The antimalarial drug halofantrine is bound mainly to low and high density lipoproteins in human serum.

• DOI: 10.1111/j.1365-2125.1995.tb04489.x
• Publication Date: 2012-07-05T05:16:29Z
• Authors: B Cenni; J Meyer; R Brandt; B Betschart
• Keywords: Halofantrine; Free fraction; Orosomucoid; Serum Albumin

1. The major serum proteins which bind halofantrine were identified by size exclusion chromatography. In addition, the binding affinity of to human erythrocytes and was measured an erythrocyte partitioning technique. influence serum‐drug on distribution in whole blood estimated simulating several disease‐related changes levels most important proteins. 2. chromatographic resolution preincubated with allowed a quantitative analysis low density lipoproteins, high alpha 1‐acid glycoprotein albumin using Very lipoproteins did not significant extent. 3. is bound (83%) (17%). Low (affinity constant nKP = 44.4 l g‐1) (nKP 14.4 serum. 4.39 0.27 had relatively affinities. 4. concentration influences both fraction unbound drug associated erythrocytes. Changes protein concentrations often encountered malaria are likely increase