetitive, indomethacin and tenoxicam were competitive, ketoprofen was noncompetitive. According to the results, inhibition potency was lornoxicam>indomethacin>tenoxicam> diclofenac sodium>ketoprofen> lincomycine.

Ekinci D; Beydemir S

2009-08-01

130

Analgesic effect of transcutaneous electrical nerve stimulation after laparoscopic cholecystectomy.  

UK PubMed Central (United Kingdom)

OBJECTIVE: This study aimed to assess the effect of Transcutaneous Electrical Nerve Stimulation (TENS) on pain, nausea, and emesis in patients submitted to surgery for laparoscopic cholecystectomy. DESIGN: A clinical single-masked randomized study assessed patients submitted to laparoscopic cholecystectomy, who were divided into two groups: placebo TENS (G1) and active TENS (G2). The intensity of pain was determined using the visual analog scale and the 11-point Verbal Numerical Scale, applied to the participants before (M1) and 30 mins after (M2) TENS. A conventional biphasic square pulse TENS current was used, at a frequency of 150 Hz and a pulse width of 75 ?secs. The relative risks of the occurrence of nausea and emesis were calculated for groups G1 and G2. Determination of the effect of TENS on analgesia used the Mann-Whitney U test, at a significance level of 5%, to compare independent samples (Dif G1 and Dif G2). RESULTS: The relative risk of nausea and/or emesis was 2.17 times greater for patients from the placebo group. Pain evaluation using the visual analog scale showed median differences between M1 and M2 of 0.4 and 2.4 for groups G1 and G2, respectively. The values obtained using Verbal Numerical Scale were 0.7 (G1) and 3.0 (G2). The active TENS significantly reduced postoperative pain compared with the placebo (P < 0.016). CONCLUSIONS: Active TENS promoted significant postoperative pain relief, and fewer complaints of nausea and emesis, in patients submitted to laparoscopic cholecystectomy surgery.

Silva MB; de Melo PR; de Oliveira NM; Crema E; Fernandes LF

2012-08-01

131

Spider peptide Ph?1? induces analgesic effect in a model of cancer pain.  

UK PubMed Central (United Kingdom)

The marine snail peptide ziconotide (?-conotoxin MVIIA) is used as an analgesic in cancer patients refractory to opioids, but may induce severe adverse effects. Animal venoms represent a rich source of novel drugs, so we investigated the analgesic effects and the side-effects of spider peptide Ph?1? in a model of cancer pain in mice with or without tolerance to morphine analgesia. Cancer pain was induced by the inoculation of melanoma B16-F10 cells into the hind paw of C57BL/6 mice. After 14 days, painful hypersensitivity was detected and Ph?1? or ?-conotoxin MVIIA (10-100 pmol/site) was intrathecally injected to evaluate the development of antinociception and side-effects in control and morphine-tolerant mice. The treatment with Ph?1? or ?-conotoxin MVIIA fully reversed cancer-related painful hypersensitivity, with long-lasting results, at effective doses 50% of 48 (32-72) or 33 (21-53) pmol/site, respectively. Ph?1? produced only mild adverse effects, whereas ?-conotoxin MVIIA induced dose-related side-effects in mice at analgesic doses (estimated toxic dose 50% of 30 pmol/site). In addition, we observed that Ph?1? was capable of controlling cancer-related pain even in mice tolerant to morphine antinociception (100% of inhibition) and was able to partially restore morphine analgesia in such animals (56 ± 5% of inhibition). In this study, Ph?1? was as efficacious as ?-conotoxin MVIIA in inducing analgesia in a model of cancer pain without producing severe adverse effects or losing efficacy in opioid-tolerant mice, indicating that Ph?1? has a good profile for the treatment of cancer pain in patients.

Rigo FK; Trevisan G; Rosa F; Dalmolin GD; Otuki MF; Cueto AP; de Castro Junior CJ; Romano-Silva MA; Cordeiro Mdo N; Richardson M; Ferreira J; Gomez MV

2013-09-01

132

Spider peptide Ph?1? induces analgesic effect in a model of cancer pain.  

Science.gov (United States)

The marine snail peptide ziconotide (?-conotoxin MVIIA) is used as an analgesic in cancer patients refractory to opioids, but may induce severe adverse effects. Animal venoms represent a rich source of novel drugs, so we investigated the analgesic effects and the side-effects of spider peptide Ph?1? in a model of cancer pain in mice with or without tolerance to morphine analgesia. Cancer pain was induced by the inoculation of melanoma B16-F10 cells into the hind paw of C57BL/6 mice. After 14 days, painful hypersensitivity was detected and Ph?1? or ?-conotoxin MVIIA (10-100 pmol/site) was intrathecally injected to evaluate the development of antinociception and side-effects in control and morphine-tolerant mice. The treatment with Ph?1? or ?-conotoxin MVIIA fully reversed cancer-related painful hypersensitivity, with long-lasting results, at effective doses 50% of 48 (32-72) or 33 (21-53) pmol/site, respectively. Ph?1? produced only mild adverse effects, whereas ?-conotoxin MVIIA induced dose-related side-effects in mice at analgesic doses (estimated toxic dose 50% of 30 pmol/site). In addition, we observed that Ph?1? was capable of controlling cancer-related pain even in mice tolerant to morphine antinociception (100% of inhibition) and was able to partially restore morphine analgesia in such animals (56 ± 5% of inhibition). In this study, Ph?1? was as efficacious as ?-conotoxin MVIIA in inducing analgesia in a model of cancer pain without producing severe adverse effects or losing efficacy in opioid-tolerant mice, indicating that Ph?1? has a good profile for the treatment of cancer pain in patients. PMID:23718272

Rigo, Flavia Karine; Trevisan, Gabriela; Rosa, Fernanda; Dalmolin, Gerusa D; Otuki, Michel Fleith; Cueto, Ana Paula; de Castro Junior, Célio José; Romano-Silva, Marco Aurelio; Cordeiro, Marta do N; Richardson, Michael; Ferreira, Juliano; Gomez, Marcus V

2013-06-25

133

Inhibition of GTP cyclohydrolase reduces cancer pain in mice and enhances analgesic effects of morphine.  

Science.gov (United States)

Noncoding polymorphisms of the GTP cyclohydrolase gene (GCH1) reduce the risk for chronic pain in humans suggesting GCH1 inhibitors as analgesics. We assessed the effects of the GCH1 inhibitor diaminohydroxypyrimidine (DAHP) on nociception and inflammation in a mouse melanoma and a sarcoma cancer pain model, and its co-effects with morphine in terms of analgesic efficacy and respiratory depression. GCH1 inhibition did not reduce the tumor-evoked nociceptive hypersensitivity of the tumor-bearing paw. However, DAHP reduced melanoma- and sarcoma-evoked systemic hyperalgesia as determined by analyzing contralateral paws. GCH1 inhibition increased the inflammatory edema and infiltration with polymorphonuclear leukocytes surrounding the tumor but reduced the tumor-evoked microglia activation in the spinal cord suggesting that an increase of the local immune attack against the tumor may avoid general pain hypersensitivity. When used in combination with morphine at high or low doses, GCH1 inhibition increased and prolonged the analgesic effects of the opioid. It did not, however, increase the respiratory depression caused by morphine. Conversely, the GCH1-product, tetrahydrobiopterin, caused hyperalgesia, antagonized antinociceptive effects of morphine, and aggravated morphine-evoked respiratory depression, the latter mimicked by a cGMP analog suggesting that respiratory effects were partly mediated through the BH4-NO-cGMP pathway. The observed effects of GCH1 inhibition in the tumor model and its enhancement of morphine-evoked antinociception without increase of morphine toxicity suggest that GCH1 inhibitors might be useful as co-therapeutics for opioids in cancer patients. PMID:22706600

Pickert, Geethanjali; Myrczek, Thekla; Rückert, Steven; Weigert, Andreas; Häussler, Annett; Ferreirós, Nerea; Brüne, Bernhard; Lötsch, Jörn; Tegeder, Irmgard

2012-06-17

134

Comparison of the analgesic effects of dronabinol and smoked marijuana in daily marijuana smokers.  

Science.gov (United States)

Recent studies have demonstrated the therapeutic potential of cannabinoids to treat pain, yet none have compared the analgesic effectiveness of smoked marijuana to orally administered ?(9)-tetrahydrocannabinol (THC; dronabinol). This randomized, placebo-controlled, double-dummy, double-blind study compared the magnitude and duration of analgesic effects of smoked marijuana and dronabinol under well-controlled conditions using a validated experimental model of pain. Healthy male (N=15) and female (N=15) daily marijuana smokers participated in this outpatient study comparing the analgesic, subjective, and physiological effects of marijuana (0.00, 1.98, or 3.56% THC) to dronabinol (0, 10, or 20?mg). Pain response was assessed using the cold-pressor test (CPT): participants immersed their left hand in cold water (4?°C), and the time to report pain (pain sensitivity) and withdraw the hand from the water (pain tolerance) were recorded. Subjective pain and drug effect ratings were also measured as well as cardiovascular effects. Compared with placebo, marijuana and dronabinol decreased pain sensitivity (3.56%; 20?mg), increased pain tolerance (1.98%; 20?mg), and decreased subjective ratings of pain intensity (1.98, 3.56%; 20?mg). The magnitude of peak change in pain sensitivity and tolerance did not differ between marijuana and dronabinol, although dronabinol produced analgesia that was of a longer duration. Marijuana (1.98, 3.56%) and dronabinol (20?mg) also increased abuse-related subjective ratings relative to placebo; these ratings were greater with marijuana. These data indicate that under controlled conditions, marijuana and dronabinol decreased pain, with dronabinol producing longer-lasting decreases in pain sensitivity and lower ratings of abuse-related subjective effects than marijuana. PMID:23609132

Cooper, Ziva D; Comer, Sandra D; Haney, Margaret

2013-04-22

135

Comparison of the analgesic effects of dronabinol and smoked marijuana in daily marijuana smokers.  

UK PubMed Central (United Kingdom)

Recent studies have demonstrated the therapeutic potential of cannabinoids to treat pain, yet none have compared the analgesic effectiveness of smoked marijuana to orally administered ?(9)-tetrahydrocannabinol (THC; dronabinol). This randomized, placebo-controlled, double-dummy, double-blind study compared the magnitude and duration of analgesic effects of smoked marijuana and dronabinol under well-controlled conditions using a validated experimental model of pain. Healthy male (N=15) and female (N=15) daily marijuana smokers participated in this outpatient study comparing the analgesic, subjective, and physiological effects of marijuana (0.00, 1.98, or 3.56% THC) to dronabinol (0, 10, or 20?mg). Pain response was assessed using the cold-pressor test (CPT): participants immersed their left hand in cold water (4?°C), and the time to report pain (pain sensitivity) and withdraw the hand from the water (pain tolerance) were recorded. Subjective pain and drug effect ratings were also measured as well as cardiovascular effects. Compared with placebo, marijuana and dronabinol decreased pain sensitivity (3.56%; 20?mg), increased pain tolerance (1.98%; 20?mg), and decreased subjective ratings of pain intensity (1.98, 3.56%; 20?mg). The magnitude of peak change in pain sensitivity and tolerance did not differ between marijuana and dronabinol, although dronabinol produced analgesia that was of a longer duration. Marijuana (1.98, 3.56%) and dronabinol (20?mg) also increased abuse-related subjective ratings relative to placebo; these ratings were greater with marijuana. These data indicate that under controlled conditions, marijuana and dronabinol decreased pain, with dronabinol producing longer-lasting decreases in pain sensitivity and lower ratings of abuse-related subjective effects than marijuana.

Cooper ZD; Comer SD; Haney M

2013-09-01

136

Analgesic effect and bioavailability of oral ketogan given as tablets or mixture to patients with chronic pain of malignant origin.  

UK PubMed Central (United Kingdom)

Thirteen cancer patients with moderate to severe chronic pain of malignant origin on treatment with Ketogan tablets were included in an open non-randomized cross-over study comparing the analgesic effect, side effects and serum concentrations of Ketogan tablets and mixture. The patients were six days in hospital and were dosed two days with tablets, two days with mixture and finally another two days with tablets. Recordings of pain and side effects and collection of blood samples prior to dosing and hourly thereafter until remedication were performed on the second day of each dosing period in a morning dose interval. The analgesic effect judged by visual analog score (VAS) and pain intensity differences (PID), the areas under the serum concentration time curves, and the average serum concentrations for the three groups were compared. It was not possible do detect any differences among the three groups concerning the analgesic effect, duration of analgesic effect, the serum concentrations and the side effects. The mean plasma half-life of ketobemidone was 2.74 h +/- 0.90 (SD) and the mean relative bioavailability of the mixture was slightly above 100%. Linear regression analysis revealed a significant correlation between ketobemidone serum concentrations and analgesic effect, VAS, for tablet one and for the mixture but not for tablet two, possibly due to the fixed dosing schedule and to the positive effect of hospitalization on the pain.

Kjaer M; Nielsen H

1988-01-01

137

"Comparison of the analgesic profile and side effects of tramadol vs pethidine, following urologoical surgery "  

Directory of Open Access Journals (Sweden)

Full Text Available The optimization of pain management following surgery with minimal side effects, is one the major goals of surgical and medical teams. In this randomized double blind study, sixty ASA (American Society of Anesthesiologist) class I or II patients, undergoing urological surgery, were assessed to receive either pethidine or tramadol using a standard method for general anesthesia. Pain intensity was assessed by verbal rating, through a 4-step scaling system. Results of this investigation have revealed that the mean total drug administered in tramadol group were 244.53 + 56.95 mg and in pethidine group 176.78+42.99 mg respectively. There were no significant differences in analgesic effect, observed in either group during early hours following surgery, but after 8,12 and 16 hours significant differences were observed. Analgesic properties of tramadol were almost comparable with pethidine nevertheless; pethidine was superior in some extent. No significant differences in patient’s PaO2 were found, but PaCO2 at 1 and 4 hours after surgery had a greater retention in pethidine group. (P<0.001). There was a significant reduction in respiratory rate in pethidine group at 4,8,12 and 16 hours following surgery, compared with tramadol group (P<0.001). Incidence of dizziness was greater in patients who received pethidine (P<0.001), and sweating was higher in tramadol group (P<0.01). Also there was a greater need for metoclopramide to overcome nausea in tramadol group (P<0.05). Results of this study may suggest that tramadol could be considered as a safe and effective analgesic, following urological surgery as compared with pethidine

Mojtaba Mojtahedzadeh; Farshad Hashemian; Atabak Najafi; Mohammad Reza Rouini; Mohammad K. Aghamir; Hassan Tavakoli; Omid Soofinia; Mohammad R. Khajavi

2004-01-01

138

[Anticholinesterases; peripheral and central effects].  

UK PubMed Central (United Kingdom)

Anticholinesterase, such as neostigmine, was used to be a standard drug at the end of surgery for reversal of nondepolarizing neuromuscular block. Neostigmine decreases the metabolism of acetylcholine (ACh) at the neuromuscular junction and allows its concentration to increase and overcome the effect of the muscle relaxant. But this approach is ineffective against profound block. Rapid reversal from deep block is not possible and giving a reversal agent early will not speed up the recovery time. Anticholinesterases have actions both at the nicotinic and the muscarinic receptors, and even when accompanied by an antimuscarinic agent, they produce undesirable autonomic responses. Some anticholinesterase, like donepezil, exhibits high specificity for centrally active acetylcholinesterase and raise ACh levels in the brain. The deficiency in cholinergic neurotransmission in Alzheimer's disease (AD) has led to the development of cholinesterase inhibitors as the first-line treatment for symptoms of this disease. In addition to donepezil, two other cholinesterase inhibitors have recently been approved for the treatment of AD patients. The drugs have slightly different pharmacological properties, but they all work by inhibiting the breakdown of acetylcholine, an important neurotransmitter associated with memory, by blocking the enzyme acetylcholinesterase. Donepezil can also reverse opioid-induced respiratory depression.

Sato T; Nakatsuka H

2013-01-01

139

Potent analgesic effects of a store-operated calcium channel inhibitor.  

Science.gov (United States)

Chronic pain often accompanies immune responses and immune cells are known to be involved in chronic pain. Store-operated calcium (SOC) channels are calcium-selective cation channels and play an important role in the immune system. YM-58483, a potent SOC channel inhibitor, has been shown to inhibit cytokine production from immune cells and attenuate antigen-induced hypersensitivity reactions. Here, we report that YM-58483 has analgesic actions in chronic pain and produces antinociceptive effects in acute pain and prevents the development of chronic pain in mice. Oral administration of 10mg/kg or 30mg/kg YM-58483 dramatically attenuated complete Freund adjuvant (CFA)-induced thermal hyperalgesia and prevented the development of thermal and mechanical hypersensitivity in a dose-dependent manner. Analgesic effects were observed when YM-58483 was administered systemically, intrathecally and intraplantarly. YM-58483 decreased spared nerve injury (SNI)-induced thermal and mechanical hypersensitivity and prevented the development of SNI-induced pain hypersensitivity. Pretreatment with YM-58483 strongly reduced both the first and second phases of formalin-induced spontaneous nocifensive behavior in a dose-dependent manner. YM-58483 produced antinociception in acute pain induced by heat or chemical or mechanical stimuli at a dose of 30mg/kg. YM-58483 diminished CFA-induced paw edema, and reduced production of TNF-?, IL-1? and PGE2 in the CFA-injected paw. In vitro, SOC entry in nociceptors was more robust than in nonnociceptors, and the inhibition of SOC entry by YM-58483 in nociceptors was much greater than in nonnociceptors. Our findings indicate that YM-58483 is a potent analgesic and suggest that SOC channel inhibitors may represent a novel class of therapeutics for pain. PMID:23778292

Gao, Ruby; Gao, Xinghua; Xia, Jingsheng; Tian, Yuzhen; Barrett, James E; Dai, Yue; Hu, Huijuan

2013-06-15

140

Antioxidant, Analgesic, Anti-Inflammatory, and Hepatoprotective Effects of the Ethanol Extract of Mahonia oiwakensis Stem.  

Science.gov (United States)

The aim of this study was to evaluate pharmacological properties of ethanol extracted from Mahonia oiwakensis Hayata stems (MOS(EtOH)). The pharmacological properties included antioxidant, analgesic, anti-inflammatory and hepatoprotective effects. The protoberberine alkaloid content of the MOS(EtOH) was analyzed by high-performance liquid chromatography (HPLC). The results revealed that three alkaloids, berberine, palmatine and jatrorrhizine, could be identified. Moreover, the MOS(EtOH) exhibited antioxidative activity using the DPPH assay (IC(50), 0.743 mg/mL). The DPPH radical scavenging activity of MOS(EtOH) was five times higher that that of vitamin C. MOS(EtOH) was also found to inhibit pain induced by acetic acid, formalin, and carrageenan inflammation. Treatment with MOS(EtOH) (100 and 500 mg/kg) or silymarin (200 mg/kg) decreased the serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared with the CCl(4)-treated group. Histological evaluation showed that MOS(EtOH) reduced the degree of liver injury, including vacuolization, inflammation and necrosis of hepatocytes. The anti-inflammatory and hepatoprotective effect of MOS(EtOH) were found to be related to the modulation of antioxidant enzyme activity in the liver and decreases in malondialdehyde (MDA) level and nitric oxide (NO) contents. Our findings suggest that MOS(EtOH) has analgesic, anti-inflammatory and hepatoprotective effects. These effects support the use of MOS(EtOH) for relieving pain and inflammation in folk medicine. PMID:23364614

Chao, Jung; Liao, Jiunn-Wang; Peng, Wen-Huang; Lee, Meng-Shiou; Pao, Li-Heng; Cheng, Hao-Yuan

2013-01-30

 
 
 
 
141

Antioxidant, Analgesic, Anti-Inflammatory, and Hepatoprotective Effects of the Ethanol Extract of Mahonia oiwakensis Stem  

Science.gov (United States)

The aim of this study was to evaluate pharmacological properties of ethanol extracted from Mahonia oiwakensis Hayata stems (MOSEtOH). The pharmacological properties included antioxidant, analgesic, anti-inflammatory and hepatoprotective effects. The protoberberine alkaloid content of the MOSEtOH was analyzed by high-performance liquid chromatography (HPLC). The results revealed that three alkaloids, berberine, palmatine and jatrorrhizine, could be identified. Moreover, the MOSEtOH exhibited antioxidative activity using the DPPH assay (IC50, 0.743 mg/mL). The DPPH radical scavenging activity of MOSEtOH was five times higher that that of vitamin C. MOSEtOH was also found to inhibit pain induced by acetic acid, formalin, and carrageenan inflammation. Treatment with MOSEtOH (100 and 500 mg/kg) or silymarin (200 mg/kg) decreased the serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared with the CCl4-treated group. Histological evaluation showed that MOSEtOH reduced the degree of liver injury, including vacuolization, inflammation and necrosis of hepatocytes. The anti-inflammatory and hepatoprotective effect of MOSEtOH were found to be related to the modulation of antioxidant enzyme activity in the liver and decreases in malondialdehyde (MDA) level and nitric oxide (NO) contents. Our findings suggest that MOSEtOH has analgesic, anti-inflammatory and hepatoprotective effects. These effects support the use of MOSEtOH for relieving pain and inflammation in folk medicine.

Chao, Jung; Liao, Jiunn-Wang; Peng, Wen-Huang; Lee, Meng-Shiou; Pao, Li-Heng; Cheng, Hao-Yuan

2013-01-01

142

Antioxidant, Analgesic, Anti-Inflammatory, and Hepatoprotective Effects of the Ethanol Extract of Mahonia oiwakensis Stem.  

UK PubMed Central (United Kingdom)

The aim of this study was to evaluate pharmacological properties of ethanol extracted from Mahonia oiwakensis Hayata stems (MOS(EtOH)). The pharmacological properties included antioxidant, analgesic, anti-inflammatory and hepatoprotective effects. The protoberberine alkaloid content of the MOS(EtOH) was analyzed by high-performance liquid chromatography (HPLC). The results revealed that three alkaloids, berberine, palmatine and jatrorrhizine, could be identified. Moreover, the MOS(EtOH) exhibited antioxidative activity using the DPPH assay (IC(50), 0.743 mg/mL). The DPPH radical scavenging activity of MOS(EtOH) was five times higher that that of vitamin C. MOS(EtOH) was also found to inhibit pain induced by acetic acid, formalin, and carrageenan inflammation. Treatment with MOS(EtOH) (100 and 500 mg/kg) or silymarin (200 mg/kg) decreased the serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared with the CCl(4)-treated group. Histological evaluation showed that MOS(EtOH) reduced the degree of liver injury, including vacuolization, inflammation and necrosis of hepatocytes. The anti-inflammatory and hepatoprotective effect of MOS(EtOH) were found to be related to the modulation of antioxidant enzyme activity in the liver and decreases in malondialdehyde (MDA) level and nitric oxide (NO) contents. Our findings suggest that MOS(EtOH) has analgesic, anti-inflammatory and hepatoprotective effects. These effects support the use of MOS(EtOH) for relieving pain and inflammation in folk medicine.

Chao J; Liao JW; Peng WH; Lee MS; Pao LH; Cheng HY

2013-01-01

143

Antioxidant, Analgesic, Anti-Inflammatory, and Hepatoprotective Effects of the Ethanol Extract of Mahonia oiwakensis Stem  

Directory of Open Access Journals (Sweden)

Full Text Available The aim of this study was to evaluate pharmacological properties of ethanol extracted from Mahonia oiwakensis Hayata stems (MOSEtOH). The pharmacological properties included antioxidant, analgesic, anti-inflammatory and hepatoprotective effects. The protoberberine alkaloid content of the MOSEtOH was analyzed by high-performance liquid chromatography (HPLC). The results revealed that three alkaloids, berberine, palmatine and jatrorrhizine, could be identified. Moreover, the MOSEtOH exhibited antioxidative activity using the DPPH assay (IC50, 0.743 mg/mL). The DPPH radical scavenging activity of MOSEtOH was five times higher that that of vitamin C. MOSEtOH was also found to inhibit pain induced by acetic acid, formalin, and carrageenan inflammation. Treatment with MOSEtOH (100 and 500 mg/kg) or silymarin (200 mg/kg) decreased the serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared with the CCl4-treated group. Histological evaluation showed that MOSEtOH reduced the degree of liver injury, including vacuolization, inflammation and necrosis of hepatocytes. The anti-inflammatory and hepatoprotective effect of MOSEtOH were found to be related to the modulation of antioxidant enzyme activity in the liver and decreases in malondialdehyde (MDA) level and nitric oxide (NO) contents. Our findings suggest that MOSEtOH has analgesic, anti-inflammatory and hepatoprotective effects. These effects support the use of MOSEtOH for relieving pain and inflammation in folk medicine.

Jung Chao; Jiunn-Wang Liao; Wen-Huang Peng; Meng-Shiou Lee; Li-Heng Pao; Hao-Yuan Cheng

2013-01-01

144

A study on anti-inflammatory and analgesic effects of alkaloids of Toddalia asiatica  

Directory of Open Access Journals (Sweden)

Full Text Available Objective: To study the pharmacological activities and toxicity of the crude alkaloids of Toddalia asiatica and to provide pharmacological data for the further development of this herbal medicine. Methods: We observed the anti-inflammatory effects of the crude alkaloids of Toddalia asiatica, using xylol and agra to induce the turgidness and sodium carboxymethyl cellulose (CMC-Na) to induce leucocyte strolling in the rats. The analgesic effects were observed by body-distortion methods. The effects of alkaloids of Toddalia asiatica on hepatic function were observed by testing the contents of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in serum and calculating the liver index. The LD50 and 95% creditability were calculated with developed Karber Method. Results: The administration of alkaloids of Toddalia asiatica had the function of inhibiting the auricle swelling caused by xylol and joint swelling caused by agar and leucocyte migration caused by CMC-Na, decreasing the body-distortion of the rats. After two-week administration, the contents of ALT and AST showed that there was no obvious difference between administered group and control group. The LD50 of the crude alkaloids of Toddalia asiatica was 1.622 g/kg and the 95% creditability was 1.29-2.03 g/kg. Conclusion: Toddalia asiatica has anti-inflammatory and analgesic effects, and there is no injury to the liver after long-term administration in rats

HAO Xiao-Yan

2004-01-01

145

Performance characteristics and validation of the Opioid-Related Symptom Distress Scale for evaluation of analgesic side effects after orthopedic surgery.  

UK PubMed Central (United Kingdom)

BACKGROUND: The Opioid-Related Symptom Distress Scale (ORSDS) is a 4-point scale that evaluates 3 symptom distress dimensions (frequency, severity, bothersomeness) for 12 symptoms. The symptom-specific ORSDS is the average of the 3 symptom distress dimensions. The composite ORSDS is the average of 12 symptom-specific scores. The ORSDS was validated for outpatient laparoscopic cholecystectomy (under general anesthesia) by assessment of internal consistency, content validity, construct validity, principal components analysis, known group validity, responsiveness, and opioid dose dependency. Additional validation studies were suggested. We investigated performance characteristics and validity of the ORSDS for postoperative analgesia after 4 types of anesthetic and analgesic regimens. METHODS: The ORSDS and validation questions were administered to 4 groups of 50 orthopedic patients. Peripheral nerve blockade (Peripheral) was performed for distal upper extremity surgery; neuraxial anesthesia (Neuraxial) was performed for anterior cruciate ligament reconstruction; combined spinal-epidural anesthesia/femoral nerve block/epidural analgesia (Regional) was performed for total knee arthroplasty; and general anesthesia/IV opioids (GA) was performed for posterior lumbar spine fusion. All patients also received oral opioid analgesics. RESULTS: Median composite ORSDS scores on postoperative day 1 were 0.19 (Peripheral), 0.52 (Neuraxial), 0.51 (Regional), and 0.94 (GA). The following symptoms had median symptom-specific ORSDS scores >0: Neuraxial = drowsiness, dry mouth; Regional = dizziness, dry mouth; GA = nausea, fatigue, dizziness, drowsiness, dry mouth. Problematic symptoms (symptoms for which at least 25%of patients reported symptom-specific ORSDS scores >1) were: all groups = drowsiness, dry mouth, fatigue; Neuraxial = nausea, dizziness, itchiness; Regional = nausea, dizziness, itchiness; GA = difficulty concentrating, headache, nausea, dizziness, itchiness. High symptom-specific ORSDS scores were associated with clinically meaningful adverse events. In some cases, relevant ORSDS scores were related to activity level, patient satisfaction, and nausea and vomiting measures. Many components occurred in correlated clusters. Responsiveness statistics (the ability of an instrument to detect changes once they have occurred) were high for nausea and vomiting. Linear regression analysis indicated that opioid use was associated with composite ORSDS scores for Peripheral, Regional, and GA. CONCLUSIONS: Validity of the ORSDS was supported by predetermined validation criteria, including measures of internal consistency, content validity, construct validity, principal components analysis, known group validity, responsiveness, and correlation with opioid intake. The ORSDS is a valid tool for assessment of opioid side effects after orthopedic surgery, and can be used in clinical trials involving a wide variety of anesthetic and analgesic regimens.

Yadeau JT; Liu SS; Rade MC; Marcello D; Liguori GA

2011-08-01

146

Evaluation of the analgesic effect of Echium amoenum Fisch & C.A. Mey. extract in mice: possible mechanism involved.  

UK PubMed Central (United Kingdom)

Echium amoenum Fisch & C.A. Mey. has been used in Iranian traditional medicine as demulcent and analgesic in common cold from long ago. In this investigation, the analgesic effect of the methanolic extract of the petals of this plant on male albino mice was evaluated by formalin and hot-plate test. The methanolic percolated extract with different doses 5, 10, 20 and 30 mg/kg were injected intraperitoneally to mice. The results showed that the dose of 10 mg/kg of extract had the highest analgesia in formalin (P<0.05) and hot-plate test (P<0.01) compared to the control group. The analgesic effect of extract was lower than morphine 2.5 mg/kg and ASA 300 mg/kg in the chronic phase of pain in formalin test (P<0.05) and in hot-plate test too (P<0.05). Pretreatment of animal with naloxone 4 mg/kg, s.c. 5 min before extract, decreased the analgesia induced by extract in hot-plate and acute phase of formalin tests; therefore, the opioid receptor may be involved at least partly in the analgesic effect of Echium amoenum extract. The results suggested that Echium amoenum extract has a suitable analgesic effect and further studies are required to evaluate these effects and the potential of the plant.

Heidari MR; Azad EM; Mehrabani M

2006-02-01

147

Synergism between analgesics.  

DEFF Research Database (Denmark)

The concept and value of 'multimodal' or 'balanced' analgesia in the treatment of postoperative pain is reviewed. Based upon the relatively few multimodal studies compared to unimodal studies, it is concluded that a combination of analgesics will improve pain relief including movement-associated pain. Since analgesic combination therapy is rational, further studies are needed to evaluate the optimal combination for each surgical procedure, as well as to assess the risk of side effects and need for surveillance in large-scale studies.

Kehlet, H

1995-01-01

148

Comparison of Postoperative Analgesic Effect of Tramadol With Lidocaine When Used as Subcutaneous Local Anesthetic  

Directory of Open Access Journals (Sweden)

Full Text Available We conducted a double blind, controlled trial comparing postoperative analgesic effect of tramadol with lidocaine when used as subcutaneous local anesthetic. Seventy ASA physical status 1 or 2 patients aged 20-50 years, who were scheduled for elective surgery under general anesthesia with flank incision, were randomly assigned to receive either 2 mg kg-1 tramadol or 1 mg kg-1 lidocaine at the end of operation. Postoperative pain was evaluated with a Verbal Analogue Scale (VAS). First VAS and patient’s satisfaction with operation were recorded at recovery room, second record was in the ward (12 h later) and third on the next day of surgery (24 h later). Local reactions, nausea and vomiting in recovery and the ward and time to first request for analgesic after operation were also recorded. Satisfaction with operation in recovery room was better in tramadol group (p = 0.016). The VAS score did not differ significantly between the two groups in recovery (p = 0.119), 12 h (p = 0.316) and 24 h after the operation (p = 0.108). Time to first analgesic requirement in tramadol group was longer (4.3±0.3 h) than lidocaine group (2.1±0.9 h) (p = 0.012). Ten patients in tramadol and 2 in lidocaine group had nausea in recovery room (p = 0.01). Eight and three patients had nausea in the ward, respectively (p = 0.101). There was not significant difference in vomiting between two groups in the recovery and the ward (p = 0.106 and p = 0.112, respectively). No local reactions were recorded in either group. This study showed that subcutaneous administration of tramadol provided local anesthesia equal to lidocaine with longer pain-free period after operation.

Sussan Soltanimohammadi; Mirsadegh Seyedi

2007-01-01

149

Behavioral effects of a novel kappa opioid analgesic, U-50488, in rats and rhesus monkeys.  

UK PubMed Central (United Kingdom)

U-50488 [trans-3,4-dichloro-N-(2-(1-pyrrolidinyl) cyclohexyl)-benzeneacetamide] is a structurally novel analgesic reported to have specific kappa opioid receptor agonist properties. Potent antinociceptive activity was demonstrated in rhesus monkeys and the effect was reversed by naloxone. The overt behavioral effects of U-50488 at supra-analgesic doses more closely resembled those of ethylketocyclazocine (EKC) than morphine. In monkeys trained to discriminate a 10-micrograms/kg dose of EKC from saline, the stimulus effects generalized completely to U-50488 and other kappa agonists (e.g., bremazocine, cyclazocine), but not to the pure mu agonists. Like the other kappa agonists, U-50488 produced diuresis in monkeys by a naloxone-sensitive mechanism. In drug-naive rats offered continuous opportunity to self-administer drugs IV, most rats self-administered morphine or EKC, but none of the rats self-administered U-50488 at a rate above that of a group offered saline. Rats with continuous IV infusion of U-50488 for 3 weeks exhibited few abstinence signs and no weight loss when challenged with an injection of naloxone or after abrupt cessation of drug infusion. These experimental results support the previous reports in mice that U-50488 is a very selective kappa opioid agonist in rats and rhesus monkeys.

Tang AH; Collins RJ

1985-01-01

150

Analgesic effect of topical diclofenac versus betamethasone after posterior segment surgery.  

UK PubMed Central (United Kingdom)

BACKGROUND: In clinical use, topical diclofenac, a nonsteroidal antiinflammatory, was found to be remarkably effective as an analgesic. A trial was therefore conducted to quantify and compare this effect with that of other drugs commonly used after posterior segment surgery. METHODS: A single-blind, randomized study of 37 patients undergoing posterior segment surgery was conducted. On the day of surgery and for 30 days thereafter, one group received topical diclofenac 0.1% and one group received topical betamethasone 0.1%. Pain intensity was assessed by two standard psychologic tests, the McGill Pain Questionnaire (MPQ) and Scott's Visual Analogic Scale (VAS). RESULTS: The group receiving diclofenac had significantly lower pain scores on the MPQ at days 1 and 15 (P < 0.05 and P < 0.03, respectively). The VAS scores were also statistically lower for this group on day 15 (P < 0.03). CONCLUSION: Topical diclofenac 0.1% has greater analgesic action than topical betamethasone 0.1% without the side effects of steroids, and may be useful after posterior segment surgery.

Lesnoni G; Coppe AM; Manni G; Billi B; Stirpe M

1995-01-01

151

Analgesic and anti-inflammatory effects of ethanol extracted leaves of selected medicinal plants in animal model  

Directory of Open Access Journals (Sweden)

Full Text Available Aim: The research was carried out to investigate the analgesic and anti-inflammatory effects of ethanol extract of Desmodium pauciflorum, Mangifera indica and Andrographis paniculata leaves. Materials and Methods: In order to assess the analgesic and anti-inflammatory effects acetic acid induced writhing response model and carrageenan induced paw edema model were used in Swiss albino mice and Wistar albino rats, respectively. In both cases, leaves extract were administered (2gm/kg body weight) and the obtained effects were compared with commercially available analgesic and anti-inflammatory drug Dclofenac sodium (40mg/kg body weight). Distilled water (2ml/kg body weight) was used as a control for the study. Results: In analgesic bioassay, oral administration of the ethanol extract of leaves were significantly (p<0.01) reduced the writhing response. The efficacy of leaves extract were almost 35% in Desmodium pauciflorum, 56% in Mangifera indica and 34% in Andrographis paniculata which is found comparable to the effect of standard analgesic drug diclofenac sodium (76%). Leaves extract reduced paw edema in variable percentages but they did not show any significant difference among the leaves. Conclusion: We recommend further research on these plant leaves for possible isolation and characterization of the various active chemical substances which has the toxic and medicinal values. [Vet World 2013; 6(2.000): 68-71

Mohammad M. Hassan; Shahneaz A. Khan; Amir H. Shaikat; Md. Emran Hossain; Md. Ahasanul Hoque; Md Hasmat Ullah; Saiful Islam

2013-01-01

152

Effect of transcutaneous electrical stimulation on nociception and edema induced by peripheral serotonin.  

UK PubMed Central (United Kingdom)

Transcutaneous electrical nerve stimulation (TENS) is defined as the application of an electrical current to the skin through surface electrodes for pain relief. Various theories have been proposed in order to explain the analgesic mechanism of TENS. Recent studies have demonstrated that part of this analgesia is mediated through neurotransmitters acting at peripheral sites. The aim of this study was to investigate the effects of low frequency (LF: 10 HZ) TENS and high frequency (HF: 130 HZ) TENS on hyperalgesia and edema when applied before the serotonin (5-HT) administered into the rat paw. LF and HF TENS were applied to the right paw for 20 min, and 5-HT was administered immediately after TENS. The Hargreaves method was used to measure nociception, while the hydroplethysmometer (Ugo Basile®) was used to measure edema. Neither HF nor LF TENS inhibited 5-HT-induced edema. However, LF TENS, but not HF TENS, completely reduced 5-HT-induced hyperalgesia. Pre-treatment of the paw with naltrexone, prior to application of TENS, (Nx: 50 ?g; I.pl.) showed a complete blockade of the analgesic effect induced by low frequency TENS. Thus, our results confirmed the lack of an anti-inflammatory effect through the use of TENS as well as the participation of peripheral endogenous opioid receptors in LF TENS analgesia in addition to its central action.

Santos CM; Francischi JN; Lima-Paiva P; Sluka KA; Resende MA

2013-07-01

153

Effect of transcutaneous electrical stimulation on nociception and edema induced by peripheral serotonin.  

Science.gov (United States)

Transcutaneous electrical nerve stimulation (TENS) is defined as the application of an electrical current to the skin through surface electrodes for pain relief. Various theories have been proposed in order to explain the analgesic mechanism of TENS. Recent studies have demonstrated that part of this analgesia is mediated through neurotransmitters acting at peripheral sites. The aim of this study was to investigate the effects of low frequency (LF: 10 HZ) TENS and high frequency (HF: 130 HZ) TENS on hyperalgesia and edema when applied before the serotonin (5-HT) administered into the rat paw. LF and HF TENS were applied to the right paw for 20 min, and 5-HT was administered immediately after TENS. The Hargreaves method was used to measure nociception, while the hydroplethysmometer (Ugo Basile®) was used to measure edema. Neither HF nor LF TENS inhibited 5-HT-induced edema. However, LF TENS, but not HF TENS, completely reduced 5-HT-induced hyperalgesia. Pre-treatment of the paw with naltrexone, prior to application of TENS, (Nx: 50 ?g; I.pl.) showed a complete blockade of the analgesic effect induced by low frequency TENS. Thus, our results confirmed the lack of an anti-inflammatory effect through the use of TENS as well as the participation of peripheral endogenous opioid receptors in LF TENS analgesia in addition to its central action. PMID:23336713

Santos, Cristiane M F; Francischi, Janetti N; Lima-Paiva, Patrícia; Sluka, Kathleen A; Resende, Marcos A

2013-03-15

154

Analgesic effect of acupuncture at hegu (LI 4) on transvaginal oocyte retrieval with ultrasonography.  

