Short answer: Sitagliptin has a half-life of about 12.4 hours. Levels peak about 1 to 4 hours after a dose. People vary, so treat these as estimates.
Sitagliptin is a DPP-4 inhibitor: it slows the breakdown of the gut hormones GLP-1 and GIP, which the body releases after meals, so they act for longer. It is sold as Januvia, a once-daily tablet for type 2 diabetes. It works on the same hormone system as GLP-1 drugs, but it is not a GLP-1 receptor agonist.
Also known as: Januvia.
Januvia comes as 25 mg, 50 mg and 100 mg tablets.
The FDA Januvia label approves it, with diet and exercise, to improve blood sugar control in adults with type 2 diabetes. It is not used in type 1 diabetes, and it has not been studied in people with a history of pancreatitis. The label dose is 100 mg once a day, with or without food. Because the kidneys clear it, the dose is 50 mg once a day when eGFR is 30 to under 45, and 25 mg once a day when eGFR is under 30 or on dialysis; the label says to check kidney function before starting and from time to time after.
The label warns of acute pancreatitis (including fatal cases), heart failure seen with two other drugs in the same class, acute kidney failure, serious allergic reactions, severe joint pain and bullous pemphigoid (a blistering skin condition). With insulin or a sulfonylurea, low blood sugar was more common than on placebo, and a lower dose of those may be needed. In trials, the side effects seen in at least 5% of people and more often than on placebo were upper respiratory infection, stuffy or runny nose with sore throat (nasopharyngitis) and headache.
The FDA Januvia label gives an apparent terminal half-life of about 12.4 hours after a 100 mg dose, with peak levels 1 to 4 hours after the dose (median). Absolute bioavailability is about 87%, and about 79% of a dose leaves the body unchanged in the urine, which is why the dose is lowered when kidney function is reduced.
Numbers shown are taken from the source above. Half-life varies from person to person.
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