Linagliptin

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Linagliptin
Linagliptin.svg
Clinical data
Pronunciation/ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin
Trade namesTradjenta, Trajenta, others
SynonymsBI-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 mass472.54 g/mol g·mol−1
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

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.[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]

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] A month supply in the United Kingdom costs the NHS about £33.26 as of 2019.[3] In the United States the wholesale cost of this amount is about 391 USD.[4] In 2016 it was the 196th most prescribed medication in the United States with more than 3 million prescriptions.[5]

Medical uses[edit]

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

Side effects[edit]

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][circular reference].

Mechanism of action[edit]

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

Terminology[edit]

Linagliptin is the INN.[10]

See also[edit]

References[edit]

  1. ^ a b "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016.
  2. ^ a b c d e f g h i j "Linagliptin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 6 April 2019.
  3. ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
  4. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
  5. ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
  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". 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.

External links[edit]