Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H14N2O3S |
Molecular Weight | 314.359 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(N)(=O)=O
InChI
InChIKey=LNPDTQAFDNKSHK-UHFFFAOYSA-N
InChI=1S/C16H14N2O3S/c1-11-15(12-7-9-14(10-8-12)22(17,19)20)16(18-21-11)13-5-3-2-4-6-13/h2-10H,1H3,(H2,17,19,20)
Molecular Formula | C16H14N2O3S |
Molecular Weight | 314.359 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.drugbank.ca/drugs/DB08439 | http://www.fda.gov/ohrms/dockets/ac/05/briefing/2005-4090B1_28_CC-FDA-Tab-Q.htmhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf | http://www.rotlaw.com/legal-library/bextra-valdecoxib/Curator's Comment: Description was created based on several sources, including https://www.medicines.org.uk/emc/medicine/8771
Sources: https://www.drugbank.ca/drugs/DB08439 | http://www.fda.gov/ohrms/dockets/ac/05/briefing/2005-4090B1_28_CC-FDA-Tab-Q.htmhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf | http://www.rotlaw.com/legal-library/bextra-valdecoxib/
Curator's Comment: Description was created based on several sources, including https://www.medicines.org.uk/emc/medicine/8771
Valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib was manufactured and marketed under the brand name Bextra. Bextra was indicated for relief of the signs and symptoms of osteoarthritis and adult rheumatoid arthritis. For the treatment of primary dysmenorrhea. But in 2005 FDA requested that Pfizer withdraw Bextra from the American market, because the Agency had concluded that the overall risk versus benefit profile of Bextra was unfavorable. That conclusion was based on the potential increased risk for serious cardiovascular (CV) adverse events, an increased risk of serious skin reactions (e.g., toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme) compared to other NSAIDs, and the fact that Bextra had not been shown to offer any unique advantages over the other available NSAIDs.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17687276 | http://www.fda.gov/ohrms/dockets/ac/05/briefing/2005-4090B1_28_CC-FDA-Tab-Q.htmhttps://books.google.ru/books?id=n6PQxWEaXuwC&pg=PA758&lpg=PA758&dq=valdecoxib+cross+blood-brain+barrier&source=bl&ots=6Nfyvw7tlS&sig=4XEOhf5CMVcVUtn1gMzA-MZkJxU&hl=ru&sa=X&ved=0ahUKEwiSptrY-OXSAhVrw4MKHX2_DhsQ6AEISzAF#v=onepage&q=valdecoxib%20cross%20blood-brain%20barrier&f=false
Curator's Comment: Known to be CNS penetrant in rodent. Human data not available
Originator
Sources: http://adisinsight.springer.com/drugs/800009724http://www.rotlaw.com/legal-library/bextra-valdecoxib/
Curator's Comment: # Pfizer
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL230 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15494548 |
0.005 µM [IC50] | ||
5.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | Dynastat Approved UseDynastat is used for the short-term treatment of pain in adults after an operation. Launch Date2002 |
|||
Palliative | BEXTRA Approved UseBEXTRA Tablets are indicated: For relief of the signs and symptoms of osteoarthritis and adult rheumatoid arthritis. For the treatment of primary dysmenorrhea. Launch Date2001 |
|||
Palliative | BEXTRA Approved UseBEXTRA Tablets are indicated: For relief of the signs and symptoms of osteoarthritis and adult rheumatoid arthritis. For the treatment of primary dysmenorrhea. Launch Date2001 |
|||
Primary | BEXTRA Approved UseBEXTRA Tablets are indicated: For relief of the signs and symptoms of osteoarthritis and adult rheumatoid arthritis. For the treatment of primary dysmenorrhea. Launch Date2001 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
39.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
1 mg single, intramuscular dose: 1 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
16.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
1 mg single, intramuscular dose: 1 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
57.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
2 mg single, intramuscular dose: 2 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
26.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
2 mg single, intramuscular dose: 2 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
276 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
5 mg single, intramuscular dose: 5 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
66.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
5 mg single, intramuscular dose: 5 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
437 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
10 mg single, intramuscular dose: 10 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
130 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
10 mg single, intramuscular dose: 10 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1013 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
20 mg single, intramuscular dose: 20 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
263 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
20 mg single, intramuscular dose: 20 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1681 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
40 mg single, intramuscular dose: 40 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
498 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
40 mg single, intramuscular dose: 40 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
