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Article
SYNTHESIS OF ESTRONE-OPIOID PEPTIDE ANALOGUE WITH EXPECTED ANALGESIC ACTIVITY

Authors: Ayad A. AL-Hamashi --- Kawkab Y. Saour
Journal: Al-Nahrain Journal of Science مجلة النهرين للعلوم ISSN: (print)26635453,(online)26635461 Year: 2010 Volume: 13 Issue: 2 Pages: 20-31
Publisher: Al-Nahrain University جامعة النهرين

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Abstract

The search for new peptides to be used as analgesics in place of morphine has been mainlydirected to develop peptide analogues to have higher biological stability and receptor selectivity.Therefore extensive researches have been carried out on naturally occurring and syntheticopiates in order to enhance the analgesic potency, so we intended to prepare opioiod peptideanalogue linked to estrone which may increase the analgesic effect of this compound. Sterichindrance clearly will be produced by estrone may affect the enzymatic activity on the synthesizedanalogue and this in turn may enhance the bioavailability of the analogue itself, meanwhile estronemay affect physicochemical properties of the analogue by increasing its lipophilicity and sofacilitate its passage through the biological barriers, also estrone may affect receptor bindingselectivity of this analogue and decrease the side effect of the original opioid peptide.The designed analogue is (estrone-3-O-acyl-tyr-gly-gly-phe-met-OH), where this opioidpeptide synthesized following the conventional solution method, then linked to estrone by amidelinkage and it was characterized using: thin layer chromatography (TLC), melting point, infraredspectroscopy (IR), elemental microanalysis(CHN), optical rotation, amino acid analysis, andhydrogen-nuclear magnetic resonance(1H-NMR).

البحث عن ببتيدات جديدة لاستخدامها كمسكنات للآلامبدلا من المورفين موجها أساسا لتطوير ببتيدات مماثلةلتمتلك أعلى استقرار أحيائي وأكثر ارتباط انتقائيللمستقبلات. لذلك أجريت بحوث على نطاق واسع تخصالأفيونات المصنعة والطبيعية لزيادة الفعالية المسكنة للألام،لذا فإننا بهدف تحضير ببتيد أفيوني مماثل يرتبط معالأسترون من أجل زيادة فعالية تسكين الآلام. أن الإعاقةالفراغية التي تنتج عن ارتباط الاسترون يمكن أن تؤثر فيفعالية الإنزيمات التي تؤثر على المركب المصنع وهذابدوره قد يعزز توافره الأحيائي، ومن ناحية أخرى فأنالاسترون قد يؤثر على الخصائص الفيزيوكيمائية للمركبعن طريق زيادة خصائصه ألدهنية وبذلك سيسهل المرورعبر الحواجز الحياتية، كما يمكن للاسترون أن يؤثر علىانتقائية الارتباط مع المستقبلات، وتقليل الآثار الجانبيةللببتيد الأفيوني.أن المماثل المخلق في هذه الدراسة هو:(estrone-3-O-acyl-tyr-gly-gly-phe-met-OH)وتم تخليقه بأتباع طريقة المحلول التقليدية، وتم ربطالاسترون مع الببتيد الأفيوني من خلال آصرة الأمايد، وتمتمييزه باستخدام: كروماتوكرافيا الطبقة الرقيقة، مقياسدرجة الانصهار، مطياف الأشعة دون الحمراء، التحليلالدقيق للعناصر المكونة، تحليل الحامض الأميني، وقياس

Keywords

estrone --- opioid peptide --- analgesia


Article
Analgesic Effect of Melatonin in Mice

Author: Imad Hashim Mohammad, M.Sc., Ph.D.
Journal: Al-Kindy College Medical Journal مجلة كلية الطب الكندي ISSN: 18109543 Year: 2012 Volume: 8 Issue: 2 Pages: 28-31
Publisher: Baghdad University جامعة بغداد

