Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 83

Search results for: analgesic

83 Analgesic and Antipyretic Activity of Thunbergia laurifolia Lindl. Extract

Authors: Nantawan Soonklang, Linda Chularojanamontri, Urarat Nanna

Abstract:

Ethnopharmacological relevance: Thunbergia laurifolia Lindl. belongs to the family Acanthaceae commonly known as Rang jeud in Thailand. This plant is traditionally used in Thailand for centuries as an antidote for several poisons and drug overdose. Aim of the study: This research aimed to study the analgesic and antipyretic activities of T. laurifolia water extract by using animal models. Materials and Methods: The analgesic activity was studied using 2 methods of pain induction including acetic acid and heat induced pain. And the antipyretic activity study was performed by yeast-induced hyperthermia. Results: The results showed that the administration of T. laurifolia extract possessed analgesic activity by reducing acetic acid-induced writhing response and heat-induced pain as well as showed antipyretic activity by decreasing body temperature of hyperthermic rats induced by brewer’s yeast. Conclusion: The study indicates that the T. laurifolia extract possesses analgesic and antipyretic activities in animals.

Keywords: Thunbergia laurifolia extract, analgesic activity, antipyretic activity, hyperthermia

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82 Evaluation of the Analgesic Activity of Defatted Methanol Extract of Capparis spinosa L. Root Barks

Authors: Asma Meddour, Mouloud Yahia, Afaf Benhouda, Souhila Benbia, Hachani Khadhraoui

Abstract:

Peripheral analgesic activity of defatted methanol extract of root barks of Capparis spinosa was tested orally at the dose of 100 and 200 mg/kg against pain induced by acetic acid in rats. The dose of 200 mg/kg presents significant analgesic effect with a percentage of inhibition of torsions of 88.51% compared to the positive control which is the acetylsalicylic acid which represents a percentage of inhibition of 92.55%. The dose of 100 mg/kg presents a percentage of inhibition of 81.68%.

Keywords: peripheral analgesic activity, Capparis spinosa, percentage of inhibition of torsions, chemical sciences

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81 Analgesic Efficacy of Opiorphin and Its Analogue

Authors: Preet Singh, Kavitha Kongara, Dave Harding, Neil Ward, Paul Chambers

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The objective of this study was to compare the analgesic efficacy of opiorphin and its analogue with a mu-receptor agonist; morphine. Opiorphins (Gln-Arg-Phe-Ser-Arg) belong to the family of endogenous enkephalinase inhibitors, found in saliva of humans. They are inhibitors of two Zinc metal ectopeptidases (Neutral endopeptidase NEP, and amino-peptidase APN) which are responsible for the inactivation of the endogenous opioids; endorphins and enkephalins. Morphine and butorphanol exerts their analgesic effects by mimicking the actions of endorphins and enkephalins. The opiorphin analogue was synthesized based on the structure activity relationship of the amino acid sequence of opiorphin. The pharmacological profile of the analogue was tested by replacing Serine at position 4 with Proline. The hot plate and tail flick test were used to demonstrate the analgesic efficacy. There was a significant increase in the time for the tail flick response after an injection of opiorphin, which was similar to the morphine effect. There was no increase in time in the hot plate test after an injection of opiorphin. The results suggest that opiorphin works at spinal level only rather than both spinal and supraspinal. Further work is required to confirm our results. We did not find analgesic activity of the opiorphin analogue. Thus, Serine at position 4 is also important for its pharmacological action. Further work is required to illustrate the role of serine at position 4 in opiorphin.

Keywords: analgesic peptides, endogenous opioids, morphine, opiorphin

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80 Analgesic, Toxicity and Anti-Pyretic Activities of Methanolic Extract from Hyoscyamus albus Leaves in Albinos Rats

Authors: Yahia Massinissa, Henhouda Affaf, Yahia Mouloud

Abstract:

The aim of this study was to investigate the toxicity; analgesic and anti-pyretic properties of standardized HA methanolic extract (HAMeOH) in vivo. The acute toxicity study was performed on rats while adopting the OECD-420 Guidelines (fixed dose procedure). Assessment of analgesic activity was performed in rats with two analgesic models. One was acetic acid induced writhing response and the other formalin-induced paw licking. The anti-pyretic effect was tested by brewer’s yeast induced fever in rats. For the acute toxicity test, the higher dose administration of 2000 mg/kg bw. of Hyoscyamus albus did not produce any toxic signs or deaths in rats. There were no significant differences (p>0.05) in the body and organ weights between control and treated groups. The (LD50) of Hyoscyamus albus was higher than 2000 g/kg bw. In subacute toxicity study, no mortality and toxic signs were observed with the doses of 100 and 200 mg/kg bw. of extracts of for 28 consecutive days. These analgesic experimental results indicated that HAMeOH (100 mg/kg and 200 mg/kg) decreased the acetic acid-induced writhing responses and HAMeOH (100 mg/kg and 200 mg/kg) decreased the licking time in the second phase of the formalin test. Moreover, in the model of yeast induced elevation of the body temperature HAMeOH showed dose-dependent lowering of the body temperature up to 3h at both the doses these results obtained, were comparable to that of paracetamol. The present findings indicate that the leaves of Hyoscyamus albus L. possess potent analgesic and antipyretic activity.

Keywords: Hyoscyamus albus, methanolic extract, toxicity, analgesic activity, antipyretic activity, formalin test

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79 In vivo Anti-inflammatory, Analgesic, and Antipyretic Activities of Aqueous Extract of Leaves of Brocchia cinerea (Vis.)

Authors: Nisrine Chlif, Mohammed Diouri, Amar Bentayeb

Abstract:

Background: The Leaves of Brocchia cinerea (Vis.) (Asteraceae) is used traditionally and ethnomedicinally to alleviate pain, fever, and inflammation conditions. Objective: The current study investigates the anti-inflammatory, analgesic, and antipyretic activities of aqueous extract of the leaves of Brocchia cinerea (LBC). Material and methods: The extract was screened for anti-inflammatory (carrageenan-induced paw edema) and analgesic (acetic acid-induced writhing) activities in Wistar rats. Before acetic acid or carrageenan injection, rats were orally fed LBC (200 and 400 mg/ kg), Indomethacin (10 mg/kg), or Aspirin (100 mg/kg). The antipyretic effect was studied in brewer’s yeast-induced pyrexia model in rats using Paracetamol (100 mg/kg) as a standard drug. Results: The crude extract tested significantly prevented the increase in paw volume as compared to the control at 200 mg/kg and 400 mg/kg. The LBC treatment significantly inhibited pain at 400 mg/kg with a percent inhibition of 55.82%, as well as showing a significant reduction in hyperpyrexia in rats at 400 mg/kg. LBC extract produced a comparable activity to paracetamol at 100 mg/kg (p <0.01). Conclusion: The results of the present study that the leaves of B. cinerea extract exhibited strongly anti-inflammatory, analgesic, and antipyretic properties and justify the traditional use of this plant in inflammation, pain, and fever.

