Interaction between enoxacin, a new antimicrobial, and nimesulide, a new non-steroidal anti-inflammatory agent in mice

Taniguchi, Yasuaki; Deguchi, Yoshiki; Noda, Kanji

doi:10.1007/bf02252931

Cited by 6 publications

(4 citation statements)

References 8 publications

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“…The interaction potential of nimesulide might also differ from that of other NSAIDs (Perucca 1993). NIMESULIDEÐAN UPDATE Taniguchi et al (1996) demonstrated that the administration of nimesulide alone induced clonic convulsions at a dose greater than 300 mg kg À1 and that enoxicam induced no convulsions even at a dose above 5000 mg kg À1 , in mice. However, a combination of nimesulide (200 mg kg À1 ) and enoxicam (400 mg kg À1 ) induced no convulsions.…”

Section: Drug Interactionsmentioning

confidence: 99%

Review Nimesulide: Some Pharmaceutical and Pharmacological Aspects—An Update

Singla

Chawla

Singh

2000

Journal of Pharmacy and Pharmacology

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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 beta-cyclodextrin, as has been reported by various researchers. However, absence of any in-vivo data regarding the relative absorption of nimesulide from beta-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.

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Section: Drug Interactionsmentioning

confidence: 99%

Review Nimesulide: Some Pharmaceutical and Pharmacological Aspects—An Update

Singla

Chawla

Singh

2000

Journal of Pharmacy and Pharmacology

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“…The proconvulsive effect of nimesulide in combination with kainate was unexpected in the doses we used (10 mg/ kg), since only extremely high doses (300 mg/kg) have been reported to induce convulsions in mice (Taniguchi et al 1996). Whether nimesulide in therapeutic doses can augment epileptic seizures in humans is unknown, but our observation suggests that nimesulide should be used with caution in patients with convulsive disorders until further experience.…”

Section: Discussionmentioning

confidence: 79%

Nimesulide Aggravates Kainic Acid‐Induced Seizures in the Rat

Kunz¹,

Oliw

2001

Pharmacology & Toxicology

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Treatment of rats with kainic acid (10 mg/kg, intraperitoneally) triggers limbic seizures. Cyclooxygenase‐2 mRNA is expressed in the hippocampus and cortex after 8 hr and marked cell loss occurs after 72 hr in the CA1‐CA3 areas of the hippocampus. We examined the effect of the cyclooxygenase‐2 inhibitor, nimesulide (N‐(4‐nitro‐2‐phenoxyphenyl)‐methanesulfonamide), on kainate‐induced seizures and delayed neurotoxicity. Nimesulide (10 mg/kg, intraperitoneally) was well tolerated given alone or 6–8 hr after kainate. However, pretreatment with nimesulide augmented seizures and increased the mortality rate from ∼10% to 69%. We examined the effect of nimesulide on delayed cell loss after 72 hr in the surviving animals with histological staining. Cell loss did not seem to be reduced in animals treated with nimesulide 6–8 hr after kainate, but in the surviving animals pretreated with nimesulide less cell loss occurred. We conclude that nimesulide should be used with caution as an antiinflammatory drug in patients with convulsive disorders.

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“…Nimesulide was injected in a constant volume of 0.01 ml/g by the subcutaneous route. The dose of nimesulide was selected based on effective doses published for mice (Gupta et al, 1998;Taniguchi et al, 1996). Delivery times were recorded, and as in Experiment 1, parturition was defined as delivery of the first pup.…”

Section: Methodsmentioning

confidence: 99%