Short answer: Linagliptin has a half-life of about 12 hours (effective, for build-up); over 100 hours terminal. Levels peak about 1.5 hours after a dose. People vary, so treat these as estimates.
Linagliptin is a DPP-4 inhibitor, a tablet that helps lower blood sugar in type 2 diabetes by letting the body's own GLP-1 and GIP hormones act for longer. It is sold as Tradjenta, taken as one 5 mg tablet a day. Unlike sitagliptin, it is mostly cleared through the bile rather than the kidneys.
Also known as: Tradjenta.
Tradjenta comes as a single 5 mg tablet strength.
The FDA Tradjenta label approves it, with diet and exercise, to improve blood sugar control in adults with type 2 diabetes; it is not recommended in type 1 diabetes and has not been studied in people with a history of pancreatitis. The label dose is 5 mg once a day, with or without food, and the label recommends no dose change for kidney impairment. Strong drugs that speed up the CYP3A4 enzyme or P-gp, such as rifampin, can lower linagliptin to levels that likely do not work.
The label warns of pancreatitis, low blood sugar when combined with insulin or a sulfonylurea, serious allergic reactions, severe joint pain, bullous pemphigoid and heart failure seen with two other drugs in the class. In CARMELINA, a heart-safety trial in about 7,000 adults with type 2 diabetes and heart or kidney disease (median follow-up 2.2 years), the risk of heart attack, stroke or heart-related death was similar to placebo (hazard ratio 1.02). In that trial pancreatitis was reported in 0.3% on linagliptin versus 0.1% on placebo, and bullous pemphigoid in 0.2% versus none. The most common side effect in trials was nasopharyngitis.
The FDA Tradjenta label gives peak levels about 1.5 hours after a 5 mg dose. Linagliptin binds tightly to the DPP-4 enzyme, so its blood levels fall in two phases: a long terminal half-life of over 100 hours (about 200 hours at steady state) that does not cause build-up, and an effective half-life for build-up of about 12 hours. Absolute bioavailability is about 30%, and about 80% of a dose leaves through the bile and gut, with about 5% in the urine.
Numbers shown are taken from the source above. Half-life varies from person to person.
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