Oral Antidiabetics

Oral antidiabetic drugs such as sulfonylureas are administered to patients who have Type 2 diabetes mellitus to stimulate beta cells to secrete insulin. This results in an increase in insulin cell receptors, enabling cells to bind to insulin during glucose metabolism. Sulfonylureas are chemically related to sulfonamides but lack antibacterial activity.

Sulfonylureas are classified as first- and second-generation drugs and each generation is divided into short-acting, intermediate-acting, and long-acting antidiabetics.

First-generation sulfonylureas are:

• Tolbutamide (Orinase)

• Acetohexamide (Dymelor)

• Tolazamide (Tolinase)

• Chlorpropamide (Diabinese)

Second-generation sulfonylureas include

• Glipizide (Glucotrol)

• Glyburide nonmicronized (DiaBeta, Micronase)

Second-generation sulfonylureas increase tissue response to insulin and decrease glucose production by the liver. This results in greater hypoglycemic potency at smaller doses. Second-generation sulfonylureas have a longer duration of action and cause few side effects, but should not be used if the patient has liver or kidney dysfunction.

Nonsulfonylureas are new drugs that affect the hepatic and GI production of glucose. For example, metformin (Glucophage) is a nonsulfonylurea biguanide compound that acts by decreasing hepatic production of glucose from stored glycogen. The result is a reduced increase in serum glucose following a meal and limits the degree of post-prandial (after a meal) hyperglycemia.

Metformin (Glucophage) also decreases the absorption of glucose from the small intestine and may increase insulin receptor sensitivity as well as peripheral glucose uptake at the cellular level. Metformin does not produce hypoglycemia or hyperglycemia and can cause GI disturbances. Metformin can be used alone. When combined with a sulfonylurea, however, it is useful in cases resistant to oral antidiabetics.

Alpha-glucosidase inhibitors (acarbose [Precose]) inhibit alpha glucosidase, the digestive enzyme in the small intestine that is responsible for the release of glucose from the complex carbohydrates in the diet. By inhibiting alpha glu-cosidase, carbohydrates cannot be absorbed and instead, pass into the large intestine. Acarbose has no systemic effects, is not absorbed into the body in significant amounts, and does not cause a hypoglycemic reaction.

Thiazolidinediones such as Pioglitazone (Actos), decrease insulin resistance and help muscle cells to respond to insulin and use glucose more effectively. Thiazolidinediones may be used in addition to sulfonylurea, metformin, or insulin for insulin-resistant patients. Pioglitazone (Actos) has no significant side effects or adverse effects.

Rapaglinide (Prandin) is used alone or in combination with metformin as a short-acting similar to sulfonylureas, however Rapaglinide does not cause a hypoglycemic reaction.

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