Tolbutamide

DEA Class; Rx

Common Brand Names; Orinase

  • Antidiabetics, Sulfonylureas

First-generation oral sulfonylurea; least potent and shortest-acting sulfonylurea; lacks active metabolites
Used in adults for the treatment of type 2 diabetes mellitus; however, second-generation agents are preferred
May be useful in the elderly or patients with renal disease

Indicated for adjunctive treatment of type 2 diabetes mellitus not controlled by diet and exercise alone.

Hypersensitivity, sulfa allergy

Type I diabetes, diabetic ketoacidosis

  • Hypoglycemia
  • Dermatologic recations
  • Disulfiram-like reactions
  • Agranulocytosis
  • Hyponatremia
  • Aplastic anemia
  • Thrombocytopenia
  • Heartburn
  • Nausea/vomiting
  • Cholestatic jaundice and hepatitis may occur rarely which may progress to liver failure

Patients with hypoglycemia, when caloric intake is decreased or there is increased stress due to infection, fever, trauma, or surgery (may need to discontinue treatment)

Risk of cardiovascular mortality increases with oral hypoglycemic drug treatments compared to treatment with diet alone or diet plus insulin

Risk of sulfonylurea-induced hemolytic anemia may increase in patients iwth glucose-6-phosphate dehydrogenase deficiency

Pregnancy Category: C

Lactation: Controversial, avoid

Adults

3,000 mg/day PO.

Geriatric

3,000 mg/day PO.

Adolescents

Safety and efficacy have not been established.

Children

Safety and efficacy have not been established.

Tolbutamide

tablet

  • 25mg
  • 50mg
  • 100mg

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