Search
tolazamide (Tolinase)
Tradename: Tolinase. 1st generation sulfonylurea.
Indications:
- treatment on non-insulin-dependent diabetes mellitus
Dosage:
1) start with 100-250 mg PO QD
2) max: 1000 mg QD or divided BID
3) best given QAM with morning meal
4) conservative dosing in patients with hepatic failure
Tabs: 100, 250, 500 mg.
Pharmacokinetics:
1) onset of action is within 4-6 hours
2) duration of action is 10-24 hours
3) > 98% protein binding
4) extensively metabolized by the liver
5) excreted in the urine
Adverse effects:
1) common (> 10%)
- headache, constipation, diarrhea, heartburn, anorexia, epigastric fullness, dizziness
2) less common (1-10%)
- rash, urticaria, photosensitivity
3) uncommon (< 1%)
- aplastic anemia, hemolytic anemia,
- bone marrow suppression
- cholestatic jaundice
- thrombocytopenia, agranulocytosis
- hypoglycemia
4) other [2]
- nausea/vomiting
Drug interactions:
1) drugs that may enhance hypoglycemic effect of tolazamide:
- anticoagulants, fluconazole, gemfibrozil
- H2 receptor antagonists, MAO inhibitors
- probenecid, salicylates, sulfonamides
- tricyclic antidepressants (TCA)
- alcohol (may cause disulfiram-type reaction when used in combination)
2) drugs that may diminish hypoglycemic effect of tolazamide:
- beta blockers, diazoxide, cholestyramine, hydantoins (phenytoin, dantrolene etc), rifampin, thiazide diuretics
Laboratory:
- tolazamide in specimen
- tolazamide in serum/plasma
- tolazamide in urine
Mechanism of action: stimulates insulin release from the pancreas
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with sulfonylureas
General
sulfonylurea
Properties
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 7 HOURS
protein-binding >98%
pregnancy-category C [
D ][
safety in lactation ?]
Database Correlations
PUBCHEM cid=5503
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998 - not on National VA formulary
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998