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Amarjit Singh - One of the best experts on this subject based on the ideXlab platform.
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review Nimesulide some pharmaceutical and pharmacological aspects an update
Journal of Pharmacy and Pharmacology, 2000Co-Authors: Anil K Singla, Manish Chawla, Amarjit SinghAbstract:Nimesulide, a non-steroidal anti-inflammatory drug (NSAID), is administered orally or rectally twice daily for a variety of inflammation and pain states. This is a unique NSAID, not only because of its chemical structure but also because of its specific affinity to inhibit cyclooxygenase-2 (COX-2), thus exerting milder effects on the gastrointestinal mucosa. Current data on selective COX-2 inhibitors suggest that they may have an efficacy similar to that of standard NSAIDs. Initial general clinical experience with selective COX-2 inhibitors appears to show that they are particularly promising in individuals at risk because of renal diseases, hypertension or congestive heart failure. Various experimental models and clinical studies have demonstrated the anti-inflammatory efficacy of Nimesulide. Nimesulide is superior, or at least comparable in efficacy, to other NSAIDs, but is better tolerated and has less potential for adverse reactions. Thus, selective COX-2 inhibitors should have anti-inflammatory effects devoid of side effects on the kidney and stomach. They may also demonstrate new important therapeutic benefits as anticancer agents as well as help prevention of premature labour and even retard the progression of Alzheimer's disease. No clinically significant drug interactions have been reported for Nimesulide. Not much has been reported about the pharmaceutical aspects of Nimesulide. Its poor aqueous solubility poses bioavailability problems in-vivo. This could be overcome by the formation of inclusion complexes with β-cyclodextrin, as has been reported by various researchers. However, absence of any in-vivo data regarding the relative absorption of Nimesulide from β-cyclodextrin complex compared with that from conventional formulations of the drug makes the use of such fast-releasing complexes rather questionable. Only a limited number of assay procedures (HPLC, spectrophotometric, spectrofluorimetric) for the determination of Nimesulide and its metabolite in plasma/urine samples or in dosage forms have been reported in the literature. The purpose of this review is to provide a concise overview of the pharmacological and pharmaceutical profile of Nimesulide. Various investigations carried out recently are reported, although older references to research performed on Nimesulide have also been included, where appropriate.
Halis Suleyman - One of the best experts on this subject based on the ideXlab platform.
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Nimesulide is a selective cox 2 inhibitory atypical non steroidal anti inflammatory drug
Current Medicinal Chemistry, 2008Co-Authors: Halis Suleyman, Elif Cadirci, Abdulmecit Albayrak, Zekai HaliciAbstract:In this review it is shown that Nimesulide, a selective cyclooxigenase-2 (COX-2) inhibitor, is different from other selective COX-2 inhibitors and classical non-steroidal anti-inflammatory drugs (NSAIDs). The anti-inflammatory effect mechanism of Nimesulide (inhibition of inflammatory mediators) is similar to other classic NSAIDs, but the protective effect of Nimesulide on classic NSAIDinduced ulcers elucidates the difference between Nimesulide and these other drugs. It is known that the selective COX-2 inhibitor Nimesulide prevents NSAID-induced ulcers, while celecoxib and rofecoxib, which are more selective to COX-2, failed to prevent these ulcers. Nimesulide produces gastro-protective effects via a completely different mechanism. In addition, while selective COX-2 inhibitors increase the risk for cardiovascular diseases, Nimesulide does not exert significant cardiotoxicity. This data suggests that gastrointestinal side effects of classic NSAIDs cannot be related to the COX-1 inhibition alone and also suggest that Nimesulide is an atypical NSAID, which is different from both non-selective and selective COX-2 inhibitors.
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Beneficial interaction of Nimesulide with NSAIDs
Medicinal Chemistry Research, 2007Co-Authors: Halis Suleyman, Elif Cadirci, Emine Salamci, Zekai HaliciAbstract:In this study, the effects of Nimesulide on the antiinflammatory and ulcerative action of some nonsteroidal antiinflammatory drugs (NSAIDs; (diclofenac sodium, ibuprofen, meloxicam) were investigated in rats, and it was determined whether Nimesulide interacts with these drugs in vivo and in vitro. Results showed that while diclofenac sodium, ibuprofen, and meloxicam reduced carrageenan-induced paw edema in rats by 66%, 39.6%, and 58%, respectively, when used alone, they reduced carrageenan-induced paw edema by 69.8%, 56.6%, and 66%, respectively, when combined with Nimesulide. Diclofenac (25 mg kg-1) and meloxicam (7.5 mg kg-1) produced 9.3 and 19.6 mm2 ulcer areas in stomachs of rats, respectively, when used alone, but when combined with Nimesulide diclofenac and meloxicam did not cause any injury in rat stomachs. While ranitidine at 100 mg kg-1 dose prevented diclofenac-induced ulcer formation, it reduced meloxicam-induced ulcer formation significantly. We conclude that Nimesulide does not interact with these drugs in terms of antiinflammatory action and antagonizes their side effects on gastric tissue without reacting chemically.
