No abstract available.
Pyrazoles ; Sulfonamides ; Celecoxib

OBJECTIVE: The aim of this study was to define the efficacy and safety of celecoxib in Korean patients with rheumatoid arthritis and osteoarthritis. In addition, the impact of gastrointestinal symptom severity on health related quality of life (HRQoL) was measured before and after the treatment with celecoxib. METHODS: Three hundred seventy nine patients with rheumatoid arthritis (n=175) and osteoarthritis (n=204) were enrolled from 25 centers from May 2004 to December 2004. After treatment of celecoxib for 4 weeks, efficacy was determined by physician's global assessment and EQ-5D. Severity of gastrointestinal (GI) symptom was assessed by visual analogue scale. RESULTS: Treatment made improvement in 263 patients (69.4%), but 108 patients (28.5%) didn't show change in their symptom and 8 patients (2.1%) were aggravated after treatment. Mean change was 0.129+/-0.3 in EQ-5D utility score (p<0.05), 11.8+/-17.8 in VAS in EQ-5D (p<0.05) and -7.9+/-19.6 in GI symptom severity (p<0.05). Blood pressure was not elevated after treatment and there was no cardiovascular adverse event. Gastrointestinal symptom improvement correlates with improvement in VAS (r=0.2, p<0.01). CONCLUSION: Celecoxib is not only effective in patients with rheumatoid arthritis and osteoarthritis but also helpful in reducing GI symptom.
Arthritis, Rheumatoid* ; Blood Pressure ; Humans ; Osteoarthritis* ; Quality of Life ; Celecoxib

Acute generalized exanthematous pustulosis (AGEP) is manifested by rapid development of many sterile, nonfollicular pustules on a background of edematous erythema. More than 90 percent of AGEP are induced by medication, mostly antibiotics. Drug patch test can be helpful in the diagnosis of AGEP. This paper reports the first case of celecoxib-induced AGEP confirmed by patch test in Korean literature.
Acute Generalized Exanthematous Pustulosis ; Anti-Bacterial Agents ; Erythema ; Patch Tests ; Pyrazoles ; Sulfonamides ; Celecoxib

Cyclooxygenase-2 (Cox-2) is known as one of the critical factor in carcinomas of various organs. However, the importance of Cox-2 in oral squamous cell carcinoma has not been fully described yet. The purpose of this study is to evaluate the anti-cancer effect of selective cox-2 inhibitor, celecoxib in an oral squamous cell carcinoma cell line, KB with respect to cytotoxicity test, in vitro invasion and MMP-2 expression. In cytotoxicity test, celecoxib treated group showed definitely concentration dependent cytotoxicity. In addition, administration of celecoxib reduced the invasive potential of KB cell line significantly in invasion assay. However, there was no remarkable difference of the MMP-2 expression between the celecoxib treated group and the control group. Considering these data, celecoxib had a potential cytotoxic agent to oral squamous cell carcinoma cells. Also, it had anti-invasive property without acting on the MMP-2 expression mechanism. Therefore, it was postulated that celecoxib had the possibility of anti-cancer agent in treatment strategies of oral squamous cell carcinoma.
Carcinoma, Squamous Cell* ; Cell Line* ; Cyclooxygenase 2 ; Humans ; Celecoxib ; KB Cells

OBJECTIVETo establish a high-performance liquid chromatography (HPLC)-based method for determining celecoxib concentration in the tongue tissue of hamsters.

METHODSCelecoxib mixed with the matrix (final concentration of 6%) was smeared on the surface of the tongue mucosa of hamsters, and the concentration and absorption rate of celecoxib in the tongue tissue were determined by HPLC at 5, 10, 15, 30, 60, 90, 120 min after the application.

RESULTSIn this system, the retention time of celecoxib was 4.4 min. Celecoxib concentration showed a good linear range within 25-800 microg/L (R2=0.9991, n=6), with the detection limit for celecoxib of 10 g/L (S/N=3). The extraction recoveries and method recoveries for celecoxib were 83.75%-90.01% and 91.98%-99.07%, respectively. The inter-day RSDs were 2.15%, 3.16% and 3.67%, and intra-day RSDs were 3.40%, 4.56% and 4.42%, respectively. The concentration of celecoxib in hamster tongue tissue within the first 120 min ranged from 0.685-/+0.019 microg/g to 3.168-/+0.143 g/g, reaching the peak level at 15 min.

