MedWorm: Celebrex

Incidence of gastroduodenal ulcers during treatment with celecoxib or diclofenac: pooled results from three 12-week trials in Chinese patients with osteoarthritis or rheumatoid arthritis

APLAR Journal of Rheumatology — Mon, 15 Mar 2010 00:00:00 +0100

Conclusions: In Asian patients with minimal significant risk factors, treatment with celecoxib was associated with a modest but significantly reduced incidence of gastric ulcers at the end of 12 weeks. (Source: APLAR Journal of Rheumatology)

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Synthesis of New 2,3-Dihydroquinazolin-4(1H)-one Derivatives for Analgesic and Anti-inflammatory Evaluation

Archiv der Pharmazie — Mon, 15 Mar 2010 00:00:00 +0100

Starting from isatoic anhydrides, several new 2,3-dihydroquinazolin-4(1H)-one derivatives bearing chalcone or pyrazole or thiazole moieties at the third position were synthesized. The analgesic and anti-inflammatory activities for most compounds were studied at a dose level of 50 mg/kg via the acetic-acid-induced writhing-response method and carrageenan-induced edema method, respectively. The study showed that the chalcones bearing a 4-chlorophenyl group 4c or 4-nitrophenyl group 4b were the most active ones as analgesics. Both chalcone 4c and N-phenyl pyrazole bearing 4-methoxy phenyl group 5b showed a higher anti-inflammatory activity than celecoxib but still lower than that of diclofenac sodium. Moreover, the chalcone 4c has nearly the same ulcerogenic index as the selective cyclooxygen...

Preventing chemoresistance of human breast cancer cell line, MCF-7 with celecoxib

Journal of Cancer Research and Clinical Oncology — Sun, 14 Mar 2010 11:26:24 +0100

Conclusion Celecoxib effectively prevents the development of chemoresistance in breast cancer cell line MCF-7 induced by doxorubicin, which was partly involved in inhibiting the expression and DNA-binding activity of nuclear transcription factors AP-1 and NF-κB and downstream expression and function of P-gp. Furthermore, cytostatic efficacy of celecoxib and doxorubicin on MCF-7 cell was synergistic. Content Type Journal ArticleCategory Original PaperDOI 10.1007/s00432-010-0854-3Authors Chen Chen, Jiangsu University The Affiliated People’s Hospital Zhenjiang People’s Republic of ChinaHui Ling Shen, Jiangsu University The Affiliated People’s Hospital Zhenjiang People’s Republic of ChinaJing Yang, Jiangsu University The Affiliated People’s Hospital Zhenjian...

Cost Effectiveness of Etoricoxib versus Celecoxib and Non-Selective NSAIDS in the Treatment of Ankylosing Spondylitis

PharmacoEconomics — Sat, 13 Mar 2010 15:50:45 +0100

(Source: PharmacoEconomics)

Wettability and Surface Chemistry of Crystalline and Amorphous Forms of a Poorly Water Soluble Drug.

European Journal of Pharmaceutical Sciences — Fri, 12 Mar 2010 00:00:00 +0100

In conclusion, the crystalline and amorphous forms of CLB exhibited disparate surface milieu, which in turn can have implications on the surface mediated events. PMID: 20230893 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)

Multimodal therapy for synergic inhibition of tumour cell invasion and tumour-induced angiogenesis

BMC Cancer — Thu, 11 Mar 2010 00:00:00 +0100

Conclusions: A combined approach targeting different families of proteases and cyclooxygenases represents a promising adjuvant therapy. (Source: BMC Cancer)

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Rosuvastatin Prevents Conduit Artery Endothelial Dysfunction Induced by Ischemia and Reperfusion by a Cyclooxygenase-2–Dependent Mechanism

Journal of the American College of Cardiology — Thu, 04 Mar 2010 13:56:40 +0100

Conclusions: Rosuvastatin pharmacologically prevents the development of IR-induced conduit artery endothelial dysfunction. This beneficial effect of rosuvastatin is mediated by a COX-2–dependent mechanism, evidence that may also provide potential mechanistic insight into the reported cardiotoxic effects of COX-2 inhibitors. (Source: Journal of the American College of Cardiology)

Risk of upper gastrointestinal bleeding among NSAIDs: systematic review of observational studies

NeLM - News — Thu, 04 Mar 2010 00:00:00 +0100

Source: Arthr Rheum Area: News The risk of risk of upper gastrointestinal bleeding (UGIB) among NSAID users (traditional NSAIDs and coxibs) has been evaluated in a systematic review of observational studies published between 2000 and 2008. The review included 18 original studies initially, 9 of which were excluded for a number of reasons, leaving 9 for the meta-analysis. The following findings were reported: . The relative risk (RR) of UGIB for traditional NSAIDs was 4.50 (3.82 to 5.31) and for coxibs 1.88 (0.96 to 3.71). . Lower RRs than that reported overall were observed for ibuprofen 2.6 (2.17 to 3.33), rofecoxib 2.12 (1.5 to 2.84), aceclofenac 1.44 (0.65 to 3.2) and celecoxib 1.42 (0.85 to 2.37). . Higher RRs than that report...

Low direct cytotoxicity of loxoprofen on gastric mucosal cells.

Biological and Pharmaceutical Bulletin — Wed, 03 Mar 2010 07:28:05 +0100

Authors: Yamakawa N, Suemasu S, Kimoto A, Arai Y, Ishihara T, Yokomizo K, Okamoto Y, Otsuka M, Tanaka K, Mizushima T Pro-drugs of non-steroidal anti-inflammatory drugs (NSAIDs), such as loxoprofen are widely used for clinical purposes because they are not so harmful to the gastrointestinal mucosa. We recently showed that NSAIDs such as indomethacin and celecoxib have direct cytotoxicity (ability to induce necrosis and apoptosis in gastric mucosal cells) due to their membrane permeabilizing activities, which is involved in NSAID-induced gastric lesions. We show here that under conditions where indomethacin and celecoxib clearly induce necrosis and apoptosis, loxoprofen and its active metabolite loxoprofen-OH, do not have such effects in primary culture of guinea pig gastric mucosal cell...

Uterine-specific p53 deficiency confers premature uterine senescence and promotes preterm birth in mice

Journal of Clinical Investigation — Tue, 02 Mar 2010 17:25:43 +0100

Many signaling pathways that contribute to tumorigenesis are also functional in pregnancy, although they are dysregulated in the former and tightly regulated in the latter. Transformation-related protein 53 (Trp53), which encodes p53, is a tumor suppressor gene whose mutation is strongly associated with cancer. However, its role in normal physiological processes, including female reproduction, is poorly understood. Mice that have a constitutive deletion of Trp53 exhibit widespread development of carcinogenesis at early reproductive ages, compromised spermatogenesis, and fetal exencephaly, rendering them less amenable to studying the role of p53 in reproduction. To overcome this obstacle, we generated mice that harbor a conditional deletion of uterine Trp53 and examined pregnancy outcome in...

COX-2 Inhibitors Blunt "Preconditioning" Effect of Statin

Medscape Medical News Headlines — Mon, 01 Mar 2010 23:09:07 +0100

The COX-2 inhibitor celecoxib completely abolished the beneficial preconditioning effect of rosuvastatin in a small mechanistic study in human volunteers. Heartwire (Source: Medscape Medical News Headlines)

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COX-2 inhibitors blunt "preconditioning" effect of statin

theHeart.org — Mon, 01 Mar 2010 22:00:00 +0100

The COX-2 inhibitor celecoxib completely abolished the beneficial preconditioning effect of rosuvastatin in a small mechanistic study in human volunteers. For complete story visit theheart.org. (Source: theHeart.org)

Sheldon Gilgore, Physician Who Led Drug Giants Pfizer and Searle, Dies at 77

NYT > Health — Mon, 01 Mar 2010 05:50:09 +0100

Mr. Gilgore, an opera lover, had roles in the advancement of drugs like Ambien and Celebrex. (Source: NYT > Health)

Celecoxib enhances the inhibitory effect of cisplatin on Tca8113 cells in human tongue squamous cell carcinoma in vivo and in vitro

Journal of Oral Pathology and Medicine — Mon, 01 Mar 2010 00:00:00 +0100

Conclusions: Those findings indicate that a low dose of celecoxib could augment CDDP-induced growth inhibition of Tca8113 cells and its xenograft in Balb/c nude mice. (Source: Journal of Oral Pathology and Medicine)

Inhibition of Secretion of Interleukin (IL)-12/IL-23 Family Cytokines by 4-Trifluoromethyl-celecoxib Is Coupled to Degradation via the Endoplasmic Reticulum Stress Protein HERP [Protein Structure and Folding]

Journal of Biological Chemistry — Fri, 26 Feb 2010 14:42:01 +0100

Interleukin-12 (IL-12), p80, and IL-23 are structurally related cytokines sharing a p40 subunit. We have recently demonstrated that celecoxib and its COX-2-independent analogue 4-trifluoromethyl-celecoxib (TFM-C) inhibit secretion but not transcription of IL-12 (p35/p40) and p80 (p40/p40). This is associated with a mechanism involving altered cytokine-chaperone interaction in the endoplasmic reticulum (ER). In the present study, we found that celecoxib and TFM-C also block secretion of IL-23 (p40/p19 heterodimers). Given the putative ER-centric mode of these compounds, we performed a comprehensive RT-PCR analysis of 23 ER-resident chaperones/foldases and associated co-factors. This revealed that TFM-C induced 1.5–3-fold transcriptional up-regulation of calreticulin, GRP78, GRP94, GRP...

Focus on therapy: hemicrania continua and new daily persistent headache

The Journal of Headache and Pain — Fri, 26 Feb 2010 06:45:38 +0100

Abstract Hemicrania continua (HC) and new daily-persistent headache (NDPH) represent the only two forms of chronic daily headache in Chap. IV “Other Primary Headaches” of the second edition of the International Classification of Headache Disorders. HC and NDPH are rare and poorly defined from a pathophysiological point of view; as a consequence, their management is largely empirical. Indeed, there is a lack of prospective, controlled trials in this field, and treatment effectiveness is basically inferred from the results of sparse open-label trials, retrospective case series, clinical experience and expert opinions. In this narrative review we have summarised the information collected from an extensive analysis of the literature on the treatment of HC and NDPH in order...

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Doctor Pleads Guilty To Falsifying Data For Celebrex Pain Study

LexisNexis® Mealey's™ Arthritis Drugs Legal News — Thu, 25 Feb 2010 14:41:04 +0100

BOSTON - A former member of Pfizer Inc.'s speakers' bureau pleaded guilty Feb. 22 to health care fraud for falsifying data in support of a published study on pain management, according to documents filed in the U.S. District Court for the District of Massachusetts (United States of America v. Scott Reuben, No. 10-30002, D. Mass.; See January 2010, Page 4). Full story on lexis.com (Source: LexisNexis® Mealey's™ Arthritis Drugs Legal News)

IL-1β Suppresses the Formation of Osteoclasts by Increasing OPG Production via an Autocrine Mechanism Involving Celecoxib-Related Prostaglandins in Chondrocytes

Mediators of Inflammation — Wed, 24 Feb 2010 16:46:06 +0100

Elevated interleukin (IL)-1 concentrations in synovial fluid have been implicated in joint bone and cartilage destruction. Previously, we showed that IL-1β stimulated the expression of prostaglandin (PG) receptor EP4 via increased PGE2 production. However, the effect of IL-1β on osteoclast formation via chondrocytes is unclear. Therefore, we examined the effect of IL-1β and/or celecoxib on the expression of macrophage colony-stimulating factor (M-CSF), receptor activator of NF-κB ligand (RANKL), and osteoprotegerin (OPG) in human chondrocytes, and the indirect effect of IL-1β on osteoclast-like cell formation using RAW264.7 cells. OPG and RANKL expression increased with IL-1β; whereas M-CSF expression decreased. Celecoxib blocked the stimulatory ef...

