pharm endo goshko info.txt

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tallone4830
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pharm endo goshko info.txt
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2012-12-12 10:28:50
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pharm endo goshko info.txt
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  1. Biguanides MOA
    Less gluconeogenesis, possibly via inhibition of AMP kinase (needed for glucose formation). also improves muscle/adipose tissues' sensitivity to insulin. also delayed absorption of glucose from GI tract.
  2. Biguanides kinetics
    PO
  3. Biguanides indications
    DM type 2, off-label PCOS.
  4. Biguanides contraindications
    many, including DKA, iodinated contrast, and renal impairment (CrCl < 60).
  5. Biguanides side effects
    BBW lactic acidosis. several GI (start low go slow, take after meals). metallic taste, malabsorption of B12/folate. No weight gain.
  6. metformin dosing
    metformin IR 850-1000mg PO BID
  7. Biguanides hypoglycemia
    No -- since metformin does not stimulate pancreatic beta cell insulin secretion, the risk of hypoglycemia is low if metformin is used alone.
  8. Sulfonylureas MOA
    increase insulin secretion by binding to sulfonylurea receptor on pancreatic beta cells (less K efflux -> depolarization -> insulin release). also decrease glucagon release from pancreatic alpha cells.
  9. Sulfonylureas kinetics
    PO. second generation agents are 100 times more potent than first generation agents
  10. Sulfonylureas indications
    DM type 2
  11. Sulfonylureas contraindications
    DKA, prone to hypoglycemia. caution w/ sulfa allergy.
  12. Sulfonylureas side effects
    weight gain, rash. only 65% will respond to treatment (of those, 5-10% per year will gradually lose glycemic control)
  13. Sulfonylureas hypoglycemia
    yes (start low, go slow) -- because we are "squeezing the pancreas"
  14. glyburide dosing
    glyburide 1.25-20mg PO qday
  15. Thiazolidinediones also known as
    TZDs, glitazones, insulin sensitizers
  16. Thiazolidinediones MOA
    increase the sensitivity of cells to insulin by agonizing PPARs. These receptors decrease glucose production (liver), increase glucose uptake (muscle/adipose), and increase free fatty acid uptake/storage (adipose tissue).
  17. Thiazolidinediones kinetics
    PO
  18. Thiazolidinediones indications
    DM type 2
  19. Thiazolidinediones contraindications
    Heart failure (worsen CHF by fluid retention -- BBW). Rosiglitazone additional BBW for MI.
  20. Thiazolidinediones side effects
    weight gain, edema, fracture risk, anemia. pioglitazone also bladder cancer.
  21. Thiazolidinediones hypoglycemia
    No -- only messing with insulin sensitivity, not insulin release
  22. pioglitazone dosing
    rosiglitazone 15-45mg PO qday
  23. Incretins MOA
    Incretins such as GLP-1 (glucagon-like peptide 1) are hormones released after meals that lower blood glucose by stimulating insulin release. Their activity is typically blunted in diabetes. Mimetics mimic incretins (structurally modified to resist degradation) -- DPP-4 inhibitors prevent their breakdown (block incretin inactivation by DPP-4).
  24. Incretins kinetics
    SC
  25. Incretins indications
    DM type 2
  26. Incretins contraindications
    liraglutide personal/family hx of thyroid CA (BBW).
  27. Incretins side effects
    NAUSEA. Serious side effects include pancreatitis, anaphylaxis, renal failure.
  28. Incretins hypoglycemia
    Yes -- stimulate insulin release
  29. exenatide dosing
    exenatide 5-10mcg SC BID w/i 60min of meal
  30. Alpha Glucosidase Inhibitors MOA
    These drugs are carbohydrate analogues that competitively bind to alpha-glucosidase (enzymes that break down carbs into glucose) with greater affinity than natural dietary carbs. This helps prevent an after-meal glucose spike.
  31. Alpha Glucosidase Inhibitors kinetics
    PO
  32. Alpha Glucosidase Inhibitors indications
    DM type 2
  33. Alpha Glucosidase Inhibitors contraindications
    IBD, DKA, GI obstruction, elevated LFTs. acarbose also renal dysfunction.