146 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
284 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
568 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1385 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16599270/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
161.1 ng/mL |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
16 ng/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
12 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
14 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1 ng/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
0.8 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
26 ng/mL |
5 mg 2 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
24 ng/mL |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
26 ng/mL |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2 ng/mL |
5 mg 2 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2 ng/mL |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2 ng/mL |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
37.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
1 mg single, intramuscular dose: 1 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
127 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
1 mg single, intramuscular dose: 1 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
41.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
2 mg single, intramuscular dose: 2 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
258 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
2 mg single, intramuscular dose: 2 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
130 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
5 mg single, intramuscular dose: 5 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
563 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
5 mg single, intramuscular dose: 5 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
275 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
10 mg single, intramuscular dose: 10 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1133 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
10 mg single, intramuscular dose: 10 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
579 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
20 mg single, intramuscular dose: 20 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2782 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
20 mg single, intramuscular dose: 20 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1167 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
40 mg single, intramuscular dose: 40 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
5215 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
40 mg single, intramuscular dose: 40 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1787 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3450 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6957 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
9062 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16599270/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1479 ng × h/mL |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
198 ng × h/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
167 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
175 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
18 ng × h/mL |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
15 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
19 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
332 ng × h/mL |
5 mg 2 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
341 ng × h/mL |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
371 ng × h/mL |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
31 ng × h/mL |
5 mg 2 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
33 ng × h/mL |
10 mg 2 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
36 ng × h/mL |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
1-HYDROXYVALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.36 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
1 mg single, intramuscular dose: 1 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.83 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
1 mg single, intramuscular dose: 1 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.43 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
2 mg single, intramuscular dose: 2 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.28 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
2 mg single, intramuscular dose: 2 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.25 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
5 mg single, intramuscular dose: 5 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
5.67 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
5 mg single, intramuscular dose: 5 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.41 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
10 mg single, intramuscular dose: 10 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
5.44 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
10 mg single, intramuscular dose: 10 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.48 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
20 mg single, intramuscular dose: 20 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
9.94 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
