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Titolo:
DISPOSITION OF C-14-EPTIFIBATIDE AFTER INTRAVENOUS ADMINISTRATION TO HEALTHY-MEN
Autore:
ALTON KB; KOSOGLOU T; BAKER S; AFFRIME MB; CAYEN MN; PATRICK JE;
Indirizzi:
SCHERING PLOUGH CORP,RES INST,CLIN PHARMACOL K154,4455,2015 GALLOPINGHILL RD KENILWORTH NJ 07033 SCHERING PLOUGH CORP,RES INST,CLIN PHARMACOL K154 KENILWORTH NJ 07033
Titolo Testata:
Clinical therapeutics
fascicolo: 2, volume: 20, anno: 1998,
pagine: 307 - 323
SICI:
0149-2918(1998)20:2<307:DOCAIA>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
CORONARY-ARTERY DISEASE; FIBRINOGEN RECEPTOR ANTAGONIST; IIB/IIIA INTEGRIN RECEPTOR; ISCHEMIC-HEART-DISEASE; PLATELET; INTERVENTION; MECHANISMS; INHIBITOR; PATHOGENESIS; MULTICENTER;
Keywords:
EPTIFIBATIDE; ANTITHROMBOTICS; PHARMACOKINETICS; GLYCOPROTEIN IIB/IIIA RECEPTOR;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
K.B. Alton et al., "DISPOSITION OF C-14-EPTIFIBATIDE AFTER INTRAVENOUS ADMINISTRATION TO HEALTHY-MEN", Clinical therapeutics, 20(2), 1998, pp. 307-323

Abstract

Eptifibatide, a synthetic peptide inhibitor of the platelet glycoprotein IIb/IIIa receptor, has been studied as an antithrombotic agent in a variety of acute ischemic coronary syndromes. The purpose of the present study was to characterize the disposition of C-14-eptifibatide inman after a single intravenous (IV) bolus dose. C-14-Eptifibatide (similar to 50 mu Ci) was administered to eight healthy men as a single 135-mu g/kg IV bolus. Blood, breath carbon dioxide, urine, and fecal samples were collected for up to 72 hours postdose and analyzed for radioactivity by liquid scintillation spectrometry. Plasma and urine samples were also assayed by liquid chromatography with mass spectrometry for eptifibatide and deamidated eptifibatide (DE). Mean (+/-SD) peak plasma eptifibatide concentrations of 879 +/- 251 ng/mL were achieved atthe first sampling time (5 minutes), and concentrations then generally declined biexponentially, with a mean distribution half-life of 5 +/- 2.5 minutes and a mean terminal elimination half-life of 1.13 +/- 0.17 hours. Plasma eptifibatide concentrations and radioactivity declined in parallel, with most of the radioactivity (82.4%) attributed to eptifibatide. A total of approximately 73% of administered radioactivitywas recovered in the 72-hour period following C-14-eptifibatide dosing. The primary route of elimination was urinary (98% of the total recovered radioactivity), whereas fecal (1.5%) and breath (0.8%) excretionwas small. Eptifibatide is cleared by both renal and nonrenal mechanisms, with renal clearance accounting for approximately 40% of total body clearance. Within the first 24 hours, the drug is primarily excreted in the urine as unmodified eptifibatide (34%), DE (19%), and more polar metabolites (13%).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/11/20 alle ore 09:43:38