  34. Alpha Glucosidase Inhibitors side effects
    GI (bloating, flatulence, diarrhea, abdominal pain), elevated LFTs
  35. Alpha Glucosidase hypoglycemia
    No -- keeps sugars from being digested, does not spike insulin levels
  36. Meglitinides MOA
    Bind to a receptor (SUR-1) on pancreatic beta cells that blocks the efflux of potassium. The resultant depolarization eventually results in insulin release. Stimulate only glucose dependent insulin secretion (sulfonylureas are glucose-independent).
  37. Meglitinides kinetics
    PO. Rapid onset, short duration of action. Give up to 30 minutes prior to meal. repaglinide more effective than nateglinide.
  38. Meglitinides indications
    DM type 2
  39. Meglitinides contraindications
    DKA. Adjust dose for liver (both) and kidney (only repaglinide) issues.
  40. Meglitinides interactions
    repaglinide + gemfibrozil (raises repaglinide levels due to inhibition of hepatic metabolism)
  41. Meglitinides side effects
    GI (diarrhea, flatulence, abdominal cramps, bloating)
  42. Meglitinides hypoglycemia
    Yes -- stimulating insulin release
  43. Amylin Analogues MOA
    amylin is a hormone that works with insulin to help regulate glucose levels by inhibiting post-prandial glucagon secretion, slowing gastric emptying, and decreasing appetite.
  44. Amylin Analogues kinetics
    SC
  45. Amylin Analogues indications
    DM types 1 and 2
  46. Amylin Analogues contraindications
    when initiating, premeal doses of rapid and short-acting insulins should be reduced by 50% to prevent hypoglycemia (BBW)
  47. Amylin Analogues interactions
    avoid other agents that slow GI motility, may delay absorption of PO medications (give 1 hr prior or 3 hrs after).
  48. Amylin Analogues hypoglycemia
    Yes -- inhibits secretion of glucagon -- BBW FOR HYPOGLYCEMIA
  49. Amylin Analogues side effects
    GI (N/V, anorexia), HA.
  50. Glucagon MOA
    mimics endogenous glucagon secreted from alpha cells of pancreas -- leads to decreased glycogen synthesis, increased glycogenolysis/glucose, increased glycolysis, and increased ketogenesis. At higher concentrations, also increases ionotropy/chronotropy (via increased cAMP).
  51. Glucagon kinetics
    available SC, IM, and IV. T1/2 is 3-6min.
  52. Glucagon indications
    Refractory hypoglycemia, Hyperinsulin states (insulinoma), b-blocker/CCB/insulin overdose.
  53. Glucagon side effects
    hypokalemia, hyperglycemia
  54. Insulin MOA
    Naturally occurring hormone that reduces blood glucose via increasing glucose uptake in liver, muscle, and adipose tissues. Also decreases glucose production in liver, decreases lypolysis, increases storage of triglycerides, enhances amino acid uptake, and prevents protein breakdown.
  55. Insulin hypoglycemia
    Yes -- we're giving insulin
  56. Insulin kinetics
    Take rapid acting insulins immediately before eating (w/i 30 min). Take short acting 30 to 60 min prior to meals (peak 2-4hrs). Intermediates onset 1-4h, peak 4-14hrs, duration 10-24 hrs. Long-acting mimics basal insulins. SC, Rapid/short acting are the only ones available IV.
  57. Insulin indications
    DM type 1. DM type 2 if severe sx, marked hyperglycemia, DKA, oral agents contraindicated/not effective, during pregnancy.
  58. Insulin side effects
    injection site reactions (including lipohypertrophy), weight gain
  59. Insulin dosing
    typical insulin dosing for DM type 1: 0.3-0.6 U/kg/d
  60. Insulin interactions
    once prandial insulins started, sulfonylureas and meglitinides are usually stopped (though sensitizers should be continued in obese, insulin resistant patients).

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