Author: Miyahara, R. ; Ohmiya, N. ; Ando, T. ; Itoh, A. ; Ishihara, M. ; Funasaka, K. ; Ohno, E. ; Nakamura, M. ; Kawashima, H. ; Watanabe, O. ; Goto, H. ; Hirooka, Y.

SummaryBackgroundThe aetiology for nonsteroidal anti‐inflammatory drug (NSAID)‐induced small intestinal injuries has not been well characterised.AimTo determine the risk factors of symptomatic NSAID‐induced small intestinal injuries, including diaphragm disease.MethodsOf the 1262 symptomatic patients who underwent videocapsule endoscopy and/or double‐balloon enteroscopy, 156 consecutive patients were verified as having taken NSAIDs. Their CYP2C9*2, *3 and *13 single nucleotide polymorphisms (SNPs) were determined by allelic discrimination with Taqman 5’‐nuclease assays.ResultsOf the 156 NSAIDs users, 31 patients (20%) were diagnosed with NSAID‐induced small intestinal injury. Multivariate analysis indicated that the presence of comorbidities and the use of oxicams (meloxicam, ampiroxicam and lornoxicam) or diclofenac were associated with an increased risk of NSAID‐induced small intestinal injury (adjusted OR: 2.97, 95% CI: 1.05–8.41, P = 0.041 and adjusted OR: 7.05, 95% CI: 2.04–24.40, P = 0.002, respectively). The combination of aspirin and non‐aspirin NSAID was more damaging than aspirin alone. Age, sex, concomitant use of proton pump inhibitors, indications for NSAIDs use, duration of NSAIDs use and CYP2C9*2, *3 and *13SNPs were unrelated. The use of meloxicam and CYP2C9*3SNPs were significantly associated with an increased risk for diaphragm disease (adjusted OR: 183.75, 95% CI: 21.34–1582.38; P < 0.0001 and adjusted OR: 12.94, 95% CI: 1.55–108.36, P = 0.018, respectively).ConclusionThe use of specific NSAIDs and the factors interfering with NSAIDs metabolism might associate with small intestinal injury, especially with diaphragm disease.

01 Apr 2013·Forensic Science InternationalQ3 · MEDICINE

Simultaneous determination for oxicam non-steroidal anti-inflammatory drugs in human serum by liquid chromatography–tandem mass spectrometry

Q3 · MEDICINE

ArticleOA

Author: Kotoe Komine ; Wataru Irie ; Yoko Kunisue ; Marina Kawasaki ; Tatsuo Shinozuka ; Masaru Terada ; Koji Tomobe ; Keiko Tonooka ; Chizuko Sasaki ; Chikako Murakami ; Junichi Shirako

A high-performance liquid chromatography-tandem mass spectrometry (LC/MS/MS) technique was developed for the simultaneous determination of five non-steroidal anti-inflammatory oxicam drugs (ampiroxicam, tenoxicam, piroxicam, meloxicam and lornoxicam) in human plasma. These five oxicam drugs and isoxicam (internal standard) were extracted from human plasma with an Oasis(®) MAX cartridge column and analysed on a Unison UK-C18 column (2.0 mm × 100 mm, 3 μm) with an acetonitrile:10mM formic ammonium buffer (pH 3.0) (50:50) mobile phase at 0.20 ml/min at 37°C. The analytes were detected using a tandem mass spectrometer, equipped with an electrospray ion source (ESI). The instrument was used in multiple-reaction-monitoring (MRM) mode. The extraction yields from a 200 μl human plasma sample (containing 10 ng of each drugs) with the Oasis(®) MAX cartridge column were 93.3-102.5%. The detection limits were 0.01-6.5 ng/ml (S/N=3). Our developed method is very useful for the simultaneous determination of five oxicam (non-steroidal anti-inflammatory) drugs in human plasma by LC/MS/MS.

01 Feb 2012·European Journal of PharmacologyQ3 · MEDICINE

Oxicam structure in non-steroidal anti-inflammatory drugs is essential to exhibit Akt-mediated neuroprotection against 1-methyl-4-phenyl pyridinium-induced cytotoxicity

Q3 · MEDICINE

Article

Author: Tomohiro Omura ; Tomoko Ohkubo ; Yoshikazu Tasaki ; Toshihiro Noda ; Tomoki Sakaguchi ; Joe Yamamoto ; Kazuo Matsubara ; Machiko Satomi ; Naoya Kamiyama ; Masaru Asari ; Keiko Shimizu ; Koichi Yoshida

In the treatment of Parkinson's disease, potent disease-modifying drugs are still needed to halt progressive dopaminergic neurodegeneration. We have previously shown that meloxicam, an oxicam non-steroidal anti-inflammatory drug (NSAID), elicits a potent neuroprotective effect against 1-methyl-4-phenyl pyridinium (MPP(+))-induced toxicity in human dopaminergic SH-SY5Y neuroblastoma cells. This cyclooxygenase-independent neuroprotection of meloxicam is mediated via the phosphatidylinositol 3-kinase (PI3K)/Akt pathway; however, the specific chemical structure involved in inducing neuroprotection remains unresolved. In this study, we therefore investigated the structure-specific for eliciting the neuroprotective effect by examining a series of NSAIDs against MPP(+) toxicity in SH-SY5Y cells. Three oxicam-bearing NSAIDs showed potent neuroprotective effects, although none of the other 10 oxicam-nonbearing NSAIDs (3 salicylates, 6 coxibs and 1 polyphenol) or 3 piroxicam analogs (including ampiroxicam, a precursor of piroxicam) exerted any neuroprotection. Tenoxicam and piroxicam prevented MPP(+)-induced reduction of phosphorylated Akt levels in cells: a protective mechanism similar to that of meloxicam. Therefore, the oxicam structure was likely to be responsible for exhibiting the neuroprotection by sustaining survival-signaling in dopaminergic cells. The present results raise the possibility that the oxicam-bearing NSAIDs may serve as potential therapeutic drugs to retard or terminate progression of Parkinson's disease via a novel mechanism.

100 Deals associated with Ampiroxicam

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KEGG	Wiki	ATC	Drug Bank
D01397	Ampiroxicam	M01AC	-

R&D Status

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Indication	Country/Location	Organization	Date
Pain, Postoperative	JP	Pfizer Japan, Inc.	03 Apr 2008
Rheumatic Diseases	JP	FUJIFILM Toyama Chemical Co., Ltd.	30 Sep 1994
Bursitis	JP	Pfizer Japan, Inc.	01 Oct 1993
Cervicobrachial syndrome	JP	Pfizer Japan, Inc.	01 Oct 1993
Low Back Pain	JP	Pfizer Japan, Inc.	01 Oct 1993
Osteoarthritis	JP	Pfizer Japan, Inc.	01 Oct 1993
Rheumatoid Arthritis	JP	Pfizer Japan, Inc.	01 Oct 1993

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