Red blood cell partitioning of gallopamil, verapamil and norverapamil.
In-vitro binding of calcium-antagonists gallopamil and verapamil (and its main metabolite norverapamil) to human red blood cells (RBCs) was investigated. The drugs are bound reversibly and dose dependent to RBCs in the same order of magnitude, with partition-coefficients of kRBC = 0.12-0.34 for gallopamil, kRBC = 0.10-0.30 for verapamil and kRBC = 0.10-0.27 for norverapamil. The data indicate that, although RBCs may act as subcompartments of the blood for this class of compounds, they may have no influence on therapeutic plasma concentrations, due to their low kRBC.
Czejka
M J
MJ
Institute for Pharmaceutical Chemistry, University of Vienna, Austria.
Zwoelfer
N
N
Podesser
B
B
D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004912:Erythrocytes / Q000737:chemistry / Q000378:metabolism* / Q000648:ultrastructure; D005711:Gallopamil / Q000097:blood* / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D012044:Regression Analysis; D014700:Verapamil / Q000031:analogs & derivatives* / Q000097:blood* / Q000493:pharmacokinetics
D005711:Gallopamil; C016904:norverapamil; D014700:Verapamil