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Titolo:
Measurement of cyclooxygenase isozyme inhibition in humans: exploring the clinical relevance of biochemical selectivity
Autore:
Patrono, C;
Indirizzi:
Univ Chieti G DAnnunzio, Catedra Farmacol, Dept Med & Ageing, I-66013 Chieti, Italy Univ Chieti G DAnnunzio Chieti Italy I-66013 eing, I-66013 Chieti, Italy
Titolo Testata:
CLINICAL AND EXPERIMENTAL RHEUMATOLOGY
fascicolo: 6, volume: 19, anno: 2001, supplemento:, 25
pagine: S45 - S50
SICI:
0392-856X(200111/12)19:6<S45:MOCIII>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
NONSTEROIDAL ANTIINFLAMMATORY DRUGS; RANDOMIZED CONTROLLED TRIAL; RHEUMATOID-ARTHRITIS; GASTROINTESTINAL TOXICITY; HEALTHY-SUBJECTS; DOUBLE-BLIND; ROFECOXIB; CELECOXIB; COX-2; CYCLO-OXYGENASE-2;
Keywords:
coxibs; platelet COX-1; monocyte COX-2; whole blood assay;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Patrono, C Univ Chieti G DAnnunzio, Catedra Farmacol, Dept Med & Ageing, Via Vestini No 31, I-66013 Chieti, Italy Univ Chieti G DAnnunzio Via VestiniNo 31 Chieti Italy I-66013
Citazione:
C. Patrono, "Measurement of cyclooxygenase isozyme inhibition in humans: exploring the clinical relevance of biochemical selectivity", CLIN EXP RH, 19(6), 2001, pp. S45-S50

Abstract

Treatment with highly selective cyclooxygenase-2 inhibitors is associated with significantly fewer serious adverse gastrointestinal events than is treatment with non-selective NSAIDs, provided that the drug employed inhibitsCOX-2 but not COX-1 at therapeutic plasma levels. Several factors might influence the gastrointestinal (GI) safety of a COX-2 inhibitor administered to an individual patient. These factors include pharmacokinetic and pharmacodynamic variables (e.g. COX-2 selectivity), the interaction of these features with preexisting risk factors for drug-dependent adverse effects, as well as the variability in the individual response. Biochemical selectivity is one of the determinants of the risk of experiencing a serious GI complication during long-term NSAID therapy. The wider theseparation between the COX-2 and COX-1 dose-response curves of the inhibitor (an index of biochemical selectivity), the lower the probability of experiencing a clinically relevant inhibition of platelet COX-1 due to an unusually high drug level or intense pharmacodynamic response to a normal drug level. The clinical relevance of biochemical selectivity has to be studied in large GI outcome trials with adequate statistical power to detect realistic differences in these relatively rare events.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/20 alle ore 04:00:53