| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2017-10-05 |
| タイトル |
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タイトル |
Morphine glucuronosyltransferase activity in human liver microsomes is inhibited by a variety of drugs that are co-administered with morphine. |
| 言語 |
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言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| ID登録 |
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ID登録 |
10.24517/00027014 |
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ID登録タイプ |
JaLC |
| 著者 |
Hara, Yusuke
Nakajima, Miki
Miyamoto, Ken-ichi
Yokoi, Tsuyoshi
|
| 著者別表示 |
原, 祐輔
中嶋, 美紀
宮本, 謙一
横井, 毅
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| 提供者所属 |
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内容記述タイプ |
Other |
|
内容記述 |
金沢大学附属病院薬剤部 |
| 書誌情報 |
Drug metabolism and pharmacokinetics
巻 22,
号 2,
p. 103-112,
発行日 2007-04-01
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| ISSN |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
1347-4367 |
| NCID |
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収録物識別子タイプ |
NCID |
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収録物識別子 |
AA1162652X |
| DOI |
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関連タイプ |
isIdenticalTo |
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識別子タイプ |
DOI |
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関連識別子 |
10.2133/dmpk.22.103 |
| 出版者 |
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出版者 |
日本薬物動態学会=Japanese Society for the Study of Xenobiotics (JSSX) |
| 抄録 |
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内容記述タイプ |
Abstract |
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内容記述 |
Morphine is an analgesic drug used for the treatment of acute and chronic pain syndromes for cancer patients. Glucuronidation is a major pathway of the elimination of morphine in humans. Morphine is metabolized to 3-glucuronide (no analgesic effect) and 6-glucuronide (more potently analgesic than morphine) mainly by UGT2B7. In the present study, we investigated the inhibitory effects of a variety of drugs on the morphine glucuronosyltransferase activities in human liver microsomes. Twenty-one drugs including anticancer drugs, immunosuppressants, analgesics, anticonvulsants, antidepressants, antipsychotic drugs were selected in this study, because they are frequently co-administered with morphine. We found that 10 out of 21 drugs, tamoxifen, tacrolimus, diclofenac, carbamazepine, imipramine, clomipramine, amitriptyline, diazepam, lorazepam and oxazepam extensively inhibited the morphine 3- and 6-glucuronosyltransferase activities. Although some of the drugs are not substrates of UGT2B7, they would be potent inhibitors of UGT2B7. If patients receive morphine and these drugs simultaneously, the drug-drug interaction may change the levels of morphine and these glucuronides, resulting in altered analgesic efficacy and the risk of side effects. The results presented here will assist clinicians in choosing the proper drugs and/or dosages, and enable them to anticipate potential drug-drug interactions. |
| 著者版フラグ |
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出版タイプ |
VoR |
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出版タイプResource |
http://purl.org/coar/version/c_970fb48d4fbd8a85 |
HO-PR-HARA-Y-103.pdf (412.0 kB)
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