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Titolo:
EXPERIMENTAL-MODELS USED TO INVESTIGATE THE DIFFERENTIAL INHIBITION OF CYCLOOXYGENASE-1 AND CYCLOOXYGENASE-2 BY NONSTEROIDAL ANTIINFLAMMATORY DRUGS
Autore:
PAIRET M; VANRYN J;
Indirizzi:
BOEHRINGER INGELHEIM PHARMA DEUTSCHLAND,RESP RES,BIRKENDORFER STR 65 D-88397 BIBERACH GERMANY
Titolo Testata:
Inflammation research
, volume: 47, anno: 1998, supplemento:, 2
pagine: 93 - 101
SICI:
1023-3830(1998)47:<93:EUTITD>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
NONSTEROIDAL ANTIINFLAMMATORY DRUGS; PROSTAGLANDIN-G/H SYNTHASE-1; SELECTIVE COX-2 INHIBITOR; PLATELET-AGGREGATION; WHOLE-BLOOD; COX-2-SELECTIVE INHIBITOR; RHEUMATOID-ARTHRITIS; PLASMA-CONCENTRATION; HEALTHY-VOLUNTEERS; ARACHIDONIC-ACID;
Keywords:
NONSTEROIDAL ANTIINFLAMMATORY DRUGS CYCLOOXYGENASE; IN VITRO IN VIVO ASSAYS; SELECTIVITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
65
Recensione:
Indirizzi per estratti:
Citazione:
M. Pairet e J. Vanryn, "EXPERIMENTAL-MODELS USED TO INVESTIGATE THE DIFFERENTIAL INHIBITION OF CYCLOOXYGENASE-1 AND CYCLOOXYGENASE-2 BY NONSTEROIDAL ANTIINFLAMMATORY DRUGS", Inflammation research, 47, 1998, pp. 93-101

Abstract

Numerous in vitro assays have been developed for testing and comparing the relative inhibitory activities of non-steroidal anti-inflammatory drugs against cyclooxygenase (COX)-1 and COX-2. Despite variability among these systems, which precludes direct comparison of data, analysis of the ratio of inhibition of COX-1 to COX-2 by non-steroidal anti-inflammatory drugs, suggests inhibitors can be classified based on their COX selectivity. Standard non-steroidal antiinflammatory drugs can be considered nonselective; compounds such as meloxicam and nimesulidecan be classified as COX-2 preferential; and compounds such as SC 58125 and L-754,337 are selective for COX-2. Although in vitro systems are important for characterizing COX-1 and COX-2 inhibitory activity, the clinical relevance of these data should be considered carefully. Thelevel of inhibition of COX-I and COX-2, in vivo at a given dose in patients, cannot be predicted from in vitro data alone. The pharmacokinetic properties of each compound including plasma levels, distribution and binding to plasma proteins, have to be taken into account. Human pharmacology studies concentrating on the inhibition of prostanoid synthesis in target tissues are of paramount importance in determining theclinical relevance of COX-2 selectivity.

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Documento generato il 07/07/20 alle ore 22:03:27