CELEBREX (Celecoxib) Capsule [Stat Rx USA]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Wed, 24 Feb 2010 05:00:00 +0100

Updated Date: Feb 24, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Cyclooxygenase-2 Inhibition Does Not Improve the Reduction in Ductal Carcinoma In situ Proliferation with Aromatase Inhibitor Therapy: Results of the ERISAC Randomized Placebo-Controlled Trial.

Clinical Breast Cancer — Tue, 23 Feb 2010 00:00:00 +0100

CONCLUSIONS: Exemestane reduces proliferation in ER-positive DCIS. Aromatase inhibition is a potential alternative to tamoxifen in patients who have undergone breast conservation for ER-positive DCIS. Clin Cancer Res; 16(5); 1605-12. PMID: 20179229 [PubMed - as supplied by publisher] (Source: Clinical Breast Cancer)

Mass. doctor accused of faking painkiller studies pleads guilty to federal health care fraud

OrlandoSentinel: Medical Research — Mon, 22 Feb 2010 16:58:00 +0100

BOSTON (AP) — A doctor accused of faking research for a dozen years in published studies that suggested after-surgery benefits from painkillers including Vioxx and Celebrex pleaded guilty Monday to one count of federal health care fraud. An... (Source: OrlandoSentinel: Medical Research)

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Big Pharma researcher admits to faking dozens of research studies for Pfizer, Merck (opinion)

NaturalNews.com — Thu, 18 Feb 2010 07:00:00 +0100

(NaturalNews) It's being called the largest research fraud in medical history. Dr. Scott Reuben, a former member of Pfizer's speakers' bureau, has agreed to plead guilty to faking dozens of research studies that were published in medical journals.Now being reported across the mainstream media is the fact that Dr. Reuben accepted a $75,000 grant from Pfizer to study Celebrex in 2005. His research, which was published in a medical journal, has since been quoted by hundreds of other doctors and researchers as "proof" that Celebrex helped reduce pain during post-surgical recovery. There's only one problem with all this: No patients were ever enrolled in the study!Dr. Scott Reuben, it turns out, faked the entire study and got it published anyway.It wasn't the first study faked by Dr. Reuben: He...

Progress in COX-2 Inhibitors: A Journey So Far.

Current Medicinal Chemistry — Thu, 18 Feb 2010 00:00:00 +0100

Authors: Chakraborti AK, Garg SK, Kumar R, Motiwala HF, Jadhavar PS The non-steroidal anti-inflammatory drugs (NSAIDs) are diverse group of compounds used for the treatment of inflammation, since the introduction of acetylsalicylic acid in 1899. Traditional (first generation) NSAIDs exert antiinflammatory, analgesic, and antipyretic effects through the blockade of prostaglandin synthesis via non-selective inhibition of cyclooxygenase (COX-1 and COX-2) isozymes. Their use is associated with side effects such as gastrointestinal and renal toxicity. A number of selective (second generation) COX-2 inhibitors (rofecoxib, celecoxib, valdecoxib etc.) were developed as safer NSAIDs with improved gastric safety profile. Observation of increased cardiovascular risks in APPROVe (Adenomatous Polyp...

New Insights into the Structural Features and Functional Relevance of Human Cytochrome P450 2C9. Part I.

Current Drug Metabolism — Thu, 18 Feb 2010 00:00:00 +0100

Authors: Mo SL, Zhou ZW, Yang LP, Wei MQ, Zhou SF CYP2C9 is one of the most abundant CYP enzymes in the human liver ( approximately 20% of hepatic total CYP content). CYP2C9 metabolizes approximately 20% clinical drugs (>120 drugs), including a number of drugs with narrow therapeutic ranges. Some natural compounds are also metabolized, probably leading to the formation of toxic metabolites. CYP2C9 also plays a role in the metabolism of several endogenous compounds such as steroids, melatonin, retinoids and arachidonic acid. Typical substrates of CYP2C9 such as celecoxib, ibuprofen, flurbiprofen, and diclofenac are relatively small, lipophilic and contain acidic groupings with pK(a) values in the range 3.8-8.1 which will be ionized at physiological pH. The carboxylate groups of tieni...

Dextran Carrier Macromolecule for Colon Specific Delivery of Celecoxib.

Current Drug Delivery — Wed, 17 Feb 2010 00:00:00 +0100

Authors: Shrivastava PK, Shrivastava SK The colon specific polymeric conjugates of celecoxib were prepared with dextran of different molecular weight Mr approximately 40 000, 70 000, and 100 000 (CSD-40, CSD-70 and CSD-100). Succinic acid was used as linker between the drug and dextran. The prepared conjugates were characterized by UV, IR, 1H NMR and HPLC. The maximum degree of substitution 3.9+/-0.20 % was found with the dextran CSD-100 conjugates. The percent release of drug obtained by in-vitro hydrolysis studies, was found to be 24.37+/- 0.6, 23.0 +/- 0.5 and 20.13+/- 0.8 in simulated colonic fluid (SCF) pH 6.8 while 17.90 +/- 0.4, 16.8+/- 0.75 and 15.47 +/- 0.5 in simulated intestinal fluid (SIF) pH 7.4 for CSD-40, CSD-70 and CSD-100, respectively, in both medium. The drug release...

Certain Pain Medications Do Not Appear To Be Associated With Skin Cancer Risk

Health News from Medical News Today — Tue, 16 Feb 2010 08:00:00 +0100

Contrary to previous hypotheses, the use of non-steroidal anti-inflammatory drugs does not appear associated with risk of squamous cell skin cancer, according to a report posted online today that will appear in the April print issue of Archives of Dermatology, one of the JAMA/Archives journals. Non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and celecoxib reduce pain and inflammation by blocking an enzyme involved in producing inflammatory compounds, according to background information in the article... (Source: Health News from Medical News Today)

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Rofecoxib, but not celecoxib, increases the risk of thromboembolic cardiovascular events in young adults—a nationwide registry-based study

European Journal of Clinical Pharmacology — Mon, 15 Feb 2010 17:57:52 +0100

Conclusion This Icelandic nationwide registry-based study amounting to 163,406 patient-years showed increased risk of cardiovascular events, i.e. cerebral infarction, myocardial infarction and unstable angina pectoris, among rofecoxib and naproxen users in comparison to diclofenac users. The added risk was most pronounced in young adults using rofecoxib. Content Type Journal ArticleCategory Pharmacoepidemiology and PrescriptionDOI 10.1007/s00228-010-0789-2Authors Bjorn Gudbjornsson, Landspitali University Hospital Centre for Rheumatology Research Reykjavik IcelandSigurdur B. Thorsteinsson, Landspitali University Hospital Division of Pharmaceutical Services Reykjavik IcelandHelgi Sigvaldason, Directorate of Health Reykjavik IcelandRannveig Einarsdottir, Landspitali Uni...

Synthesis and biological evaluation of N-difluoromethyl-1,2-dihydropyrid-2-one acetic acid regioisomers: Dual Inhibitors of cyclooxygenases and 5-lipoxygenase.

Bioorganic & Medicinal Chemistry Letters — Sat, 13 Feb 2010 00:00:00 +0100

Authors: Yu G, Praveen Rao PN, Chowdhury MA, Abdellatif KR, Dong Y, Das D, Velázquez CA, Suresh MR, Knaus EE A new group of acetic acid (7a-c, R(1)=H), and propionic acid (7d-f, R(1)=Me), regioisomers wherein a N-difluoromethyl-1,2-dihydropyrid-2-one moiety is attached via its C-3, C-4, and C-5 position was synthesized. This group of compounds exhibited a more potent inhibition, and hence selectivity, for the cyclooxygenase-2 (COX-2) relative to the COX-1 isozyme. Attachment of the N-difluoromethyl-1,2-dihydropyrid-2-one ring system to an acetic acid, or propionic acid, moiety confers potent 5-LOX inhibitory activity, that is, absent in traditional arylacetic acid NSAIDs. 2-(1-Difluoromethyl-2-oxo-1,2-dihydropyridin-5-yl)acetic acid (7c) exhibited the best combination of dual COX-...

Clinical relevance of C-reactive protein in ankylosing spondylitis and evaluation of the NSAIDs/coxibs' treatment effect on C-reactive protein

Rheumatology — Thu, 11 Feb 2010 12:45:03 +0100

Conclusions. Increased CRP was frequently observed in patients with painful axial AS and was correlated both with activity and functional severity of the disease. The treatment effect of NSAIDs/coxibs was relevant in the subgroup of patients with increased CRP at baseline. (Source: Rheumatology)

Celecoxib inhibits Helicobacter pylori colonization-related factors.

World Journal of Gastroenterology : WJG — Wed, 10 Feb 2010 17:56:41 +0100

CONCLUSION: Celecoxib inhibits flagellar motility and adherence of H. pylori to AGS cells, and destructs their normal structure in vitro. PMID: 20143463 [PubMed - in process] (Source: World Journal of Gastroenterology : WJG)

Celecoxib/etoricoxib: Exanthema: 2 case reports

Reactions — Wed, 10 Feb 2010 14:08:42 +0100

(Source: Reactions)

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CELEBREX (Celecoxib) Capsule [4UORTHO LLC]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Wed, 03 Feb 2010 05:00:00 +0100

Updated Date: Feb 3, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Cyclooxygenase-derived mediators regulate the immunological control of Strongyloides venezuelensis infection

FEMS Immunology and Medical Microbiology — Wed, 03 Feb 2010 00:00:00 +0100

The aim of this study was to define the immunoregulatory role of prostaglandins in a mouse model of Strongyloides venezuelensis infection. Strongyloides venezuelensis induced an increase of eosinophils and mononuclear cells in the blood, peritoneal cavity fluid, and bronchoalveolar lavage fluid. Treatment with the dual cyclooxygenase (COX-1/-2) inhibitors indomethacin and ibuprofen, and the COX-2-selective inhibitor celecoxib partially blocked these cellular responses and was associated with enhanced numbers of infective larvae in the lung and adult worms in the duodenum. However, the drugs did not interfere with worm fertility. Cyclooxygenase inhibitors also inhibited the production of the T-helper type 2 (Th2) mediators IL-5, IgG1, and IgE, while indomethacin alone also inhibited IL-4, I...

Markedly reduced toxicity of a hydrogen sulphide-releasing derivative of naproxen (ATB-346)

British Journal of Pharmacology — Tue, 02 Feb 2010 00:00:00 +0100

Conclusions and implications: ATB-346 exhibits anti-inflammatory properties similar to naproxen, but with substantially reduced gastrointestinal toxicity. (Source: British Journal of Pharmacology)

Protective Effect of Rebamipide against Celecoxib-induced Gastric Mucosal Cell Apoptosis.