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Abstract

Background: Melatonin is the main hormone secreted by the pineal gland. This indole compound (N-acetyl-5-methoxytryptamine) is derived from serotonin after two biochemical steps. Melatonin has been implicated in some pharmacological effects including sedative/hypnotic, anticonvulsant activity and others. The aim of this study was to investigate the antinociceptive effect of different doses of melatonin administered i.p. to mice, and then, to find the dose- response line of melatonin in mice as analgesic agent.Methods: The dose response effect of melatonin (10, 50, and 100mg/kg) were assessed against control using tail flick test in mice as a model of nociceptive pain. In this model, all doses of melatonin were given intraperitoneally 15 min before immersion of tail in hot water 50°C, and Tail Flick Latency was measured before, and after (15, 30, 60 and 120 min ) administration of melatonin.Results: Administration of melatonin i.p. to mice significantly P ≤ 0.05 increase tail flick latency in melatonin treated groups after 30 min and 60 min compared to baseline values; while after 120 min, administration of melatonin produce significant and dose dependent antinociceptive effect following its i.p. administration. The percentage increase in tail flick latency produced by i.p. administration of melatonin doses of 10, 50, and 100 mg/kg were 86.59%, 156.05% and 169.19% respectively when compared to baseline values.Conclusions: The present study showed that melatonin produces analgesic effect in a dose dependent manner in mice, further studies are required to know the exact mechanism by which melatonin exerts this analgesic effect.Keywords: melatonin, analgesia, pain

Keywords

melatonin --- analgesia --- pain


Article
Exploration of antinociceptive, antipyretic and anti-inflammatory activities of Curcumin in male rat
الكشف عن الفعالية المسكنة للالم والخافضة للحرارة والمضادة للالتهاب للكركمين (Curcumin) في ذكور الجرذان

Author: Fraid J. Al-Tahan فريد جميل عمر الطحان
Journal: Iraqi Journal of Science المجلة العراقية للعلوم ISSN: 00672904/23121637 Year: 2012 Volume: 53 Issue: 4 Pages: 786-793
Publisher: Baghdad University جامعة بغداد

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Abstract

Curcumin, one of active ingredients of Curcuma spp. Roxb (Zingiberaceae) is referred to main medicinal part in this spice. In the present study, the analgesic, antipyretic and anti-inflammatory actions of Curcumin were investigated in male rats. Ninety Albino male rats (110-125g) were used in this study (six animals were used in each test for Curcumin, aspirin and Pethedine). The effects of curcumin on nociceptive response using writhing, tail flicking and formalin tests in rats were evaluated. The antipyretic activity in yeast-induced fever and anti-inflammatory activity in carrageenin-induced edema in rats were examined. Administration of curcumin significantly P<0.05 decreased the number of writhing and stretching induced by acetic acid, and suppressed the licking activity of the late phase in formalin test in rats. Curcumin had significant decrease P<0.05 effects on yeast-induced fever and carrageenin-induced edema in rats. Furthermore, the ED50 from Log dose response curve exhibited sequence order potency in formalin test, writhing reflex and tail flick as aspirin < curcumin. Curcumin showed synergistic effect centrally acting pethidine and peripheral analgesic aspirin. From these results it can be concluded that curcumin possesses analgesic effect via a different mechanism from that of aspirin and pethidine.

