Antihyperglycemic

Antihyperglycemic

Antihyperglycemic agents are a class of medications used to lower blood glucose levels in individuals with diabetes mellitus. These agents are primarily used in the management of type 2 diabetes, where the body becomes resistant to insulin or when the pancreas fails to produce enough insulin. Antihyperglycemic drugs work through various mechanisms to control blood sugar levels and prevent complications associated with diabetes.

Mechanisms of Action

Antihyperglycemic agents can be categorized based on their mechanisms of action:

Insulin Sensitizers

• Metformin: This is the most commonly used first-line medication for type 2 diabetes. Metformin works by decreasing hepatic glucose production and increasing insulin sensitivity in peripheral tissues.
• Thiazolidinediones (TZDs): These include drugs like pioglitazone and rosiglitazone. They improve insulin sensitivity by acting on the peroxisome proliferator-activated receptor gamma (PPAR-γ) in adipose tissue, muscle, and the liver.

Insulin Secretagogues

• Sulfonylureas: These drugs, such as glipizide and glyburide, stimulate the pancreas to release more insulin by closing ATP-sensitive potassium channels on the beta cells.
• Meglitinides: Similar to sulfonylureas, drugs like repaglinide and nateglinide stimulate insulin secretion but have a shorter duration of action.

Alpha-glucosidase Inhibitors

• Acarbose and Miglitol: These drugs delay the absorption of carbohydrates in the intestine by inhibiting the alpha-glucosidase enzyme, leading to a slower rise in blood glucose levels post-meal.

Dipeptidyl Peptidase-4 (DPP-4) Inhibitors

• Sitagliptin, Saxagliptin, and Linagliptin: These medications work by inhibiting the DPP-4 enzyme, which increases the levels of incretin hormones, thereby enhancing insulin secretion and decreasing glucagon levels.

Sodium-glucose Cotransporter-2 (SGLT2) Inhibitors

• Canagliflozin, Dapagliflozin, and Empagliflozin: These drugs lower blood glucose by preventing the reabsorption of glucose in the kidneys, leading to increased glucose excretion in the urine.

Glucagon-like Peptide-1 (GLP-1) Receptor Agonists

• Exenatide, Liraglutide, and Dulaglutide: These injectable medications mimic the incretin hormone GLP-1, which increases insulin secretion, decreases glucagon secretion, and slows gastric emptying.

Clinical Use

Antihyperglycemic agents are used in combination with lifestyle modifications such as diet and exercise to manage blood glucose levels in patients with type 2 diabetes. The choice of medication depends on various factors, including the patient's blood glucose levels, presence of comorbidities, risk of hypoglycemia, and patient preferences.

Side Effects

Common side effects of antihyperglycemic agents vary by class but may include:

• Metformin: Gastrointestinal upset, lactic acidosis (rare)
• Sulfonylureas: Hypoglycemia, weight gain
• Thiazolidinediones: Weight gain, edema, risk of heart failure
• SGLT2 Inhibitors: Genital infections, dehydration, ketoacidosis

Also see

• Diabetes mellitus
• Insulin therapy
• Hypoglycemia
• Glycemic index