UK PubMed Central (United Kingdom)

OBJECTIVE: To observe the analgesic effect of acupuncture at Hegu (LI 4) in vitro fertilization-embryo transfer (IVF-ET) transvaginal oocyte retrieval using ultrasonography and explore its mechanism. METHODS: Ninety patients undergoing IVF-EF oocyte retrieval were randomly divided into three groups: an acupuncture group with needles inserted into bilateral Hegu (LI 4) points, a placebo group given placebo needles, and a control group with routine oocyte retrieval. Each group had an indometacin enema 30 min before the operation. We compared the pain-rated index (PRI), visual analogy scale (VAS), and present pain intensity (PPI) immediately after operation and 1 h after operation. We also determined the neuropeptide Y (NPY) level of the follicular fluid. RESULTS: PRI, VAS, and PPI after operation and 1 h after operation in the acupuncture group were significantly lower than those in the control group (P < 0.01). No obvious difference (P > 0.05) was observed in PRI, VAS, and PPI after operation and 1 h after operation between the placebo group and the control group. The NPY level of the follicular fluid in the acupuncture group was significantly higher than that in the control group (P < 0.01). No obvious difference (P > 0.05) was observed in the NPY level of the follicular fluid between the placebo group and the control group. CONCLUSION: The analgesic effect of acupuncture at Hegu in transvaginal oocyte retrieval using ultrasonography may be related to the increase in the NPY level of the follicular fluid.

Zhang J; Wang X; Lü R

2013-06-01

155

Role of serotonin in pathogenesis of analgesic induced headache  

Energy Technology Data Exchange (ETDEWEB)

Analgesic abuse has recently been recognized as a cause of deterioration in primary headache patients. Although the pathogenesis of this headache transformation is still obscure, and alteration of central pain control system is one possible mechanism. A number of recent studies indicated that simple analgesics exert their effect by modulating the endogenous pain control system rather than the effect at the peripheral tissue, as previously suggested. Serotonin (5-hydroxytryptamine ; 5-HT) has long been known to play a pivotal role in the pain modulatory system in the brainstem. In the present study, we investigated the changes in 5-HT system in platelets and brain tissue. A significant decrease in platelet 5-HT concentration (221.8{+-}30.7, 445.3{+-}37.4 and 467.2{+-}38.5 ng/10{sup 9} platelets, for patients with analgesic-induced headache and migraine patients, respectively, p<0.02) were evident in patients with analgesic induced headache. Chronic paracetamol administration induced a decrease in 5-HT{sub 2} serotonin receptor in cortical and brain stem tissue in experimental animals (B{sub max}=0.93{+-}0.04 and 1.79{+-}0.61 pmol/mg protein for paracetamol treated rat and controls, respectively, p<0.05). Our preliminary results suggested that chronic administration of analgesics interferes with central and peripheral 5-HT system and therefore possibly alters the 5-HT dependent antinociceptive system. (author)

Srikiatkhachorn, A.

1999-12-16

156

Evaluation of the analgesic effect of Echium amoenum Fisch & C.A. Mey. extract in mice: possible mechanism involved.  

Science.gov (United States)

Echium amoenum Fisch & C.A. Mey. has been used in Iranian traditional medicine as demulcent and analgesic in common cold from long ago. In this investigation, the analgesic effect of the methanolic extract of the petals of this plant on male albino mice was evaluated by formalin and hot-plate test. The methanolic percolated extract with different doses 5, 10, 20 and 30 mg/kg were injected intraperitoneally to mice. The results showed that the dose of 10 mg/kg of extract had the highest analgesia in formalin (PEchium amoenum extract. The results suggested that Echium amoenum extract has a suitable analgesic effect and further studies are required to evaluate these effects and the potential of the plant. PMID:16185831

Heidari, Mahmoud Reza; Azad, Elham Moein; Mehrabani, Mitra

2005-09-26

157

Comparison of tolerance to morphine-induced respiratory and analgesic effects in mice.  

UK PubMed Central (United Kingdom)

Morphine is responsible for severe poisonings in chronically treated patients. We hypothesize that toxicity could be related to the development of weaker tolerance for morphine-induced deleterious respiratory effects in comparison to analgesic effects. Our objectives were to compare tolerance to both effects in mice and investigate possible mechanisms for such possible differences. Tolerance to morphine-induced analgesia and respiratory effects was assessed using hot plate response latencies and plethysmography, respectively. Mechanisms of tolerance were investigated using binding studies to mu-opioid receptors (MOR) and adenylate cyclase (AC) activity measurement in homogenates of cell membranes from the periaqueductal gray region (PAG) and brainstem. Morphine (2.5 mg/kg) was responsible for analgesia with significant increase in inspiratory time. Acute tolerance to analgesia (p<0.01) and effects on respiratory frequency (p<0.05) was observed in mice pre-treated with 100 mg/kg morphine in comparison to saline. Following repetitive administration (2.5 mg/kg/day during 10 days), we observed a 13-fold increase in the effective dose-50% (ED??) of morphine-induced analgesia in comparison to a 2- or 4-fold increase in the ED?? of its related increase in inspiratory time determined in air and 4% CO?, respectively. No significant alteration in MOR expression was observed in either PAG or brainstem following repeated morphine administration. However, in PAG, in contrast to brainstem, superactivation of AC was observed in morphine-treated mice in comparison to controls (p<0.05). In conclusion, tolerance to morphine-induced respiratory effects is much more limited than tolerance to its analgesic effects in repeatedly morphine-treated mice. The difference in morphine-induced AC activation between the brainstem and the PAG contributes to the observed difference in tolerance between both morphine effects.

Mohammed W; Alhaddad H; Marie N; Tardy F; Lamballais F; Risčde P; Noble F; Baud FJ; Mégarbane B

2013-03-01

158

The recent progress in research on effects of anesthetics and analgesics on G protein-coupled receptors.  

UK PubMed Central (United Kingdom)

The exact mechanisms of action behind anesthetics and analgesics are still unclear. Much attention was focused on ion channels in the central nervous system as targets for anesthetics and analgesics in the 1980s. During the 1990s, major advances were made in our understanding of the physiology and pharmacology of G protein coupled receptor (GPCR) signaling. Thus, several lines of studies have shown that G protein coupled receptors (GPCRs) are one of the targets for anesthetics and analgesics and especially, that some of them inhibit the functions of GPCRs, i.e,, muscarinic receptors and substance P receptors. However, these studies had been focused on only G(q) coupled receptors. There has been little work on G(s)- and G(i)-coupled receptors. In the last decade, a new assay system, using chimera G(i/o)-coupled receptor fused to Gq(i5), has been established and the effects of anesthetics and analgesics on the function of G(i)-coupled receptors is now more easily studied. This review highlights the recent progress of the studies regarding the effects of anesthetics and analgesics on GPCRs.

Minami K; Uezono Y

2013-04-01

159

The analgesic effect of inhalational Entonox for extracorporeal shock wave lithotripsy.  

Science.gov (United States)

Extracorporeal shock wave lithotripsy (ESWL) is a non-invasive procedure that allows urinary stones to be fragmented using acoustic shock waves. The impact of the shock waves causes transient stinging pain at the entry site as well as deep visceral discomfort, requiring analgesia during the procedure. The objective of this study was to compare the clinical efficacy of Entonox and pethidine for pain relief during outpatient ESWL. We randomized 150 outpatients undergoing elective ESWL into three groups of 50 patients, each group receiving inhalational Entonox, intravenous pethidine, or inhalational compressed air during ESWL. Quantitative evaluation of pain was performed according to a visual analogue scale (VAS), before and after the intervention. Analysis of variance (ANOVA) and paired t tests were used to compare VAS scores in the three groups, before and after the intervention. Entonox and pethidine decreased the pain score significantly, while compressed air did not. There was no significant difference between pain relief by Entonox and pethidine. This study demonstrates for the first time that inhalational Entonox is an effective analgesic regimen for ESWL. Entonox can be regarded as an appropriate alternative to analgesics like opioids in relieving pain during ESWL. PMID:17982746

Mazdak, Hamid; Abazari, Parvaneh; Ghassami, Fatemeh; Najafipour, Shekoofeh

2007-11-03

160

The analgesic effect of inhalational Entonox for extracorporeal shock wave lithotripsy.  

UK PubMed Central (United Kingdom)

Extracorporeal shock wave lithotripsy (ESWL) is a non-invasive procedure that allows urinary stones to be fragmented using acoustic shock waves. The impact of the shock waves causes transient stinging pain at the entry site as well as deep visceral discomfort, requiring analgesia during the procedure. The objective of this study was to compare the clinical efficacy of Entonox and pethidine for pain relief during outpatient ESWL. We randomized 150 outpatients undergoing elective ESWL into three groups of 50 patients, each group receiving inhalational Entonox, intravenous pethidine, or inhalational compressed air during ESWL. Quantitative evaluation of pain was performed according to a visual analogue scale (VAS), before and after the intervention. Analysis of variance (ANOVA) and paired t tests were used to compare VAS scores in the three groups, before and after the intervention. Entonox and pethidine decreased the pain score significantly, while compressed air did not. There was no significant difference between pain relief by Entonox and pethidine. This study demonstrates for the first time that inhalational Entonox is an effective analgesic regimen for ESWL. Entonox can be regarded as an appropriate alternative to analgesics like opioids in relieving pain during ESWL.

Mazdak H; Abazari P; Ghassami F; Najafipour S

2007-12-01

 
 
 
 
161

[Effects of dietary proteins on analgesic activity of tolerance and physical dependence on morphine in rats  

UK PubMed Central (United Kingdom)

Effects of dietary proteins such as casein and egg albumin on analgesic activity of, tolerance to and physical dependence on morphine in rats were examined. There was no difference in analgesic activity after acute administration of morphine 10 mg/kg, s.c. between rats treated with casein food or egg albumin food and normal food for 5 or 21 days. The development of tolerance to morphine analgesia in rats treated with albumin food but not with casein food was suppressed during daily morphine 10 mg/kg, s.c. on 5 consecutive days. Rats were treated with casein or albumin food mixed with morphine (0.5 mg/g of food) for 5 days. Morphine intake in rats treated with albumin food was significantly decreased as compared to that with morphine admixed casein or normal food. Body weight loss by naloxone in morphine-dependent rats was significantly less in both casein food and albumin food groups than in the normal food group. These results suggest that chronic dietary treatment with albumin may produce a partial inhibition of development of tolerance to morphine analgesia and that with casein may attenuate morphine withdrawal manifestation in rats.

Fukagawa Y; Funada M; Mizoguchi H; Narita M; Suzuki T; Misawa M

1992-06-01

162

Anticonvulsant, Analgesic and Hypothermic Effects of Aridanin Isolated from Tetrapleura tetrapetra Fruit in Mice  

Directory of Open Access Journals (Sweden)

Full Text Available Aridanin (an N-acetylglycoside of oleanolic acid) isolated from Tetrapleura tetraptera fruit was investigated for anticonvulsant, analgesic and hypothermic activities in mice. Aridanin at doses of 15 and 30 mg kg-1 by intraperitoneal administration was shown to protect animals in pentylenetetrazole (PTZ)-induced seizure but not in strychnine and picrotoxin induced convulsions. The same dose of aridanin equally decreased rectal temperature and acetic acid-induced writhes in mice. The hypothermic action of aridanin was reversed by pretreatment with cyproheptadine (0.1 mg kg-1), atropine (2 mg kg-1), naltrexone (0.25 mg kg-1), but not with haloperidol (0.1 mg kg-1). The effect on acetic acid-induced writhes was completely blocked by naltrexone, but not by atropine, cyproheptadine and haloperidol. The results suggest that aridanin could be acting as a Central Nervous System (CNS) depressant and that its anticonvulsant property is mediated through the membrane stabilizing property and not through GABA and glycine neurotransmitters respectively. Analgesic and hypothermic actions were mediated through opioids and cholinergic, 5-HT receptors, respectively.

A.O. Aderibigbe; E.O. Iwalewa; S.K. Adesina; A.O. Adebanjo; O.E. Ukponmwan

2007-01-01

163

Topical analgesics in neuropathic pain.  

UK PubMed Central (United Kingdom)

Neuropathic pain can be difficult to treat clinically, as current therapies involve partial effectiveness and significant adverse effects. Following the development of preclinical models for neuropathic pain, significant advances have been made in understanding the neurobiology of neuropathic pain. This includes an appreciation of the molecular entities involved in initiation of pain, the role of particular afferents (small and large diameter, injured and uninjured), and the contribution of inflammation. Currently, topical formulations of capsaicin (cream) and lidocaine (patch) are available for treating neuropathic pain in humans. Preclinical studies provide evidence that peripheral applications of opioids, alpha-adrenergic agents, and antidepressants also may be beneficial in neuropathic pain, and some clinical reports provide support for topical applications of such agents. An appreciation of the ability of drug application, to sites remote from the site of injury, to alleviate aspects of neuropathic pain will provide a significant impetus for the further development of novel topical analgesics for this condition.

Sawynok J

2005-01-01

164

Topical analgesics in neuropathic pain.  

Science.gov (United States)

Neuropathic pain can be difficult to treat clinically, as current therapies involve partial effectiveness and significant adverse effects. Following the development of preclinical models for neuropathic pain, significant advances have been made in understanding the neurobiology of neuropathic pain. This includes an appreciation of the molecular entities involved in initiation of pain, the role of particular afferents (small and large diameter, injured and uninjured), and the contribution of inflammation. Currently, topical formulations of capsaicin (cream) and lidocaine (patch) are available for treating neuropathic pain in humans. Preclinical studies provide evidence that peripheral applications of opioids, alpha-adrenergic agents, and antidepressants also may be beneficial in neuropathic pain, and some clinical reports provide support for topical applications of such agents. An appreciation of the ability of drug application, to sites remote from the site of injury, to alleviate aspects of neuropathic pain will provide a significant impetus for the further development of novel topical analgesics for this condition. PMID:16178758

Sawynok, Jana

2005-01-01

165

Effects of topical analgesics on the pressor response evoked by muscle afferents.  

UK PubMed Central (United Kingdom)

PURPOSE: Pressor responses are reflexly evoked by the activation of groups III and IV muscle afferents, which are also known to mediate nociceptive responses. In this experiment, the effects of analgesic balm (AB) application on these responses were investigated without the interference of other types of anesthesia or effects from the higher brain. METHODS: Heart rate (HR), blood pressure, and end-tidal CO(2) were monitored in midcollicularly decerebrated cats. Static contractions (30 s) of hindlimb muscles were evoked by electric stimulation of L7 and S1 ventral roots. After control runs, a commercial AB (1% capsaicin, 12.5% methyl salicylate) was applied to the skin surface over the contracting muscles. Muscle contractions were evoked every 10 min, alternating between the two hindlimbs. RESULTS: Changes in mean arterial pressure (MAP) evoked by static ipsilateral muscular contraction were significantly attenuated 20 min and 40 min after AB application. The decreases in the pressor response were significant at both the initial and the last parts of the stimulus intervention after 20 min of AB application. There were no significant changes in the response to contraction of the hindlimb contralateral to the AB application. Application of AB to the contralateral leg did not add to the ipsilateral effects. CONCLUSIONS: AB application to the skin surface over contracting muscles significantly decreased autonomic responses to static muscular contraction. This effect was independent of higher cortical processing and strongly suggests that application of methyl salicylate and capsaicin on the skin has analgesic effects on signals from receptors located in muscle.

Ichiyama RM; Ragan BG; Bell GW; Iwamoto GA

2002-09-01

166

Study of interaction between opioid and ?-2 adrenergic systems in analgesic effect of oxytocin in locus coeruleus nucleus  

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Introduction: Oxytocin is a active neuropeptide of central nervous system. In this study the effects of naloxone (opioid receptor antagonist) and yohimbine (?-2 adrenergic receptor antagonist) on analgesic effect of oxytocin applied into the locus coeruleus (LC) nucleus were investigated. Methods: A...

Nasrin haghighi; Mahnaz Kessmati; Hadi fathi Moghadam2

167

Analgesic Effect of Meloxicam in Canine Acute Dermatitis – a Pilot Study  

Directory of Open Access Journals (Sweden)

Full Text Available A double-blind trial was performed on 12 client-owned dogs suffering from acute and painful dermatitis. Clinically these cases represented pyotraumatic dermatitis and pyotraumatic folliculitis. Six dogs were injected with meloxicam and 6 were given placebo. Signs of pain were recorded on a visual analogue scale before administering the drug. This was repeated over the following 2–3 days. All dogs were treated with cephalexin orally. Six dogs given meloxicam and cephalexin showed an average decrease of pain on day 2 of 28.3%, whereas the 6 dogs given placebo and cephalexin showed an average decrease of pain on day 2 of 8.3%. When compared in the Wilcoxon two-sample test, using change in percent and absolute change, the 2 groups yielded p = 0.026 and p = 0.064 respectively. These findings indicate that meloxicam has an analgesic effect on acute dermatitis in dogs.

Höglund O Viking; Frendin J

2002-01-01

168

Assessing the Analgesic Effects of Sucrose to Cold Pressor Pain in Human Adults  

Directory of Open Access Journals (Sweden)

Full Text Available Previous studies report that the ingestion of highly concentrated sweet solutions produces a morphine-like analgesia in rats, human infants, and in adult males. To determine whether sweet-induced analgesia occurs with more commonly consumed substances, 30 adult males (Mage = 22.4 years) were exposed to a cold pressor test and pain responsivity was assessed both before and after consuming either an 8% sucrose solution, water, or nothing. Between-groups comparisons revealed that relative to the Sucrose or Nothing groups, the Water group showed increased pain tolerance. Neither pain thresholds nor ratings of pain intensity and unpleasantness on a visual analogue scale differed among groups. The results support previous findings in both humans and animals that the palatability or hedonic value of food or drink may be the key predictor of its analgesic effect.

Michele E. Mercer; Mark D. Holder

2013-01-01

169

Does transcutaneous electrical nerve stimulation (TENS) have a clinically relevant analgesic effect on different pain conditions? A literature review  

Directory of Open Access Journals (Sweden)

Full Text Available Transcutaneous electric nerve stimulation (TENS) is a standard therapy used in different painful conditions such as low back pain, diabetic polyneuropathy or arthrosis. However, literature reviews focusing on the effects and the clinical implication of this method in various painful conditions are yet scarce. The purpose of this literature research was to determine, whether TENS provides an analgesic effect on common painful conditions in clinical practice. Literature research was performed using three data bases (Pubmed, Embase, Cochrane Database), focusing on papers published in the space of time from 2007 to 2012. Papers were evaluated from two reviewers independently concerning the clinical outcome, taking account for the level of external evidence according to the German Cochrane levels of evidence (Ia – IV). 133 papers of varying methodological quality dealing with different painful conditions were selected in total. A clinically relevant analgesic effect was described in 90 painful conditions (67%). In 30 painful states (22%), the outcome was inconclusive due to the study design. No significant analgesic effect of TENS was observed in 15 painful conditions (11%). The vast majority of the papers were classified as Cochrane evidence level Ib (n = 64; 48%), followed by level Ia (n = 23; 17%), level III (n = 18; 14%), level IV (n = 15; 11%), level IIb (n = 10; 8%) and level IIa (n = 3; 2%). Most of the studies revealed an analgesic effect in various painful conditions, confirming the usefulness of TENS in clinical practice.

Asami Naka; Mohammed Keilani; Stefan Loefler; Richard Crevenna

2013-01-01

170

Non-analgesic effects of opioids: opioid-induced respiratory depression.  

UK PubMed Central (United Kingdom)

Opioids induce respiratory depression via activation of ?-opioid receptors at specific sites in the central nervous system including the pre-Bötzinger complex, a respiratory rhythm generating area in the pons. Full opioid agonists like morphine and fentanyl affect breathing with onset and offset profiles that are primarily determined by opioid transfer to the receptor site, while the effects of partial opioid agonists such as buprenorphine are governed by transfer to the receptor site together with receptor kinetics, in particular dissociation kinetics. Opioid-induced respiratory depression is potentially fatal but may be reversed by the opioid receptor antagonist naloxone, an agent with a short elimination half-life (30 min). The rate-limiting factor in naloxone-reversal of opioid effect is the receptor kinetics of the opioid agonists that requires reversal. Agents with slow dissociation kinetics (buprenorphine) require a continuous naloxone infusion while agents with rapid kinetics (fentanyl) will show complete reversal upon a single naloxone dose. Since naloxone is non-selective and will reverse analgesia as well, efforts are focused on the development of compounds that reverse opioid-induced respiratory depression without affecting analgesic efficacy. Such agents include ampakines and serotonin agonists which are aimed at selectively enhancing central respiratory drive. A novel approach is aimed at the reduction of respiratory depression from opioid-activation of (micro-)glia cells in the pons and brainstem using micro-glia cell stabilizers. Since this approach simultaneously enhances opioid analgesic efficacy it seems an attractive alternative to the classical reversal strategies with naloxone.

Boom M; Niesters M; Sarton E; Aarts L; Smith TW; Dahan A

2012-01-01

171

Analgesic Effect of Chronic Oral Administration of Nigella Sativa Seeds in Diabetic Rats  

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Full Text Available Introduction: Hyperalgesia is considered as one the marked signs of subchronic diabetes mellitus that could affect the life style of patients. Considering the evidence on the antidiabetic and analgesic effects of Nigella sativa (NS), this study was designed to investigate the analgesic effects of NS on formalin-induced nociceptive responses (standard formalin test) in streptozotocin (STZ)-induced diabetic rats. Methods: In this experimental study, male rats (n = 60) were randomly divided into control, NS-treated control, diabetic, sodium salicylate (SS)-treated diabetic, and NS-treated diabetic groups. For induction of diabetes, streptozotocin was used at a single dose. The treatment groups received oral administration of NS seed-mixed pelleted food (6.25%) for two months. Results: Diabetic rats exhibited a higher score of pain at both phases of the formalin test (p = 0.031 and p = 0.034 respectively) and NS-treated diabetic rats exhibited a lower nociceptive score as compared to untreated-diabetic ones at both acute and chronic phases (p = 0.008 and p = 0.009 respectively). Meanwhile, SS administration significantly reduced pain score only during the chronic phase of the test (p = 0.009). On the other hand, NS administration in control rats caused a lower nociceptive score as compared to untreated controls (p= 0.046 and p = 0.039). Conclusion: Two-month oral administration of NS seeds can attenuate nociceptive scores in an experimental model of diabetes mellitus and therefore could be considered as a potential treatment for painful diabetic neuropathy

M Roghani; T Baluchnejadmojarad; M Sajadi; E Kavandi; F Kargar-sharif

2006-01-01

172

Anti-Inflammatory and Analgesic Effects of Leaf Extracts of Hibiscus Populnea Linn.  

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Full Text Available Hibiscus populnea or Indian Tulip Tree or Pacific Rosewood, has been traditionally used for thetreatment of many diseases including inflammatory conditions. A number of chemical constituentsnamely, thespesin, gossypol, DL-gossypol, populnin, populneol, glycosides of quercetin, epoxylic acid,rutin, kaemferol-3-flucoside, lupenone, mansonone, myricyl alcohol, lipids and ? sitosterol have beenisolated from the plant. Many of these compounds are proved to have the claimed activities. But nowork has been specifically carried out to establish the anti inflammatory effects of the ripe and olderleaves. Hence in the present study an attempt was made, with the leaves, for the phytochemicalscreening of the methanol, pet. ether and aqueous extracts along with their anti-inflammatory andanalgesic potential also. In order to study the anti-inflammatory effects, dextran-induced paw edemamethod and carrageenan - induced paw edema methods were used. Similarly analgesic activity wastested using acetic acid writhing. Anti arthritic study was also tried. Regarding carrageenan- inducedpaw edema, the level of activity of the petroleum ether extract was less than that of the reference drugand the methanolic extract exhibited the most potent inhibitory activity. But the activity of the aqueousextract was more than that of Indomethacin. From the results of the experimentally induced arthriticstudy it was seen that the activity of the petroleum ether extract was quite stable throughout the period ofassay where as the methanolic extract was proved to be more active against the chronic phase thanagainst the acute phase. The aqueous extract was seen to be a very potent anti inflammatory agentagainst both phases of the inflammatory process with more or less the same activity as that ofindomethacin, the reference standard. The analgesic activities of aqueous and methanolic extracts werefound to be very significant (P < 0.001).

Hareeshbabu E; Molly Mathew

2013-01-01

173

A comparison of the analgesic effects of butorphanol with those of meloxicam after elective ovariohysterectomy in dogs  

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This study was designed to compare the analgesic effects of butorphanol with those of meloxicam following ovariohysterectomy. Fifteen dogs were premedicated with 0.05 mg/kg body weight (BW) of acepromazine by intramuscular (IM) injection, plus 0.2 mg/kg BW of meloxicam by subcutaneous (SC) injection...

Caulkett, Nigel; Read, Matt; Fowler, David; Waldner, Cheryl

174

Analgesic, Antipyretic and Anti-inflammatory Effect of the Whole Plant Extract of Desmostachya bipinnata Stapf (Poaceae) in Albino Rats  

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Analgesic, Antipyretic and anti-inflammatory effect of petroleum ether, benzene chloroform, ethanol and aqueous extract of the whole parts of Desmostachya b...

Somezeet Panda1*, N. S. K Choudhury 2, V. Jagannath Patro3 Dipti Kanta Pradhan, Goutam Kumar Jana1

175

Electroencephalography and analgesics.  

UK PubMed Central (United Kingdom)

AIMS: To assess centrally mediated analgesic mechanisms in clinical trials with pain patients, objective standardized methods such as electroencephalography (EEG) has many advantages. The aim of this review is to provide the reader with an overview of present findings in analgesics assessed with spontaneous EEG and evoked brain potentials (EPs) in humans. Furthermore, EEG methodologies will be discussed with respect to translation from animals to humans and future perspectives in predicting analgesic efficacy. METHODS: We searched PubMed with MeSH terms "analgesics", "electroencephalography" and "evoked potentials" for relevant articles. Combined with a search in their reference lists 15 articles on spontaneous EEG and 55 papers on EPs were identified. RESULTS: Overall, opioids produced increased activity in the delta band in the spontaneous EEG, but increases in higher frequency bands were also seen. The EP amplitudes decreased in the majority of studies. Anticonvulsants used as analgesics showed inconsistent results. The N-Methyl-D-aspartate receptor antagonist ketamine showed an increase in the theta band in spontaneous EEG and decreases in EP amplitudes. Tricyclic antidepressants increased the activity in the delta, theta and beta bands in the spontaneous EEG while EPs were inconsistently affected. Weak analgesics were mainly investigated with EPs and a decrease in amplitudes was generally observed. CONCLUSIONS: This review reveals that both spontaneous EEG and EPs are widely used as biomarkers for analgesic drug effects. Methodological differences are common and a more uniform approach will further enhance the value of such biomarkers for drug development and prediction of treatment response in individual patients.

Malver LP; Brokjaer A; Staahl C; Graversen C; Andresen T; Drewes AM

2013-04-01

176

Effects of various analgesics on the level of prostaglandin E2 during orthodontic tooth movement.  

UK PubMed Central (United Kingdom)

AIM:The aim of this double-blind, randomized, placebo-controlled clinical study was to evaluate the analgesic effects of preoperative/postoperative ibuprofen and acetaminophen use after bonding and to find a relation between the pain level and the amount of prostaglandin released.MATERIALS AND METHODS:Forty-eight patients were included and randomly divided to three equal groups that received either ibuprofen, acetaminophen or placebo for pain relief. The pain levels were measured before bonding, after bonding, at first, second, third, and seventh days on a 100mm visual analogue scale (VAS) and gingival crevicular fluid (GCF) samples were collected at the same time intervals to measure the amount of prostaglandin E2 (PGE2) released. PGE2 levels were determined with ELISA test. The results were evaluated with Wilcoxon and Kruskal-Wallis tests with Bonferroni correction.RESULTS:Acetaminophen and placebo groups showed similar pain levels during the first 2 days, whereas ibuprofen group showed lower pain levels during the first day after bonding. PGE2 levels did not show statistically significant difference in time within the analgesic groups. No significant relation between the pain perceived and PGE2 released was found.LIMITATIONS:The biggest limitation of this study is the subjective nature of pain and its method of evaluation.CONCLUSIONS:The perception of pain by patients taking ibuprofen and acetaminophen at pre/post appliance placement was not different from patients taking placebo. No time-related differences in PGE2 level were found between the groups and no significant correlation was found between the perception of pain and PGE2 levels.

Tunçer Z; Polat-Ozsoy O; Demirbilek M; Bostanoglu E

2013-07-01

177

B-vitamin mixture improves the analgesic effect of diclofenac in patients with osteoarthritis: a double blind study.  

UK PubMed Central (United Kingdom)

According to the high consumption of the mixture of B vitamins and diclofenac in several countries, this combination has constituted a frequently used option in pain therapy from inflammatory origin. Although the evidence obtained from inflammatory pain animal models has shown the existence of analgesic synergy between diclofenac and the B vitamins mixture, the corresponding clinical evidence is scarce. A double-blind, randomized clinical trial study was designed to characterize the analgesic effect and safety of diclofenac and B vitamins against diclofenac alone in patients with severe osteoarthritis. Forty eight patients programmed to total knee arthroplasty with a pain level ?7 in a 1-10 cm visual analogue scale were allocated to receive a single intramuscular injection of sodium diclofenac (75 mg) alone or combined with thiamine (100 mg), pyridoxine (100 mg) and cyanocobalamin (5 mg), and the pain level was evaluated during 12 h post-injection. Diclofenac+B vitamins mixture showed a superior analgesic effect during the assessed period and also a better assessment of the pain relief perception by patients than diclofenac alone. This study constitutes a clinical support on the improvement of the analgesic effect of diclofenac by B vitamins in patients with osteoarthritis programmed to total knee arthroplasty, as a clinical model of inflammatory pain.

Magańa-Villa MC; Rocha-González HI; Fernández del Valle-Laisequilla C; Granados-Soto V; Rodríguez-Silverio J; Flores-Murrieta FJ; Carrasco-Portugal MC; Reyes-García JG

2013-06-01

178

Analgesic effects and anti-inflammatory properties of the crude methanolic extract of Schwenckia americana Linn (Solanaceae).  

UK PubMed Central (United Kingdom)

AIM OF THE STUDY: To evaluate analgesic effect and anti-inflammatory properties of Schwenckia americana (Solanaceae), a medicinal plant used for treating rheumatic pains and swelling in North-western Nigeria. MATERIALS AND METHODS: Three doses (25mg/kg, 50mg/kg and 100mg/kg) of the crude methanolic extract of Schwenkia americana were evaluated for analgesic and anti-inflammatory activities using acetic acid induced writhing test, formalin induced nociception, and formalin induced hind paw oedema in rats. RESULTS: All doses (25, 50, 100mg/kg) of the extract tested were effective. The extract at the tested doses produced a percentage inhibition of the acetic acid induced abdominal constriction of (53.3, 58.0 and 86.7%), respectively. A percentage inhibition of the formalin induced nociception of 44.00, 56.04, and 56.04% (early phase) and 33.00, 36.63 and 59.71% (late phase) was also produced. The inhibition of oedema formation increased with increasing dosage from 25 to 100mg/kg. The crude extract produced a statistically significant analgesic and anti-inflammatory activity comparable to the effect of standard drug (10mg/kg Piroxicam). CONCLUSION: This study demonstrated the potential analgesic and anti-inflammatory properties of crude methanolic extract of Schwenkia americana thus justifying its traditional usage.

Jimoh AO; Chika A; Umar MT; Adebisi I; Abdullahi N

2011-09-01

179

B-vitamin mixture improves the analgesic effect of diclofenac in patients with osteoarthritis: a double blind study.  

Science.gov (United States)

According to the high consumption of the mixture of B vitamins and diclofenac in several countries, this combination has constituted a frequently used option in pain therapy from inflammatory origin. Although the evidence obtained from inflammatory pain animal models has shown the existence of analgesic synergy between diclofenac and the B vitamins mixture, the corresponding clinical evidence is scarce. A double-blind, randomized clinical trial study was designed to characterize the analgesic effect and safety of diclofenac and B vitamins against diclofenac alone in patients with severe osteoarthritis. Forty eight patients programmed to total knee arthroplasty with a pain level ?7 in a 1-10 cm visual analogue scale were allocated to receive a single intramuscular injection of sodium diclofenac (75 mg) alone or combined with thiamine (100 mg), pyridoxine (100 mg) and cyanocobalamin (5 mg), and the pain level was evaluated during 12 h post-injection. Diclofenac+B vitamins mixture showed a superior analgesic effect during the assessed period and also a better assessment of the pain relief perception by patients than diclofenac alone. This study constitutes a clinical support on the improvement of the analgesic effect of diclofenac by B vitamins in patients with osteoarthritis programmed to total knee arthroplasty, as a clinical model of inflammatory pain. PMID:23526240

Magańa-Villa, M C; Rocha-González, H I; Fernández del Valle-Laisequilla, C; Granados-Soto, V; Rodríguez-Silverio, J; Flores-Murrieta, F J; Carrasco-Portugal, M C; Reyes-García, J G

2013-03-22

180

The analgesic effect of pregabalin in chronic pain patients is reflected by changes in pharmaco-EEG spectral indices  

DEFF Research Database (Denmark)

What this paper adds What is already known about this subject • Pregabalin is an anticonvulsive agent prescribed as a secondary analgesic for patients when standard pain treatment is insufficient. • The analgesic effect resides to the central nervous system. • The central analgesic effect can be evaluated by electroencephalographic. What this study adds • The analgesic effect of pregabalin is reflected as a slowing of brain oscillations. • The slowing of brain oscillations for each individual patient is correlated to subjective pain scores. • The developed methodology may be used as a mechanistic approach to monitor the analgesic effect of pregabalin in pharmacological studies. SUMMARY: Aim: To identify electroencephalographic (EEG) biomarkers for the analgesic effect of pregabalin in patients with chronic visceral pain. Methods: This was a double-blind, placebo-controlled study in thirty-one patients suffering from visceral pain due to chronic pancreatitis. Patients received increasing doses of pregabalin (75mg-300mg twice a day) or matching placebo during 3 weeks of treatment. Pain scores were documented in a diary based on the visual analogue scale. In addition, brief pain inventory-short form (BPI) and quality of life questionnaires were collected prior to and after the study period. Multi-channel resting EEG was recorded before treatment onset and at the end of the study. Changes in EEG spectral indices were extracted, and individual changes were classified by a support vector machine (SVM) to discriminate the pregabalin and placebo responses. Changes in individual spectral indices and pain scores were correlated. Results: Pregabalin increased normalized intensity in low spectral indices, most prominent in the theta band (3.5-7.5Hz), difference of -3.18, 95%CI -3.57, -2.80; P = 0.03. No changes in spectral indices were seen for placebo. The maximum difference between pregabalin and placebo treated patients were seen in the parietal region, with a classification accuracy of 85.7% (P = 0.009). Individual changes in EEG indices were correlated to changes in pain diary (P = 0.04) and BPI pain composite scores (P = 0.02). Conclusions: Changes in spectral indices caused by slowing of brain oscillations were identified as a biomarker for the central analgesic effect of pregabalin. The developed methodology may provide perspectives to assess individual responses to treatment in personalized medicine.

Gravesen, Carina; Olesen, SŘren S

2012-01-01

 
 
 
 
181

Effects of histamine on spontaneous neuropathic pain induced by peripheral axotomy.  

UK PubMed Central (United Kingdom)

The present study was designed to investigate the effects of histamine on spontaneous neuropathic pain (NP) induced by peripheral axotomy. Rats and mice were subjected to complete transection of the left sciatic and saphenous nerves to induce spontaneous NP (the neuroma model). Rats were then treated with drugs once daily for 30 days (histidine and loratadine, i.p.) or 21 days (histamine, i.c.v.). Autotomy behavior was scored daily until day 50 post-operation (PO). On days 14 to 21 PO, some rats in the control group were subjected to single-fiber recording. Autotomy behavior was also monitored daily in histidine decarboxylase (the key enzyme for histamine synthesis) knockout (HDC(-/-)) and wild-type mice for 42 days. We found that both histidine (500 mg/kg) (a precursor of histamine that increases histamine levels in the tissues) and histamine (50 ?g/5 ?L) significantly suppressed autotomy behavior in rats. HDC(-/-) mice lacking endogenous histamine showed higher levels of autotomy than the wild-type. In addition, the analgesic effect of histidine was not antagonized by loratadine (a peripherally-acting H1 receptor antagonist), while loratadine alone significantly suppressed autotomy. Electrophysiological recording showed that ectopic spontaneous discharges from the neuroma were blocked by systemic diphenhydramine (an H1 receptor antagonist). Our results suggest that histamine plays an important role in spontaneous NP. It is likely that histamine in the central nervous system is analgesic, while in the periphery, via H1 receptors, it is algesic. This study justifies the avoidance of a histamine-rich diet and the use of peripherally-acting H1 receptor antagonists as well as agents that improve histamine action in the central nervous system in patients with spontaneous NP.

Yu J; Lou GD; Yue JX; Tang YY; Hou WW; Shou WT; Ohtsu H; Zhang SH; Chen Z

2013-06-01

182

Effects of histamine on spontaneous neuropathic pain induced by peripheral axotomy.  

Science.gov (United States)

The present study was designed to investigate the effects of histamine on spontaneous neuropathic pain (NP) induced by peripheral axotomy. Rats and mice were subjected to complete transection of the left sciatic and saphenous nerves to induce spontaneous NP (the neuroma model). Rats were then treated with drugs once daily for 30 days (histidine and loratadine, i.p.) or 21 days (histamine, i.c.v.). Autotomy behavior was scored daily until day 50 post-operation (PO). On days 14 to 21 PO, some rats in the control group were subjected to single-fiber recording. Autotomy behavior was also monitored daily in histidine decarboxylase (the key enzyme for histamine synthesis) knockout (HDC(-/-)) and wild-type mice for 42 days. We found that both histidine (500 mg/kg) (a precursor of histamine that increases histamine levels in the tissues) and histamine (50 ?g/5 ?L) significantly suppressed autotomy behavior in rats. HDC(-/-) mice lacking endogenous histamine showed higher levels of autotomy than the wild-type. In addition, the analgesic effect of histidine was not antagonized by loratadine (a peripherally-acting H1 receptor antagonist), while loratadine alone significantly suppressed autotomy. Electrophysiological recording showed that ectopic spontaneous discharges from the neuroma were blocked by systemic diphenhydramine (an H1 receptor antagonist). Our results suggest that histamine plays an important role in spontaneous NP. It is likely that histamine in the central nervous system is analgesic, while in the periphery, via H1 receptors, it is algesic. This study justifies the avoidance of a histamine-rich diet and the use of peripherally-acting H1 receptor antagonists as well as agents that improve histamine action in the central nervous system in patients with spontaneous NP. PMID:23494529

Yu, Jie; Lou, Guo-Dong; Yue, Jia-Xing; Tang, Ying-Ying; Hou, Wei-Wei; Shou, Wen-Ting; Ohtsu, Hiroshi; Zhang, Shi-Hong; Chen, Zhong

2013-03-13

183

PK20, a new opioid-neurotensin hybrid peptide that exhibits central and peripheral antinociceptive effects  

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Full Text Available Abstract Background The clinical treatment of various types of pain relies upon the use of opioid analgesics. However most of them produce, in addition to the analgesic effect, several side effects such as the development of dependence and addiction as well as sedation, dysphoria, and constipation. One solution to these problems are chimeric compounds in which the opioid pharmacophore is hybridized with another type of compound to incease antinociceptive effects. Neurotensin-induced antinociception is not mediated through the opioid system. Therefore, hybridizing neurotensin with opioid elements may result in a potent synergistic antinociceptor. Results Using the known structure-activity relationships of neurotensin we have synthesized a new chimeric opioid-neurotensin compound PK20 which is characterized by a very strong antinociceptive potency. The observation that the opioid antagonist naltrexone did not completely reverse the antinociceptive effect, indicates the partial involvement of the nonopioid component in PK20 in the produced analgesia. Conclusions The opioid-neurotensin hybrid analogue PK20, in which opioid and neurotensin pharmacophores overlap partially, expresses high antinociceptive tail-flick effects after central as well as peripheral applications.

Kleczkowska Patrycja; Kosson Piotr; Ballet Steven; Van den Eynde Isabelle; Tsuda Yuko; Tourwé Dirk; Lipkowski Andrzej W

2010-01-01

184

Analgesic effects of morphine and loperamide in the rat formalin test: interactions with NMDA receptor antagonists.  

