- Overview
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Overview
| Generic Names: | valdecoxib |
|---|---|
| Trade Names: | Bextra |
| PharmGKB Accession Id: | PA10226 |
Description
Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke. (source: Drug Bank)
Indication
For the treatment of osteoarthritis and dysmenorrhoea (source: Drug Bank)
ATC Therapeutic Category
- M01AH:Coxibs
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does not inhibit platelet aggregation. (source: Drug Bank)
Pharmacology
Valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib is used for its anti-inflammatory, analgesic, and antipyretic activities in the management of osteoarthritis (OA) and for the treatment of dysmenorrhea or acute pain. Unlike celecoxib, valdecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (involves CYP3A4 and 2C9) (source: Drug Bank)
Protein Binding
98% (source: Drug Bank)
Absorption
Oral bioavailability is 83%. (source: Drug Bank)
Toxicity
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare. (source: Drug Bank)
Isomeric SMILES Code:
Cc1c(c(no1)c2ccccc2)c3ccc(cc3)S(=O)(=O)N (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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PTGIR |
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Publications |
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PTGS2 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| PTGS2 |
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(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Cardiovascular Diseases |
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Publications |
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Pain |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
