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Pharmacodynamics of CY 216 in healthy volunteers: inter‐individual variations
Author(s) -
Rostin M,
Montastruc JL,
Houin G,
D'Azemar P,
Bayrou B,
Boneu B
Publication year - 1990
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/j.1472-8206.1990.tb01013.x
Subject(s) - pharmacodynamics , partial thromboplastin time , heparin , thrombin time , medicine , pharmacokinetics , pharmacology , anticoagulant , anesthesia , chemistry , coagulation
Summary— The pharmacodynamic parameters of a low molecular weight heparin (LMWH, CY 216) and their inter‐individual variations were investigated. In a cross over study 100 anti‐factor Xa IC U/kg were injected, one week apart, to 12 healthy‐volunteers by intravenous (IV) or subcutaneous (SC) route. The pharmacological effects were followed by performing activated partial thromboplastin time (APTT), thrombin clotting time (TCT) and a chromogenic anti‐factor Xa assay. The main pharmacodynamic parameters were calculated from the anti‐factor Xa activity disappearance curves. Five to ten min after IV injection, the APTT ranged between 56 and 98 sec (baseline 40 sec), the TCT between 28 and 99 sec (baseline 19 sec) and the anti‐factor Xa activity between 1.58 and 2.28 IC U/ml. The anti‐factor Xa activity half‐life ranged between 1.5 and 2.9 h. After SC injection, there were no detectable APTT and TCT prolongations; the maximum anti‐factor Xa activity ranged between 0.36 and 0.88 IC U/ml and the half life between 1.5 and 6.4 h. These results indicate that, as for standard heparin, there are large inter‐individual variations in the anticoagulant responses to a given dose of CY 216 an observation which may have clinical implications.