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KMID : 0370220130570030194
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Yakhak Hoeji
2013 Volume.57 No. 3 p.194 ~ p.198
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In Vitro Assessment of Cytochrome P450 Inhibition by Ambroxol and Cetirizine
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Kim Bong-Hee
Ryu Chang-Seon
Jang Him-Chan
Lee Sang-Yoon
Lee Ji-Yoon
Chae Jung-Woo
Kwon Kwang-II
Kim Sang-Kyum
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Abstract
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In the present study we evaluated drug-drug interaction potential of ambroxol and cetirizine mediated by inhibition of CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 using pooled human liver microsomes (HLMs). As measured by liquid chromatography-electrospray ionization tandem mass spectrometry, cetirizine and ambroxol inhibited significantly CYP2E1 but the maximal inhibition was approximately 36% at 10 μM cetirizine and 28% at 3 μM ambroxol. In addition, CYP2D6 activity was decreased to approximately 83% of control activity in pooled HLM incubated with 3 μM ambroxol. Activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, and CYP3A4 were not significantly inhibited by cetirizine and ambroxol. Considering their maximal plasma concentration in human (Cmax of cetirizine is approximately 0.67 μM and Cmax of ambroxol is 0.044 μM), these two drugs have very low possibility in drug-drug interaction by CYP inhibition in clinical situations.
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KEYWORD
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CYP 450, CYP inhibition, drug interaction, amboxol, cetirizine
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