Keywords: analgesic, anti-inflammation, antipyretic, brocchia cinerea

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78 Anti-Inflammatory, Analgesic and Antipyretic Activity of Terminalia arjuna Roxb. Extract in Animal Models

Authors: Linda Chularojmontri, Seewaboon Sireeratawong, Suvara Wattanapitayakul

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Terminalia arjuna Roxb. (family Combretaceae) is commonly known as ‘Sa maw thet’ in Thai. The fruit is used in traditional medicine as natural mild laxatives, carminative and expectorant. Aim of the study: This research aims to study the anti-inflammatory, analgesic and antipyretic activities of Terminalia arjuna extract by using animal models in comparison to the reference drugs. Materials and Methods: The anti-inflammatory study was conducted by two experimental animal models namely ethyl phenylpropionate (EPP)-induced ear edema and carrageenan-induced paw edema. The study of analgesic activity used two methods of pain induction including acetic acid and heat-induced pain. In addition, the antipyretic activity study was performed by induced hyperthermia with yeast. Results: The results showed that the oral administration of Terminalia arjuna extract possessed acute anti-inflammatory effect in carrageenan-induced paw edema. Terminalia arjuna extract showed the analgesic activity in acetic acid-induced writhing response and heat-induced pain. This indicates its peripheral effect by inhibiting the biosynthesis and/or release of some pain mediators and some mechanism through Central nervous system. Moreover, Terminalia arjuna extract at the dose of 1000 and 1500 mg/kg body weight showed the antipyretic activity, which might be because of the inhibition of prostaglandins. Conclusion: The findings of this study indicated that the Terminalia arjuna extract possesses the anti-inflammatory, analgesic and antipyretic activities in animals.

Keywords: analgesic activity, anti-inflammatory activity, antipyretic activity, Terminalia arjuna extract

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77 Design, Synthesis and Anti-Inflammatory Activity of Some Coumarin and Flavone Derivatives Containing 1,4 Dioxane Ring System

Authors: Asif Husain, Shah Alam Khan

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Coumarins and flavones are oxygen containing heterocyclic compounds which are present in various biologically active compounds. Both the heterocyclic rings are associated with diverse biological actions, therefore considered as an important scaffold for the design of molecules of pharmaceutical interest. Aim: To synthesize and evaluate the in vivo anti-inflammatory activity of few coumrain and flavone derivatives containing 1,4 dioxane ring system. Materials and methods: Coumarin derivatives (3a-d) were synthesized by reacting 7,8 dihydroxy coumarin (2a) and its 4-methyl derivative (2b) with epichlorohydrin/ethylene dibromide. The flavone derivatives (10a-d) were prepared by using quercetin and 3,4 dihydroxy flavones. Compounds of both the series were also evaluated for their anti-inflammatory, analgesic activity and ulcerogenicity in animal models by reported methods. Results and Discussion: The structures of all newly synthesized compounds were confirmed with the help of IR, 1H NMR, 13C NMR and Mass spectral studies. Elemental analyses data for each element analyzed (C, H, N) was found to be within acceptable range of ±0.4 %. Flavone derivatives, but in particular quercetin containing 1,4 dioxane ring system (10d) showed better anti-inflammatory and analgesic activity along with reduced gastrointestinal toxicity as compared to other synthesized compounds. The results of anti-inflammatory and analgesic activities of both the series are comparable with the positive control, diclofenac. Conclusion: Compound 10d, a quercetin derivative, emerged as a lead molecule which exhibited potent anti-inflammatory and analgesic activity with significant reduced gastric toxicity.

Keywords: analgesic, anti-inflammatory, 1, 4 dioxane, coumarin, flavone

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76 Toxicity, Analgesic, and Anti-Pyretic Activities of Methanolic Extract from Hyoscyamus albus’ Leaves in Albinos Rats

Authors: Yahia Massinissa, Afaf Benhouda, Mouloud Yahia

Abstract:

Objective: The aim of this study was to investigate the toxicity; analgesic and anti-pyretic properties of standardized HA methanolic extract (HAMeOH) in vivo. Methods: The acute toxicity study was performed on rats while adopting the OECD-420 Guidelines (fixed dose procedure). Assessment of analgesic activity was performed in rats with two analgesic models. One was acetic acid induced writhing response and the other formalin-induced paw licking. The anti-pyretic effect was tested by Brewer’s yeast induced fever in rats. Results: For the acute toxicity test, the higher dose administration of 2000 mg/kg bw. of H.albus did not produce any toxic signs or deaths in rats. There were no significant differences (p>0.05) in the body and organ weights between control and treated groups. The (LD50) of 'H. albus' was higher than 2000 g/kg bw. In subacute toxicity study, no mortality and toxic signs were observed with the doses of 100 and 200 mg/kg bw. of extracts of for 28 consecutive days. These analgesic experimental results indicated that HAMeOH (100 mg/kg and 200 mg/kg) decreased the acetic acid-induced writhing responses and HAMeOH (100 mg/kg and 200 mg/kg) decreased the licking time in the second phase of the formalin test. Moreover, in the model of yeast-induced elevation of the body temperature HAMeOH showed dose-dependent lowering of the body temperature up to 3h at both the doses these results obtained, were comparable to that of paracetamol. Conclusion: The present findings indicate that the leaves of Hyoscyamus albus L. possess potent analgesic and antipyretic activity.

Keywords: Hyoscyamus albus, Umbilicus rupestris, secondary metabolites, NMR with protons, pharmacobiologic activities, methanolic extract

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75 Synthesis and Analgesic activity of 2-(p-Substituted phenyl)-3-[4-(N-Substituted amino) methyl-2-oxo indoilin-3-ylidene]benzenesulfonyl Quinazolin-4(3H)-One Derivatives

Authors: N. Gopal, K. Jaasminerjiit, L. Z. Xiang

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Quinazoline-4(3H)-one ring system has been consistently regarded as promising privileged structural icon owing to its pharmacodynamic versatility in many of its synthetic derivatives as well as in several naturally occurring alkaloids. The literature reveals that 2nd & 3rd positions of the quinazolin-4(3H)-one pharmacophore are the target for substitution with other moieties. On the other hand, sulphanilamide derivatives and isatin moiety also displayed valuable biological activities. Hence, it was thought worthwhile to study the effects of three pharmacophoric moieties like quinazolinone, sulphanilamide and isatin in a single molecule for the better analgesic activity with lower toxicity. Series of novel 2,3-disubstituted quinazolin-4(3H)-one derivatives have been synthesised from the intermediate Schiff base of 2-(4’-substitutedphenyl)-3-[(N-2-oxoindolin-3-ylidene)-4”-sulphonamidophenyl]-quinazolin-4(3H)-one derivatives, which was prepared from reacting 2-(substituted phenyl)-4H-benzo[d][1,3]-oxazin-4-one with sulphanilamide. The required benzoxazinone derivatives were prepared by reacting anthranilic acid with benzoyl chloride. All the compounds structure was characterised by using H1 NMR, IR and Mass spectroscopy. The intermediate Schiff base and final Mannich base compounds were evaluated for their analgesic activity by acetic acid-induced writhing method at the dose of 25mg/kg, 50 mg/kg, and 100 mg/kg (bw) and Diclofenac (25mg/kg of body weight) will be used as the reference drugs. From the results of the study, it has been observed that final Mannich base showed a better analgesic activity when compared to the parent Schiff bases, it was found that compound substituted with N-methyl piperazine at 1st position of the indole nucleus of the final quinazolinone derivatives (GA4B1) i.e. 2-(4’-methoxy phenyl)-3-[4-(N-(1-N-methyl piperazine amine) methyl-2-oxo indoilin-3-ylidene] benzenesulfonyl quinazolin-4(3H)-one increases the analgesic activity and among the synthesised compounds, GA4B1 exhibited quite superior analgesic activity. The remaining Schiff bases and Mannich base derivatives exhibited moderate analgesic activity. All the compounds showed a dose dependent activity. None of the synthesised compound showed ulcer index whereas the standard drug, diclofenac [25 mg/kg (bw)] showed significantly higher gross ulcer index values.