20 mg single, intramuscular dose: 20 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.87 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
40 mg single, intramuscular dose: 40 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
PARECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
7.35 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583480/ |
40 mg single, intramuscular dose: 40 mg route of administration: Intramuscular experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8.31 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
8.53 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
8.84 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16599270/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VALDECOXIB serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8.11 h |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2% |
PARECOXIB plasma | Homo sapiens |
||
2% |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VALDECOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
80 mg 1 times / day multiple, oral Highest studied dose Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-92 Health Status: unhealthy Age Group: 18-92 Sex: M+F Sources: |
Other AEs: Gastrointestinal ulcer haemorrhage... Other AEs: Gastrointestinal ulcer haemorrhage (significant, 0.48%) Sources: |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, 32.3 ±10.9 Health Status: unhealthy Age Group: 32.3 ±10.9 Sex: M+F Sources: |
Disc. AE: Allergic rash, Dizziness... Other AEs: Dyspepsia, Gastritis... AEs leading to discontinuation/dose reduction: Allergic rash (grade 2, 1%) Other AEs:Dizziness (grade 2, 1%) Dyspepsia (2%) Sources: Gastritis (5.9%) |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Disc. AE: Hypertension, Peripheral edema... AEs leading to discontinuation/dose reduction: Hypertension (1.7%) Sources: Peripheral edema (1.7%) Abdominal pain (2.7%) Duodenal ulcer (0.2%) Dyspepsia (2.2%) Gastric ulcer (1.5%) Nausea (0.5%) Vomiting (0.2%) Rash (1%) |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Gastrointestinal perforation, Gastrointestinal ulcer... Other AEs: Exfoliative dermatitis... AEs leading to discontinuation/dose reduction: Gastrointestinal perforation (grade 3-5) Other AEs:Gastrointestinal ulcer (grade 3-5) Gastrointestinal bleeding (grade 3-5) Exfoliative dermatitis Sources: |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Toxic epidermal necrolysis, Stevens-Johnson syndrome... AEs leading to discontinuation/dose reduction: Toxic epidermal necrolysis (grade 3-5) Sources: Stevens-Johnson syndrome (grade 3-5) |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Erythema multiforme... Other AEs: Erythema multiforme (grade 3-5) Sources: |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Other AEs: Anaphylactic reaction, Angioedema... Other AEs: Anaphylactic reaction Sources: Angioedema |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Disc. AE: Peripheral edema, Halitosis... AEs leading to discontinuation/dose reduction: Peripheral edema (2.2%) Sources: Halitosis (0.3%) Abdominal pain (5.5%) Dyspepsia (6.2%) Gastroenteritis (1.2%) |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Disc. AE: Abdominal pain, Diarrhea... AEs leading to discontinuation/dose reduction: Abdominal pain (1.6%) Sources: Diarrhea (0.7%) Dyspepsia (1.4%) Nausea (0.9%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Gastrointestinal ulcer haemorrhage | significant, 0.48% | 80 mg 1 times / day multiple, oral Highest studied dose Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-92 Health Status: unhealthy Age Group: 18-92 Sex: M+F Sources: |
Dyspepsia | 2% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, 32.3 ±10.9 Health Status: unhealthy Age Group: 32.3 ±10.9 Sex: M+F Sources: |
Gastritis | 5.9% | 40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, 32.3 ±10.9 Health Status: unhealthy Age Group: 32.3 ±10.9 Sex: M+F Sources: |
Allergic rash | grade 2, 1% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, 32.3 ±10.9 Health Status: unhealthy Age Group: 32.3 ±10.9 Sex: M+F Sources: |
Dizziness | grade 2, 1% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, 32.3 ±10.9 Health Status: unhealthy Age Group: 32.3 ±10.9 Sex: M+F Sources: |
Duodenal ulcer | 0.2% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Vomiting | 0.2% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Nausea | 0.5% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Rash | 1% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Gastric ulcer | 1.5% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Hypertension | 1.7% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Peripheral edema | 1.7% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Dyspepsia | 2.2% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Abdominal pain | 2.7% Disc. AE |
40 mg 2 times / day multiple, oral Highest studied dose Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Exfoliative dermatitis | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Gastrointestinal bleeding | grade 3-5 Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Gastrointestinal perforation | grade 3-5 Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Gastrointestinal ulcer | grade 3-5 Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Stevens-Johnson syndrome | grade 3-5 Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Toxic epidermal necrolysis | grade 3-5 Disc. AE |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Erythema multiforme | grade 3-5 | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Anaphylactic reaction | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Angioedema | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