Biochemical Pharmacology — Mon, 01 Feb 2010 00:00:00 +0100

In this study, we have examined the effect of rebamipide on celecoxib-induced production of gastric lesions. In mice pre-administered with a low dose of indomethacin, orally administered rebamipide suppressed celecoxib-induced mucosal apoptosis and lesion production but did not decrease in PGE(2) levels in the stomach. Rebamipide also suppressed celecoxib-induced increases in intracellular Ca(2+) concentration, the ER stress response, mitochondrial dysfunction and apoptosis in vitro. We also found that rebamipide suppresses the increases in intracellular Ca(2+) concentration induced by an activator of voltage-dependent L-type Ca(2+) channels and that another blocker of this channel suppresses celecoxib-induced increases in intracellular Ca(2+) concentration. These results suggest that cele...

Cytotoxic effects of celecoxib on Raji lymphoma cells correlate with aggravated endoplasmic reticulum stress but not with inhibition of cyclooxygenase-2

Leukemia Research — Sat, 30 Jan 2010 14:33:16 +0100

Abstract: Inhibition of cyclooxygenase 2 (COX-2) by the selective COX-2 inhibitor celecoxib has been suggested as potentially useful for B-cell lymphoma therapy. However, additional pharmacological activities of celecoxib have been discovered and have challenged the notion that its antitumor effects are mediated primarily via the inhibition of COX-2. To shed light on this issue, we have investigated the effects of different pharmacological agents with greatly varying COX-2 inhibitory potency in Raji lymphoma cells in vitro. We found that cytotoxic potency of these compounds did not at all correlate with their COX-2 inhibitory activity; in fact, the most potent COX-2 inhibitors lacked the ability to kill Raji cells. Instead, the cytotoxic outcome was closely aligned with these agents’ abi...

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A phase 2 pilot trial of low-dose, continuous infusion, or "metronomic" paclitaxel and oral celecoxib in patients with metastatic melanoma

Cancer — Fri, 29 Jan 2010 00:00:00 +0100

Tumor angiogenesis has been associated with a poor prognosis in patients with metastatic melanoma (MM). Microtubule stabilizers and cyclooxygenase 2 (COX-2) inhibitors, alone and in combination, have produced inhibitory effects on endothelial cells and tumor angiogenesis. Angiogenesis, which is the growth of new blood vessels, is necessary for tumor growth and progression. Thus, the authors tested the safety and efficacy of a low dose of paclitaxel and celecoxib in patients with MM.Patients received paclitaxel 10 mg/m2 for 96 hours weekly as a continuous intravenous infusion and oral celecoxib 400 mg twice daily. Systemic tumor response was assessed at 6-week intervals. Tumor measurements at the end of Cycle 1 were used as the baseline for assessment of tumor progression. Patients with una...

Parties Accuse Each Other Of Redefining Science For Purpose Of Litigation

LexisNexis® Mealey's™ Arthritis Drugs Legal News — Thu, 28 Jan 2010 14:48:07 +0100

NEW YORK - Pfizer Inc. says shareholder derivative plaintiffs seek to redefine the science over its painkillers Bextra and Celebrex, while the plaintiffs say it is the company that attempts to change the scientific facts underlying the litigation, in responses to each other's proposed findings of fact filed Jan. 8 in the U.S. District Court for the Southern District of New York (In re Pfizer Inc. Securities Litigation, No. 04-9866, S.D. N.Y.; See December 2009, Page 6). Full story on lexis.com (Source: LexisNexis® Mealey's™ Arthritis Drugs Legal News)

Severe adverse skin reactions to nonsteroidal antiinflammatory drugs: A review of the literature.

American Journal of Health-System Pharmacy : AJHP — Thu, 28 Jan 2010 13:32:22 +0100

CONCLUSION: The risk of SJS or TEN in patients receiving NSAIDs is extremely low; older patients, women, and patients within the first month of treatment initiation appear to have the greatest risk. Health care providers and patients should be aware of the signs and symptoms of SJS and TEN. PMID: 20101062 [PubMed - in process] (Source: American Journal of Health-System Pharmacy : AJHP)

Nonsteroidal antiinflammatory drugs and prostaglandin E2 modulate the synthesis of osteoprotegerin and RANKL in the cartilage of patients with severe knee osteoarthritis

Arthritis and Rheumatism — Thu, 28 Jan 2010 00:00:00 +0100

Although the osteoprotegerin (OPG)/RANK/RANKL system is the main modulator of bone remodeling, it remains unclear whether it is regulated in cartilage during osteoarthritis (OA). The aim of this study was to examine whether nonsteroidal antiinflammatory drug (NSAID) treatment modulates the synthesis of OPG and RANKL in the cartilage of patients with OA, and to investigate whether prostaglandin E2 (PGE2) modifies this system in human OA chondrocytes in culture.A 3-month clinical trial was carried out in 20 patients with severe knee OA, all of whom were scheduled to undergo knee replacement surgery. Ten of these patients were treated with celecoxib, and the other 10 patients, who did not want to be treated, served as the control group. After surgery, cartilage was processed for molecular bio...

TLR4-dependent induction of vascular adhesion molecule-1 in rheumatoid arthritis synovial fibroblasts: Roles of cytosolic phospholipase A2[alpha]/cyclooxygenase-2

Journal of Cellular Physiology — Thu, 28 Jan 2010 00:00:00 +0100

In this study, we identified that cPLA2[alpha] acted as a modulator of LPS-induced VCAM-1 expression and THP-1 (human acute monocytic leukemia cell line) adherence. Treatment of RA synovial fibroblasts (RASFs) with LPS, a TLR4 agonist, promoted the VCAM-1 expression and THP-1 adherence which were decreased by pretreatment with a selective cytosolic phospholipase A2 (cPLA2) inhibitor (AACOCF3), implying the involvement of cPLA2[alpha] in these responses. This notion was further confirmed by knockdown of cPLA2[alpha] expression by transfection with cPLA2[alpha] small interfering RNA (siRNA) leading to a decrease in VCAM-1 expression and THP-1 adherence induced by LPS. Subsequently, the LPS-stimulated cPLA2[alpha] phosphorylation was attenuated by pretreatment with a MEK1/2 inhibitor (U0126),...

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Responder analysis for pain relief and numbers needed to treat in a meta-analysis of etoricoxib osteoarthritis trials: bridging a gap between clinical trials and clinical practice

Annals of the Rheumatic Diseases — Tue, 26 Jan 2010 10:24:11 +0100

Conclusion: Responder rates and NNTs are reproducible for different levels of response over 12 weeks and have relevance for clinical practice at the individual patient level. An average 10 mm improvement in pain equates to almost one in two patients having substantial benefit. (Source: Annals of the Rheumatic Diseases)

Overexpression of Cyclooxygenase-2 in Celecoxib-Resistant Breast Cancer Cell Lines

Journal of Surgical Research — Mon, 25 Jan 2010 16:42:25 +0100

Introduction: Cyclooxygenase-2 (COX-2) is a mediator of inflammation that has been shown to play a key role in breast cancer progression and metastasis. COX-2 is highly overexpressed in inflammatory breast cancer (IBC), an aggressive subset of breast cancers. A clearer understanding of the mechanisms of celecoxib resistance should identify new models for COX-2 inhibition as a therapeutic approach for IBC and other aggressive forms of breast cancer that overexpress COX-2. Herein we tested the hypothesis that celecoxib-resistance involves selection of cancer cells that overexpress COX-2. Methods: We selected celecoxib-resistant (CER) cell lines by culturing the following breast cancer cell lines in the presence of 10 micromolar celecoxib in their respective culture media: 1) SUM149 IBC cell ...

Celecoxib Inhibits CD133-Positive Cell Migration via Reduction of CCR2 in Helicobacter pylori -Infected Mongolian Gerbils

Karger Publishers — Mon, 18 Jan 2010 23:00:00 +0100

Digestion 2010;81:193203 (DOI:10.1159/000252790) (Source: Karger Publishers)

Celecoxib Inhibits CD133-Positive Cell Migration via Reduction of CCR2 in Helicobacter pylori-Infected Mongolian Gerbils

Digestion — Mon, 18 Jan 2010 23:00:00 +0100

Digestion 2010;81:193203 (DOI:10.1159/000252790) (Source: Digestion)

Effect of a cyclooxygenase-2 inhibitor on postexercise muscle protein synthesis in humans

AJP: Endocrinology and Metabolism — Fri, 15 Jan 2010 01:51:49 +0100

Nonselective blockade of the cyclooxygenase (COX) enzymes in skeletal muscle eliminates the normal increase in muscle protein synthesis following resistance exercise. The current study tested the hypothesis that this COX-mediated increase in postexercise muscle protein synthesis is regulated specifically by the COX-2 isoform. Sixteen males (23 ± 1 yr) were randomly assigned to one of two groups that received three doses of either a selective COX-2 inhibitor (celecoxib; 200 mg/dose, 600 mg total) or a placebo in double-blind fashion during the 24 h following a single bout of knee extensor resistance exercise. At rest and 24 h postexercise, skeletal muscle protein fractional synthesis rate (FSR) was measured using a primed constant infusion of [2H5]phenylalanine coupled with muscle bi...

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NSAIDs May Help Slow Basal Cell Carcinoma Development

Modern Medicine — Fri, 15 Jan 2010 00:00:00 +0100

The nonsteroidal anti-inflammatory drug celecoxib (Celebrex) effectively inhibits the development of skin basal cell carcinoma in highly susceptible patients compared to placebo, according to a study in the January issue of Cancer Prevention Research. (Source: Modern Medicine)

Celecoxib activates PI-3K/Akt and mitochondrial redox signaling to enhance heme oxygenase-1-mediated anti-inflammatory activity in vascular endothelium.

Free Radical Biology and Medicine — Fri, 15 Jan 2010 00:00:00 +0100

Authors: Hamdulay SS, Wang B, Birdsey GM, Ali F, Dumont O, Evans PC, Haskard DO, Wheeler-Jones CP, Mason JC Although non-steroidal anti-inflammatory drugs provide important control of pain and inflammation, they have been over-shadowed by concerns regarding atherothrombotic complications. However, celecoxib appears to have a relatively good cardiovascular profile and may improve endothelial function in coronary heart disease. This led us to the hypothesis that celecoxib induces the vasculoprotective enzyme heme oxygenase-1 (HO-1). In human umbilical vein and aortic endothelial cells, 24-48 hours treatment with celecoxib induced HO-1 mRNA and protein expression and increased HO-1 enzyme activity. This effect was not seen with rofecoxib or indomethacin. Supplementation of culture media w...

In response to Fox and Sonis

Radiotherapy and Oncology — Thu, 14 Jan 2010 00:00:00 +0100

In this study, neither inhibition of TNF-α (by the antibody infliximab) nor of COX-2 (by the tyrosine kinase inhibitor celecoxib) resulted in modulation of the epithelial response of oral mucosa during fractionated irradiation. The conclusion from these observations was that those inflammatory changes mediated through TNF-α or COX-2 are not relevant for the radiation effects of oral epithelium. In their letter, Fox and Sonis stress that one explanation for the missing effect of infliximab (not of celecoxib) might be a lack of cross-reactivity with murine TNF-α. This possibility was discussed in the original paper , where we explained that infliximab (administered in protocols comparable to those used in our study) was effective in a number of mouse models of various diseases, such as di...

