Tolbutamide

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Denmark: Arcosal; Germany: Orabet; Italy: Tolbutam; Luxembourg: Rastinon; Malta: Tolbutamide; Netherlands: Tolbutamid; Poland: Diabetol; Slovakia: Dirastan; UK: Tolbutamide.

North America

Canada: Tolbutamide; USA: Tolbutamide.

Latin America

Mexico: Artosin, Dabetil, Diatelan, Diaval, Flusan, Rastinon.

Asia

Japan: Butamide, Diabetose, Rastinon.

Drug combinations

Chemistry

Tolbutamide: C~12~H~18~N~2~O~3~S. Mw: 270.35. (1) Benzenesulfonamide, N-[(butylamino)carbonyl]-4-methyl-; (2) 1-Butyl-3-(p-tolylsulfonyl)urea. CAS-64-77-7.

Pharmacologic Category

Diagnostic Agents; Pancreatic Function. Antidiabetic Agents; Sulfonylureas. (ATC-Code: A10BB03; V04CA01).

Mechanism of action

Stimulates insulin release from pancreatic β-cells. Reduces glucose output from liver. Insulin sensitivity increased at peripheral target sites, suppression of glucagon may also contribute.

Therapeutic use

Adjunct to diet for management of type 2 diabetes mellitus (non-insulin-dependent).

Pregnancy and lactiation implications

Adverse events observed in animal studies. Crosses placenta. Teratogenic effects noted in some case reports. Use of oral agents generally not recommended as routine management of gestational diabetes mellitus or type 2 diabetes mellitus during pregnancy. Insulin is drug of choice for control of diabetes mellitus during pregnancy. Enters breast milk (caution).

Unlabeled use

Contraindications

Hypersensitivity to tolbutamide, sulfonylureas, or any component of the formulation. Treatment of type 1 diabetes. Diabetic ketoacidosis.

Warnings and precautions

All sulfonylurea drugs are capable of producing severe hypoglycemia (use with caution). Oral hypoglycemic drugs may be associated with increased cardiovascular mortality. It may be necessary to discontinue therapy and administer insulin if patient is exposed to stress (fever, trauma, infection, surgery). Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, loop diuretics (except ethacrynic acid). Use in patients with sulfonylurea allergy contraindicated; however, risk of cross-reaction exists in patients with allergy to any of these compounds (avoid use when previous reaction severe).

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