Keywords: analgesic activity, isatin, mannich base, quinazolin-4(3H)-one

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74 Anti-Inflammatory and Analgesic Effects of Methanol Extract of Rhizophora racemosa Leaf in Albino Rats

Authors: Angalabiri-Owei E. Bekekeme, Brambaifa Nelson

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In view of the peculiar environment of the Niger Delta, access to modern health care is limited, hence the inhabitants especially those in the swampy areas resorts to sourcing for alternatives cure for their ailments using plants commonly found in this area without scientific evaluation. Rhizophora racemosa, G. F. Meyer (Rhizophoraceae) is the most abundant mangrove plant in the Niger Delta Area of Nigeria. The plant has been observed to be used for relief of a toothache and dysmenorrhoea among some Ijaw communities in the region. This work has revealed the likely potential of the plant in drug discovery and development. The crude methanol extract at doses of 300 mg/kg and 600 mg/kg (intraperitoneal) were tested for analgesic effect using fresh egg albumin induced inflammatory pain and Randall–Sellito method to assess the pain threshold. The anti-inflammatory effect was also evaluated with the extract at doses of 300 mg/kg and 600 mg/kg (intraperitoneal) using acute inflammatory model; fresh egg albumin induced paw oedema and assessed using Plethysmometer in rats. The methanol extracts 300 mg/kg and 600 mg/kg exhibited a significant (P < 0.001) and dose-dependent analgesic activity compared with the negative control and a standard drug diclofenac using ANOVA with Least Significant Difference post hoc test as evidenced by increased pain threshold. Also, the extract significantly (P < 0.001) reduced the rat paw oedema induced by the sub plantar injection of fresh egg albumin when compared with the negative control and a standard diclofenac using above statistical methods. This study revealed that the plant possesses analgesic and anti-inflammatory activities hence provide scientific bases for use as medicine.

Keywords: analgesic, anti-inflammatory, plethysmometer, Rhizophora racemosa

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73 Is Sodium Channel Nav1.7 an Ideal Therapeutically Analgesic Target? A Systematic Review

Authors: Yutong Wan, John N. Wood

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Introduction: SCN9A encoded Nav1.7 is an ideal therapeutic target with minimal side effects for the pharmaceutical industry because SCN9A variants can cause both human gains of function pain-related mutations and loss of function pain-free mutations. This study reviews the clinical effectiveness of existing Nav1.7 inhibitors, which theoretically should be powerful analgesics. Methods: A systematic review is conducted on the effectiveness of current Nav1.7 blockers undergoing clinical trials. Studies were mainly extracted from PubMed, U.S. National Library of Medicine Clinical Trials, World Health Organization International Clinical Trials Registry, ISRCTN registry platform, and Integrated Research Approval System by NHS. Only studies with full text available and those conducted using double-blinded, placebo controlled, and randomised designs and reporting at least one analgesic measurement were included. Results: Overall, 61 trials were screened, and eight studies covering PF 05089771 (Pfizer), TV 45070 (Teva & Xenon), and BIIB074 (Biogen) met the inclusion criteria. Most studies were excluded because results were not published. All three compounds demonstrated insignificant analgesic effects, and the comparison between PF 05089771 and pregabalin/ibuprofen showed that PF 05089771 was a much weaker analgesic. All three drug candidates only have mild side effects, indicating the potentials for further investigation of Nav1.7 antagonists. Discussion: The failure of current Nav1.7 small molecule inhibitors might attribute to ignorance of the key role of endogenous systems in Nav1.7 null mutants, the lack of selectivity and blocking potency, and central impermeability. The synergistic combination of analgesic drugs, a recent UCL patent, combining a small dose of Nav1.7 blockers and opioids or enkephalinase inhibitors dramatically enhanced the analgesic effects. Conclusion: The current clinical testing Nav1.7 blockers are generally disappointing. However, the newer generation of Nav1.7 targeting analgesics has overcome the major constraints of its predecessors.

Keywords: chronic pain, Nav1.7 blockers, SCN9A, systematic review

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72 Bioactivities and Phytochemical Studies of Petroleum Ether Extract of Pleiogynium timorense Bark

Authors: Gehan F. Abdel Raoof, Ataa A. Said, Khaled Y. Mohamed, Hala M. Mohammed

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Pleiogynium timorense(DC.) Leenh is one of the therapeutically active plants belonging to the family Anacardiaceae. The bark of Pleiogynium timorense needs further studies to investigate its phytochemical and biological activities. This work was carried out to investigate the chemical composition of petroleum ether extract of Pleiogynium timorense bark as well as to evaluate the analgesic and anti-inflammatory activities. The unsaponifiable matter and fatty acid methyl esters were analyzed by Gas chromatography–mass spectrometry (GC-MS). Moreover, analgesic and anti-inflammatory activities were evaluated using acetic acid-induced writhing test and carrageen hind paw oedema models in rats, respectively. The results showed that twenty one compounds in the unsaponifiable fraction were identified representing 92.54 % of the total beak area, the major compounds were 1-Heptene (35.32%), Butylated hydroxy toluene (19.42%) and phytol (12.53%), whereas fifteen compounds were identified in the fatty acid methyl esters fraction representing 94.15% of the total identified peak area. The major compounds were 9-Octadecenoic acid methyl ester (35.34%) and 9,12-Octadecadienoic acid methyl ester (29.32%). Moreover, petroleum ether extract showed a significant reduction in pain and inflammation in a dose dependent manner. This study aims to be the first step toward the use of petroleum ether extract of Pleiogynium timorense bark as analgesic and anti-inflammatory drug.

Keywords: analgesic, anti-inflammatory, bark, petroleum ether extract, Pleiogynium timorense

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71 Analgesic and Anti-inflammatoryactivities of Camel Thorn in Experimental Animals

Authors: Abdelkader H. El Debani, Huda Gargoum, Awad G. Abdellatif

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The aim of this study is to investigate analgesic and the anti-inflammatory effects Camel Thorn Extract (CTE) in rodents. Male albino mice weighing 20-25 gm. were divided into different groups each of 8 mice. The control was given normal saline i. p., the first group was given normal saline i. p. the 2nd, 3rd, 4th, groups received different doses of CTE (330, 660, and 1300 mg/kg) respectively and the 6th group received 5mg/kg of morphine i. p. All groups (except the control group) were given acetic acid 40 min after receiving the different treatment. The number of writhes was recorded 5 min after acetic acid injection for 15 min and the % of inhibition of writhing were calculated. Different groups of rats weighing 180- 220 gm., were divided into three groups each of 5 rats. At the beginning, the volumes of the right and left paw in animals were measured by using of the plethysmometer. The 1st group was given 660 mg /kg i. p. of CTE, the 2nd group received indomethacin (5 mg/kg i. p.). One hour later, edema was induced by sub planter injection of 0.1 ml of 1 % freshly prepared suspension of carrageenan into the right hind paws of the rats. The volume of the injected paws and contra-lateral paws were measured at 0, 0.5, 1, 2, 3, 4, and 5 hours using plethysmometer. The volume of the left paw of the rat was subtracted from the volume of the right paw of the same animal. Our results showed that 330,660 and 1300 mg/kg produced 14, 49 and 84%of inhibition of writhes, indicating that CTE has a strong analgesic activity. Our data also showed that the % of inhibition of edema at 30, 60, 120, 180, and 240 min was 14,51,71,61, and 56% in the animals given camel thorn extract whereas these figures in animals given endomethacin were 14, 24, 54, 52, and 54%. These results indicate that camel thorn has anti-inflammatory activities. The mechanism of analgesic and anti-inflammatory activities needs further investigations.

