Introduction:
Sitagliptin was developed by Merck & Co. and approved for medical use in the United States in 2006. In 2020, it was the 74th most commonly prescribed medication in the United States, with more than 9 million prescriptions.
Sitagliptin, sold under the brand name Januvia among others, is an anti-diabetic medication used to treat type II diabetes. In the United Kingdom it is listed as less preferred than metformin or a sulfonylurea.It is taken by mouth.It is also available in the fixed-dose combination medication sitagliptin metformin (Janumet, Janumet XR).
Janumet and Janumet XR drugs are approved to improve blood sugar control in adults aged 18 and older with type II diabetes.
Sitagliptin is a medicine used to treat type II diabetes. Type II diabetes is a condition where the body does not make enough insulin, or the insulin that it makes does not work properly. This can cause high blood sugar levels (hyperglycaemia).
Metformin reduces the absorption of sugar from the stomach, reduces the release of stored sugar from the liver, and helps your body use sugar better. Sitagliptin helps to control blood sugar levels by increasing substances -incretins in the body that make the pancreas release more insulin.
It increases the amount of circulating incretins, which stimulate insulin secretion and inhibit glucose production. Sitagliptin was approved by the US Food and Drug Administration (FDA) for use with diet and exercise to improve glycemic control in adult patients with type II diabetes.
Sitagliptin reduces HbA1c levels:
In the study, HbA1c levels decreased by 0.56–0.67% at 3 months after sitagliptin add-on to the other oral anti-diabetic drugs. Therefore, sitagliptin add-on is considered a good option to decrease HbA1c levels in patients already treated with any drug regimens without GLP-1-based drugs.
Sitagliptin has no clinically significant impact on cardiovascular or CKD outcomes, irrespective of baseline eGFR.
Sitagliptin reduces the urine albumin-to-creatinine ratio in type II diabetes through decreasing both blood pressure and estimated glomerular filtration rate. J of Diabetes.
Side effects:
The most common side effect of sitagliptin, which happens in more than 1 in 100 people, is headaches. Talk to your doctor if headaches last longer than a week or are severe. If taking sitagliptin gives you a headache, make sure you rest and drink plenty of fluids. Do not drink too much alcohol.
Sitagliptin oral tablet is used for long-term treatment. It comes with serious risks if you don't take it as prescribed. If you don't take it at all: Your symptoms of type II diabetes may not improve or may even get worse.
Sitagliptin also reduced plasma glucose levels at 60 and 120 min during OGTT compared with glimepiride, while achieving a similar improvement in HbA1c during treatment. Body weight did not change in either of the two groups, and one case of hypoglycemia was observed in the glimepiride group.
Over time it gets harder to control blood sugar levels, so your doctor might eventually recommend stopping sitagliptin and trying a different treatment. Do not stop taking sitagliptin without speaking to your doctor.
Comparative efficacy of vildagliptin and sitagliptin in Japane:
After adjusting for baseline differences among trials of vildagliptin and sitagliptin in Japanese patients with type II diabetes, vildagliptin 50 mg twice daily was associated with significantly greater HbA(1c) reduction than sitagliptin 50 mg or 100 mg once daily.
Sitagliptin helps to control blood sugar levels by increasing substances in the body that make the pancreas release more insulin. It also signals the liver to stop producing sugar (glucose) when there is too much sugar in the blood.
Not used in type I diabetes patients:
This medicine does not help patients who have insulin-dependent or type I diabetes.
Mechanism of action:
Dipeptidyl peptidase-4 inhibitors
Sitagliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones released in response to a meal.By preventing breakdown of GLP-1 and GIP, they are able to increase the secretion of insulin and suppress the release of glucagon by the alpha cells of the pancreas.This drives blood glucose levels towards normal.] As the blood glucose level approaches normal, the amounts of insulin released and glucagon suppressed diminishes, thus tending to prevent an "overshoot" and subsequent low blood sugar (hypoglycemia), which is seen with some other oral hypoglycemic agents.
Information compiled by :
Dr. Bhairavsinh Raol
