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  1. TZDs also known as:
    insulin sensitizers/insulin enhancers
  2. TZD MOA
    direct stimulation of PPAR-gamma --> inc in GLUT-4 on cell surface --> increase in insulin uptake in muscle and adipose and dec in hepatic glucose production
  3. Diff btwn TZD's and metformin

    • metformin: 1-dec hepatic glucose output; 2-better insulin sensitivity in muscle and adipose
    • TZD: 1-better insulin sensitivity in muscle and adipose; 2-dec hepatic glucose output
  4. rosiglitazone metabolism and elimination
    • hepatic metabolism
    • elimination in urine (more) and feces (less)
  5. pioglitazone metabolism and elimination
    • hepatic metabolism
    • eliminated in feces
  6. TZD's effects seen when?
    • dec in BG seen in 2-4 wks
    • full effects in up to 12 wks
    • perseverance of effect for 1-2 yrs
  7. effect of TZDs on lipid
    • rosiglitazone: inc cholesterol, LDL, HDL
    • pioglitazone: inc HDL, dec TGs
  8. TZD contraindication
    • Heart failure (especially rosiglitazone)
    • - fluid retention

    MI (rosiglitazone) - can only get with distribution program
  9. pioglitzone precautions
    • heart failure inc risk (lowest dose if in Class 2 HF)
    • macular edema (use with caution in pts with edema)
    • more bone fracture in women
    • resumption of ovulation in perimenopausal anovulatroy women
    • bladder cancer
  10. TZD side effects
    • no signs of hepatotoxicity
    • rosi: MI,┬ádeath from CV causes
    • pio: bladder cancer
    • weight gain (dose dependent)
    • edema (dose dependent; more common with insulin)
    • dec in Hbg and Hct (bc of fluid imbalance)
    • resumption of ovulation
    • bone fracture
    • macular edema
  11. TZD monitoring
    • LFTs b4 starting
    • don't start if ALT > 2.5x upper limit
    • get LFT's at first signs of hepatic dysfuntion (fatigue, anorexia, nausea, vomiting, ab pain, dark urine, jaundice) -->if continues, d/c
Card Set:
2013-09-21 18:54:46

Dr. Drab
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