SCHOOL OF MEDICINE

Department of Medicine

Clinical Pharmacology

2C8 REFERENCES

 2C8 SUBSTRATES: 

AMODIAQUINE
Fluvoxamine-tricyclic antidepressant interaction. An accidental finding. [ PMID 11805197 ]
Li XQ, Bjorkman A, Andersson TB, Ridderstrom M, Masimirembwa CM.
J Pharmacol Exp Ther. 2002 Feb;300(2):399-407.

CERIVASTATIN
Clinical pharmacokinetics of cerivastatin. [ PMID 10976657 ]
Mück W.
Clin Pharmacokinet. 2000 Aug;39(2):99-116.

Gemfibrozil inhibits CYP2C8-mediated cerivastatin metabolism in human liver microsomes. [ PMID 12433802 ]
Wang JS, Neuvonen M, Wen X, Backman JT, Neuvonen PJ.
Drug Metab Dispos. 2002 Dec;30(12):1352-6.

PACLITAXEL
Paclitaxel metabolism in rat and human liver microsomes is inhibited by phenolic antioxidants. [ PMID 12920504 ]
Vaclavikova R, Horsky S, Simek P, Gut I.
Naunyn Schmiedebergs Arch Pharmacol. 2003 Sep;368(3):200-9.

REPAGLINIDE
CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. [ PMID 12919179 ]
Bidstrup TB, Bjornsdottir I, Sidelmann UG, Thomsen MS, Hansen KT.
Br J Clin Pharmacol. 2003 Sep;56(3):305-14.

Polymorphism in CYP2C8 is associated with reduced plasma concentrations of repaglinide. [ PMID 14534525 ]
Niemi M, Leathart JB, Neuvonen M, Backman JT, Daly AK, Neuvonen PJ.
Clin Pharmacol Ther. 2003 Oct;74(4):380-7.

SORAFENIB
Prescribing Information

TORSEMIDE
The xenobiotic inhibitor profile of cytochrome P4502C8. [ PMID 11136296 ]
Ong CE, Coulter S, Birkett DJ, Bhasker CR, Miners JO.
Br J Clin Pharmacol. 2000 Dec;50(6):573-80.
 

 2C8 INHIBITORS: 

GEMFIBROZIL
Gemfibrozil inhibits CYP2C8-mediated cerivastatin metabolism in human liver microsomes. [ PMID 12433802 ]
Wang JS, Neuvonen M, Wen X, Backman JT, Neuvonen PJ.
Drug Metab Dispos. 2002 Dec;30(12):1352-6.

Gemfibrozil greatly increases plasma concentrations of cerivastatin. [ PMID 12496749 ]
Backman JT, Kyrklund C, Neuvonen M, Neuvonen PJ.
Clin Pharmacol Ther. 2002 Dec;72(6):685-91.

Gemfibrozil considerably increases the plasma concentrations of rosiglitazone. [ PMID 12898007 ]
Niemi M, Backman JT, Granfors M, Laitila J, Neuvonen M, Neuvonen PJ.
Diabetologia. 2003 Oct;46(10):1319-23.

GLITAZONES (thiazolidinediones)
Comparative effects of thiazolidinediones on in vitro P450 enzyme induction and inhibition. [ PMID 12642470 ]
Sahi J, Black CB, Hamilton GA, Zheng X, Jolley S, Rose KA, Gilbert D, LeCluyse EL, Sinz MW.
Drug Metab Dispos. 2003 Apr;31(4):439-46.

MONTELUKAST
Selective inhibition of human cytochrome P4502C8 by montelukast. [ PMID 15608135 ]
Walsky RL, Obach RS, Gaman EA, Gleeson JP, Proctor WR.
Drug Metab Dispos. 2005 Mar;33(3):413-8.

QUERCETIN
Human cytochrome P450s involved in the metabolism of 9-cis- and 13-cis-retinoic acids. [ PMID 11911845 ]
Marill J, Capron CC, Idres N, Chabot GG.
Biochem Pharmacol. 2002 Mar 1;63(5):933-43.

TRIMETHOPRIM
Trimethoprim and sulfamethoxazole are selective inhibitors of CYP2C8 and CYP2C9, respectively. [ PMID 12019187 ]
Wen X, Wang JS, Backman JT, Laitila J, Neuvonen PJ.
Drug Metab Dispos. 2002 Jun;30(6):631-5.

Effects of trimethoprim and rifampin on the pharmacokinetics of the cytochrome P450 2C8 substrate rosiglitazone. [ PMID 15371985 ]
Niemi M, Backman JT, Neuvonen PJ..
Clin Pharmacol Ther. 2004 Sep;76(3):239-49.

The effect of trimethoprim on CYP2C8 mediated rosiglitazone metabolism in human liver microsomes and healthy subjects. [ PMID 15606443 ]
Hruska MW, Amico JA, Langaee TY, Ferrell RE, Fitzgerald SM, Frye RF.
Br J Clin Pharmacol. 2005 Jan;59(1):70-9.

The CYP2C8 inhibitor trimethoprim increases the plasma concentrations of repaglinide in healthy subjects. [ PMID 15025742 ]
Niemi M, Kajosaari LI, Neuvonen M, Backman JT, Neuvonen PJ.
Br J Clin Pharmacol. 2004 Apr;57(4):441-7.
 

 2C8 INDUCERS: 

RIFAMPICIN
Expression and Induction of CYP2C P450 Enzymes in Primary Cultures of Human Hepatocytes. [ PMID 12130704 ]
J Pharmacol Exp Ther. 2002 Aug;302(2):475-82.