Keywords: camel thorn, imdomethacin, morphine, pharmaceutical medicine

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70 Synthesis, Molecular Modeling and Study of 2-Substituted-4-(Benzo[D][1,3]Dioxol-5-Yl)-6-Phenylpyridazin-3(2H)-One Derivatives as Potential Analgesic and Anti-Inflammatory Agents

Authors: Jyoti Singh, Ranju Bansal

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Fighting pain and inflammation is a common problem faced by physicians while dealing with a wide variety of diseases. Since ancient time nonsteroidal anti-inflammatory agents (NSAIDs) and opioids have been the cornerstone of treatment therapy, however, the usefulness of both these classes is limited due to severe side effects. NSAIDs, which are mainly used to treat mild to moderate inflammatory pain, induce gastric irritation and nephrotoxicity whereas opioids show an array of adverse reactions such as respiratory depression, sedation, and constipation. Moreover, repeated administration of these drugs induces tolerance to the analgesic effects and physical dependence. Further discovery of selective COX-2 inhibitors (coxibs) suggested safety without any ulcerogenic side effects; however, long-term use of these drugs resulted in kidney and hepatic toxicity along with an increased risk of secondary cardiovascular effects. The basic approaches towards inflammation and pain treatment are constantly changing, and researchers are continuously trying to develop safer and effective anti-inflammatory drug candidates for the treatment of different inflammatory conditions such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, psoriasis and multiple sclerosis. Synthetic 3(2H)-pyridazinones constitute an important scaffold for drug discovery. Structure-activity relationship studies on pyridazinones have shown that attachment of a lactam at N-2 of the pyridazinone ring through a methylene spacer results in significantly increased anti-inflammatory and analgesic properties of the derivatives. Further introduction of the heterocyclic ring at lactam nitrogen results in improvement of biological activities. Keeping in mind these SAR studies, a new series of compounds were synthesized as shown in scheme 1 and investigated for anti-inflammatory, analgesic, anti-platelet activities and docking studies. The structures of newly synthesized compounds have been established by various spectroscopic techniques. All the synthesized pyridazinone derivatives exhibited potent anti-inflammatory and analgesic activity. Homoveratryl substituted derivative was found to possess highest anti-inflammatory and analgesic activity displaying 73.60 % inhibition of edema at 40 mg/kg with no ulcerogenic activity when compared to standard drugs indomethacin. Moreover, 2-substituted-4-benzo[d][1,3]dioxole-6-phenylpyridazin-3(2H)-ones derivatives did not produce significant changes in bleeding time and emerged as safe agents. Molecular docking studies also illustrated good binding interactions at the active site of the cyclooxygenase-2 (hCox-2) enzyme.

Keywords: anti-inflammatory, analgesic, pyridazin-3(2H)-one, selective COX-2 inhibitors

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69 A Randomised Controlled Study to Compare Efficacy and Safety of Bupivacaine plus Dexamethasone Versus Bupivacaine plus Fentanyl for Caudal Block in Children

Authors: Ashwini Patil

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Caudal block is one of the most commonly used regional anesthetic techniques in children. Currently, fentanyl is used as an adjuvant to bupivacaine to prolong analgesia but fentanyl is a narcotic. Dexamethasone, a glucocorticoid with strong anti-inflammatory effects provides improvement in post-operative analgesia and post-operative side effects. However, its analgesic efficacy and safety in comparison with fentanyl has not been extensively studied. So the objective of this randomized controlled study is to compare dexamethasone with fentanyl as an adjuvant to bupivacaine for caudal block in children in relation to the duration of caudal analgesia, post-operative analgesic requirement and incidence of post-operative nausea and vomiting. This study included 100 children, aged 1–6 years, undergoing lower abdominal surgeries. Patients were randomized into two groups, 50 each to receive a combination of dexamethasone 0.2 mg/kg along with 1 ml/kg bupivacaine 0.25% (group A) or combination of fentanyl (1 ug/kg) along with 1ml/kg bupivacaine 0.25% (group B). In the post-operative period, pain was assessed using a Modified Objective Pain Scale (MOPS) until 12 hr after surgery and rescue analgesia is administered when MOPS score 4 or more is recorded. Residual motor block, number of analgesic doses required within 24 hr after surgery, sedation scores, intra-operative and post-operative hemodynamic variables, post-operative nausea and vomiting (PONV), and other adverse effects were recorded. Data is analysed using unpaired t test and Significance level of P< 0.05 is considered statistically significant. Group A showed a significantly longer time to first analgesic requirement than group B (p<0.05). The number of rescue analgesic doses required in the first 24 h was significantly less in group A (p<0.05). Group A showed significantly lower MOPS scores than group B(p<0.05). Intra-operative and post-operative hemodynamic variables, Modified Bromage Scale scores, and sedation scores were comparable in both the groups. Group A showed significantly fewer incidences of PONV compared with group B(p<0.05). This study reveals that adding dexamethasone to bupivacaine prolongs the duration of postoperative analgesia and decreases the incidence of PONV as compared to combination of fentanyl to bupivacaine after a caudal block in pediatric patients.

Keywords: bupivacaine, caudal analgesia, dexamethasone, pediatric

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68 Temporary Ureteric Catheterization after Ureteropyeloscopy: Experience from Regional Australia

Authors: Jake Tempo, Jack Crozier, Huay Ann Chia, Philip Tan

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Purpose: A prospective study was performed to determine whether temporary ureteric catheterization should be eliminated as a prophylactic method for preventing ureteric obstruction after uncomplicated ureteropyeloscopic lithotripsy. Material and Methods: From 2010 to 2014, 227 patients underwent uncomplicated ureteroscopic and/or pyeloscopic lithotripsy. Three patient-groups based on postoperative drainage method were analysed: temporary uretericcatheter (TUC), -ureteric JJ stent, and no-stent groups. Exclusion criteria included urosepsis, ureteric injury, and non-surgical complications delaying hospital-discharge. Outcome measures included parenteral analgesic requirements, prolonged hospitalization ≥2 days due to postoperative-pain, and readmissions rate. Results: Delayed discharge was reported in 14.5%(9 of 62) patients in the TUC group compared to 3.4%(4 of 119) in theureteric JJ stent group and 8.7%(4 of 46) in the no-drainage-group (p=0.02). Odds ratio for delayed-discharge between catheter- versus-ureteric JJ stent is 4.9 (95% CI = 1.6-15.0; p < 0.01). Parenteral analgesic requirements in the TUC group (12.9%) was also significantly higher than theureteric JJ stent group (1.7%; p=0.003). Readmissions were negligible between groups. Conclusions: Patients with ureteric catheters after uncomplicated ureteroscopy have a prolonged hospital stay with increased pain and parenteral analgesic requirements. There is a 7.6-fold increased requirement for parenteral analgesia and a 4.2-fold increased risk of delayed-discharge compared to a patient with a ureteric JJ stent.

