An acute bromisoval intoxication

Essen, E. J. van; Csanky-Treels, J. C.; Krom, M.C.T.F.M. de; Tjoeng, M. M.

doi:10.1007/bf00278037

Cited by 4 publications

(1 citation statement)

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“…It is controversial which enantiomer of BVU exhibits the pharmacological activity and acute toxicity. The consciousness level correlated roughly to the total parent drug concentration in blood in our experience and in literature (van Essen et al, 1980;Iwasaki et al, 1998), but we cannot conclude whether the activities of the enantiomer pair are equal or unequal because of the imprecise measurement of central nervous system function. In mice, all the compounds of (À)-, (AE)-and ()-BVU exhibited hypnotic activity after intraperitoneal injection with a slight difference in ED 50 of 139, 183 and 195 mg/kg, respectively (personal communication from Nippon Shinyaku Co.).…”

Section: Discussionmentioning

confidence: 89%

Enantioselective determination of bromoisovalerylurea by liquid chromatography on chiral stationary phase in reversed- or normal-phase partition mode

Nishikawa

Ohtani

Kamijo

et al. 2000

Biomed. Chromatogr.

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Bromoisovalerylurea (bromvalerylurea) is a sedative-hypnotic given orally as a racemate. Enantiomers of this drug could be separated by high-performance liquid chromatography on the three chiral stationary phases (a vancomycin-bonded, beta-cyclodextrin derivative-bonded, or urea derivative-bonded phase). Biological fluids of human subjects who had ingested toxic or therapeutic doses of the racemate were chromatographed after liquid-liquid extraction. The (+)-enantiomer concentration was almost equal to the (-)-enantiomer concentration in the serum of one overdosed patient. In all the other subjects, the (+)-enantiomer was less than the (-)-enantiomer in their sera and saliva. The data suggest that the drug is absorbed non-stereoselectively from the gastrointestinal tract and eliminated from the blood stereoselectively.

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Section: Discussionmentioning

confidence: 89%