Science.gov (United States)

To reveal peripheral components of opiate analgesia, effects of loperamide, opioid agonist which does not penetrate the blood-brain barrier, were examined in formalin and acute thermal pain tests in comparison with morphine. Formalin administration induces pain behaviour such licking/biting of injected paw expressed as two phases. The first phase is caused by C-fibre activation due to peripheral stimulation, the second phase attributed to ongoing input from peripheral site, leading to spinal hyperexcitability, which is dependent on N-methyl-D-aspartate (NMDA) receptor activation. Loperamide (3-10 mg/kg) and morphine (6 mg/kg) reduced formalin-induced nociceptive behaviours and these effects were reversed by naloxone methiodide (0.03-10 mg/kg), opioid receptor antagonist which poorly penetrates the blood-brain barrier. Loperamide action was enhanced only by centrally active NMDA receptor antagonists memantine (3 mg/kg) and CGP 37849 (3 mg/kg), but not by NMDA/glycineB receptor antagonists showing weak or no central nervous system (CNS) activity. Present results suggest that central NMDA receptor blockade may be necessary to enhance analgesia induced through peripheral opioid mechanisms in formalin-evoked nociception. PMID:16297905

Sevostianova, Natalja; Danysz, Wojciech; Bespalov, Anton Y

2005-11-17

185

Nonopioid and adjuvant analgesics in chronic pain management: strategies for effective use.  

UK PubMed Central (United Kingdom)

Nonopioid and adjuvant analgesics encompass a huge range of heterogenous drugs that differ chemically and mechanistically. These drugs generally are prescribed for mild-to-moderate pain, as coanalgesics for severe pain, or to target specific pain-generating mechanisms. This article provides an overview of some of the more commonly used nonopioid and adjuvant analgesics used to treat chronic pain, including salicylates, acetaminophen, nonsteroidal anti-inflammatory drugs, tricyclic antidepressants, anticonvulsants, N-Methyl-D-Aspartate receptor antagonists, lidocaine, skeletal muscle relaxants, and topical analgesics.

Gordon DB

2003-09-01

186

Nonopioid and adjuvant analgesics in chronic pain management: strategies for effective use.  

Science.gov (United States)

Nonopioid and adjuvant analgesics encompass a huge range of heterogenous drugs that differ chemically and mechanistically. These drugs generally are prescribed for mild-to-moderate pain, as coanalgesics for severe pain, or to target specific pain-generating mechanisms. This article provides an overview of some of the more commonly used nonopioid and adjuvant analgesics used to treat chronic pain, including salicylates, acetaminophen, nonsteroidal anti-inflammatory drugs, tricyclic antidepressants, anticonvulsants, N-Methyl-D-Aspartate receptor antagonists, lidocaine, skeletal muscle relaxants, and topical analgesics. PMID:14567202

Gordon, Debra B

2003-09-01

187

[Metamizol--a new effective analgesic with a long history. Overview of its pharmacology and clinical use  

UK PubMed Central (United Kingdom)

Metamizol is an effective, non-opioid analgesics which was originally introduced to the therapy in the year 1922. However, with the reference to the side effects of other related pyrazolone derivatives its administration, similarly as the usage of other pyrazolones, was significantly limited. Later, metamizol has been used, usually mixed, with spasmolytic agents and quite recently it has been introduced as a mono-component medicament. Metamizol proved to be a very effective analgesic. When administered in equipotent doses, it had its effects comparable to various opioid analgesics, such as tramadol, pentazocine and pethidine. Beside the strong analgesic effect, it produces also significant antipyretic and splasmolytic effects without the adverse, unpleasant anticholinergic impact. Its spasmolytic effect on the smooth muscle of the sphincter Oddi, urinary tract, and the gal bladder is comparable to the effects of buthylscopolamine. Unlike aspirin and other nonsteroidal antiinflammatory drugs it has, however, no antiinflammatory activity when administered in clinical doses. Similarly, metamizol has no effect on the CNS, cardiovascular system, renal and metabolic functions. On the other hand, metamizol, like aspirin, has got a significant effect on the aggregation of platelets. Metamizol is basically a prodrug. The parent substance is not effective before its conversion into two active metabolites (4-methylaninoantipyrine and 4-aminoantipyrine) in the body. Metamizol is well absorbed from the small intestine but only two above mentioned active metabolites and no parent drug can be detected in the blood. The active metabolites are consequently metabolised to ineffective metabolites including the relevant acetylderivatives, in which the acetylation phenotypes can be distinguished. In the therapy, metamizol can be used, as an analgesic, at post-surgical pain, patient's controlled analgesia (PCA), at the cancer's pain and in the pains of different origin (post-traumatic pain, the pain at myocardial infarction, craniocerebral trauma, and the invasive diagnostic interventions), as well as at he pain of neuromuscular origin, headache and migraine. Its spasmolytic effect in connection with a strong analgesic activity is very useful at various colic attacks. Further, metamizol is a useful antipyretic both in the adults and children. Its adverse effects are not pronounced and drug interactions are minimal. Only when metamizol is administered together with cyclosporine, the blood levels of the last substance should be regularly checked.

Fendrich Z

2000-07-01

188

Tapentadol hydrochloride: A novel analgesic  

Science.gov (United States)

Tapentadol is a novel, centrally acting analgesic with dual mechanism of action, combining mu-opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule. It has an improved side effect profile when compared to opioids and nonsteroidal anti-inflammatory drugs. The dual mechanism of action makes Tapentadol a useful analgesic to treat acute, chronic, and neuropathic pain.

Singh, Dewan Roshan; Nag, Kusha; Shetti, Akshaya N.; Krishnaveni, N.

2013-01-01

189

Tapentadol hydrochloride: A novel analgesic.  

UK PubMed Central (United Kingdom)

Tapentadol is a novel, centrally acting analgesic with dual mechanism of action, combining mu-opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule. It has an improved side effect profile when compared to opioids and nonsteroidal anti-inflammatory drugs. The dual mechanism of action makes Tapentadol a useful analgesic to treat acute, chronic, and neuropathic pain.

Singh DR; Nag K; Shetti AN; Krishnaveni N

2013-07-01

190

An update on analgesics.  

Science.gov (United States)

Recent introduction of new analgesics into the clinic is best described as a slow process with activity classified into two main areas: improving analgesic efficacy/potency and reducing side-effect profile. This review article describes some of the recent advances with an emphasis on use in the acute setting. In this respect, opioids continue to be the mainstay (but not the only) analgesic and there have been important improvements in their clinical effect profile. For example, tapentadol has been introduced as a mixed opioid and norepinephrine uptake inhibitor which, unlike tramadol, does not require metabolic activation and does not suffer from isomer-dependent pharmacodynamics. Opioid antagonists have received much attention recently either used alone, methylnaltrexone (s.c) or alvimopan (p.o), or in combination, Targinact (oxycodone/naloxone), and appear to be effective in reducing opioid side-effects such as those in the gastrointestinal tract. Other agents where there has been recent development include the use of gabapentin, methylxanthines, and local anaesthetics. An interesting area of translation of basic research is in the inhibition of breakdown of endogenous opioids with opiorphin, targeting of the endocannabinoid system, and the use of ampakines to obtund opioid-induced side-effects. It is clear that there is still much work to be done, but the need for highly efficacious analgesics with good side-effect profile remains. PMID:21624966

Power, I

2011-05-30

191

An update on analgesics.  

UK PubMed Central (United Kingdom)

Recent introduction of new analgesics into the clinic is best described as a slow process with activity classified into two main areas: improving analgesic efficacy/potency and reducing side-effect profile. This review article describes some of the recent advances with an emphasis on use in the acute setting. In this respect, opioids continue to be the mainstay (but not the only) analgesic and there have been important improvements in their clinical effect profile. For example, tapentadol has been introduced as a mixed opioid and norepinephrine uptake inhibitor which, unlike tramadol, does not require metabolic activation and does not suffer from isomer-dependent pharmacodynamics. Opioid antagonists have received much attention recently either used alone, methylnaltrexone (s.c) or alvimopan (p.o), or in combination, Targinact (oxycodone/naloxone), and appear to be effective in reducing opioid side-effects such as those in the gastrointestinal tract. Other agents where there has been recent development include the use of gabapentin, methylxanthines, and local anaesthetics. An interesting area of translation of basic research is in the inhibition of breakdown of endogenous opioids with opiorphin, targeting of the endocannabinoid system, and the use of ampakines to obtund opioid-induced side-effects. It is clear that there is still much work to be done, but the need for highly efficacious analgesics with good side-effect profile remains.

Power I

2011-07-01

192

Postoperative Analgesic Effects of Carprofen Following Osteotomy and Laparotomy in Dogs  

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Full Text Available This study investigated the effects of postoperative pain following soft and hard tissue operations in dogs on Adrenocorticotrophic Hormone (ACTH) levels, dopamine levels, haemocoel values and blood gases. It also evaluated the results of the applied treatments. The study was carried out in 4 groups each comprising 6 dogs. Dogs in the 1st and 3rd groups underwent laparotomy and those in the 2nd and 4th groups underwent osteotomy. Carprofen (4.4 mg kg-1) (Rimadyl, Pfizer) was administered subcutaneously as an analgesic to the dogs in the 1st and 2nd groups following the operation. Venous blood samples were collected from the animals before the operation and in the subsequent hours to determine the ACTH and dopamine levels. In the postoperative period, ACTH and dopamine levels were significantly higher in the groups that underwent osteotomy than in the groups that underwent laparotomy (p<0.05). Statistically significant decreases were observed in the groups that received analgesia after the 2nd h (p<0.05). In this study, effective postoperative analgesia is required after both soft and hard tissue operations. Furthermore, effective and rapid implementation of the process is important for postoperative animal welfare and rapid return to normal physiological functions.

Muharrem Erol; Celal Izci

2011-01-01

193

Paroxetine Augments while Naloxone Abolishes the Analgesic Effect of Paracetamol in Acute Nociceptive Pain in Mice  

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Full Text Available The mechanism(s) of analgesic action of paracetamol (acetaminophen; N-acetyl-p-aminophenol) remains controversial. Previous studies on rats suggested that the antinociceptive action of paracetamol might involve the central descending inhibitory pain pathways recruiting both a serotoninergic and an opioidergic system. This study explores this issue in mice using paroxetine, the most potent selective serotonin re-uptake inhibitor, and the nonselective opioid pure antagonist naloxone. Animals were divided into two main groups for two separate experiments, each subdivided into 3 subgroups. In both experiments; the first group served as control, the second group received paracetamol (200 mg/kg, i.p). In one experiment, the third group received paroxetine (20 mg/kg p.o for 7 days) before paracetamol. In the other experiment, animals of the third group were pretreated with naloxone (5 mg/kg, i.p) 30 min before paracetamol. The antinociceptive effect of paracetamol was tested using the hot plate test. Paracetamol displayed a significant antinociceptive activity that was augmented by pretreatment with paroxetine as was shown by maintenance of its effect beyond that shown by paracetamol alone. On the other hand, pretreatment with naloxone abolished paracetamol’s antinociceptive activity in the hot-plate test. These results extended the previous observation in rats that the antinociceptive effect of paracetamol involved activation of a central descending pain inhibitory pathway with serotonin and opioidergic peptides being potential mediators recruited.

Mohammad Raafat Abdalla; Waleed Al Malki; Muhammad Ahmed

2013-01-01

194

Effects of peripherally restricted ? opioid receptor agonists on pain-related stimulation and depression of behavior in rats.  

Science.gov (United States)

? opioid receptor agonists that do not readily cross the blood-brain barrier are peripherally restricted and distribute poorly to the central nervous system after systemic administration. Peripherally restricted ? agonists have promise as candidate analgesics, because they may produce antinociception mediated by peripheral ? receptors more potently than they produce undesirable sedative and psychotomimetic effects mediated by central ? receptors. The present study used assays of pain-related stimulation and depression of behavior in rats to compare effects of 1) two peripherally restricted ? agonists [the tetrapeptide D-Phe-D-Phe-D-Ile-D-Arg-NH(2) (ffir) and the nonpeptidic compound ((R,S)-N-[2-(N-methyl-3,4-dichlorophenylacetamido)-2-(3-carboxyphenyl)-ethyl]pyrrolidine hydrochloride (ICI204448)], 2) a centrally penetrating ? agonist (salvinorin A), and 3) several reference drugs, including a nonsteroidal anti-inflammatory drug (NSAID; ketoprofen). Intraperitoneal injection of dilute lactic acid served as a noxious stimulus to stimulate a stretching response and depress intracranial self-stimulation (ICSS) maintained by the delivery of electrical brain stimulation to the medial forebrain bundle. Acid-stimulated stretching was blocked by ketoprofen, the peripherally restricted ? agonists, and salvinorin A. However, acid-induced depression of ICSS was blocked only by ketoprofen. The peripherally restricted ? agonists had little effect, and salvinorin A exacerbated acid-induced depression of ICSS. These results suggest that peripherally restricted ? agonists may be safer than centrally penetrating ? agonists but less efficacious than NSAIDS or ? opioid receptor agonists to block pain-related depression of behavior; however, the peripheral selectivity of ffir and ICI204448 is limited, and future studies with ? agonists capable of greater peripheral selectivity are warranted. PMID:22128346

Negus, S Stevens; O'Connell, Robert; Morrissey, Ember; Cheng, Kejun; Rice, Kenner C

2011-11-29

195

Effects of peripherally restricted ? opioid receptor agonists on pain-related stimulation and depression of behavior in rats.  

UK PubMed Central (United Kingdom)

? opioid receptor agonists that do not readily cross the blood-brain barrier are peripherally restricted and distribute poorly to the central nervous system after systemic administration. Peripherally restricted ? agonists have promise as candidate analgesics, because they may produce antinociception mediated by peripheral ? receptors more potently than they produce undesirable sedative and psychotomimetic effects mediated by central ? receptors. The present study used assays of pain-related stimulation and depression of behavior in rats to compare effects of 1) two peripherally restricted ? agonists [the tetrapeptide D-Phe-D-Phe-D-Ile-D-Arg-NH(2) (ffir) and the nonpeptidic compound ((R,S)-N-[2-(N-methyl-3,4-dichlorophenylacetamido)-2-(3-carboxyphenyl)-ethyl]pyrrolidine hydrochloride (ICI204448)], 2) a centrally penetrating ? agonist (salvinorin A), and 3) several reference drugs, including a nonsteroidal anti-inflammatory drug (NSAID; ketoprofen). Intraperitoneal injection of dilute lactic acid served as a noxious stimulus to stimulate a stretching response and depress intracranial self-stimulation (ICSS) maintained by the delivery of electrical brain stimulation to the medial forebrain bundle. Acid-stimulated stretching was blocked by ketoprofen, the peripherally restricted ? agonists, and salvinorin A. However, acid-induced depression of ICSS was blocked only by ketoprofen. The peripherally restricted ? agonists had little effect, and salvinorin A exacerbated acid-induced depression of ICSS. These results suggest that peripherally restricted ? agonists may be safer than centrally penetrating ? agonists but less efficacious than NSAIDS or ? opioid receptor agonists to block pain-related depression of behavior; however, the peripheral selectivity of ffir and ICI204448 is limited, and future studies with ? agonists capable of greater peripheral selectivity are warranted.

Negus SS; O'Connell R; Morrissey E; Cheng K; Rice KC

2012-03-01

196

Effects of Peripherally Restricted ? Opioid Receptor Agonists on Pain-Related Stimulation and Depression of Behavior in Rats  

Science.gov (United States)

? Opioid receptor agonists that do not readily cross the blood-brain barrier are peripherally restricted and distribute poorly to the central nervous system after systemic administration. Peripherally restricted ? agonists have promise as candidate analgesics, because they may produce antinociception mediated by peripheral ? receptors more potently than they produce undesirable sedative and psychotomimetic effects mediated by central ? receptors. The present study used assays of pain-related stimulation and depression of behavior in rats to compare effects of 1) two peripherally restricted ? agonists [the tetrapeptide d-Phe-d-Phe-d-Ile-d-Arg-NH2 (ffir) and the nonpeptidic compound ((R,S)-N-[2-(N-methyl-3,4-dichlorophenylacetamido)-2-(3-carboxyphenyl)-ethyl]pyrrolidine hydrochloride (ICI204448)], 2) a centrally penetrating ? agonist (salvinorin A), and 3) several reference drugs, including a nonsteroidal anti-inflammatory drug (NSAID; ketoprofen). Intraperitoneal injection of dilute lactic acid served as a noxious stimulus to stimulate a stretching response and depress intracranial self-stimulation (ICSS) maintained by the delivery of electrical brain stimulation to the medial forebrain bundle. Acid-stimulated stretching was blocked by ketoprofen, the peripherally restricted ? agonists, and salvinorin A. However, acid-induced depression of ICSS was blocked only by ketoprofen. The peripherally restricted ? agonists had little effect, and salvinorin A exacerbated acid-induced depression of ICSS. These results suggest that peripherally restricted ? agonists may be safer than centrally penetrating ? agonists but less efficacious than NSAIDS or ? opioid receptor agonists to block pain-related depression of behavior; however, the peripheral selectivity of ffir and ICI204448 is limited, and future studies with ? agonists capable of greater peripheral selectivity are warranted.

O'Connell, Robert; Morrissey, Ember; Cheng, Kejun; Rice, Kenner C.

2012-01-01

197

Effects of some analgesic anaesthetic drugs on human erythrocyte glutathione reductase: an in vitro study.  

UK PubMed Central (United Kingdom)

Inhibitory effects of some analgesic and anaesthetic drugs on human erythrocyte glutathione reductase were investigated. For this purpose, human erythrocyte glutathione reductase was initially purified 2139-fold in a yield of 29% by using 2', 5'-ADP Sepharose 4B affinity gel and Sephadex G-200 gel filtration chromatography. SDS polyacrylamide gel electrophoresis confirmed the purity of the enzyme by sharing a single band. A constant temperature (+4 degrees C) was maintained during the purification process. Diclofenac sodium, ketoprofen, lornoxicam, tenoxicam, etomidate, morphine and propofol exhibited inhibitory effects on the enzyme in vitro using the Beutler assay method. K(i) constants and IC(50) values for drugs were determined from Lineweaver-Burk graphs and plotting activity % versus [I] graphs, respectively. The IC(50) values of diclofenac sodium, ketoprofen, lornoxicam, propofol, tenoxicam, etomidate and morphine were 7.265, 6.278, 0.3, 0.242, 0.082, 0.0523 and 0.0128 mM and the K(i) constants were 23.97 +/- 2.1, 22.14 +/- 7.6, 0.42 +/- 0.18, 0.418 +/- 0.056, 0.13 +/- 0.025, 0.0725 +/- 0.0029 and 0.0165 +/- 0.0013 mM, respectively. While diclofenac sodium, ketoprofen, lornoxicam, tenoxicam etomidate and morphine showed competitive inhibition, propofol displayed noncompetitive inhibition.

Senturk M; Irfan Kufrevioglu O; Ciftci M

2009-04-01

198

Effects of some analgesic anaesthetic drugs on human erythrocyte glutathione reductase: an in vitro study.  

Science.gov (United States)

Inhibitory effects of some analgesic and anaesthetic drugs on human erythrocyte glutathione reductase were investigated. For this purpose, human erythrocyte glutathione reductase was initially purified 2139-fold in a yield of 29% by using 2', 5'-ADP Sepharose 4B affinity gel and Sephadex G-200 gel filtration chromatography. SDS polyacrylamide gel electrophoresis confirmed the purity of the enzyme by sharing a single band. A constant temperature (+4 degrees C) was maintained during the purification process. Diclofenac sodium, ketoprofen, lornoxicam, tenoxicam, etomidate, morphine and propofol exhibited inhibitory effects on the enzyme in vitro using the Beutler assay method. K(i) constants and IC(50) values for drugs were determined from Lineweaver-Burk graphs and plotting activity % versus [I] graphs, respectively. The IC(50) values of diclofenac sodium, ketoprofen, lornoxicam, propofol, tenoxicam, etomidate and morphine were 7.265, 6.278, 0.3, 0.242, 0.082, 0.0523 and 0.0128 mM and the K(i) constants were 23.97 +/- 2.1, 22.14 +/- 7.6, 0.42 +/- 0.18, 0.418 +/- 0.056, 0.13 +/- 0.025, 0.0725 +/- 0.0029 and 0.0165 +/- 0.0013 mM, respectively. While diclofenac sodium, ketoprofen, lornoxicam, tenoxicam etomidate and morphine showed competitive inhibition, propofol displayed noncompetitive inhibition. PMID:18608753

Senturk, Murat; Irfan Kufrevioglu, O; Ciftci, Mehmet

2009-04-01

199

Antiallodynic and analgesic effects of maslinic acid, a pentacyclic triterpenoid from Olea europaea.  

UK PubMed Central (United Kingdom)

The effects of maslinic acid (1), a pentacyclic triterpenoid obtained from Olea europaea, were studied in several tests for nociception in mice. Systemic administration of 1 reduced acetic acid-induced writhing, the inflammatory phase of formalin-induced pain, and capsaicin-induced mechanical allodynia. However, it did not induce motor incoordination in the rotarod test. The topical administration of 1 also reduced the inflammatory phase of the formalin test, indicating that at least some of its effects are mediated peripherally. The present results demonstrate for the first time that maslinic acid induces antinociceptive and antiallodynic effects.

Nieto FR; Cobos EJ; Entrena JM; Parra A; García-Granados A; Baeyens JM

2013-04-01

200

Antiallodynic and analgesic effects of maslinic acid, a pentacyclic triterpenoid from Olea europaea.  

Science.gov (United States)

The effects of maslinic acid (1), a pentacyclic triterpenoid obtained from Olea europaea, were studied in several tests for nociception in mice. Systemic administration of 1 reduced acetic acid-induced writhing, the inflammatory phase of formalin-induced pain, and capsaicin-induced mechanical allodynia. However, it did not induce motor incoordination in the rotarod test. The topical administration of 1 also reduced the inflammatory phase of the formalin test, indicating that at least some of its effects are mediated peripherally. The present results demonstrate for the first time that maslinic acid induces antinociceptive and antiallodynic effects. PMID:23540838

Nieto, Francisco R; Cobos, Enrique J; Entrena, José M; Parra, Andrés; García-Granados, Andrés; Baeyens, José M

2013-03-29

 
 
 
 
201

[The effect of flupirtine, various analgesics and muscle relaxants on skeletal muscle tone in the conscious rat  

UK PubMed Central (United Kingdom)

The influence of the skeletal muscle tone by flupirtine (D-9998, Katadolon; CAS 56995-20-1), some selected analgesics and muscle relaxants was investigated in conscious rats after intraperitoneal administration. Benzodiazepines (diazepam and tetrazepam), baclofen, dantrolene and mephenesine reduced the tone of the skeletal muscle. Opiate analgesics, such as morphine, codeine and tramadol, enhanced the muscle tone. Flupirtine reduced the skeletal muscle tone at doses comparable with its antinociceptive effective doses. In this dose range no sedative side effects as ataxia or decrease of spontaneous motor activity could be observed. The mode of this muscle relaxing effect of flupirtine is not known in all details. It is, however, likely that flupirtine is able to inhibit the mono- and/or polysynaptic reflexes at the spinal level.

Nickel B; Jakovlev V; Szelenyi I

1990-08-01

202

[The effect of flupirtine, various analgesics and muscle relaxants on skeletal muscle tone in the conscious rat].  

Science.gov (United States)

The influence of the skeletal muscle tone by flupirtine (D-9998, Katadolon; CAS 56995-20-1), some selected analgesics and muscle relaxants was investigated in conscious rats after intraperitoneal administration. Benzodiazepines (diazepam and tetrazepam), baclofen, dantrolene and mephenesine reduced the tone of the skeletal muscle. Opiate analgesics, such as morphine, codeine and tramadol, enhanced the muscle tone. Flupirtine reduced the skeletal muscle tone at doses comparable with its antinociceptive effective doses. In this dose range no sedative side effects as ataxia or decrease of spontaneous motor activity could be observed. The mode of this muscle relaxing effect of flupirtine is not known in all details. It is, however, likely that flupirtine is able to inhibit the mono- and/or polysynaptic reflexes at the spinal level. PMID:2242082

Nickel, B; Jakovlev, V; Szelenyi, I

1990-08-01

203

Efecto del zumo de Morinda citrifolia L. (noni) en modelos de analgesia/ Effect of Morinda citrifolia L. (noni) in analgesic models  

Scientific Electronic Library Online (English)

Full Text Available Abstract in spanish Introducción: Morinda citrifolia L. (noni) ha despertado gran interés y expectativa dentro de la población cubana debido a las propiedades medicinales que se le atribuyen. Investigaciones realizadas evidencian las propiedades analgésicas de algunas de sus partes. Objetivos: evaluar el efecto del zumo de noni en diferentes modelos de analgesia. Métodos: se utilizaron dosis (450, 900 y 1 800 mg/kg) del zumo de noni, a partir de contenido en peso seco; se administró po (more) r vía intraperitoneal a ratones OF1 en el modelo de irritación peritoneal por ácido acético 0,6 % y se cuantificó el número de contorsiones o estiramientos. Además, se utilizó el modelo del plato caliente y el de la retirada de la cola. Resultados: el zumo de noni fue efectivo de manera dependiente de la dosis en reducir el número de contorsiones inducidas por el ácido acético. En los modelos del plato caliente y de retirada de la cola, solo la dosis más alta prolongó de manera estadísticamente significativa el tiempo de reacción. Conclusiones: los resultados sugieren que el efecto analgésico de noni es fundamentalmente de mecanismo periférico. Abstract in english Introduction: Morinda citrifolia L. (noni) has aroused great interest and expectations in the Cuban population due to attributed medicinal properties. Several research works have suggested the analgesic effect of several parts of the plant. Objectives: to evaluate the effect of Noni juice in different analgesic models. Methods: there were used 450, 900, and 1 800 mg/kg doses of the juice, based on the dry content weight. They were administered intraperitonealy to adult ma (more) le mice OF1 in the peritoneal irritation model induced by acetic acid at 0.6 % concentration, and the number of contorsions or stretchings was quantified. Additionally, the hot plate and the tail immersed in hot water models were applied. Results: the noni juice was effective in reducing the number of contortions induced by the acetic acid in a dose-dependent manner. Just the highest dose of the juice increased significantly the time of reaction in the hot plate and in the tail immersion test. Conclusions: these results suggest that the analgesic effect of Noni juice is basically peripheral.

Sánchez Rodríguez, Nora; Bu Wong, Margarita; Pérez-Saad, Héctor; Lara Fernández, Gloria; Scull, Isidoro

2012-09-01

204

Efecto del zumo de Morinda citrifolia L. (noni) en modelos de analgesia Effect of Morinda citrifolia L. (noni) in analgesic models  

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Full Text Available Introducción: Morinda citrifolia L. (noni) ha despertado gran interés y expectativa dentro de la población cubana debido a las propiedades medicinales que se le atribuyen. Investigaciones realizadas evidencian las propiedades analgésicas de algunas de sus partes. Objetivos: evaluar el efecto del zumo de noni en diferentes modelos de analgesia. Métodos: se utilizaron dosis (450, 900 y 1 800 mg/kg) del zumo de noni, a partir de contenido en peso seco; se administró por vía intraperitoneal a ratones OF1 en el modelo de irritación peritoneal por ácido acético 0,6 % y se cuantificó el número de contorsiones o estiramientos. Además, se utilizó el modelo del plato caliente y el de la retirada de la cola. Resultados: el zumo de noni fue efectivo de manera dependiente de la dosis en reducir el número de contorsiones inducidas por el ácido acético. En los modelos del plato caliente y de retirada de la cola, solo la dosis más alta prolongó de manera estadísticamente significativa el tiempo de reacción. Conclusiones: los resultados sugieren que el efecto analgésico de noni es fundamentalmente de mecanismo periférico.Introduction: Morinda citrifolia L. (noni) has aroused great interest and expectations in the Cuban population due to attributed medicinal properties. Several research works have suggested the analgesic effect of several parts of the plant. Objectives: to evaluate the effect of Noni juice in different analgesic models. Methods: there were used 450, 900, and 1 800 mg/kg doses of the juice, based on the dry content weight. They were administered intraperitonealy to adult male mice OF1 in the peritoneal irritation model induced by acetic acid at 0.6 % concentration, and the number of contorsions or stretchings was quantified. Additionally, the hot plate and the tail immersed in hot water models were applied. Results: the noni juice was effective in reducing the number of contortions induced by the acetic acid in a dose-dependent manner. Just the highest dose of the juice increased significantly the time of reaction in the hot plate and in the tail immersion test. Conclusions: these results suggest that the analgesic effect of Noni juice is basically peripheral.

Nora Sánchez Rodríguez; Margarita Bu Wong; Héctor Pérez-Saad; Gloria Lara Fernández; Isidoro Scull

2012-01-01

205

ANALGESIC AND ANTI INFLAMMATORY EFFECT OF LEECH THERAPY (JALAUKAVCHARAN) IN THE PATIENTS OF OSTEOARTHRITIS (SANDHIGATA VATA)  

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Full Text Available Osteoarthritis (degenerative joint disease) is the most common joint disorder. It mostly affects cartilage. The top layer of cartilage breaks down and wears away. Osteoarthritis is of two types, primary (idiopathic) and secondary. In idiopathic osteoarthritis, the most common form of the disease, no predisposing factor is apparent. Secondary OA is pathologically indistinguishable from idiopathic OA but is attributable to an underlying cause. The NSAID’S are main drug of choice in modern medicine which have lots of side effect therefore are not safe for long term therapy. Raktamokshan viz bloodletting is one of the ancient and important parasurgical procedure described in Ayurveda for treatment of various diseases. Of them, Jalaukavacharana or Leech Therapy has gained greater attention globally, because of its medicinal values. The saliva of leech contains numerous biologically active substances, which has anti-inflammatory, analgesic as well as anesthetic property. Keeping this view in mind we have started leech therapy in the patients of osteoarthritis and found encouraging results.

Singh Akhilesh Kumar; Singh Om Prakash

2012-01-01

206

[Eutectic mixture of local anesthetics (EMLA): evaluation of the analgesic effectiveness during ND: YAG laser turbinoplasty  

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The analgesic effect of EMLA anesthetic cream is evaluated during contact turbinoplasty with a Neodymium: yttrium-aluminum-garnet (Nd: Yag) laser. A total of 48 patients were selected and randomized in two groups. EMLA was applied on the nasal mucosa, respectively, for 15 and 30 minutes after using vasoconstrictor cottonoids. Both groups underwent turbinate reduction by contact with Nd: Yag laser using three discharge incisions traced parallel on the medial surface of the lower turbinate working from the tail to the head. The pain induced by the surgical procedure was evaluated with a visual analogic scale. The score obtained was significantly lower in the 1st group than in the 2nd group and this difference was statistically significant (p < 0.01). The EMLA anesthetic cream applied on the mucosa for 15 minutes allows to obtain a good analgesia during the functional contact turbinate surgery with a Nd: Yag laser and thus can be considered a valid alternative to anesthesia by local infiltration.

Di Carlo R; Lombardo P; Modugno V; Pastore A

2001-10-01

207

[Eutectic mixture of local anesthetics (EMLA): evaluation of the analgesic effectiveness during ND: YAG laser turbinoplasty].  

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The analgesic effect of EMLA anesthetic cream is evaluated during contact turbinoplasty with a Neodymium: yttrium-aluminum-garnet (Nd: Yag) laser. A total of 48 patients were selected and randomized in two groups. EMLA was applied on the nasal mucosa, respectively, for 15 and 30 minutes after using vasoconstrictor cottonoids. Both groups underwent turbinate reduction by contact with Nd: Yag laser using three discharge incisions traced parallel on the medial surface of the lower turbinate working from the tail to the head. The pain induced by the surgical procedure was evaluated with a visual analogic scale. The score obtained was significantly lower in the 1st group than in the 2nd group and this difference was statistically significant (p < 0.01). The EMLA anesthetic cream applied on the mucosa for 15 minutes allows to obtain a good analgesia during the functional contact turbinate surgery with a Nd: Yag laser and thus can be considered a valid alternative to anesthesia by local infiltration. PMID:11865786

Di Carlo, R; Lombardo, P; Modugno, V; Pastore, A

2001-10-01

208

Analgesics and ENT surgery. A clinical comparison of the intraoperative, recovery and postoperative effects of buprenorphine, diclofenac, fentanyl, morphine, nalbuphine, pethidine and placebo given intravenously with induction of anaesthesia.  

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1. Vomiting and restlessness following ENT and eye surgery are undesirable, and may be related to the emetic and analgesic effects of any analgesic given to augment anaesthesia during surgery. 2. To rationalise the choice of analgesic for routine ENT surgery we examined the intraoperative, recovery ...

van den Berg, A A; Honjol, N M; Prabhu, N V; Datta, S; Rozario, C J; Muraleedaran, R; Savva, D

209

Analgesic effects of electroacupuncture combined with Celebrex on rats with tibial cancer pain  

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Full Text Available Objective: To establish a proper experimental model of bone cancer pain in rat for acupuncture research, and observe the pain-relieving effect of electroacupuncture (EA) and/or Celebrex on bone cancer pain in rats.Methods: The rat model of bone cancer pain was established by percutaneous direct puncture technique and inoculating the rat mammary gland carcinoma cells Walker 256 into tibial medullary cavity directly, and evaluated by detecting the bone tumor growth and mechanical allodynia. The effects of daily EA treatment and/or Celebrex treatment on the rat mechanical allodynia after intratibial Walker 256 inoculation was observed in this study.Results: Significant mechanical allodynia in ipsilateral hind paw and tumor growth in proximal end of tibial bone of rats in the untreated group were observed after intratibial Walker 256 inoculation. The mechanical allodynia thresholds in rats that received EA or 5 mg/(kg·d) Celebrex treatment showed no significant difference as compared with that of rats in the untreated group. However, the mechanical allodynia thresholds of rats in 10 mg/(kg·d) Celebrex group showed significant increase after 22- and 26-day treatment as compared with that in the methyl cellulose (MC) group. There was significant difference between rats with EA combined with 5 mg/(kg·d) Celebrex treatment and rats in the untreated group after 10-, 18- and 23-day treatment.Conclusion: EA and 5 mg/(kg·d) Celebrex have synergistic effect on pain relieving and their combined use may enhance the analgesic effect on bone cancer pain.

Qi-liang MAO-YING; Yan-qing WANG

2008-01-01

210

Participation of ATP-sensitive K+ channels in the peripheral antinociceptive effect of fentanyl in rats  

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Full Text Available We examined the effect of several K+ channel blockers such as glibenclamide, tolbutamide, charybdotoxin (ChTX), apamin, tetraethylammonium chloride (TEA), 4-aminopyridine (4-AP), and cesium on the ability of fentanyl, a clinically used selective µ-opioid receptor agonist, to promote peripheral antinociception. Antinociception was measured by the paw pressure test in male Wistar rats weighing 180-250 g (N = 5 animals per group). Carrageenan (250 µg/paw) decreased the threshold of responsiveness to noxious pressure (delta = 188.1 ± 5.3 g). This mechanical hyperalgesia was reduced by fentanyl (0.5, 1.5 and 3 µg/paw) in a peripherally mediated and dose-dependent fashion (17.3, 45.3 and 62.6%, respectively). The selective blockers of ATP-sensitive K+ channels glibenclamide (40, 80 and 160 µg/paw) and tolbutamide (80, 160 and 240 µg/paw) dose dependently antagonized the antinociception induced by fentanyl (1.5 µg/paw). In contrast, the effect of fentanyl was unaffected by the large conductance Ca2+-activated K+ channel blocker ChTX (2 µg/paw), the small conductance Ca2+-activated K+ channel blocker apamin (10 µg/paw), or the non-specific K+ channel blocker TEA (150 µg/paw), 4-AP (50 µg/paw), and cesium (250 µg/paw). These results extend previously reported data on the peripheral analgesic effect of morphine and fentanyl, suggesting for the first time that the peripheral µ-opioid receptor-mediated antinociceptive effect of fentanyl depends on activation of ATP-sensitive, but not other, K+ channels.

Rodrigues A.R.A.; Castro M.S.A.; Francischi J.N.; Perez A.C.; Duarte I.D.G.

2005-01-01

211

Analgesic and Anti-Inflammatory Effects of Ethanolic Root Extract of Hippocratea africana  

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Full Text Available The ethanolic root extract of Hippocratea africana (200-600 mg kg-1) was evaluated for analgesic, anti-inflammatory and antipyretic properties. The extract dose dependently inhibited acetic acid-induced writhing, formalin-induced paw licking and thermally -induced pain in mice. The extract also inhibited fresh egg albumin, carrageenin and xylene-induced inflammation in mice. These inhibitions were statistically significant (p<0.05) when compared to control. The roots extracts was also found to reduce pyrexia in rats. The analgesic, anti-inflammatory and antipyretic activities of the extract may be related to its active constituents such as tannins, saponins, steroid and flavonoids.

Jude E. Okokon; Bassey S. Antia; Emem Umoh

2008-01-01

212

Comparing Analgesic Effects of a Topical Herbal Mixed Medicine with Salicylate in Patients with Knee Osteoarthritis  

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Full Text Available Knee osteoarthritis is the most common cause of disability among people and it is a common disease of joints that can lead to cartilage damage. In this study the analgesic effects of a herbal ointment containing cinnamon, ginger, mastic (Saghez) and sesame oil is compared with Salicylate ointment in patients suffering from knee osteoarthritis. It was a double-blind randomized controlled trail study. Patients with diagnosed arthritis were involved in the study and they were divided in two groups via block randomization method. For six weeks, twice a day, intervention group applied herbal ointment and control group used Salicylate ointment. The severity of pain, morning stiffness and limited motion were measured using Visual Analog Pain Scale. In order to analyze the trends of these three indexes, repeated measurement test was used. Ninety two participates with the mean age of 52.2 (12.4) years and with the mean disease period of 30.45 (30.3) months were involved in the study. There was no significant difference between two groups regarding the distribution of sex, weight, height, BMI and the duration of illness. No statistical difference was observed between two groups regarding pain relief, morning stiffness and limited motion; nevertheless in repeated measurements during second, forth and sixth weeks in both groups the decreasing trend of these three indexes had been statistically significant (p<0.0001). It seems that using this herbal combination is clinically effective for patients suffering from knee osteoarthritis in order to decrease their pain, morning stiffness and limited motion; its effect is comparable with Salicylate ointment.

Mohsen Zahmatkash; Mohammad Reza Vafaeenasab

2011-01-01

213

Randomized prospective study of the analgesic effect of nefopam after orthopaedic surgery.  

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BACKGROUND: Balanced postoperative analgesia combines non-narcotic drugs and opioids. We organized a large study to evaluate nefopam analgesia and tolerance in combination with morphine for patient-controlled analgesia (PCA) after orthopaedic surgery. METHODS: Two hundred and one patients scheduled to undergo hip arthroplasty were included in this multicentre (n=24), double-blind, randomized study comparing nefopam (20 mg every 4 h for 24 h) with placebo, the first dose being infused peroperatively. The primary outcome measure was the cumulative morphine dose received postoperatively by PCA over 24 h. Secondary outcome measures were the amount of morphine received as a loading dose in the postanaesthesia care unit (PACU) and during the 24-h observation period, and pain assessments using a visual analogue scale (VAS) and a verbal pain scale (VPS), patient's satisfaction with analgesia and treatment tolerance. RESULTS: The two groups were comparable with respect to their characteristics and preoperative pain assessment. PCA-administered morphine over 24 h was significantly less for the nefopam group than the control group (21.2 (15.3) and 27.3 (19.2) mg respectively; P=0.02). This morphine-sparing effect was greater (35.1%) for patients with severe preoperative pain (VAS>30/100). For the entire study period (loading dose and PCA), morphine use was less for the nefopam group (34.5 (19.6) vs 42.7 (23.6) mg; P=0.01). Pain VAS at PACU arrival and during the whole PACU period was significantly lower for the nefopam than for the placebo group (P=0.002 and 0.04 respectively). Patient satisfaction was similar for the nefopam and placebo groups. CONCLUSION: In combination with PCA morphine, nefopam gives significant morphine-sparing with lower immediate postoperative pain scores without major side-effects. This analgesic effect seems to be particularly notable for patients with intense preoperative pain.

