diabetes drugs

  1. Rapid acting insulins
    • Analogs. Bolus p meal tx
    • lispro (Humalog)
    • aspart (Novolog)
    • glulisine (Apidra)
    • Onset: 15-30 min
    • Peak: 1-3 hr
    • Duration: 3-4 hr
  2. Short acting insulin
    • Regular insulin (Humulin R, Novolin R)
    • Onset: 0.5-1 hr
    • Peak: 2-4 hr
    • Duration: 3-7h
    • neutral pH
  3. Intermediate acting insulin
    • NPH (neutral protamine Hagedorn)
    • Humulin N, Novolin N
    • Onset: 1-2 hr
    • Peak: 6-10 hr
    • Duration: 16-20 hr
    • cloudy
  4. Long acting insulins
    • Analogs. no peaks, basal tx, forms depot
    • glargine (Lantus) - pH 4, precipitates at phys pH
    • detemir (Levemir) - 98% binds to plasma albumin
    • Onset: 1-2 hr
    • Peak: no peak
    • Duration: 20-24 hr
    • Don't mix with other insulin
  5. SE of exogenous insulin
    • hypoglycemia
    • weight gain
    • lipohypertrophy (enlargement of SQ fat depot)
    • lipoatrophy (destruction of SQ fat @ site)
  6. Sulfonylureas
    1st gen: acetohexamide, chlorpropamide - longest t1/2 36h, tolazamide, tolbutamide
    2nd gen: glimepiride, glipizide (GITS), glyburide
    • MOA: stim phase 2 ins release from b-cells (bind, close K, open Ca --> translocation of granules)
    • bioavailability ~90%, protein bound
    • Hepatic metabolism (CYP2C9) - rifampin is inducer, amiodarone is inhibitor
    • SE: hypoglycemia (risk ^w/longer t1/2), weight gain, disulfiram like w/tolbutamide or chlorpropamide
  7. Short-Acting insulin secretagogues (Meglitinides)
    repaglinide (Prandin)
    nateglinide (Starlix)
    • MOA stimulate insulin secretion from b-cells (phase1)
    • given before each meal
    • regaglinide 2C8/3A4
    • nateglinide 2C9/3A4
    • rifampin inducer of all 3, grapefruit inhibitor 3A4, gemfibrozil inhibitor 2C8
    • SE hypoglycemia, weight gain
  8. Biguanides
    • MOA decrease hepatic glucose production by decreasing gluconeogenesis
    • Renally eliminated
    • Drugs renal tubule secretion (cimet, dig, triamt) may increase met levels.
    • SE GI, maybe weight loss, LACTIC ACIDOSIS -->metabolic acidosis.
    • CI- renal insuff, liver impari, CHF, ETOHic, metabolic acidosis, hypoxic lung disease
  9. Thiazolidinediones (TZDs)
    PPARy agonists
    rosiglitazone (Avandia)
    pioglitazone (Actos)
    • MOA stim PPARy (reg gene transcription)
    • increases insulin sensitivity in muscle, liver, fat
    • rosi 2C8>2C9 - gemfib is 2C8 inhibitor
    • pio 2C8>3A4 - rifampin is 2C8 inducer
    • SE weight gain, CHF (bbw), anemia
  10. a-Glucosidase inhibitors
    acarbose (Precose)
    miglitol (Glyset)
    • MOA inhibit glucosidases in small intestine (prevent breakdwn of polysaccharides to glucose)
    • Best for post-prandial glucose concentrations
    • SE GI (low dose then titrate), increase in LFT
  11. pramlintide acetate (Symlin)
    • MOA amylin agonist - dec postpran glucose, dec amt short acting insulin req postpran, delays gastric empty, improves satiety.
    • Metabolized by kidneys
    • SE hypoglycemia, N/V, loss of appetite, HA
    • may delay abs of other drugs (delay gastric empty)
    • Don't use w/GI motility moderators
  12. Incretin Mimetic Drugs
    exenatide (Byetta)
    • MOA mimic incretins - binds to /stim GLP-1 receptor
    • net result - decrease fasting/postpran glucose levels.
    • Renally eliminated - CL reduced w/ESRD
    • SE decreased appetite, N/V, hypoglycemia
    • may delay absorption of oral drugs (pain, antibiotics)
  13. liraglutide (Victoza)
    • MOA-GLP-1 receptor agonist, activates GLP-1 receptors on b-cells
    • Delays gastric empty time, may dec abs of oral drugs
    • SE - HA, N, diarrhea, inj site rxns, hypoglycemia, pancreatits, thyroid tumor (bbw)
    • CI - hx of medullary thryoid carcinoma
  14. DPP-4 inhibitors
    sitagliptin (Januvia)
    saxagliptin (Onglyza)
    • MOA slows inactivation of incretin-->increase in GLP-1
    • net result- decreased fast/postpran glucose
    • Renal elim - dose red w/renal impair
    • sax -3A4/5 - dec dose w/strong inh (grapefruit, azoles)
Card Set
diabetes drugs
DM pharmacotherapy