Rosiglitazone pharmacokinetics

Cimetidine appears to reduce the clearance of metformin, and may have contributed to a case of metformin-associated lactic acidosis. Cimetidine did not alter repaglinide pharmacokinetics, and ranitidine did not alter pioglitazone or rosiglitazone pharmacokinetics. Acarbose did not alter ranitidine pharmacokinetics, but miglitol decreased the AUC of ranitidine by 60%. 

In 16 male volunteers aged 22-55 years, rosiglitazone 2 mg bd had no effect on the steady-state pharmacokinetics of oral metformin 500 mg bd there were no clinically significant episodes of hypoglycemia and blood lactic acid concentrations did not increase (150). 

Di Cicco RA, Allen A, Carr A, Fowles S, Jorkasky DK, Freed MI. Rosiglitazone does not alter the pharmacokinetics of metformin. J Clin Pharmacol 2000 40(ll) 1280-5. 

In 16 healthy men taking metformin 500 mg bd and/or rosiglitazone 2 mg bd for 4 days there were no significant effects on the steady-state pharmacokinetics of either drug (142). 

Chapelski MC, Thompson-Culkin K, Miller AK, Sack M, Blum R, Freed MI. Pharmacokinetics of rosiglitazone in patients with various degrees of renal insufficiency. J Clin Pharmacol 2003 43 252-9. 

Park J-Y, Kim K-A, Kang M-H, Kim S-L, Shin J-G. Pharmacokinetics and drug disposition. Effect of rifampi-cin on the pharmacokinetics of rosiglitazone in healthy subjects. Clin Pharmacol Ther 2004 75 157-62. 

Niemi M, Backman JT, Neuvonen PJ. Effects of trimethoprim and rifampicin on the pharmacokinetics of the cytochrome P450 2C8 substrate rosiglitazone. Clin Pharmacol Ther 2004 76 239 19. 

Kalliokoski, A., Neuvonen, M., Neuvonen, P.J. and Niemi, M. (2008) No significant effect of SLCOIBI polymorphism on the pharmacokinetics of rosiglitazone and pioglitazone. British Journal of Clinical Pharmacology, 65, 78-86. 

Isley WL, Oki JC (2000) Rosiglitazone and liver failure. Ann Intern Med 133 393 Izumi T, Enomoto S, Hoshiyama K, Sasahara K, Sugiyama Y (1997a) Pharmacokinetic stereoselectivity of troglitazone, an antidiabetic agent, in the KK mouse. Biophaim Drug Dispos... 

Rosiglitazone has been studied in combination with acarbose, digoxin, metformin, nifedipine, ranitidine, warfarin, and oral contraceptives [67,72] There have been no clinically significant effects on the pharmacokinetics of any of these agents in combination with rosiglitazone. 

Inglis AML, Miller AK, Culkin KT, et al. Rosiglitazone, a PPARy agonist, does not alter the pharmacokinetics of oral contraceptives [abstract 0443]. Diabetes. 2000 48(suppll) A103. 

Pioglitazone does not appear to alter the pharmacokinetics or anticoagulant effect of warfarin or phenprocoumon. Rosiglitazone did not affect the pharmacokinetics of warfarin. 

Rosiglitazone has been found to have no clinically relevant effect on the steady-state pharmacokinetics of warfarin. ... 

Miller AK, IngUs A Culkin KT, Jeekaksy DK, Freed MI. The effect of aearbose on the pharmacokinetics of rosiglitazone. EurJ Clin Pharmacol (2001) 57, 105-9. 

Pioglitazone or Rosi itazone. Rosiglitazone 8 mg daily for 2 weeks was found to have no clinically relevant effect on the pharmacokinetics of nifedipine in 28 healthy subjects. The manufacturer notes that pioglitazone 45 mg once daily for 7 days given with nifedipine extended-release 30 mg once daily for 4 days resulted in a small hut highly variable change in nifedipine pharmacokinetics. ... 

Some women may require small increases or decreases in their dosage of antidiabetic while taking oral contraceptives or HRT, but it is unusual for the control of diabetes to be seriously disturbed. Irrespective of diabetic control, HRT or oral contraceptives should be used with caution in patients with diabetes because of the increased risk of arterial disease. PiogUtazone, rosiglitazone and repaglinide do not appear to alter the pharmacokinetics of contraceptive steroids, and ethinylestradiol/levonoi estrel do not appear to have an important effect on the pharmacokinetics of repaglinide. 

Rosi itazone. Rosiglitazone 8 mg daily, given for the first two weeks of two cycles in 32 women taking an oral contraceptive (ethinylestradi-ol/norethisterone 35 micrograms/1 mg, Ortho-Novum), was found to have no effect on the pharmacokinetics of either steroid. ... 

No clinically relevant adverse interactions appear to have been reported between the statins and the sulphonylureas. One study reported an increased incidence of adverse effects with repaglinide and simvastatin, the clinical relevance of which is unclear. Most studies have shown no pharmacokinetic interaction or increased incidence of adverse effects when pioglitazone or rosiglitazone were used with atorvastatin or simvastatin. Subcutaneous exenatide modestly decreased the AUC of lovastatin, but no clear pattern of altered efficacy of statins was noted in exenatide clinical trials. 

However, in a study in healthy subjects, pioglitazone 45 mg daily did not significantly affect the pharmacokinetics of simvastatin 80 mg daily and concurrent use was well tolerated. Similarly, there was no pharmacokinetic interaction between pioglitazone 45 mg daily and atorvastatin 80 mg daily Moreover, clinical use of rosiglitazone with atorvastatin in patients with type 2 diabetes for 16 weeks was well tolerated, as was the clinical use of rosiglitazone or pioglitazone with simvastatin."... 

Sucralfate appears not to affect the pharmacokinetics of chlorpropamide or rosiglitazone. 

A single-dose study found that sucralfate 2 g taken 45 minutes before rosiglitazone 8 mg had no significant effect on the pharmacokinetics of rosiglitazone. No special precautions are needed during concurrent use. ... 

Rao MNVS, Mullangi R, Katneni K, vikanth B, Babu AP, Rani UP, Naidu MUR, Srinivas NR, Rajagopalan R. Lack of effect of sucralfate on the absorption and pharmacokinetics of rosiglitazone. J Clin Pharmacol (2002) 42, 670-5. 

Trimethoprim increases the AUC of repaglinide and would be expected to increase its effects in some patients. The effect of trimethoprim on the AUC of rosiglitazone is more modest and less likely to be clinically relevant. Trimethoprim does not appear to significantly affect the pharmacokinetics of intravenous tolbutamide. 

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