Antidiabetic Agents Hypoglycemic Agents

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See also Antidiabetic Agents: Insulins. See also the following individual entries:


Chlorpropamide Glimepiride Glipizide Glyburide

Metformin hydrochloride Miglitol Tolazamide Tolbutamide Tolbutamide sodium Troglitazone Action/Kinetics: Oral hypoglyce-mic drugs are classified as either first or second generation. Generation refers to structural changes in the basic molecule. Second-generation oral hypoglycemic drugs are more lipophilic and, as such, have greater hypoglycemic potency.

The oral hypoglycemics are believed to act by one or more of the following mechanisms: (1) stimulating insulin release from pancreatic beta cells; (2) the peripheral tissues become more sensitive to insulin due to an increase in the number of insulin receptors or an increased ability of circulating insulin to combine with receptors; or (3) extrapancreatic effects, including decreased glucagon release and hepatic glucose production. To be effective, the client must have some ability for endogenous insulin production. Differences in oral hypoglycemic drugs are mainly in their pharmacokinetic properties and duration of action. Uses: Non-insulin-dependent diabetes mellitus (type II) that does not respond to diet management alone. Concurrent use of insulin and an oral hypoglycemic for type II diabetics who are difficult to control with diet and sulfonylurea therapy alone. Contraindications: Stress before and during surgery, ketosis, severe trauma, fever, infections, pregnancy, diabetes complicated by recurrent episodes of ketoacidosis or coma; juvenile, growth-onset, insulin-dependent, or brittle diabetes; impaired endocrine, renal, or liver function. Use in diabetics who can be controlled by diet alone. Relapse may occur with the sulfonylureas in undernourished clients. Long-acting products in geriatric clients. Special Concerns: Use with caution in debilitated and malnourished clients and during lactation since hy-poglycemia may occur in the infant. Safety and effectiveness in children have not been established. Geriatric clients may be more sensitive to oral hypoglycemics and hypoglycemia may be more difficult to recognize in these clients. Use of sulfonylureas has been associated with an increased risk of CV mortality compared to treatment with either diet alone or diet plus insulin. There may be loss of blood glucose control if the client experiences stress such as infection, fever, surgery, or trauma. Side Effects: Hypoglycemia is the most common side effect. GI: Nausea, heartburn, full feeling. CNS: Fatigue, dizziness, fever, headache, weakness, malaise, vertigo. Hepatic: Cholestatic jaundice, aggravation of hepatic porphyria. Dermatologic: Skin rashes, urticaria, erythema, pruritus, eczema, photophobia, mor-billiform or maculopapular eruptions, lichenoid reactions, porphyria cutanea tardia. Hematologic: Throm-bocytopenia, leukopenia, agranulo-cytosis, aplastic anemia, pancytopenia, hemolytic anemia. Endocrine: Inappropriate secretion of ADH resulting in excessive water retention, hyponatremia, low serum os-molality, and high urine osmolality. Miscellaneous: Paresthesia, tinnitus, resistance to drug action develops in a small percentage of clients.

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