Sitagliptin : Uses, Interactions, Mechanism Of Action

Sitagliptin: Uses, Interactions, Mechanism Of Action

Sitagliptin belongs to the group of oral antidiabetic agents, which is applied for the treatment of type 2 diabetes mellitus in adults. Sitagliptin regulates blood glucose levels by enhancing the secretion of insulin in the pancreas and reducing the generation of glucose by the liver. The drug is usually prescribed together with the use of a proper diet and exercise to have beneficial effects on the glycaemic level in diabetes.

USES

The primary use of sitagliptin is to improve glycaemic control in adults with type 2 diabetes. It is not suitable for use in type 1 diabetic patients because it is developed for managing type 2 diabetes patients with endogenous insulin secretion. Sitagliptin alleviates blood glucose concentrations decreasing the chances of cardiovascular diseases, kidney, nerve and retinopathy complications among diabetic patients. Sitagliptin is typically used as a second-line treatment in cases where other methods such as diet and exercise, and medications do not suffice to regulate the blood glucose levels well enough. There are different dosages of the medication, and it is approved as an individual pill or as a combination with other drugs.

MECHANISM OF ACTION

Sitagliptin operates by blocking the enzyme that breaks down incretin hormones in the body known as dipeptidyl peptidase-4 (DPP-4). These hormones are useful in the maintenance of glucose homeostasis by promoting the release of insulin from pancreatic beta cells and inhibiting glucagon synthesis. Inhibition of DPP-4 prolongs the persistence of incretins that in turn stimulates insulin secretion and suppresses glucagon. Sitagliptin works by inhibiting DPP-4, thereby raising the levels of endogenous incretin hormones in the body thus enhancing glycaemic control in patients with type 2 diabetes. This helps in reducing blood sugar levels and consequently reducing the risks associated with the disease.

INTERACTION

Sitagliptin is generally well-tolerated, but certain drug interactions and adverse effects should be noted:

Other Antidiabetic Medications: When used in combination with antibiotic drugs like sulfonylureas or insulin, there is an increased risk of hypoglycaemia. In such cases, healthcare providers may consider reducing the dose of sulfonylurea or insulin to mitigate this risk.

ACE Inhibitors: There have been reports of increased risk of angioedema in patients taking DPP-4 inhibitors and ACE inhibitors at the same time. Patients should be monitored for any symptoms that may arise as a result of consuming these drugs.

Digoxin: Sitagliptin may increase plasma concentrations of digoxin, a medication used to treat heart conditions. It is recommended to monitor digoxin levels if these two drugs are used together.

Corticosteroids and Diuretics: These medications can affect blood glucose control, potentially reducing the effectiveness of sitagliptin or necessitating adjustments in dosing.

Sitagliptin is usually well-tolerated but can have some side effects. Common side effects include upper respiratory infections, headaches, and gastrointestinal symptoms such as nausea. Although rare, serious side effects can include pancreatitis, hypersensitivity reactions, and kidney dysfunction. Patients should be monitored regularly for signs of pancreatitis, such as severe abdominal pain.