|
Halitosis | 0.3% Disc. AE |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Gastroenteritis | 1.2% Disc. AE |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Peripheral edema | 2.2% Disc. AE |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Abdominal pain | 5.5% Disc. AE |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Dyspepsia | 6.2% Disc. AE |
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Diarrhea | 0.7% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Nausea | 0.9% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Dyspepsia | 1.4% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Abdominal pain | 1.6% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
PubMed
Title | Date | PubMed |
---|---|---|
Parecoxib (parecoxib sodium). | 2001 |
|
A double-blind, randomized comparison of intramuscularly and intravenously administered parecoxib sodium versus ketorolac and placebo in a post-oral surgery pain model. | 2001 Jul |
|
A pharmacokinetic study of intramuscular (i.m.) parecoxib sodium in normal subjects. | 2001 Oct |
|
Upper gastrointestinal safety evaluation of parecoxib sodium, a new parenteral cyclooxygenase-2-specific inhibitor, compared with ketorolac, naproxen, and placebo. | 2001 Sep |
|
The injectable cyclooxygenase-2-specific inhibitor parecoxib sodium has analgesic efficacy when administered preoperatively. | 2001 Sep |
|
Cox-2 inhibitors: today and tomorrow. | 2002 Apr |
|
Effects of parecoxib, a parenteral COX-2-specific inhibitor, on the pharmacokinetics and pharmacodynamics of propofol. | 2002 Jan |
|
[Clinical pharmacology of the selective COX-2 inhibitors]. | 2003 Dec |
|
The role of cyclooxygenase selective inhibitors in the gastrointestinal tract. | 2003 Dec |
|
Efficacy and safety of the first parenteral selective COX-2 inhibitor, parecoxib sodium, in adult patients with postoperative pain. | 2003 Jul |
|
Differential inhibition of fracture healing by non-selective and cyclooxygenase-2 selective non-steroidal anti-inflammatory drugs. | 2003 Jul |
|
Meloxicam and selective COX-2 inhibitors in the management of pain in the palliative care population. | 2003 Jul-Aug |
|
Efficacy and safety of the cyclooxygenase 2 inhibitors parecoxib and valdecoxib in patients undergoing coronary artery bypass surgery. | 2003 Jun |
|
Clinical pharmacology of selective COX-2 inhibitors. | 2003 May-Aug |
|
Stability of reconstituted parecoxib for injection with commonly used diluents. | 2003 Oct |
|
Effects of rofecoxib, celecoxib, and parecoxib on anti-IgE-induced histamine release from human skin mast cells and basophils. | 2003 Oct |
|
Single doses of parecoxib sodium intravenously are as effective as ketorolac in reducing pain after oral surgery. | 2003 Sep |
|
Selective cyclo-oxygenase-2 inhibition with parecoxib acutely impairs endothelium-dependent vasodilatation in patients with essential hypertension. | 2003 Sep |
|
Effect of selective inhibition of cyclooxygenase-2 on lipopolysaccharide-induced hyperalgesia. | 2004 |
|
Clinical pharmacology of novel selective COX-2 inhibitors. | 2004 |
|
Pharmacological profile of parecoxib: a novel, potent injectable selective cyclooxygenase-2 inhibitor. | 2004 Apr 26 |
|
First and second generations of COX-2 selective inhibitors. | 2004 Aug |
|
[Review of analgesics]. | 2004 Dec |
|
Reporting of clinical trials of analgesia. | 2004 Feb |
|
Effective treatment of laparoscopic cholecystectomy pain with intravenous followed by oral COX-2 specific inhibitor. | 2004 Feb |
|
S-adenosyl methionine (SAMe) versus celecoxib for the treatment of osteoarthritis symptoms: a double-blind cross-over trial. [ISRCTN36233495]. | 2004 Feb 26 |
|
Gastrointestinal side-effects of traditional non-steroidal anti-inflammatory drugs and new formulations. | 2004 Jul |
|
Early analgesic effects of parecoxib versus ketorolac following laparoscopic sterilization: a randomized controlled trial. | 2004 Jun |
|
Parecoxib: a shift in pain management? | 2004 Mar |
|
The cyclooxygenase isozyme inhibitors parecoxib and paracetamol reduce central hyperalgesia in humans. | 2004 Mar |
|
Collision-induced dissociation of valdecoxib metabolites: a novel rearrangement involving an isoxazole ring. | 2004 Mar |
|
Parecoxib sodium, an injectable COX-2-specific inhibitor, does not affect unfractionated heparin-regulated blood coagulation parameters. | 2004 May |
|
A systematic review of COX-2 inhibitors compared with traditional NSAIDs, or different COX-2 inhibitors for post-operative pain. | 2004 May |
|
Differential inhibition of fracture healing by non-selective and cyclooxygenase-2 selective non-steroidal anti-inflammatory drugs. | 2004 May |
|
Parecoxib for parenteral analgesia in postsurgical patients. | 2004 May |
|
Valdecoxib versus rofecoxib in acute postsurgical pain: results of a randomized controlled trial. | 2004 May |
|
Cyclooxygenases: new forms, new inhibitors, and lessons from the clinic. | 2004 May |
|
A clinical trial demonstrates the analgesic activity of intravenous parecoxib sodium compared with ketorolac or morphine after gynecologic surgery with laparotomy. | 2004 Oct |
