Which concentration of the inhibitor should be used to predict in vivo drug interactions from in vitro data?

When the metabolism of a drug is competitively or noncompetitively inhibited by another drug, the degree of in vivo interaction can be evaluated from the [I]u/Ki ratio, where [I]u is the unbound concentration around the enzyme and Ki is the inhibition constant of the inhibitor. In the present study,...

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Veröffentlicht in:	AAPS PharmSci 2002-01, Vol.4 (4), p.E25-60
Hauptverfasser:	Ito, Kiyomi, Chiba, Koji, Horikawa, Masato, Ishigami, Michi, Mizuno, Naomi, Aoki, Jun, Gotoh, Yasumasa, Iwatsubo, Takafumi, Kanamitsu, Shin-ichi, Kato, Motohiro, Kawahara, Iichiro, Niinuma, Kayoko, Nishino, Akiko, Sato, Norihito, Tsukamoto, Yuko, Ueda, Kaoru, Itoh, Tomoo, Sugiyama, Yuichi
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding, Competitive Cytochrome P-450 Enzyme Inhibitors Drug Interactions Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Humans Kinetics Substrate Specificity
Online-Zugang:	Volltext
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