Antidiabetic Oral Medications

Oral Hypoglycemic Agents


Action Adverse Effects Remarks

1st Generation:

Chlorpropamide (Diabinese)

2n Generation:

Glyburide (DiaBeta)

Glipizide (Glucotrol)

  • Stimulates release of insulin.
  • Increases insulin receptor sensitivity.
  • Hypoglycemia
  • Wt gain
  • GI distress
  • Hepatotoxicity
  • Possible disulfirim reaction if taken concurrently with alcohol.
The sulfonamide component in the typical sulfa antibiotics is of a slightly different molecular structure than that in sulfonylureas. Although cross-reactivity is technically possible, current literature does not consider this likely, and sulfonylureas are typically well tolerated in patients with a sulfa allergy.

nateglinide (Starlix)

repaglinide (Prandin)

Stimulate insulin release.
  • Hypoglycemia
  • Upper resp infections
  • Flulike symptoms
  • Back pain
Short duration

Metformin – generic name – only drug in this class

Immediate release brand names:

Glucophage, Riomet

Extended release brand names:

Fortamet, Glucophage XR, and Glumetza

  • Delays gi uptake of glucose
  • Decreases gluconeogenesis
  • Decreases glycogenolysis
  • Decreases insulin resistance
  • Mostly GI: A/N/V/D
  • Metallic taste
  • Lactic acidosis – treat with hemodialysis

Does not cause wt gain and rarely causes hypoglycemia.

Should not be given to patients with impaired renal function, due to possibility of lactic acidosis.
Heart failure, liver failure, hx of lactic acidosis, or concurrent serious infections.
Two days before or after IV contrast.
Garlic and ginseng may increase hypoglycemia.
Alpha-Glucosidase Inhibitors

Acarbose (Precose)

Block enzyme action in small intestine inhibiting breakdown of complex CHO into mondosaccharides. CHO must be in monosaccharide form for absorption.
  • Mostly GI: flatulence, diarrhea, abdominal distention
  • Hypoglycemia
Hypoglycemia must be treated with glucose and not sucrose (table sugar).
Garlic and ginsing may increase hypoglycemia.
Thiazolidinediones (or glitazones)

Pioglitazone (Actos)

Rosiglitazone (Avandia)

  • Decreases insulin resistance.
  • Inhibits hepatic gluconeogenesis.
  • Fluid retention
  • Headache
  • Wt gain
  • Hepatotoxicity
  • Hypoglycemia rare
Monitor liver function
Heart failure

Source: Adams, M.P., & Holland, L.N. (2011). Pharmacology for nurses: A pathophysiologic approach. Pearson; Boston, Mass.
Pharm Oral Hypoglycemic Agents