Safety, Tolerability and Biological Effects of Long-Term Metronomic Administration of Non-Cytotoxic Anti-Angiogenic Agents.

Oncology — Mon, 11 Jan 2010 00:00:00 +0100

Conclusions: In pretreated patients with advanced slow-growing solid tumours, long-term metronomic administration of two-drug combinations of alpha-interferon, thalidomide or celecoxib was well tolerated and had antitumour activity. Low baseline CEPs in patients with subsequent clinical benefit suggest that CEC count may identify patients likely to benefit from long-term metronomic anti-angiogenic treatment. PMID: 20068365 [PubMed - as supplied by publisher] (Source: Oncology)

Celecoxib analogs possessing a N-(4-nitrooxybutyl)piperidin-4-yl or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridin-4-yl nitric oxide donor moiety: Synthesis, biological evaluation and nitric oxide release studies.

Bioorganic & Medicinal Chemistry Letters — Mon, 11 Jan 2010 00:00:00 +0100

Authors: Chowdhury MA, Abdellatif KR, Dong Y, Yu G, Huang Z, Rahman M, Das D, Velázquez CA, Suresh MR, Knaus EE A new group of hybrid nitric oxide (NO) releasing anti-inflammatory (AI) coxib prodrugs (NO-coxibs) wherein the para-tolyl moiety present in celecoxib was replaced by a N-(4-nitrooxybutyl)piperidyl 15a-b, or N-(4-nitrooxybutyl)-1,2,3,6-tetrahydropyridyl 17a-b, NO-donor moiety was synthesized. All compounds released a low amount of NO upon incubation with phosphate buffered saline (PBS) at pH 7.4 (2.4-5.8% range). In comparison, the percentage NO released was higher (3.1-8.4% range) when these nitrate prodrugs were incubated in the presence of l-cysteine. In vitro COX-1/COX-2 isozyme inhibition studies showed this group of compounds are moderately more potent, and hence s...

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Celebrex Might Thwart Inherited Skin Cancers

MedlinePlus Health News — Fri, 08 Jan 2010 22:00:00 +0100

Drug led to fewer basal cell carcinoma lesions in study patients Source: HealthDay Related MedlinePlus Topics: Pain Relievers, Skin Cancer (Source: MedlinePlus Health News)

Insights From the Adenoma Prevention With Celecoxib Trial and Risk for Cardiovascular Adverse Events

Current Colorectal Cancer Reports — Fri, 08 Jan 2010 21:42:13 +0100

Content Type Journal ArticleCategory Clinical Trial ReportDOI 10.1007/s11888-009-0043-4Authors Sarah Kraus, Tel Aviv Medical Center Integrated Cancer Prevention Center 6 Weizmann Street Tel Aviv 64239 IsraelNadir Arber, Tel Aviv Medical Center Integrated Cancer Prevention Center 6 Weizmann Street Tel Aviv 64239 Israel Journal Current Colorectal Cancer ReportsOnline ISSN 1556-3804Print ISSN 1556-3790 (Source: Current Colorectal Cancer Reports)

In Vitro and In Vivo Evaluation of Proniosomes Containing Celecoxib for Oral Administration.

AAPS PharmSciTech — Fri, 08 Jan 2010 00:00:00 +0100

In conclusion, the proniosomal oral delivery system of celecoxib with improved bioavailability was established. PMID: 20058106 [PubMed - as supplied by publisher] (Source: AAPS PharmSciTech)

Celecoxib Effective in Inhibiting Genetic Basal Cell Carcinoma

Medscape Today Headlines — Thu, 07 Jan 2010 22:13:02 +0100

In patients genetically predisposed to develop the disease, celecoxib was effective in reducing the tumor burden, especially in those with less severe symptoms. Medscape Medical News (Source: Medscape Today Headlines)

Common Anti-Inflammatory Drug Could Help Prevent Skin Cancers, Stanford Researcher Says

Health News from Medical News Today — Thu, 07 Jan 2010 08:00:00 +0100

A widely-available anti-inflammatory prescription drug can reduce the risk of a common skin cancer in humans, according to a researcher at Stanford's School of Medicine. Although oral administration of the drug, celecoxib, is associated with an increased risk of heart attack and stroke in some people, it's possible that topical application could have a safer, protective effect for people prone to developing the cancers, called basal cell carcinomas, the researcher believes... (Source: Health News from Medical News Today)

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Celebrex inhibits burden of skin cancer in high-risk patients, research finds

ScienceDaily Headlines — Wed, 06 Jan 2010 15:49:55 +0100

COX-2 Inhibitor May Ease Skin Cancer Burden (CME/CE)

MedPage Today Pain Management — Wed, 06 Jan 2010 12:13:10 +0100

For people with a rare condition putting them at high risk for skin basal cell carcinomas, the COX-2 inhibitor celecoxib (Celebrex) could substantially cut down on the hundreds or thousands of tumors they develop over a lifetime, researchers said. (Source: MedPage Today Pain Management)

Celebrex May Slow, Prevent Skin Cancers

MedicineNet Chronic Pain General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Chronic Pain General)

Celebrex May Slow, Prevent Skin Cancers

MedicineNet Cancer General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Cancer General)

Celebrex May Slow, Prevent Skin Cancers

MedicineNet Cholesterol General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Cholesterol General)

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Celebrex May Slow, Prevent Skin Cancers

MedicineNet Heart General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Heart General)

Celebrex May Slow, Prevent Skin Cancers

MedicineNet Skin General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Skin General)

Celebrex May Slow, Prevent Skin Cancers

MedicineNet Senior Health General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Senior Health General)

Celebrex May Slow, Prevent Skin Cancers

eMedicineHealth.com — Wed, 06 Jan 2010 07:00:00 +0100

(Source: eMedicineHealth.com)

Celebrex May Slow, Prevent Skin Cancers

MedicineNet Arthritis General — Wed, 06 Jan 2010 07:00:00 +0100

Title: Celebrex May Slow, Prevent Skin CancersCategory: Health NewsCreated: 1/6/2010 10:28:00 AMLast Editorial Review: 1/6/2010 10:28:21 AM (Source: MedicineNet Arthritis General)

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Common NSAID Could Prevent Skin Cancer

Medical Headlines From Ivanhoe.com — Wed, 06 Jan 2010 05:00:00 +0100

The widely available anti-inflammatory drug celecoxib (Celebrex) could protect against certain types of skin cancer. (Source: Medical Headlines From Ivanhoe.com)

Celebrex May Slow, Prevent Skin Cancers

WebMD Health — Tue, 05 Jan 2010 23:14:17 +0100

There is mounting evidence that nonsteroidal anti-inflammatory drugs (NSAIDs) may help prevent or slow the growth of non-melanoma skin cancers. (Source: WebMD Health)

Celebrex may prevent skin cancers

Medicineworld.org: New Article Alert — Tue, 05 Jan 2010 15:04:46 +0100

A widely-available anti-inflammatory prescription drug can reduce the risk of a common skin cancer in humans, as per a researcher at Stanford's School of Medicine. Eventhough oral administration of the drug, celecoxib, is linked to an increased risk of heart attack and stroke in some people, it's possible that topical application could have a safer, protective effect for people prone to developing the cancers, called basal cell carcinomas, the researcher believes........ (Source: Medicineworld.org: New Article Alert)

Celebrex Inhibited The Burden Of Skin Cancer In High-Risk Patients

Cancer / Oncology News From Medical News Today — Tue, 05 Jan 2010 10:00:00 +0100

Celebrex Inhibited The Burden Of Skin Cancer In High-Risk Patients

Health News from Medical News Today — Tue, 05 Jan 2010 10:00:00 +0100

People with the heritable disorder of the skin called Gorlin syndrome who are genetically predisposed to develop basal cell carcinoma of the skin may have a new chemoprevention therapy on the horizon. According to results of a placebo-controlled, randomized, double-blind, Phase II study, the use of celecoxib was effective in inhibiting the development of basal cell carcinomas in a relatively rare group of patients who are highly susceptible to carcinoma. These findings are published in the January issue of Cancer Prevention Research, a journal of the American Association for Cancer Research... (Source: Health News from Medical News Today)

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Common anti-inflammatory drug could help prevent skin cancers, Stanford researcher says

EurekAlert! - Medicine and Health — Tue, 05 Jan 2010 05:00:00 +0100

(Stanford University Medical Center) A widely-available anti-inflammatory prescription drug can reduce the risk of a common skin cancer in humans, according to a researcher at Stanford's School of Medicine. Although oral administration of the drug, celecoxib, is associated with an increased risk of heart attack and stroke in some people, it's possible that topical application could have a safer, protective effect for people prone to developing the cancers, called basal cell carcinomas, the researcher believes. (Source: EurekAlert! - Medicine and Health)

Celebrex inhibited the burden of skin cancer in high-risk patients

EurekAlert! - Medicine and Health — Tue, 05 Jan 2010 05:00:00 +0100

(American Association for Cancer Research) People with the heritable disorder of the skin called Gorlin syndrome who are genetically predisposed to develop basal cell carcinoma of the skin may have a new chemoprevention therapy on the horizon. (Source: EurekAlert! - Medicine and Health)

Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors.

Bioorganic & Medicinal Chemistry — Mon, 04 Jan 2010 00:00:00 +0100

Authors: Ghodsi R, Zarghi A, Daraei B, Hedayati M A new group of 2,3-diarylquinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para-position of the C-2 phenyl ring were synthesized and evaluated as selective COX-2 inhibitors. In vitro COX-1/COX-2 structure-activity relationships were determined by varying the substituents on the C-4 quinoline ring. Among the 2,3-diarylquinolines, 2-(4-(methylsulfonyl) phenyl)-3-phenylquinoline-4-carboxylic acid (8) exhibited the highest potency and selectivity for COX-2 inhibitory activity (COX-2 IC(50)=0.07muM; selectivity index=687.1) that was more selective than the reference drug celecoxib (COX-2 IC(50)=0.06muM; selectivity index=405). A molecular modeling study where 8 was docked in the binding site of COX-2 indicated that...

Study find NSAID's are no protection against skin cancer

About.com Skin Cancer — Mon, 04 Jan 2010 00:00:00 +0100

According to a new study, published in the Feb. 15 online issue of the Archives of Dermatology, prolonged use of non-steroidal anti-inflammatory drugs (NSAID's) such as aspirin, ibuprofen, and celecoxib offers no protection against skin cancer. Researchers at Kaiser Permanente Northern California compared the medical records of 415 patients between the ages 43-85, diagnosed with squamous cell carcinoma in 2004 to 415 patients of similar age, race, sex and gender with no history of cancer. Participants were required to provide information about their NSAID use 10 years prior to the study. Sixty-one percent of participants reported regular use of NSAID pain relievers. The results of the study revealed that irrespective of type of drug used or the dosage taken the NSAID's did not reduce ...

Influence of LOX/COX inhibitors on cell differentiation induced by all-trans retinoic acid in neuroblastoma cell lines.

