Which medications in the drug class Antidiabetics, Biguanides are used in the treatment of Type 2 Diabetes Mellitus?

Updated: Sep 27, 2021
  • Author: Romesh Khardori, MD, PhD, FACP; Chief Editor: George T Griffing, MD  more...
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Antidiabetics, Biguanides

These agents are considered the first choice for oral type 2 diabetes treatment. They reduce hyperglycemia by decreasing hepatic gluconeogenesis (primary effect) and increasing peripheral insulin sensitivity (secondary effect). They do not increase insulin levels or cause weight gain. Alone, they rarely cause hypoglycemia.

Biguanides are absorbed from the intestines and are not bound to plasma proteins. They are not metabolized and are rapidly eliminated by the kidneys. Drug levels increase markedly in renal insufficiency. Lactic acidosis is a rare, but serious, complication that may occur with drug accumulation.

Metformin (Glucophage, Fortamet, Glumetza, Riomet)

Metformin is used as monotherapy or in combination with sulfonylureas, thiazolidinediones, or insulin. It is taken with food to minimize adverse GI effects. Metformin is available in immediate-release and extended-release formulations, as well as in combination with other antidiabetic drugs.

Metformin is contraindicated in patients with impaired renal function, as indicated by a serum creatinine level of greater than 1.5 mg/dL in men or of more than 1.4 mg/dL in women, or an estimated GFR of less than 60 mL/min. It also should not be used within 48 hours of IV iodinated contrast medium.

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