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Titolo:
INTRANASAL ANTIPLATELET ANTITHROMBOTIC EFFICACY OF A NOVEL PLATELET GPIIB/IIIA RECEPTOR ANTAGONIST DMP755/
Autore:
MOUSA SA; MU DX; HUSSAIN MA;
Indirizzi:
DUPONT PHARMACEUT CO,EXPT STN,E400-3456 WILMINGTON DE 19880
Titolo Testata:
Thrombosis research
fascicolo: 3, volume: 92, anno: 1998,
pagine: 115 - 124
SICI:
0049-3848(1998)92:3<115:IAAEOA>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
GLYCOPROTEIN IIB/IIIA RECEPTOR; UNSTABLE ANGINA; ACTIVATION; ANTIPLATELET; INVIVO; AGGREGATION; DISEASE; CANINE; MODEL; BLOOD;
Keywords:
INTRANASAL; ANTIPLATELET; ANTITHROMBOTIC; GPIIB/IIIA; DMP755;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
26
Recensione:
Indirizzi per estratti:
Citazione:
S.A. Mousa et al., "INTRANASAL ANTIPLATELET ANTITHROMBOTIC EFFICACY OF A NOVEL PLATELET GPIIB/IIIA RECEPTOR ANTAGONIST DMP755/", Thrombosis research, 92(3), 1998, pp. 115-124

Abstract

This article describes the equivalent antiplatelet/antithrombotic effects of DMP755 at comparable doses by intranasal and IV administrationbut required substantially higher doses with the oral administration route. Antiplatelet and antithrombotic efficacy of DMP755 or its free acid form XV459 were determined in dogs. Arterial thrombosis models were induced either electrolytically (200 mu A anodal current) in the carotid artery or mechanically by external clamping of femoral artery along with stenosis, which result in either total occlusive thrombus formation or cyclic flow reduction (CFR), respectively. Either DMP755 or its free acid form, XV459 demonstrated maximal and comparable antiplatelet efficacy at 0.025-0.1 mg/kg, intravenous (IV) or intranasal but not oral (PO) in mongrel dogs. The antiplatelet efficacy of DMP755 at 0.1 mg/kg, intranasal, or IV was determined in a cross-over design (n=8in each group). In this study, a comparable and maximal antiplatelet efficacy for DMP755 after intranasal or IV was demonstrated suggesting100% intranasal bioavailability as compared with the modest antiplatelet efficacy at 0.1 mg/kg, PO. DMP755 administered at 0.1 mg/kg, intranasally or IV or at 0.3 mg/kg, PO prevented the incidence of electrolytic injury-induced arterial thrombosis in the carotid artery thrombosis model and prevented the incidence of cyclic flow reduction in mechanically injured and stenosed femoral artery. In conclusion, DMP755 has a comparable intranasal and intravenous antiplatelet/antithrombotic profiles along with a significant improvement over its oral profiles. These data also suggest the potential utility of intranasal DMP755 in various acute and chronic thromboembolic disorders. This is the first report of intranasal bioavailability of a glycoprotein receptor antagonist. (C) 1998 DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 04:19:57