What is tolazamide? How does it work (mechanism of action)?

Tolazamide is used with diet and exercise to reduce blood glucose levels in adult patients with type 2 diabetes mellitus. Other diabetes drugs are sometimes used in combination with tolazamide if needed. Tolazamides initial effect is to increase beta-cell insulin secretion. Tolazamide causes the pancreas to produce insulin and increases the body’s response to it. Tolazamide also may decrease rate of hepatic glucose production, increases insulin receptor sensitivity, and increases number of insulin receptors.

  • There are no brand names for tolazamide.
  • Tolazamide is available in generic form.
  • You need a prescription to obtain tolazamide.

What is tolazamide used for?

Tolazamide is used with diet and exercise to reduce blood glucose levels in adult patients with type 2 diabetes mellitus.

What is the dosage for tolazamide?


  • Generally, patients are started on 100 to 250 mg of tolazamide once daily with breakfast or first meal of the day.
  • Start with 100 mg/day for fasting blood sugar <200 mg/dL or 250 mg for fasting blood sugar >200 mg/dL.
  • Use 100 mg/day for patients who are malnourished, underweight, elderly, or those not eating properly.
  • Dosage may be increased by 100-250 mg at weekly intervals.
  • The maximum daily dose is 500 mg orally twice daily (1000 mg/day).

The safety and efficacy of tolazamide has not been established in pediatric patients. No specific dose adjustments are recommended in patients with kidney or liver disease.

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Which drugs or supplements interact with tolazamide?

  • Coadministration of tolazamide with quinolone antibiotics may cause abnormal changes in blood glucose. Therefore, blood glucose must be closely monitored if these agents must be used together.
  • Tolazamide may increase blood levels of methotrexate (Rheumatrex, Trexall) by interfering with the binding of methotrexate to blood proteins.
  • Anti-retroviral protease inhibitors, a type of anti-HIV medication, may decrease the effectiveness of tolazamide and consequently worsen blood glucose control.

Is tolazamide safe to take during pregnancy or while breastfeeding?

  • There are no adequate studies of the effects of tolazamide for pregnant women.
  • It is not known if tolazamide is secreted in breast milk.

What else should you know about tolazamide?

What preparations of tolazamide are available?

Oral tablets: 100, 250, and 500 mg

How should I keep tolazamide stored?

Tablets should be stored at room temperature, between 15 C and 30 C (59 F to 86 F).


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Medically Reviewed on 11/29/2019


FDA Prescribing Information.