Keywords: ureteric catheter, ureteric stent, ureteroscopy, pyeloscopy

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67 Utilization of Informatics to Transform Clinical Data into a Simplified Reporting System to Examine the Analgesic Prescribing Practices of a Single Urban Hospital’s Emergency Department

Authors: Rubaiat S. Ahmed, Jemer Garrido, Sergey M. Motov

Abstract:

Clinical informatics (CI) enables the transformation of data into a systematic organization that improves the quality of care and the generation of positive health outcomes.Innovative technology through informatics that compiles accurate data on analgesic utilization in the emergency department can enhance pain management in this important clinical setting. We aim to establish a simplified reporting system through CI to examine and assess the analgesic prescribing practices in the EDthrough executing a U.S. federal grant project on opioid reduction initiatives. Queried data points of interest from a level-one trauma ED’s electronic medical records were used to create data sets and develop informational/visual reporting dashboards (on Microsoft Excel and Google Sheets) concerning analgesic usage across several pre-defined parameters and performance metrics using CI. The data was then qualitatively analyzed to evaluate ED analgesic prescribing trends by departmental clinicians and leadership. During a 12-month reporting period (Dec. 1, 2020 – Nov. 30, 2021) for the ongoing project, about 41% of all ED patient visits (N = 91,747) were for pain conditions, of which 81.6% received analgesics in the ED and at discharge (D/C). Of those treated with analgesics, 24.3% received opioids compared to 75.7% receiving opioid alternatives in the ED and at D/C, including non-pharmacological modalities. Demographics showed among patients receiving analgesics, 56.7% were aged between 18-64, 51.8% were male, 51.7% were white, and 66.2% had government funded health insurance. Ninety-one percent of all opioids prescribed were in the ED, with intravenous (IV) morphine, IV fentanyl, and morphine sulfate immediate release (MSIR) tablets accounting for 88.0% of ED dispensed opioids. With 9.3% of all opioids prescribed at D/C, MSIR was dispensed 72.1% of the time. Hydrocodone, oxycodone, and tramadol usage to only 10-15% of the time, and hydromorphone at 0%. Of opioid alternatives, non-steroidal anti-inflammatory drugs were utilized 60.3% of the time, 23.5% with local anesthetics and ultrasound-guided nerve blocks, and 7.9% with acetaminophen as the primary non-opioid drug categories prescribed by ED providers. Non-pharmacological analgesia included virtual reality and other modalities. An average of 18.5 ED opioid orders and 1.9 opioid D/C prescriptions per 102.4 daily ED patient visits was observed for the period. Compared to other specialties within our institution, 2.0% of opioid D/C prescriptions are given by ED providers, compared to the national average of 4.8%. Opioid alternatives accounted for 69.7% and 30.3% usage, versus 90.7% and 9.3% for opioids in the ED and D/C, respectively.There is a pressing need for concise, relevant, and reliable clinical data on analgesic utilization for ED providers and leadership to evaluate prescribing practices and make data-driven decisions. Basic computer software can be used to create effective visual reporting dashboards with indicators that convey relevant and timely information in an easy-to-digest manner. We accurately examined our ED's analgesic prescribing practices using CI through dashboard reporting. Such reporting tools can quickly identify key performance indicators and prioritize data to enhance pain management and promote safe prescribing practices in the emergency setting.

Keywords: clinical informatics, dashboards, emergency department, health informatics, healthcare informatics, medical informatics, opioids, pain management, technology

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66 Comparative Evaluation of Pentazocine and Tramadol as Pre-Emptive Analgesics for Ovariohysterectomy in Female Dogs

Authors: Venkatgiri, Ranganath, L. Nagaraja, B. N. Sagar Pandav, S. M. Usturge, D. Dilipkumar, B. V. Shivprakash, B. Bhagwanthappa, D. Jahangir

Abstract:

A comparative evaluation of Tramadol and Pentazocine as a pre-emptive analgesic in clinical cases of female dogs undergoing ovariohysterectomy was undertaken during this study. During the study, the following parameters were assessed viz., Rectal temperature (ᵒF), Respiratory rate (breaths/min) and Heart rate (beats/min). Hematological and biochemical parameters viz., total erythrocyte count (TEC) (millions/cmm), hemoglobin (g %), otal leucocytes count (TLC) (thousands/cmm), differential leucocytes count (DLC) (%), serum creatinine (mg/dl), plasma protein (mg/dl), blood glucose (mg/dl) was estimated before the surgery and after administration of general anaesthesia and immediate postoperative periods of 0, 12 and 24 hr respectively. Mean Total Pain Score (MTPS) includes measurement of parameters like posture, vocalization, activity level, response to palpation and agitation at different intervals was calculated before surgery and after administration of general anesthesia and post-operative periods of 1, 2, 4, 6, 12hrs and 24 hrs respectively. Mean Total Pain Score (MTPS) was given for each parameter (Posture, Vocalization, Activity Level, Response to Palpation and Agitation) like 0,1,2,3. (maximum score will be given was 4.). Results were revealed in all three groups including control group. There were significant minor alterations in physiological, hematological and biochemical parameters. MTPS (mean total pain score) were revealed and found a significant alteration when compared with control group. In conclusion, Tramadol found to be a better analgesic and had up to 8hrs of analgesic effect and Pentazocine is superior in post-operative pain management when compared to Tramadol because this group of dogs experienced less surgical stress, consumed less anesthetic dose, they recovered early, and they had less MTPS score.

Keywords: dog, pentazocine, tramadol, ovariohysterectomy

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65 Partnering With Key Stakeholders for Successful Implementation of Inhaled Analgesia for Specific Emergency Department Presentations

Authors: Sarah Hazelwood, Janice Hay

Abstract:

Methoxyflurane is an inhaled analgesic administered via a disposable inhaler, which has been used in Australia for 40 years for the management of pain in children & adults. However, there is a lack of data for methoxyflurane as a frontline analgesic medication within the emergency department (ED). This study will investigate the usefulness of methoxyflurane in a private inner-city ED. The study concluded that the inclusion of all key stakeholders in the prescribing, administering & use of this new process led to comprehensive uptake & vastly positive outcomes for consumer & health professionals. Method: A 12-week prospective pilot study was completed utilizing patients presenting to the ED in pain (numeric pain rating score > 4) that fit the requirement of methoxyflurane use (as outlined in the Australian Prescriber information package). Nurses completed a formatted spreadsheet for each interaction where methoxyflurane was used. Patient demographics, day, time, initial numeric pain score, analgesic response time, the reason for use, staff concern (free text), & patient feedback (free text), & discharge time was documented. When clinical concern was raised, the researcher retrieved & reviewed patient notes. Results: 140 methoxyflurane inhalers were used. 60% of patients were 31 years of age & over (n=82) with 16% aged 70+. The gender split; 51% male: 49% female. Trauma-related pain (57%) saw the highest use of administration, with the evening hours (1500-2259) seeing the greatest numbers used (39%). Tuesday, Thursday & Sunday shared the highest daily use throughout the study. A minimum numerical pain score of 4/10 (n=13, 9%), with the ranges of 5 - 7/10 (moderate pain) being given by almost 50% of patients. Only 3 instances of pain scores increased post use of methoxyflurane (all other entries showed pain score < initial rating). Patients & staff noted obvious analgesic response within 3 minutes (n= 96, 81%, of administration). Nurses documented a change in patient vital signs for 4 of the 15 patient-related concerns; the remaining concerns were due to “gagging” on the taste, or “having a coughing episode”; one patient tried to leave the department before the procedure was attended (very euphoric state). Upon review of the staff concerns – no adverse events occurred & return to therapeutic vitals occurred within 10 minutes. Length of stay for patients was compared with similar presentations (such as dislocated shoulder or ankle fracture) & saw an average 40-minute decrease in time to discharge. Methoxyflurane treatment was rated “positively” by > 80% of patients – with remaining feedback related to mild & transient concerns. Staff similarly noted a positive response to methoxyflurane as an analgesic & as an added tool for frontline analgesic purposes. Conclusion: Methoxyflurane should be used on suitable patient presentations requiring immediate, short term pain relief. As a highly portable, non-narcotic avenue to treat pain this study showed obvious therapeutic benefit, positive feedback, & a shorter length of stay in the ED. By partnering with key stake holders, this study determined methoxyflurane use decreased work load, decreased wait time to analgesia, and increased patient satisfaction.

