Linagliptin

Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat diabetes mellitus type 2.[2] It is generally less preferred than metformin and sulfonylureas as an initial treatment.[2][3] It is used together with exercise and diet.[2] It is not recommended in type 1 diabetes.[2] It is taken by mouth.[2]

Linagliptin
Clinical data
Pronunciation/ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin
Trade namesTradjenta, Trajenta, others
Other namesBI-1356
AHFS/Drugs.comMonograph
MedlinePlusa611036
License data
Pregnancy
category
  • US: B (No risk in non-human studies)
    Routes of
    administration    		By mouth (tablets)
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Bioavailability~30% (Tmax = 1.5 hours)
    Protein binding75–99% (concentration-dependent)
    MetabolismMinimal (~10% metabolized)
    MetabolitesPharmacologically inactive
    Elimination half-life~24 hours
    ExcretionFeces (80%), urine (5%)[1]
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    Chemical and physical data
    FormulaC25H28N8O2
    Molar mass472.553 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    Common side effects include inflammation of the nose and throat.[2] Serious side effects may include angioedema, pancreatitis, joint pain.[3][2] Use in pregnancy and breastfeeding is not recommended.[3] Linagliptin is a dipeptidyl peptidase-4 inhibitor.[2] It works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[2]

    Linagliptin was approved for medical use in the United States in 2011.[2] In 2017, it was the 200th most commonly prescribed medication in the United States, with more than two million prescriptions.[4][5]

    Medical uses

    Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[6]

    Side effects

    Linagliptin may cause severe joint pain.[1][7]

    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.

    Trajenta's Prescribing Information[8] states the drug is contraindicated for people with bronchial hyperreactivity. Asthma is a form of bronchial hyperreactivity[9].

    Mechanism of action

    Linagliptin belongs to a class of drugs called DPP-4 inhibitors.

    Terminology

    Linagliptin is the INN.[10]

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    See also

    References
    1. "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016.
    2. "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 6 April 2019.
    3. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
    4. "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
    5. "Linagliptin - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
    6. "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010.
    7. "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". U.S. Food and Drug Administration (FDA). 2015-08-28. Retrieved 1 September 2015.
    8. https://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Tradjenta/Tradjenta.pdf?DMW_FORMAT=pdf)
    9. Bronchial hyperresponsiveness
    10. "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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