International Journal of Molecular Medicine — Fri, 01 Jan 2010 22:58:19 +0100

Authors: Redova M, Chlapek P, Loja T, Zitterbart K, Hermanova M, Sterba J, Veselska R We investigated the possible modulation by LOX/ COX inhibitors of all-trans retinoic acid (ATRA)-induced cell differentiation in two established neuroblastoma cell lines, SH-SY5Y and SK-N-BE(2). Caffeic acid, as an inhibitor of 5-lipoxygenase, and celecoxib, as an inhibitor of cyclooxygenase-2, were chosen for this study. The effects of the combined treatment with ATRA and LOX/COX inhibitors on neuroblastoma cells were studied using cell morphology assessment, detection of differentiation markers by immunoblotting, measurement of proliferation activity, and cell cycle analysis and apoptosis detection by flow cytometry. The results clearly demonstrated the potential of caffeic acid to enhance ATRA-indu...

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[11C]-PK11195 PET: Quantification of neuroinflammation and a monitor of anti-inflammatory treatment in Parkinson's disease?

Parkinsonism and Related Disorders — Fri, 01 Jan 2010 00:00:00 +0100

Conclusions: In current practice, [11C]-PK11195 seems an unsuitable tracer for accurate or reliable quantification of neuroinflammation. Refinement of [11C]-PK11195 uptake analysis and, more importantly, further development of better tracers is necessary to enable accurate measurement of neuroinflammation and effects of anti-inflammatory treatment in patients. (Source: Parkinsonism and Related Disorders)

Myeloperoxidase Content is a Marker of Systemic Inflammation in a Chronic Condition: The Example Given by the Periodontal Disease in Rats

Mediators of Inflammation — Thu, 31 Dec 2009 15:46:31 +0100

The study aimed to evaluate the suitability of myeloperoxidase (MPO) content as a local indicator of chronic inflammation, using the periodontal disease model. Anesthetized adult male Holtzman rats had their second left maxilar molar tied by a thread for 11 days and were then killed. Blood samples and photographic images from histopathological inflamed and noninflamed (contralateral) neighboring gingivomucosal specimens were collected for cell counts and MPO level analysis. Diseased animals were also treated with pharmacological tools such as the anti-inflammatory drug celecoxib or the opioid morphine. Increased blood neutrophils and local cell numbers characterized diseased animals. However, local MPO content was increased in inflamed and noninflamed tissues from diseased animals. Celecox...

Anti-Inflammatory Drugs (Coxibs) Counter The Positive Effects Of Aspirin In Preventing Blood Clots

Health News from Medical News Today — Wed, 30 Dec 2009 08:00:00 +0100

A new study conducted at Ben-Gurion University of the Negev (BGU) reveals that Celebrex and other anti-inflammatory coxib medications may counter the positive effects of aspirin in preventing blood clots. The research, published in the Proceedings of the National Academy of Sciences (PNAS), indicates that people who are taking aspirin and coxibs together are in fact inhibiting the aspirin's effectiveness in preventing heart attacks and strokes... (Source: Health News from Medical News Today)

Anti-Inflammatory Drugs (Coxibs) Counter The Positive Effects Of Aspirin In Preventing Blood Clots

Pain / Anesthetics News From Medical News Today — Wed, 30 Dec 2009 08:00:00 +0100

Anti-Inflammatory Drugs (Coxibs) Counter The Positive Effects Of Aspirin In Preventing Blood Clots

Health News from Medical News Today — Wed, 30 Dec 2009 08:00:00 +0100

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Anti-Inflammatory Drugs (Coxibs) Counter The Positive Effects Of Aspirin In Preventing Blood Clots

Pain / Anesthetics News From Medical News Today — Wed, 30 Dec 2009 08:00:00 +0100

CELEBREX (Celecoxib) Capsule [Rebel Distributors Corp.]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Tue, 29 Dec 2009 05:00:00 +0100

Updated Date: Dec 29, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Anti-inflammatory drugs may disrupt aspirin's effectiveness

OrlandoSentinel: Medical Research — Tue, 29 Dec 2009 00:00:00 +0100

Anti-inflammatory drugs interfere with aspirin

Medicineworld.org: New Article Alert — Thu, 24 Dec 2009 05:03:55 +0100

A newly released study conducted at Ben-Gurion University of the Negev (BGU) reveals that Celebrex and other anti-inflammatory coxib medications may counter the positive effects of aspirin in preventing blood clots. The research, reported in the Proceedings of the National Academy of Sciences (PNAS), indicates that people who are taking aspirin and coxibs together are in fact inhibiting the aspirin's effectiveness in preventing heart attacks and strokes........ (Source: Medicineworld.org: New Article Alert)

Cytokine Profiles Induced by the Novel Swine‐Origin Influenza A/H1N1 Virus: Implications for Treatment Strategies

The Journal of Infectious Diseases Latest Issue — Wed, 23 Dec 2009 17:10:34 +0100

Conclusions. No major cytokine storm, as seen in H5N1 infection, is associated with S‐OIV infection of cell lines. The mainstay of treatment for uncomplicated S‐OIV infections should be antiviral agents without immunomodulators. For individual S‐OIV–infected patients with severe primary viral pneumonia, severe sepsis, and multiorgan failure, immunomodulators may be considered as an adjunctive therapy in clinical trials. (Source: The Journal of Infectious Diseases Latest Issue)

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Suppressive effect of COX2 inhibitor on the progression of adipose inflammation in high-fat-induced obese rats

European Journal of Clinical Investigation — Tue, 22 Dec 2009 00:00:00 +0100

Conclusions Our findings suggest that COX2 activation is crucially involved in the development of inflammatory response in adipose tissues of high-fat-induced obese rats. (Source: European Journal of Clinical Investigation)

Coxibs May Inhibit Effects of Low-Dose Aspirin

Modern Medicine — Tue, 22 Dec 2009 00:00:00 +0100

Celecoxib and other coxibs may interfere with the antiplatelet activity of low-dose aspirin, according to a study published online Dec. 16 in the Proceedings of the National Academy of Sciences. (Source: Modern Medicine)

Celebrex may affect low-dose aspirin use

Health News - UPI.com — Fri, 18 Dec 2009 18:48:07 +0100

ANN ARBOR, Mich., Dec. 18 (UPI) -- U.S. researchers suggest celecoxib or Celebrex may keep low-dose aspirin from limiting blood clots. (Source: Health News - UPI.com)

[Comment] A protocol for labrador retrievers?

LANCET — Fri, 18 Dec 2009 00:00:00 +0100

On Christmas Day, 2000, Navy, a golden retriever aged 18 months, began a cocktail of celecoxib, tamoxifen, and doxycycline to target blood vessels supplying a tumour on her chest. Her owner Marion Haber, a veterinary student at Tufts University, Boston, MA, USA, was acquainted with the work of angiogenesis pioneer Judah Folkman at the nearby Children's Hospital, Harvard Medical School. Soon, the golden retriever became a golden guineapig. The treatment was blinded to the patient, who unknowingly polished off the regimen with her dog biscuits. 3 months later, Navy was cancer free, and the following year a healthy report was published in a US national newspaper. The excitement around the story led to the drug combination being renamed the Navy protocol, which remains a familiar term in veter...

Celecoxib Could Impede Effects of Low-Dose Aspirin

Medscape Today Headlines — Thu, 17 Dec 2009 23:34:59 +0100

New research in dogs suggests that the COX-2 inhibitor celecoxib might impede the action of "baby" aspirin. However, the results need to be confirmed in human studies, say the researchers. Heartwire (Source: Medscape Today Headlines)

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Painkiller undermines aspirin's anti-clotting action

ScienceDaily Headlines — Thu, 17 Dec 2009 15:46:56 +0100

Celecoxib could impede effects of low-dose aspirin

theHeart.org — Thu, 17 Dec 2009 15:00:25 +0100

Cox-2 Inhibitor Blunts Aspirin's Cardioprotection (CME/CE)

MedPage Today Psychiatry — Wed, 16 Dec 2009 13:39:04 +0100

The pain killer celecoxib (Celebrex) may interfere with the cardioprotective benefit of low-dose aspirin, researchers found. (Source: MedPage Today Psychiatry)

Cox-2 Inhibitor Blunts Aspirin's Cardioprotection (CME/CE, with audio)

MedPage Today Pain Management — Wed, 16 Dec 2009 13:39:04 +0100

The pain killer celecoxib (Celebrex) may interfere with the cardioprotective benefit of low-dose aspirin, researchers found. (Source: MedPage Today Pain Management)

Celebrex and aspirin combination may reduce cardiac gain

Arthritis Research Campaign — Wed, 16 Dec 2009 00:00:00 +0100

People who take low-dose aspirin to reduce their risk of heart attack or stroke may gain little benefit if they have also been prescribed the painkiller Celebrex (celecoxib), a study has found. (Source: Arthritis Research Campaign)

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Combining Celebrex With Low-Dose Aspirin May Reduce Protection From Heart Attack And Stroke, Study Suggests

Stroke / Neuroprotection News From Medical News Today — Tue, 15 Dec 2009 11:00:00 +0100

Combining Celebrex With Low-Dose Aspirin May Reduce Protection From Heart Attack And Stroke, Study Suggests

Health News from Medical News Today — Tue, 15 Dec 2009 11:00:00 +0100

Millions of Americans take Celebrex for arthritis or other pain. Many, if they are middle-aged or older, also take a low-dose aspirin tablet daily to reduce the risk of heart attack and stroke. Yet they may be getting little protection, because Celebrex keeps the aspirin from doing its job effectively, a new study suggests. In laboratory studies, University of Michigan researchers found that several coxibs, the drug class to which Celebrex belongs, interfere with aspirin's ability to discourage blood clots, if the aspirin is taken in low doses... (Source: Health News from Medical News Today)

Combining Celebrex With Low-Dose Aspirin May Reduce Protection From Heart Attack And Stroke, Study Suggests

Pain / Anesthetics News From Medical News Today — Tue, 15 Dec 2009 11:00:00 +0100

Mechanisms of Kv2.1 channel inhibition by celecoxib – modification of gating and channel block

British Journal of Pharmacology — Tue, 15 Dec 2009 00:00:00 +0100

Conclusions and implications: Celecoxib reduced current through Kv2.1 channels by modifying gating and inducing closed- and open-channel block, with the three effects manifesting at different concentrations. These data will help to elucidate the mechanisms of action of this widely prescribed drug on ion channels and those underlying its neurological, cardiovascular and other effects. (Source: British Journal of Pharmacology)

NSAID prescribing precautions.

American Family Physician — Tue, 15 Dec 2009 00:00:00 +0100

Authors: Risser A, Donovan D, Heintzman J, Page T Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used, but have risks associated with their use, including significant upper gastrointestinal tract bleeding. Older persons, persons taking anticoagulants, and persons with a history of upper gastrointestinal tract bleeding associated with NSAIDs are at especially high risk. Although aspirin is cardioprotective, other NSAIDs can worsen congestive heart failure, can increase blood pressure, and are related to adverse cardiovascular events, such as myocardial infarction and ischemia. Cyclooxygenase-2 inhibitors have been associated with increased risk of myocardial infarction; however, the only cyclooxygenase-2 inhibitor still available in the United States, celecoxib, seems to be ...