الكركمين، احد المكونات الفعالة لنبات الكركم والذي تعزى اليه اغلب الفعاليات الطبية لتلك النبتة. استهدف البحث دراسة الفعالية المسكنة للالم وخفض الحرارة والمضادة للالتهاب للكركمين في ذكور الجرذان. قيمت فعالية الكركمين المسكنة من خلال التحري عن قدرته على خفض عدد حركات التلوي (writhing) وخفق الذنب (flicking) وعتبة التحمل ضد التاثير المهيج للفورملين، كما تم التحري عن قدرته على خفض حرارة الجسم المحدثة باستخدام احدى الخمائر والفعل المضاد للالتهاب المحدث بالكاراغينان (carrageenan). ادت المعامله بالكركمين الى انخفاض معنوي في عدد مرات التلوي المحدث بفعل حمض الخليك وعدد مرات لعق القدم في المرحلة الاجله (late phase) من تاثير الفورمالين في الجرذان. كما ادت المعامله الكركمين الى انحفاض معنوي P<0.05 لحجم الوذمة في اقدام الجرذان المعاملة بالكاراغينان. اظهرت الجرعة المؤثرة الوسطى المستخرجة من منحني تاثير لوغاريتمات الجرعات للفحوصات الانفة الذكر ان الكركمين يقع تاليا للاسبرين من حيث شدة الفعالية، كما اظهر الكركمين فعلا تأزريا لكل من المسكن المركزي (البثدين) والمحيطي (الاسبرين). يمكن الاستنتاج من هذه الدراسه ان الكركمين يحدث مفعوله المسكن عبر الية مختلفة عن تلك التي يعمل بموجبها كل من البثدين والاسبرين.


Article
EXPLORE THE SYNERGISM OF SEDATIVE DOSE MEDETOMIDINE WITH TRAMADOL TO INDUCE ANALGESIC EFFECTS IN RABBITS
تاثيرات الجرعه تحت المسكنه ( المسدره) للميديتوميدين والترامدول معا لاحداث التسكين في الارانب

Author: Mahmood. B. Mahmood
Journal: Basrah Journal of Veterinary Research. مجلة البصرة للابحاث البيطرية ISSN: Print:18138497 E; 24108456 Year: 2016 Volume: 15 Issue: 2 Pages: 97-110
Publisher: Basrah University جامعة البصرة

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Abstract

The study was designed to evaluate the analgesic effects of Medetomidine and Tramadol in rabbits, to detect the best dose (as onset and duration) for antinociceptive in this model, also evaluate the antinociceptive effect as sedative doses in these drugs as a mixture by using electrical stimulator. Administration of Medetomidine alone at 200 µgkg B.W. (I.M) and Tramadol alone at 2 mg kg B.W. (I.P) were the best doses for relief pain induced by electrical stimuli. There was increased in the voltage change for pain ( 15, 30, 45, 60, 75, 90 minutes) in comparison with control and other doses for each drug. Administration of Medetomidine at 50 µg kg B.W. (I.M) with Tramadol at 0.5 mg kg B.W. I.P) significantly referred to synergism of the antinociceptive effect which induced analgesia in 100 % of the rabbits in comparison with other groups for each drug alone (at the same analgesic doses) without any overt side effects and without differences in glucose, glutathione, ALT and AST level in animals. The data of this study demonstrated the mixture of Medetomidine and Tramadol at low doses (subanalgesic doses) had a typical synergistic effect (super-additive) for inducing good and safe analgesia as well as its skeletal muscle relaxation in rabbits.


Article
Epidural Labor Analgesia during the First Stage of Labor: A Double-Blind Clinical Trial

Author: Ali Hadi Muslih
Journal: Mustansiriya Medical Journal مجلة المستنصرية الطبية ISSN: 20701128 22274081 Year: 2012 Volume: 11 Issue: 1 Pages: 20-23
Publisher: Al-Mustansyriah University الجامعة المستنصرية

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Abstract

Background: although severe pain is not life-threatening in healthy parturient women, it can have neuropsychological consequences. Postnatal depression may be more common when analgesia is not used, and pain during labor has been correlated with the development of post-traumatic stress disorder. In addition, one study suggested that the impairment of cognitive function in the postpartum period can be mitigated by the use of any form of intrapartum analgesia.Aims: to compare a combination of epidural fentanyl and bupivacaine with bupivacaine alone for epidural analgesia in labor and to evaluate factors in addition to analgesia that may influence maternal satisfaction.Patients and methods: a double blind controlled clinical trial carried on 218 multiparous parturient. The patients were randomly allocated in 2 groups. Group 1 (n=109) had received bupivacaine 0.1% with fentanyl 50µg and group 2 (n=109) (control group) had received bupivacaine 0.1% only.Results: in the bupivacaine group, 40 cases (37.7%) had required 2 top-ups and 26 cases (23.9%) had asked for 3 top-ups. On the other hand 14 (12.8%) cases from bupivacaine fentanyl group had asked for 2 top-ups and no cases had recorded request for 3 doses, which was statistically significant (P<0.0001).Conclusions: maternal satisfactory rate is high in both groups; the bupivacaine fentanyl group had shown a good response to the effect of analgesia with the minimal medical intervention.


