Effects of the antiepileptic drug carbamazepine on human erythrocytes.
The structural effects of the antiepileptic drug carbamazepine (CBZ) on the human erythrocyte membrane and molecular models have been investigated in the present work. This report presents the following evidence that CBZ interacts with red cell membranes: (a) X-ray diffraction and fluorescence spectroscopy of phospholipid bilayers showed that CBZ perturbed a class of lipids found in the outer moiety of the erythrocyte membrane; (b) in isolated unsealed human erythrocytes (IUM) the drug induced a disordering effect on the polar head groups and acyl chains of the membrane lipid bilayer; (c) in scanning electron microscopy (SEM) studies on human erythrocytes the formation of echinocytes was observed, due to the preferential insertion of CBZ in the outer monolayer of the red cell membrane. The effects of the drug detected in the present work were observed at concentrations of the order of those currently appearing in serum when it is therapeutically administered. This is the first time that toxic effects of carbamazepine on the human erythrocyte membrane have been described.
Suwalsky
Mario
M
Faculty of Chemical Sciences, University of Concepción, Casilla 160-C, Concepción, Chile. msuwalsk@udec.cl
Mennickent
Sigrid
S
Norris
Beryl
B
Villena
Fernando
F
Sotomayor
Carlos P
CP
D000927:Anticonvulsants / Q000494:pharmacology*; D002220:Carbamazepine / Q000494:pharmacology*; D004134:Dimyristoylphosphatidylcholine; D004910:Erythrocyte Membrane / Q000187:drug effects / Q000648:ultrastructure; D004912:Erythrocytes / Q000187:drug effects* / Q000648:ultrastructure; D005456:Fluorescent Dyes; D006801:Humans; D066298:In Vitro Techniques; D008567:Membranes, Artificial; D008855:Microscopy, Electron, Scanning; D008856:Microscopy, Fluorescence; D014961:X-Ray Diffraction
D000927:Anticonvulsants; D005456:Fluorescent Dyes; D008567:Membranes, Artificial; D002220:Carbamazepine; D004134:Dimyristoylphosphatidylcholine