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Painkiller undermines aspirin's anti-clotting action

EurekAlert! - Medicine and Health — Mon, 14 Dec 2009 05:00:00 +0100

(University of Michigan Health System) Millions of Americans take Celebrex for arthritis or other pain. Many, if they are middle-aged or older, also take a low-dose aspirin tablet daily to reduce the risk of heart attack and stroke. Yet they may be getting little protection, because Celebrex keeps the aspirin from doing its job effectively, a new study suggests. (Source: EurekAlert! - Medicine and Health)

COX-2 expression in chondrosarcoma: A role for celecoxib treatment?

European Journal of Cancer — Thu, 10 Dec 2009 00:00:00 +0100

Abstract: Chondrosarcomas are resistant to conventional chemo- and radiotherapy. A subset of chondrosarcomas arises secondarily in the benign tumour syndromes enchondromatosis (EC) and multiple osteochondromas (MO), and prevention of tumour development would greatly improve prognosis. We therefore investigated the effect of selective COX-2 inhibition on chondrosarcoma growth.COX-2 expression was studied in central- and peripheral cartilaginous tumours. The effect of COX-2 inhibition was assessed in four high-grade chondrosarcoma cell lines using celecoxib and NS-398 treatment. COX-2 activity (prostaglandin E2 (PGE2) ELISA) and cell viability were measured. The (prophylactic) effect of celecoxib on chondrosarcoma growth in vivo was studied for 8weeks using a xenograft model of cell line CH2...

Celecoxib Benefits Not Seen in Acute Renal Colic Patients

Modern Medicine — Wed, 09 Dec 2009 00:00:00 +0100

In patients with ureteral stones and acute renal colic, the use of celecoxib was not associated with time until stone passage or decreased pain, according to research published in the November issue of Urology. (Source: Modern Medicine)

Celecoxib: Liver failure: case report

Reactions — Mon, 07 Dec 2009 14:04:26 +0100

(Source: Reactions)

Abstract A37: Mechanistic study involving antiproliferative effect of Etoricoxib, a highly selective COX-2 inhibitor on human cancer cell lines

Cancer Research — Wed, 02 Dec 2009 04:15:23 +0100

In conclusion this study shows that in the human cervical cancer cell lines, HeLa & C33A, Etoricoxib suppresses proliferation, induces apoptosis and causes cell death by DNA damage in both Cox-2 dependent as well as independent pathway.Citation Information: Cancer Res 2009;69(23 Suppl):A37. (Source: Cancer Research)

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Bextra/Celebrex Objectors Claim Disparate Treatment In Consumer Settlement

LexisNexis® Mealey's™ Arthritis Drugs Legal News — Tue, 01 Dec 2009 15:33:34 +0100

SAN FRANCISCO - Two objectors to a proposed $89 million class settlement of purchase price claims over Pfizer's painkillers Bextra and Celebrex have withdrawn their appeal to the Ninth Circuit U.S. Court of Appeals, according to a Nov. 12 stipulation (In Re: Bextra and Celebrex Marketing Sales Practices and Product Liability Litigation, MDL Docket No. 1699, No. 05-1699, N.D. Calif.; See September 2009, Page 12). Full story on lexis.com (Source: LexisNexis® Mealey's™ Arthritis Drugs Legal News)

Preventive effects of COX-2 inhibitor, celecoxib on renal tubular injury induced by shock wave lithotriptor

Urological Research — Tue, 01 Dec 2009 08:29:00 +0100

This study suggests that celecoxib would be useful prior and after SWL because of renal protective effects. Content Type Journal ArticleCategory Original PaperDOI 10.1007/s00240-009-0243-zAuthors Hyoung Keun Park, College of Medicine, Dongguk University Department of Urology Kyongju KoreaHae Won Lee, College of Medicine, Dongguk University Department of Urology Kyongju KoreaKwang Soo Lee, College of Medicine, Dongguk University Department of Urology Kyongju KoreaJong Sun Choi, College of Medicine, Dongguk University Department of Pathology Kyongju KoreaByong Chang Jeong, College of Medicine, Sungkyunkwan University Department of Urology Seoul KoreaHyeon Hoe Kim, College of Medicine, Seoul National University Department of Urology Seoul Korea Journal Urological ResearchOnline IS...

Preventive effects of COX-2 inhibitor, celecoxib on renal tubular injury induced by shock wave lithotriptor.

Urological Research — Tue, 01 Dec 2009 00:00:00 +0100

This study suggests that celecoxib would be useful prior and after SWL because of renal protective effects. PMID: 19949782 [PubMed - as supplied by publisher] (Source: Urological Research)

CELEBREX (Celecoxib) Capsule [Blenheim Pharmacal, Inc.]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Mon, 30 Nov 2009 05:00:00 +0100

Updated Date: Nov 30, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Cyclooxygenase-2 mediated regulation of E-cadherin occurs in conventional but not early-onset gastric cancer cell lines.

Cellular Oncology — Sat, 28 Nov 2009 03:04:02 +0100

Conclusion: The results suggest that COX-2 has an impact on transcriptional regulation of E-cadherin in gastric cancer and our findings further highlight the intriguing nature of EOGCs which appear to have a molecular phenotype distinct from conventional gastric cancer. In addition, our findings also suggest that reduction of COX-2 using nonsteroidal anti-inflammatory drugs in gastric cancer chemoprevention may only be relevant for older patients. PMID: 19940363 [PubMed - in process] (Source: Cellular Oncology)

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COX-2 Inhibitors Are Contraindicated for Treatment of Combined Injury.

Radiation Research — Fri, 27 Nov 2009 15:16:28 +0100

This study points to potential contraindications for use of COX-2 inhibitors in patients undergoing therapy for radiation injury and combined injury. PMID: 19929415 [PubMed - as supplied by publisher] (Source: Radiation Research)

Celecoxib treatment reduces peritoneal fibrosis and angiogenesis and prevents ultrafiltration failure in experimental peritoneal dialysis

Nephrology Dialysis Transplantation — Tue, 24 Nov 2009 09:02:16 +0100

Conclusions. Altogether, celecoxib treatment improves UF capacity and reduces morphological alterations in our rat PD model. (Source: Nephrology Dialysis Transplantation)

Effect of a cyclooxygenase-2 inhibitor on postexercise muscle protein synthesis in humans.

Am J Physiol Endocri... — Tue, 24 Nov 2009 00:00:00 +0100

Authors: Burd NA, Dickinson JM, Lemoine JK, Carroll CC, Sullivan BE, Haus JM, Jemiolo B, Trappe SW, Hughes GM, Sanders CE, Trappe TA Non-selective blockade of the cyclooxygenase (COX) enzymes in skeletal muscle eliminates the normal increase in muscle protein synthesis following resistance exercise. The current study tested the hypothesis that this COX-mediated increase in postexercise muscle protein synthesis is specifically regulated by the COX-2 isoform. Sixteen males (23+/-1y) were randomly assigned to one of two groups that received three doses of either a selective COX-2 inhibitor (celecoxib; 200 mg/dose, 600 mg total) or a placebo in double-blind fashion during the 24h following a single bout of knee extensor resistance exercise. At rest and 24h postexercise skeletal muscle prot...

[Inhibitory effects of COX-2 inhibitor on migration of human tongue squamous cell carcinoma Tca8113 cells.]

Journal of Southern Medical University — Fri, 20 Nov 2009 00:00:00 +0100

CONCLUSION: COX-2 inhibitor celecoxib can inhibit Tca8113 cell migration, the mechanism of which awaits further investigation. PMID: 19923064 [PubMed - as supplied by publisher] (Source: Journal of Southern Medical University)

Hospitalizations for gastrointestinal and cardiovascular events in the CADEUS cohort of traditional or Coxib NSAID users

British Journal of Clinical Pharmacology — Fri, 20 Nov 2009 00:00:00 +0100

CONCLUSIONS Hospitalization rates for GI bleeding were 10[ndash]20 times lower than expected from published randomized clinical trials, probably because of differences in drug usage and concomitant gastroprotection. CV event rates conformed to those expected from general population data. These results emphasize the necessity of developing population healthcare databases to explore such low event rates. (Source: British Journal of Clinical Pharmacology)

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Novel nitro-oxy derivatives of celecoxib for the regulation of colon cancer cell growth.

Chemico-Biological Interactions — Wed, 18 Nov 2009 10:23:06 +0100

Authors: Bozzo F, Bassignana A, Lazzarato L, Boschi D, Gasco A, Bocca C, Miglietta A Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) developed as a selective inhibitor of cyclooxygenase-2 (COX-2). Despite the associated cardiovascular toxicity risk, celecoxib has been found to be effective in reducing cancer risk in animal and human studies. In the present study the antiproliferative activity of novel nitro-oxy-methyl substituted analogues of celecoxib (NO-cel), potentially less cardiotoxic, has been investigated in vitro on human colon cancer cells and compared with action of the parent drug. Moreover, experiments were performed in order to evaluate whether COX-2 pharmacological inhibition may affect beta-catenin/E-cadherin signalling pathway. All the tested analogues of c...

Pregabalin, celecoxib, and their combination for treatment of chronic low-back pain

Journal of Orthopaedics and Traumatology — Wed, 18 Nov 2009 09:28:48 +0100

Conclusions Combination of celecoxib and pregabalin is more effective than monotherapy for chronic low-back pain, with similar adverse effects. Content Type Journal ArticleCategory Original ArticleDOI 10.1007/s10195-009-0077-zAuthors Carlo Luca Romanò, Istituto Ortopedico I.R.C.C.S. Galeazzi Via Riccardo Galeazzi, 4 20166 Milan ItalyDelia Romanò, Istituto Ortopedico I.R.C.C.S. Galeazzi Via Riccardo Galeazzi, 4 20166 Milan ItalyCristina Bonora, Istituto Ortopedico I.R.C.C.S. Galeazzi Via Riccardo Galeazzi, 4 20166 Milan ItalyGiuseppe Mineo, Università degli Studi di Milano Istituto Ortopedico I.R.C.C.S. Galeazzi Via Riccardo Galeazzi, 4 20166 Milan Italy Journal Journal of Orthopaedics and TraumatologyOnline ISSN 1590-9999Print ISSN 1590-9921 (Source: Journal ...

Matrix Metalloproteinase (MMP)-1 and MMP-3 Induce Macrophage MMP-9: Evidence for the Role of TNF-{alpha} and Cyclooxygenase-2.

Journal of Immunology — Wed, 18 Nov 2009 00:00:00 +0100

Authors: Steenport M, Khan KM, Du B, Barnhard SE, Dannenberg AJ, Falcone DJ Matrix metalloproteinase (MMP)-9 (gelatinase B) participates in a variety of diverse physiologic and pathologic processes. We recently characterized a cyclooxygenase-2 (COX-2)-->PGE(2)-->EP4 receptor axis that regulates macrophage MMP-9 expression. In the present studies, we determined whether MMPs, commonly found in inflamed and neoplastic tissues, regulate this prostanoid-EP receptor axis leading to enhanced MMP-9 expression. Results demonstrate that exposure of murine peritoneal macrophages and RAW264.7 macrophages to MMP-1 (collagenase-1) or MMP-3 (stromelysin-1) lead to a marked increase in COX-2 expression, PGE(2) secretion, and subsequent induction of MMP-9 expression. Proteinase-induced MMP-9 expr...