Du Manoir B; Aubrun F; Langlois M; Le Guern ME; Alquier C; Chauvin M; Fletcher D

2003-12-01

214

Tolerance develops to the antiallodynic effects of the peripherally acting opioid loperamide hydrochloride in nerve-injured rats.  

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Peripherally acting opioids are potentially attractive drugs for the clinical management of certain chronic pain states due to the lack of centrally mediated adverse effects. However, it remains unclear whether tolerance develops to peripheral opioid analgesic effects under neuropathic pain conditions. We subjected rats to L5 spinal nerve ligation (SNL) and examined the analgesic effects of repetitive systemic and local administration of loperamide hydrochloride, a peripherally acting opioid agonist. We found that the inhibition of mechanical hypersensitivity, an important manifestation of neuropathic pain, by systemic loperamide (1.5mg/kg subcutaneously) decreased after repetitive drug treatment (tolerance-inducing dose: 0.75 to 6.0mg/kg subcutaneously). Similarly, repeated intraplantar injection of loperamide (150?g/50?L intraplantarly) and D-Ala(2)-MePhe(4)-Glyol(5) enkephalin (300?g/50?L), a highly selective mu-opioid receptor (MOR) agonist, also resulted in decreased inhibition of mechanical hypersensitivity. Pretreatment with naltrexone hydrochloride (5mg/kg intraperitoneally) and MK-801 (0.2mg/kg intraperitoneally) attenuated systemic loperamide tolerance. Western blot analysis showed that repetitive systemic administration of morphine (3mg/kg subcutaneously), but not loperamide (3mg/kg subcutaneously) or saline, significantly increased MOR phosphorylation in the spinal cord of SNL rats. In cultured rat dorsal root ganglion neurons, loperamide dose-dependently inhibited KCl-induced increases in [Ca(2+)]i. However, this drug effect significantly decreased in cells pretreated with loperamide (3?M, 72hours). Intriguingly, in loperamide-tolerant cells, the delta-opioid receptor antagonist naltrindole restored loperamide's inhibition of KCl-elicited [Ca(2+)]i increase. Our findings indicate that animals with neuropathic pain may develop acute tolerance to the antiallodynic effects of peripherally acting opioids after repetitive systemic and local drug administration. PMID:23880055

He, Shao-Qiu; Yang, Fei; Perez, Federico M; Xu, Qian; Shechter, Ronen; Cheong, Yong-Kwan; Carteret, Alene F; Dong, Xinzhong; Sweitzer, Sarah M; Raja, Srinivasa N; Guan, Yun

2013-07-20

215

Effects of the novel analgesic, cizolirtine, in a rat model of neuropathic pain.  

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Cizolirtine (5-9[(N,N-dimethylaminoethoxy)phenyl]methyl0-1-methyl-1H-pyrazol citrate) is a centrally acting analgesic with a currently unknown mechanism of action, whose efficacy has been demonstrated in various models of acute and inflammatory pain in rodents. Further studies were performed in order to assess its potential antinociceptive action in a well-validated model of neuropathic pain, i.e. that produced by unilateral sciatic nerve constriction in rats. Animals were subjected to relevant behavioural tests based on mechanical (vocalization threshold to paw pressure) and thermal (struggle latency to paw immersion in a cold (10 degrees C) water bath) stimuli, 2 weeks after sciatic nerve constriction, when pain-related behaviour was fully developed. Acute pretreatment with 2.5-10 mg/kg p.o. of cizolirtine reversed both mechanical and thermal allodynia. These effects were antagonized by prior injection of the alpha(2)-adrenoceptor antagonist idazoxan (0.5 mg/kg i.v.), but not the opioid receptor antagonist naloxone (0.1 mg/kg i.v.). On the other hand, cizolirtine (10 mg/kg p.o.) produced no motor deficits in animals using the rotarod test. Our study showed that cizolirtine suppressed pain-related behavioural responses to mechanical and cold stimuli in neuropathic rats, probably via an alpha(2)-adrenoceptor-dependent mechanism. These results suggest that cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects. PMID:12855326

Kayser, Valérie; Farré, Antonio; Hamon, Michel; Bourgoin, Sylvie

2003-07-01

216

Effects of the novel analgesic, cizolirtine, in a rat model of neuropathic pain.  

UK PubMed Central (United Kingdom)

Cizolirtine (5-9[(N,N-dimethylaminoethoxy)phenyl]methyl0-1-methyl-1H-pyrazol citrate) is a centrally acting analgesic with a currently unknown mechanism of action, whose efficacy has been demonstrated in various models of acute and inflammatory pain in rodents. Further studies were performed in order to assess its potential antinociceptive action in a well-validated model of neuropathic pain, i.e. that produced by unilateral sciatic nerve constriction in rats. Animals were subjected to relevant behavioural tests based on mechanical (vocalization threshold to paw pressure) and thermal (struggle latency to paw immersion in a cold (10 degrees C) water bath) stimuli, 2 weeks after sciatic nerve constriction, when pain-related behaviour was fully developed. Acute pretreatment with 2.5-10 mg/kg p.o. of cizolirtine reversed both mechanical and thermal allodynia. These effects were antagonized by prior injection of the alpha(2)-adrenoceptor antagonist idazoxan (0.5 mg/kg i.v.), but not the opioid receptor antagonist naloxone (0.1 mg/kg i.v.). On the other hand, cizolirtine (10 mg/kg p.o.) produced no motor deficits in animals using the rotarod test. Our study showed that cizolirtine suppressed pain-related behavioural responses to mechanical and cold stimuli in neuropathic rats, probably via an alpha(2)-adrenoceptor-dependent mechanism. These results suggest that cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects.

Kayser V; Farré A; Hamon M; Bourgoin S

2003-07-01

217

[Analgesic effect of sinomenine on SSNI model rats and monoamine neurotransmitters in striatal extracellular fluid].  

UK PubMed Central (United Kingdom)

OBJECTIVE: To observe the analgesic effect of sinomenine on the neuropathic pain rat model induced by SSNI, and discuss its impact on monoamine neurotransmitters in striatal extracellular fluid. METHOD: Male SD rats were randomly divided into the sham operation group, the SSNI model group, the gabapentin group (100 mg x kg(-1)), the sinomenine high dose group (40 mg x kg(-1)) and the sinomenine low dose group (20 mg x kg(-1)). Mechanical hyperalgesia and cold pain sensitivity were evaluated by Von Frey hairs and cold spray. Striatum was sampled by microdialysis. High performance liquid chromatography-electrochemical detector (HPLC-ECD) were used to detect the content of such neurotransmitters as monoamine neurotransmitters noradrenaline (NE), dopamine (DA), 5-hydroxy tryptamine (5-HT) and their metabolites dihydroxyphenylacetic phenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA). RESULT: SSNI model rats showed significant improvement in mechanical withdrawal threshold and cold pain sensitivity, significant decrease in intracerebral NE and notable increase in DA, 5-HT and their metabolites. Compared with the model group, the sinomenine high dose group showed significant increase in mechanical withdrawal threshold at 60, 90, 180 and 240 min after abdominal administration (P < 0.01), significant decrease in cold pain sensitivity score during 30-240 min (P < 0.05). Sinomenine can significantly up-regulated NE content in striatal extracellular fluid during 45-135 min (P < 0.05), remarkably reduce DA content and DOPAC at 45, 75 and 135 min (P < 0.05), 5-HT content during 45-135 min, DOPAC during 75-165 min (P < 0.05), and 5-HIAA during 45-135 min (P < 0.05). CONCLUSION: Sinomenine has the intervention effect on neuropathic pain in SSNI model rats. Its mechanism may be related to disorder of monoamine neurotransmitters in striatal extracellular fluid.

Zhang MY; Li P; Wang DQ; Niu XH; Wang Y; Wang ZG; Zhang Y; Xu S; Xu XJ

2013-02-01

218

Analgesic effects of meloxicam administration on postoperative orthopedic pain in domestic pigeons (Columba livia).  

UK PubMed Central (United Kingdom)

OBJECTIVE: To assess the analgesic effects of 2 doses of meloxicam on the degree of postoperative orthopedic pain in pigeons. ANIMALS: 21 domestic pigeons (Columba livia). PROCEDURES: In each bird, a standardized osteotomy of 1 femur was performed and the fracture was immobilized with an intramedullary pin. Birds were randomly allocated to receive saline (0.9% NaCl) solution (control) or meloxicam (0.5 mg/kg [low dose] or 2.0 mg/kg [high dose]). The first treatment was administered i.m. after surgery was completed. Subsequent treatments were administered p.o. every 12 hours for 9 days. Degree of postoperative pain was assessed for the first 4 days after surgery by use of 3 methods: an electronic perch for assessment of weight-bearing load differential of the pelvic limbs, 4 pain scales, and analysis of video-recorded partial ethograms for bird activity and posture. RESULTS: No significant differences were observed between the control group and the low-dose meloxicam group in any tested variable. The high-dose meloxicam group had a greater degree of weight bearing on the affected limb from the second to the fourth postoperative day as well as lower pain scores for at least the first 2 postoperative days, compared with the other groups. Return to presurgical behavior was achieved faster in pigeons that received high-dose meloxicam than in the other groups. No adverse effects were observed. CONCLUSIONS AND CLINICAL RELEVANCE: Administration of meloxicam at 0.5 mg/kg appeared ineffective in minimizing postoperative orthopedic pain in pigeons, but the 2.0 mg/kg dose provided quantifiable analgesia that appeared safe in this species in experimental conditions.

Desmarchelier M; Troncy E; Fitzgerald G; Lair S

2012-03-01

219

[Optimal analgesic effect of continuous supraclavicular brachial plexus block with ropivacaine after shoulder surgery].  

UK PubMed Central (United Kingdom)

BACKGROUND: Optimal dose of local anesthetics for supraclavicular brachial plexus block (BPB) is still unknown. We prospectively investigated the analgesic effect of ultrasound-guided continuous supraclavicular BPB with ropivacaine at different infusion rates. METHODS: Thirty-nine patients scheduled to undergo shoulder surgery were randomly assigned to four groups; receiving no continuous BPB (control group, n = 10), BPB with 0.2% of ropivacaine at an infusion rate of 4 ml x hr(-1) (n = 12), BPB with 6 ml x hr(-1) (n = 12) or BPB with 8 ml x hr(-1) (n = 5). All patients were permitted to receive nonsteroidal anti-inflammatory drugs (NSAIDs) after surgery. Visual analogue scale (VAS) for postoperative pain was assessed and frequencies of the requirement of NSAIDs were recorded in each group. RESULTS: The pain scores during 24 hours after surgery in the 6 ml x hr(-1) group (3-24 mm) were significantly lower than those in the 4 ml x hr(-1) group (4-42 mm) and control group (6-56 mm). Mean frequency of administrations of NSAIDs for 24 hours after surgery in the 6 ml x hr(-1) (0.8 +/- 0.8) group was significantly lower than that in the control group (1.7 +/- 1.0). Continuous administration in two cases in the 8 ml x hr(-1) group was discontinued due to leakage of local anesthetics and headache. CONCLUSIONS: Continuous supraclavicular BPB with 0.2% ropivacaine at 6 ml x hr(-1) is effective for the pain management after shoulder surgery and is not an excess dose.

Niiya T; Yamauchi M; Mizukami N; Niiyama Y; Ohsone J; Honma H; Kawamata T; Yamakage M; Hirose T

2010-11-01

220

Analgesic and cardiopulmonary effects of intrathecally administered romifidine or romifidine and ketamine in goats (Capra hircus)  

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Full Text Available The study was conducted to evaluate the effects of romifidine alone (50 µg/kg) and a combination of romifidine (50 µg/kg) and ketamine (2.5 mg/kg) after intrathecal administration in goats. Ten adult goats of either sex weighing between 15 and 20 kg were randomly placed in 2 groups (groups I and II). The agents were administered at the lumbosacral subarachnoid space. Clinico-physiological parameters such as analgesia, motor incoordination, sedation, salivation, heart rate, respiratory rate, arterial pressure, central venous pressure and rectal temperature were studied. Other haematobiochemical parameters monitored were packed cell volume, haemoglobin, plasma proteins, glucose, urea and creatinine. The onset of analgesia was faster in group II (35.5 ±6.25 s) compared to that of group I (5.2 ±0.54 min). Analgesia of the tail, perineum, hind limbs, flank and thorax was mild to moderate in group I, but complete analgesia of tail, perineum and hind limbs was recorded in group II. Motor incoordination was mild in group I and severe in group II. Significant reduction in heart rate (more pronounced in group I) and respiratory rate (more pronounced in group II), and a significant increase in central venous pressure were recorded in both groups. Mean arterial pressure was reduced in both groups, but more markedly in group I. Sedation, electro-cardiogram, rectal temperature and haemato-biochemical parameters did not show significant differences between the 2 groups. The results of this study indicated a possible synergistic analgesic interaction between intrathecally administered romifidine and ketamine, without causing any marked systemic effects in goats.

H.P. Aithal; P. Kinjavdekar; A.M. Pawde; K. Pratap

2012-01-01

 
 
 
 
221

Compare the Analgesic Effectiveness of Diclofenac and Paracetamol in Patients with Renal Colic  

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Full Text Available    Aim: This retrospective study was aimed to compare the analgesic effectiveness of paracetamol and diclofenac sodium by using visual analog acale (VAS) in patients applying to emergency room with renal colic. Material and Method: Group I (n=40) patients diagnosed with renal colic and treated with diclofenac sodium (75 mg intramuscular) and Group II (n=40) patients diagnosed with renal colic and treated with paracetamol (1 g intravenous) were included in this study. In both groups, patients were between 19-64 years old. In all groups, the intensity of the pain was ranked between 0 (no pain) and 10 (intolerable) by using VAS. VAS score of the groups were compared. Result: Before the treatment VAS values of at Group I; 7.95 ± 1.48 while Group II; 7.92 ± 1.76. Respectively in the 10th and 30th minutes VAS value of patient Group I; 5.35±2.19/ 3.73±1.93 and Group II; 4.28±1.9/2.33±1.77. Before the treatment VAS value of paracetamol group was not different from the diclofenac sodium group. However, after the treatment, in the 10th and 30th minutes, VAS values of the paracetamol group scores were lower than diclofenac group (P=0.022 ve 0.002). Discussion: According to our study’s finding, paracetamol gives good results in the renal colic pain treatment. Moreover, paracetamol which lower side effects than non-steroidal antiinflammatory drug (NSAIDs) may be a good alternative in the treatment of renal colic.

Murat Ayan

2013-01-01

222

Analgesic and systemic effects of xylazine, lidocaine and their combination after subarachnoid administration in goats  

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Full Text Available The objective of the study was to determine the analgesic and systemic effects of subarachnoid administration of xylazine hydrochloride (XY), lidocaine hydrochloride (LI) and their combination (XYLI) in goats. Six healthy goats were used in a prospective randomised study. Three treatments were administered to each goat, with 1-week intervals between each treatment. Treatments consisted of 0.1 mg/kg xylazine, 2.5 mg/kg lidocaine and a combination of xylazine 0.05 (mg/kg) and lidocaine (1.25 mg/kg). Analgesia, ataxic, sedative, cardiovascular and respiratory effects, and rectal temperature were evaluated before (baseline) and at 5, 10, 15, and 30 min after subarachnoid injection, and then at 30-min intervals until loss of analgesia occurred. Lidocaine induced analgesia in 3.1 + 1min (mean + SD), which lasted for 66 + 31 min. Heart and respiratory rates and blood pressure remained unchanged after lidocaine-induced analgesia. Xylazine induced analgesia in 9.5 + 2.6 min and xylazine-lidocaine in 3.2 + 1.2 min. Xylazine-lidocaine-induced analgesia lasted longer (178.3 + 37 min) than that induced by xylazine (88.3 + 15 min). The XYLI treatment induced prolonged motor blocking (115 min), more than the XY (80 min) and LI (90 min) treatments. Both xylazine and xylazine-lidocaine caused significant decreases in the heart and respiratory rates, but not in blood pressure. The combination of xylazine (0.05 mg/kg) and lidocaine (1.25 mg/kg) can be administered subarachnoidally (between last lumbar vertebra and 1st sacral vertebra) to produce prolonged (>2.5 h) analgesia of the tail, perineum, hind limbs, flanks and caudodorsal rib areas in goats. Despite the prolonged analgesia, using this combination is desirable for relieving postoperative pain, but it may be a disadvantage due to a motor block when dealing with goats.

R. DeRossi; A.L. Junqueira; M.P. Beretta

2012-01-01

223

Comparison of analgesic effects of nimesulide, paracetamol, and their combination in animal models  

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Objectives: To compare the analgesic activity of nimesulide and paracetamol alone and their combination in animal models for the degree of analgesia and the time course of action. Materials and Methods: Analgesia was studied in albino rats using formalin test and in albino mice using ...

Ahmed Mushtaq; Upadhyaya Prerna; Seth Vikas

224

Comparison of postoperative analgesic effect of intrathecal magnesium and fentanyl added to bupivacaine in patients undergoing lower limb orthopedic surgery.  

UK PubMed Central (United Kingdom)

OBJECTIVE: To compare the analgesic efficacy and side effects of magnesium and fentanyl as an additive to intrathecal bupivacaine. METHODS: Ninety adult patients scheduled for femur surgery under spinal anesthesia were randomly allocated to one of the following three groups to receive intrathecally: bupivacaine 15 mg combined with 0.5 mL magnesium 10%; bupivacaine 15 mg combined with 0.5 mL fentanyl; or bupivacaine 15 mg combined with 0.5 mL distilled water (control). The time to first analgesic request, sensory and motor blockade onset time, duration of sensory and motor blockade, analgesic requirement in the first 12 hours after surgery, and the incidences of hypotension, bradycardia, hypoxemia and ephedrine were recorded. RESULTS: Magnesium caused a significant delay in the onset of both sensory and motor blockade compared with the fentanyl (95% CI 3 to 4; p < 0.001) and control (95% CI 3.5-5; p < 0.001) groups. The duration of spinal analgesia in group F (fentanyl) was significantly greater than in group C (control) (95% CI 365-513; p < 0.001) and group M (magnesium) (95% CI 385-523; p < 0.001). The total amount of methadone consumption over 12 hours was significantly lower in the magnesium and fentanyl groups than in the control group (5 mg vs. 5.666 ± 1.728 mg; p = 0.04). CONCLUSION: Addition of intrathecal magnesium sulfate to spinal anesthesia induced by bupivacaine significantly prolonged the onset of both sensory and motor blockade compared with fentanyl. Although magnesium failed to prolong the time to first analgesic requirement as seen with fentanyl, it reduced the total consumption of opioids in the first 12 hours postoperatively compared with the control group.

Khezri MB; Yaghobi S; Hajikhani M; Asefzadeh S

2012-03-01

225

[Evaluation of the analgesic effects of the lumiracoxib compared with placebo in the 24 first postoperative hours].  

UK PubMed Central (United Kingdom)

OBJECTIVES: To test lumiracoxib used preemptively against a placebo,and to analyse the analgesic administration (dipirona and tramadol) in the 24 first postoperative hours. METHODS: Sixty patients undergone to a breast aumentation, under epidural anesthesia, were selected and put randomly in two groups - GI and GII. Sixty minutes before the surgery, it was administered orally, one pill of lumiracoxib 400mg to the 30 GI patients and one pill of placebo to the 30 GII patients. The postoperative pain was evaluated through the visual analogic scale, ranged from 0 (painless) to 10 (most intensive pain), being applied to the patient whenever having pain. For the same scores or under 4, it was administered intravenously 15mg/kg of dipirona up to a maximum of 1g. For scores of 5, 6 or 7, the patient had intravenously 50mg of tramadol.Scores 8 or more were treated intravenously with 0,5 mg/kg of meperidine. RESULTS: The scores in GI were significantly lower than the ones obtained in GII within the first 24 hours, with the need of 20% less dipirona and 56% of tramadol in this period of time. In the same way, it was observed that analgesic solicitation for the first time had a delay of 191 minutes in GI in comparison to GII. CONCLUSION: The use of lumiracoxib preemptively, was effective in the treatment of postoperative pain, reducing considerably the consume of analgesics, and enlarging the time for the first medication.

Molon V; Kruel CD; Maioli DT; Caran JZ; Lovison RC

2009-02-01

226

Action at the mu receptor is sufficient to explain the supraspinal analgesic effect of opiates.  

UK PubMed Central (United Kingdom)

Mu, delta and kappa opiate receptors have been implicated in the production of analgesia. In order to study the relative contributions of these receptor types to supraspinally mediated analgesia, apparent pA2 values and rank order potencies were determined for i.c.v. injected highly selective opioid agonists in the mouse using a thermal nociceptive test. Drugs used included the prototypical mu agonist morphine, putative mu agonists [D-Ala2, N-methyl-Phe4, Gly5-ol] enkephalin and BAM 22P, putative delta agonists [D-Pen2, D-Pen5] enkephalin, [D-Thr2, Thr6, Leu5] enkephalin and [D-Ser2, Leu5, Thr6] enkephalin and the putative kappa agonists [trans-3,4-dichloro-N-methyl-N[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide methane sulfonate hydrate] and Dynorphin A (1-13). We were unable to demonstrate significant analgesic potencies for i.c.v. injected Dynorphin A (1-13) or BAM 22P in the absence of marked behavioral abnormalities. The rank order potency of the remaining compounds studied was found to be: [D-Ala2, N-methyl-Phe4, Gly5-ol] enkephalin greater than [D-Thr2, Thr6, Leu5] enkephalin greater than [D-Ser2, Leu5, Thr6] enkephalin greater than Morphine greater than [D-Pen2, D-Pen5] enkephalin greater than [trans-3, 4-dichloro-N-methyl-N[2-(1-pyrrolidinyl)-cyclohexyl]-benzeneacetamide methane sulfonate hydrate]. Apparent pA2 values of morphine, [D-Ala2, N-methyl-Phe4, Gly5-ol] enkephalin and [D-Pen2, D-Pen5] enkephalin in naloxone antagonism trials did not differ significantly. These results indicate that although both mu- and delta-selective ligands produce potent analgesia, a single receptor (mu) is sufficient to explain the supraspinal effects of opiate drugs.

Fang FG; Fields HL; Lee NM

1986-09-01

227

Cardiopulmonary and analgesic effects of caudal epidurally administered ropivacaine in cattle.  

UK PubMed Central (United Kingdom)

OBJECTIVE: To assess cardiopulmonary and analgesic effects after administration of ropivacaine into the caudal epidural space of cattle. STUDY DESIGN: Prospective, single-dose trial. ANIMALS: Eight healthy mixed breed cows aged 8 ± 5 years and weighing 507 ± 112 kg. METHODS: Caudal epidural anesthesia was produced in cows with 0.75% ropivacaine (0.11 mg kg(-1)). Onset time, duration and cranial spread of analgesia were recorded. Heart rate (HR), respiratory rate (f(R)), rectal temperature (RT), and mean arterial blood pressure (MAP) were measured prior to epidural administration (T(0) ) and at 15, 30, 60, 120, 180 and 240 minutes after epidural administration (T(15), T(30), T(60) , T(120) , T(180) and T(240) ). Arterial blood acid-base balance (pH, standard bicarbonate and base excess), gas tension (PaO(2), PaCO(2), SaO(2)) and electrolytes (Na(+), K(+), iCa(2+),Cl(-)) were recorded at T(0), T(30), T(60), T(120), T(180) and T(240). Ataxia was evaluated at T(0), T(30), T(60), T(120), T(180) and T(240) and at 1 hour intervals thereafter until analgesia was no longer present in each animal. RESULTS: Epidurally administered ropivacaine induced variable analgesia extending bilaterally from the coccyx to S3. Time to onset of analgesia and mean duration in the perineal area were 15 ± 4 and 359 ± 90 minutes, respectively. Respiratory rate and RT increased from T(120) to T(240) when compared to the value at T(0) . Ionized calcium and chloride concentrations increased at T(180) and T(240) when compared to T(0). The other variables were not significantly different from baseline values (p > 0.05). Four animals were mildly ataxic. CONCLUSION AND CLINICAL RELEVANCE: Ropivacaine (0.75%, 0.11 mg kg(-1)) can be administered by caudal epidural injection to produce prolonged bilateral perineal analgesia with minimal ataxia and cardiopulmonary changes in standing cattle.

Araújo MA; Albuquerque VB; Deschk M; Santos GG; Rodrigues CA; Oliva VN; Santos PS

2012-07-01

228

Induction of anesthesia in coronary artery bypass graft surgery: the hemodynamic and analgesic effects of ketamine  

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Full Text Available OBJECTIVE: The aim of this prospective, randomized study was to evaluate the hemodynamic and analgesic effects of ketamine by comparing it with propofol starting at the induction of anesthesia until the end of sternotomy in patients undergoing coronary artery bypass grafting surgery. INTRODUCTION: Anesthetic induction and maintenance may induce myocardial ischemia in patients with coronary artery disease. A primary goal in the anesthesia of patients undergoing coronary artery bypass grafting surgery is both the attenuation of sympathetic responses to noxious stimuli and the prevention of hypotension. METHODS: Thirty patients undergoing coronary artery bypass grafting surgery were randomized to receive either ketamine 2 mg.kg-1 (Group K) or propofol 0.5 mg.kg-1 (Group P) during induction of anesthesia. Patients also received standardized doses of midazolam, fentanyl, and rocuronium in the induction sequence. The duration of anesthesia from induction to skin incision and sternotomy, as well as the supplemental doses of fentanyl and sevoflurane, were recorded. Heart rate, mean arterial pressure, central venous pressure, pulmonary arterial pressure, pulmonary capillary wedge pressure, cardiac index, systemic and pulmonary vascular resistance indices, stroke work index, and left and right ventricular stroke work indices were obtained before induction of anesthesia; one minute after induction; one, three, five, and ten minutes after intubation; one minute after skin incision; and at one minute after sternotomy. RESULTS: There were significant changes in the measured and calculated hemodynamic variables when compared to their values before induction. One minute after induction, mean arterial pressure and the systemic vascular resistance index decreased significantly in group P (p<0.01). CONCLUSION: There were no differences between groups in the consumption of sevoflurane or in the use of additional fentanyl. The combination of ketamine, midazolam, and fentanyl for the induction of anesthesia provided better hemodynamic stability during induction and until the end of sternotomy in patients undergoing coronary artery bypass grafting surgery.

Elif Basagan-Mogo; Suna Goren; Gulsen Korfali; Gurkan Turker; Fatma Nur Kaya

2010-01-01

229

Induction of anesthesia in coronary artery bypass graft surgery: the hemodynamic and analgesic effects of ketamine  

Scientific Electronic Library Online (English)

Full Text Available Abstract in english OBJECTIVE: The aim of this prospective, randomized study was to evaluate the hemodynamic and analgesic effects of ketamine by comparing it with propofol starting at the induction of anesthesia until the end of sternotomy in patients undergoing coronary artery bypass grafting surgery. INTRODUCTION: Anesthetic induction and maintenance may induce myocardial ischemia in patients with coronary artery disease. A primary goal in the anesthesia of patients undergoing coronary ar (more) tery bypass grafting surgery is both the attenuation of sympathetic responses to noxious stimuli and the prevention of hypotension. METHODS: Thirty patients undergoing coronary artery bypass grafting surgery were randomized to receive either ketamine 2 mg.kg-1 (Group K) or propofol 0.5 mg.kg-1 (Group P) during induction of anesthesia. Patients also received standardized doses of midazolam, fentanyl, and rocuronium in the induction sequence. The duration of anesthesia from induction to skin incision and sternotomy, as well as the supplemental doses of fentanyl and sevoflurane, were recorded. Heart rate, mean arterial pressure, central venous pressure, pulmonary arterial pressure, pulmonary capillary wedge pressure, cardiac index, systemic and pulmonary vascular resistance indices, stroke work index, and left and right ventricular stroke work indices were obtained before induction of anesthesia; one minute after induction; one, three, five, and ten minutes after intubation; one minute after skin incision; and at one minute after sternotomy. RESULTS: There were significant changes in the measured and calculated hemodynamic variables when compared to their values before induction. One minute after induction, mean arterial pressure and the systemic vascular resistance index decreased significantly in group P (p

Basagan-Mogo, Elif; Goren, Suna; Korfali, Gulsen; Turker, Gurkan; Kaya, Fatma Nur

2010-01-01

230

Analgesic, CNS Depressant and Anthelmintic Activity of Sarcostemma viminale  

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Full Text Available Various extracts of Sarcostemma viminale were screened for central analgesic activity by hot plate test, peripheral analgesic activity by acetic acid-induced writhings, CNS depressant activity by pentobarbitone-induced sleep and locomotor activity testing methods and anthelmintic activity on the earthworms Pheretima posthuma. Results showed that petroleum ether and ethyl acetate extracts had good central analgesic activity; ethyl acetate and methanol extracts had good peripheral analgesic activity; chloroform and ethyl acetate extracts had good CNS depressant activity and methanol extract had good anthelmintic activity.

Aboli S Girme; Sunil A Nirmal; Rasika D Bhalke; Machindra J Chavan

2008-01-01

231

Possible role for integrins in the development of tolerance to the analgesic effect of morphine in male rats  

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Full Text Available There is some evidence supporting the reduced activity of integrins following chronic administration of morphine. This reduction might play a role in morphine tolerance development. Manganese binds to the extracellular domain of integrins and makes them to be activated. The effect of integrins activation using manganese on tolerance development to the analgesic effect of morphine was investigated in this study. Methods: To induce tolerance to analgesic effect of morphine, morphine (15 ?g/rat) was injected intrathecally (i.t.) to male adult Wistar rats twice a day for five days. To investigate the effect of manganese, it was injected (20 nmol/rat-i.t.) 15 minutes prior to morphine injections during mentioned period. The analgesic effect of morphine (15 ?g/rat) was measured using tail flick test on day 6. Results: The results indicated that in animals which received both manganese and morphine during first 5 days, morphine induced a significant analgesia on day 6. Chronic administration of manganese did not change the pain threshold and morphine induced analgesia. Comparison of morphine analgesia following a single dose of morphine (15 ?g/rat) or chronic manganese+morphine, indicated that manganese did not have any effect on the morphine analgesia. Conclusion: Our results showed that, manganese administration prior to morphine is able to prevent morphine tolerance development. It seems that decreased activity of integrins following chronic administration of morphine plays a pivotal role in tolerance development to morphine analgesia. Further investigation needs to determine whether manganese effect is dependent on the integrins role in cell adhesions, or on their intracellular signaling pathways.

Jamal Ghorbi; Mohammad Javan; Vahid Sheibani; Leila Satarian; Amir Zarebkohan

2007-01-01

232

The analgesic effect of Magnesium Sulfate in postoperative pain of inguinal hernia repair  

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Full Text Available Background: Magnesium Sulfate (MgSO4) has been used as a pharmacologic agent in different situations for many years in the treatment of tachyarrhythmias, myocardial ischemia, preeclampsia, and tocolysis among others. The analgesic effect of MgSO4 for postoperative pain has been used since the 1990s. Postoperative pain is one of the most common complications in the perioperative period and can result in serious consequences in different organs if left untreated. Inguinal herniorrhaphy is among the most common surgeries and is almost always accompanied by severe pain. The object of this study is to determine the effect of a pre-induction infusion of MgSO4 on the reduction of postsurgical pain after herniorrhaphy. Methods: This double-blind, randomized clinical trial included 105 ASA class I and class II herniorrhaphy patients at Shariati Hospital in years 2004 and 2005. For statistical analysis, the ?2 and T tests were used. The patients were divided into three groups based on block randomization. Patients in the following groups received: Group A, 200 ml of normal saline infusion (placebo); Group B, 25 mg/kg MgSO4 in 200 ml of normal saline; Group C, 50 mg/kg MgSO4 in 200 ml of normal saline. All groups were infused twenty minutes before induction of anesthesia using identical methods and dosage in all three groups. Heart rate and mean arterial pressure (MAP) at pre- and postintubation and so at skin incision time were charted. Visual analog scale (VAS) pain score, nausea, vomiting and the amount of morphine used before recovery room discharge and in six, twelve and twenty-four hours after recovery discharge was recorded. Results: The average age for the different groups was as follows: Group A: 33.6, Group B: 37.37, Group C: 32.74. Nausea and vomiting between the case and control groups were not statistically different (60% vs. 71.4%, p=0.0499), nor was the amount of Morphine used. On recovery room discharge, the VAS scores were 8.1, 7.2, and 5.5 for the first, second and third groups, respectively (P<0.001). However, no statistical significance was found for the VAS scores six hours after recovery room discharge. Conclusion: The results in this study show that pre-induction with MgSO4 has no remarkable effect on decreasing postoperative pain or morphine use for inguinal herniorrhaphy.

Mehraein A; Azad M A; Sadeghi M

2007-01-01

233

Differential analgesic effect of tenoxicam on post-cesarean uterine cramping pain between primiparous and multiparous women.  

UK PubMed Central (United Kingdom)

BACKGROUND AND PURPOSE: Uterine cramping pain is related to prostaglandins, which are mediated by cyclooxygenase. However, it is unknown whether the analgesic effects of the non-selective cyclooxygenase inhibitor tenoxicam are different between primiparous and multiparous women. This placebo-controlled, double-blind study compared the analgesic effect of tenoxicam on post-cesarean uterine cramping pain in primiparous and multiparous women. METHODS: Forty primiparous women and 40 multiparous women who were scheduled for elective cesarean delivery were allocated into the following 4 groups: saline-primipara (SP) group, tenoxicam-primipara (TP) group, saline-multipara (SM) group, and tenoxicam-multipara (TM) group. Saline or 20 mg tenoxicam was intravenously injected immediately after clamping of the umbilical cord. All patients received patient-controlled analgesia for postoperative pain control. Resting wound pain, uterine cramping pain, morphine consumption, and morphine-related side effects were evaluated at 4 and 24 hours after surgery. RESULTS: At 24 hours after surgery, tenoxicam-related relief of uterine cramping pain was 2.1 in primiparous women (visual analog scale: SP 5.6 (4.4-6.8) minus TP 3.5 (2.2-4.9); p < 0.01). The tenoxicam-related morphine-sparing effect was 14 mg (45%) in primiparous women (SP 31.4 mg (23.9-38.8) minus TP 17.4 mg (11.6-23.2); p < 0.01). The tenoxicam-related relief of uterine cramping pain and tenoxicam-related morphine-sparing effect were not significant in multiparous women. CONCLUSIONS: This study revealed that the analgesic effect of tenoxicam on post-cesarean uterine cramping pain is greater in primiparous women than in multiparous women. Further studies are required to determine whether a higher dosage of tenoxicam is beneficial to reduce uterine cramping pain in multiparous women.

Yeh YC; Chen SY; Lin CJ; Yeh HM; Sun WZ

2005-09-01

234

Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives.  

UK PubMed Central (United Kingdom)

We report the design, the synthesis and the biological evaluation of the analgesic and anti-inflammatory activities of furoxanyl N-acylhydrazones (furoxanyl-NAH) by applying molecular hybridization approach. Hybrid compounds with IL-8-release inhibition capabilities were identified. Among them, furoxanyl-NAH, 17, and benzofuroxanyl-derivative, 24, together with furoxanyl-NAH derivative, 31, without IL-8 inhibition displayed both orally analgesic and anti-inflammatory activities. These hybrid derivatives do not have additional LOX- or COX-inhibition activities. For instance, LOX-inhibition by furoxanyl-NAH derivative, 42, emerged as a structural lead to develop new inhibitors. The lack of mutagenicity of the active derivatives 17, 31, and 42, allow us to propose them as candidates for further clinical studies. These results confirmed the success in the exploitation of hybridization strategy for identification of novel N-acylhydrazones (NAH) with optimized activities.

Hernández P; Cabrera M; Lavaggi ML; Celano L; Tiscornia I; Rodrigues da Costa T; Thomson L; Bollati-Fogolín M; Miranda AL; Lima LM; Barreiro EJ; González M; Cerecetto H

2012-03-01

235

Evaluation of the Anti-inflammatory, Analgesic, and Anti-pyretic Effects of Origanum majorana Ethanolic Extract in Experimental Animals  

International Nuclear Information System (INIS)

In the present investigation, various biological studies (toxicological, pharmacological, biochemical and histopathological) were carried out on Origanum majorana ethanolic extract. The acute toxicity study revealed that 0. majorana ethanolic extract is quietly safe. Both doses (0.25 and 0.5 g/kg b.wt.) of 0. majorana ethanolic extract showed a significant anti-inflammatory (acute and systemic), analgesic, and anti-pyretic effect. Moreover, histopathological findings of stomach and intestine of irradiated rats revealed that both doses of tested extract possess a gastrointestinal protective effect against radiation induced gastritis and enteritis

2009-01-01

236

Effect of a pharmacist on timing of postintubation sedative and analgesic use in trauma resuscitations.  

UK PubMed Central (United Kingdom)

PURPOSE: Pharmacists' impact in reducing the time interval from intubation to sedative and analgesic use during trauma patient resuscitations is investigated. METHODS: A retrospective cohort study was conducted at a level 1 trauma center to compare medication-use outcomes in consecutive cases in which trauma patients underwent rocuronium-assisted rapid-sequence intubation (RSI) and subsequent sedation and analgesia with or without a pharmacist's participation on the resuscitation team. The primary and secondary outcomes were, respectively, the time to sedative provision and the time to analgesic provision after intubation. RESULTS: Relative to resuscitation cases not involving a pharmacist, the presence of the pharmacist during RSI was associated with decreased mean times to provision of postintubation sedation (9 minutes versus 28 minutes, p = 0.007) and analgesia (21 minutes versus 44 minutes, p = 0.057). The cumulative proportions of patients receiving appropriate sedation 5, 10, and 15 minutes after intubation were 11%, 26%, and 41% in the pharmacist-absent group and 33%, 53%, and 63% in the pharmacist-present group (p = 0.009, 0.008, and 0.045, respectively); for postintubation analgesic use, the corresponding figures were 9%, 14%, and 23% in the pharmacist-absent group and 17%, 30%, and 43% in the pharmacist-present group (p = 0.236, 0.066, and 0.039, respectively). CONCLUSION: The presence of a pharmacist during RSI procedures was associated with decreased times to postintubation sedative and analgesic use, indicating that pharmacist participation in trauma-resuscitation responses can facilitate appropriate drug therapy.

Amini A; Faucett EA; Watt JM; Amini R; Sakles JC; Rhee P; Erstad BL; Patanwala AE

2013-09-01

237

Antiinflammatory and Analgesic Effects of Phlomis lanceolata Boiss. and Hohen. Extracts and Examination of their Components  

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Full Text Available The purpose of this investigation was to study the anti-inflammatory and analgesic properties of total extract and four fractions (ether, ethyl acetate, n-butanol and water) from Phlomis lanceolata (Lamiaceae) in mice. The plant material was extracted with methanol. In order to estimate the polarity of the active compounds, the total extract was dissolved in water and the water soluble portion was successively partitioned between ether, ethyl acetate and n-buthanol. The total extract and four fractions were analyzed by Thin Layer Chromatography (TLC) by use of specific reagents. Dose of 100 mg kg 1 of each extracts were used in carrageenan-induced paw edema, formalin and writhing nociception tests in mice. All compounds reduced paw edema in comparison to the control group at 1, 3, 5 and 7 h post carrageenan injection. The total, ether and aqueous extracts were similar to indomethacin while the ethyl acetate extract was weaker than indomethacin in reduction of paw edema. All extracts induced antinociception in both phases of formalin test. The total and ether extracts were as potent as indomethacin in both phases of formalin test. The ethyl acetate extract was weaker than indomethacin in the second phase of formalin-test while the n-butanol and aqueous extracts showed more antinociception than indomethacin in the second phase of formalin test. All extracts as well as indomethacin induced antinociception in writhing test in comparison to control. The total and aqueous extracts induced the same antinociception as indomethacin while ether, ethyl acetate and n-butanol showed weaker antinociception than indomethacin. Positive results for iridoids and phenolic compounds were indicated by phytochemical analysis of total extract. Phenolic compounds were found in four fractions whereas only n-butanol and aqueous fractions showed positive results for iridoid glycosides. The higher antinociceptive effects of n-butanol and aqueous extracts in the inflammatory phase of formalin test among different extracts tested, might back to the presence of iridoid glycosides, phenolic glycosides or other glycosides. These data suggest that different extracts of P. lanceolata produce different antinociceptive activities that could be due to the effect of one or a combination of the bioactive components in each extract.

