Linagliptin
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Pronunciation | /ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin |
Trade names | Tradjenta, Trajenta, Trazenta |
Other names | BI-1356 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a611036 |
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | ~30% (Tmax = 1.5 hours) |
Protein binding | 75–99% (concentration-dependent) |
Metabolism | Minimal (~10% metabolized) |
Metabolites | Pharmacologically inactive |
Elimination half-life | ~24 hours |
Excretion | Feces (80%), urine (5%)[6] |
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Chemical and physical data | |
Formula | C25H28N8O2 |
Molar mass | 472.553 g·mol−1 |
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Melting point | 202 °C (396 °F) |
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Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat type 2 diabetes (but not type 1) in conjunction with exercise and diet.[8][9] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[8][10] It is taken by mouth.[8]
Common side effects include inflammation of the nose and throat.[8] Serious side effects may include angioedema, pancreatitis, joint pain.[10][8] Use in pregnancy and breastfeeding is not recommended.[10] Linagliptin is a dipeptidyl peptidase-4 inhibitor[8] that works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[8]
Linagliptin was approved for medical use in the United States,[11] Japan, the European Union, Canada, and Australia in 2011.[8][12] In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[13][14] From August 2021 linagliptin became available as a generic medicine in the US.[15]
Medical uses
[edit]Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[6]
Side effects
[edit]Linagliptin may cause severe joint pain.[6][16]
Mechanism of action
[edit]Linagliptin belongs to a class of drugs called DPP-4 inhibitors.[6]
Names
[edit]Linagliptin is the international nonproprietary name (INN).[17] Brand names: Trajenta,[18] Tradjenta.
See also
[edit]References
[edit]- ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
- ^ "Linagliptin, tablet, 5 mg, Trajenta". Pharmaceutical Benefits Scheme (PBS). July 2012. Archived from the original on 31 March 2015. Retrieved 26 September 2014.
- ^ "AusPAR: Linagliptin". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 9 April 2023.
- ^ "Trajenta Product information". Health Canada. 25 April 2012. Archived from the original on 27 September 2021. Retrieved 3 October 2022.
- ^ "Trajenta 5 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 27 September 2021. Archived from the original on 19 January 2022. Retrieved 3 October 2022.
- ^ Jump up to: a b c d e "Tradjenta- linagliptin tablet, film coated". DailyMed. 21 April 2022. Archived from the original on 15 August 2022. Retrieved 3 October 2022.
- ^ "Trajenta EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 29 December 2019. Retrieved 11 February 2020.
- ^ Jump up to: a b c d e f g h "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 6 April 2019. Retrieved 6 April 2019.
- ^ Neumiller JJ (March 2012). "Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus". The Annals of Pharmacotherapy. 46 (3): 358–67. doi:10.1345/aph.1Q522. PMID 22318932. S2CID 207264493.
- ^ Jump up to: a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
- ^ "Drug Approval Package: Tradjenta (linagliptin) Tablets NDA #201280". U.S. Food and Drug Administration (FDA). 7 June 2011. Archived from the original on 3 April 2022. Retrieved 3 October 2022.
- ^ "10 years". Boehringer Ingelheim Limited. Archived from the original on 3 October 2022. Retrieved 3 October 2022.
- ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
- ^ "Linagliptin - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
- ^ "Linagliptin: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 25 September 2021. Retrieved 24 September 2021.
- ^ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". U.S. Food and Drug Administration (FDA). 28 August 2015. Archived from the original on 13 December 2019. Retrieved 1 September 2015.
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Archived (PDF) from the original on 3 October 2020. Retrieved 10 November 2016.
- ^ "Linagliptin: medicine to treat type 2 diabetes". NHS UK. 25 March 2022. Retrieved 21 November 2022.