Celecoxib resources

DRUG INFO
Celecoxib

Drug Name: Celecoxib

Indication: For relief and management of osteoarthritis (OA), rheumatoid arthritis (RA), ankylosing spondylitis, acute pain, primary dysmenorrhea and oral adjunct to usual care for patients with familial adenomatous polyposis

Pharmacology: Celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Celecoxib is used to treat rheumatoid arthritis, osteoarthritis, and familial adenomatous polyposis (FAP). It is not known if there are any effects of Celecoxib on platelets.

Mechanism Of Action: The mechanism of action of Celecoxib is believed to be due to inhibition of prostaglandin synthesis. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), Celecoxib is a noncompetitive inhibitor of cyclooxygenase-2 (COX-2) enzyme. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region close to the active COX-2 binding site. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane.

Drug Category: Cyclooxygenase Inhibitors; Anti-inflammatory Agents; Nonsteroidal Antiinflammatory Agents (NSAIDs); ATC:L01XX33; ATC:M01AH01

Brand Names/Synonyms: Celebra; Celebrex; Celecoxib; Celocoxib; HSDB 7038; YM 177

Dosage Forms: CELEBREX oral capsules contain 100 mg and 200 mg of celecoxib.

Absorption: When CELEBREX capsules were taken with a high fat meal, peak plasma levels were delayed for about 1 to 2 hours with an increase in total absorption (AUC) of 10% to 20%. Coadministration of CELEBREX with an aluminum-and magnesium-containing antacid resulted in a reduction in plasma celecoxib concentrations with a decrease of 37% in Cmax and 10% in A.C. CELEBREX capsules can be administered without regard to the timing of meals.

Interactions: General: Significant interactions may occur when celecoxib is administered together with drugs that inhibit P450 2C9. Celecoxib metabolism is predominantly mediated via cytochrome P450 2C9 in the liver. Co-administration of celecoxib with drugs that are known to inhibit 2C9 should be done with caution. In vitro studies indicate that celecoxib is not an inhibitor of cytochrome P450 2C9, 2C19 or 3A4. In vitro studies also indicate that celecoxib, although not a substrate, is an inhibitor of cytochrome P450 2D6. Therefore, there is a potential for an in vivo drug interaction with drugs that are metabolized by P450 2D6. Clinical studies with celecoxib have identified potentially significant interactions with fluconazole and lithium. Experience with nonsteroidal anti-inflammatory drugs (NSAIDs) suggests the potential for interactions with furosemide and ACE inhibitors. The effects celecoxib on the pharmacokinetics and/or pharmacodynamics of glyburide, ketoconazole, methotrexate, phenytoin, tolbutamide, and warfarin have been studied in vivo and clinically important interactions have not been found. ACE inhibitors: Reports suggest that NSAIDs may diminish the antihypertensive effect of Angiotensin Converting Enzyme (ACE) inhibitors. This interaction should be given consideration in patients taking CELEBREX concomitantly with ACE-inhibitors. Furosemide: Clinical studies, as well as post marketing observations, have shown that NSAIDs can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. Aspirin: CELEBREX can be used with low dose aspirin. However, concomitant administration of aspirin with CELEBREX may result in an increased rate of GI ulceration or other complications, compared to use of CELEBREX alone. Because of its lack of platelet effects, CELEBREX is not a substitute for aspirin for cardiovascular prophylaxis. Fluconazole: Concomitant administration of fluconazole at 200 mg QD resulted in a two-fold increase in celecoxib plasma concentration. This increase is due to the inhibition of celecoxib metabolism via P450 2C9 by fluconazole (see CLINICAL PHARMACOLOGY - Pharmacokinetics: Metabolism). CELEBREX should be introduced at the lowest recommended dose in patients receiving fluconazole. Lithium: In a study conducted in healthy subjects, mean steady-state lithium plasma levels increased approximately 17% in subjects receiving lithium 450 mg BID with CELEBREX 200 mg BID as compared to subjects receiving lithium alone. Patients on lithium treatment should be closely monitored when CELEBREX is introduced or withdrawn. Methotrexate: In an interaction study of rheumatoid arthritis patients taking methotrexate, CELEBREX did not have a significant effect on the pharmacokinetics of methotrexate. Warfarin: The effect of celecoxib on the anti-coagulant effect of warfarin was studied in a group of healthy subjects receiving daily doses of 2-5 mg of warfarin. In these subjects, celecoxib did not alter the anticoagulant effect of warfarin as determined by prothrombin time. However, caution should be used when administering CELEBREX with warfarin since these patients are at increased risk of bleeding complications.

Chemical IUPAC Name: 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide

Chemical Formula: C17H14F3N3O2S

Half Life: ~11 hours

Drug Type: Approved Drug

# Accession No: APRD00373

CAS Registry Number: 169590-42-5

Celecoxib News
(When available)

Pain Killers Help Bowel Disease Feb 7, 2006
Patients were treated with either celecoxib (Celebrex) or a placebo for two weeks. They were observed for disease exacerbation. ... - Ivanhoe,

Regular use of COX-2 inhibitors reduces breast cancer risk Feb 2, 2006
...control study published today in the open access journal BMC Cancer observed that daily use of selective COX-2 inhibitors, including celecoxib (Celebrex) and ... - News-Medical.net,

Women sought in cancer study Jan 13, 2006
A national study sponsored by the National Cancer Institute aims to find out if the mechanism that allows celecoxib, or Celebrex, to ease pain by stopping ... - Cincinnati Enquirer,