M. Mohajer; P. Sarkhail; N. Hajarolasvadi; M.J. Zamani; R. Khorasani; A. Shafiee; G. Amin; M. Abdollahi

2006-01-01

238

Intra- and post-operative analgesic effects of carprofen in medetomidine premedicated dogs undergoing ovariectomy  

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Full Text Available Intra- and post-operative analgesic effects of pre-operative administration of carprofen were investigated in 16 medetomidine-premedicated dogs undergoing elective ovariectomy. Dogs were randomly allocated into carprofen (n=8; 4 mg/kg, intramuscularly) or placebo group (n = 8). After medetomidine (1000 [xg/m2, intramuscularly) premedication, they were induced with propofol (1 mg/kg, intravenously) and maintained with isoflurane (FE'ISO 1.0 %) in 100% oxygen. During anaesthesia, the analgesia was assessed in terms of changes in heart rate, respiratory rate and arterial blood pressure as a response to the surgery. Assessments of post-operative sedation (simple numerical rating scale) and pain (multifactorial pain scale) were made at 15 minutes, 30 minutes, 1,2,3, 4, 5, and 6 hours after the surgery. In addition, pulse rate, respiratory rate and body temperature were measured at the same time. During anaesthesia, lower heart rate, respiratory rate and mean arterial blood pressure and higher tidal volume of respiration were observed in the carprofen group. Post-operative pain score was relatively low in both groups of dogs, however it was higher, but not significantly, in the placebo group. There was no difference between the groups in terms of respiratory and pulse rate after surgery. The post-operative sedation score was higher in the placebo group only in the early post-operative period most probably due to misinterpretation of pain behaviour. Carprofen together with other anaesthetic drugs provided sufficient intra-operative analgesia only until major painful surgical stimulus occurred, after which analgesia had to be supplemented with a subanaesthetic dose of ketamine. Comparing to that analgesia was insufficient in the placebo group throughout the procedure. The post-operative pain scoring system was probably not sensitive enough to detect the differences between the groups; however, the effects of other drugs that extended in the post-operative period may be responsible for a low post­operative pain score in both groups of dogs.

Seliškar Alenka; Rostaher Ana; Ostrouška Maja; Butinar J.

2005-01-01

239

Continuous peripheral nerve blockade for postoperative analgesia.  

UK PubMed Central (United Kingdom)

PURPOSE OF REVIEW: To review the recent literature involving the use of continuous peripheral nerve sheath catheters in the management of postoperative pain. RECENT FINDINGS: Continuous peripheral nerve blocks provide superior analgesia and are associated with fewer opioid-induced side effects for patients undergoing extremity surgery. Ultrasound technology is being used with increasing frequency to guide the placements of continuous peripheral nerve blocks. The evidence is still equivocal regarding the superiority of stimulating versus nonstimulating catheters for the delivery of continuous peripheral nerve blockade. The incidence of major complications associated with continuous peripheral nerve blocks is very low and probably no different from single injection peripheral nerve blocks. SUMMARY: Continuous peripheral nerve blocks are an excellent additional modality to compliment other multimodal analgesics to control moderate to severe postoperative pain.

Le-Wendling L; Enneking FK

2008-10-01

240

Analgesic efficacy and safety of the novel p38 MAP kinase inhibitor, losmapimod, in patients with neuropathic pain following peripheral nerve injury: a double-blind, placebo-controlled study.  

UK PubMed Central (United Kingdom)

BACKGROUND: Inhibitors of p38 mitogen-activated protein kinase are undergoing evaluation as a novel class of anti-rheumatic drugs, by virtue of their ability to suppress the production of pro-inflammatory cytokines. Emerging data suggests that they may also attenuate peripheral or central sensitization in neuropathic pain. A double-blind, placebo-controlled study was undertaken to evaluate the analgesic efficacy of losmapimod (GW856553), a novel p38?/? inhibitor, in subjects with neuropathic pain following traumatic peripheral nerve injury. METHODS: One hundred and sixty-eight subjects with pain of at least moderate intensity (average daily score ?4 on an 11-point pain intensity numeric rating scale; PI-NRS) at baseline were randomized to receive oral losmapimod, 7.5?mg BID or placebo for 28?days. Efficacy and safety assessments were undertaken at weekly clinic visits. RESULTS: The mean treatment difference for the change in average daily pain score from baseline to week 4 of treatment based on the PI-NRS was -0.22 (95% CI -0.73, 0.28) in favour of losmapimod over placebo (p?=?0.39). There were no statistically significant or clinically meaningful differences between the treatment groups over the 4-week dosing period for either the primary or secondary efficacy variables. There were no unexpected safety or tolerability findings following dosing with losmapimod. CONCLUSIONS: Losmapimod could not be differentiated from placebo in terms of a primary analgesia response in patients with pain following peripheral nerve injury. The lack of response could reflect inadequate exposure at central sites of action or differences between rodent and human with respect to the target or neuropathic pain mechanisms.

Ostenfeld T; Krishen A; Lai RY; Bullman J; Baines AJ; Green J; Anand P; Kelly M

2013-07-01

 
 
 
 
241

Local peripheral antinociceptive effects of 14-O-methyloxymorphone derivatives in inflammatory and neuropathic pain in the rat.  

Science.gov (United States)

Antinociception achieved after peripheral administration of opioids has opened a new approach to the treatment of severe and chronic pain. Additionally, opioid analgesics with restricted access to the central nervous system could improve safety of opioid drugs used in clinical practice. In the present study, peripheral components of antinociceptive actions of 6-amino acid-substituted derivatives of 14-O-methyloxymorphone were investigated after local intraplantar (i.pl.) administration in rat models of inflammatory and neuropathic pain. Their antinociceptive activities were compared with those of morphine, the classical mu-opioid receptor agonist. Intraplantar administration of morphine and the 6-amino acid derivatives produced dose-dependent reduction of formalin-induced flinching of the inflamed paw, without significant effect on the paw edema. Local i.pl. administration of the new derivatives in rats with neuropathic pain induced by sciatic nerve ligation produced antiallodynic and antihyperalgesic effects; however, the antinociceptive activity was lower than that observed in inflammatory pain. In both models, the 6-amino acid derivatives and morphine at doses that produced analgesia after i.pl. administration were systemically (s.c.) much less active indicating that the antinociceptive action is due to a local effect. Moreover, the local opioid antinociceptive effects were significantly attenuated by naloxone methiodide, a peripherally acting opioid receptor antagonist, demonstrating that the effect was mediated by peripheral opioid receptors. The present data indicate that the peripherally restricted 6-amino acid conjugates of 14-O-methyloxymorphone elicit antinociception after local administration, being more potent in inflammatory than in neuropathic pain. Opioid drugs with peripheral site of action can be an important target for the treatment of long lasting pain. PMID:17204264

Obara, Ilona; Makuch, Wioletta; Spetea, Mariana; Schütz, Johannes; Schmidhammer, Helmut; Przewlocki, Ryszard; Przewlocka, Barbara

2006-11-25

242

Assessment of the analgesic effect of remifentanil using three pain models in healthy Korean volunteers: a randomized, controlled study.  

UK PubMed Central (United Kingdom)

Quantitative pain assessment in human beings is useful for developing new analgesics. This study assessed the analgesic effect of remifentanil in 20 healthy Korean men using three pain models to investigate whether these models can be used in Asians. The study was a double-blind, placebo-controlled, two-way cross-over study. The subjects received intravenous remifentanil with doses starting at 0.01 ?g/kg/min. and increasing by 0.01 ?g/kg/min. up to 0.10 ?g/kg/min. in one session; they received placebo in another session. Heat pain thresholds were assessed at dose levels of 0.02, 0.05, 0.08 and 0.10 ?g/kg/min. Pressure pain threshold and tolerance and mechanical pain threshold were assessed at 0.08 ?g/kg/min. Remifentanil dose-dependently increased the heat pain threshold. The differences (95% confidence interval) between remifentanil and placebo were 1.54°C (0.78, 2.31), 1.82°C (1.11, 2.54) and 2.47°C (1.55, 3.38) at 0.05, 0.08 and 0.10 ?g/kg/min. remifentanil, respectively. Remifentanil conferred a significantly higher pressure pain threshold and tolerance than placebo (p = 0.0001). There was a trend of increasing mechanical pain threshold with remifentanil, although it was not statistically significant. The results suggest that heat pain and pressure pain models are valid in East Asians for assessing analgesic effects.

Kim TE; Kim KP; Shin D; Chung YJ; Price J; Mistry P; Jang IJ; Yu KS

2012-06-01

243

Analgesic , anti-inflammatory and antipyretic activity of Cissus quadrangularis  

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Full Text Available This study was intended to evaluate the analgesic anti-inflammatory and antipyretic activity of ethanolic extract of Cissus quadrangularis in experimental standard modals i.e. albino rats following oral administration. The results showed that the ethanolic extractsignificantly reduce the edema induced by carrageenan within 1 to 5 hrs. post dosing at all the dose levels used. On the analgesic property acetic acid induce writhing was significantly reduce in the formalin test, the extract also significantly decreases thepainful stimulus in both phases of test which confirms central and peripheral effects of the drugs. Its effects on antipyretic activity were also appreciable it significantly reduces fever at higher doses within 2 hrs. on yeast induce hyperthermia in rats.

Priyanka Vijay; Rekha Vijayvergia

2010-01-01

244

Involvement of Y(5) receptors in neuropeptide Y agonist-induced analgesic-like effect in the rat hot plate test.  

UK PubMed Central (United Kingdom)

Neuropeptide Y (NPY) induces analgesic-like effects after central administration across diverse pain models in rodents. In spinal pain models, previous studies indicate a prominent role for Y(1) receptors at mediating this effect of NPY. In supraspinal pain models like the hot plate test, the NPY receptors involved have not been thoroughly explored. By intracerebroventricular (i.c.v.) administration of selective NPY receptor ligands, the possible involvement of Y(5) receptors in analgesic-like mechanisms was investigated using the hot plate test in rats. Both NPY and selective Y(5) agonists induced analgesic-like effects as revealed by prolonged hot plate latencies. Further consistent with a role for Y(5) receptors, pretreatment with a selective Y(5) receptor antagonist blocked the Y(5) agonist-induced analgesic-like effect. The present study indicates involvement of Y(5) receptors probably at the supraspinal level in mediation of NPY agonist-induced analgesic-like effects in the hot plate test.

Thomsen M; Wörtwein G; Olesen MV; Begtrup M; Havez S; Bolwig TG; Woldbye DP

2007-06-01

245

Involvement of Y(5) receptors in neuropeptide Y agonist-induced analgesic-like effect in the rat hot plate test.  

Science.gov (United States)

Neuropeptide Y (NPY) induces analgesic-like effects after central administration across diverse pain models in rodents. In spinal pain models, previous studies indicate a prominent role for Y(1) receptors at mediating this effect of NPY. In supraspinal pain models like the hot plate test, the NPY receptors involved have not been thoroughly explored. By intracerebroventricular (i.c.v.) administration of selective NPY receptor ligands, the possible involvement of Y(5) receptors in analgesic-like mechanisms was investigated using the hot plate test in rats. Both NPY and selective Y(5) agonists induced analgesic-like effects as revealed by prolonged hot plate latencies. Further consistent with a role for Y(5) receptors, pretreatment with a selective Y(5) receptor antagonist blocked the Y(5) agonist-induced analgesic-like effect. The present study indicates involvement of Y(5) receptors probably at the supraspinal level in mediation of NPY agonist-induced analgesic-like effects in the hot plate test. PMID:17498669

Thomsen, Morgane; Wörtwein, Gitta; Olesen, Mikkel V; Begtrup, Mikael; Havez, Sophie; Bolwig, Tom G; Woldbye, David P D

2007-04-13

246

Analgesic effect of auricular acupuncture for cancer pain: a randomized, blinded, controlled trial.  

UK PubMed Central (United Kingdom)

PURPOSE: During the last 30 years, auricular acupuncture has been used as complementary treatment of cancer pain when analgesic drugs do not suffice. The purpose of this study is to examine the efficacy of auricular acupuncture in decreasing pain intensity in cancer patients. PATIENTS AND METHODS: Ninety patients were randomly divided in three groups; one group received two courses of auricular acupuncture at points where an electrodermal signal had been detected, and two placebo groups received auricular acupuncture at points with no electrodermal signal (placebo points) and one with auricular seeds fixed at placebo points. Patients had to be in pain, attaining a visual analog score (VAS) of 30 mm or more after having received analgesic treatment adapted to both intensity and type of pain, for at least 1 month of therapy. Treatment efficacy was based on the absolute decrease in pain intensity measured 2 months after randomization using the VAS. RESULTS: The main outcome was pain assessed at 2 months, with the assessment at 1 month carried over to 2 months for the eight patients who interrupted treatment after 1 month. For three patients, no data were available because they withdrew from the study during the first month. Pain intensity decreased by 36% at 2 months from baseline in the group receiving acupuncture; there was little change for patients receiving placebo (2%). The difference between groups was statistically significant (P <.0001). CONCLUSION: The observed reduction in pain intensity measured on the VAS represents a clear benefit from auricular acupuncture for these cancer patients who are in pain, despite stable analgesic treatment.

Alimi D; Rubino C; Pichard-Léandri E; Fermand-Brulé S; Dubreuil-Lemaire ML; Hill C

2003-11-01

247

Analgesic Treatment in Patients With Acute Extremity Trauma and Effect of Training  

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Full Text Available Objectives: Studies indicate that emergency physicians (EP) under-evaluate and undertreat the pain experienced by their patients. The objective of this study was to investigate how EPs treat pain in adult patients with limb trauma and to determine if their behavior could be affected by training in the short-term. Methods: All consecutive adult patients admitted to the university-based emergency department (ED) within two months were enrolled in the study. The patients were asked to rate their level of pain on the NRS in triage. NRS scores were noted again after 30 minutes and 60 minutes, and on discharge. Patient prescriptions were also tracked to identify any analgesics. After completion of the pre-education phase, four hours of training on pain evaluation and treatment were undertaken under the leadership of experienced staff faculty. The aforementioned outcomes were gathered again in a 30-day period after training and we compared the pre and post training periods. Results: A hundred and forty-three patients (81 female) were enrolled in the pre-education phase, and 130 patients (58 female) were eligible for the post-education phase. The mean NRS scores of the females noted on admission were significantly higher than those of the males (7.4±2.3 vs. 6.7±2.5, respectively; p=0.020). Patients included in the first phase received analgesia less frequently (42.7% vs. 70.0%, respectively; p<0.001). The mean period of time between admission and initial analgesic administration was shorter in the second phase (41.3 vs. 19.3 minutes, respectively; p<0.001). The ratio of patients receiving analgesia within thirty minutes was greater after training. All patients in the second phase received analgesia within 60 minutes. The residents prescribed analgesics more frequently after training. Conclusions: A four-hour training program resulted in apparent changes in the residents’ management of pain in patients with extremity trauma. In addition to a more timely administration, the rates of analgesic treatment increased.

Funda KARBEK AKARCA; Özgür KARCIO?LU; Tanzer KORKMAZ; Bülent ERB?L; Ömer Faruk DEM?R

2012-01-01

248

Peripheral nerve toxic effects of nitrofurantoin.  

UK PubMed Central (United Kingdom)

OBJECTIVE: To investigate the role of skin biopsy in nitrofurantoin peripheral neuropathy. DESIGN: We describe the clinical features and skin biopsies of 2 cases of non-length-dependent small-fiber neuropathy/ganglionopathy attributable to nitrofurantoin. SETTING: Clinical evaluation and skin biopsies were performed at a tertiary teaching hospital in Baltimore, Maryland. PATIENTS: A 59-year-old woman with disabling generalized dysesthesia and a 53-year-old woman with progressive burning pain in the perineum and extremities. MAIN OUTCOME MEASURES: Slow or incomplete recovery and possibly irreversible damage. RESULTS: The neuropathy was neither dose dependent nor associated with impaired renal function. Results from nerve conduction studies were normal. Skin biopsies revealed distinctive morphologic changes with clustered terminal nerve swellings without evidence of nerve fiber degeneration. CONCLUSIONS: These distinct morphologic changes associated with nitrofurantoin have not been previously reported to our knowledge. Skin biopsy appears to be helpful in confirming the diagnosis in these patients.

Tan IL; Polydefkis MJ; Ebenezer GJ; Hauer P; McArthur JC

2012-02-01

249

Vagal afferent mediates the anorectic effect of peripheral secretin.  

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Secretin (SCT) is a classical peptide hormone that is synthesized and released from the gastrointestinal tract after a meal. We have previously shown that it acts both as a central and peripheral anorectic peptide, and that its central effect is mediated via melanocortin system. As peripheral satiety signals from the gastrointestinal tract can be sent to the brain via the vagal afferent or by crossing the blood-brain barrier (BBB), we therefore sought to investigate the pathway by which peripheral SCT reduces appetite in this study. It is found that bilateral subdiaphragmatic vagotomy and treatment of capsaicin, an excitotoxin for primary afferent neurons, could both block the anorectic effect of peripherally injected SCT. These treatments are found to be capable of blunting i.p. SCT-induced Fos activation in pro-opiomelanocortin (POMC) neurons within the hypothalamic Arcuate Nucleus (Arc). Moreover, we have also found that bilateral midbrain transaction could block feeding reduction by peripheral SCT. Taken together, we conclude that the satiety signals of peripheral SCT released from the gastrointestinal tract are sent via the vagus nerves to the brainstem and subsequently Arc, where it controls central expression of other regulatory peptides to regulate food intake. PMID:23738005

Chu, Jessica Y S; Cheng, Carrie Y Y; Sekar, Revathi; Chow, Billy K C

2013-05-30

250

Vagal afferent mediates the anorectic effect of peripheral secretin.  

UK PubMed Central (United Kingdom)

Secretin (SCT) is a classical peptide hormone that is synthesized and released from the gastrointestinal tract after a meal. We have previously shown that it acts both as a central and peripheral anorectic peptide, and that its central effect is mediated via melanocortin system. As peripheral satiety signals from the gastrointestinal tract can be sent to the brain via the vagal afferent or by crossing the blood-brain barrier (BBB), we therefore sought to investigate the pathway by which peripheral SCT reduces appetite in this study. It is found that bilateral subdiaphragmatic vagotomy and treatment of capsaicin, an excitotoxin for primary afferent neurons, could both block the anorectic effect of peripherally injected SCT. These treatments are found to be capable of blunting i.p. SCT-induced Fos activation in pro-opiomelanocortin (POMC) neurons within the hypothalamic Arcuate Nucleus (Arc). Moreover, we have also found that bilateral midbrain transaction could block feeding reduction by peripheral SCT. Taken together, we conclude that the satiety signals of peripheral SCT released from the gastrointestinal tract are sent via the vagus nerves to the brainstem and subsequently Arc, where it controls central expression of other regulatory peptides to regulate food intake.

Chu JY; Cheng CY; Sekar R; Chow BK

2013-01-01

251

Comparing the analgesic effect of heat patch containing iron chip and ibuprofen for primary dysmenorrhea: a randomized controlled trial  

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Full Text Available Abstract Background Primary dysmenorrhea is a common and sometimes disabling condition. In recent years, some studies aimed to improve the treatment of dysmenorrhea, and therefore, introduced several therapeutic measures. This study was designed to compare the analgesic effect of iron chip containing heat wrap with ibuprofen for the treatment of primary dysmenorrhea. Methods In this randomized (IRCT201107187038N2) controlled trial, 147 students (18–30?years old) with the diagnosis of primary dysmenorrhea were enrolled considering the CONSORT guideline. Screening for primary dysmenorrhea was done by a two-question screening tool. The participants were randomly assigned into one of the intervention groups (heat Patch and ibuprofen). Data regarding the severity and emotional impact of the pain were recorded by a shortened version of McGill Pain Questionnaire (SF-MPQ). Student's?t test was used for statistical analysis. Results The maximum and minimum pain severities were observed at 2 and 24?hours in both groups. The severity of sensual pain at 8, 12, and 24?hours was non-significantly less in the heat Patch group. There was also no significant difference between the groups regarding the emotional impact of pain at the first 2, 4, 8, 12 and 12?hours of menstruation. Conclusions Heat patch containing Iron chip has comparable analgesic effects to ibuprofen and can possibly be used for primary dysmenorrhea. Trial registration IRCT201107187038N2

Navvabi Rigi Shahindokht; kermansaravi Fatihe; Navidian Ali; Safabakhsh Leila; Safarzadeh Ameneh; Khazaian Somaye; Shafie Shahla; Salehian Tahmineh

2012-01-01

252

Comparing the analgesic effects of periaqueductal gray matter injection of orexin A and morphine on formalin- induced nociceptive behaviors.  

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Full Text Available Introduction: Orexin-A and B (Hypocretin 1 and 2) are neuropeptides that are mostly expressed in the posterior and lateral hypothalamus (LH). Intracisternal (ICV) and intratechal (IT) injections of orexin-A (hypocretin-1) have been shown to elicit analgesic responses in formalin test. However, the locations of central sites that may mediate these effects have not been clearly elucidated. Orexin-containing fibers are projected to periaqueductal gray matter (PAG), which is involved in pain modulation. Methods: Behavioral study was done on male Sprague Dawley rats (200-300 g) in formalin induced nociceptive behaviour. Results: Intra-PAG microinjection of orexin-A produced a dose-dependent inhibition of formalin-evoked behaviour in interphase and phase 2, but not in phase 1, indicating an antinociceptive role of exogenous orexin-A in the PAG. Analgesic effect of orexin-A was less than and specific to inter- and late phase of formalin test, when compared with that of morphine (5 ?g/0.5?l) after intra-PAG administration. Conclusion: The obtained results suggest that orexin-A plays an anti-nociceptive role in PAG, on the interphase and late phase of formalin test in rats. So it is possible that orexin-A might be involved in the mechanisms of inter- and last phases of formalin induced behaviours.

Hassan azhdari Zarmehri; Saead Semnanian; Yaghoub Fathollahi

2008-01-01

253

Analgesic effect of 30% glucose, milk and non-nutritive sucking in neonates.  

UK PubMed Central (United Kingdom)

BACKGROUND: The aim of this study was to evaluate nondrug management practices concerning pain induced by blood sampling in newborns in a Moroccan neonatal unit and to determine whether the results reported from a randomized clinical study of nondrug analgesia could be reproduced in a routine care setting. METHODS: Standardized prospective observation of analgesic practices used during blood sampling was performed. Pain was assessed using the Douleur Aiguë Nouveau-né (DAN, [Newborn Acute Pain]) scale that incorporates facial expression, vocal expression, and limb movements of the newborn during realization of a painful procedure. Five different nondrug analgesic practices were investigated in 125 infants. RESULTS: Median DAN scores for the five methods were 6 (1-10) for venous sampling with oral administration of 30% glucose, 5 (1-10) for venous sampling with sucking, 3 (0-6) for venous sampling with oral administration of 30% glucose combined with sucking, 4 (0-10) for venous sampling with oral administration of 30% glucose combined with sucking and administration of 2 mL of adapted infant formula, and 6 (3-8) for venous sampling with administration of 2 mL of adapted infant formula. CONCLUSION: Oral administration of 30% glucose combined with sucking provided better control of pain induced by blood sampling in newborns at our neonatal unit.

Mekkaoui N; Issef I; Kabiri M; Barkat A

2012-01-01

254

Efecto analgésico del extracto acuoso liofilizado de Ocimum tenuiflorum L./ Analgesic effect of the freeze-dried aqueous extract of Ocimum tenuiflorum L.  

Scientific Electronic Library Online (English)

Full Text Available Abstract in spanish Drogas con capacidad de inhibir la síntesis o acción de mediadores como los eicosanoides, histamina, bradicinina, entre otras, impiden la acción sensibilizadora de éstos sobre las terminaciones nerviosas nociceptivas. Teniendo en cuenta la actividad antiinflamatoria demostrada del extracto acuoso liofilizado de Ocimum tenuiflorum L., fue objetivo de este trabajo evaluar sus propiedades analgésicas en modelos animales. Dosis de O. tenuiflorum de 250, 500 y 1 000 mg/kg (more) fueron evaluadas en modelos de inducción del dolor por vías química y térmica. Como resultado de este estudio se obtuvo que el extracto acuoso liofilizado de O tenuiflorum mostró efecto analgésico en los modelos del plato caliente a la dosis de 1 000 mg/kg; en el de contorsiones por ácido acético en ratones y foco calorífico en ratas a las dosis de 250, 500 y 1 000 mg/kg. Estos resultados indicaron que el extracto acuoso liofilizado de O. tenuiflorum ejerce un efecto antinociceptivo, preferentemente sobre la vía periférica. Abstract in english Drugs with the capacity of inhibiting the synthesis or action of mediators such as eikosanoids, histamine, bradycine, and others, hinder the sensitizing action of them on the nociceptive nervous terminationes. Taking into account the shown antiinflammatory activity of the freeze-dried aqueous extract of Ocimum tenuiflorum L., it was the objective of this paper to evaluate the analgesic properties of it in animal models. Doses of O. tenuiflorum of 250, 500 and 1 000 mg/kg (more) were evaluated in pain-induction models by chemical and thermic ways. As a result of this study it was observed that the freeze-dried aqueous extract of O. tenuiflorum. had an analgesic effect in the hot dish model at a dose of 1 000 mg/kg, and in that of contortions by acetic acid in mice and calorific focus in rats at doses of 250, 500 and 1 000 mg/kg. These results indicated that the freeze-dried aqueous extract of O. tenuiflorum has an antinociceptive effect, mainly on the peripheral pathway.

Barzaga Fernández, Pedro; Núńez Figueredo, Yanier; Agüero Fernández, Sarah; Chávez Hernández, Ismael; González Sanabria, María Lidia; Iser Valdés, Yadira; Olivera Carpio, Maylin

2005-04-01

255

[Comparative clinical multicenter study to evaluate analgesic effectiveness of intramuscular etofenamate and diclofenac in patients with post-surgical pain].  

UK PubMed Central (United Kingdom)

OBJECTIVE: The analgesic efficacy of intramuscular etofenamate (1 g/day) and intramuscular diclofenac (75 mg/day) was assessed in post-surgical pain relief during a period of 3 days. MATERIAL AND METHODS: One hundred ten hospitalized patients undergoing elective surgery were evaluated in an open-label, comparative, randomized, parallel-group, multicenter study. Fifty five patients received etofenamate and 55 patients diclofenac, 1 h before surgery. The doses were administered after 24 and 48 h. Baseline evaluations were carried out 30 min after anesthesia recovery and the clinical efficacy variables were assessed at 1, 6, 12, 24, 36, 48, 60 and 72 h. The efficacy variables were Pain Visual-Analogue Scale (VAS), Pain Analogous Verbal Scale (AVERS), and Well-Being Scale. Adverse events were documented. RESULTS: Patients in both groups showed similar values in post-surgical pain relief (VAS, AVERS). According to VAS, etofenamate at 24 h had a better analgesic action than diclofenac even though it was not statistically significant. Both drugs demonstrated to be safe. Patients in both groups reported nausea, vomiting, flatulence, and pain at injection site. CONCLUSIONS: We find that both etofenamate and diclofenac were safe, tolerable, and effective treatments for the relief of post-surgical pain.

Guevara-López U; Uscanga-Sánchez S; Márquez J; Bárcenas-Olivares J; Martínez-Arenas A; Palma-Aguirre JA

2004-11-01

256

Opioid analgesics for rheumatoid arthritis pain.  

UK PubMed Central (United Kingdom)

CLINICAL QUESTION Do the benefits of opioid analgesics outweigh the risks in patients with persistent pain due to rheumatoid arthritis? BOTTOM LINE Weak opioids (such as codeine, dextropropoxyphene, and tramadol) may be effective in the short-term management of rheumatoid arthritis pain, but adverse effects are common and may outweigh the benefits; alternative analgesics should be considered first.

Whittle SL; Richards BL; Buchbinder R

2013-02-01

257

Phytochemical profile and analgesic evaluation of Vitex cymosa leaf extracts  

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Full Text Available Vitex cymosa Bertero ex Spreng., Lamiaceae, is found in Central and Amazon regions of Brazil, where it is popularly used as antirheumatic. Extracts from the leaves of V. cymosa were tested in analgesia models such as abdominal contortions induced by acetic acid and formalin to test peripheral analgesia; as well as the tail flick and hot plate models, to test spinal and supraspinal analgesia. A significant reduction was observed in the number of contortions with all extracts and in all doses. In the formalin model, a reduction in the second phase (inflammatory) was observed with all extracts, whereas only the n-butanol extract was able to act in the first, neurogenic, phase. In the tail flick model, all extracts increased latency time. Naloxone treatment reverted analgesic effect of all extracts with the exception of the dichloromethane one. All extracts developed peripheral and central analgesic activity. In the hot plate model no antinociceptive effect was observed for all tested extracts. All these results taken together suggest that V. cymosa leaf extracts were able to promote peripheral and central antinociceptive activity mediated by the opioid system.Twenty three substances were isolated and identified in the extracts and include flavonoids (C-glucosyl flavones, flavones and flavonols), triterpene acids from ursane and oleanane types, iridoids (free and glucosides), as well as simple phenols.

Suzana Guimarăes Leităo; Tereza Cristina dos Santos; Franco Delle Monache; Maria Eline Matheus; Patrícia Dias Fernandes; Bruno Guimarăes Marinho

2011-01-01

258

Phytochemical profile and analgesic evaluation of Vitex cymosa leaf extracts  

Scientific Electronic Library Online (English)

Full Text Available Abstract in english Vitex cymosa Bertero ex Spreng., Lamiaceae, is found in Central and Amazon regions of Brazil, where it is popularly used as antirheumatic. Extracts from the leaves of V. cymosa were tested in analgesia models such as abdominal contortions induced by acetic acid and formalin to test peripheral analgesia; as well as the tail flick and hot plate models, to test spinal and supraspinal analgesia. A significant reduction was observed in the number of contortions with all extrac (more) ts and in all doses. In the formalin model, a reduction in the second phase (inflammatory) was observed with all extracts, whereas only the n-butanol extract was able to act in the first, neurogenic, phase. In the tail flick model, all extracts increased latency time. Naloxone treatment reverted analgesic effect of all extracts with the exception of the dichloromethane one. All extracts developed peripheral and central analgesic activity. In the hot plate model no antinociceptive effect was observed for all tested extracts. All these results taken together suggest that V. cymosa leaf extracts were able to promote peripheral and central antinociceptive activity mediated by the opioid system.Twenty three substances were isolated and identified in the extracts and include flavonoids (C-glucosyl flavones, flavones and flavonols), triterpene acids from ursane and oleanane types, iridoids (free and glucosides), as well as simple phenols.

Leităo, Suzana Guimarăes; Santos, Tereza Cristina dos; Delle Monache, Franco; Matheus, Maria Eline; Fernandes, Patrícia Dias; Marinho, Bruno Guimarăes

2011-10-01

259

The formalin test in the naked mole-rat (Heterocephalus glaber): analgesic effects of morphine, nefopam and paracetamol.  

UK PubMed Central (United Kingdom)

The present experiments were initiated to study the effects of morphine, nefopam and paracetamol in the naked mole-rat, a hairless rodent that lives in subterranean colonies of up to 300, following the inability to demonstrate morphine analgesia in the hot-plate test in the rodent. The formalin test was used. Injection of 20 microliters 10% formalin produced two periods of high licking and pain behaviour, the early (0-5 min) and the late phase (15-60 min). Morphine (10 or 20 mg/kg), nefopam (10 or 20 mg/kg) and paracetamol (200 mg/kg) significantly inhibited the two phases. Paracetamol (400 mg/kg) produced significant analgesia only during the late phase. It is concluded that, unlike in the hot-plate test, it is possible to demonstrate the analgesic effects of morphine in the naked mole-rat, in the formalin test.

Kanui TI; Karim F; Towett PK

1993-01-01

260

Analgesic effects of JCM-16021 on neonatal maternal separation-induced visceral pain in rats  

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Full Text Available AIM: To investigate the pharmacological effect of JCM-16021, a Chinese herbal formula, and its underlying mechanisms.METHODS: JCM-16021 is composed of seven herbal plant materials. All raw materials of the formula were examined according to the quality control criteria listed in the Chinese Pharmacopeia (2005). In a neonatal maternal separation (NMS) model, male Sprague-Dawley rats were submitted to daily maternal separation from postnatal day 2 to day 14, or no specific handling (NH). Starting from postnatal day 60, rats were administered JCM-16021 (2, 4, 8 g/kg per day) orally twice a day for 28 d. Pain threshold pressure and electromyographic activities of external oblique muscles in response to colorectal distention recorded with a Power Lab System (AD Instruments International), were tested as pain indices. Changes in serotonin (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) concentrations in the colon of rats were analyzed; the enterochromaffin cell numbers and serotonin transporter in the colon of rats were also evaluated with an immunohistochemistry method.RESULTS: NMS treatment significantly reduced pain threshold pressure (37.4 ± 1.4 mmHg), as compared to that of NH rats (57.7 ± 1.9 mmHg, P < 0.05). After JCM-16021 treatment, the pain threshold pressure significantly increased when compared to that before treatment (34.2 ± 0.9 mmHg vs 52.8 ± 2.3 mmHg in the high dose group, 40.2 ± 1.6 mmHg vs 46.5 ± 1.3 mmHg in the middle dose group, and 39.3 ± 0.7 mmHg vs 46.5 ± 1.6 mmHg in the low dose group, P < 0.05). Also JCM-16021 significantly and dose-dependently decreased electromyographic activity to the graded colorectal distension (CRD), (the mean ?AUC values were: 0.17 ± 0.03, 0.53 ± 0.15, 1.06 ± 0.18, 1.22 ± 0.24 in the high dose group; 0.23 ± 0.04, 0.68 ± 0.17, 1.27 ± 0.26, 1.8 ± 0.3 in the middle dose group; and 0.29 ± 0.06, 0.8 ± 0.16, 1.53 ± 0.24, 2.1 ± 0.21 in the low dose group for the pressures 20, 40, 60, 80 mmHg), as compared to the NMS vehicle group. The mean ?AUC values were: 0.57 ± 0.12, 1.33 ± 0.18, 2.57 ± 0.37, 3.08 ± 0.37 for the pressures 20, 40, 60, 80 mmHg (P < 0.05). JCM-16021 treatment significantly reduced the 5-HT concentrations (from high, middle and low dosage groups: 60.25 ± 5.98 ng/100 mg, 60.32 ± 4.22 ng/100 mg, 73.31 ± 7.65 ng/100 mg), as compared to the NMS vehicle groups (93.11 ± 9.85 ng/100 mg, P < 0.05); and increased the 5-HIAA concentrations (after treatment, from high, middle and low dosage groups: 54.24 ± 3.27 ng/100 mg, 50.34 ± 1.26 ng/100 mg, 51.37 ± 2.13 ng/100 mg) when compared to that in the NMS vehicle group (51.75 ± 1.98 ng/100 mg, P < 0.05); but did not change the enterochromaffin cell numbers in the colon of rats. In addition, NMS rats had higher SERT expression (n = 10) than NH rats (n = 8, P < 0.05). JCM-16021 treatment significantly decreased SERT expression when compared to the NMS group (P < 0.01-0.001).CONCLUSION: JCM-16021 can attenuate visceral hypersensitivity, and this analgesic effect may be mediated through the serotonin signaling pathway in the colon of rats.

Zhao-Xiang Bian, Man Zhang, Quan-Bin Han, Hong-Xi Xu, Joseph JY Sung

2010-01-01

 
 
 
 
261

Effect of the frequency of transcutaneous electrical nerve stimulation on the postoperative opioid analgesic requirement and recovery profile.  

UK PubMed Central (United Kingdom)

BACKGROUND: Transcutaneous electrical nerve stimulation (TENS) at either an acupoint or dermatome corresponding to the surgical incision produces comparable decreases in postoperative opioid requirements and opioid-related side effects. However, the effect of the frequency of the electrical stimulus on the postoperative analgesic response to TENS therapy has not been studied. METHODS: One hundred women undergoing major gynecological procedures with a standardized general anesthetic technique were enrolled in the study. Patients were randomly assigned to four groups: group I, patient-controlled analgesia (PCA) plus sham TENS (no stimulation); group II, PCA plus low-frequency (2-Hz) TENS; group m, PCA plus high-frequency (100-Hz) TENS; group IV, PCA plus mixed-frequency (2- and 100-Hz) TENS. The PCA device was programmed to deliver 2-3 mg intravenous boluses of morphine with a lockout interval of 10 min. The TENS device was used every 2 h during the day. Standard 100-mm visual analog scales were used to assess pain, sedation, fatigue, and nausea at specific intervals after surgery. RESULTS: Mixed frequency (2 and 100 Hz) of stimulation decreased morphine requirements by 53% compared with the sham group; low (2-Hz) and high (100-Hz) frequencies produced 32% and 35% decreases, respectively. All three "active" TENS groups reduced the duration of PCA therapy, as well as the incidence of nausea, dizziness, and itching. CONCLUSIONS: TENS decreased postoperative opioid analgesic requirements and opioid-related side effects when utilized as an adjunct to PCA after lower abdominal surgery. Use of TENS at mixed (2- and 100-Hz) frequencies of stimulation produced a slightly greater opioid-sparing effect than either low (2-Hz) or high (100 Hz) frequencies alone.

Hamza MA; White PF; Ahmed HE; Ghoname EA

1999-11-01

262

Differential proteomics analysis of the analgesic effect of electroacupuncture intervention in the hippocampus following neuropathic pain in rats  

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Full Text Available Abstract Background Evidence is building steadily on the effectiveness of acupuncture therapy in pain relief and repeated acupuncture-induced pain relief is accompanied by improvement of hippocampal neural synaptic plasticity. To further test the cellular and molecular changes underlying analgesic effect of acupuncture, the global change of acupuncture associated protein profiles in the hippocampus under neuropathic pain condition was profiled. Methods The chronic constrictive injury (CCI) model was established by ligature of the unilateral sciatic nerve in adult Wistar rats. Rats were randomized into normal control (NC) group, CCI group, and CCI with electroacupuncture (EA) stimulation group. EA was applied to bilateral Zusanli (ST36) and Yanglingquan (GB34) in the EA group. Differentially expressed proteins in the hippocampus in the three groups were identified by two-dimensional gel electrophoresis and matrix-assisted laser desorption/ionization time of flight mass spectrometry. The functional clustering of the identified proteins was analyzed by Mascot software. Results After CCI, the thermal pain threshold of the affected hind footpad was decreased and was reversed gradually by 12 sessions of acupuncture treatment. Following EA, there were 19 hippocampal proteins identified with significant changes in expression (>2-fold), which are involved in metabolic, physiological, and cellular processes. The top three canonical pathways identified were “cysteine metabolism”, “valine, leucine, and isoleucine degradation” and “mitogen-activated protein kinase (MAPK) signaling”. Conclusions These data suggest that the analgesic effect of EA is mediated by regulation of hippocampal proteins related to amino acid metabolism and activation of the MAPK signaling pathway.

Gao Yong-Hui; Chen Shu-Ping; Wang Jun-Ying; Qiao Li-Na; Meng Fan-Ying; Xu Qiu-Ling; Liu Jun-Ling

2012-01-01

263

Comparison of the Anti-Inflammatory and Analgesic Effects in Rats of Diclofenac-Sodium, Felbinac and Indomethacin Patches  

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Full Text Available Background: Topically applied nonsteroidal anti-inflammatory drugs (NSAIDs) are used widely for the treatment of pain and inflammation in musculoskeletal disorders. This study compared the analgesic and anti-inflammatory effects of patches of 1% diclofenac-sodium, 3.5% and 0.5% felbinac and 3.75% indomethacin in rats using the carrageenan-induced paw pad edema model and the brewer’s yeast-induced hyper algesia model. Two studies were conducted: in the preliminary study, the patch was removed at 2 or 24 hrs after application, and in the main study the patch was removed at 2 hrs. The volume of the right hind paw and the pain threshold were assessed at 1, 3, 5, and 7 hrs after induction of inflammation in both studies. Results: In the main study, the edema ratio in the 1% diclofenac group at 5 hrs after induction of inflammation and the AUEC (Area Under the Effect Curve) were significantly lower than in the control animals (p=0.009). The edema suppression rate in the 1% diclofenac group (12.1–33.2%) was higher than in the 3.5% and 0.5% felbinac and 3.75% indomethacin groups. The pain threshold ratio did not decrease in the 1% diclofenac group and it was significantly higher than in the control group at 3 (p=0.0004) and 5 hrs (p=0.029). The 1/AUEC was significantly lower than that in the control group (p=0.004) and the lowest among all the NSAID groups. Conclusions: This study demonstrated that the analgesic and anti-inflammatory effects of the 1% diclofenac sodium patch in a rat model may be exerted more promptly and persistently than with the 3.5% and 0.5% felbinac and 3.75% indomethacin patches.