Keywords: analgesia, benefits, emergency, methoxyflurane

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64 Raw Japanese Quail Egg Produces Analgesic, Anti-Inflammatory and Gastro-Protective Effects in Rats

Authors: Sani Ismaila, Shafiu Yau, Abubakar Salisu, Buhari Salisu, Sharifat Balogun, Mustapha Abubakar, Biobaku Khalid, Agaie Bello

Abstract:

Over the years, Japanese quail egg has been in use in the management of diseases. The objective of this study was to evaluate the analgesic, anti-inflammatory and gastroprotective effects of raw Quail egg (yolk + albumin) in rats. Pain was assessed in rats by recording the latent period and writing reflex, anti-inflammatory effect was determined using both motility and compression test, while the gastro-protective effects were assessed by observing the histology of the stomach after diclofenac-induced gastric ulcers and subsequent treatment with the quail egg, Rats were randomly assigned into 4 groups; Groups I: were the control non-treated (NT), Group II were treated with Tramadol 50 mg/kg/Os (TMD) or Indomethacin (IND) 5mg/kg/Os (positive control for the writhing reflex determination), while group III and IV were treated with 3 and 6g/kg of raw quail egg respectively). Groups treated with quail egg in both doses showed a significant increase in the latent period (p <0 .05) when compared to the control NT, but lower than the group treated with tramadol at 20mins interval (p<0.05). Writing reflexes decrease in groups II, III, and IV compared to the NT group (p < 0.05). While motility increases significantly (p < 0.05) in groups II, compared to I (p<0.05). Control non-treated rats showed a quicker and extensive response to compression using the Vanier calliper on the inflamed paw compared to groups II-IV (p < 0.05). Histological studies of the stomach revealed sloughing of the epithelia, cellular infiltration with micro abscesses in the non-treated, while groups treated concurrently with quail egg showed proliferation of the glandular epithelia and goblet cells, and those treated 30 minutes before diclofenac administration showed proliferation of glands and thickening of the squamous epithelia. This study showed that quail egg has analgesic, anti-inflammatory and gastro-protective potentials and can be used as adjuvant treatment whenever COX-2 enzymes inhibitors are indicated.

Keywords: analgesia, anti-inflammatory, gastroprotective effect, japanese quail egg

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63 Clinical Use of Opioid Analgesics in China: An Adequacy of Consumption Measure

Authors: Mengjia Zhi, Xingmei Wei, Xiang Gao, Shiyang Liu, Zhiran Huang, Li Yang, Jing Sun

Abstract:

Background: To understand the consumption trend of opioid analgesics and the consumption adequacy of opioid analgesic treatment for moderate to severe pain in China, as well as the pain control level of China with international perspective. Importance: To author’s best knowledge, this is the first study in China to measure the adequacy of opioid analgesic treatment for moderate to severe pain considering disease pattern and with the standardized pain treatment guideline. Methods: A retrospective analysis was carried out to show the consumption frequency (daily defined doses, DDDs) of opioid analgesics and its trend in China from 2006 to 2016. Adequacy of consumption measure (ACM) was used to measure the number of needed morphine equivalents and the overall adequacy of opioid analgesic treatment of moderate to severe pain in China, and compared with international data. Results: The consumption frequency of opioid analgesics (DDDs) in China increased from 13,200,000 DDDs in 2006 to 44,200,000 DDDs in 2016, and showed an increasing trend. The growth rate was faster at first, especially in 2013, then slowed down, decreased slightly in 2015. The ACM of China increased from 0.0032 in 2006 to 0.0074 in 2016, with an overall trend of growth. The ACM level of China has been always a very poor level during 2006-2016. Conclusion: The consumption of opioid analgesics for the treatment of moderate to severe pain in China has always been inadequate. There is a huge gap between China and the international level. There are many reasons behind this problem, which lie in different aspects, including medical staff, patients and the public, health systems and social & cultural aspects. It is necessary to strengthen the training and education of medical staff and the patients, to use mass media to disseminate scientific knowledge of pain management, to encourage communications between doctors and patients, to improve regulatory system for the controlled medicines and the overall health systems, and to balance the regulatory goal for avoidance of abuse, and the social goal of meeting the increasing needs of the people for better life.

Keywords: opioid analgesics, adequate consumption measure, pain control, China

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62 Identification of a Lead Compound for Selective Inhibition of Nav1.7 to Treat Chronic Pain

Authors: Sharat Chandra, Zilong Wang, Ru-Rong Ji, Andrey Bortsov

Abstract:

Chronic pain (CP) therapeutic approaches have limited efficacy. As a result, doctors are prescribing opioids for chronic pain, leading to opioid overuse, abuse, and addiction epidemic. Therefore, the development of effective and safe CP drugs remains an unmet medical need. Voltage-gated sodium (Nav) channels act as cardiovascular and neurological disorder’s molecular targets. Nav channels selective inhibitors are hard to design because there are nine closely-related isoforms (Nav1.1-1.9) that share the protein sequence segments. We are targeting the Nav1.7 found in the peripheral nervous system and engaged in the perception of pain. The objective of this project was to screen a 1.5 million compound library for identification of inhibitors for Nav1.7 with analgesic effect. In this study, we designed a protocol for identification of isoform-selective inhibitors of Nav1.7, by utilizing the prior information on isoform-selective antagonists. First, a similarity search was performed; then the identified hits were docked into a binding site on the fourth voltage-sensor domain (VSD4) of Nav1.7. We used the FTrees tool for similarity searching and library generation; the generated library was docked in the VSD4 domain binding site using FlexX and compounds were shortlisted using a FlexX score and SeeSAR hyde scoring. Finally, the top 25 compounds were tested with molecular dynamics simulation (MDS). We reduced our list to 9 compounds based on the MDS root mean square deviation plot and obtained them from a vendor for in vitro and in vivo validation. Whole-cell patch-clamp recordings in HEK-293 cells and dorsal root ganglion neurons were conducted. We used patch pipettes to record transient Na⁺ currents. One of the compounds reduced the peak sodium currents in Nav1.7-HEK-293 stable cell line in a dose-dependent manner, with IC50 values at 0.74 µM. In summary, our computer-aided analgesic discovery approach allowed us to develop pre-clinical analgesic candidate with significant reduction of time and cost.

Keywords: chronic pain, voltage-gated sodium channel, isoform-selective antagonist, similarity search, virtual screening, analgesics development

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61 Combined Effect of Vesicular System and Iontophoresis on Skin Permeation Enhancement of an Analgesic Drug