Synthesis and antitumor properties of selenocoxib-1 against rat prostate adenocarcinoma cells

International Journal of Cancer — Mon, 16 Nov 2009 00:00:00 +0100

This study demonstrates that Selenocoxib-1 is more effective against prostate cancer than Celecoxib. (Source: International Journal of Cancer)

Synergistic anticancer effects of combined gamma-tocotrienol and celecoxib treatment are associated with suppression in Akt and NFkappaB signaling.

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie — Sat, 14 Nov 2009 00:00:00 +0100

Authors: Shirode AB, Sylvester PW The selective cyclooxygenase (COX)-2 inhibitor, celecoxib, and the vitamin E isoform, gamma-tocotrienol, both display potent anticancer activity. However, high dose clinical use of selective COX-2 inhibitors has been limited by gastrointestinal and cardiovascular toxicity, whereas limited absorption and transport of gamma-tocotrienol by the body has made it difficult to obtain and sustain therapeutic levels in the blood and target tissues. Studies were conducted to characterize the synergistic anticancer antiproliferative effects of combined low dose celecoxib and gamma-tocotrienol treatment on mammary tumor cells in culture. The highly malignant mouse +SA mammary epithelial cells were maintained in culture on serum-free defined control or treatment me...

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Celecoxib loaded liposomes: effect of cholesterol on encapsulation and in vitro release characteristics.

Bioscience Reports — Tue, 10 Nov 2009 00:00:00 +0100

We describe here the encapsulation of CLX in multilamellar vesicles (MLVs) composed of DSPC and variable amounts of cholesterol. The effect of cholesterol content on liposome size, percent drug loading and in vitro drug release profiles were investigated. Differential scanning calorimetry and Fourier transform infrared (FTIR) spectroscopy were used to determine molecular interactions between CLX, cholesterol and DSPC. The phase transition temperature (Tm) of vesicles was reduced in a synergistic manner in the presence of both CLX and cholesterol. Encapsulation efficiency, loading and release of CLX decreased with increasing cholesterol content. FTIR data indicated that this decrease was due to a competition between CLX and cholesterol for the cooperativity region of the phospholipids. In t...

Biotransformation of Celecoxib Using Microbial Cultures.

Applied Biochemistry and Biotechnology — Sat, 07 Nov 2009 00:00:00 +0100

Authors: Srisailam K, Veeresham C Microbial transformation studies can be used as models to simulate mammalian drug metabolism. In the present investigation, biotransformation of celecoxib was studied in microbial cultures. Bacterial, fungal, and yeast cultures were employed in the present study to elucidate the metabolism of celecoxib. The results indicate that a number of microorganisms metabolized celecoxib to various levels to yield eight metabolites, which were identified by high-performance liquid chromatography diode array detection and liquid chromatography tandem mass spectrometry analyses. HPLC analysis of biotransformed products indicated that majority of the metabolites are more polar than the substrate celecoxib. The major metabolite was found to be hydroxymethyl metabolit...

The Effects of Nepafenac and Amfenac on Retinal Angiogenesis.

Brain Research Bulletin — Thu, 05 Nov 2009 00:00:00 +0100

CONCLUSIONS: Nepafenac and amfenac inhibit OIR more effectively than the commercially available topical and injectable NSAIDs used in this study. Our data suggests there are COX-dependent and COX-independent mechanisms by which amfenac inhibits OIR. Because it is bioavailable to the posterior segment following topical delivery, nepafenac appears to be a promising advancement in the development of therapies for neovascular eye diseases. PMID: 19897019 [PubMed - as supplied by publisher] (Source: Brain Research Bulletin)

Aspirin-triggered lipoxin in patients treated with aspirin and selective vs. nonselective COX-2 inhibitors

British Journal of Clinical Pharmacology — Thu, 05 Nov 2009 00:00:00 +0100

CONCLUSIONS Neither selective nor nonselective COX-2 inhibition appreciably interferes with ATL biosynthesis, suggesting that this mediator is not involved in exacerbating gastrotoxicity by the association of aspirin with COX-2 inhibitors. (Source: British Journal of Clinical Pharmacology)

Pharmacological Inhibition of 5-Lipoxygenase Accelerates and Enhances Fracture-Healing

JBJS [Am] — Mon, 02 Nov 2009 18:02:22 +0100

Conclusions: Systemic inhibition of 5-lipoxygenase with an orally delivered drug significantly accelerated and enhanced fracture-healing in this rat model. Gene expression analysis indicates that cyclooxygenase-2 is necessary for callus chondrocytes to progress into hypertrophy so as to complete endochondral ossification. Conversely, inhibition of 5-lipoxygenase alters the inflammatory response, which enhances callus chondrocyte hypertrophy and accelerates endochondral ossification. Clinical Relevance: These results suggest a novel approach to the treatment of human fractures and demonstrate that arachidonic acid metabolism can be manipulated to inhibit or accelerate fracture-healing, underscoring the importance of this pathway in bone regeneration. (Source: JBJS [Am])

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A Novel Composite Endpoint to Evaluate the Gastrointestinal (GI) Effects of Nonsteroidal Antiinflammatory Drugs Through the Entire GI Tract.

J Rheumatol — Mon, 02 Nov 2009 00:00:00 +0100

CONCLUSION: By providing clinicians with a new, descriptive language for adverse events through the entire GI tract, the CSULGIE endpoint has the potential to become a standard tool for evaluating the GI effects of a range of therapies. PMID: 19884267 [PubMed - as supplied by publisher] (Source: J Rheumatol)

Pharmacological inhibition of 5-lipoxygenase accelerates and enhances fracture-healing.

The Journal of Bone and Joint Surgery. American volume — Sun, 01 Nov 2009 00:00:00 +0100

CONCLUSIONS: Systemic inhibition of 5-lipoxygenase with an orally delivered drug significantly accelerated and enhanced fracture-healing in this rat model. Gene expression analysis indicates that cyclooxygenase-2 is necessary for callus chondrocytes to progress into hypertrophy so as to complete endochondral ossification. Conversely, inhibition of 5-lipoxygenase alters the inflammatory response, which enhances callus chondrocyte hypertrophy and accelerates endochondral ossification. PMID: 19884440 [PubMed - in process] (Source: The Journal of Bone and Joint Surgery. American volume)

Effects of No.2 Renal Failure Recipe on expressions of cyclooxygenase-2 and -1 mRNAs in rats with chronic renal failure.

Zhong xi yi jie he xue bao : Journal of Chinese Integrative Medicine. — Sun, 01 Nov 2009 00:00:00 +0100

Authors: Pu GJ, Wang C, Zheng PD, He LQ Objective: To observe the effects of No.2 Renal Failure Recipe (No.2RFR), a compound traditional Chinese herbal medicine, on expressions of cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1) mRNAs in rats with chronic renal failure (CRF). Methods: A rat model of CRF was successfully established by infarction of approximately two-thirds of the left kidney and removal of the right kidney (ablation/infarction, A/I). Thirty A/I rats were randomly divided into untreated group, celebrex group and No.2RFR group. Another 10 SD rats were selected as normal control group. After 2-month treatment, the pathology of the nephridial tissue was observed with hematoxylin and eosin straining under a light microscope. Renal function including serum creatinine (S...

Is Short-Term Celecoxib Intervention A Effective Method For Preventing Gastric Carcinogenesis?

Health News from Medical News Today — Fri, 30 Oct 2009 07:00:00 +0100

Since the isolation and culture of Helicobacter pylori (H. pylori) in 1983, this bacterium has become accepted as an important human pathogen for the development of gastritis, peptic ulcer, and gastric cancer. Cyclooxgenase-2 (COX-2) is a prostaglandin-synthesizing enzyme. Elevated expression of COX-2 is observed in a wide variety of human malignancies, including gastric cancer. (Source: Health News from Medical News Today)

The PI3K/Akt/FOXO3a/p27(Kip1) signaling contribuTES to Anti-inflammatory Drug-suppressed proliferation of human osteoblasts.

Biochemical Pharmacology — Fri, 30 Oct 2009 00:00:00 +0100

In this study, we hypothesized that these drugs might increase p27(Kip1) expression in hOBs by altering the Akt/FOXO signaling. We tested this hypothesis by examining the influences of three anti-inflammatory drugs on the levels and/or activities of Akt, FOXO and p27(Kip1) as well as the relationship between these factors and proliferation of hOBs. We tested the effects of indomethacin (10(-5) and 10(-4)M), celecoxib (10(-6) and 10(-5)M), and dexamethasone (10(-7) and 10(-6)M) using PI3K inhibitor, LY294002 (10(-5)M) as the basis of comparison. The three drugs suppressed the canonical level of phosphorylated Akt in hOBs. This was accompanied by elevated FOXO3a level and increased promoter activity, mRNA expression and protein level of p27(Kip1). Furthermore, the anti-inflammatory drugs sup...

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Bextra-Celebrex Judge Approves $89M Settlement Resolving Consumer Claims

LexisNexis® Mealey's™ Arthritis Drugs Legal News — Thu, 29 Oct 2009 14:30:33 +0100

SAN FRANCISCO - An $89 million settlement of consumer claims over Pfizer Inc.'s painkillers Bextra and Celebrex was approved Sept. 28 by the federal judge supervising consolidated litigation (In Re: Bextra and Celebrex Marketing Sales Practices and Product Liability Litigation, MDL Docket No. 1699, No. M:05-CV-1699, N.D. Calif.; See September 2009, Page 12). Full story on lexis.com (Source: LexisNexis® Mealey's™ Arthritis Drugs Legal News)

Bextra/Celebrex Objectors Claim Disparate Treatment In Consumer Settlement

LexisNexis® Mealey's™ Arthritis Drugs Legal News — Thu, 29 Oct 2009 14:30:33 +0100

SAN FRANCISCO - Two objectors to a proposed $89 million class settlement of purchase price claims over Pfizer's painkillers Bextra and Celebrex filed a supplemental objection on Sept. 23, arguing that class members who purchased both drugs should be able to recover for purchases of Celebrex (In Re: Bextra and Celebrex Marketing Sales Practices and Product Liability Litigation, MDL Docket No. 1699, No. 05-1699, N.D. Calif.; See September 2009, Page 12). Full story on lexis.com (Source: LexisNexis® Mealey's™ Arthritis Drugs Legal News)

Judge Says Sealed Papers Were Not Relevant To Summary Judgment

LexisNexis® Mealey's™ Arthritis Drugs Legal News — Thu, 29 Oct 2009 14:30:33 +0100

NEWARK, N.J. - The judge presiding over shareholder derivative litigation brought in New Jersey by labor union pension funds over Pfizer Inc.'s painkiller Celebrex has denied a plaintiffs' motion to unseal internal corporate communications, saying Oct. 20 that the documents were irrelevant to the only decision in the case - her grant of summary judgment on statute of limitations grounds (Robert L. Garber, et al. v. Pharmacia Corp., et al., No. 3:03-cv-01519, D. N.J.; See July 2009, Page 12). Full story on lexis.com (Source: LexisNexis® Mealey's™ Arthritis Drugs Legal News)

Is short-term Celecoxib intervention a effective method for preventing gastric carcinogenesis?