COX-2 inhibitors reduce breast cancer risk Jan 30, 2006
A new study has found that daily use of selective COX-2 inhibitors, such as celecoxib (Celebrex) and rofecoxib (Vioxx), reduces the risk of breast cancer by up ... - Newindpress,

COX-2 inhibitors Lessen Breast Cancer Risk Jan 30, 2006
Selective usage of COX-2 inhibitors like rofecoxib (Vioxx) and celecoxib (Celebrex) reduces breast cancer risk by 71%, according to a study. ... - MedIndia,

Some NSAIDS Safe in Ulcerative Colitis or Crohn's -- Sometimes Feb 3, 2006
...study, researchers at the Mayo Clinic here showed that patients whose inflammatory bowel disease (IBD) is in remission can use Celebrex (celecoxib) safely for ... - MedPage Today,

Intensifying research to fight diseases Feb 3, 2006
Other products also available are olmesartan (Olmetec) for high blood pressure, celecoxib capsules (Celebrex 400) for acute pain and atorvastatin calcium ... - INQ7.net,

A COX-2 comeback? Feb 2, 2006
...understand more about the nature of cancer, we have more options and opportunities to develop new drugs or use old ones - such as with celecoxib and rofecoxib ... - myDNA.com,

Regular Use Of Selective COX-2 Inhibitors Decreases Risk Of Breast ... Jan 30, 2006
Celecoxib Shows Surprising Activity Against Estrogen Receptors (December 23, 2004) -- Six months of treatment with celecoxib (Celebrex) in women at risk of ... - Science Daily (press release)

Drug's impact on cervical cancer studied Jan 11, 2006
...cancer. A Phase 2 trial will test the effectiveness of celecoxib (Celebrex) in stopping the disease in its precancerous stage. The ... - Cincinnati Business Courier,

Some dangerous drugs get by FDA Jan 29, 2006
Consumer Reports' dirty dozen are: celecoxib (Celebrex), estrogen (when taken alone), isotretinoin (Accutane), malathion (Ovide), medroxyprogesterone ... - Sarasota Herald-Tribune,

Aspirin linked to breast cancer reduction Jan 29, 2006
COX-2 inhibitors are used to treat pain and inflammation and scientists in the US have discovered that daily use of the drugs, such as celecoxib (Celebrex) and ... - DeHavilland,

Painkillers can stave off breast cancer Jan 30, 2006
The controversial class of analgesics known as selective COX-2 inhibitors, including Celebrex (celecoxib) and Vioxx (rofecoxib), produced a 71 per cent ... - Scenta.co.uk,

NSAIDs Somewhat Better Than Tylenol for Osteoarthritis, Review ... Jan 24, 2006
The studies under review also included two drugs from the relatively new class of NSAIDs known as Cox-2 inhibitors, celecoxib (sold as Celebrex) and rofecoxib ... - Health Behavior News Service

COX-2 Inhibitors Decrease Breast Cancer Risk Jan 29, 2006
Researchers found the daily use of the selective COX-2 inhibitor celecoxib (Celebrex) is associated with an 83-percent reduction in the risk of breast cancer. ... - Ivanhoe,

Ibuprofen, diclofenac are equally effective Jan 29, 2006
...strokes. For that reason, all but one COX-2 inhibitor – celecoxib, known as Celebrex – has been withdrawn from the market. And ... - Fort Wayne Journal Gazette,

Better Fix for Rheumatoid Arthritis Feb 1, 2006
...pain. These are medications such as aspirin, ibuprofen, indomethacin and COX-2 inhibitors such as valdecoxib and celecoxib. Analgesic ... - ABC7Chicago.com,

Controversial painkillers could slash cancer risk Jan 29, 2006
...used to fight pain and reduce inflammation, includes the controversial selective COX-2 inhibitors, such as Vioxx (rofecoxib) and Celebrex (celecoxib), made by ... - New Scientist (subscription),

Novartis: Prexige launches in the UK Jan 20, 2006
Novartis recently published efficacy data showing that Prexige is comparable to celecoxib (Pfizer's Celebrex) over one year in OA patients, to naproxen in pain ... - Pharmaceutical Business Review

Lancet study faked Jan 16, 2006
Institute. One co-author has consulted for Pfizer, maker of celecoxib (Celebrex); no other conflicts of interest were declared. - Scientist,

The ALS Association Awards TREAT ALS Funding to Three Clinical ... Jan 16, 2006
120 patients. Celecoxib and minocycline will each be tested in combination with creatine, in separate groups of ALS patients. If ... - Genetic Engineering News,

Better Fix for Rheumatoid Arthritis Jan 19, 2006
These are medications such as aspirin, ibuprofen, indomethacin and COX-2 inhibitors such as valdecoxib (BEXTRA) and celecoxib (Celebrex). ... - News 14 Carolina,

Beximco Pharma begins exporting medicines to Sri Lanka Jan 20, 2006
The four generics of exported drugs are Azithrocin (Azithromycin), Decomit (Beclomethasone dipropionate), Cox B (celecoxib) and Deflux (Domperidone). ... - The New Nation,

Generics bite into Pfizer's 4Q figures Jan 20, 2006
Meanwhile, the withdrawal of COX-2 inhibitor Bextra (valdecoxib) on safety concerns and pressure on related drug Celebrex (celecoxib) continued to weigh heavy ... - Pharma Times (subscription),

Arthritis patients have new hope Jan 19, 2006
These are medications such as aspirin, ibuprofen, indomethacin and COX-2 inhibitors such as valdecoxib (BEXTRA) and celecoxib (Celebrex). ... - News 14 Charlotte, [an error occurred while processing this directive]

Celecoxib resources

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Celecoxib