Detail

Valdecoxib

Description

Name: Valdecoxib
Type: small molecule
Groups: Array
Indication: For the treatment of osteoarthritis and dysmenorrhoea
Accession Number: DB00580 ( APRD00183, DB07576)
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.
Structure:
Prescription Products: Not Available
Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients

Categories
  • Anti-Inflammatory Agents, Non-Steroidal

Pharmacology

Indication: For the treatment of osteoarthritis and dysmenorrhoea
Pharmacodynamics: Not Available
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.
Absorption: Oral bioavailability is 83%.
Volume of distribution:
  • 86 L

Protein binding: 98%
Metabolism: Not Available
Route of elimination: Valdecoxib is eliminated predominantly via hepatic metabolism with less than 5% of the dose excreted unchanged in the urine and feces. About 70% of the dose is excreted in the urine as metabolites, and about 20% as valdecoxib N-glucuronide.
Half life: 8-11 hours
Clearance: Not Available
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.
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Gd searle llc

Packagers:
Dosage forms
FormRouteStrength

Prices
Unit descriptionCostUnit

Patents
CountryPatent NumberApprovedExpires (estimated)
2212836Canada2003-08-122016-02-12
5633272United States1995-02-132015-02-13
7135489United States1997-08-122017-08-12

Interactions

Drug Interactions
DrugInteraction

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Aminosulfonyl compounds
  • Azacyclic compounds
  • Heteroaromatic compounds
  • Hydrocarbon derivatives
  • Isoxazoles
  • Organonitrogen compounds
  • Organooxygen compounds
  • Oxacyclic compounds
  • Oxazoles
  • Sulfonamides

substituent:
  • Aminosulfonyl compound
  • Aromatic heteromonocyclic compound
  • Azacycle
  • Azole
  • Benzenesulfonamide
  • Heteroaromatic compound
  • Hydrocarbon derivative
  • Isoxazole
  • Organoheterocyclic compound
  • Organonitrogen compound
  • Organooxygen compound
  • Organosulfur compound
  • Oxacycle
  • Oxazole
  • Sulfonamide
  • Sulfonic acid derivative
  • Sulfonyl

References

Synthesis Reference: Eswaraiah Sajja, Anumula Reddy, Aalla Sampath, Gilla Goverdhan, "Process for preparing crystalline form A of valdecoxib." U.S. Patent US20050272787, issued December 08, 2005.
General Reference: Not Available
External Links:
ResourceLink
RxListhttp://www.rxlist.com/cgi/generic/bextra.htm
Drugs.comhttp://www.drugs.com/mtm/valdecoxib.html

ATC Codes:
  • Array

AHFS Codes:
  • Not Available

MSDS: Download
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