Pioglitazone/sitagliptin

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An article about the combination medication Pioglitazone/sitagliptin used in the treatment of type 2 diabetes.


Pioglitazone/sitagliptin is a combination medication used in the management of type 2 diabetes mellitus. It combines two active ingredients: pioglitazone, a thiazolidinedione, and sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor. This combination is designed to improve glycemic control in adults with type 2 diabetes, particularly when diet and exercise alone do not provide adequate control.

Pharmacology[edit | edit source]

Pioglitazone[edit | edit source]

Pioglitazone is a member of the thiazolidinedione class of medications. It works primarily by increasing the sensitivity of liver, fat, and muscle cells to insulin, thereby enhancing glucose uptake and reducing blood glucose levels. Pioglitazone acts as an agonist of the peroxisome proliferator-activated receptor gamma (PPAR-γ), which plays a role in the regulation of glucose and lipid metabolism.

Sitagliptin[edit | edit source]

Sitagliptin is a dipeptidyl peptidase-4 inhibitor, which functions by inhibiting the DPP-4 enzyme. This inhibition increases the levels of incretin hormones, which are involved in the regulation of glucose homeostasis. Incretins, such as glucagon-like peptide-1 (GLP-1), increase insulin synthesis and release from pancreatic beta cells and decrease glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production.

Clinical Use[edit | edit source]

Pioglitazone/sitagliptin is indicated for the treatment of type 2 diabetes in adults. It is typically used when monotherapy with either pioglitazone or sitagliptin, along with diet and exercise, does not result in adequate glycemic control. The combination may also be used in conjunction with other antidiabetic medications, such as metformin or sulfonylureas, to achieve better control of blood sugar levels.

Side Effects[edit | edit source]

Common side effects of pioglitazone/sitagliptin include:

  • Weight gain
  • Edema
  • Upper respiratory tract infections
  • Headache

More serious side effects can include:

  • Heart failure, particularly in patients with pre-existing cardiac conditions
  • Bladder cancer, associated with long-term use of pioglitazone
  • Pancreatitis, a potential risk with sitagliptin

Contraindications[edit | edit source]

Pioglitazone/sitagliptin is contraindicated in patients with:

  • Type 1 diabetes
  • Diabetic ketoacidosis
  • Severe renal impairment
  • Active bladder cancer

Also see[edit | edit source]


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