Authors: Jigar N. Shah, Hiral J. Shah, Praful D. Bharadia

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The major challenge faced by formulation scientists in transdermal drug delivery system is to overcome the inherent barriers related to skin permeation. The stratum corneum layer of the skin is working as the rate limiting step in transdermal transport and reduce drug permeation through skin. Many approaches have been used to enhance the penetration of drugs through this layer of the skin. The purpose of this study is to investigate the development and evaluation of a combined approach of drug carriers and iontophoresis as a vehicle to improve skin permeation of an analgesic drug. Iontophoresis is a non-invasive technique for transporting charged molecules into and through tissues by a mild electric field. It has been shown to effectively deliver a variety of drugs across the skin to the underlying tissue. In addition to the enhanced continuous transport, iontophoresis allows dose titration by adjusting the electric field, which makes personalized dosing feasible. Drug carrier could modify the physicochemical properties of the encapsulated molecule and offer a means to facilitate the percutaneous delivery of difficult-to-uptake substances. Recently, there are some reports about using liposomes, microemulsions and polymeric nanoparticles as vehicles for iontophoretic drug delivery. Niosomes, the nonionic surfactant-based vesicles that are essentially similar in properties to liposomes have been proposed as an alternative to liposomes. Niosomes are more stable and free from other shortcoming of liposomes. Recently, the transdermal delivery of certain drugs using niosomes has been envisaged and niosomes have proved to be superior transdermal nanocarriers. Proniosomes overcome some of the physical stability related problems of niosomes. The proniosomal structure was liquid crystalline-compact niosomes hybrid which could be converted into niosomes upon hydration. The combined use of drug carriers and iontophoresis could offer many additional benefits. The system was evaluated for Encapsulation Efficiency, vesicle size, zeta potential, Transmission Electron Microscopy (TEM), DSC, in-vitro release, ex-vivo permeation across skin and rate of hydration. The use of proniosomal gel as a vehicle for the transdermal iontophoretic delivery was evaluated in-vitro. The characteristics of the applied electric current, such as density, type, frequency, and on/off interval ratio were observed. The study confirms the synergistic effect of proniosomes and iontophoresis in improving the transdermal permeation profile of selected analgesic drug. It is concluded that proniosomal gel can be used as a vehicle for transdermal iontophoretic drug delivery under suitable electric conditions.

Keywords: iontophoresis, niosomes, permeation enhancement, transdermal delivery

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60 Opioid Administration on Patients Hospitalized in the Emergency Department

Authors: Mani Mofidi, Neda Valizadeh, Ali Hashemaghaee, Mona Hashemaghaee, Soudabeh Shafiee Ardestani

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Background: Acute pain and its management remained the most complaint of emergency service admission. Diagnostic and therapeutic procedures add to patients’ pain. Diminishing the pain increases the quality of patient’s feeling and improves the patient-physician relationship. Aim: The aim of this study was to evaluate the outcomes and side effects of opioid administration in emergency patients. Material and Methods: patients admitted to ward II emergency service of Imam Khomeini hospital, who received one of the opioids: morphine, pethidine, methadone or fentanyl as an analgesic were evaluated. Their vital signs and general condition were examined before and after drug injection. Also, patient’s pain experience were recorded as numerical rating score (NRS) before and after analgesic administration. Results: 268 patients were studied. 34 patients were addicted to opioid drugs. Morphine had the highest rate of prescription (86.2%), followed by pethidine (8.5%), methadone (3.3%) and fentanyl (1.68). While initial NRS did not show significant difference between addicted patients and non-addicted ones, NRS decline and its score after drug injection were significantly lower in addicted patients. All patients had slight but statistically significant lower respiratory rate, heart rate, blood pressure and O2 saturation. There was no significant difference between different kind of opioid prescription and its outcomes or side effects. Conclusion: Pain management should be always in physicians’ mind during emergency admissions. It should not be assumed that an addicted patient complaining of pain is malingering to receive drug. Titration of drug and close monitoring must be in the curriculum to prevent any hazardous side effects.

Keywords: numerical rating score, opioid, pain, emergency department

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59 Anti-Inflammatory, Anti-Nociceptive and Anti-Arthritic Effects of Mirtazapine, Venalfaxine and Escitalopram in Rats

Authors: Sally A. El Awdan

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Objective and Design: The purpose of this study was to evaluate the anti inflammatory, anti-arthritic and analgesic effects of antidepressants. Methods: Carrageenan model was used to assess effect on acute inflammation. Paw volume were measured at 1, 2, 3 and 4th hour post challenge. Anti-nociceptive effect was evaluated by hot plate method. Chronic inflammation was developed using Complete Freund's Adjuvant (CFA). The animals were injected with Freund’s adjuvant in sub-plantar tissue of the right posterior paw. Paw volume, ankle flexion scores, adjuvant-induced hyperalgesia and serum cytokine levels were assessed. Results: Results obtained demonstrate that mirtazapine, venalfaxine and escitalopram significantly and dose-dependently inhibited carrageenan-induced rat paw oedema. Mirtazapine, venalfaxine and escitalopram increased the reaction time of rats in hot plate test. We observed an increase in paw volume, ankle flexion scores, thermal hyperalgesia, serum levels of interleukin-1β, PGE2 and TNF-α, induced by intraplantar CFA injection. Regular treatment up to 28 days of adjuvant-induced arthritic rats with mirtazapine, venalfaxine and escitalopram showed anti anti-inflammatory and analgesic activities by suppressing the paw volume, recovering the paw withdrawal latency, and by inhibiting the ankle flexion scores in CFA-induced rats. In addition significant reduction in serum levels of interleukin-1β, PGE2 and TNF-α level in arthritic rats was reduced by treatment with drugs. Conclusion: These results suggest that antidepressants have significant anti-inflammatory and anti-nociceptive effects in acute and chronic models in rats, which may be associated with the reduction of interleukin-1β, PGE2 and TNF-α levels.

Keywords: antidepressants, carrageenan, anti-nociceptive, Complete Freund's Adjuvant

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58 Comparative Study of Analgesic Efficacy of Ultrasound Guided Femoral Nerve Block Versus Intravenous Fentanyl Injection in Fracture Femur Patients at Emergency Department

Authors: Asmaa Hamdy, Israa Nassar, Tarek Aly

Abstract:

Introduction: Femoral fractures are the most common presentation in the Emergency Department (ED), and they can present as isolated injuries or as part of a polytrauma situation. To provide optimum pain management care to these patients, practitioners must be well prepared and current with utilizing modern evidence-based knowledge and practices. Management of pain associated with fracture femur in the emergency department has a critical role in the satisfaction of patients and preventing further complications. This study aimed to evaluate the analgesic efficacy of ultrasound-guided femoral nerve block compared with intravenous fentanyl in fractures of the femur in patients presented to the Emergency Department. Patients and Methods: Fifty patients with femur fractures were divided into two groups: Group A: In this group (twenty-five patients) were given intravenous fentanyl 2 micro-grams/kg and re-assessed for pain by Visual Analogue Score (VAS). Group B: In this group (twenty-five patients) underwent ultrasonography-guided femoral nerve block and were re-assessed for pain by VAS. Results: VAS score on the movement of the fractured limb between group A and group B at a 10-minute post-intervention period shows P= 0.043, and hence the difference is significant. VAS score on the movement of the fractured limb between group A and group B during a 10-minute post-intervention period showed a significant difference. Seventeen patients in group A had major PID with a percentage of 63% VS 10 patients in group B with a percentage of 37%. conclusion: both femoral nerve block and intravenous fentanyl are effective in relieving pain in patients with femur fractures. But femoral nerve block provides better and more intense analgesia and major pain intensity difference in less time. Moreover, the use of FNB had fewer side effects and more Hemodynamics stability compared to opioids.

