Oral Hypoglycemic Agents

Updated: Jul 09, 2021
  • Author: Abimbola Farinde, PharmD, PhD; more...
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Oral Antihyperglycemic Drugs

Oral antihyperglycemic agents lower glucose levels in the blood. They are commonly used in the treatment of diabetes mellitus. [1, 2]


  • Biguanides decrease hepatic glucose production, decrease gastrointestinal glucose absorption, and increase target cell insulin sensitivity

  • Example: Metformin [3, 4]

  • Contraindications: Metabolic acidosis with or without coma, abnormal creatinine clearance from any cause including diabetic ketoacidosis, shock, acute myocardial infarction, septicemia, renal disease (serum creatinine level ≥1.5 mg/dL in males or ≥1.4 mg/dL in females), lactation, radiologic contrast study within 48 hours


  • Sulfonylureas increase beta-cell insulin secretion, decrease hepatic glucose output, and increase insulin receptor sensitivity at peripheral target tissues

  • Contraindications: Sulfa allergy, type 1 diabetes, diabetic ketoacidosis, concomitant use with bosentan


  • Thiazolidinediones increase insulin receptor sensitivity and influence the production of gene products involved in lipid and glucose metabolism; their mechanism of action depends on the presence of insulin for activity [5]

  • Contraindications: Hypersensitivity to product or components, established NYHA class III/IV heart failure

Alpha-glucosidase inhibitors

  • Inhibit the upper gastrointestinal enzymes that convert dietary starch and other complex carbohydrates into simple sugars, which can be absorbed
  • Examples: Acarbose (Precose) & Miglitol (Glycet)
  • Contraindications: Diabetic ketoacidosis; cirrhosis; inflammatory bowel disease, colonic ulceration, partial intestinal obstruction,

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