CONCLUSIONCelecoxib can be rapidly absorbed through the tongue mucosa to reach a high concentration in the tongue tissue, indicating the possibility of oral COX-2 inhibitors to prevent oral cancer and precancerous lesions.

Animals ; Celecoxib ; Chromatography, High Pressure Liquid ; methods ; Cricetinae ; Pyrazoles ; analysis ; pharmacokinetics ; Sulfonamides ; analysis ; pharmacokinetics ; Tongue ; metabolism

BACKGROUND: The aim of this study was to evaluate the safety and analgesic efficacy of polmacoxib 2 mg versus placebo in a superiority comparison or versus celecoxib 200 mg in a noninferiority comparison in patients with osteoarthritis (OA). METHODS: This study was a 6-week, phase III, randomized, double-blind, and parallel-group trial followed by an 18-week, single arm, open-label extension. Of the 441 patients with knee or hip OA screened, 362 were randomized; 324 completed 6 weeks of treatment and 220 completed the extension. Patients were randomized to receive oral polmacoxib 2 mg (n = 146), celecoxib 200 mg (n = 145), or placebo (n = 71) once daily for 6 weeks. During the extension, all participants received open-label polmacoxib 2 mg. The primary endpoint was the change in Western Ontario and McMaster Universities (WOMAC)-pain subscale score from baseline to week 6. Secondary endpoints included WOMAC-OA Index, OA subscales (pain, stiffness, and physical function) and Physician's and Subject's Global Assessments at weeks 3 and 6. Other outcome measures included adverse events (AEs), laboratory tests, vital signs, electrocardiograms, and physical examinations. RESULTS: After 6 weeks, the polmacoxib-placebo treatment difference was −2.5 (95% confidence interval [CI], −4.4 to −0.6; p = 0.011) and the polmacoxib-celecoxib treatment difference was 0.6 (CI, −0.9 to 2.2; p = 0.425). According to Physician's Global Assessments, more subjects were “much improved” at week 3 with polmacoxib than with celecoxib or placebo. Gastrointestinal and general disorder AEs occurred with a greater frequency with polmacoxib or celecoxib than with placebo. CONCLUSIONS: Polmacoxib 2 mg was relatively well tolerated and demonstrated efficacy superior to placebo and noninferior to celecoxib after 6 weeks of treatment in patients with OA. The results obtained during the 18-week trial extension with polmacoxib 2 mg were consistent with those observed during the 6-week treatment period, indicating that polmacoxib can be considered safe for long-term use based on this relatively small scale of study in a Korean population. More importantly, the results of this study showed that polmacoxib has the potential to be used as a pain relief drug with reduced gastrointestinal side effects compared to traditional nonsteroidal anti-inflammatory drugs for OA.
Arm ; Celecoxib* ; Electrocardiography ; Hip ; Humans ; Knee ; Ontario ; Osteoarthritis* ; Outcome Assessment (Health Care) ; Physical Examination ; Vital Signs

OBJECTIVE: To estimate the cardiovascular (CV) and gastrointestinal (GI) risks of etoricoxib in the treatment of osteoarthritis (OA) compared to a placebo and other non-steroidal anti-inflammatory drugs (NSAIDs). METHODS: A systematic review of randomized, controlled trials (RCTs) of etoricoxib were performed. Bayesian network meta-analysis was used over a duration of 12 weeks. The incidence of CV and GI events for a duration ≥26 weeks were also tabulated and presented using descriptive statistics. RESULTS: From this search, 10 studies were identified. Of these, 6 and 5 RCTs that measured the CV and GI events at 12 weeks were included in meta-analysis. They showed that etoricoxib did not increase the CV events compared to the placebo or NSAIDs during the 12 week period (odds ratio [OR]=0.59 compared to celecoxib, OR=0.89 with ibuprofen, OR=0.70 with placebo, and OR=2.16 with naproxen). The risk of GI events was comparable to that of most comparators, with the exception of naproxen, which had a significantly lower risk of GI events (OR=0.18) during the 12 week period. For a duration ≥26 weeks, the incidence of CV and GI events with etoricoxib increased with increasing duration. CONCLUSION: Etoricoxib is an alternative short-term treatment option for OA, showing comparable CV and GI complications to other NSAIDs. Nevertheless, further studies will be needed to elucidate the long-term safety of etoricoxib in the treatment of OA.
Anti-Inflammatory Agents ; Anti-Inflammatory Agents, Non-Steroidal ; Celecoxib ; Ibuprofen ; Incidence ; Naproxen ; Osteoarthritis*

