Translations:Discovery and development of angiotensin receptor blockers/41/ja: Difference between revisions

Latest revision as of 12:38, 28 March 2024

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Message definition (Discovery and development of angiotensin receptor blockers)

All of the ARBs, except for valsartan and olmesartan, are metabolized in some way by the [[cytochrome P450]] (CYP) enzyme [[CYP2C9|2C9]], that is found in the human liver. [[CYP2C9]] is for example responsible for the metabolizing of losartan to EXP 3174 and the slow metabolizing of valsartan and candesartan to their inactive metabolites. Telmisartan is, on the other hand, in part metabolized by [[glucuronidation]] and olmesartan is excreted as the unchanged drug.
Telmisartan is the only ARB that can cross the [[blood–brain barrier]] and can therefore inhibit centrally mediated effects of Ang II, contributing to even better blood pressure control.

バルサルタンとオルメサルタンを除くすべてのARBは、ヒトの肝臓に存在するチトクロームP450（CYP）酵素2C9によって何らかの形で代謝される。例えば、CYP2C9はロサルタンをEXP 3174に代謝し、バルサルタンとカンデサルタンを不活性代謝物にゆっくりと代謝する。一方、テルミサルタンの一部はグルクロン酸抱合によって代謝され、オルメサルタンは未変化体の薬物として排泄される。テルミサルタンは血液脳関門を通過できる唯一のARBであるため、AngⅡの中枢性作用を阻害することができ、より優れた血圧コントロールに貢献する。

Translations:Discovery and development of angiotensin receptor blockers/41/ja: Difference between revisions

Latest revision as of 12:38, 28 March 2024

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