Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats

Drug Metabolism and Disposition

Volumn 36, Issue 6, 2008, Pages 1097-1101

  Quinney, Sara K ^a   Galinsky, Raymond E ^a,b,d   Jiyamapa Serna, Vanida A ^c   Chen, Yong ^a,b,c,d   Hamman, Mitchell A ^a   Hall, Stephen D ^a,e   Kimura, Robert E ^c  

^a INDIANA UNIVERSITY   (United States)

^b PURDUE UNIVERSITY   (United States)

^c RUSH UNIVERSITY MEDICAL CENTER   (United States)

^d WISHARD MEMORIAL HOSPITAL   (United States)

^e ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 3A; HYDROXYITRACONAZOLE; ITRACONAZOLE; MIDAZOLAM;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG METABOLISM; ENZYME INHIBITION; FIRST PASS EFFECT; HEPATIC VEIN; HYDROXYLATION; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; ANTIFUNGAL AGENTS; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 CYP3A; INTESTINES; ITRACONAZOLE; LIVER; MALE; RATS; RATS, SPRAGUE-DAWLEY;

RATTUS;

EID: 44149087132     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.108.020644     Document Type: Article

References (15)

1. Beno DW, Uhing MR, Goto M, Chen Y, Jiyamapa-Serna VA, and Kimura RE (2001) Endotoxin-induced reduction in biliary indocyanine green excretion rate in a chronically catheterized rat model. Am J Physiol Gastrointest Liver Physiol 280:G858-G865.
2. Dennison JB, Jones DR, Renbarger JL, and Hall SD (2007) Effect of CYP3A5 expression on vincristine metabolism with human liver microsomes. J Pharmacol Exp Ther 321:553-563.
3. Esguerra LEO, Beno DWA, Deriy L, Kimura RE, and Uhing MR (2000) The effect of surgical stress on the endotoxin-induced interferon-gamma response. Shock 14:561-564.
4. Hardin TC, Graybill JR, Fetchick R, Woestenborghs R, Rinaldi MG, and Kuhn JG (1988) Pharmacokinetics of itraconazole following oral administration to normal volunteers. Antimicrob Agents Chemother 32:1310-1313.
5. Heykants J, Van Peer A, Van de Velde V, Van Rooy P, Meuldermans W, Lavrijsen K, Woestenborghs R, Van Cutsem J, and Cauwenbergh G (1989) The clinical pharmacokinetics of itraconazole: an overview. Mycoses 32 (Suppl 1):67-87.
6. Isoherranen N, Kunze KL, Allen KE, Nelson WL, and Thummel KE (2004) Role of itraconazole metabolites in CYP3A4 inhibition. Drug Metab Dispos 32:1121-1131.
7. Poirier JM and Cheymol G (1998) Optimisation of itraconazole therapy using target drug concentrations. Clin Pharmacokinet 35:461-473.
8. Richter S, Vollmar B, Mucke I, Post S, and Menger MD (2001) Hepatic arteriolo-portal venular shunting guarantees maintenance of nutritional microvascular supply in hepatic arterial buffer response of rat livers. J Physiol 531:193-201.
9. Shaw AA, Hall SD, Franklin MR, and Galinsky RE (2002) The influence of L-glutamine on the depression of hepatic cytochrome P450 activity in male rats caused by total parenteral nutrition. Drug Metab Dispos 30:177-182.
10. Shin JH, Choi KY, Kim YC, and Lee MG (2004) Dose-dependent pharmacokinetics of itraconazole after intravenous or oral administration to rats: intestinal first-pass effect. Antimicrob Agents Chemother 48:1756-1762.
11. Templeton IE, Thummel KE, Kharasch ED, Kunze KL, Hoffer C, Nelson WL, and Isoherranen N (2008) Contribution of itraconazole metabolites to inhibition of CYP3A4 in vivo. Clin Pharmacol Ther 83:77-85.
12. Uhing MR, Beno DW, Jiyamapa-Serna VA, Chen Y, Galinsky RE, Hall SD, and Kimura RE (2004) The effect of anesthesia and surgery on CYP3A activity in rats. Drug Metab Dispos 32:1325-1330.
13. Uhing MR and Kimura RE (1995a) Active transport of 3-O-methyl-glucose by the small intestine in chronically catheterized rats. J Clin Invest 95:2799-2805.
14. Uhing MR and Kimura RE (1995b) The effect of surgical bowel manipulation and anesthesia on intestinal glucose absorption in rats. J Clin Invest 95:2790-2798.
15. Yoo SD, Kang E, Jun H, Shin BS, Lee KC, and Lee KH (2000) Absorption, first-pass metabolism, and disposition of itraconazole in rats. Chem Pharm Bull 48:798-801.