Valdecoxib
Synonym(s):4-(5-Methyl-3-phenyl-4-isoxazolyl)benzenesulfonamide
- CAS NO.:181695-72-7
- Empirical Formula: C16H14N2O3S
- Molecular Weight: 314.36
- MDL number: MFCD00950568
- EINECS: 803-082-3
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-03-19 15:37:51
What is Valdecoxib?
Absorption
Oral bioavailability is 83%.
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.
Description
Valdecoxib is a second-generation COX-2 inhibitor, developed as a follow-up to celecoxib for the oral once-daily treatment of osteoarthritis, adult rheumatoid arthritis and menstrual pain. Valdecoxib is approximately 28,000-fold more selective against human recombinant COX-2 than human recombinant COX-1. In an ex viva human whole blood assay, the I&O values against COX-2 and COX-1 were respectively 0.89 PM and 25.4 FM. In animal models, valdecoxib possesses excellent oral activity as an antiinflammatory. In rats, valdecoxib potently inhibited carrageenan footpad edema and adjuvant-induced arthritis.
The Uses of Valdecoxib
Valdecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties in animal models. It is a potent and selective inhibitor of prostaglandin synthesis primarily through inhibition of COX-2. Valdecoxib is used to relieve some symptoms caused by arthritis (rheumatism), such as inflammation, swelling, stiffness, and joint pain.
Background
Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about a possible increased risk of heart attack and stroke.
Indications
For the treatment of osteoarthritis and dysmenorrhoea
Pharmacokinetics
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.
Metabolism
Hepatic (involves CYP3A4 and 2C9)
Properties of Valdecoxib
Melting point: | 162-164°C |
Boiling point: | 481.2±55.0 °C(Predicted) |
Density | 1.303±0.06 g/cm3(Predicted) |
storage temp. | room temp |
solubility | DMSO: >25mg/mL |
form | powder |
color | white to off-white |
Safety information for Valdecoxib
Signal word | Warning |
Pictogram(s) |
Health Hazard GHS08 Environment GHS09 |
GHS Hazard Statements |
H373:Specific target organ toxicity, repeated exposure H410:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P201:Obtain special instructions before use. P202:Do not handle until all safety precautions have been read and understood. P260:Do not breathe dust/fume/gas/mist/vapours/spray. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P308+P313:IF exposed or concerned: Get medical advice/attention. |
Computed Descriptors for Valdecoxib
InChIKey | LNPDTQAFDNKSHK-UHFFFAOYSA-N |
SMILES | C1(S(N)(=O)=O)=CC=C(C2=C(C)ON=C2C2=CC=CC=C2)C=C1 |
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