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Cytochrome P450 3A4 Cytochrome P450 2C9 Cytochrome P450 2C19 Cytochrome P450 3A5 P-glycoprotein P-glycoprotein P-glycoprotein ATP-dependent translocase ABCB1 Solute carrier family 15 member 1 Canalicular multispecific organic anion transporter 2 UDP- glucuronosyltransferase 2B7 Cytochrome P450 1A2 Fluconazole Fluconazole Fluconazole Fluconazole, Glucuronidated metabolite Fluconazole N-oxide Fluconazole Fluconazole Fluconazole N-oxide Fluconazole, Glucuronidated metabolite Uridine diphosphate glucuronic acid UDP H+ NADPH O2 H+ NADP H2O Heme Heme Heme Heme Heme Fluconazole Pathway Renal Excretion Fluconazole ingested through a pill Blood Vessel Intestinal Lumin Hepatocyte Intestinal Epithelial Cell Only 6.5% become Glucuronidated metabolite, Fluconazole 2% become Fluconazole N-oxide Fluconazole is sent to target cells unchanged Fluconazole inhibits 4 Cytochrome exzymes which causes hepatotoxicity in the liver when taken frequently or with previous liver dysfunction Endoplasmic Reticulum membrane 93.3% of the dose, 80% as unchanged Fluconazole, is excreted through the urine
Endoplasmic Reticulum CYP3A4 CYP2C9 CYP2C19 CYP3A5 ABCB1 ABCB1 ABCB1 ABCB1 SLC15A1 ABCC3 UGT2B7 CYP1A2 Fluconazole Fluconazole Fluconazole Fluconazole, Glucuronidated metabolite Fluconazole N-oxide Fluconazole Fluconazole Fluconazole N-oxide Fluconazole, Glucuronidated metabolite Uridine diphosphate glucuronic acid UDP Hydrogen Ion NADPH Oxygen Hydrogen Ion NADP Water Fluconazole Pathway Renal Excretion
CYP3A4 CYP2C9 CYP2C19 CYP3A5 ABCB1 ABCB1 ABCB1 ABCB1 SLC15A1 ABCC3 UGT2B7 CYP1A2 Elazor Elazor Elazor Fl Gl m Fl N-ox Elazor Elazor Fl N-ox Fl Gl m UDPGlcA UDP H+ NADPH O2 H+ NADP H2O Heme Heme Heme Heme Heme PW126614 Ren Exc Fluconazole ingested through a pill Blood Vessel Intestinal Lumin Hepatocyte Intestinal Epithelial Cell Only 6.5% become Glucuronidated metabolite, Fluconazole 2% become Fluconazole N-oxide Fluconazole is sent to target cells unchanged Fluconazole inhibits 4 Cytochrome exzymes which causes hepatotoxicity in the liver when taken frequently or with previous liver dysfunction Endoplasmic Reticulum membrane 93.3% of the dose, 80% as unchanged Fluconazole, is excreted through the urine
Endoplasmic Reticulum CYP3A4 CYP2C9 CYP2C19 CYP3A5 ABCB1 ABCB1 ABCB1 ABCB1 SLC15A1 ABCC3 UGT2B7 CYP1A2 Elazor Elazor Elazor Fl Gl m Fl N-ox Elazor Elazor Fl N-ox Fl Gl m UDPGlcA UDP H+ NADPH O2 H+ NADP H2O PW126614 Ren Exc