tolbutamide (Orinase)
Jump to navigation
Jump to search
Introduction
Tradename: Orinase.
Indications
- management of non-insulin dependent diabetes mellitus (especially useful in patients with renal insufficiency)
- islet cell tumor
Dosage
250-3000 mg/day PO divided QD-TID
Tabs: 500 mg. Pharmocokinetics:
- peak hypoglycemic action: 1-3 hours after PO dose
- metabolized in the liver by cyt P450 2C9
- duration of action: 12 hours
Adverse effects
- common (> 10%)
- headache, constipation, diarrhea, heartburn, anorexia, epigastric fullness, dizziness
- less common (1-10%)
- uncommon (< 1%)
- aplastic anemia, hemolytic anemia, bone marrow suppression, cholestatic jaundice, thrombocytopenia, agranulocytosis, hypoglycemia, venospasm, thrombophlebitis, disulfiram- like reaction, leukopenia, tinnitus, SIADH, hypersensitivity
Drug interactions
- agents which increase risk of hypoglycemia
- any drug which inhibits cyt P450 2C9 can increase tolbutamide levels
- any drug which induces cyt P450 2C9 can diminish tolbutamide levels
- drug interaction(s) of sulfonylureas with warfarin
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of fluroquinolones with sulfonylureas
- drug interaction(s) of macrolides with sulfonylureas
- drug interaction(s) of salicylates with sulfonylureas
- drug interaction(s) of gliptins with sulfonylureas
- drug interaction(s) of fluoroquinolones with hypoglycemic agents
Laboratory
Mechanism of action
- 1st generation sulfonylurea.
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Deprecated Reference