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A sensitive radioimmunoassay is described for the determination of astemizole in human plasma. Immunization of rabbits with an astemizole hapten, conjugated with bovine serum albumin, resulted in the production of antiserum, capable of detecting less than 0.05 ng/ml of astemizole. Because of the cross‐reactivity of the antibodies with structurally related metabolites, plasma samples had to be submitted to two distinct extraction procedures prior to radioimmunoassay. The most selective procedure enabled the measurement of unchanged astemizole as confirmed by high‐performance liquid chromatography. The other extraction procedure allowed the determination of the fraction astemizole plus hydroxylated metabolites, which consisted mainly of astemizole and its major metabolite desmethylastemizole.
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Woestenborghs et al. (1986) studied this question.
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