Tolbutamide pharmacokinetics

Miners, J. (2002). CYP2C9 polymorphism Impact on tolbutamide pharmacokinetics and response. Pharmacogenetics 12, 91-92. 

Tolcapone did not alter tolbutamide pharmacokinetics in a singledose study. 

Nagata, M., M. Hidaka, H. Sekiya, et al. 2007. Effects of pomegranate juice on human cytochrome P450 2C9 and tolbutamide pharmacokinetics in rats. Drug Metab. Dispos. 35(2) 302-305. 

Ishihara K, Kashida H, Yuzurihara M, et al. Interaction of drugs and Chinese herbs pharmacokinetic changes of tolbutamide and diazepam caused by extract of Angelica dahurica. J Pharm Pharmacol 2000 52 1023-1029. 

Dixit AA, Rao YM. Pharmacokinetic interaction between diltiazem and tolbutamide. Drug Metabol Drug Interact 1999 15(4) 269-77. 

Nishimura, N., et al. 2004. Transepithelial permeation of tolbutamide across the human intestinal cell line, Caco-2. Drug Metab Pharmacokinet 19 48. 

The tolbutamide test has the most convincing ability to discriminate between genotype variants and pharmacokinetics. There could be an analytical issue linked to the urine assay precision, as the urinary concentrations of the parent drug are very low in comparison with those of its metabolites. 

Sugita O, Sawada Y, Sugiyama Y, Iga T, Hanano M. 1982. Physiologically based pharmacokinetics of drug-drug interaction a study of tolbutamide-sulfonamide interaction in rats. J Pharmacokinet Biopharm 10 297-316. 

Not known. Based on in vitro data, both entacapone and tolcapone were thought to potentially interfere with the metabolism of drugs by the cytochrome P450 isoenzyme CYP2C9, such as 5-warfarin. " However, the above study shows that entacapone does not alter 5-warfarin pharmacokinetics, and tolcapone is also thought not expected to interact by this mechanism because it does not interact with tolbutamide , (p.516), another CYP2C9 substrate. 

Glibenclamide (glyburide) causes a small reduction in valsartan plasma levels, but this is unlikely to be of any clinical significance. No clinically relevant pharmacokinetic interaction occurs between glibenclamide and candesartan or tehnisartan, or between tolbutamide and irbesartan. Eprosartan does not alter the efficacy of glibenclamide. Losartan and possibly eprosartan may reduce awareness of hypoglycaemic symptoms. 

Dextropropoxyphene doe not appear to affect the pharmacokinetics of tolbutamide. Hypoglycaemia was seen in a patient taking an unnamed sulphonylurea with co-proxamol, and has also been reported in non-diabetic patients given dextropropoxyphene alone. 

Disulfiram appears not to affect the control of diabetes mellitus. Disulfiram does not appear to affect the pharmacokinetics of tolbutamide and there appears to be no evidence that disulfiram interacts with any other antidiabetics. 

The pharmacokinetics of tolbutamide 250 mg daily for 4 days were not significantly changed in 7 healthy subjects when cimetidine 800 mg daily was added for a further 4 days. Other studies also found no pharmacokinetic interaction between tolbutamide and cimetidine, or between tolbutamide and ranitidine, and the hypoglycaemic activity of tolbutamide remained unaltered by cimetidine. ... 

Jayasagar G, Dixit AA, Kirshan V, o YM. Effect of claritiiromycin on the pharmacokinetics of tolbutamide. Drug Metcdrol Drug Interact (2000) 16,207-15. 

Tremaine LM, Wilner KD, Preskom SH. A stucfy of the potential effect of sertraline on the pharmacokinetics and protein binding of tolbutamide. Clin Pharmacc net ( 99T)32 (Su f>l 1), 31-6. 

A single 1-g oral dose of tolbutamide was given to two groups of 16 healthy subjects taking fluvastatin 40 mg or simvastatin 20 mg. The pharmacokinetics of the tolbutamide were affected only to a very minor extent, and the blood glucose-lowering effects of the tolbutamide were unchanged." ... 

A detailed study of the pharmacokinetics of tolbutamide in 6 healthy subjects found that sulfinpyrazone 200 mg every 6 hours for a week, almost doubled the half-life of a 500-mg intravenous dose of tolbutamide, from 7.3 to 13.2 hours, and reduced the plasma clearance by 40%. ... 

The blood glucose-lowering effects of some of the sulphonylureas are increased by some, but not all, sulfonamides, due to inhibition of their metabolism. However, sulfaphenazole, which was shown to have an important pharmacokinetic interaction with tolbutamide, is no longer used clinically, and other sulfonamides appear less likely to interact. Nevertheless, occasionally and unpredicta-... 

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. 

Echinacea does not have a clinically relevant effect on the pharmacokinetics of tolbutamide. 

In a pharmacokinetic study, 12 healthy subjects were given Echinacea purpurea root 400 mg four times daily for 8 days with a single 500-mg dose of tolbutamide on day 6. The AUC of tolbutamide was increased by 14%, and the time to maximum levels was increased from 4 to 6 hours. ... 

Chlorpropamide appears to reduce the serum levels of carbenoxolone. Tolbutamide does not appear to have any significant effect on the pharmacokinetics of carbenoxolone. 

---