Kozo Takayama; Akihiko Hirose; Ikuko Suda; Atsushi Miyazaki; Masao Oguchi; Masako Onotogi; Grigorios Fotopoulos

2011-01-01

264

Analgesic Effects of Meloxicam, Morphine Sulfate, Flunixin Meglumine, and Xylazine Hydrochloride in African-Clawed Frogs (Xenopus laevis)  

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We evaluated analgesic use and analgesiometry in aquatic African-clawed frogs (Xenopus laevis). We used the acetic acid test (AAT) to assess the analgesic potential of systemic xylazine hydrochloride, meloxicam, flunixin meglumine, and morphine sulfate after injection into the dorsal lymph sac. Flun...

Coble, Dondrae J; Taylor, Douglas K; Mook, Deborah M

265

Peripheral antinociceptive effects of morphine after burn injury.  

DEFF Research Database (Denmark)

In a double-blind study, 2 mg of morphine in saline, or saline only, was given subcutaneously into a second-degree bilateral leg-burn injury in 12 volunteers. Heat-pain thresholds and pressure-pain thresholds were significantly increased by local morphine administration. These results confirm experimental data demonstrating a peripheral antinociceptive effects of opioids in inflamed tissue.

MŘiniche, S; Dahl, J B

1993-01-01

266

Comparing analgesic and hemodynamic effects of unilateral spinal levobupivacaine, levobupivacaine-fentanyl and levobupivacaine-morphine combinations for arthroscopic procedures  

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Full Text Available Objectives: Aim of the study was to compare the analgesic and hemodynamic effects of levobupivacaine, levobupivacaine-fentanyl, levobupivacaine-morphine for arthroscopic knee surgery under unilateral spinal anesthesia.Methods: A total of 44 ASA I/II patients scheduled for arthroscopy were included in the study. After prehydration patients kept in a lateral position on the nondependent side. Spinal puncture was performed at L3–4/L4–5 intervertebral space. Patients divided into three subgroups: Group L (n=14) received 0.5% levobupivacaine 1 ml+1 ml distilled water; Group LF (n=15), 25 mcg fentanyl (0.5 ml)+0.5 ml distilled water; and Group LM (n=15), 0.01 mg morphine (0.5 ml)+0.5 ml distilled water. Patients remained in that position for 15 minutes. Blood pressure and heart rate were recorded before and 1st, 3rd, 5th, 10th, 15th, 20th and 30th minutes after the block and every 15 minutes during the operation. Motor blockade and sensorial level, side effects, motor block regression time (MBRT), first urination time and first analgesic need (FAN) were recorded.Results: Group LM had the longest MBRT, but difference with other groups did not reach to a significant level (p>0.05). Group LM had significantly longer FAN time compare with other groups (p<0.05). The first urination time was latest in Group LM (p<0.05). Motor blockade was least in Group L (p<0.05) and almost 50% patients had not motor block.Conclusion: All three groups had successful anesthesia. Morphine group added group had significantly longer analgesia without significant urinary retention and motor blockade regression time. We concluded that additional low doses of morphine will be a better choice.

Pakize K?rdemir; Dilek Karaaslan; Tülay Tuncer Peker; Sinem Sar?; Özlem Özorak; Sad?k Özmen

2010-01-01

267

The analgesic effect of pregabalin in patients with chronic pain is reflected by changes in pharmaco-EEG spectral indices.  

UK PubMed Central (United Kingdom)

AIM: To identify electroencephalographic (EEG) biomarkers for the analgesic effect of pregabalin in patients with chronic visceral pain. METHODS: This was a double-blind, placebo-controlled study in 31 patients suffering from visceral pain due to chronic pancreatitis. Patients received increasing doses of pregabalin (75mg-300mg twice a day) or matching placebo during 3 weeks of treatment. Pain scores were documented in a diary based on a visual analogue scale. In addition, brief pain inventory-short form (BPI) and quality of life questionnaires were collected prior to and after the study period. Multi-channel resting EEG was recorded before treatment onset and at the end of the study. Changes in EEG spectral indices were extracted, and individual changes were classified by a support vector machine (SVM) to discriminate the pregabalin and placebo responses. Changes in individual spectral indices and pain scores were correlated. RESULTS: Pregabalin increased normalized intensity in low spectral indices, most prominent in the theta band (3.5-7.5Hz), difference of -3.18, 95% CI -3.57, -2.80; P= 0.03. No changes in spectral indices were seen for placebo. The maximum difference between pregabalin and placebo treated patients was seen in the parietal region, with a classification accuracy of 85.7% (P= 0.009). Individual changes in EEG indices were correlated with changes in pain diary (P= 0.04) and BPI pain composite scores (P= 0.02). CONCLUSIONS: Changes in spectral indices caused by slowing of brain oscillations were identified as a biomarker for the central analgesic effect of pregabalin. The developed methodology may provide perspectives to assess individual responses to treatment in personalized medicine.

Graversen C; Olesen SS; Olesen AE; Steimle K; Farina D; Wilder-Smith OH; Bouwense SA; van Goor H; Drewes AM

2012-03-01

268

Analgesic effect of electroacupuncture on inflammatory pain in collagen-induced arthritis rats: mediation by alpha2- and beta-adrenoceptors.  

UK PubMed Central (United Kingdom)

This study was designed to investigate whether alpha- and beta-adrenergic systems mediate the analgesic effect of electroacupucture (EA) on inflammatory pain in a rat model of collagen-induced arthritis (CIA). To induce CIA, male Sprague-Dawley rats were immunized with bovine type II collagen emulsified in Freund's incomplete adjuvant, followed by a booster injection 14 days later. After induction of arthritis, the inflammatory pain threshold by the tail flick latency decreased as time passed and reached the minimum value at 4th week. Four weeks after the first immunization, low-frequency EA stimulation (2 Hz, 0.07 mA, 0.3 ms) delivered to Zusanli (ST(36)) for 30 min showed the analgesic effect. And also, the analgesic effect of EA was blocked by pretreatment with yohimbine (alpha2-adrenoceptor antagonist, 2 mg/kg, i.p.), but not by pretreatment with prazosin (alpha1-adrenoceptor antagonist, 1 mg/kg, i.p.) and propranolol (non-selective beta-adrenoceptor antagonist, 10 mg/kg, i.p.). These results suggest that the low-frequency EA can relieve the inflammatory pain in CIA, and the analgesic effect of EA can be mediated by alpha2- and beta-adrenoceptor, but not by alpha1-adrenoceptor.

Park DS; Seo BK; Baek YH

2013-02-01

269

Effect of analgesics and sedatives on the occurrence of spreading depolarizations accompanying acute brain injury.  

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Spreading depolarizations are waves of mass neuronal and glial depolarization that propagate across the injured human cortex. They can occur with depression of neuronal activity as spreading depressions or isoelectric spreading depolarizations on a background of absent or minimal electroencephalogram activity. Spreading depolarizations are characterized by the loss of neuronal ion homeostasis and are believed to damage functional neurons, leading to neuronal necrosis or neurological degeneration and poor outcome. Analgesics and sedatives influence activity-dependent neuronal ion homeostasis and therefore represent potential modulators of spreading depolarizations. In this exploratory retrospective international multicentre analysis, we investigated the influence of midazolam, propofol, fentanyl, sufentanil, ketamine and morphine on the occurrence of spreading depolarizations in 115 brain-injured patients. A surface electrode strip was placed on the cortex, and continuous electrocorticographical recordings were obtained. We used multivariable binary logistic regression to quantify associations between the investigated drugs and the hours of electrocorticographical recordings with and without spreading depolarizations or clusters of spreading depolarizations. We found that administration of ketamine was associated with a reduction of spreading depolarizations and spreading depolarization clusters (P?ratio analysis, we also found a significant association between ketamine administration and reduced occurrence of isoelectric spreading depolarizations in patients suffering from traumatic brain injury, subarachnoid haemorrhage and malignant hemispheric stroke (P?

Hertle, Daniel N; Dreier, Jens P; Woitzik, Johannes; Hartings, Jed A; Bullock, Ross; Okonkwo, David O; Shutter, Lori A; Vidgeon, Steven; Strong, Anthony J; Kowoll, Christina; Dohmen, Christian; Diedler, Jennifer; Veltkamp, Roland; Bruckner, Thomas; Unterberg, Andreas W; Sakowitz, Oliver W

2012-06-19

270

Effect of a centralized prescription network on inappropriate prescriptions for opioid analgesics and benzodiazepines.  

UK PubMed Central (United Kingdom)

BACKGROUND: Opioid analgesics and benzodiazepines are often misused in clinical practice. We determined whether implementation of a centralized prescription network offering real-time access to patient-level data on filled prescriptions (PharmaNet) reduced the number of potentially inappropriate prescriptions for opioids and benzodiazepines. METHODS: We conducted a time series analysis using prescription records between Jan. 1, 1993, and Dec. 31, 1997, for residents of the province of British Columbia who were receiving social assistance or were 65 years or older. We calculated monthly percentages of filled prescriptions for an opioid or a benzodiazepine that were deemed inappropriate (those issued by a different physician and dispensed at a different pharmacy within 7 days after a filled prescription of at least 30 tablets of the same drug). RESULTS: Within 6 months after implementation of PharmaNet in July 1995, we observed a relative reduction in inappropriate filled prescriptions for opioids of 32.8% (95% confidence interval [CI] 31.0%-34.7%) among patients receiving social assistance; inappropriate filled prescriptions for benzodiazepines decreased by 48.6% (95% CI 43.2%-53.1%). Similar and statistically significant reductions were observed among residents 65 years or older. INTERPRETATION: The implementation of a centralized prescription network was associated with a dramatic reduction in inappropriate filled prescriptions for opioids and benzodiazepines.

Dormuth CR; Miller TA; Huang A; Mamdani MM; Juurlink DN

2012-11-01

271

Effect of Erythropoietin on Peripheral Nerve Regeneration  

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Full Text Available The aim of this study was to identify the effect of erythropoietin (EPO) on a sciatic nerve injury model. The effect of single or repeated doses was also determined. Twenty-one Wistar rats were anesthetised and the sciatic nerve was transected 1 cm above the trifurcation and the nerve was repaired with four epineural 10/0 nylon sutures placed at 90 degrees intervals under microscope magnification.The rats were divided into 4 groups as follows: the sham,the saline, the single dose EPO and the multiple dose EPO. The skin was incised and closed and no treatment was given in sham group. In the saline group, 1 mL saline was given intraperitoneally; in the single EPO group, 5000 U/kg EPO was given intraperitoneally immediately after the procedure. In the multiple EPO group, 5000 U/kg EPO was given after the procedure and the same dose was repeated after the 1st, 2nd, 3rd and 4th weeks. Functional recovery was evaluated by static sciatic functional index(SSI).Single EPO group had greater myofibril size, axon number, diameter, and ratio M than the saline group. The multiple EPO treatment was not found to be more effective than single EPO treatment. However, no significant difference was found between the single EPO, multiple EPO, and saline groups based on the 3rd and 4th postoperative month SSI scores. Thus, EPO treatment increased axonal regeneration in our study. However, repeated dose therapy was not found to be more effective than single dose therapy. The optimum dose and duration should be researched in further studies.

Mustafa OZKAN; Necati GOKMEN; Osman YILMAZ; Serhat ERBAYRAKTAR; Alper BAGRIYANIK

2010-01-01

272

Effects of the extracts from Mitragyna speciosa Korth. leaves on analgesic and behavioral activities in experimental animals  

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Full Text Available The leaves of Mitragyna speciosa Korth. (M. speciosa) were extracted with methanol to give methanol extract. The methanol extract was made in acid and then in alkaline and extracted with chloroform to give alkaloid extract. The effects of the methanol and alkaloid extracts on analgesic activities in hot plate test in mice and tail flick test in rats and behavioral activities in locomotor activity and pentobarbital-induced sleep in mice, were examined. In acute toxicity test, the LD50 values of oral administration of the methanol and alkaloid extracts of M. speciosa leaves in mice were 4.90 g/kg and 173.20 mg/kg, respectively. Oral administration (50, 100 and 200 mg/kg) of the methanol extract of M. speciosa leaves significantly prolonged the latency of nociceptive response on hot plate test in mice. The alkaloid extract of M. speciosa also increased the pain response latency at the dose of 20 mg/kg but less potent than those of the methanol extract (100 mg/kg) in mice (comparing 5-10 mg/kg alkaloid extract with corresponding to approximately 200 mg/kg of methanol extract). The antinociceptive action of either methanol extract (100 mg/kg, p.o.) or alkaloid extract (20 mg/kg, p.o.) of M. speciosa leaves was blocked by naloxone (2 mg/kg, i.p.) in mice. Neither the methanol extract nor the alkaloid extract significantly prolonged latency of nociceptive response on tail flick test in rats. Both of the extracts had no significant change on spontaneous motor activity or pentobarbital-induced sleep in mice, respectively. These results suggest that the methanol and alkaloid extracts of M. speciosa leaves possess the analgesic activity which partly acted at opioid receptors in the supraspinal opioid system.

Wantana Reanmongkol; Niwat Keawpradub; Kitja Sawangjaroen

2007-01-01

273

Specific down-regulation of spinal mu-opioid receptor and reduced analgesic effects of morphine in mice with postherpetic pain.  

Science.gov (United States)

The analgesic effects of opioid agonists and the expression of mu- and kappa-opioid receptors were compared between mice with herpetic pain and those with postherpetic pain induced by herpetic virus inoculation. Morphine inhibited herpetic pain more effectively than postherpetic pain. Intrathecal injection reduced the analgesic effects of morphine on postherpetic pain, but intracerebroventricular injection did not. The kappa-opioid receptor agonist nalfurafine suppressed herpetic and postherpetic pain to similar degrees. mu-Opioid receptor-like immunoreactivities in the lumbar dorsal horn were markedly decreased at the postherpetic, but not herpetic, stage of pain. In the dorsal root ganglia, the expression of mu-opioid receptor mRNA was significantly decreased in mice with postherpetic pain, whereas the kappa-opioid receptor mRNA level was not altered. These results suggest that specific down-regulation of the mu-opioid receptor in the primary sensory neurons is responsible for the reduced analgesic action of morphine on postherpetic pain. The kappa-opioid receptor may be a useful target for the analgesic treatment of postherpetic neuralgia. PMID:17026987

Takasaki, Ichiro; Nojima, Hiroshi; Shiraki, Kimiyasu; Kuraishi, Yasushi

2006-09-06

274

Specific down-regulation of spinal mu-opioid receptor and reduced analgesic effects of morphine in mice with postherpetic pain.  

UK PubMed Central (United Kingdom)

The analgesic effects of opioid agonists and the expression of mu- and kappa-opioid receptors were compared between mice with herpetic pain and those with postherpetic pain induced by herpetic virus inoculation. Morphine inhibited herpetic pain more effectively than postherpetic pain. Intrathecal injection reduced the analgesic effects of morphine on postherpetic pain, but intracerebroventricular injection did not. The kappa-opioid receptor agonist nalfurafine suppressed herpetic and postherpetic pain to similar degrees. mu-Opioid receptor-like immunoreactivities in the lumbar dorsal horn were markedly decreased at the postherpetic, but not herpetic, stage of pain. In the dorsal root ganglia, the expression of mu-opioid receptor mRNA was significantly decreased in mice with postherpetic pain, whereas the kappa-opioid receptor mRNA level was not altered. These results suggest that specific down-regulation of the mu-opioid receptor in the primary sensory neurons is responsible for the reduced analgesic action of morphine on postherpetic pain. The kappa-opioid receptor may be a useful target for the analgesic treatment of postherpetic neuralgia.

Takasaki I; Nojima H; Shiraki K; Kuraishi Y

2006-11-01

275

Analgesic effects of an ethanol extract of the fruits of Xylopia aethiopica (Dunal) A. Rich (Annonaceae) and the major constituent, xylopic acid in murine models.  

UK PubMed Central (United Kingdom)

BACKGROUND: Fruit extracts of Xylopia aethiopica are used traditionally in the management of pain disorders including rheumatism, headache, colic pain, and neuralgia. Little pharmacological data exists in scientific literature of the effect of the fruit extract and its major diterpene, xylopic acid, on pain. The present study evaluated the analgesic properties of the ethanol extract of X. aethiopica (XAE) and xylopic acid (XA), in murine models. MATERIALS AND METHODS: XAE and XA were assessed in chemical (acetic acid-induced abdominal writhing and formalin tests), thermal (Tail-flick and Hargreaves thermal hyperalgesia tests), and mechanical (Randall-Selitto paw pressure test) pain models. RESULTS: XAE and XA exhibited significant analgesic activity in all the pain models used. XAE (30-300 mg kg(-1), p.o.) and XA (10-100 mg kg(-1), p.o.) inhibited acetic acid-induced visceral nociception, formalin- induced paw pain (both neurogenic and inflammatory), thermal pain as well as carrageenan-induced mechanical and thermal hyperalgesia in animals. Morphine (1-10 mg kg(-1), i.p.) and diclofenac (1-10 mg kg(-1), i.p.), used as controls, exhibited similar anti-nociceptive activities. XAE and XA did not induce tolerance to their respective anti-nociceptive effects in the formalin test after chronic administration. Morphine tolerance did not also cross-generalize to the analgesic effects of XAE or XA. CONCLUSIONS: These findings establish the analgesic properties of the ethanol fruit extract of X. aethiopica and its major diterpene, xylopic acid.

Woode E; Ameyaw EO; Boakye-Gyasi E; Abotsi WK

2012-10-01

276

Comparative Free Radical Scavenging and Analgesic Activity of Ethanolic Leaves and Stem Extracts of Solanum nigrum  

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Full Text Available In the present investigation a comparative analysis of the Free radical scavenging potential and analgesic activity of the Ethanolic Leaf (ELS) and stem extracts (ESS) of Solanum nigrum was performed. The extracts were evaluated for its DPPH and hydroxyl free radicals scavenging effect and inhibitory potential on protein carbonyl formation. Total phenolic and flavonoid content of the extracts were also determined by a colorimetric method. The ethanolic extracts of Solanum nigrum were evaluated for its peripheral analgesic activity by Acetic-acid induced writhing response and central analgesic activity by Tail flicking method and Hot plate method in mice. Both the plant extracts scavenged the free radicals in a dose dependent manner. However the scavenging effect was more pronounced in ELS extract when comparable to ESS extract. Both the extract possessed considerable quantity of phenols and flavonoids. In Tail flicking and Hot plate methods the ELS extract of Solanum nigrum showed higher mean basal latency time when comparable to ESS extract suggesting its central analgesic activity. Similarly in Acetic acid induced writhing response the ELS extract exhibited a significant inhibition of writhing 53.28% when comparable to ESS which exhibited an inhibition of 46.53%. The positive control Diclofenac sodium showed 70.66% of writhing inhibition. The analgesic activity of the plants extracts is probably due to its free radical scavenging activity.

Rajeswary Hari; R. Vasuki; J. Anbu; B. Muralikrishna; G. Manasa; Geethanjali

2013-01-01

277

The analgesic effect of electroacupuncture on acute thermal pain perception-a central neural correlate study with fMRI  

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Full Text Available Abstract Background Electrical acupuncture (EA) has been utilized in acute pain management. However, the neuronal mechanisms that lead to the analgesic effect are still not well defined. The current study assessed the intensity [optimal EA (OI-EA) vs. minimal EA (MI-EA)] effect of non-noxious EA on supraspinal regions related to noxious heat pain (HP) stimulation utilizing an EA treatment protocol for acute pain and functional magnetic resonance imaging (fMRI) with correlation in behavioral changes. Subjects underwent five fMRI scanning paradigms: one with heat pain (HP), two with OI-EA and MI-EA, and two with OI-EA and HP, and MI-EA and HP. Results While HP resulted in activations (excitatory effect) in supraspinal areas known for pain processing and perception, EA paradigms primarily resulted in deactivations (suppressive effect) in most of these corresponding areas. In addition, OI-EA resulted in a more robust supraspinal sedative effect in comparison to MI-EA. As a result, OI-EA is more effective than MI-EA in suppressing the excitatory effect of HP in supraspinal areas related to both pain processing and perception. Conclusion Intensities of EA plays an important role in modulating central pain perception.

Shukla Shivshil; Torossian Artour; Duann Jeng-Ren; Leung Albert

2011-01-01

278

The Radiation Effect on Peripheral Blood Cell  

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To evaluate radiation effect on the hematopoietic system, we analyzed 44 patients who were treated with conventionally fractionated radiation therapy (RT) at Chonbuk National University Hospital. According to the treatment sites, we classified them into three groups: group I as head and neck, group II as thorax, and group III as pelvis. White blood cell, lymphocyte, platelet and hemoglobin were checked before and during RT The results were as follow; 1. White blood cell (WBC) and lymphocyte count were declined from the first week of RT to the third week, and then slightly recovered after the third or fourth week. There was prominent decrease in lymphocyte counts than WBC. 2. Platelet counts were declined until the second week of the RT, showed slight recovery at fourth week in all groups. Hemoglobin values were slightly decreased in the first week and then recovered the level of pretreatment value, gradually. 3. Lymphocyte count were declined significantly on group III(p<0.01), WBC and platelet counts were decreased on group II but statistically not significant.

Lee, Tae June; Kwon, Hyoung Cheol; Kim, Jung Soo; Im, Sun Kyun; Choi, Ki Chul [Chonbuk National University College of Medicine, Chonju (Korea, Republic of)

1988-12-15

279

[Analgesics and palliative care  

UK PubMed Central (United Kingdom)

Pain is an important and often under-treated symptom of life-threatening illness. A complete evaluation of pain facilitate optimal treatment. Correct use of analgesic medication, following the guidelines of the W.H.O. step ladder, with attention to detail, with addition of adjuvant analgesics, should control the pain in most of the cases. The use of weak and strong opioid analgesics, their tolerance, the breakthrough doses, principle of opioid rotation and the place of adjuvant drugs are discussed. Proper pain management in end-of-life is never easy and require to become more familiar with the use of these analgesics and to surround oneself with a multidisciplinary team.

Mathieu N; Tuna T

2008-09-01

280

Effect of analgesics and sedatives on the occurrence of spreading depolarizations accompanying acute brain injury.  

UK PubMed Central (United Kingdom)

Spreading depolarizations are waves of mass neuronal and glial depolarization that propagate across the injured human cortex. They can occur with depression of neuronal activity as spreading depressions or isoelectric spreading depolarizations on a background of absent or minimal electroencephalogram activity. Spreading depolarizations are characterized by the loss of neuronal ion homeostasis and are believed to damage functional neurons, leading to neuronal necrosis or neurological degeneration and poor outcome. Analgesics and sedatives influence activity-dependent neuronal ion homeostasis and therefore represent potential modulators of spreading depolarizations. In this exploratory retrospective international multicentre analysis, we investigated the influence of midazolam, propofol, fentanyl, sufentanil, ketamine and morphine on the occurrence of spreading depolarizations in 115 brain-injured patients. A surface electrode strip was placed on the cortex, and continuous electrocorticographical recordings were obtained. We used multivariable binary logistic regression to quantify associations between the investigated drugs and the hours of electrocorticographical recordings with and without spreading depolarizations or clusters of spreading depolarizations. We found that administration of ketamine was associated with a reduction of spreading depolarizations and spreading depolarization clusters (P?

Hertle DN; Dreier JP; Woitzik J; Hartings JA; Bullock R; Okonkwo DO; Shutter LA; Vidgeon S; Strong AJ; Kowoll C; Dohmen C; Diedler J; Veltkamp R; Bruckner T; Unterberg AW; Sakowitz OW

2012-08-01

 
 
 
 
281

Effect of sildenafil on peripheral nerve regeneration.  

UK PubMed Central (United Kingdom)

In this study, we investigated whether sildenafil, a cyclic guanosine monophosphate-dependent phospodiesterase-5 inhibitor, could promote functional nerve regeneration after surgical section and repair of the sciatic nerve in rats. Nerve regeneration was studied in a rat sciatic nerve transected and repair model. The animals were randomly assigned to one of the following 3 treatment groups (n = 20/group): sildenafil-treated group 1 (5 mg/kg/d subcutaneously, for 7 days), sildenafil-treated group 2 (5 mg/kg/d subcutaneously, for 42 days), and control group given saline solution (once per day subcutaneously). Walking track analysis, electromyography, and histological evaluation were performed on day 90 after repair operation. The results showed that the sciatic functional index of sildenafil-treated group 1 (data) was slightly better than that of sildenafil-treated group 2 (data) and control group (data) on postoperative day 90. However, the difference was not statistically significant (P = 0.073). No significant differences of the motor nerve conduction velocity were found between experimental groups [18 (2.4) and 20 (4.1 m/s)] and saline control group [19.5 (3.0) m/s] (P = 0.68). Comparison of myelinated axon count of regenerated nerve of the rat between the sildenafil-treated group 1, sildenafil-treated group 2, and saline group was also not significantly different (P = 0.56). In conclusion, administration of sildenafil after nerve repair surgery was found to have positive but insignificant effects on several parameters of nerve regeneration. Further studies could clarify this trend suggesting enhanced nerve regeneration mediated by sildenafil.

Fang T; Shao Y; Oswald T; Lineaweaver WC; Zhang F

2013-01-01

282

Effect of glial inhibition in attenuation of neuropathic pain and improvement of morphine analgesic effect in a rat model of neuropathy  

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Full Text Available Introduction: Pharmacological blockage of glial activity has been proved useful for treatment of neuropathic pain by lowering proinflammatory cytokines. The present study is to confirm the effect of post-injury administration of pentoxifylline on chronic constriction injury (CCI)-induced neuropathic pain symptoms_ and improved the efficacy of morphine anti-nociception. Methods: Male Wistar rats (230-270 g) underwent surgery for induction of CCI model of neuropathy. In the sham group the nerve was exposed but not ligated. In 5 groups (n=8) morphine (2.5, 5, 7.5, 10, 15 mg/kg s.c.) was administered in post-operative days (POD) 0, 6 and 14. To evaluate the analgesic effect of different doses of morphine, Von Frey and Hargreaves tests were performed before and 30 minutes after morphine administration. In different groups, pentoxifylline (8, 15, 30 mg/kg i.p.) or normal saline (vehicle) were administered from POD6 to POD13. Behavioral tests were utilized after last dose of pentoxifylline and also on POD14 again after injection of a single dose of morphine (5 mg/kg, s.c.). Results: The analgesic effect of morphine (5 mg/kg) on POD6 and morphine (5, 7.5, 10, 15 mg/kg) on POD14 was significantly decreased in comparison to POD0. Pentoxifylline effectively attenuated thermal hyperalgesia (at 15 and 30 mg/kg) and mechanical allodynia (at 30 mg/kg) on POD13. However, pentoxifylline (15, 30 mg/kg) improved the antihyperalgesic effect of morphine (5 mg/kg s.c.) on POD14. Conclusion: Analgesic effect of morphine was reduced after nerve injury and it may be due to the activation of glia. Inhibition of glial activity is an effective way to attenuate CCI-induced neuropathic pain and also to improve the antihyperalgesic effect of morphine, without significant effect on its anti-allodynic effect.

samad nazemi; homa manaheji; Abbas Haghparast; Jalal Zaringhalam moghadam; mehdi sadegi

2012-01-01

283

Study of interaction between opioid and ?-2 adrenergic systems in analgesic effect of oxytocin in locus coeruleus nucleus  

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Full Text Available Introduction: Oxytocin is a active neuropeptide of central nervous system. In this study the effects of naloxone (opioid receptor antagonist) and yohimbine (?-2 adrenergic receptor antagonist) on analgesic effect of oxytocin applied into the locus coeruleus (LC) nucleus were investigated. Methods: Adult male Wistar rats were used. Animals divided into different groups receiving saline, oxytocin (3 nmol / 2?l), naloxone (3 nmol / 2?l) + oxytocin, yohimbine (3 nmol / 2?l) + oxytocin, and naloxone + yohimbine + oxytocin. Hot-plate and tail-flick tests were used to evaluate pain threshold. Results: Data showed that the injection of oxytocin into the LC nucleus increases the response time to thermal stimulations in both tail flick and hot plate tests. Injection of naloxone and yohimbine either separately and or in combination inhibite the antinociception effect of oxytocin. Conclusion: It seems that oxytocin induces its inhibitory effect on acute pain via LC nucleus. This effect is probably mediated by the combination of opioid and ?-2 adrenergic systems.

Nasrin haghighi; Mahnaz Kessmati; Hadi fathi Moghadam2

2006-01-01

284

Superior analgesic effect of an active distraction versus pleasant unfamiliar sounds and music: The influence of emotion and cognitive style  

DEFF Research Database (Denmark)

Previous studies have shown a superior analgesic effect of favorite music over other passive or active distractive tasks. However, it is unclear what mediates this effect. In this study we investigated to which extent distraction, emotional valence and cognitive styles may explain part of the relationship. Forty-eight healthy volunteers received heat stimuli during an active mental arithmetic task (PASAT), and passive listening to music (Mozart), environmental sounds (rain and water), and control (noise). The participants scored the conditions according to affective scales and filled out questionnaires concerning cognitive styles (Baron – Cohen and self-report). Active distraction with PASAT led to significantly less pain intensity and unpleasantness as compared to music and sound. In turn, both music and sound relieved pain significantly more than noise. When music and sound had the same level of valence they relieved pain to a similar degree. The emotional ratings of the conditions were correlated with the amount of pain relief and cognitive styles seemed to influence the analgesia effect. These findings suggest that the pain relieving effect previously seen in relation to music may be at least partly mediated by distraction, emotional factors and cognitive styles rather than by the music itself.

Garza Villarreal, Eduardo A.; Brattico, Elvira

2012-01-01

285

The effect of music therapy on postoperative pain, heart rate, systolic blood pressures and analgesic use following nasal surgery.  

UK PubMed Central (United Kingdom)

The prevalence of unrelieved postoperative pain is high and may lead to adverse effects including prolonged hospitalization and delayed recovery. Distraction may be an effective pain-relieving strategy, and can be implemented by several means including affective imaging, games, and possibly music. The aim of this study was to explore the effect of music therapy on postoperative pain. Fifty-seven patients (24 females, 33 males; mean +/- SD age 39.9 +/- 14.35 years [range 15 to 69 years] were matched for age and sex and then nonselectively assigned to either an experimental (n = 27) or a control (n = 30) group. Music was played intermittently to members of the experimental group during the first 24 hour postoperative period. Pain intensity was measured using the Pain Verbal Rating Scales (VRS). Significant decreases in pain intensity over time were found in the experimental group compared to the control group (p < 0.0001). In addition, the experimental group had a lower systolic blood pressure and heart rate, and took fewer oral analgesics for pain. These findings suggest that music therapy is an effective nonpharmacologic approach for postoperative pain management.

Tse MM; Chan MF; Benzie IF

2005-01-01

286

Analgesic effects of intra-articular botulinum toxin Type B in a murine model of chronic degenerative knee arthritis pain  

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Full Text Available Stephanie Anderson1,2, Hollis Krug1,2, Christopher Dorman1, Pari McGarraugh1, Sandra Frizelle1, Maren Mahowald1,21Rheumatology Section, Veteran’s Affairs Medical Center, Minneapolis, Minnesota; 2Division of Rheumatology and Autoimmune Diseases, University of Minnesota Medical School, Minneapolis, Minnesota, USAObjective: To evaluate the analgesic effectiveness of intra-articular botulinum toxin Type B (BoNT/B) in a murine model of chronic degenerative arthritis pain.Methods and materials: Chronic arthritis was produced in adult C57Bl6 mice by intra-articular injection of Type IV collagenase into the left knee. Following induction of arthritis, the treatment group received intra-articular BoNT/B. Arthritic control groups were treated with intra-articular normal saline or sham injections. Pain behavior testing was performed prior to arthritis, after induction of arthritis, and following treatments. Pain behavior measures included analysis of gait impairment (spontaneous pain behavior) and joint tenderness evaluation (evoked pain response). Strength was measured as ability to grasp and cling.Results: Visual gait analysis showed significant impairment of gait in arthritic mice that improved 43% after intra-articular BoNT/B, demonstrating a substantial articular analgesic effect. Joint tenderness, measured with evoked pain response scores, increased with arthritis induction and decreased 49.5% after intra-articular BoNT/B treatment. No improvement in visual gait scores or decrease in evoked pain response scores were found in the control groups receiving intra-articular normal saline or sham injections. Intra-articular BoNT/B was safe, and no systemic effects or limb weakness was noted.Conclusions: This study is the first report of intra-articular BoNT/B for analgesia in a murine model of arthritis pain. The results of this study validate prior work using intra-articular neurotoxins in murine models. Our findings show chronic degenerative arthritis pain can be quantitated in a murine model by measuring gait impairment using visual gait analysis scores (spontaneous pain behavior) and joint tenderness scores (evoked pain responses). Reduction of joint pain seen in this study is consistent with our hypothesis of inhibition of release of pain mediators by intra-articular BoNT/B, supporting further investigation of this novel approach to treatment of arthritis pain with intra-articular neurotoxins.Keywords: intra-articular BoNT/B, osteoarthritis

Stephanie Anderson; Hollis Krug; Christopher Dorman; et al

2010-01-01

287

Evaluation of the tail formalin test in mice as a new model to assess local analgesic effects.  

Science.gov (United States)

Opioids are effective topical analgesics in the radiant heat tailflick assay and display synergistic interactions with a number of other classes of drugs. To determine whether these actions extend to other types of nociception, we examined the actions of topical morphine and lidocaine in a tail formalin assay in the mouse. Formalin responses in the tail were similar to those seen in the hind paw, but were limited to licking. Unlike the traditional hind paw assay, the time-course of nociceptive behavior in the tail was monophasic; lasting 40-60 min. Morphine, MK-801 and acetylsalicylic acid (ASA) were active systemically in the tail formalin assay with potencies similar to those seen in the second phase of the paw formalin test. Both morphine and lidocaine were active topically in the tail formalin assay, although their time-course of action appeared to be shorter than that of the formalin. However, morphine displayed ceiling effect not seen when it was administered systemically. Lidocaine also had a ceiling effect. When given together, the response to the combination was supra-additive, consistent with our prior studies showing synergy in the radiant heat tailflick assay. These studies validate the formalin assay in the tail and support the topical actions of opioids and other drugs in a second pain model. They also suggest supra-additive interactions between morphine and lidocaine similar to those previously seen. The tail formalin assay will be valuable in assessing the activity of topical drugs. PMID:15542077

Kolesnikov, Yuri; Cristea, Marcela; Oksman, Galina; Torosjan, Armen; Wilson, Roger

2004-12-17

288

Evaluation of the tail formalin test in mice as a new model to assess local analgesic effects.  

UK PubMed Central (United Kingdom)

Opioids are effective topical analgesics in the radiant heat tailflick assay and display synergistic interactions with a number of other classes of drugs. To determine whether these actions extend to other types of nociception, we examined the actions of topical morphine and lidocaine in a tail formalin assay in the mouse. Formalin responses in the tail were similar to those seen in the hind paw, but were limited to licking. Unlike the traditional hind paw assay, the time-course of nociceptive behavior in the tail was monophasic; lasting 40-60 min. Morphine, MK-801 and acetylsalicylic acid (ASA) were active systemically in the tail formalin assay with potencies similar to those seen in the second phase of the paw formalin test. Both morphine and lidocaine were active topically in the tail formalin assay, although their time-course of action appeared to be shorter than that of the formalin. However, morphine displayed ceiling effect not seen when it was administered systemically. Lidocaine also had a ceiling effect. When given together, the response to the combination was supra-additive, consistent with our prior studies showing synergy in the radiant heat tailflick assay. These studies validate the formalin assay in the tail and support the topical actions of opioids and other drugs in a second pain model. They also suggest supra-additive interactions between morphine and lidocaine similar to those previously seen. The tail formalin assay will be valuable in assessing the activity of topical drugs.

Kolesnikov Y; Cristea M; Oksman G; Torosjan A; Wilson R

2004-12-01

289

Evaluation of in vitro effects of some analgesic drugs on erythrocyte and recombinant carbonic anhydrase I and II.  

UK PubMed Central (United Kingdom)

The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was compared to recombinant hCA I and hCA II expressed in Ecoli. IC(50) values of the drugs that caused inhibition were determined by means of activity percentage diagrams. The IC(50) concentrations of dexketoprofen trometamol and dexamethasone sodium phosphate on hCA I were 683 ?M and 4250 ?M and for hCA II 950 ?M and 6200 ?M respectively. Conversely, the enzyme activity was increased by diflofenac sodium. In addition, thiocolchicoside has not any affect on hCA I and hCA II. The effect of these drugs on erythrocyte hCA I and hCA II were consistent with the inhibition of recombinant enzymes.

Gökçe B; Gençer N; Arslan O; Turko?lu SA; Alper M; Köçkar F

2012-02-01

290

Evaluation of in vitro effects of some analgesic drugs on erythrocyte and recombinant carbonic anhydrase I and II.  

Science.gov (United States)

The in vitro effects of the injectable form of analgesic drugs, dexketoprofen trometamol, dexamethasone sodium phosphate, metamizole sodium, diclofenac sodium, thiocolchicoside, on the activity of purified human carbonic anhydrase I and II were evaluated. The effect of these drugs on erythrocyte hCA I and hCA II was compared to recombinant hCA I and hCA II expressed in Ecoli. IC(50) values of the drugs that caused inhibition were determined by means of activity percentage diagrams. The IC(50) concentrations of dexketoprofen trometamol and dexamethasone sodium phosphate on hCA I were 683 ?M and 4250 ?M and for hCA II 950 ?M and 6200 ?M respectively. Conversely, the enzyme activity was increased by diflofenac sodium. In addition, thiocolchicoside has not any affect on hCA I and hCA II. The effect of these drugs on erythrocyte hCA I and hCA II were consistent with the inhibition of recombinant enzymes. PMID:21534860

Gökçe, Ba?ak; Gençer, Nahit; Arslan, Oktay; Turko?lu, Sumeyye Aydogan; Alper, Meltem; Köçkar, Feray

2011-05-03

291

The study of Analgesic, Antidiarrhoeal and Anti-oxidant Effect of Ethanolic Extracts of Ecbolium linnaenum in Albino Mice  

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Full Text Available The Ecbolium linnaenum(leaves) is used as a folk medicine in Bangladesh for pain, diarrhea and infectious diseases. Phytochemical evaluation of the ethanolic extracts of Ecboliumlinnaenumleaves demonstratesthese pharmacologic effect for the presence of alkaloids, tannins, gums,flavonoids and absence of carbohydrates, steroids, saponins. In this present study an attempt was made to determine the analgesic, antidiarrhoel, antioxidantand antimicrobial effectin Swiss Albino mice. Ethanolic extracts of250 and 500 mg/kg showed significant inhibition of writhing reflex 36.20% (P< 0.01) and 54.48% (P< 0.001), respectively while the standard drug diclofenac-Na was 75.52% (P< 0.001) at a dose of 25 mg/kg body weight.In the castor oil-induced diarrhoealmice, the ethanolic extracts of 250 mg/kg & 500 mg/kg, raised the latent period and reduced the number of stools comparing with standard drug Loperamide. 0.02% DPPH solution of ethanol on TLC plate showed the presence of anti-oxidant components in the Ecboliumlinnaenum.From the % inhibition of ascorbic acid and Ecboliumlinnaenum we observe that it has anti-oxidation effect. The IC50 (inhibitory conc. 50%) for ascorbic acid is approximately 1 µg/ml and for the sample it is more than 500 µg/ml. The ethanolic extract of Ecboliumlinnaenum was tested for antimicrobial activity against a number of both gram positive and gram-negative bacteria but it does not show any anti-microbial effect.