OBJECTIVETo observe whether Celecoxib could inhibit the growth, regulate the expression of COX-2 and induce apoptosis of Tca8113 cells.

METHODSTca8113 cells were incubated with different concentrations of Celecoxib for 24, 48 and 72 h, and MTT was used to calculate growth inhibition rate. The expression of COX-2 protein and mRNA in Tca8113 cells was detected with SP immunohistochemistry staining and fluorescent quantitative real-time RT-PCR. Morphology of apoptosis cells was observed by fluorescence microscopy, and Annexin V-FITC/PI double labeling method was employed to detect early stage cell apoptosis.

RESULTSCOX-2 protein was strongly expressed in Tca8113 cells and was suppressed by Celecoxib. The growth and proliferation of Tca8113 cells treated with Celecoxib were inhibited in a dose-dependent manner. Celecoxib treatment resulted in significant increase in apoptosis and early apoptotic rate. Fluorescent quantitative real-time RT-PCR results showed no significant effet on regulating expression of COX-2 mRNA.

CONCLUSIONCelecoxib shows a significant effect on inhibiting expression of COX-2 in Tca8113 cells, this is probably related to growth inhibition and inducing apoptosis of Tca8113 cells.

Apoptosis ; Celecoxib ; Cell Line ; Cell Line, Tumor ; Cell Proliferation ; Cyclooxygenase 2 ; Humans ; Pyrazoles ; Sulfonamides

Familial adenomatous polyposis(FAP) is an autosomal dominant disease characterized by numerous adenomas in the colorectum. Patients with FAP are always at risk of malignant transformation, so that colectomy is unavoidable. NSAID, such as sulindac, and selective COX-2 inhibitor, such as celecoxib, have shown a positive effect on FAP by causing polyp regression in some patients. We report a case of FAP in a 9-year-old female whose polyposis regressed markedly after six months-treatment with celecoxib.
Adenoma ; Adenomatous Polyposis Coli* ; Child* ; Colectomy ; Female ; Humans ; Polyps ; Sulindac ; Celecoxib

PURPOSE: To investigate the modulation of radiosensitivity by celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, on cancer cells over- and under-expressing COX-2. MATERIALS AND METHODS: A clonogenic radiation survival analysis was performed on A549 human lung and MCF-7 human breast cancer cell lines incubated in both 1 and 10% fetal bovine serum (FBS) containing media. The apoptosis in both cell lines was measured after treatment with radiation and/or celecoxib. RESULTS: Celecoxib enhanced the radiation sensitivity of the A549 cells in the medium containing the 10% FBS, with radiation enhancement ratios of 1.58 and 1.81 respectively, at surviving fractions of 0.1, with 30 microM and 50 microM celecoxib. This enhanced radiosensitivity disappeared in the medium containing the 1% FBS. Celecoxib did not change the radiation sensitivity of the MCF-7 cells in either media. The induction of apoptosis by celecoxib and radiation was not synergistic in either cell line. CONCLUSION: Celecoxib, a selective COX-2 inhibitor, preferentially enhanced the effect of radiation on COX-2 over-expressing cancer cells compared to the cells with a low expression, and this effect disappeared on incubation of the cells during drug treatment in the medium with suboptimal serum concentration. Apoptosis did not appear to be the underlying mechanism of this radiation enhancement effect due to celecoxib on the A549 cells. These findings suggest radiosensitization by a selective COX-2 inhibitor is COX-2 dependent.
Apoptosis ; Breast Neoplasms ; Cell Line ; Cyclooxygenase 2* ; Humans* ; Lung ; MCF-7 Cells ; Radiation Tolerance* ; Celecoxib