Article
A comparison of high versus low intensity transcutaneous electrical nerve stimulation for chronic pain
مقارنة بين التحفيز العصبي الكهربائي عبر الجلد المرتفع مقابل المنخفض الكثافة للألم المزمن

Author: Diyar Hussein Tahir
Journal: Zanco Journal of Medical Sciences مجلة زانكو للعلوم الطبية ISSN: 19955588/19955596 Year: 2011 Volume: 15 Issue: 2 Pages: 51-56
Publisher: Hawler Medical Univeristy جامعة هولير الطبية

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Abstract

Background and objectives: Over the last 35 years electrical nerve stimulation has been employed increasingly in the treatment of chronic pain. This study was carried out to compare the analgesic effect that produced by applying a fixed frequency (50 Hz) high intensity tolerably painful transcutaneous electrical nerve stimulation (TENS) with the conventional low intensity TENS.Methods:Thirty six patients (26 Females and 10 males with age 18 – 54 years) were selected from patients consulting a private psychiatric clinic in Erbil city from March 2009 to march 2010. They had chronic pain in head and neck for more than 2 years. The cases were allocated randomly into two groups; group A treated by the conventional TENS of high frequency 100 Hz with low intensity current, by applying the electrical electrodes on the nucheal region (back of neck) for 20 minutes once daily for six days, and once weekly for one month then follow up the patients after 3 months, while in group B; the same procedure was applied but with fixed frequency 50 Hz and high intensity current adjusted to a tolerably painful level. The pain measured by verbal scale ranged from 0 to 4. Results: Patients who received high intensity TENS; 94% of them got immediate pain relief and 17% got long lasting pain relief more than three months, while with the conventional TENS only 33% got immediate pain relief and no one got long lasting pain relief.Conclusion: The tolerably painful high intensity TENS gives better analgesic effect than the conventional TENS, and in some patients it may leads to long lasting analgesic effect(this may be attributed to the pan stimulation involving a variety of afferent fibers; Aa/β, Ad & C).


Article
Evaluation of Analgesic Activity of Newly SynthesizedPhthalyl- tyrosyl-glycin Sodium

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Abstract

Alteration in the backbone structure of the endogenously released opioid peptides Leu5/Met5 enkephalins may result in compounds having comparable profile of pharmacological activity but with different physicochemical properties and side effects. Phthalyl amino acid and phthalyl esters are among the derivatives that have been synthesized and evaluated for their antibacterial and antifungal activities.This study was conducted to evaluate the possible analgesic activity of phthalyl-tyrosyl-glycin sodium that has been recently synthesized by our team.The study was carried out on 24 albino mice using hot plate method. The animals were allocated in to three groups; the first group received saline and represent a control group; the second group received morphine HCl as a standard drug; and the third group received phthalyl-tyrosyl-glycin sodium. The onset with which the animal lift his forearm and the number of jumps per 25 seconds were recorded for each group. The results of this study showed that phthalyl-tyrosyl-glycin sodium resulted in significant improvement (P<0.05) in analgesia score as well as significant delay in the onset of induced hyperalgesia in comparison to saline-treated group, and in comparison to morphine HCl, no significant difference (P>0.05) was observed in analgesia score but with significant delay in induced hyperalgesia.The results obtained in this study provide experimental evidences for the effectiveness of the prepared compound as analgesic with comparable effect to that of morphine.

