INVESTIGATION ON PLASMA-LEVELS OF THE NEU ROTOXIN -TRICHLOROMETHYL-1,2,3,4-TETRAHYDRO-BETA-CARBOLINE AFTER ORAL-ADMINISTRATION OF CHLORAL HYDRATE IN MAN
J. Leuschner et al., INVESTIGATION ON PLASMA-LEVELS OF THE NEU ROTOXIN -TRICHLOROMETHYL-1,2,3,4-TETRAHYDRO-BETA-CARBOLINE AFTER ORAL-ADMINISTRATION OF CHLORAL HYDRATE IN MAN, Arzneimittel-Forschung, 48(1), 1998, pp. 1-5
Chloral hydrate (GAS 302-17-0) is a widely used hypnotic and sedative
agent. It was recently reported in the literature that a neurotoxin, T
aClo richloromethyl-1,2,3,4-tetrahydro-beta-carboline), may be formed
in vitro from tryptamine (Ta) and chloral (Clo). Intraperitoneal admin
istration of TaClo led to parkinson-like symptoms in the rat. Hence, t
he plasma levels of TaClo were determined at various time-points in 18
healthy volunteers in two periods each during a bioavailability study
of several chloral hydrate preparations. The limit of quantitation fo
r TaClo was 5 ng/ml. No TaClo could be determined in the plasma of the
various volunteers following administration of human therapeutic dose
s of chloral hydrate. Hence, it is unlikely that TaClo will be formed
in man after application of therapeutic doses of chloral hydrate to pa
tients.