|Trade names||Tradjenta, Trajenta, others|
|By mouth (tablets)|
|Bioavailability||~30% (Tmax = 1.5 hours)|
|Protein binding||75–99% (concentration-dependent)|
|Metabolism||Minimal (~10% metabolized)|
|Elimination half-life||~24 hours|
|Excretion||Feces (80%), urine (5%)|
|Chemical and physical data|
|Molar mass||472.54 g/mol g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat diabetes mellitus type 2. It is generally less preferred than metformin and sulfonylureas. It is used together with exercise and diet. It is not recommended in type 1 diabetes. It is taken by mouth.
Common side effects include inflammation of the nose and throat. Serious side effects may include angioedema, pancreatitis, joint pain. Use in pregnancy and breastfeeding is not recommended. Linagliptin is a dipeptidyl peptidase-4 inhibitor. It works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.
Linagliptin was approved for medical use in the United States in 2011. A month supply in the United Kingdom costs the NHS about £33.26 as of 2019. In the United States the wholesale cost of this amount is about 391 USD. In 2016 it was the 196th most prescribed medication in the United States with more than 3 million prescriptions.
The U.S. Food and Drug Administration (FDA) is warning that the type 2 diabetes medicines like sitagliptin, saxagliptin, linagliptin, and alogliptin may cause joint pain that can be severe and disabling. FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors.
Mechanism of action
Linagliptin belongs to a class of drugs called DPP-4 inhibitors.
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- "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 6 April 2019.
- British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
- "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
- "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
- "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010.
- "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.
- Bronchial hyperresponsiveness
- "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Retrieved 10 November 2016.
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