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the effect of Nimesulide on the indomethacin and ethanol induced gastric ulcer in rats
Pharmacological Research, 2002Co-Authors: Halis Suleyman, Fatih Akcay, Konca AltinkaynakAbstract:Abstract In the present study, we investigated the effects of Nimesulide, indomethacin, naproxene, ibuprofen and diclofenac, at anti-inflammatory doses, on the rat gastric tissue (total number = 102). In addition, the effect of Nimesulide at doses of 100, 300 and 500 mg kg−1on indomethacin-induced and ethanol-induced damage (ulcer) was examined. The potency of Nimesulide was compared with that of ranitidine (at 150 mg kg−1). Results indicated that Nimesulide did not produce any gastric damage. Additionally, it has a therapeutic effect on indomethacin- and ethanol-induced gastric lesions. Ulcer areas were measured in the rats given nonsteroidal anti-inflammatory drugs (NSAIDs). Nimesulide (at doses of 100, 300 and 500 mg kg−1) and ranitidine (at a dose of 150 mg kg−1) treated completely indomethacin-induced ulcer. The mean ulcer area was 21.9 ± 8.9 mm2in the indomethacin-given control group. Nimesulide and ranitidine reduced the ethanol-induced gastric ulcer. The ulcer area was 114.3 ± 10.3 mm2in the ethanol-given group and it was 4.5 ± 4.8, 20.1 ± 1.66, 15.16 ± 4.05 mm2for Nimesulide (at doses of 100, 300 and 500 mg kg−1), respectively, and 64.16 ± 3.97 mm2for ranitidine.
Zekai Halici - One of the best experts on this subject based on the ideXlab platform.
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Nimesulide is a selective cox 2 inhibitory atypical non steroidal anti inflammatory drug
Current Medicinal Chemistry, 2008Co-Authors: Halis Suleyman, Elif Cadirci, Abdulmecit Albayrak, Zekai HaliciAbstract:In this review it is shown that Nimesulide, a selective cyclooxigenase-2 (COX-2) inhibitor, is different from other selective COX-2 inhibitors and classical non-steroidal anti-inflammatory drugs (NSAIDs). The anti-inflammatory effect mechanism of Nimesulide (inhibition of inflammatory mediators) is similar to other classic NSAIDs, but the protective effect of Nimesulide on classic NSAIDinduced ulcers elucidates the difference between Nimesulide and these other drugs. It is known that the selective COX-2 inhibitor Nimesulide prevents NSAID-induced ulcers, while celecoxib and rofecoxib, which are more selective to COX-2, failed to prevent these ulcers. Nimesulide produces gastro-protective effects via a completely different mechanism. In addition, while selective COX-2 inhibitors increase the risk for cardiovascular diseases, Nimesulide does not exert significant cardiotoxicity. This data suggests that gastrointestinal side effects of classic NSAIDs cannot be related to the COX-1 inhibition alone and also suggest that Nimesulide is an atypical NSAID, which is different from both non-selective and selective COX-2 inhibitors.
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Beneficial interaction of Nimesulide with NSAIDs
Medicinal Chemistry Research, 2007Co-Authors: Halis Suleyman, Elif Cadirci, Emine Salamci, Zekai HaliciAbstract:In this study, the effects of Nimesulide on the antiinflammatory and ulcerative action of some nonsteroidal antiinflammatory drugs (NSAIDs; (diclofenac sodium, ibuprofen, meloxicam) were investigated in rats, and it was determined whether Nimesulide interacts with these drugs in vivo and in vitro. Results showed that while diclofenac sodium, ibuprofen, and meloxicam reduced carrageenan-induced paw edema in rats by 66%, 39.6%, and 58%, respectively, when used alone, they reduced carrageenan-induced paw edema by 69.8%, 56.6%, and 66%, respectively, when combined with Nimesulide. Diclofenac (25 mg kg-1) and meloxicam (7.5 mg kg-1) produced 9.3 and 19.6 mm2 ulcer areas in stomachs of rats, respectively, when used alone, but when combined with Nimesulide diclofenac and meloxicam did not cause any injury in rat stomachs. While ranitidine at 100 mg kg-1 dose prevented diclofenac-induced ulcer formation, it reduced meloxicam-induced ulcer formation significantly. We conclude that Nimesulide does not interact with these drugs in terms of antiinflammatory action and antagonizes their side effects on gastric tissue without reacting chemically.
