When first approved, the dosing regimens for zidovudine were 1,200-1,5
00 mg/day; however, because toxicity developed. the daily dose had to
be reduced to 500-600 mg/day. At these lower doses, plasma concentrati
ons for a considerable segment of the dosing interval are often below
the assay sensitivity for the high-performance liquid chromatography (
HPLC) method. Although commonly used, the zidovudine radioimmunoassay
has had minimal documentation for the quantitative analysis of clinica
l samples, especially at current doses. The authors' findings indicate
that plasma, urine treated with phosphate buffer, and cerebrospinal f
luid samples may be assayed using a commercially available radioimmuno
assay. A good correlation was found for clinical samples measured by r
adioimmunoassay and HPLC (R-2 = 0.85). The greater assay sensitivity,
ability to process multiple specimens, and the relatively rapid turnar
ound time suggest that the zidovudine radioimmunoassay may have an imp
ortant role in clinical trials evaluating zidovudine pharmacokinetics.
This report summarizes the authors' experience with the zidovudine ra
dioimmunoassay and focuses on its potential use in studying the role o
f therapeutic drug monitoring for zidovudine.