Pharmacokinetics of a glycine site antagonist (gavestinel) following multiple dosing in patients with acute stroke

The objective of this study was to characterize the pharmacokinetics of gavestinel in patients with acute stroke. Gavestinel was administered as an 800-mg loading dose and followed by either 100-, 200-, or 400-mg maintenance doses given every 12 h for five doses. Blood and urine samples were collect...

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Veröffentlicht in:European journal of clinical pharmacology 2000-02, Vol.55 (11-12), p.867-872
Hauptverfasser: HOKE, J. F, DYKER, A. G, BARNABY, R. J, LEES, K. R
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Sprache:eng
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Zusammenfassung:The objective of this study was to characterize the pharmacokinetics of gavestinel in patients with acute stroke. Gavestinel was administered as an 800-mg loading dose and followed by either 100-, 200-, or 400-mg maintenance doses given every 12 h for five doses. Blood and urine samples were collected for pharmacokinetic evaluation. The pharmacokinetics of gavestinel were determined using compartmental analysis. The mean clearance (CL) and central (Vc) and steady-state (Vss) volumes of distribution across the dose groups were 0.31-0.40 l x h(-1), 3.3-3.9 l, and 9.8-17 l, respectively. The mean terminal half-life ranged from 29 h to 56 h. Gavestinel was extensively bound to plasma protein (median percentage free
ISSN:0031-6970
1432-1041
DOI:10.1007/s002280050709