Chemistry:Linagliptin
 | |
| Clinical data | |
|---|---|
| Pronunciation | /ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin |
| Trade names | Tradjenta, Trajenta, Trazenta |
| Other names | BI-1356 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a611036 |
| License data |
|
| Routes of administration | By mouth |
| ATC code | |
| Legal status | |
| Legal status | |
| 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%)[5] |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C25H28N8O2 |
| Molar mass | 472.553 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 202 °C (396 °F) |
| |
| |
  (what is this?) (verify) | |
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.[7][8] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[7][9] It is taken by mouth.[7]
Common side effects include inflammation of the nose and throat.[7] Serious side effects may include angioedema, pancreatitis, joint pain.[9][7] Use in pregnancy and breastfeeding is not recommended.[9] Linagliptin is a dipeptidyl peptidase-4 inhibitor[7] that works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[7]
Linagliptin was approved for medical use in the United States,[10] Japan, the European Union, Canada, and Australia in 2011.[7][11] In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[12][13] From August 2021 linagliptin became available as a generic medicine in the US.[14]
Medical uses
Linagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[5]
Side effects
Common side effects of linagliptin may include:
Upper respiratory tract infection, Headache, Hypoglycemia, Joint pain, Allergic reactions.[5][15]
Mechanism of action
Linagliptin belongs to a class of drugs called DPP-4 inhibitors.[5] It is a reversible, competitive inhibitor of DPP-4. GLP-1 and the glucose-dependent insulinotropic polypeptide (GIP) are broken down more slowly when this enzyme is inhibited. While glucagon release from pancreatic beta cells is inhibited, GLP-1 and GIP promote the production of insulin from the organ's beta cells. Together, these effects improve insulin release in response to glucose and decrease the liver's breakdown of glycogen[16]
Names
Linagliptin is the international nonproprietary name (INN).[17] Trade names: Trajenta,[18] Tradjenta.
See also
- Empagliflozin/linagliptin
References
- ↑ "Linagliptin, tablet, 5 mg, Trajenta". July 2012. http://www.pbs.gov.au/info/industry/listing/elements/pbac-meetings/psd/2012-07/linagliptin.
- ↑ "AusPAR: Linagliptin". 21 June 2022. https://www.tga.gov.au/resources/auspar/auspar-linagliptin-0.
- ↑ "Trajenta Product information". 25 April 2012. https://health-products.canada.ca/dpd-bdpp/info.do?lang=en&code=85612.
- ↑ "Trajenta 5 mg film-coated tablets - Summary of Product Characteristics (SmPC)". 27 September 2021. https://www.medicines.org.uk/emc/product/4762/smpc.
- ↑ 5.0 5.1 5.2 5.3 5.4 "Tradjenta- linagliptin tablet, film coated". 21 April 2022. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f.
- ↑ "Trajenta EPAR". 17 September 2018. https://www.ema.europa.eu/en/medicines/human/EPAR/trajenta.
- ↑ 7.0 7.1 7.2 7.3 7.4 7.5 7.6 7.7 "Linagliptin Monograph for Professionals". American Society of Health-System Pharmacists. https://www.drugs.com/monograph/linagliptin.html.
- ↑ "Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus". The Annals of Pharmacotherapy 46 (3): 358–67. March 2012. doi:10.1345/aph.1Q522. PMID 22318932.
- ↑ 9.0 9.1 9.2 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 680. ISBN 9780857113382.
- ↑ "Drug Approval Package: Tradjenta (linagliptin) Tablets NDA #201280". 7 June 2011. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/201280Orig1s000TOC.cfm.
- ↑ "10 years". https://pro.boehringer-ingelheim.com/products/trajenta/10years#pre2011.
- ↑ "The Top 300 of 2020". https://clincalc.com/DrugStats/Top300Drugs.aspx.
- ↑ "Linagliptin - Drug Usage Statistics". https://clincalc.com/DrugStats/Drugs/Linagliptin.
- ↑ "Linagliptin: FDA-Approved Drugs". https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=208335.
- ↑ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". 28 August 2015. https://www.fda.gov/drugs/drug-safety-and-availability/fda-drug-safety-communication-fda-warns-dpp-4-inhibitors-type-2-diabetes-may-cause-severe-joint-pain.
- ↑ "Linagliptin" (in en). https://go.drugbank.com/drugs/DB08882.
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61". World Health Organization. p. 66. https://www.who.int/medicines/publications/druginformation/innlists/RL61.pdf.
- ↑ "Linagliptin: medicine to treat type 2 diabetes". 25 March 2022. https://www.nhs.uk/medicines/linagliptin/.
External links
- "Linagliptin". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/linagliptin.
 |  |
