Metabolism of an Antiallergic Agent, Azelastine (4-(p-Chlorobenzyl)-2-[N-Methylperhydroazepinyl-(4)]- 1-(2H)-Phthalazinone Hydrochloride) in Rats and Guinea Pigs
Hiroshima Journal of Medical Sciences Volume 33 Issue 4
Page 669-678
published_at 1984-12
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| File | |
| Title ( eng ) |
Metabolism of an Antiallergic Agent, Azelastine (4-(p-Chlorobenzyl)-2-[N-Methylperhydroazepinyl-(4)]- 1-(2H)-Phthalazinone Hydrochloride) in Rats and Guinea Pigs
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| Title ( jpn ) |
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
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| Creator |
Tatsumi Kiyoshi
Yamada Hideyuki
Yoshimura Hidetoshi
Nishizawa Yukio
Sakai Misao
Mizuo Hitoshi
Yamato Chiyuki
|
| Source Title |
Hiroshima Journal of Medical Sciences
|
| Volume | 33 |
| Issue | 4 |
| Start Page | 669 |
| End Page | 678 |
| Journal Identifire |
[PISSN] 0018-2052
[EISSN] 2433-7668
[NCID] AA00664312
|
| 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.
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| Keywords |
Metabolism
Azelastine
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| NDC |
Medical sciences [ 490 ]
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| Language |
eng
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| Resource Type | departmental bulletin paper |
| Publisher |
Hiroshima University School of Medicine
|
| Date of Issued | 1984-12 |
| Publish Type | Version of Record |
| Access Rights | open access |
| Source Identifier |
[ISSN] 0018-2052
[NCID] AA00664312
[PMID] 6152559
|