EurekAlert! - Medicine and Health — Wed, 28 Oct 2009 04:00:00 +0100

(World Journal of Gastroenterology) Helicobacter pylori has been accepted as an important pathogen inducing gastric cancer. A research group from Taiwan investigated optimal intervention point of Celecoxib, to inhibit H. pylori-associated gastric carcinogenesis in Mongolian gerbils. They found that short-term use resulted in less severe inflammation and inhibited the invasion degree of gastric cancer. Therefore, Celecoxib could be used in the later stages of H. pylori infection to achieve safe and effective chemoprevention of gastric adenocarcinoma. (Source: EurekAlert! - Medicine and Health)

Effect of celecoxib on emotional stress and pain-related behaviors evoked by experimental tooth movement in the rat.

The Angle Orthodontist — Tue, 27 Oct 2009 19:19:33 +0100

Conclusions: The administration of celecoxib relieves pain- and stress-related behavior evoked by orthodontic tooth movement in the rat. This model might be a useful tool for the evaluation of pain and stress. PMID: 19852611 [PubMed - in process] (Source: The Angle Orthodontist)

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NSAID switching and short-term gastrointestinal outcome rates after the withdrawal of rofecoxib

Pharmacoepidemiology and Drug Safety — Tue, 20 Oct 2009 23:00:00 +0100

The consequences of the rofecoxib withdrawal on upper GI toxicity are largely unknown. We sought to estimate the effect of switching from selective Cox-2 inhibitors to non-selective non-steroidal anti-inflammatory drugs (nsNSAIDs) on the incidence of upper GI adverse events following the withdrawal of rofecoxib on 30 September 2004.We identified a cohort of 33 045 patients with arthritis and chronic use of any selective Cox-2 inhibitor during the 6 months before the withdrawal of rofecoxib in claims data from several US health plans. We calculated monthly rates of hospitalization for upper GI adverse events or upper GI endoscopy for the 6 months before and 3 months after the switching and compared the time trends in outcomes.In the subgroup of 15 916 patients using rofecoxib immediately be...

Role of selective cyclooxygenase-2 inhibitors in exacerbation of inflammatory bowel disease: a systematic review and meta-analysis

NeLM - Patient Safety — Tue, 20 Oct 2009 23:00:00 +0100

Source: DARE Area: Evidence > Medication Safety CRD Summary: This review concluded that there is insufficient data to determine the impact of cyclooxygenase-2 inhibitors on the risk of inflammatory bowel disease exacerbations. The review was well conducted and the authors' cautious conclusion is justified given the evidence presented. [One study randomised participants to etoricoxib 60-120mg/d for three months, while the other trial used oral celecoxib 200mg or placebo twice a day for 14 days. ] CRD Commentary: This review addressed a clear question in terms of inclusion criteria, study design and participants. Relevant databases were searched and the search terms were reported. No language restrictions were applied and efforts were made to retrieve unpublished data, minimising the ri...

Short-term Celecoxib intervention is a safe and effective chemopreventive for gastric carcinogenesis based on a Mongolian gerbil model.

World Journal of Gastroenterology : WJG — Tue, 20 Oct 2009 23:00:00 +0100

CONCLUSION: Short-term treatment with Celecoxib has an anti-carcinogenic effect, and resulted in less severe inflammation and inhibited the invasive degree of gastric cancer. PMID: 19842220 [PubMed - in process] (Source: World Journal of Gastroenterology : WJG)

Proteomic analysis in NSAIDs-Treated primary cardiomyocytes.

Journal of Proteomics — Mon, 19 Oct 2009 00:00:00 +0100

In this study, we tried to identify proteins responding to the cellular toxicity in NSAIDs-treated primarily cultured cardiomyocytes using 2-D proteomic analysis. We used seven different NSAIDs (celecoxib, rofecoxib, valdecoxib, diclofenac, naproxen, ibuprofen, meloxicam) possessing each different degree of cardiovascular risk. Overall protein spots were similar in all NSAIDs-treated cells although numbers of decreased proteins were about 2-fold higher in celecoxib or rofecoxib-treated cells than in cells incubated with other NSAIDs. Many stress-related proteins, cardiac muscle movement proteins and proteins involving in membrane organization have been isolated. Among them, Septin-8, a filament scaffolding protein, showed its specific expression pattern depending on the extent of drug toxi...

Investigators At Massachusetts General Hospital Have Published New Data On Colon Cancer

Cancercompass News: Colorectal Cancer — Sat, 17 Oct 2009 00:00:00 +0100

Although evidence suggests that aspirin and celecoxib may reduce the risk of colorectal cancer (CRC), these drugs can also cause harmful side effects. The aim of this study was to characterize patient preferences for celecoxib and aspirin, scientists in the United States report. (Source: Cancercompass News: Colorectal Cancer)

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Phase II, Randomized, Placebo-Controlled Trial of Neoadjuvant Celecoxib in Men With Clinically Localized Prostate Cancer: Evaluation of Drug-Specific Biomarkers [Genitourinary Cancer]

Journal of Clinical Oncology — Fri, 16 Oct 2009 22:02:50 +0100

Conclusion Treatment with 4 to 6 weeks of celecoxib had no effect on intermediate biomarkers of prostate carcinogenesis, despite the achievement of measurable tissue levels. We caution against using celecoxib 400 mg twice daily as a preventive agent for prostate cancer in additional studies. (Source: Journal of Clinical Oncology)

Celecoxib induces hepatic stellate cell apoptosis through inhibition of Akt activation and suppresses hepatic fibrosis in rats

Gut — Thu, 15 Oct 2009 22:22:00 +0100

Conclusions: Celecoxib shows a proapoptotic effect on HSCs through Akt inactivation and shows antifibrogenic effects in BDL- and TAA-treated rats, suggesting celecoxib as a novel antifibrotic agent of hepatic fibrosis. (Source: Gut)

Inhibition of Azoxymethane-Induced Colorectal Cancer by CP-31398, a TP53 Modulator, Alone or in Combination with Low Doses of Celecoxib in Male F344 Rats

Cancer Research — Thu, 15 Oct 2009 04:07:39 +0100

Tumor suppressor p53 plays a major role in colorectal cancer development. The present study explores the effects of p53-modulating agent CP-31398 alone and combined with celecoxib on azoxymethane-induced aberrant crypt foci (ACF) and colon adenocarcinomas in F344 rats. Maximum tolerated doses were 400 and 3,000 ppm for CP-31398 and celecoxib, respectively. ACF and tumor efficacy endpoints were carried out on azoxymethane-treated 7-week-old rats (48 per group) fed the control AIN-76A diet. Two weeks after carcinogen treatment, rats were fed the diets containing 0, 150, or 300 ppm CP-31398, 300 ppm celecoxib, or 150 ppm CP-31398 plus 300 ppm celecoxib. ACF and colon adenocarcinomas were determined at 8 and 48 weeks after azoxymethane treatment, respectively. Dietary CP-31398 was shown to sup...

Celecoxib: Multifocal fixed drug eruption: case report

Reactions — Mon, 12 Oct 2009 13:02:30 +0100

(Source: Reactions)

Familial adenomatous polyposis

Orphanet Journal of Rare Diseases — Sun, 11 Oct 2009 23:00:00 +0100

(FAP) is characterized by the development of hundreds to thousands of adenomas in the rectum and colon during the second decade of life. FAP has an incidence at birth of about 1/8,300, manifests equally in both sexes, and accounts for less than 1% colorectal cancer (CRC) cases. In the European Union, prevalence has been estimated at 1/11,300-37,600. Most patients are asymptomatic for years until the adenomas are large and numerous, and cause rectal bleeding or even anemia, or cancer develops. Generally, cancers start to develop a decade after the appearance of the polyps. Nonspecific symptoms may include constipation or diarrhea, abdominal pain, palpable abdominal masses and weight loss. FAP may present some extraintestinal manifestations such as osteomas, dental abnormalities (unerupted ...

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Chemopreventive effect of nonsteroidal anti-inflammatory drugs on 9,10-dimethylbenz[a]anthracene-induced lung carcinogenesis in mice.

Oncology Research — Fri, 09 Oct 2009 00:44:03 +0100

Authors: Saini RK, Sanyal SN Nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin, celecoxib, and etoricoxib were studied as chemopreventive agents in lung cancer in mice induced by 9,10-dimethylbenz[a]anthracene (DMBA). The animals were subjected to a single intratracheal instillation of DMBA by surgical intervention, while they were treated with oral NSAIDs daily at their following anti-inflammatory dose: aspirin 25 mg/kg, celicoxib 6 mg/kg, and etoricoxib 0.6 mg/kg body weight, respectively. The animals were sacrificed after 18 weeks of treatment. Results showed a significant incidence of pulmonary tumors, dysplastic changes in histopathology, and signs of inflammatory occurrence in the DMBA-treated animals, which were grossly reversed by the NSAIDs. A greater number of mac...

PC-407, a celecoxib derivative, inhibited the growth of colorectal tumor in vitro and in vivo

Cancer Science — Thu, 08 Oct 2009 23:00:00 +0100

This study aimed to observe the growth-inhibitory effect of PC-407 (4-[5-naphthyl-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide), a celecoxib derivative synthesized in our lab, in human colorectal cancer cells and a colitis-associated colorectal cancer (CACC) model, and investigate the relative molecular mechanisms. SW-1116 (expressing a high level of cyclooxygenase-2 [COX-2]), HT-29 (expressing a moderate level of COX-2), and SW-480 (no expression of COX-2) cell lines were exposed to different concentrations of celecoxib (0[ndash]100 [mu]mol/L) or PC-407 (0[ndash]100 [mu]mol/L). Then, COX-2 levels were assessed by reverse transcription-PCR and Western blotting. COX-2 activity was evaluated by measuring prostaglandin E2 concentration using enzyme-linked immunoassay. A mouse model...

Phase II nonrandomized study of the efficacy and safety of COX-2 inhibitor celecoxib on patients with cancer cachexia

Journal of Molecular Medicine — Sat, 03 Oct 2009 06:29:23 +0100

Abstract Chronic inflammation is one of the main features of cancer cachexia. Experimental and clinical studies showed that cyclooxygenase-2 inhibitors, such as celecoxib, may be beneficial in counteracting major symptoms of this devastating syndrome. We carried out a prospective phase II clinical trial to test the safety and effectiveness of an intervention with the COX-2 inhibitor celecoxib (300 mg/day for 4 months) on key variables of cachexia (lean body mass, resting energy expenditure, serum levels of proinflammatory cytokines, and fatigue) in patients with advanced cancer at different sites. A sample of 24 patients was enrolled from January to December 2008 and all were deemed assessable. A significant increase of lean body mass and a significant decrease o...

The effects of celecoxib, a COX-2 selective inhibitor, on acute inflammation induced in irradiated rats

Inflammopharmacology — Thu, 01 Oct 2009 18:22:43 +0100

Abstract The potential value of selective and non-selective COX-2 inhibitors in preventing some of the biochemical changes induced by ionizing radiation was studied in rats exposed to carrageenan-induced paw edema and 6-day-old air pouch models. The animals were exposed to different exposure levels of γ-radiation, namely either to single doses of 2 and 7.5 Gy or a fractionated dose level of 7.5 Gy delivered as 0.5 Gy twice weekly for 7.5 weeks. The inflammatory response produced by carrageenan in irradiated rats was markedly higher than that induced in non-irradiated animals, and depended on the extent of irradiation. Celecoxib, a selective COX-2 inhibitor, in doses of 3, 5, 10, and 15 mg/kg was effective in reducing paw edema in irradiated and no...