The following agents are indicated for the treatment of type 2 diabetes, when used as directed by a clinician. NDEI members are advised that decisions regarding drug therapy are the responsibility of the clinician. These descriptions are provided for informational purposes only. The entire monograph for an agent should be reviewed for a thorough understanding of the drug's indications, actions, uses, and side effects.
a-Glucosidase Inhibitors
Acarbose (Precose®) is indicated as monotherapy as an adjunct to diet and exercise to lower blood glucose levels in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone. Acarbose may also be used in combination with a sulfonylurea when diet and exercise plus either acarbose or a sulfonylurea does not result in adequate glycemic control. In addition, acarbose may be used in combination with insulin or metformin.
Miglitol (Glyset®) is indicated as monotherapy as an adjunct to diet and exercise to lower blood glucose in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone. Miglitol may also be used in combination with a sulfonylurea when diet and exercise plus either miglitol or a sulfonylurea alone does not result in adequate glycemic control.
Biguanides
Metformin is indicated as monotherapy as an adjunct to diet and exercise to lower blood glucose levels in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone. Metformin may be used in combination with a sulfonylurea or insulin to improve glycemic control.
DPP-IV Inhibitors
Sitagliptin(Januvia™) is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Sitagliptin is also indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin or a PPAR-gamma agonist (e.g., thiazolidinediones) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Sitagliptin/metformin HCl (Janumet™) is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus who are not adequately controlled on metformin or sitagliptin alone or in patients already being treated with the combination of sitagliptin and metformin.
Incretin Mimetics
Exenatide (Byetta®) is indicated as adjunctive therapy to improve glycemic control in patients with type 2 diabetes mellitus who are taking metformin, a sulfonylurea, a thiazolidinedione, a combination of metformin and a sulfonylurea, or a combination of metformin and a thiazolidinedione, but have not achieved adequate glycemic control.
Insulin
Insulin, in its various forms (lispro [human]; human NPH; human regular; human regular and human NPH mixture; human [zinc suspension]; NPH; regular; and zinc suspension), is indicated as an adjunct to diet and exercise to lower blood glucose levels in patients with type 1 or 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone.
The various forms of insulin can be used in combination with various oral antidiabetic agents to regulate blood glucose levels.
Meglitinides
Repaglinide (Prandin®) is indicated as an adjunct to diet and exercise to lower blood glucose levels in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone. Repaglinide is also indicated for use in combination with metformin to lower blood glucose in patients whose hyperglycemia cannot be controlled by exercise, diet, and either repaglinide or metformin alone.
Sulfonylureas
First-Generation Agents Tolbutamide (Orinase®), tolazamide (Tolinase®), or chlorpropamide (Diabinese®). Indicated as an adjunct to diet and exercise to lower blood glucose levels in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone. Tolbutamide, tolazamide, or chlorpropamide may be used in combination with insulin when sulfonylurea monotherapy fails to reduce symptoms and/or blood glucose levels.
Second-Generation Agents Glipizide (Glucotrol®), glyburide, or glimepiride. Indicated as an adjunct to diet and exercise to lower blood glucose levels in patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone. Glipizide, glyburide, or glimepiride may be used in combination with insulin when sulfonylurea monotherapy fails to reduce symptoms and/or blood glucose levels.
Thiazolidinediones
Pioglitazone
WARNING: CONGESTIVE HEART FAILURE
Thiazolidinediones, including pioglitazone (Actos®), cause or exacerbate congestive heart failure in some patients. After initiation of Actos®, Actosplus Met™, or Duetact™ and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, the heart failure should be managed according to the current standards of care. Furthermore, discontinuation or dose reduction of Actos®, Actosplus Met™, or Duetact™ must be considered.
Actos®, Actosplus Met™, and Duetact™ are not recommended in patients with symptomatic heart failure. Initiation of Actos®, Actosplus Met™, or Duetact™ in patients with established NYHA Class III or IV heart failure is contraindicated.
Pioglitazone hydrochloride (Actos®) is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes (non-insulin-dependent diabetes mellitus, NIDDM). Pioglitazone hydrochloride is indicated for monotherapy. Pioglitazone hydrochloride is also indicated for use in combination with a sulfonylurea, metformin, or insulin when diet and exercise plus the single agent does not result in adequate glycemic control.
Pioglitazone hydrochloride and metformin hydrochloride (Actoplus Met™) is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes who are already treated with a combination of pioglitazone and metformin or whose diabetes is not adequately controlled with metformin alone, or for those patients who have initially responded to pioglitazone alone and require additional glycemic control.
Pioglitazone hydrochloride and glimepiride (Duetact™) is indicated as an adjunct to diet and exercise as a once-daily combination therapy to improve glycemic control in patients with type 2 diabetes who are already treated with a combination of pioglitazone and a sulfonylurea or whose diabetes is not adequately controlled with a sulfonylurea alone, or for those patients who have initially responded to pioglitazone alone and require additional glycemic control.
Rosiglitazone
WARNING: CONGESTIVE HEART FAILURE
Thiazolidinediones, including rosiglitazone (Avandia®), cause or exacerbate congestive heart failure in some patients. After initiation of Avandia®, Avandamet®, or Avandaryl™, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, the heart failure should be managed according to current standards of care. Furthermore, discontinuation or dose reduction of Avandia®, Avandamet®, or Avandaryl™, must be considered.
Avandia®, Avandamet®, and Avandaryl™, are not recommended in patients with symptomatic heart failure. Initiation of Avandia®, Avandamet®, or Avandaryl™, in patients with established NYHA Class III or IV heart failure is contraindicated.
Rosiglitazone maleate (Avandia®) is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Rosiglitazone maleate is indicated as monotherapy. Rosiglitazone maleate is also indicated for use in combination with a sulfonylurea, metformin, or insulin when diet, exercise, and a single agent do not result in adequate glycemic control. For patients inadequately controlled with a maximum dose of a sulfonylurea or metformin, rosiglitazone maleate should be added to, rather than substituted for, a sulfonylurea or metformin. Rosiglitazone maleate is also indicated for use in combination with a sulfonylurea plus metformin when diet, exercise, and both agents do not result in adequate glycemic control.
Rosiglitazone maleate and metformin hydrochloride (Avandamet®) is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus when treatment with dual rosiglitazone and metformin therapy is appropriate.
Rosiglitazone maleate and glimepiride (Avandaryl™) is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes who are already treated with a combination of rosiglitazone and sulfonylurea or who are not adequately controlled on a sulfonylurea alone or for those patients who have initially responded to rosiglitazone alone and require additional glycemic control.
Troglitazone
Troglitazone (Rezulin®) was the first in the thiazolidinediones class to be launched (March 1997), was taken off the market in March 2000.