Md Shamsuddin Sultan Khan; Rabiul Islam; Md Kamrul Hasan Chowdhury

2013-01-01

292

Anti-inflammatory, analgesic and anti-ulcerogenic effect of total alkaloidal extract from Murraya koenigii leaves in animal models.  

UK PubMed Central (United Kingdom)

The fresh leaves of Murraya koenigii are often added to various dishes in Asian countries due to the delicious taste and flavour that they impart. In the present study, the effect of the total alkaloidal extract from Murraya koenigii leaves (MKA) with respect to anti-inflammatory, analgesic and anti-ulcerogenic effects were evaluated using different experimental animal models. Oral supplementation of MKA at 10, 20 and 40 mg kg(-1) body weight successfully and dose-dependently reduced the formation of oedema induced by carrageenan, histamine and serotonin as well as formaldehyde-induced arthritis. In addition, the extract (10, 20 and 40 mg kg(-1), p.o.) attenuated the writhing responses induced by an intraperitoneal injection of acetic acid and late phase of pain response induced by a subplantar injection of formalin in mice. MKA at higher doses (20 and 40 mg kg(-1), p.o) reduced the early phase response induced by formalin as well as reaction time on hot plate models. Interestingly, there was no ulcer score with the ulcerogenic effect of MKA. Moreover, all the doses of MKA (10, 20 and 40 mg kg(-1), p.o) showed promising anti-ulcerogenic activity with protection against acute gastric ulcers induced by ethanol plus hydrochloric acid and aspirin models in a dose dependent manner.

Mani V; Ramasamy K; Abdul Majeed AB

2013-04-01

293

Analgesic effect of sustained-release flurbiprofen administered at the site of tissue injury in the oral surgery model.  

UK PubMed Central (United Kingdom)

Nonsteroidal anti-inflammatory drugs produce their analgesic and adverse effects through interaction with cyclooxygenase in a variety of tissues. The authors evaluated the therapeutic potential of administering a sustained-release formulation of flurbiprofen into a surgical wound following oral surgery to produce analgesia at the site of injury while minimizing exposure to potential targets for toxicity. Subjects (N = 98) received 1 of 8 treatments: flurbiprofen in a microparticle formulation in doses of 3.125 mg, 6.25 mg, 12.5 mg, 25 mg, or 50 mg; PO flurbiprofen 25 mg or 50 mg; or placebo. The flurbiprofen microparticle formulation or matching placebo was placed into the extraction sites at the end of surgery (removal of 2 lower impacted third molars). The sum of the pain visual analog scale over the 6-hour observation period demonstrated significantly less pain (P < .05) for flurbiprofen microparticle in comparison with placebo. Fewer subjects remedicated in the flurbiprofen microparticle drug groups, primarily for the 12.5-mg and higher doses. The incidence of adverse effects and local complications did not differ across groups. These data suggest that direct administration of flurbiprofen in a microparticle formulation at a site of tissue injury delays the onset and lowers the intensity of postoperative pain at lower doses than usually administered orally.

Dionne RA; Haynes D; Brahim JS; Rowan JS; Guivarc'h PH

2004-12-01

294

The Evaluation of the Analgesic Effect of Hydro-Alcoholic Extract of Solanum Melongena in Syrian Mice Using Tail Flick Test  

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Full Text Available Introduction: Nowadays, many researches are being conducted in order to evaluate the analgesic effects of different plants which have been used as sedative in traditional medicine. Solanum Melongena is a plant with different theories about its analgesic effects. In this experimental trial research, the effects of intraperitoneal(IP) injection of hydro-alcoholic extract of Solanum Melongena were assessed and compared with different doses of morphine and distilled water in Syrian mice. Methods: The effects of different doses of Solanum Melongena (1, 10, 100, and 1000µg/Kg), different doses of morphine sulfate (1, 2, and 4 µg/Kg) and distilled water on acute pain was assessed in Syrian mice. Tail flick latency after IP injection was measured for 75 minutes as the index of pain tolerance, using a tail flick apparatus which projects a condensed light stimulus on the animal's tail. Results: Our findings showed that different doses of Solanum increased analgesia index. This effect was more prominent in 45-60 minutes after IP injections which was significantly greater than the control group (p<0.05(. Conclusion: Our findings indicated that the hydro-alcoholic extract of Solanum Melongena produces analgesic effect in a dose- related manner.

M Rezaeisadrabadi; MH Dashti-R; M Anvari; H Falah-Tafti; S Zanbagh

2011-01-01

295

Study of the anti-inflammatory and analgesic effects of novel rigid benzofuran-3, 4-dihydroxy chalcone by formalin, hot-plate and carrageenan tests in mice.  

Science.gov (United States)

It is reported that dihydroxy chalcones have analgesic and anti-inflammatory effects. Study of the structure activity relationship (SAR) shows that benzofuran-3-one derivatives may be more effective in this respect. In this study, a new (Z)-2-(3,4-dihydroxybenzylidene)-5-methoxybenzofuran-3(2H)-one (compound 5) was synthesized and its analgesic and anti-inflammatory effects were evaluated by formalin, carrageenan and hot-Plate methods in mice. The results showed that, compound 5 induced significant antinociceptive and anti-inflammatory effect (P<0.01). Maximum analgesia (42.6%) was obtained at dose of 25 mg/kg in the first phase of formalin test. The effect of compound 5 was higher (87.7%) in chronic phase of inflammation induced by formalin (P<0.01). Administration of 25 mg/kg of compound 5 inhibited the inflammation induced by carrageenan, 32.8% and 41.7%, 1 and 3 hour after carrageenan injection, respectively. In addition, this dose of compound 5, induces significant analgesia (20.2%) in hot plate test 45 minutes after injection (P<0.01). Therefore it seems that compound 5 has potential for discovery of a compound with potent anti-inflammatory and analgesic effects and its scaffold could be use for further structural modifications. PMID:19783518

Heidari, Mahmoud Reza; Foroumadi, Alireza; Noroozi, Hojat; Samzadeh-Kermani, Ali; Azimzadeh, Behzad Sarvar

2009-10-01

296

Analgesic, Antipyretic and Anti-inflammatory Effect of the Whole Plant Extract of Desmostachya bipinnata Stapf (Poaceae) in Albino Rats  

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Full Text Available Analgesic, Antipyretic and anti-inflammatory effect of petroleum ether, benzene chloroform, ethanol and aqueous extract of the whole parts of Desmostachya bipinnata Stapf (Poaceae) was investigated in albino rats. Animals were given a subcutaneous injection of 12% w/v suspension of yeast (1ml /100gm Body weight) suspended in 0.5% w/v methylcellulose solution which leads to pyrexia. Oral administration of petroleum ether, chloroform, ethanol and aqueous extract of the whole parts of Desmostachya bipinnata Stapf (Poaceae) at a dose 300 mg/kg body weight into six groups of animal for both the activities were shown significantly reduce the elevated body temperature of rat which was compared with standard paracetamol (marketed product) and diclofenac sodium respectively. The anti-inflammatory activity was evaluated by using Digital plethysmometer. The study was carried out using dose of 300 mg/kg orally. All the extracts produced statistically significant and dose dependent inhibition of edema induced by carrageenan at all doses when compared to the control groups.

Somezeet Panda1*, N. S. K Choudhury 2, V. Jagannath Patro3, Dipti Kanta Pradhan, Goutam Kumar Jana1

2009-01-01

297

[Addition of fentanyl to mepivacaine in axillary brachial plexus block. Effects on the anesthetic and postoperative analgesic quality  

UK PubMed Central (United Kingdom)

The possible potentiating effect of phentanyl on mepivacaine in brachial plexus blockade was evaluated, both for operative anesthesia and postoperative analgesia. Sixty ASA I patients, scheduled for upper limb surgery, were selected and distributed in 3 groups: 1) Mepivacaine 1% 40 ml (control group); 2) Mepivacaine 1% 40 ml + phentanyl 100 micrograms; 3) Mepivacaine 1% 40 ml + subcutaneous phentanyl 100 micrograms. The latency time and the quality of anesthesia were evaluated. The duration of analgesia was evaluated on the basis of the time from the administration of the first analgesic. There were no significant differences between the 3 groups in the latency times of the development of blockade nor in the quality of surgical anesthesia. Also, there were no significant differences in the duration of postoperative analgesia (307, 316 and 326 minutes, respectively, in each group). It was concluded that the addition of phentanyl 100 micrograms to the local anesthetic in the axillary blockade of the brachial plexus does not change the anesthetic characteristics nor the time of postoperative analgesia.

Morros Vińoles C; Pérez Cuenca MD; Castillo Monsegur J; Cedo Valloba F

1991-03-01

298

Analgesic and sympatholytic effects of low-dose intrathecal clonidine compared with bupivacaine: a dose-response study in female volunteers.  

UK PubMed Central (United Kingdom)

BACKGROUND: A wide range of doses has been suggested for intrathecal clonidine, but no dose-ranging study has examined analgesic effects below 100 µg. The primary aim of this volunteer study was to assess the dose vs analgesic effect relationship for doses of intrathecal clonidine below 100 µg. METHODS: After IRB approval and signed informed consent, 11 healthy female volunteers participated in this randomized, double-blinded, cross-over study using a dose-ranging sparse-sampling technique. Participants received intrathecal clonidine (doses 0-100 µg; n=10) and intrathecal bupivacaine (doses 0-8.8 mg; n=9) on separate study days. At baseline, 30, and 60 min from drug administration, experimental heat pain tolerance was assessed at both a lumbar and a cranial dermatome. Heat and cold perception thresholds were assessed at the same time intervals. Heart rate (HR), arterial pressure, and forearm-finger and toe-leg cutaneous temperature gradients (Tfinger-arm and Ttoe-leg) were used as measures of sympatholysis. RESULTS: Both intrathecal clonidine and bupivacaine caused significant, dose-dependent analgesic effects at the leg but not the head. Significant analgesia to experimental heat pain was detected above 25 µg clonidine and 3 mg bupivacaine. Administration of bupivacaine but not clonidine resulted in a significant dose-related decrease in HR and Ttoe-leg; neither drug caused dose-related sympatholytic effects in the doses used. CONCLUSIONS: After 50 µg clonidine or 5 mg bupivacaine, the heat pain tolerance increased by ?1°C, similar to the analgesic effect of 5 mg epidural morphine or 30 µg epidural fentanyl in previous studies using this experimental heat pain model. Our results provide additional data for rational dose selection of intrathecal clonidine.

Ginosar Y; Riley ET; Angst MS

2013-08-01

299

Comparison of analgesic effects of morphine, fentanyl, and remifentanil with intravenous patient-controlled analgesia after cardiac surgery.  

UK PubMed Central (United Kingdom)

OBJECTIVE: The purpose of this study was to compare the analgesic effects of remifentanil with 2 other opioid agents, morphine and fentanyl, after cardiac surgery. DESIGN: Prospective, randomized, and double-blinded study. SETTINGS: This study was performed at Uludag University hospital. PARTICIPANTS: Seventy-five patients undergoing off-pump coronary artery bypass surgery were included in the study. INTERVENTIONS: Anesthesia was standardized. Cases were randomized into 3 groups consisting of 25 patients in each. Groups M, F, and R were given morphine HCl (1 mg/mL) with an infusion rate of 0.3 mg/h and 1-mg bolus doses; fentanyl (50 microg/mL) with an infusion rate of 1 microg/kg/h and 10-microg bolus; and, remifentanil (50 microg/mL) with an infusion rate of 0.05 microg/kg/min and 0.5-microg/kg bolus, respectively. Continuous infusion was started immediately after the completion of the surgery. MEASUREMENTS AND MAIN RESULTS: Pain was assessed by using a visual analog scale (0-10), and sedation was assessed with the Ramsey sedation score (1-6) 30 minutes, 1, 2, 4, 12, and 24 hours after extubation. The number of boluses and demands, time to extubation, and side effects were analyzed. Visual analog scale, sedation scores, and mean extubation times were similar in all groups. Total number of boluses and demands were statistically more in the remifentanil group. Regarding the side effects, nausea and vomiting was higher in group M (p < 0.05), whereas itching was prominent in group F (p < 0.05). CONCLUSIONS: Despite the different durations of these 3 opioid agents, the infusion dose of remifentanil was as effective as morphine and fentanyl after OPCAB surgery with fewer side effects.

Gurbet A; Goren S; Sahin S; Uckunkaya N; Korfali G

2004-12-01

300

Effects of Melatonin and Vitamin E on Peripheral Neuropathic Pain in Streptozotocin-Induced Diabetic Rats  

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Full Text Available Objective(s)Previous studies have indicated that diabetes mellitus might be accompanied by neuropathic pain. Oxidative stress is implicated as a final common pathway in development of diabetic neuropathy. Pharmacological interventions targeted at inhibiting free radical production have shown beneficial effects in diabetic neuropathy. The aim of this study was to investigate and compare the possible analgesic effects of melatonin and vitamin E in diabetic rats.Materials and MethodsThis study was performed on 32 male Wistar rats divided into 4 groups: control, diabetic, melatonin-treated diabetic and vitamin E-treated diabetic. Experimental diabetes was induced by intraperitoneal streptozotocin (50 mg/kg) injection. Melatonin (10 mg/kg, i.p.) and vitamin E (100 mg/kg, i.p.) were injected for 2 weeks after 21st day of diabetes induction. At the end of administration period, pain-related behavior was assessed using 0.5% formalin test according to two spontaneous flinching and licking responses. The levels of lipid peroxidation as well as glutathione-peroxidase and catalase activities were evaluated in lumbosacral dorsal root ganglia.ResultsFormalin-evoked flinching and total time of licking were increased in both acute and chronic phases of pain in diabetic rats as compared to control rats, whereas treatment with melatonin or vitamin E significantly reduced the pain indices. Furthermore, lipid peroxidation levels increased and glutathione-peroxidase and catalase activities decreased in diabetic rats. Both antioxidants reversed the biochemical parameters toward their control values.ConclusionThese results suggest that oxidative stress may contribute to induction of pain in diabetes and further suggest that antioxidants, melatonin and vitamin E, can reduce peripheral neuropathic pain in streptozotocin-induced diabetic rats.

Farrin Babaei-Balderlou; Samad Zare; Reza Heidari; Farah Farrokhi

2010-01-01

 
 
 
 
301

Medicinal composition with anti-tumor activity and analgesic activity  

UK PubMed Central (United Kingdom)

The invention discloses a medicinal composition with anti-tumor activity and analgesic activity. The medicinal composition consists of active components of sophoridine and diazepam. The medicinal composition can be used for treating hepatic carcinoma, leucemia, malignocytoma, malignant trophoblastic tumor, gastrointestinal cancer, lung cancer, cervical carcinoma and other tumors, has remarkable centrally and peripherally analgesic activity, and is particularly capable of relieving the pain of patients with advanced cancer.

XIUJIAO GAO; JIA LIU; LIMING CHEN; HONGFU JU

302

Pharmacokinetics and analgesic effect of ropivacaine during continuous epidural infusion for postoperative pain relief.  

DEFF Research Database (Denmark)

BACKGROUND: The pharmacokinetics and clinical efficacy of ropivacaine (2.5 mg/ml) during a 24-h continuous epidural infusion for postoperative pain relief in 20 patients scheduled for abdominal hysterectomy were characterized using an open-label, increasing-dose design. METHODS: Through an epidural catheter inserted at T10-T12, a test dose of 7.5 mg ropivacaine was given 3 min before a bolus dose of 42.5 mg and immediately followed by a 24-h continuous epidural infusion with either 10 or 20 mg/h. Peripheral venous plasma samples were collected up to 48 h after infusion, and urinary excretion was followed up to the end of infusion. Postoperative pain at rest, on coughing, and at mobilization was assessed by means of a visual analog scale 2,4,6,8,12, and 24 h after the end of surgery. Sensory (pinprick) and motor block (modified Bromage scale) were assessed at the same intervals. RESULTS: The total plasma concentrations of ropivacaine increased markedly and consistently during the 24-h epidural infusion, in contrast to stable unbound concentrations. Both total and unbound plasma concentrations at the end of infusion were proportional to the total dose, although only the latter was proportional to the infusion rate. The total and unbound plasma clearance was independent of dose. Total mean clearance decreased on average by 21% (P < 0.001) during the last 12 h of epidural infusion, i.e., from 539 +/- 191 ml/min to 418 +/- 138 ml/min, indicating time-dependent kinetics. The unbound clearance also varied between estimates after 8 h of infusion and the end of treatment, i.e., a 5.3% decrease from 10.4 +/- 5.3 l/min to 9.5 +/- 3.9 l/min (P < 0.05). The unbound fraction of ropivacaine in plasma decreased during treatment, and this was related to the increase in alpha1-acid glycoprotein concentration. Pain was generally well controlled, and median visual analog scale scores during mobilization were less than 30 mm in patients receiving ropivacaine at 20 mg/h. CONCLUSIONS: The pharmacokinetics of ropivacaine were independent of dose, but total clearance decreased with time over 24 h. The consistent increase in total plasma concentration during the postoperative epidural infusion contrasted to much less variation in the unbound plasma concentrations of ropivacaine.

Erichsen, C J; Sjövall, J

1996-01-01

303

Anti-Inflammatory and Analgesic Activities of a Novel Biflavonoid from Shells of Camellia oleifera  

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Full Text Available Shells are by-products of oil production from Camellia oleifera which have not been harnessed effectively. The purpose of this research is to isolate flavonoid from shells of Camellia oleifera and evaluate its anti-inflammatory and analgesic effects. The flavonoid was identified as bimolecular kaempferol structure by UV, MS, 1H NMR and 13C NMR spectra, which is a new biflavonoid and first found in Camellia oleifera. It showed dose-dependent anti-inflammatory activity by carrageenin-induced paw oedema in rats and croton oil induced ear inflammation in mice, and analgesic activity by hot plate test and acetic acid induced writhing. The mechanism of anti-inflammation of biflavonoid is related to both bradykinin and prostaglandins synthesis inhibition. The biflavonoid showed both central and peripheral analgesic effects different from aspirin, inhibition of the synthesis or action of prostaglandins may contribute to analgesic effect of biflavonoid. The biflavonoid significantly decreased malonaldehyde (MDA) and increased superoxidase dismutase (SOD) and Glutathione peroxidase (GSH-Px) activity in serum (p < 0.01), revealed strong free radical scavenging activity in vivo. It indicates the biflavonoid can control inflammation and pain by eliminating free radical so as to inhibit the mediators and decrease the prostaglandins. The biflavonoid can be used as a prospective medicine for inflammation and pain.

Yong Ye; Ya Guo; Yue-Ting Luo

2012-01-01

304

The analgesic and anti-rheumatic effects of Thladiantha dubia fruit crude polysaccharide fraction in mice and rats.  

UK PubMed Central (United Kingdom)

ETHNOPHARMACOLOGICAL RELEVANCE: The fruit of Thladiantha dubia has been used in Chinese manchu nationality folk medicine for treatment of various pains, such as rheumatic pain, lumbocrural pain, and dysmenorrhea. The aim of the present study was to evaluate the anti-rheumatic effect of Thladiantha dubia fruit crude polysaccharide (TF-P) fraction in rats. MATERIALS AND METHODS: TF-P was evaluated in mice for analgesic activity using acetic acid-induced abdominal contractions test and for anti-inflammatory activity using xylene-induced ear oedema model. Moreover, rheumatoid arthritis (RA) was induced by injection of CFA into the subplantar surface of the hind paw of the male Wistar rats. Joint swelling was measured. In order to evaluate the effect of TF-P on disease progression, proinflammatory mediators (TNF-? and IL-2), and antioxidant indicators (SOD, MDA, and NO) were determined in rats induced by CFA. Pathologic changes of RA in rats were also observed under light microscope. RESULTS AND CONCLUSIONS: In the present study, TF-P at the dose of 200mg/kg (according to the clinical traditional dosage) significantly reduced writhings and stretchings induced by the acetic acid in mice. TF-P significantly inhibited xylene-induced ear oedema in mice, compared with control group. TF-P significantly inhibited inoculated and non-inoculated joint swellings in rats induced by CFA. TF-P had no effect of body weight in rats. The histopathological analysis suggested that TF-P obviously alleviated the degree of RA rats. TF-P treated rats preserved a nearly normal histological architecture of the joint. Results of the present study confirm the use of Thladiantha dubia traditionally for the treatment of painful and inflammatory conditions. Those results suggest TF-P has protective and therapeutic effects on RA rats induced by CFA.

Wang L; Zhao D; Di L; Xu T; Lin X; Yang B; Zhou X; Yang X; Liu Y

2011-10-01

305

Effects of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood  

DEFF Research Database (Denmark)

The in vitro and in vivo effects of therapeutical doses of acetylsalicylic acid on lymphocyte subpopulations in peripheral blood were investigated with the following results: Acetylsalicylic acid caused both in vitro and in vivo a reduction of complement receptor bearing lymphocytes and of lymphocytes identified with fluorescent rabbit antibody to human Ig (polyvalent) and to human IgG. Sheep red blood cell receptor bearing lymphocytes, and lymphocytes identified with antibody to human IgM and IgD were unaffected by acetylsalicylic acid.

SŘrensen, S F; Dirksen, Asger

1979-01-01

306

Indirect genotoxic effect of gamma rays in human peripheral lymphocytes  

Energy Technology Data Exchange (ETDEWEB)

The aim of this study was to investigate the indirect genotoxic effect of various doses of gamma rays in human peripheral lymphocytes. For this aim, chromosome mediums were irradiated with various doses (2000, 4000, 8000, 16000 rad) of gamma rays. In this study, we were found that SCE (Sister Chromatid Exchange) was increased by gamma rays doses-dependently. In addition to these, percentages of abnormal cells with chromosomal abnormalities and CA (Chromosome Aberration)/Cell were increased by all doses of gamma rays compared to control. Besides, gamma rays decreased the MI dose-dependently. RI was not also reduced at all concentrations. (author)

Ahmet Kayraldiz; Mehmet Topaktas [Cukurova Univ., Adana (Turkey)

2001-03-01

307

Comparison the Analgesic Effects of Single Dose Administration of Tramadol or Piroxicam on Postoperative Pain after Cesarean Delivery  

Directory of Open Access Journals (Sweden)

Full Text Available "nA multimodal approach to postcesarean pain management may enhance analgesia and reduce side effects after surgery. We investigated postoperative pain in a double-blinded, randomized, single-dose comparison of the monoaminergic and µ-opioid agonist tramadol, 100 mg (Group T) and piroxicam 20 mg (Group P) given IM alone- single dose in 150 patients who had elective cesarean delivery. All patients were assessed at 0, 6, 12 and 24 hours post operation for pain degree (by Visual Analogue Score: VAS 1-10), nausea and vomiting. Pain degree was classified as: Painless: 0, Mild: 1-4, Moderate: 5-8, Severe: 9-10. There was no significant difference between the efficacy of tramadol and piroxicam injections (P>0.05). Pain intensity decreased markedly over time in both groups. Mean±SEM pain degrees were as follows: P=7.7±0.5, T=8.2±0.8 after 0 hours; P=5.4±0.6, T=6.1±0.5 after 6 hours; P=3.3±0.4, T=3.4±0.7 after 12 hours; P=1.1±0.4, T=1.3±0.5 after 24 hours of surgery. Side effects were similarly minimal with all treatments. It might be concluded that i.m. injections of 20 mg piroxicam (single dose therapy) could relieve postoperative pain after cesarean section as well as tramadol and it could reduce opioid analgesic requirements with less adverse side effects during the first postoperative 24 h.

Amir Farshchi; Golbarg Ghiasi

2010-01-01

308

[Effect of a novel analgesic disposable urinary catheter in prevention of restlessness caused by catheter-related bladder discomfort in general anesthesia patients in recovery period].  

UK PubMed Central (United Kingdom)

OBJECTIVE: To investigate the effect of a novel analgesic disposable urinary catheter invented by the authors in prevention of restlessness caused by catheter-related bladder discomfort (CRBD) in general anesthesia patients in anesthesia recovery period. METHODS: Two hundred patients, who underwent general anesthesia for general surgical operation, were divided randomly into 2 equal groups: observation group, undergoing insertion of F16 novel analgesic disposable Foley urinary catheter after inducement of general anesthesia, and control group undergoing insertion of conventional F16 Foley urinary catheter after induction of anesthesia. The rate of restlessness caused by CBRD and the rate of catheter pulling-off were compared. RESULTS: The CRBD rate of the observation group was 9%, significantly lower than that of the control group (61%, P < 0.01), the rate of CRBD-caused restlessness of the observation group was 0, significantly lower then that of the control group (23%, P < 0.001). The extent of CRBD of the observation group was significantly lighter than that of the control group. CONCLUSION: The catheter inserting after the induction of anesthesia is an element related to the restlessness in anesthesia recovery period and other serious postoperative complications. The novel analgesic disposable urinary catheter effectively prevents CRBD-caused restlessness in general anesthesia patients in the anesthesia recovery period.

Sun JL; Lu YP; Huang B; Tu HL; Zhou XY; Chen QM; Guo SM; Zong YM

2008-07-01

309

[Interaction between r-aminobutyric acid content of the brain regions and cell immunity in the analgesic effect of adrenocorticotropic hormone in rats  

UK PubMed Central (United Kingdom)

After intraperitoneal injection of ACTH, the content of GABA in hippocampus and the pain threshold were increased. This effect could be decreased by cyclosporin. ACTH decreased SI of MSBT and production of IL-II, and this suppression could be reversed by GABA synthesis inhibitor isoniazid, or GABA receptor blocker picrotoxin. These results suggest that: the analgesic effect of ACTH is related with the increase of GABA content in hippocampus, and cell immunity could be involved the regulation of GABA content in the brain regions. ACTH inhibited the effect of cell immunity, and this effect related to GABA content. Above effect is at least partly mediated by GABA synthesis and GABA receptor.

Li H; Li X; Zaho B; Ruan H; Huan W; Lo Z; Zho CG; Sun W

1993-01-01

310

In vivo analgesic and anti-inflammatory activities of Rosmarinus officinalis aqueous extracts, rosmarinic acid and its acetyl ester derivative.  

UK PubMed Central (United Kingdom)

CONTEXT: Despite several pharmacological applications of Rosmarinus officinalis L. (Lamiaceae), studies on its analgesic and anti-inflammatory properties have been scarce. OBJECTIVE: The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of the aqueous extracts obtained from leaves (AEL) and stems (AES) of Rosmarinus officinalis, as well as its isolated compound--rosmarinic acid (RA). We also prepared and assessed the acetyl ester derivative of RA. MATERIALS AND METHODS: The analgesic activity was evaluated using abdominal constriction and formalin tests. For the evaluation of the anti-inflammatory effects, carrageenin-induced paw edema in rats were used. The extracts were used at doses of 100, 200 and 400?mg?kg?ą compounds were tested at 10, 20 and 40?mg?kg?ą. RESULTS: Orally administered AEL, AES and RA were not significantly active at any of the doses tested during the abdominal constriction test; the acetyl ester derivative of RA displayed significant analgesic activity. In the carrageenin-induced paw edema assay, the acetyl derivative of RA at all the tested doses produced significant anti-inflammatory effects and reduced the number of paw licks in the second phase of the formalin test. DISCUSSION AND CONCLUSION: The results suggest that the analgesic effects of the acetyl derivative of RA operate via a peripheral-mediated mechanism. The acetyl ester derivative of RA is potentially applicable as a new lead compound for the management of pain and inflammation.

Lucarini R; Bernardes WA; Ferreira DS; Tozatti MG; Furtado R; Bastos JK; Pauletti PM; Januário AH; Silva ML; Cunha WR

2013-09-01

311

Analgesic effect of iridoid glycosides from Paederia scandens (LOUR.) MERRILL (Rubiaceae) on spared nerve injury rat model of neuropathic pain.  

UK PubMed Central (United Kingdom)

Iridoid glycosides of Paederia scandens (IGPS) is a major active component isolated from traditional Chinese herb P. scandens (LOUR.) MERRILL (Rubiaceae). The aim of the present study was to investigate the analgesic effect of IGPS on spared nerve injury (SNI) model of neuropathic pain. The SNI model in rats was established by complete transection of the common peroneal and tibial distal branches of the sciatic nerve, leaving the sural branch intact. The mechanical withdrawal threshold (MWT) in response to mechanical stimulation was measured by electronic von Frey filaments on day 1 before operation and on days 1, 3, 5, 7, 10, and 14 after operation, respectively. Nitric oxide synthase (NOS) activity and nitric oxide (NO) production of spinal cord were measured by spectrophotometry and its cyclic guanosine monophosphate (cGMP) content by radioimmunoassay, mRNA expression of inducible NOS (iNOS) and protein kinase G type I (PKG-I, including PKG ?? and PKG I?) of spinal cord were analyzed by RT-PCR. There was a marked mechanical hypersensitivity response observed on day 1 after operation in SNI model, which accompanied with decreased MWT. Treatment with IGPS (70, 140, 280 mg/kg) significantly alleviated SNI-induced mechanical hypersensitivity response evidenced by increased MWT; as well as markedly decreased NOS activity, NO and cGMP levels. At the same time, IGPS (70, 140, 280 mg/kg) could also inhibit mRNA expression of iNOS, PKG ?? and PKG I? in the spinal cord. The results suggested that IGPS possesses antinociceptive effect, which may be partly related to the inhibition of NO/cGMP/PKG signaling pathway in the rat SNI model of neuropathic pain.

Liu M; Zhou L; Chen Z; Hu C

2012-09-01

312

Phytochemical, Analgesic and Anti-Inflammatory Effects of the Ethylacetate Extract of the Leaves of Pseudocedrella Kotschyii  

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Phytochemical screening was carried out on the ethylacetate portion of the ethanolic extract of the leaves of Pseudocedrella kotschyii and then evaluated for its analgesic (acetic acid-induced writhing) and anti-inflammatory (raw egg albumin-induced oedema) activities in mice and rats respectively. ...

Musa, Y M; Haruna, A K; Ilyas, M; Yaro, A H; Ahmadu, A A; Usman, H

313

Lectin extracted from Canavalia grandiflora seeds presents potential anti-inflammatory and analgesic effects.  

Science.gov (United States)

Neutrophil migration is responsible for tissue damage observed in inflammatory diseases and is also implicated in inflammatory nociception. The use of lectins has been demonstrated to be effective in different activities including anti-inflammatory, antimicrobial, and in cancer therapy. In this study, we addressed the potential use of a lectin from Canavalia grandiflora seeds (ConGF) to control neutrophil migration and inflammatory hypernociception. Pretreatment of the animals intravenously (15 min before) with ConGF inhibited neutrophil migration to the peritoneal cavity in a dose-dependent fashion confirmed by an inhibition of rolling and adhesion of leukocytes by intravital microscopy. Another set of experiments showed that pretreatment of the animals with ConGF inhibited the mechanical hypernociception in mice induced by the i.pl. injection of carrageenan or formalin. This anti-nociceptive effect correlated with an effective blockade of neutrophil influx, as assessed by the hind paw tissue myeloperoxidase levels. Furthermore, ConGF had important inhibitory effects on the mouse carrageenan-induced paw edema. In addition, animals treated with ConGF showed inhibition of cytokines release. In conclusion, we demonstrated that the lectin ConGF inhibits neutrophil migration and mechanical inflammatory hypernociception. PMID:19153712

Nunes, Breno S; Rensonnet, Nathalie S; Dal-Secco, Daniela; Vieira, Silvio M; Cavada, Benildo S; Teixeira, Edson H; Moura, Tales R; Teixeira, Cícero S; Clemente-Napimoga, Juliana T; Cunha, Fernando Q; Napimoga, Marcelo H

2009-01-20

314

Lectin extracted from Canavalia grandiflora seeds presents potential anti-inflammatory and analgesic effects.  

UK PubMed Central (United Kingdom)

Neutrophil migration is responsible for tissue damage observed in inflammatory diseases and is also implicated in inflammatory nociception. The use of lectins has been demonstrated to be effective in different activities including anti-inflammatory, antimicrobial, and in cancer therapy. In this study, we addressed the potential use of a lectin from Canavalia grandiflora seeds (ConGF) to control neutrophil migration and inflammatory hypernociception. Pretreatment of the animals intravenously (15 min before) with ConGF inhibited neutrophil migration to the peritoneal cavity in a dose-dependent fashion confirmed by an inhibition of rolling and adhesion of leukocytes by intravital microscopy. Another set of experiments showed that pretreatment of the animals with ConGF inhibited the mechanical hypernociception in mice induced by the i.pl. injection of carrageenan or formalin. This anti-nociceptive effect correlated with an effective blockade of neutrophil influx, as assessed by the hind paw tissue myeloperoxidase levels. Furthermore, ConGF had important inhibitory effects on the mouse carrageenan-induced paw edema. In addition, animals treated with ConGF showed inhibition of cytokines release. In conclusion, we demonstrated that the lectin ConGF inhibits neutrophil migration and mechanical inflammatory hypernociception.

Nunes BS; Rensonnet NS; Dal-Secco D; Vieira SM; Cavada BS; Teixeira EH; Moura TR; Teixeira CS; Clemente-Napimoga JT; Cunha FQ; Napimoga MH

2009-06-01

315

Analgesic and cardiopulmonary effects of intrathecally administered romifidine or romifidine and ketamine in goats (Capra hircus)  

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The study was conducted to evaluate the effects of romifidine alone (50 µg/kg) and a combination of romifidine (50 µg/kg) and ketamine (2.5 mg/kg) after intrathecal administration in goats. Ten adult goats of either sex weighing between 15 and 20 kg were randomly placed in 2 groups (groups I and I...

H.P. Aithal; P. Kinjavdekar; A.M. Pawde; K. Pratap

316

Use of nonopioid analgesics and adjunctive agents in the management of pain in rheumatic diseases.  

Science.gov (United States)

Antirheumatic analgesic medications generally fall into one of the following categories: acetaminophen, corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDs), tramadol, traditional opioids, or adjunctive analgesics. This article does not discuss corticosteroids, opioids, or topical analgesics. Acetaminophen, usually indicated early for mild pain, is often used in combination with other drugs. It has established safety. Traditional NSAIDs are effective in relieving moderate pain in certain inflammatory and noninflammatory conditions. There are many effective choices, but as a class it is fraught with the risk of serious peptic ulcer disease and its complications. Cyclooxygenase-2 specific inhibitors are NSAIDS that reduce the gastrointestinal risk and platelet-mediated bleeding. All NSAIDs may produce peripheral edema, hypertension, and potentiate warfarin. The evidence that coxibs cause thrombotic heart disease is weak. Tramadol is an alternative to musculoskeletal pain management, particularly in patients with moderate to moderately severe pain who do not respond to or who cannot tolerate acetaminophen, NSAIDs, or opioids. The role of analgesic adjuvants is discussed. PMID:11790999

Katz, Warren A

2002-01-01

317

Use of nonopioid analgesics and adjunctive agents in the management of pain in rheumatic diseases.  

UK PubMed Central (United Kingdom)

Antirheumatic analgesic medications generally fall into one of the following categories: acetaminophen, corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDs), tramadol, traditional opioids, or adjunctive analgesics. This article does not discuss corticosteroids, opioids, or topical analgesics. Acetaminophen, usually indicated early for mild pain, is often used in combination with other drugs. It has established safety. Traditional NSAIDs are effective in relieving moderate pain in certain inflammatory and noninflammatory conditions. There are many effective choices, but as a class it is fraught with the risk of serious peptic ulcer disease and its complications. Cyclooxygenase-2 specific inhibitors are NSAIDS that reduce the gastrointestinal risk and platelet-mediated bleeding. All NSAIDs may produce peripheral edema, hypertension, and potentiate warfarin. The evidence that coxibs cause thrombotic heart disease is weak. Tramadol is an alternative to musculoskeletal pain management, particularly in patients with moderate to moderately severe pain who do not respond to or who cannot tolerate acetaminophen, NSAIDs, or opioids. The role of analgesic adjuvants is discussed.

Katz WA

2002-01-01

318

Semi-mechanistic Modelling of the Analgesic Effect of Gabapentin in the Formalin-Induced Rat Model of Experimental Pain.  

UK PubMed Central (United Kingdom)

PURPOSE: The formalin-induced rat model of nociception involves moderate continuous pain. Formalin-induced pain results in a typical repetitive flinching behaviour, which displays a biphasic pattern characterised by peaks of pain. Here we described the time course of pain response and the analgesic effect of gabapentin using a semi-mechanistic modelling approach. METHODS: Male Sprague-Dawley rats received gabapentin (10-100 mg/kg) or placebo 1 h prior to the formalin injection, as per standard protocol. A reduction in the frequency of the second peak of flinching was used as a behavioural measure of gabapentin-mediated anti-nociception. The flinching response was modelled using a mono-exponential function to characterise the first peak and an indirect response model with a time variant synthesis rate for the second. PKPD modelling was performed using a population approach in NONMEM v.7.1.2. RESULTS: The time course of the biphasic response was adequately described by the proposed model, which included separate expressions for each phase. Gabapentin was found to reversibly decrease, but not suppress the flinching frequency of the second response peak only. The mean IC50 estimate was 7,510 ng/ml, with relative standard error (RSE%) of 40%. CONCLUSIONS: A compartmental, semi-mechanistic model provides the basis for further understanding of the formalin-induced flinching response and consequently to better characterisation of the properties of gabapentin, such as the potency in individual animals. Moreover, despite high exposure levels, model predictions show that gabapentin does not completely suppress behavioural response in the formalin-induced pain model.

Taneja A; Troconiz IF; Danhof M; Della Pasqua O

2013-10-01

319

Analgesic Effect of Acupuncture Is Mediated via Inhibition of JNK Activation in Astrocytes after Spinal Cord Injury  

Science.gov (United States)

Acupuncture (AP) has been used worldwide to relieve pain. However, the mechanism of action of AP is poorly understood. Here, we found that AP relieved neuropathic pain (NP) by inhibiting Jun-N-terminal kinase (JNK) activation in astrocytes after spinal cord injury (SCI). After contusion injury which induces the below-level (L4-L5) NP, Shuigou (GV26) and Yanglingquan (GB34) acupoints were applied. At 31 d after injury, both mechanical allodynia and thermal hyperalgesia were significantly alleviated by AP applied at GV26 and GB34. Immunocytochemistry revealed that JNK activation was mainly observed in astrocytes after injury. AP inhibited JNK activation in astrocytes at L4-L5 level of spinal cord. The level of p-c-Jun known, a downstream molecule of JNK, was also decreased by AP. In addition, SCI-induced GFAP expression, a marker for astrocytes, was decreased by AP as compared to control groups. Especially, the number of hypertrophic, activated astrocytes in laminae I–II of dorsal horn at L4-5 was markedly decreased by AP treatment when compared with vehicle and simulated AP-treated groups. When animals treated with SP600125, a specific JNK inhibitor, after SCI, both mechanical allodynia and thermal hyperalgesia were significantly attenuated by the inhibitor, suggesting that JNK activation is likely involved in SCI-induced NP. Also, the expression of chemokines which is known to be mediated through JNK pathway was significantly decreased by AP and SP600125 treatment. Therefore, our results indicate that analgesic effect of AP is mediated in part by inhibiting JNK activation in astrocytes after SCI.

Lee, Jee Y.; Choi, Doo C.; Oh, Tae H.; Yune, Tae Y.

2013-01-01

320

Analgesic Effect of Acupuncture Is Mediated via Inhibition of JNK Activation in Astrocytes after Spinal Cord Injury.  