ان بعض التعديلات الكيميائية على الببتيدات الحياتية المورفينية الداخلية (ليوسين ومثيونين انكفالين) قد تنتج مركبات لها فعاليات دوائية مقاربة كمسكنات الم قوية ولكن بخواص كيمياوية وفيزياوية مختلفة مع اختلاف في بعض الأعراض الجانبية الناتجة عن استخدامها. تعتبر المركبات الحاوية على الفثاليل كحامض أميني واسترات الفثاليل من المركبات المصنعة والمقيمة فعاليتها ضد الالتهابات الجرثومية والفطرية وعليه تم تصميم هذه الدراسة لتقييم الفعالية الدوائية لببتيد يحتوي على مجموعة الفثاليل كمركب مسكن للألم. ان هذا المركب وهو (Phthalyl-tyrosyl glycin sodium) هو مركب جديد قد تم تصنيعه من قبل فرع الكيمياء الصيدلانية في كلية الصيدلة جامعة بغداد.لقد تمت الدراسة باستخدام 24 فأراً ذكراً أبيضا لتقييم الفعالية الدوائية للمركب الجديد كمسكن للألم باستخدام طريقة الصفيحة الحارة (hot plate) وتم توزيع الحيوانات على ثلاثة مجاميع، حقنت المجموعة الأولى بالماء المالح (saline) وتمثل مجموعة السيطرة والمجموعة الثانية بالمورفين كعقارقياسي والثالثة بمركب (Phthalyl-tyrosyl glycin sodium) والذي هو موضوع البحث وتم احتساب الوقت المستغرق ليسحب الحيوان قدمه عن الصفيحة الحارة وعدد القفزات خلال 25 ثانية.أظهرت النتائج أن هناك تحسن واضح ومعنوي في الوقت المستغرق ليسحب الحيوان قدميه عن الصفيحة وكذلك في عدد القفزات خلال 25 ثانية في الحيوانات المعالجة بالمركب الجديد عن مجموعة السيطرة. لا فرق معنوي قد لوحظ في معدل قفز الحيوانات المعالجة بالمركب الجيد بالمقارنة مع المجموعة المعالجة بالمورفين إلا أن سرعة سحب الحيوان لقدميه عن الصفيحة الحارة كان أبطأ.تعطي النتائج المستخلصة من هذه الدراسة أدلة تجريبية على الفعالية الدوائية لمركب (Phthalyl-tyrosyl- glycin) كمركب مسكن للألم قوي وبفعالية مقاربة للمورفين.


Article
A comparison Between the Transversus Abdominis Plane (TAP) Block Versus Traditional Parentral Analgesia Post Caesarian Section

Authors: Iyad Abbas Salman --- Hayder Saad Kamel
Journal: Iraqi Academic Scientific Journal المجلة العراقية للاختصاصات الطبية ISSN: 16088360 Year: 2012 Volume: 11 Issue: supplement Pages: 718-723
Publisher: The Iraqi Borad for Medical Specialization المجلس العراقي للاختصاصات الطبية

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Abstract

ABSTRACT:BACKGROUND:Postoperative pain, especially when poorly controlled, results in harmful acute effects (i.e., adverse physiologic responses) and chronic effects (i.e., delayed long-term recovery and chronic pain).The transversus abdominis plane (TAP) block is a new method of providing postoperative analgesia in patients undergoing lower abdominal wall incisionsOBJECTIVE:To compare the effectiveness of TAP block versus traditional parenteral analgesia post caesarian section.PATIENTS AND METHODS:A prospective randomized double blinded placebo controlled clinical trial conducted in the department of obstetrics & gynecology of medical city complex. over a period of four months from 1st of November to 1st of march. Fifty women patients were selected to be enrolled in this study who were scheduled for C.S. via pfannenstiel incision, all patients were of ASA I- II physical status. Twenty five of them were given TAP block with (bupivacaine 0.25%) & placebo i.v saline (0.9%) , the other twenty five were given i.v tramadol & i.m diclofinac sodium & placebo TAP block with normal saline 0.9%.Numerical rating scale was used to follow up the patients postoperatively at 2,6,12,16 hours.RESULTS :By comparing the means of numerical analogue scale score over the time there was a significant difference in mean score over the time, the traditional treatment had better effect on relieving pain only at the 1st 2 hours where TAP block was better on the rest time with a highly significant difference P.value < 0.05 in all comparisons.CONCLUSION:TAP block is not effective as sole analgesic, but is effective in reducing the frequency of doses of incremental analgesia. TAP block is more effective than traditional analgesia in reducing the mean of pain score .The traditional parentral analgesia require more frequent dosing.


