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Hiroshima Journal of Medical Sciences Volume 33 Issue 4
published_at 1984-12
Metabolism of an Antiallergic Agent, Azelastine (4-(p-Chlorobenzyl)-2-[N-Methylperhydroazepinyl-(4)]- 1-(2H)-Phthalazinone Hydrochloride) in Rats and Guinea Pigs
ラットおよびモルモットにおける抗アレルギー剤 azelastine の代謝
Tatsumi Kiyoshi
Yamada Hideyuki
Yoshimura Hidetoshi
Nishizawa Yukio
Sakai Misao
Mizuo Hitoshi
Yamato Chiyuki
Abstract
The in vivo metabolism of an antiallergic agent, azelastine, (4-(p-chlorobenzyl)-2-[N-methylperhydroazepinyl-(4)]-1-(2H)-phthalazinone hydrochloride) was examined following oral administration to rats and guinea pigs. As a result, it was found that the drug was metabolized to 4-(p-chlorobenzyl)-2-[N-methyl-7-oxo-perhydroazepinyl-(4)]-1-(2H)-phthalazinone, 6-hydroxy-4-(p-chlorobenzyl)-2-[N-methylperhydroazepinyl-(4)]-1-(2H)-phthalazinone (6-hydroxyazelastine), 7-hydroxy-4-(p-chlorobenzyl)-2-[N-methyl -perhydroazepinyl-(4)]-1-(2H)-phthalazinone and 4-(p-chlorobenzyl)-2-[perhydroazepinyl-(4)]-1-(2H)-phthalazinone (desmethylazelastine) in these animal bodies. A part of the hydroxy derivatives of the drug was excreted into urine as their glucuronides. In addition, the incubation of azelastine with rat liver microsomes resulted in the formation of 6-hydroxyazelastine and desmethylazelastine in the presence of an NADPH-generating system.
About This Article
Keywords
Metabolism
Azelastine
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