Dosing and uses of Tolinase (tolazamide)
Adult dosage forms and strengths
tablet
- 250mg
- 500mg
Type 2 Diabetes
100-250 mg PO qDay or q12hr
Increase dose by 100-250 mg/day at weekly intervals to response; not to exceed 1 g/day
Fasting blood sugar <200 mg/dL
- 100 mg/day PO
Fasting blood sugar >200 mg/dL
- 250 mg/day PO
Malnurished, underweight, not eating properly, or elderly
- 100 mg/day PO
Pediatric dosage forms and strengths
Safety and efficacy not established
Geriatric dosage forms and strengths
Type 2 diabetes
100-250 mg PO qDay or q12hr
Increase dose by 100-250 mg/day at weekly intervals to response; not to exceed 1 g/day
Fasting blood sugar <200 mg/dL
- 100 mg/day PO
Fasting blood sugar >200 mg/dL
- 250 mg/day PO
Malnurished, underweight, not eating properly, or elderly
- 100 mg/day PO
Tolinase (tolazamide) adverse (side) effects
Frequency not defined
Hypoglycemia
Dermatologic reactions
Heartburn
Dizziness
Vertigo
Anorexia
Constipation
Nausea/vomiting
Cholestatic jaundice and hepatitis may occur rarely which may progress to liver failure
Warnings
Contraindications
Hypersensitivity, sulfa allergy
Type I diabetes, diabetic ketoacidosis
Cautions
Patients with hypoglycemia, stress due to infection, fever, trauma, or surgery
May cause loss of glycemic control due to secondary failure
First generation sulfonylurea
Intermediate acting agent
Tolazamide demonstrates weak diuretic effect
Pregnancy and lactation
Pregnancy category: C
Lactation: not known if crosses into breast milk, avoid
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Tolinase (tolazamide)
Mechanism of action
Initial effect is to increase beta-cell insulin secretion
May also decrease rate of hepatic glucose production, increases insulin receptor sensitivity, and increases number of insulin receptors
Pharmacokinetics
Half-Life: 7 hr
Duration: 14-24 hr
Onset: 20 minutes
Protein binding: 94%
Peak hypoglycemic effect: 4-6 hr
Metabolism: Hepatic to less active metabolites
Metabolites: Inactive metabolites
Excretion: Urine (85%); feces (7%)
