W. Schanzer et I. Seinsch, THE PROBLEM OF DRUG APPLICATION IN COMPET ITION HORSES FROM THE VIEW OF THE LABORATORY, Praktische Tierarzt, 78, 1997, pp. 51-55
The detection and identification of pharmacologically active substance
s is done by chemical analysis methods, where mainly gas chromatograph
y and mass spectrometry are used. With exception of a few compounds, o
nly qualitative detection is performed and a case is determined positi
ve independent of the concentration. From the analytical data usually
no conclusion is possible as to when and in which amount a substance h
as been applied. How long before a competition should the application
be ceased? Indications given from excretion studies can only be used a
s a guide line and should be interpreted very carefully. The detection
time of a substance is mainly influenced by the elimination kinetics
and the sensitivity of the analytical method. There is a lot of indivi
dual variation, in which the amount, the kind and the duration of an a
pplication are important factors. In addition the elimination is influ
enced by condition, health status and age of the horse as well as by t
he pH of the urine. The detection period of a substance can be extende
d if the method of detection and sample preparation are improved. This
is required for compounds which are difficult to detect, as they are
are applied in very low concentrations. The two substances phenylbutaz
one and isoxsuprine are presented as an example for metabolism and eli
mination. Phenybutazone, belonging to the group of nonsteroidal antiin
flammatory drugs, is mainly excreted unmetabolized. Main metabolites a
re the pharmacologically active oxyphenbutazone and the unactive g-hyd
oxy-phenylbutazone metabolite. The halflife time of phenylbutazone was
determined as 4.3 hours and increased in correlation to the dose. Iso
xsuprin is mainly excreted as its glucuronid conjugate. It could be de
tected in plasma 72 hours after a single dose. The detection time in u
rine is much longer.