DPP-4 inhibitors

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Author:
jcu1
ID:
236199
Filename:
DPP-4 inhibitors
Updated:
2013-09-24 19:30:46
Tags:
Endo
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Description:
Dr. Drab
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  1. DPP-4 inhibitor drugs
    • sitagliptin
    • saxagliptin
    • linagliptin
    • alogliptin
  2. DPP-4 MOA
    • inhibits DPP-4 enzyme - increases and prolong ative incretin levels
    • inc insulin release and dec glucagon secretion (glucose dependent)
  3. metabolism and elimination of DPP-4 inhibitor
    all renally excreted except linagliptin (excreted unchanged by enterohepatic system)
  4. sitagliptin contraindications
    nothing significant except hypersensitivity
  5. sitagliptin warning/precautions
    • pts with renal insufficiency (dosage adjustment in mod to severe renal insufficiency and ESRD)
    • use with meds that cause hypoglycemia (sulfonylureas)
    • hypersensitivity rxn with sitagliptin
    • pancreatitis
  6. sitagliptin DDIs
    none
  7. sitagliptin AEs
    hypoglycemia when in combo with sulfonylureas

    no other significant AEs
  8. DPP-4 inhibitor body weight
    no changes
  9. saxagliptin contraindications
    hypersensitivity
  10. saxagliptin precautions
    • be careful when used with a secretagogue
    • pancreatitis
  11. saxagliptin DDIs
    • coad with strong CYP3A4/5 inhibitors (ketoconazole) --> inc saxagliptin conc.
    • don't need to make adjustments when using with moderate inhibitors and inducers
  12. saxagliptin AEs
    • URI
    • UTI
    • headache
  13. linagliptin contraindication
    hypersensitivity
  14. linagliptin precautions
    hypoclycemia with secretagogue
  15. linagliptin DDI
    coadmin with strong P-GP and CYP3A4 inducer --> reduce efficacy of linagliptin (e.g. rifampin)
  16. linagliptin AEs
    • nasopharyngitis
    • arthralgia
    • back pain
    • headache
    • hypersensitivity
    • pancreatitis
  17. alogiptin contraindication
    hypersensitivity
  18. alogliptin warnings and precautions
    • hypoglycemia when with a secretagogue
    • pancreatitis
    • hepatic effects
  19. alogliptin excretiong
    renal
  20. alogliptin DDIs
    none
  21. alogliptin AE
    • nasopharyngitis
    • headache
    • URI

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