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Type: Artigo de periódico
Title: Pathways involved in trifluoperazine-, dibucaine- and praziquantel-induced hemolysis
Author: Malheiros, SVP
Meirelles, NC
de Paula, E
Abstract: This work elucidates differences in the hemolytic pathway developed by the antipsychotic trifluoperazine (TFP), the local anesthetic dibucaine (DBC) and the antihelminthic praziquantel (PZQ). Their partition coefficients (P) were measured at pH 7.4 between n-octanol, microsomes, liposomes, erythrocyte ghosts and n-octanol/water. The effective drug:lipid molar ratios for the onset of membrane solubilization (Re-SAT) and complete hemolysis (Re-SOL) were calculated from the experimental P values and compared with a classical surface-active compound treatment [Lichtenberg, D. Biochim. Biophys. Acta 821 (1985) 470-478]. The contribution of charged/uncharged forms of TFP and DEC for the hemolytic activity was also analyzed. In all cases the hemolytic phenomena could be related to the monomeric drug insertion into the membrane. Only for TFP at isosmotic condition lysis occurs at concentrations beyond the CR;IC of the drug, indicating that micellization facilitates TFP hemolytic effect, while DEC and PZQ reach a real membrane saturation at their monomeric form. (C) 2000 Elsevier Science B.V. All rights reserved.
Subject: erythrocyte
Country: Holanda
Editor: Elsevier Science Bv
Rights: fechado
Identifier DOI: 10.1016/S0301-4622(99)00125-8
Date Issue: 2000
Appears in Collections:Unicamp - Artigos e Outros Documentos

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