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  1. Bromocriptine
    D2 agonist - binds & stimulates D2 receptors on lactotrophs. Decreases prolactin synthesis & DNA synthesis & tumor growth. Usually 1st-line medication (cabergoline has more side effects but is less effective)
  2. Cabergoline
    High affinity for D2 receptors. Used for patients with hyperprolactinemia. May be useful in patients who do not respond to bromocriptine. Risk of aortic valve fibrosis in those taking very high doses (not normally doses used for treatment of prolactinoma). May cause nausea; orthostatic hypotension; dyskinesia
  3. Levothyroxine
    Also called Synthroid. Drug of choice for treatment of hypothyroidism. Must be monitored via TSH levels. Same as T4. Those with cardiac disease must be started on very low doses. Pregnant patients will require higher doses
  4. Octreotide
    Brand name = sandostatin. Mimics natural somatostatin to inhibit growth hormone. Selective SST2R agonist. May cause GI distress & gallstones. Old formula needed to be administered subcutaneously 3x daily; new formula is administered intramuscularly once every 4 weeks
  5. Liothyroxine
    Occasionally used to treat hypothyroidism. Same as T3. Used in severe acute hypothyroidism
  6. Liotrix
    Mixture of T4/T3. Mimics natural ratio of T4/T3. No major advantage over levothyroxine
  7. Thyroid & thyroglobulin
    Thyroid hormone replacements isolated from animals. Many disadvantages. Infrequently used
  8. Thioureylines
    Includes propylthiouracil and methimazole. Drugs of choice for treatment of hyperthyroidism. Inhibit iodination of thyroglobulin by inactivating thyroid peroxidase. Propylthiouracil also blocks peripheral conversion of T4 to T3. Side effects = itchy rash & slight fever
  9. Lugol's solution
    Contains iodide - shuts down thyroxine production at high levels. Inhibits iodination of thyroglobulin and T3/T4 synthesis/release. Used only in combination with thioureylines and in specific situations - pre-op for thyroidectomy & in thyroid storm. Side effects = salivation; sore teeth/gums; hemorrhage; induction of goiter/myxedema
  10. I131
    Used to destroy thyroid tissue - emits beta rays
  11. Beta-blockers
    Hyperthyroidism can imitate sympathetic nervous system activation; beta-blockers can block sympathetic effects. Used in life-threatening thyroid storms (exacerbation of thyrotoxicosis) to prevent or reverse severe effects - tachycardia; fibrillation; shock; heart failure. Used in combination with thioureylines/Lugol's solution
  12. Somatropin/Somatrem
    Recombinant human growth hormone; used to treat GH deficiency. May lead to development of anti-GH autoantibodies
  13. Pitressin
    Broad-acting ADH analogue; acts on V1 and V2 receptors. Few uses due to broad effects; used for temporary control of GI bleeding. Side effects include skin blanching; abdominal cramps; hypertension
  14. Desmopressin acetate
    ADH analogue; acts selectively on V2 receptors. Used in diabetes insipidus and mild hemophilia. Side effects include water retention; listlessness; seizures; coma
  15. Spironolactone
    Competitive aldosterone antagonist blocks the actions of aldosterone at its receptor. May cause hypogonadism due to blockage of testosterone biosynthesis
  16. Eplerenone
    Aldosterone antagonist blocks the actions of aldosterone at its receptor
  17. Triamterene
    Potassium-sparing diuretic that works by blocking ENaC
  18. Hydrocortisone
    Cortisol replacement
  19. Fluorocortisol
    Mineralocorticoid replacement
  20. Cyproterene
    Blocks androgen receptor
  21. Ketoconazole
    Antifungal; may cause hypogonadism due to blockage of androgen receptor
  22. Leuprolide
    GnRH agonist
  23. Clomiphene
    Estrogen antagonist (NOT a SERM - antagonist in all tissues)
  24. Metformin