Keywords: femur fracture, nerve block, fentanyl, ultrasound guided

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57 Comparison of the Postoperative Analgesic Effects of Morphine, Paracetamol, and Ketorolac in Patient-Controlled Analgesia in the Patients Undergoing Open Cholecystectomy

Authors: Siamak Yaghoubi, Vahideh Rashtchi, Marzieh Khezri, Hamid Kayalha, Monadi Hamidfar

Abstract:

Background and objectives: Effective postoperative pain management in abdominal surgeries, which are painful procedures, plays an important role in reducing postoperative complications and increasing patient’s satisfaction. There are many techniques for pain control, one of which is Patient-Controlled Analgesia (PCA). The aim of this study was to compare the analgesic effects of morphine, paracetamol and ketorolac in the patients undergoing open cholecystectomy, using PCA method. Material and Methods: This randomized controlled trial was performed on 330 ASA (American Society of Anesthesiology) I-II patients ( three equal groups, n=110) who were scheduled for elective open cholecystectomy in Shahid Rjaee hospital of Qazvin, Iran from August 2013 until September 2015. All patients were managed by general anesthesia with TIVA (Total Intra Venous Anesthesia) technique. The control group received morphine with maximum dose of 0.02mg/kg/h, the paracetamol group received paracetamol with maximum dose of 1mg/kg/h, and the ketorolac group received ketorolac with maximum daily dose of 60mg using IV-PCA method. The parameters of pain, nausea, hemodynamic variables (BP and HR), pruritus, arterial oxygen desaturation, patient’s satisfaction and pain score were measured every two hours for 8 hours following operation in all groups. Results: There were no significant differences in demographic data between the three groups. there was a statistically significant difference with regard to the mean pain score at all times between morphine and paracetamol, morphine and ketorolac, and paracetamol and ketorolac groups (P<0.001). Results indicated a reduction with time in the mean level of postoperative pain in all three groups. At all times the mean level of pain in ketorolac group was less than that in the other two groups (p<0.001). Conclusion: According to the results of this study ketorolac is more effective than morphine and paracetamol in postoperative pain control in the patients undergoing open cholecystectomy, using PCA method.

Keywords: analgesia, cholecystectomy, ketorolac, morphine, paracetamol

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56 Clinical Comparative Study Comparing Efficacy of Intrathecal Fentanyl and Magnesium as an Adjuvant to Hyperbaric Bupivacaine in Mild Pre-Eclamptic Patients Undergoing Caesarean Section

Authors: Sanchita B. Sarma, M. P. Nath

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Adequate analgesia following caesarean section decreases morbidity, hastens ambulation, improves patient outcome and facilitates care of the newborn. Intrathecal magnesium, an NMDA antagonist, has been shown to prolong analgesia without significant side effects in healthy parturients. The aim of this study was to evaluate the onset and duration of sensory and motor block, hemodynamic effect, postoperative analgesia, and adverse effects of magnesium or fentanyl given intrathecally with hyperbaric 0.5% bupivacaine in patients with mild preeclampsia undergoing caesarean section. Sixty women with mild preeclampsia undergoing elective caesarean section were included in a prospective, double blind, controlled trial. Patients were randomly assigned to receive spinal anesthesia with 2 mL 0.5% hyperbaric bupivacaine with 12.5 µg fentanyl (group F) or 0.1 ml of 50% magnesium sulphate (50 mg) (group M) with 0.15ml preservative free distilled water. Onset, duration and recovery of sensory and motor block, time to maximum sensory block, duration of spinal anaesthesia and postoperative analgesic requirements were studied. Statistical comparison was carried out using the Chi-square or Fisher’s exact tests and Independent Student’s t-test where appropriate. The onset of both sensory and motor block was slower in the magnesium group. The duration of spinal anaesthesia (246 vs. 284) and motor block (186.3 vs. 210) were significantly longer in the magnesium group. Total analgesic top up requirement was less in group M. Hemodynamic parameters were similar in both the groups. Intrathecal magnesium caused minimal side effects. Since Fentanyl and other opioid congeners are not available throughout the country easily, magnesium with its easy availability and less side effect profile can be a cost effective alternative to fentanyl in managing pregnancy induced hypertension (PIH) patients given along with Bupivacaine intrathecally in caesarean section.

Keywords: analgesia, magnesium, pre eclampsia, spinal anaesthesia

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55 Development of Ketorolac Tromethamine Encapsulated Stealth Liposomes: Pharmacokinetics and Bio Distribution

Authors: Yasmin Begum Mohammed

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Ketorolac tromethamine (KTM) is a non-steroidal anti-inflammatory drug with a potent analgesic and anti-inflammatory activity due to prostaglandin related inhibitory effect of drug. It is a non-selective cyclo-oxygenase inhibitor. The drug is currently used orally and intramuscularly in multiple divided doses, clinically for the management arthritis, cancer pain, post-surgical pain, and in the treatment of migraine pain. KTM has short biological half-life of 4 to 6 hours, which necessitates frequent dosing to retain the action. The frequent occurrence of gastrointestinal bleeding, perforation, peptic ulceration, and renal failure lead to the development of other drug delivery strategies for the appropriate delivery of KTM. The ideal solution would be to target the drug only to the cells or tissues affected by the disease. Drug targeting could be achieved effectively by liposomes that are biocompatible and biodegradable. The aim of the study was to develop a parenteral liposome formulation of KTM with improved efficacy while reducing side effects by targeting the inflammation due to arthritis. PEG-anchored (stealth) and non-PEG-anchored liposomes were prepared by thin film hydration technique followed by extrusion cycle and characterized for in vitro and in vivo. Stealth liposomes (SLs) exhibited increase in percent encapsulation efficiency (94%) and 52% percent of drug retention during release studies in 24 h with good stability for a period of 1 month at -20°C and 4°C. SLs showed about maximum 55% of edema inhibition with significant analgesic effect. SLs produced marked differences over those of non-SL formulations with an increase in area under plasma concentration time curve, t₁/₂, mean residence time, and reduced clearance. 0.3% of the drug was detected in arthritic induced paw with significantly reduced drug localization in liver, spleen, and kidney for SLs when compared to other conventional liposomes. Thus SLs help to increase the therapeutic efficacy of KTM by increasing the targeting potential at the inflammatory region.

Keywords: biodistribution, ketorolac tromethamine, stealth liposomes, thin film hydration technique

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54 Day-Case Ketamine Infusions in Patients with Chronic Pancreatitis

Authors: S. M. C. Kelly, M. Goulden

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Introduction: Chronic Pancreatitis is an increasing problem worldwide. Pain is the main symptom and the main reason for hospital readmission following diagnosis, despite the use of strong analgesics including opioids. Ketamine infusions reduce pain in complex regional pain syndrome and other neuropathic pain conditions. Our centre has trialed the use of ketamine infusions in patients with chronic pancreatitis. We have evaluated this service to assess whether ketamine reduces emergency department admissions and analgesia requirements. Methods: This study collected retrospective data from 2010 in all patients who received a ketamine infusion for chronic pain secondary to a diagnosis of chronic pancreatitis. The day-case ketamine infusions were initiated in theatre by an anaesthetist, with standard monitoring and the assistance of an anaesthetic practitioner. A bolus dose of 0.5milligrams/kilogram was given in theatre. The infusion of 0.5 milligrams/kilogram per hour was then administered over a 6 hour period in the theatre recovery area. A study proforma detailed the medical history, analgesic use and admissions to hospital. Patients received a telephone follow up consultation. Results: Over the last eight years, a total of 30 patients have received intravenous ketamine infusions, with a total of 92 ketamine infusions being administered. 53% of the patients were male with the average age of 47. A total of 27 patients participated with the telephone consultation. A third of patients reported a reduction in hospital admissions with pain following the ketamine infusion. Analgesia requirements were reduced by an average of 48.3% (range 0-100%) for an average duration of 69.6 days (range 0-180 days.) Discussion: This service evaluation illustrates that ketamine infusions can reduce analgesic requirements and the number of hospital admissions in patients with chronic pancreatitis. In the light of increasing pressures on Emergency departments and the increasing evidence of the dangers of long-term opioid use, this is clearly a useful finding. We are now performing a prospective study to assess the long-term effectiveness of ketamine infusions in reducing analgesia requirements and improving patient’s quality of life.

Keywords: acute-on-chronic pain, intravenous analgesia infusion, ketamine, pancreatitis

Procedia PDF Downloads 79