Therapeutics - T2DM 3

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kyleannkelsey
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290400
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Therapeutics - T2DM 3
Updated:
2014-12-01 23:15:56
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Therapeutics T2DM
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Therapeutics - T2DM
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Therapeutics - T2DM
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  1. What is the MOA of Gliptins?
    • Dipeptidyl Peptidase-4 Inhibitors
    • Inhibits the dipeptidyl peptidase-4 enzyme responsible for the breakdown of incretin hormones glucagon-like peptide 1 and glucagon glucose-dependent insulinotropic polypeptide.
  2. What is the indication of Sitagliptin (Januvia)?
    • Monotherapy
    • Combination with metformin, pioglitazone, or glimepiride
  3. What dosage forms are available for Sitagliptin (Januvia)?
    25-, 50-, and 100-mg tablets
  4. What is the dose of Sitagliptin (Januvia)?
    • 100 mg/day
    • Decrease dosage for moderate to severe renal insufficiency
    • ClCr ≥ 50 mL/min = 100 mg QD
    • ClCr ≥ 30 ≤ 50 = 50 mg QD
    • ClCr ≤ 30 = 25 mg QD
  5. What are the AE for Sitagliptin (Januvia)?
    • Hypoglycemia (not more than placebo)
    • Severe allergic reactions (e.g., angioedema, skin reactions).
    • Pancreatitis
    • Conflicting evidence: increases hospitalizations for heart failure
  6. Is Sitagliptin (Januvia) expensive or cheap?
    Expensive
  7. What is the efficacy of Sitagliptin (Januvia)?
    • Decreases A1C by about 0.5%–0.8% in monotherapy.
    • In combination with metformin, provided an additional 0.67%
    • FBG decreased by 16.2 mg/dL, and 2-hour postprandial decreased by 61 mg/dL.
  8. What effect does Sitagliptin (Januvia) have on weight?
    Weight neutral (same as all Gliptins)
  9. _______________________ has GI effects similar to placebo.
    Sitagliptin (Januvia)
  10. What is the MOA of Sitagliptin (Januvia)?
    • Dipeptidyl Peptidase-4 Inhibitors
    • Inhibits the dipeptidyl peptidase-4 enzyme responsible for the breakdown of incretin hormones glucagon-like peptide 1 and glucagon glucose-dependent insulinotropic polypeptide.
  11. What are the Gliptins?
    • Sitagliptin (Januvia)
    • Saxagliptin (Onglyza)
    • Linagliptin (Trajenta)
    • Alogliptin (Nesina)
  12. What is the brand name for Sitagliptin?
    Januvia
  13. What is the brand name for Saxagliptin?
    Onglyza
  14. What is the brand name for Linagliptin?
    Trajenta
  15. What is the brand name for Alogliptin?
    Nesina
  16. What is the generic name for Januvia?
    Sitagliptin
  17. What is the generic name for Onglyza?
    Saxagliptin
  18. What is the generic name for Trajenta?
    Linagliptin
  19. What is the generic name for Nesina?
    Alogliptin
  20. What is the dose for Saxagliptin (Onglyza)?
    • 2.5- and 5 mg tablets; no apparent benefit to date.
    • ClCr ≥ 50 mL/min = 5 mg QD
    • ClCr ≤ 50 = 2.5 mg QD
    • strong inhibitors of CYP3A4/5: 2.5 mg QD (clarithromycin, itraconazole, ritonavir
  21. What are the disadvantages of Saxagliptin (Onglyza)?
    Some evidence increases hospitalizations for heart failure
  22. What is the dose for Linagliptin (Trajenta)?
    • 25 mg once daily
    • ClCr ≥ 30 - < 60 mL/min: 12.5 mg QD
    • ClCr < 30 mL/min or ESRD: 6.25 mg QD
    • May be taken with or without food
  23. What is the efficacy of Linagliptin (Trajenta)?
    5 mg QD decreases A1C by about 0.5%–0.7% in monotherapy
  24. How is Linagliptin (Trajenta) eliminated?
    Not renally eliminated, no renal dosage adjustment necessary
  25. Can Linagliptin (Trajenta) be used in renal impairment?
    • Yes, Ideal for patients with renal impairment = Elderly
    • Not renally eliminated
    • No dosage adjustment in renal failure
  26. What patient population is Linagliptin (Trajenta) particularly good for?
    Ideal for patients with renal impairment = Elderly
  27. How is Alogliptin (Nesina) eliminated?
    Primarily eliminated renally; check renal function prior to therapy
  28. What Pregnancy category is Alogliptin (Nesina)?
    B
  29. What is the efficacy of Alogliptin (Nesina)?
    25 mg QD decreased A1C by 0.4%-0.6%
  30. What are the DDIs of Alogliptin (Nesina)?
    No significant DDIs
  31. What is Kazano?
    Alogliptin and metformin 12.5 mg/500 mg or 12.5 mg/1000 mg
  32. Take with food; do not split tablets; increase gradually due to GI
  33. What is the benefit of Alogliptin combo with Metformin (Kazano)?
    Combination dropped A1C by 1.1% over either agent alone
  34. What is Oseni?
    Alogliptin and pioglitazone (12.5 mg/15 mg up to max 25 mg/45 mg) QD
  35. What is the benefit of Alogliptin combo with Pioglitazone (Oseni)?
    Combination dropped A1C by 0.4% to 0.9% over either agent alone
  36. How should you take Kazano (Alogliptin/Metformin)?
    May be taken with or without food; do not split tablets
  37. What is the dose for Oseni (Alogliptide/Piogltazone)?
    • NYHA Class I or II HF: start at 25 mg/15 mg
    • ClCr ≥ 30 - < 60 mL/min: 12.5 mg/30 mg or 12.5 mg/45 mg
    • ClCr < 30 mL/min or ESRD: do not use
  38. What DDIs does Oseni (Alogliptin/Pioglitazone) have?
    Concomitant gemfibrozil or other strong CYP2C8 inhibitors
  39. What is the max dose of Oseni (Alogliptide/Pioglitazone) when used with gemfobrozil or a strong CYP2C8 inhibitor?
    25/15 mg

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