T Kaya - One of the best experts on this subject based on the ideXlab platform.
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prevention of postoperative adhesion formation in rat uterine horn model by Nimesulide a selective cox 2 inhibitor
Human Reproduction, 2001Co-Authors: Tevfik Guvenal, Ali Cetin, H Ozdemir, O Yanar, T KayaAbstract:BACKGROUND: Pelvic surgery is one of the main causes of intraperitoneal (i.p.) adhesions that create various medical problems including pelvic pain, bowel obstructions and female infertility. A rat model was used to investigate the efficacy of Nimesulide, a selective cyclooxygenase-2 inhibitor, in the prevention of adhesion formation. METHODS: Fifty Wistar-Albino rats underwent bilateral uterine horn injury with a unipolar cautery. Study groups were as follows: (i) control group, no adjuvant therapy; (ii) i.p. Ringer's lactate group, 2 ml Ringer's lactate solution was instilled i.p.; (iii) i.p. Ringer's lactate plus Nimesulide group, 1 ml Ringer's lactate plus 1 ml Nimesulide (0.5 mg/ml) were given i.p.; (iv) intramuscular (i.m.) Nimesulide group, 1 ml i.m. Nimesulide (0.5 mg/ml) was given preoperatively for 5 days; and (v) i.p. Nimesulide group, 1 ml Nimesulide (0.5 mg/ml) was instilled i.p. At the end of the study all animals were killed, and a standard adhesion scoring system was applied by a blinded examiner. RESULTS: The mean adhesion extent in study groups was as follows: 1.33 +/- 0.76 in control group, 1.40 +/- 0.90 in i.p. Ringer's lactate group, 0.75 +/- 0.70 in i.p. Ringer's lactate plus Nimesulide group, 0.25 +/- 0.44 in i.m. Nimesulide group and 0.31 +/- 0.70 in i.p. Nimesulide group. The mean +/- SD adhesion severities of control, i.p. Ringer's lactate, i.p. Ringer's lactate plus Nimesulide, i.m. Nimesulide, and i.p. Nimesulide groups were 0.58 +/- 0.35, 0.30 +/- 0.41, 0.27 +/- 0.3, 0.12 +/- 0.28 and 0.15 +/- 0.35 respectively. The lowest adhesions were found in the groups treated with Nimesulide i.m. and Nimesulide i.p. ( P < 0.05). CONCLUSIONS: This study showed that preoperative i.m. or postoperative i.p. administration of Nimesulide to the site of injury reduced the formation of postoperative adhesions in a rat uterine horn model.
Anil K Singla - One of the best experts on this subject based on the ideXlab platform.
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review Nimesulide some pharmaceutical and pharmacological aspects an update
Journal of Pharmacy and Pharmacology, 2000Co-Authors: Anil K Singla, Manish Chawla, Amarjit SinghAbstract:Nimesulide, a non-steroidal anti-inflammatory drug (NSAID), is administered orally or rectally twice daily for a variety of inflammation and pain states. This is a unique NSAID, not only because of its chemical structure but also because of its specific affinity to inhibit cyclooxygenase-2 (COX-2), thus exerting milder effects on the gastrointestinal mucosa. Current data on selective COX-2 inhibitors suggest that they may have an efficacy similar to that of standard NSAIDs. Initial general clinical experience with selective COX-2 inhibitors appears to show that they are particularly promising in individuals at risk because of renal diseases, hypertension or congestive heart failure. Various experimental models and clinical studies have demonstrated the anti-inflammatory efficacy of Nimesulide. Nimesulide is superior, or at least comparable in efficacy, to other NSAIDs, but is better tolerated and has less potential for adverse reactions. Thus, selective COX-2 inhibitors should have anti-inflammatory effects devoid of side effects on the kidney and stomach. They may also demonstrate new important therapeutic benefits as anticancer agents as well as help prevention of premature labour and even retard the progression of Alzheimer's disease. No clinically significant drug interactions have been reported for Nimesulide. Not much has been reported about the pharmaceutical aspects of Nimesulide. Its poor aqueous solubility poses bioavailability problems in-vivo. This could be overcome by the formation of inclusion complexes with β-cyclodextrin, as has been reported by various researchers. However, absence of any in-vivo data regarding the relative absorption of Nimesulide from β-cyclodextrin complex compared with that from conventional formulations of the drug makes the use of such fast-releasing complexes rather questionable. Only a limited number of assay procedures (HPLC, spectrophotometric, spectrofluorimetric) for the determination of Nimesulide and its metabolite in plasma/urine samples or in dosage forms have been reported in the literature. The purpose of this review is to provide a concise overview of the pharmacological and pharmaceutical profile of Nimesulide. Various investigations carried out recently are reported, although older references to research performed on Nimesulide have also been included, where appropriate.
