Source:http://linkedlifedata.com/resource/pubmed/id/10381787
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
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| pubmed:dateCreated |
1999-7-26
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| pubmed:abstractText |
We evaluated whether therapeutic blood levels of meloxicam are associated with selective inhibition of monocyte cyclooxygenase (COX)-2 in vitro and ex vivo. Concentration-response curves for the inhibition of monocyte COX-2 and platelet COX-1 were obtained in vitro after the incubation of meloxicam with whole blood samples. Moreover, 11 healthy volunteers received placebo or 7.5 or 15 mg/day meloxicam, each treatment for 7 consecutive days, according to a randomized, double-blind, crossover design. Before dosing and 24 h after the seventh dose of each regimen, heparinized whole blood samples were incubated with lipopolysaccharide (10 microgram/ml) for 24 h at 37 degrees C, and prostaglandin E2 was measured in plasma as an index of monocyte COX-2 activity. The production of thromboxane B2 in whole blood allowed to clot at 37 degrees C for 60 min was assessed as an index of platelet COX-1 activity. The administration of placebo did not significantly affect plasma prostaglandin E2 (21. 3 +/- 7.5 versus 19.1 +/- 4 ng/ml, mean +/- S.D., n = 11) or serum thromboxane B2 (426 +/- 167 versus 425 +/- 150 ng/ml) levels. In contrast, the administration of 7.5 and 15 mg of meloxicam caused dose-dependent reductions in monocyte COX-2 activity by 51% and 70%, respectively, and in platelet COX-1 activity by 25% and 35%, respectively. Although the IC50 value of meloxicam for inhibition of COX-1 was 10-fold higher than the IC50 value of COX-2 in vitro, this biochemical selectivity was inadequate to clearly separate the effects of meloxicam on the two isozymes after oral dosing as a function of the daily dose and interindividual variation in steady-state plasma levels.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 2,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 2 Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Dinoprostone,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/PTGS1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/PTGS2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin-Endoperoxide Synthases,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazines,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Thromboxane B2,
http://linkedlifedata.com/resource/pubmed/chemical/meloxicam
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| pubmed:status |
MEDLINE
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| pubmed:month |
Jul
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| pubmed:issn |
0022-3565
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
290
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
276-80
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:10381787-Adult,
pubmed-meshheading:10381787-Blood Platelets,
pubmed-meshheading:10381787-Cross-Over Studies,
pubmed-meshheading:10381787-Cyclooxygenase 1,
pubmed-meshheading:10381787-Cyclooxygenase 2,
pubmed-meshheading:10381787-Cyclooxygenase 2 Inhibitors,
pubmed-meshheading:10381787-Cyclooxygenase Inhibitors,
pubmed-meshheading:10381787-Dinoprostone,
pubmed-meshheading:10381787-Dose-Response Relationship, Drug,
pubmed-meshheading:10381787-Double-Blind Method,
pubmed-meshheading:10381787-Female,
pubmed-meshheading:10381787-Humans,
pubmed-meshheading:10381787-Isoenzymes,
pubmed-meshheading:10381787-Male,
pubmed-meshheading:10381787-Membrane Proteins,
pubmed-meshheading:10381787-Monocytes,
pubmed-meshheading:10381787-Prostaglandin-Endoperoxide Synthases,
pubmed-meshheading:10381787-Thiazines,
pubmed-meshheading:10381787-Thiazoles,
pubmed-meshheading:10381787-Thromboxane B2
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| pubmed:year |
1999
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| pubmed:articleTitle |
Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects.
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| pubmed:affiliation |
Department of Medicine and Aging, Division of Pharmacology, University of Chieti "G. D'Annunzio" School of Medicine, Chieti, Italy.
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| pubmed:publicationType |
Journal Article,
Clinical Trial,
In Vitro,
Randomized Controlled Trial,
Research Support, Non-U.S. Gov't
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