|
Presurgical intravenous parecoxib sodium and follow-up oral valdecoxib for pain management after laparoscopic cholecystectomy surgery reduces opioid requirements and opioid-related adverse effects. | 2004 Oct |
|
Parecoxib impairs early tendon repair but improves later remodeling. | 2004 Oct-Nov |
|
[Use of low molecular weight heparin (Clexane) together with selective COX-2 inhibitor (Dynastat--once or twice per day)]. | 2005 |
|
Parecoxib: renal failure. | 2005 Apr |
|
Cyclooxygenase-2 plays a central role in the genesis of pancreatitis and associated lung injury. | 2005 Feb |
|
Reduction of opioid-related adverse events using opioid-sparing analgesia with COX-2 inhibitors lacks documentation: a systematic review. | 2005 Feb |
|
COX-2 inhibitors--a lesson in unexpected problems. | 2005 Mar 17 |
|
COX-2 inhibitors--lessons in drug safety. | 2005 Mar 17 |
|
Complications of the COX-2 inhibitors parecoxib and valdecoxib after cardiac surgery. | 2005 Mar 17 |
|
The cardioprotective effects of preconditioning with endotoxin, but not ischemia, are abolished by a peroxisome proliferator-activated receptor-gamma antagonist. | 2005 May |
|
Increased risk of cardiovascular events with parecoxib/valdecoxib: a systematic review and meta-analysis. | 2005 Nov 25 |
|
Single dose parecoxib significantly improves ventilatory function in early extubation coronary artery bypass surgery: a prospective randomized double blind placebo controlled trial. | 2006 Feb |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.medicines.org.uk/emc/medicine/8771
Curator's Comment: intravenously (IV) or intramuscularly (IM)
The recommended dose is 40 mg administered intravenously (IV) or intramuscularly (IM), followed every 6 to 12 hours by 20 mg or 40 mg as required, not to exceed 80 mg/day.
Route of Administration:
Parenteral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17632097
100 uM parecoxib inhibited rat osteoclast differentiation by 94%
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:14:41 GMT 2025
by
admin
on
Mon Mar 31 18:14:41 GMT 2025
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Record UNII |
2919279Q3W
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Validated (UNII)
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CFR |
21 CFR 216.24
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VALDYN (WITHDRAWN: ARTHRITIS, RHEUMATOID)
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WHO-ATC |
M01AH03
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EMA ASSESSMENT REPORTS |
BEXTRA (WITHDRAWN: DYSMENORRHEA)
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EMA ASSESSMENT REPORTS |
VALDYN (WITHDRAWN: DYSMENORRHEA)
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EMA ASSESSMENT REPORTS |
BEXTRA (WITHDRAWN: OSTEOARTHRITIS)
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NCI_THESAURUS |
C1323
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EMA ASSESSMENT REPORTS |
VALDYN (WITHDRAWN: OSTEOARTHRITIS)
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EMA ASSESSMENT REPORTS |
BEXTRA (WITHDRAWN: ARTHRITIS, RHEUMATOID)
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WHO-VATC |
QM01AH03
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DB00580
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m11356
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C1869
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SUB05065MIG
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Valdecoxib
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VALDECOXIB
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759846
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278567
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2919279Q3W
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100000085238
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C406224
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
FECAL; URINE
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TARGET -> INHIBITOR |
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BINDER->LIGAND |
Plasma protein binding for valdecoxib is about 98% over the concentration range (21-2384 ng/mL).
BINDING
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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METABOLIC ENZYME -> SUBSTRATE |
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Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT |
MAJOR
URINE
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METABOLITE -> PARENT |
URINE
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PRODRUG -> METABOLITE ACTIVE |
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE ACTIVE -> PARENT |
Plasma concentrations of valdecoxib were 10-20 fold higher than the corresponding SC-66905 (M1) concentrations. The metabolite M1 is a less potent COX-2 specific inhibitor than the parent.
MAJOR
PLASMA
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE ACTIVE -> PARENT |
FECAL
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
MAJOR
URINE
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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ORAL BIOAVAILABILITY | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
|
ORAL ADMINISTRATION |
|
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Biological Half-life | PHARMACOKINETIC |
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