Article
Awareness and Attitude of Pregnant Women towards Labor Analgesia in Babil Province

Authors: Mohammed Sami Hasan --- Zainab Abdulkhaliq Alsaadi --- Mazin Adnan Abbas --- Jaber Mohsin Algoraby
Journal: Medical Journal of Babylon مجلة بابل الطبية ISSN: 1812156X 23126760 Year: 2016 Volume: 13 Issue: 1 Pages: 95-104
Publisher: Babylon University جامعة بابل

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Abstract

The aim of this study is to assess the awareness and attitude of pregnant women in Babil province toward painless labour and their willingness to get the service. A questionnaire form designed and given to pregnant women in Babil province attending the antenatal clinics in seven primary health care centers, 820 pregnant women responses to the questionnaire form taken for this study.10.98% primiparas and 89.02% are multiparas. Mean age of respondents was 26.6±6.4.most of the multipararespondents report their pain in the previous labor as very severe and sever.Most of the respondents have no any information about painless labour and 5.1% have little information, their source of information was 36.2% from friends and relatives,20.3%, from TV. 62.3% have very high and high fear from next labour pain.Most of women will ask for the service of painless labour if it is available. 59.9% think labor can’t be without pain.most of the respondents don’t knew who will be responsible for relief of their labor pain.Conclusion: This study showed poor general knowledge of pregnant women in Babil province about painless labor . It is recommended that information about painless labor should be given by the antenatal physician, obstetrician or a nurses in a collaborative with anesthesiologists to inform pregnant women about benefits, modalities and limitations of painless labor, Education of the labor room staff about the service and Public education by TV programs. The persistently low request of painless labor by pregnant women could thus be ascribed to a combination of poor pregnant women awareness and inadequate provision of resources so to start with is implementing standard infrastructure for labor room that can help provision of the service and it necessary taken into consideration by the ministry of health .

Keywords

Awareness --- Attitude --- pregnant women --- Labor --- analgesia


Article
Pre-Emptive Analgesic Effect of Tramadol and Ibuprofen After Impacted Mandibular Third Molar Extraction

Author: Bara S. Minwah
Journal: Al-Rafidain Dental Journal مجلة الرافدين لطب الأسنان ISSN: 18121217 Year: 2017 Volume: 17 Issue: 1 Pages: 76-85
Publisher: Mosul University جامعة الموصل

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Abstract

Aims: to evaluate the efficacy of analgesia produced by preoperative administration of tramadol or ibuprofen on surgically extracted mandibular 3rd molars .Materials and Methods :surgical removal of lower 3rd molar was performed in 30 patients , they were divided into three groups of ten patient for each. Group I: preoperative 100mg tramadol IM injection; Group II: preoperative 800 mg Ibuprofen orally; Group III: control group with no preoperative treatment .Analgesia was assessed by visual analogue scale (VAS), Verbal pain Scale(VPS), patient satisfaction(PS), amount of analgesic consumption and time elapsed before first intake were recorded after 24 hours. Results: There was significant differences between tramadol and control group in all types of pain scales in favor of tramadol group . There was significant difference in the visual analog scale (VAS) ,number and time of tablets needed during 24 hours between Ibuprofen and control group . There was significant difference between Tramadol and Ibuprofen groups in both of (VAS) and (VPS) in favor of Tramadol group. Conclusions: The use of tramadol or ibuprofen preemptively is effective method of postoperative pain control in impacted lower 3rd molar surgery .

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