    Decreases hepatic glucose production through LKB1 - protein kinase that upregulates AMPK. Only member of biguanide family. Increases insulin-mediated muscle glucose uptake & decreases GI glucose absorption & inhibits adipose tissue lipolysis as well. Promotes some slight weight loss & improves microvascular outcomes. May be used in pre-diabetics to prevent progression. Contraindications = renal insufficiency or severe CHF or chronic liver disease. No risk of hypoglycemia but does carry risk of lactic acidosis
  25. Rhogam
    Rh negative mothers - help prevent abortion with threatened spontaneous abortion
  26. Letrozole
    Aromatase inhibitor
  27. Nafarelin
    Nasal spray - GnRH agonist
  28. Glargine
    Very long-acting insulin
  29. Detemir
    Very long-acting insulin
  30. Glipizide
    2nd-generation sulfonylurea
  31. Lispro
    Very short-acting insulin
  32. NPH
    Medium-acting insulin
  33. Thiazolidiniediones
    Enhance insulin sensitivity in muscle & liver & adipose tissue - agonist for nuclear receptor PPAR-gamma (in adipocytes & liver -PPR-gamma regulation of genes involved in adipocyte differentiation & fatty acid uptake. PPAR-gamma acts via transactivation & transrepression). Include rosiglitazone & pioglitazone (Avandia & Actos) - rosiglitazone = severely restricted & not generally used. Side effects = weight gain & edema. Contraindicated in those with CHF. LFTs are necessary during treatment. May be associated w/osteoporosis. Delayed onset (3-6 weeks). Decreases inflammation
  34. Sulfonylureas
    Bind to potassium channels on beta-cells - causes membrane depolarization -> calcium influx -> release of stored insulin. Effective but have high yearly failure rate & may cause weight gain & hypoglycemia. Examples include glipizide & glyburide
  35. Glimepiride
    3rd-generation sulfonylurea
  36. Glinides
    Different structure from sulfonylureas but work in much the same way - bind to potassium receptor (distinct site from sulfonylurea) -> calcium influx -> release of stored insulin. Have more rapid action & shorter duration than sulfonyureas. Produce comperable reductions in HbA1c vs. sufonylureas but do not produce weight gain & cause lower rates of hypoglycemia. Drawback: more expensive than sulfonylureas
  37. Biguanides
    Metformin - decreases hepatic glucose production. Increases insulin-mediated muscle glucose uptake & decreases GI glucose absorption & inhibits adipose tissue lipolysis as well. Mainly acts through LKB1 - protein kinase that upregulates AMPK. Promotes some slight weight loss & improves microvascular outcomes. May be used in pre-diabetics to prevent progression. Contraindications = renal insufficiency or severe CHF or chronic liver disease
  38. Alpha-glucosidase inhibitors
    Inhibits hydrolase enzyme on the brush border of the intestines - delays postprandial carbohydrate absorption. Side effects = bloating & flatulence & diarrhea -> poor compliance. Poor efficacy but does not cause weight gain or hypoglycemia
  39. Incretin-based therapies
    GLP-1 analogues (injection) & DPP4 blockers (oral)
  40. Diazoxide
    Potassium channel inhibitor - increases permeability of the K-ATP channel -> closing of calcium channel -> prevention of insulin release. Used for treatment of hypoglycemia due to hyperinsulinism & for malignant HTM (relaxes smooth muscle)
  41. Short-acting insulins
    Lispro & Aspart & Glulisine (very short; onset 15-30 mins) & regular insulin (short; onset 0.5-1 hr)
  42. Intermediate-acting insulins
    NPH (onset 1-4 hr)
  43. Long-acting insulins
    Detemir & Glargine (last 14-22 hrs)
  44. SERM
    "Stands for ""selective estrogen receptor modulator."" Used for the treatment of infertility in anovulatory women. Includes tamoxifen & raloxifene & toremifene"
  45. Pramlintide
    Amylin analogue. Slows gastric emptying -> aids in absorption of glucose. Also promotes satiety (similar to GLP-1 agonists) & inhibits glucagon
Card Set
Endocrine Pharmacology
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