Science.gov (United States)

Acupuncture (AP) has been used worldwide to relieve pain. However, the mechanism of action of AP is poorly understood. Here, we found that AP relieved neuropathic pain (NP) by inhibiting Jun-N-terminal kinase (JNK) activation in astrocytes after spinal cord injury (SCI). After contusion injury which induces the below-level (L4-L5) NP, Shuigou (GV26) and Yanglingquan (GB34) acupoints were applied. At 31 d after injury, both mechanical allodynia and thermal hyperalgesia were significantly alleviated by AP applied at GV26 and GB34. Immunocytochemistry revealed that JNK activation was mainly observed in astrocytes after injury. AP inhibited JNK activation in astrocytes at L4-L5 level of spinal cord. The level of p-c-Jun known, a downstream molecule of JNK, was also decreased by AP. In addition, SCI-induced GFAP expression, a marker for astrocytes, was decreased by AP as compared to control groups. Especially, the number of hypertrophic, activated astrocytes in laminae I-II of dorsal horn at L4-5 was markedly decreased by AP treatment when compared with vehicle and simulated AP-treated groups. When animals treated with SP600125, a specific JNK inhibitor, after SCI, both mechanical allodynia and thermal hyperalgesia were significantly attenuated by the inhibitor, suggesting that JNK activation is likely involved in SCI-induced NP. Also, the expression of chemokines which is known to be mediated through JNK pathway was significantly decreased by AP and SP600125 treatment. Therefore, our results indicate that analgesic effect of AP is mediated in part by inhibiting JNK activation in astrocytes after SCI. PMID:24040124

Lee, Jee Y; Choi, Doo C; Oh, Tae H; Yune, Tae Y

2013-09-09

 
 
 
 
321

[The role of humoral factors in the mechanism of the analgesic effect of electroacupuncture  

UK PubMed Central (United Kingdom)

An experimental model of acute painful trauma under electroacupuncture (EAP) protection was established. During the first 15 minutes of acute pain and EAP F2 alpha-prostaglandin, serotonin, and histamine concentrations decreased in arterial blood corresponding to increased concentrations of endogenous opiates in cerebrospinal fluid. In 30 minutes of acute pain and EAP the concentration of opiates (methionine-enkephaline, leucine-enkephaline) begins to decrease, but F2 alpha-prostaglandine, serotonin and histamine content increases significantly. The concentration of cyclic nucleotides changes significantly at investigation stages. However, they are not significant in EAP mechanism, but they are modulators of endogenous opiate effects and implement interaction between them and prostaglandines. We consider that the analgetic effect caused by EAP under acute surgical trauma is connected not only with endogenous opiate system activation, but with synthesis suppression of "pain substances".

Himmelfarb GN; Schumilowa IJ

1990-01-01

322

[Effect of haloperidol on the analgesic activity of opiate agonists administered intracisternally and intrathecally  

UK PubMed Central (United Kingdom)

The mu-agonist morphine more actively inhibited the complex reflex manifestations of pain responses (the Hafner test and hot plate) in mice as compared to the spinal pain reflexes (tail flick). The delta-agonist D-Ala2-D-Leu5-enkephalin (DADL) abolished the responses of both types in the same doses. Haloperidol potentiated the ability of morphine and DADL to inhibit nociceptive responses at the cerebral level. The potentiating effect of this neuroleptic on inhibition of spinal nociceptive responses by opiate agonists was only observed at a dose of 5 mg/kg. Haloperidol could also in some of the tests potentiate the antinociceptive effect of the kappa-agonist bremazocine and the sigma-agonist SKF 10.047, however their activity was significantly lower than that of morphine and DADL.

Chichenkov ON; Korobov NV; Petrov VE

1985-07-01

323

Analgesic effects of amlodipine and its interaction with morphine and ketorolac-induced analgesia.  

UK PubMed Central (United Kingdom)

1. The antinociceptive effects of amlodipine, administered subcutaneously (s.c.), intracerebroventricularly (i.c.v.) and intrathecally (i.t.) were examined with the acetic acid writhing and tail-flick tests in mice. Amlodipine was also tested in combination with morphine and ketorolac. Isobolographic analyses were used to define the nature of functional interactions between amlodipine and morphine or ketorolac. 2. The s.c. (0.1, 1.25, 2.5, 5 and 10 mg/kg), i.c.v. (2.5, 5, 10 and 20 micrograms/mice) and i.t. (2.5, 5, 10 and 20 micrograms/mice) administration of amlodipine exhibited a dose-dependent antinociceptive effect in the writhing test but had no effect on the tail-flick latency. Isobolographic analyses revealed an additive interaction between amlodipine and morphine or ketorolac in the writhing test. 3. These results suggest that amlodipine induces antinociception and increases antinociceptive action of morphine and ketorolac, possibly through a decrease in cellular calcium availability.

Do?rul A; Ye?ilyurt O; Deniz G; I?imer A

1997-11-01

324

The sedative and analgesic effects of detomidine-butorphanol and detomidine alone in donkeys  

Directory of Open Access Journals (Sweden)

Full Text Available Butorphanol and detomidine constitute an effective combination for sedation and analgesia in horses. This trial was undertaken to assess the effectiveness of this combination in donkeys. The detomidine and butorphanol were given intravenously one after the other. A dose of 10 mg/kg of detomidine and 25 mg/kg of butorphanol was used. Sedation is easily extended by additional doses of butorphanol. The average dose of detomidine was 11.24 mg/kg and that of butorphanol was 28.0 mg/kg. Four donkeys in the detomidine group required additional sedation and analgesia. Detomidine alone did not totally eliminate coronary band pain. Heart rates dropped significantly in the first minute after the injection of the combination. One donkey developed an atrioventricular block, while another developed a sino-atrial block. Four donkeys developed a Cheyne-Stokes respiratory pattern. The combination of detomidine and butorphanol is an effective combination for sedation and analgesia of donkeys for standing procedures.

K.E. Joubert; P. Briggs; D. Gerber; R.G. Gottschalk

2012-01-01

325

Analgesic effects of a single preoperative dose of pregabalin after laparoscopic sleeve gastrectomy.  

UK PubMed Central (United Kingdom)

BACKGROUND: The treatment of pain in obese patients is always a challenge. These patients have low pain thresholds, and the use of opioids can be especially harmful. Intraoperative nervous fiber section and the high temperatures of electrical scalpels probably contribute to the generation of postoperative neuropathic pain. We hypothesized that an antineuropathic pain drug like pregabalin could be helpful to optimize postoperative analgesia by reducing the requirement for opioids and their associated side effects. METHODS: Eighty adults undergoing laparoscopic sleeve gastrectomy were randomly assigned to orally receive either placebo capsules (control) or pregabalin (150 mg) 2 h before surgery. Postoperative morphine consumption during the first 24 postoperative hours was registered. Visual analog pain scores (VAS) were assessed at 1, 2, 4, 6, 8, 12, 16, and 24 h after surgery. Both the incidence of adverse reactions and patient satisfaction were also assessed. RESULTS: Over a 24-h period, the morphine consumption in the pregabalin group was 11.51?±?7.93 mg, whereas in the control group, it was 23.07?±?9.57 mg (p?effective and safe analgesia with a low incidence of adverse effects.

Cabrera Schulmeyer MC; de la Maza J; Ovalle C; Farias C; Vives I

2010-12-01

326

Morphine-6-glucuronide: analgesic effects and receptor binding profile in rats  

Energy Technology Data Exchange (ETDEWEB)

The antinociceptive effects of morphine-6-glucuronide (M6G) were examined in two animal models of pain, the tail immersion test (reflex withdrawal to noxious heat) and the formalin test (behavioral response to minor tissue injury). In the tail immersion test, M6G produced and increase in withdrawal latency that rose rapidly between 0.01 and 0.025 ug ICV or 1 and 2 mg/kg SC. A further increase occurred at doses greater than 0.2 ug ICV or 4 mg/kg SC and was associated with marked catelepsy and cyanosis. Naloxone, 0.1 mg/kg SC, shifted the lower component of the dose-effect relation by a factor of 24. In the formalin test, 0.01 ug M6G ICV produced hyperalgesia, while between 0.05 and 0.2 ug ICV, antinociception increased rapidly without toxicity. The dose effect relations for hyperalgesia and antinociception were shifted to the right by factors of 20- and 3-fold, respectively. By comparison, ICV morphine was 60 (formalin test) to 145-200 (tail immersion test) times less potent than M6G. At sub-nanomolar concentrations, M6G enhanced the binding of (/sup 3/H)-etorphine, (/sup 3/H)-dihydromorphine and (/sup 3/H)-naloxone to rat brain membrane receptors by 20-40%. At higher concentrations, M6G displaced each ligand from binding sites, with K/sub i/ values of about 30 nM, as compared to morphine K/sub i/ values of about 3 nM.

Abbott, F.V.; Palmour, R.M.

1988-01-01

327

Morphine-6-glucuronide: analgesic effects and receptor binding profile in rats  

International Nuclear Information System (INIS)

The antinociceptive effects of morphine-6-glucuronide (M6G) were examined in two animal models of pain, the tail immersion test (reflex withdrawal to noxious heat) and the formalin test (behavioral response to minor tissue injury). In the tail immersion test, M6G produced and increase in withdrawal latency that rose rapidly between 0.01 and 0.025 ug ICV or 1 and 2 mg/kg SC. A further increase occurred at doses greater than 0.2 ug ICV or 4 mg/kg SC and was associated with marked catelepsy and cyanosis. Naloxone, 0.1 mg/kg SC, shifted the lower component of the dose-effect relation by a factor of 24. In the formalin test, 0.01 ug M6G ICV produced hyperalgesia, while between 0.05 and 0.2 ug ICV, antinociception increased rapidly without toxicity. The dose effect relations for hyperalgesia and antinociception were shifted to the right by factors of 20- and 3-fold, respectively. By comparison, ICV morphine was 60 (formalin test) to 145-200 (tail immersion test) times less potent than M6G. At sub-nanomolar concentrations, M6G enhanced the binding of [3H]-etorphine, [3H]-dihydromorphine and [3H]-naloxone to rat brain membrane receptors by 20-40%. At higher concentrations, M6G displaced each ligand from binding sites, with K/sub i/ values of about 30 nM, as compared to morphine K/sub i/ values of about 3 nM

1988-01-01

328

Skin vasodilation and analgesic effect of a topical nitric oxide-releasing hydrogel.  

UK PubMed Central (United Kingdom)

New approaches based on topical treatments are needed for treating pain and impaired dermal blood flow. We used a topical Pluronic F127 hydrogel containing S-nitrosoglutathione (GSNO) as a prodrug to generate free NO, an effector molecule that exerts both dermal vasodilation and antinociceptive effects. GSNO-containing hydrogels underwent gelation above 12 °C and released free NO at rates that were directly dependent on the GSNO concentration in the range of 50-150 mM. The topical application of this material led to dose-response dermal vasodilation in healthy volunteers and to a reduction of up to 50 % of the hypernociception intensity in Wistar rats that were subjected to inflammatory pain. Mechanistic investigations indicated that the antinociceptive effect of the topical F127/GSNO hydrogels is produced by the local activation of the cGMP/PKG/KATP channel-signaling pathway, which was stimulated by the free NO that diffused through the skin. These results expand the scope of the biomedical applications of this material and may represent a new approach for the topical treatment of inflammatory pain.

Vercelino R; Cunha TM; Ferreira ES; Cunha FQ; Ferreira SH; de Oliveira MG

2013-09-01

329

Analgesic effects of intrathecal tramadol in patients undergoing caesarean section: a randomised, double-blind study.  

UK PubMed Central (United Kingdom)

BACKGROUND: Intrathecal tramadol combined with local anaesthetics has been used for postoperative analgesia following lower abdominal and perineal surgery. The present study evaluated the effect of intrathecal tramadol on spinal block characteristics and neonatal outcome after elective caesarean section. METHODS: Eighty full-term parturients scheduled for elective caesarean section were randomly divided into two groups. In the fentanyl group, patients received intrathecal 0.5% bupivacaine 10mg with fentanyl 10?g; in the tramadol group, patients were given the same dose of bupivacaine with tramadol 10mg. Sensory and motor block characteristics, duration of postoperative analgesia, maternal side effects, and neonatal outcome were compared. RESULTS: One patient in the tramadol group and two patients in the fentanyl group were excluded from data analysis. Median [interquartile range] duration of postoperative analgesia in the tramadol and the fentanyl groups was 300 [240-360] min and 260 [233-300] min respectively (P=0.02). The incidence of shivering was lower in patients who received tramadol (5%) than those who had fentanyl (32%) (P=0.003). Apgar scores, umbilical cord acid-base measurement and neurologic and adaptive capacity scores were comparable between the two groups. CONCLUSION: Compared to intrathecal fentanyl 10?g, tramadol 10mg, as an adjunct to bupivacaine for subarachnoid block for caesarean section, showed a longer duration of analgesia with a reduced incidence of shivering.

Subedi A; Biswas BK; Tripathi M; Bhattarai BK; Pokharel K

2013-11-01

330

Clinical effects of preemptive analgesia using three different analgesics in strabismus surgery  

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Full Text Available AIM:To compare the effects of preemptive analgesia of parecoxib, butorphanol, and pethidine used in and after strabismus surgery, and explore an effective and safe method of analgesia for strabismus surgery. METHODS: This was a prospective, randomized, double-blind, placebo-controlled study.After the ethic committee approval and written conformed consent were obtained, 80 ASA ? patients aged 18-50 years undergoing strabismus surgery under local anesthesia were randomly allocated to 4 groups(n=20 each): group P received intramuscular parecoxib(40mg), group B received intramuscular butorphanol(1mg), group D received intramuscular pethidine(50mg), and group N received intramuscular normal saline(2mL). All patients received the drug at 30 minutes before surgery. Basal heart rate(HR)and meananerial pressure(HAP)were recorded on the day before surgery. The intensity of pain was measured using(numeric rating scales)NRS(0-10, 0=no pain, 10=worst pain)and recorded during operation time(T1). Meanwhile, culocardiacreflex(OCR), nausea and vomiting, and sweating were also recorded. NRS, nausea and vomiting were recorded at 2 hours(T2), 4 hours(T3), 8 hours(T4)after operation. RESULTS: The NRS scores at T1 were significantly lower in groups P, B, and D than in group N. OCR, nausea and vomiting, and sweating at T1 were not significantly different among the 4 groups. The nausea and vomiting were significantly higher in group D than in groups P, B, and N. The NRS scores at T2 were not significantly different among the 4 groups. The NRS scores in groups D and N at T3 were significantly higher than those at T2. And the NRS scores at T3 were significantly higher in group D and N than groups P and B. The nausea and vomiting were significantly higher in group D than in groups P, B, and N. The NRS, nausea and vomiting were not significantly different among the 4 groups. The NRS scores in groups P and B were not significantly different at T2, T3, and T4. CONCLUSION:Preemptive analgesia with 40mg of parecoxib for strabismus surgery under local anesthesia is effective intraoperatively and postoperatively, and can reduce the postoperative nausea and vomiting.

Chun - Jian Li; Hui Yu; Ping Chen; Hua - Qing Gong

2013-01-01

331

Repeated naloxone treatments and exposures to weak 60-Hz magnetic fields have 'analgesic' effects in snails.  

UK PubMed Central (United Kingdom)

Results of studies with rodents have shown that animals repeatedly injected with the opioid antagonist, naloxone, acquire a hypoalgesic response to thermal nociceptive stimuli. The present study revealed a similar response in the terrestrial pulmonate snail, Cepaea nemoralis. Snails receiving daily injections of naloxone followed by measurements of thermal nociceptive sensitivity also developed hypoalgesia. Daily brief (30-min) exposures to a weak 60-Hz magnetic field (1.0 gauss or 0.1 mT), which acutely antagonize opioid-mediated nociception and antinociception in a manner comparable to that of naloxone, also led to the expression of a hypoalgesic responses. This suggests that opioid antagonist-induced thermal hypoalgesia may be a basic feature of opioid systems. This naloxone- and magnetic field-induced 'analgesia' is consistent with either a facilitation of aversive thermal conditioning and or antagonism of the excitatory, hyperalgesic effects of low levels of endogenous opioids.

Kavaliers M; Ossenkopp KP

1993-08-01

332

Repeated naloxone treatments and exposures to weak 60-Hz magnetic fields have 'analgesic' effects in snails.  

Science.gov (United States)

Results of studies with rodents have shown that animals repeatedly injected with the opioid antagonist, naloxone, acquire a hypoalgesic response to thermal nociceptive stimuli. The present study revealed a similar response in the terrestrial pulmonate snail, Cepaea nemoralis. Snails receiving daily injections of naloxone followed by measurements of thermal nociceptive sensitivity also developed hypoalgesia. Daily brief (30-min) exposures to a weak 60-Hz magnetic field (1.0 gauss or 0.1 mT), which acutely antagonize opioid-mediated nociception and antinociception in a manner comparable to that of naloxone, also led to the expression of a hypoalgesic responses. This suggests that opioid antagonist-induced thermal hypoalgesia may be a basic feature of opioid systems. This naloxone- and magnetic field-induced 'analgesia' is consistent with either a facilitation of aversive thermal conditioning and or antagonism of the excitatory, hyperalgesic effects of low levels of endogenous opioids. PMID:8402190

Kavaliers, M; Ossenkopp, K P

1993-08-20

333

Comparison of Postoperative Analgesic Effects of Thoracic Epidural Morphine and Fentanyl  

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Full Text Available Objective: In our study, we aimed to compare epidural morphine and fentanyl analgesia and the side effects in post-thoracotomy pain management. Material and Methods: Forty patients, planned for elective thoracotomy were included. Bupivacain- morphine was administered through an epidural catheter to the patients in Group-M while bupivacain-fentanyl was given in Group-F. Pain assessment was carried out with the Visual Analogue Scale (VAS) and VAS-I and VAS-II were assessed in 0, 4, 16 and 24th hour in the postoperative unit. Adverse effects were recorded after the 24th hour. Statistical analyses were performed by using Two-sample independent-t test, Mann Whitney-U test, Wilcoxon-signed ranks test and Pearson chi-squared tests. Results: Although, the VAS-I and VAS-II scores were lower in Group-M than Group-F, the difference was not significant statistically (p>0.05). When other hours were compared with initial states, beginning from the 4th hour, in both groups there was a statistically significant drop in VAS-I and VAS-II scores at all times (p<0.001). Comparing the complications between the groups, in Group-M nausea-vomiting (p<0.015) and bradycardia (p<0.012) were found significantly more frequently than in Group-F. Conclusion: We concluded that, in pain management after thoracic surgery, either morphine or fentanyl may be chosen in thoracal epidural analgesia but, especially in the early postoperative hours, close follow-up is necessary due to the risk of bradycardia development.

Gönül Sa??ro?lu

2011-01-01

334

Comparison of Analgesic Effects of Intraperitoneal Lornoxicam and Ropivacaine Administration in Laparoscopic Cholecystectomy  

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Full Text Available Objectives: In this randomized prospective study, we investigated the effects of lornoxicam vs. ropivacaine for the management of postoperative pain in patients undergoing elective laparoscopic cholecystectomy.Patients and Methods: Patients were randomized into three groups and received 150 mg (80 mL) ropivacaine or 16 mg lornoxicam (80 mL) or placebo (80 mL saline) via multi-regional intraperitoneal instillation and port sites infiltration. Patient-controlled analgesia (PCA) device was used. Tramadol 50 mg tolerable dose, 5 mg/hour basal infusion, bolus dose 20 mg, locked 30 min, 4 hour limit were applied as 200 mg. Postoperative pain was assessed with 100-mm visual analog scale (VAS) at rest, while coughing, and during mobilization. Pain scores were recorded in the post-anesthesia care unit, and at 2, 4, 8, 12,18 and 24 h after the surgery.Results: At 24 h, VAS scores at rest and while coughing were found significantly lower in ropivacaine and lornoxicam group when compared with control group (p=0.047). The percentage of patients needing tramadol was significantly lower with ropivacaine and lornoxicam compared with control (p<0.001, p=0.018). There was no statistically significant difference between ropivacaine and lornoxicam group.Conclusion: Multi-regional, intraperitoneal instillation and port site infiltration of ropivacaine and lornoxicam during laparoscopic cholecystectomy reduces the postoperative pain.

Ceyhun MEMEDOV

2010-01-01

335

Analgesic Effects of Microwave Ablation of Bone and Soft Tissue Tumors Under Local Anesthesia.  

UK PubMed Central (United Kingdom)

OBJECTIVE: To assess the feasibility and efficacy of microwave ablation (MWA) of painful refractory bone and soft tissue tumors performed under local anesthesia. STUDY DESIGN: A retrospective study between 2011 and 2013. SETTING: A single center, Academic Interventional Pain Management Unit. SUBJECTS: Fifteen patients with 25 refractory painful bone (N?=?19) or soft tissue (N?=?6) tumors treated with MWA were consecutively included. METHOD: Local Institutional Review Board approval was obtained, and written informed consent was waived. Lesions included spinal (N?=?3), sacral (N?=?4), and extraspinal (N?=?18) locations. Pain was measured on a visual analog scale (VAS) from 0 to 10 before and immediately after procedure, at 1 week, and on a monthly basis following procedure. MWA procedures were always performed under computed tomography guidance and local anesthesia along with nitrous oxide inhalation. RESULTS: Mean ablation time was 4.09 minutes (range 1-11) with an average of 4.2 cycles with a mean ablation power of 60?W. Preprocedure mean VAS score was 7.2?±?0.97 (range 6-9). Follow-up postprocedure VAS scores were as follows: day 0: 1.64?±?1.86, day 7: 1.82?±?1.79, month 1: 2.05?±?2.03 (14/15 patients), month 3: 2.13?±?1.81, month 6: 2.36?±?2.17; and were statistically significant (P?effective in the management of painful refractory bone and soft tissue tumors. It may therefore be considered as a potential alternative to existing percutaneous ablation techniques in the management of bone and soft tissue tumors.

Kastler A; Alnassan H; Pereira PL; Alemann G; Barbé DA; Aubry S; Tiberghien F; Kastler B

2013-09-01

336

[Preventive analgesic effect of intraoperative administration of ibuprofen-arginine on postmastectomy pain syndrome  

UK PubMed Central (United Kingdom)

The efficacy of preemptive analgesia on postoperative pain is discussed. From experimental neurophysiological data, the present policy of preventive analgesia aims at precluding modifications of the nervous system secondary to a nervous lesion and the appearance of chronic pain, particularly of the neurogenic kind. The post-mastectomy pain syndrome (PMPS) falls within the realm of neurogenic pain and is still poorly understood and underestimated. This study evaluated the preemptive effect of a perioperative administration of an oral non steroid anti-inflammatory, the ibuprofen-arginine, on PMPS. Thirty patients scheduled for partial or total mastectomy with axillary dissection were prospectively and randomly assigned to 2 groups. The ibuprofen-arginine group (group I) (n = 15), received an oral administration of 400 mg of ibuprofen-arginine, 90 min before surgery, 2 h after surgery and then every 8 h in the first 32 postoperative hours. The control group (group C) received in doubled blind a placebo at the same time. At 6 months, we looked after pain or dysesthesia. We confirmed the diagnosis of PMPS in presence of association of diagnosis criterias. Fourteen patients in each group have been included. Eighty-six percent of the patients (13 patients in group I and 11 patients in group C) presented at 6 months dysesthesia of the upper member ipsilateral to the mastectomy and/or the operated breast, appearing either immediately or after a laps of time. Nine patients (group I) and 6 patients (group C) had PMPS. Postoperative radiotherapy and lymphoedema were statistically associated with PMPS (p = 0.019 and p = 0.011). The perioperative preventive administration of a non-steroid anti-inflammatory drug reduces neither the incidence of pain in the first post-operative months, nor the appearance of PMPS at 6 months. These results suggest that others factors than the nervous lesion may play a role in the occurrence of PMPS, as radiotherapy, lymphoedema, but also psychosocials factors.

Lakdja F; Dixmérias F; Bussičres E; Fonrouge JM; Lobéra A

1997-03-01

337

Effects of limited peripheral vision on shuttle sprint performance of soccer players.  

UK PubMed Central (United Kingdom)

This study examined the effect of limited peripheral vision on the shuttle sprint performance of soccer players. Participants were 14 male soccer players of a student soccer club (M age = 22.1 yr., SD = 1.3 yr.). They performed a repeated shuttle sprint with full and limited peripheral vision. Mean total sprint time and mean turning time increased significantly with limited peripheral vision. It is concluded that only turning during shuttle sprint performance decreases when sprinting with a restricted peripheral field of view, indicating the use of peripheral vision for the control of directional changes while sprinting.

Lemmink KA; Dijkstra B; Visscher C

2005-02-01

338

Effects of limited peripheral vision on shuttle sprint performance of soccer players.  

Science.gov (United States)

This study examined the effect of limited peripheral vision on the shuttle sprint performance of soccer players. Participants were 14 male soccer players of a student soccer club (M age = 22.1 yr., SD = 1.3 yr.). They performed a repeated shuttle sprint with full and limited peripheral vision. Mean total sprint time and mean turning time increased significantly with limited peripheral vision. It is concluded that only turning during shuttle sprint performance decreases when sprinting with a restricted peripheral field of view, indicating the use of peripheral vision for the control of directional changes while sprinting. PMID:15773707

Lemmink, Koen A P M; Dijkstra, Baukje; Visscher, Chris

2005-02-01

339

N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.  

UK PubMed Central (United Kingdom)

It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists.

Deur C; Agrawal AK; Baum H; Booth J; Bove S; Brieland J; Bunker A; Connolly C; Cornicelli J; Dumin J; Finzel B; Gan X; Guppy S; Kamilar G; Kilgore K; Lee P; Loi CM; Lou Z; Morris M; Philippe L; Przybranowski S; Riley F; Samas B; Sanchez B; Tecle H; Wang Z; Welch K; Wilson M; Yates K

2007-08-01

340

N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.  

Science.gov (United States)

It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists. PMID:17562362

Deur, Christopher; Agrawal, Arun K; Baum, Heidi; Booth, John; Bove, Susan; Brieland, Joan; Bunker, Amy; Connolly, Cleo; Cornicelli, Joseph; Dumin, JoAnn; Finzel, Barry; Gan, Xinmin; Guppy, Sheila; Kamilar, Gregg; Kilgore, Kenneth; Lee, Pil; Loi, Cho-Ming; Lou, Zhen; Morris, Mark; Philippe, Laurence; Przybranowski, Sally; Riley, Frank; Samas, Brian; Sanchez, Brian; Tecle, Haile; Wang, Ziqiang; Welch, Kathryn; Wilson, Michael; Yates, Karen

2007-05-31

 
 
 
 
341

ANALGESIC AND ANTI-INFLAMMATORY POTENTIAL OF THE PLANT ERVATAMIA CORONARIA (STAPF.)  

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Full Text Available ABSTRACT: The present study was conducted to evaluate the analgesic and anti-inflammatory potential of the flowers of Ervatamia coronaria. The analgesic activity of the extract was assessed by the acetic acid induced writhing test. Aspirin was used as a standard drug. The anti-inflammatory activity was evaluated by carrageenan induced rat hind paw edema method. The initial paw volume was measured plethysmographically immediately before subplanter injection. The relative increase in the paw volume was measured in control, standard and treated groups, 4h after carrageenan injection. The results of acetic acid writhing test in mice showed a significant decrease in number of wriths in ethanolic extracts of flowers of E. coronaria, suggesting peripheral analgesic effect. In carrageenan induced rat hind paw method; it was found that ethanolic extract of the flowers of E. coronaria, at a dose of 400 mg/kg body weight significantly reduced the oedema volume, which was comparable to standard drug diclofenac sodium. The flowers of the plant exhibited significant analgesic and anti-inflammatory activity, thereby justifying their use in traditional system of medicine.

Himanshu Joshi*, Arun B Joshi, D. Satyanarayana, M.P. Gururaja and C.S Shastry

2013-01-01

342

Analgesic synergy between topical lidocaine and topical opioids.  

UK PubMed Central (United Kingdom)

Topical drugs avoid many of the problematic side effects of systemic agents. Immersion of the tail of a mouse into a solution of dimethyl sulfoxide (DMSO)-containing morphine produces a dose-dependent, naloxone-sensitive, analgesia (ED(50) 6.1 mM; CL 4.3, 8.4) limited to the portion of the tail exposed to the drug. DMSO alone in this paradigm had no analgesic activity. Like morphine, the opioids levorphanol (ED(50) 5.0 mM; CL 3.8, 7.8) and buprenorphine (ED(50) 1. 1 mM; CL 0.7, 1.5) were effective topical analgesics. Lidocaine also was active in the tail-flick assay (ED(50) 2.5 mM; CL 2.0, 3.4), with a potency greater than morphine. As expected, the free base of lidocaine was more potent than its salt. Combinations of a low dose of lidocaine with a low dose of an opioid yielded significantly greater than additive effects for all opioids tested. Isobolographic analysis confirmed the presence of synergy between lidocaine and morphine, levorphanol and buprenorphine. These studies demonstrate a potent interaction peripherally between opioids and a local anesthetic and offer potential advantages in the clinical management of pain.

Kolesnikov YA; Chereshnev I; Pasternak GW

2000-11-01

343

Analgesic synergy between topical lidocaine and topical opioids.  

Science.gov (United States)

Topical drugs avoid many of the problematic side effects of systemic agents. Immersion of the tail of a mouse into a solution of dimethyl sulfoxide (DMSO)-containing morphine produces a dose-dependent, naloxone-sensitive, analgesia (ED(50) 6.1 mM; CL 4.3, 8.4) limited to the portion of the tail exposed to the drug. DMSO alone in this paradigm had no analgesic activity. Like morphine, the opioids levorphanol (ED(50) 5.0 mM; CL 3.8, 7.8) and buprenorphine (ED(50) 1. 1 mM; CL 0.7, 1.5) were effective topical analgesics. Lidocaine also was active in the tail-flick assay (ED(50) 2.5 mM; CL 2.0, 3.4), with a potency greater than morphine. As expected, the free base of lidocaine was more potent than its salt. Combinations of a low dose of lidocaine with a low dose of an opioid yielded significantly greater than additive effects for all opioids tested. Isobolographic analysis confirmed the presence of synergy between lidocaine and morphine, levorphanol and buprenorphine. These studies demonstrate a potent interaction peripherally between opioids and a local anesthetic and offer potential advantages in the clinical management of pain. PMID:11046087

Kolesnikov, Y A; Chereshnev, I; Pasternak, G W

2000-11-01

344

Studies on the analgesic and anti-inflammatory effects of Sideritis candicans Ait. var. eriocephala Webb aerial part.  

UK PubMed Central (United Kingdom)

Different extracts and fractions from Sideritis candicans Ait. var. eriocephala Webb aerial part were investigated for their analgesic, anti-inflammatory and antimicrobial activities in mice. Results indicated that the extracts assayed showed anti-nociceptive activities because they were able to reduce the nociceptive response to chemical pain stimuli, such as in the acetic acid-induced writhing test. Moreover the extracts also possessed anti-inflammatory activity against carrageenan-induced paw oedema and TPA-induced ear oedema, being the chloroform fraction the most active. Further fractionation and analysis of this fraction revealed that the analgesic and anti-inflammatory activities found could be related in part to the presence of phytosterols, alpha and beta amyrin triterpenic derivatives and ent-kaurene type diterpenes in this species, since some of these compounds are endowed with these activities.

Hernández-Pérez M; Sánchez-Mateo CC; Montalbetti-Moreno Y; Rabanal RM

2004-08-01

345

Studies on the analgesic and anti-inflammatory effects of Sideritis candicans Ait. var. eriocephala Webb aerial part.  

Science.gov (United States)

Different extracts and fractions from Sideritis candicans Ait. var. eriocephala Webb aerial part were investigated for their analgesic, anti-inflammatory and antimicrobial activities in mice. Results indicated that the extracts assayed showed anti-nociceptive activities because they were able to reduce the nociceptive response to chemical pain stimuli, such as in the acetic acid-induced writhing test. Moreover the extracts also possessed anti-inflammatory activity against carrageenan-induced paw oedema and TPA-induced ear oedema, being the chloroform fraction the most active. Further fractionation and analysis of this fraction revealed that the analgesic and anti-inflammatory activities found could be related in part to the presence of phytosterols, alpha and beta amyrin triterpenic derivatives and ent-kaurene type diterpenes in this species, since some of these compounds are endowed with these activities. PMID:15234765

Hernández-Pérez, M; Sánchez-Mateo, C C; Montalbetti-Moreno, Y; Rabanal, R M

2004-08-01

346

Comparison of the analgesic effect of acetaminophen codeine and acetaminophen codeine plus caffeine in orthodontic pain and their effect on rate of tooth movement  

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Full Text Available Background and purpose : Pain control during orthodontic treatments is important for patients and dentists. The purpose of this study was to compare the effects of acetaminophen codeine and acetaminophen codeine plus caffeine in orthodontic pain and tooth movement.Materials and methods : This clinical trial was performed on 18 orthodontic patients who voluntarily participated in the study of pain and tooth movement. Patients were divided into two groups: acetaminophen codeine (300mg +20mg) and acetaminophen codeine + caffeine (40mg). Patients received two doses of drug, the first dose was administered 30 min before and another dose 8 hours after chain placement. The horizontal Visual Analogue Scale (VAS) was recruited to evaluate the degree of pain after placement of the chain. The space of the teeth was measured to evaluate the rate of tooth movement before chain placement and also on the days 7 and 14.Results : There was a significant difference between the two groups in pain scores (p=0.048) and acetaminophen codeine plus caffeine caused more analgesic effect than acetaminophen codeine alone. The highest difference of pain levels between the two groups was found 6 hours after chain the placement and there was a decrease of pain during the 2nd to 7th days after treatment. Maximum pain scores recorded in acetaminophen codeine and acetaminophen codeine plus caffeine groups were 4.67±0.96 and 2.44±0.67, respectively which happened in both groups at 17th hours after the treatment. There was no singificant difference between the two groups in the rate of tooth movement.Conclusion : According to the results, a combination of caffeine and acetaminophen codeine could be suggested in orthodontic pain relief. It is also suggested that concurrent use of caffeine can decrease the dose of analgesic drugs and their side effects.

V. Arash; A.A. Moghadamnia; M. Amoozadeh

2005-01-01

347

Brief exposure of mice to 60 Hz magnetic fields reduces the analgesic effects of the neuroactive steroid, 3alpha-hydroxy-4-pregnen-20-one.  

Science.gov (United States)

Relatively weak, extremely low frequency (ELF), magnetic fields have been shown to exert a variety of biological effects, although the modes of action remain to be established. Neuroactive steroids and neurosteroids have been shown to produce a diverse range of rapid centrally mediated behavioral and physiological effects that are reported to be sensitive to magnetic fields. Here we show that brief exposure of male mice to an ELF magnetic field (30 min, 60 Hz, 141 microT peak) significantly reduces the analgesic effects arising from intracerebroventricular (i.c.v.) administration of the centrally produced allylic neuroactive steroid, 3alpha-hydroxy-4-pregnen-20-one (3alphaHP) and that the dihydropyridine (DHP) calcium channel antagonists, diltiazem and nifedipine, block the inhibitory effects of the 60 Hz ELF on 3alphaHP-induced analgesia. These results indicate that exposure to 60 Hz ELF affects the analgesic effects of neuroactive steroids such as 3alphaHP through alterations in calcium channel function. These findings raise the possibility that ELF magnetic fields may, in part, exert their actions through effects on diverse neuroactive steroid modulated processes. PMID:9870343

Kavaliers, M; Wiebe, J P; Ossenkopp, K P

1998-12-01

348

Brief exposure of mice to 60 Hz magnetic fields reduces the analgesic effects of the neuroactive steroid, 3alpha-hydroxy-4-pregnen-20-one.  

UK PubMed Central (United Kingdom)

Relatively weak, extremely low frequency (ELF), magnetic fields have been shown to exert a variety of biological effects, although the modes of action remain to be established. Neuroactive steroids and neurosteroids have been shown to produce a diverse range of rapid centrally mediated behavioral and physiological effects that are reported to be sensitive to magnetic fields. Here we show that brief exposure of male mice to an ELF magnetic field (30 min, 60 Hz, 141 microT peak) significantly reduces the analgesic effects arising from intracerebroventricular (i.c.v.) administration of the centrally produced allylic neuroactive steroid, 3alpha-hydroxy-4-pregnen-20-one (3alphaHP) and that the dihydropyridine (DHP) calcium channel antagonists, diltiazem and nifedipine, block the inhibitory effects of the 60 Hz ELF on 3alphaHP-induced analgesia. These results indicate that exposure to 60 Hz ELF affects the analgesic effects of neuroactive steroids such as 3alphaHP through alterations in calcium channel function. These findings raise the possibility that ELF magnetic fields may, in part, exert their actions through effects on diverse neuroactive steroid modulated processes.

Kavaliers M; Wiebe JP; Ossenkopp KP

1998-12-01

349

Possible analgesic effect of vigabatrin in animal experimental chronic neuropathic pain/ Possível efeito analgésico da vigabatrina na dor neuropática crônica experimental animal  

Scientific Electronic Library Online (English)

Full Text Available Abstract in portuguese O uso de anticonvulsivantes no tratamento de neuralgias despertou um interesse em testar novas drogas anticonvulsivantes, e dentre essas a vigabatrina por possuir mecanismo de açăo gabaérgico. Para isso, foram usados 41 ratos Wistar e em 25 deles induziu-se neuropatia ciática constritiva (modelo de Bennett & Xie). Para testar sintomas de dor, foram quantificados comportamentos espontâneos (coçar-se) e evocados, por meio de estímulos térmicos nocivos (46oC) e năo- (more) nocivos (40oC). Além disso, realizou-se estudo comparativo da vigabatrina com outros anticonvulsivantes analgésicos. Os resultados mostraram um possível efeito analgésico, dose-dependente, de vigabatrina (gama-vinil-GABA) em dor neuropática experimental. Isso foi evidenciado pela diminuiçăo significativa (p<0,05) do comportamento de coçar-se e pelo aumento significativo (p<0,05) da latęncia de retirada da pata posterior direita a estímulos térmicos nocivos. Isso foi corroborado por achados semelhantes em experimentos com anticonvulsivantes (carbamazepina, fenitoína e ácido valpróico) analgésicos. Esse possível efeito analgésico da vigabatrina (ainda năo descrito na literatura) năo é mediado pelo sistema opióide. Abstract in english Since anticonvulsants have been used for treating neuralgias, an interest has arisen to experimentally test vigabatrin for its gabaergic mechanism of action. For this, 41 Wistar rats were used, and in 25 of them a constrictive sciatic neuropathy was induced (Bennet & Xie model). For testing pain symptoms, spontaneous (scratching) and evoked behaviors to noxious (46o C) and non-noxious (40o C) thermal stimuli were quantified. Moreover, a comparative pharmacological study o (more) f vigabatrin with other analgesic anticonvulsant drugs was also performed. The results showed a possible dose-dependent analgesic effect of vigabatrin (gamma-vinyl-GABA) on experimental neuropathic pain, as shown by the significant (p<0.05) decreasing effect of vigabatrin on scratching and by its significant (p<0.05) increasing effect on the latency of the right hindpaw withdrawal of the animals to noxious thermal stimulus. This was corroborated by similar findings with analgesic anticonvulsants (carbamazepine, phenytoin and valproic acid). This possible and not yet described analgesic effect of vigabatrin seems not to be opioid mediated.

ALVES, NILZA D.; CASTRO-COSTA, CARLOS M. DE; CARVALHO, ALBA M. DE; SANTOS, FRANKLIN J. C.; SILVEIRA, DELANO G.

1999-12-01

350

Advances in topical analgesics.  

UK PubMed Central (United Kingdom)

SUMMARY: This review will allow physicians to understand the role of topical agents in the treatment of intractable pain syndromes. Increasing medical providers' familiarity with these agents will allow their incorporation as part of a complex analgesic regimen for an improved pain management plan benefiting the patient population at large.

Anitescu M; Benzon HT; Argoff CE

2013-08-01

351

Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream  

Directory of Open Access Journals (Sweden)

Full Text Available Muthanna F Abdulkarim1*, Ghassan Z Abdullah1*, Mallikarjun Chitneni2, Ibrahim M Salman1, Omar Z Ameer1, Mun F Yam1,3, Elrashid S Mahdi1, Munavvar A Sattar1, Mahiran Basri4, Azmin M Noor11School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia; 2School of Pharmacy and Health Sciences, International Medical University, Kuala Lumpur, Malaysia; 3Faculty of Medicine and Health Sciences, 4Faculty of Science, Universiti Putra Malaysia, Selangor, Malaysia; *The First and Second Authors have Contributed Equally to this WorkIntroduction: During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, antipyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs)-based nanocream containing piroxicam for topical delivery.Methods: A ratio of 25:37:38 of POEs: external phase: surfactants (Tween 80:Span 20, in a ratio 80:20), respectively was selected as th