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Celecoxib
drug data and news
Celecoxib drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Celecoxib | ||
| Brand Names/Synonyms | Celebra; Celebrex; Celecoxib; Celocoxib; HSDB 7038; YM 177 | ||
| 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 | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Celecoxib News (When available) |
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| Dosage Forms | CELEBREX oral capsules contain 100 mg and 200 mg of celecoxib. | ||
| Drug_Category | Cyclooxygenase Inhibitors; Anti-inflammatory Agents; Nonsteroidal Antiinflammatory Agents (NSAIDs); ATC:L01XX33; ATC:M01AH01 | ||
| 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. | ||
| Toxicity | severe rash, itching, or hivesswelling in the face, lips, mouth, or throat,severe or steady stomach pain, blood in the stool, urine, or vomit,swollen, puffy hands or feet, yellowing of skin or eyes,?continued vomiting, fever, chills signs of allergic reaction: rash or hives, wheezing, trouble breathing | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide | ||
| Chemical Formula | C17H14F3N3O2S | ||
| Molecular Weight | 381.373 g/mol | ||
| Smiles String | CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F | ||
| Melting Point | 157- 158 C | ||
| Water Solubility | very low water solubility | ||
| State | solid | ||
| LogP/Hphobicity | 4.157 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | hepatic | ||
| Half Life | ~11 hours | ||
| Protein Binding [%] | 97% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Celecoxib.html http://www.rxlist.com/cgi/generic/coxib.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00373 | ||
| CAS Registry Number | 169590-42-5 | ||
| KEGG Compound ID | C07589 | ||
| PubChem ID | SID:205043 | ||
| PharmGKB ID | PA448871 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2239941 |
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