The objective of this review is to survey the recent literature regard
ing the various applications of microdialysis in pharmacokinetics. Mic
rodialysis is a relatively new technique for sampling tissue extracell
ular fluid that is gaining popularity in pharmacokinetic and pharmacod
ynamic studies, both in experimental animals and humans. The first par
t of this review discusses various aspects of the technique with regar
d to its use in pharmacokinetic studies, such as: quantitation of the
microdialysis probe relative recovery, interfacing the sampling techni
que with analytical instrumentation, and consideration of repeated pro
cedures using the microdialysis probe. The remainder of the review is
devoted to a survey of the recent literature concerning pharmacokineti
c studies that apply the microdialysis sampling technique. While the m
ajority of the pharmacokinetic studies that have utilized microdialysi
s have been done in the central nervous system, a growing number of ap
plications are being found in a variety of peripheral tissue types, e.
g. skin, muscle, adipose, eye, lung, liver, and blood, and these are c
onsidered as well. Given the rising interest in this technique, and th
e ongoing attempts to adapt it to pharmacokinetic studies, it is clear
that microdialysis sampling will have an important place in studying
drug disposition and metabolism.