Winter quarter potpourri

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Author:
jlolson83
ID:
136593
Filename:
Winter quarter potpourri
Updated:
2012-02-21 17:31:32
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Pharm
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Description:
endocrine, lipids, hormonal
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  1. Bile Acid Resins
    • Decrease cholesterol absorption
    • Cholestyramine, colestipol
    • Anion exchange resins
    • High non-compliance - like sand, tastes bad, steatorrhea, anal fissures, bloating
  2. Cholesterol Transport inhibitor
    • Zetia (Ezetimibe)
    • Little effect on HDL
    • Blocks chol absorption in small intestine
    • Side effects - few, elevates transam's
  3. Statins
    • HMG CoA reductase inhibitors
    • Well tol, but small chance of rhabdomyolysis (didn't see in clinical trials)
    • Newer are more effective (eg crestor)
  4. Niacin
    • Enhances lipoprotein lipase in muscle
    • #1 for increase HDL
    • x: pg
    • :( flushing, pruritis, (aspirin helps), n/v, hyperurecemia, hyperglycemia, hepatotox
  5. Niacinamide
    • Doesn't alter HDL/LDL!
    • Does cause flushing like niacin
  6. Fibric acid derivative
    • Gemfibrozil/Clifibrate
    • #1 for decreasing triglycerides
    • :( dyspepsia, gallstones, myopathy
  7. Cholesterol combos
    • Statin + bile acid resin :) timing issues
    • Statin + fibric acid - increase myopathy
    • Statin + niacin - inc AST/ALT, myosistis, rhabdomyolysis - eek
    • Statin + Ezetimibe = Vytorin - bigger drop in chol, but does it matter...
  8. Anti-thyroid meds
    • Decrease peroxidase-mediated iodination of precursor (dec T3/T4)
    • Methimazole (#1)
    • Propylthiouracil (PTU) (inh periph deiodination)
    • only for temporary use before surgery/radioactive tx
    • Risks: aganulocytosis (sore throat/fever), hepatotox
  9. Anti-androgens
    • GnRH antagonist: cetrorelix, degarelix (Ganirelix - prostate ca)
    • Ketoconazole, spironolactone
    • Flutamine, bicalutamine, nilutamide (hursuitism in women)
    • Finasteride (BPH, hair loss)
  10. Flutamine, bicalutamine, nilutamide
    Treats hursuitism in women
  11. Finasteride
    • Oral
    • Treats BPH
    • Treats hair loss (decreases male libido/sperm potency)
  12. Calcitonin
    • Can treat hypercalcemia
    • Suppresses bone resorption by inhibiting osteoclasts
    • Normally secreted by thyroid
    • Rapid/short acting
  13. Glucocorticoid bone effects
    • Osteoporosis, especially long bone
    • Antagonize Vitamin D mediated GI absorption of calcium and phosphate, partially block in kidney, enhance bone resorption, inhibit PTH activity
  14. Estrogen effect on bone
    • Estrogen R in bone, unknown function
    • Adsorb to bone rendering bone resistant to hydrolysis
    • (inc breast ca risk, ovarian ca risk)
  15. Bisphosphonates
    • Prophylaxis for osteoporosis
    • :( erosive esophagitis (therefore not often given as pill)
    • Fosamax (q-week) (not with food, must drink water and not lie down for an hour)
    • Alendronate (strongest), etidronate, pamidronate
    • Inhibit osteoclasts
    • Used for Paget's disease
  16. PTH
    Parathyroid Hormone
  17. Insulin secretagogue
    • Sulfonylureas: glyburide, glipizide, glimiperide
    • SU - QD or BD
    • Glinides: repaglinide, nateglinide
    • Take with meals - better for elderly/people that skip meals
    • :( Weight gain
    • Act on R on beta cell, inc intracell Ca, inc insulin release
  18. Biguanides: Metformin
    • Acts on liver (a bit on skel m too)
    • Reduces insulin resistance
    • Decreases hepatic glucose production
    • BID
    • :( GI, lactic acidosis, so contraindicated in kidney failure
    • Does not cause hypoglycemia
    • First choice in tx!
  19. Thiazolidinediones
    • Troglitazone (liver tox)
    • Rosiglitazone (inc risk MI)
    • Pioglitazone :)
    • Work on skel m, nuc R, inc mRNA for glucose transporter
    • Takes a month to work
    • :( excess fluid retention (contraind for HF pt)
  20. a-Glucosidase Inhibitors
    • Acarbose/Miglitol
    • Delay carbohydrate absorption at intestinal brush border by inhibiting disaccaride break down
    • Still absorb as much carbs, just over more time
    • Take before every meal
    • :( flatulence, liver enzyme elevation(rare)
  21. Combination therapy with diabetes
    • Metformin first
    • When A1C >7%, add
    • Sulfonylurea + metformin
    • Sulfonylurea + glitazone
    • May require insulin after years of increased resistance
  22. GLP-1
    • Released from L cells in ileum/colon
    • Stimulates insulin release (glc dep)
    • Inhibits glucagon release (glucose dep)
    • Inhibits gastric emptying - induces satiety
    • Rapidly degraded by DPP-4
  23. GIP
    • Released from K cells in duodenum
    • Stim insulin
    • Rapidly degraded by DPP-4
  24. DPP-4 inhibitors
    • Increases GLP-1 and GIP
    • Increases Insulin, dec glucagon, inc satiety
    • Sitagliptin, Saxagliptin, Linagliptin
    • B cells give limited amount of insulin, so drug doesn't cause hypoglycemia
  25. Insulin
    • NPH - insoluble
    • Analogs - aspart, glulisine, lispro, glargine, detemir (longer lasting)
    • Premix for immediate and long lasting together
  26. Rapid acting Insulin Analogues
    • Aspart, Glulisine, Lispro
    • Limited self-aggregation (monomers act faster)
    • 4-6 hours
    • Better, bc mimic normal insulin release profile when taken with meals
  27. Slow acting insulin analogues
    • Glargine, detemir
    • 24hours
  28. Heparin
    • Anticoagulant
    • "unfractionated heparin" Lots of variability in solution
    • Acts on 2a and 10a
    • Short acting, infusion (for in-pt)
    • Problems from misdosing
    • From porcine/bovine intestine
    • Monitor with aPTT
    • :( HAT heparin associated thrombocytopenia (<7d, temp); HIT heparin induced thrombocytopenia (more severe, 7-14days, PLT <150, treat with direct thrombin inhibitor and warfarin)
    • Safe in pg
    • Reverse with protamine
  29. LMWH
    • Low molecular weight heparin
    • Only inhibits 10a
    • Enoxaparin, Dalteparin, Tinzaparin
    • Less HIT, less side effects
    • Indicated: DVT, PE, acute MI, TIA(stroke)
    • Contraindic: kidney disease, recent surgery unless inpt, bleeding, dissecting aortic aneurym
    • Safe in pg
  30. Direct Thrombin Inhibitors
    • Lepirudin, Argatroban, Bivalirudin
    • L(from leeches, not ideal)
    • A(adjust for hepatic dysf, use for HIT/coronary angioplasty)
    • B(coronary angioplasty)
    • :( bleeding
  31. Warfarin
    • Inhibits F2,7,9,10. analog for vitamin K
    • Onset = 3-5 days
    • Half life F2 (60 hours) ergo slower acting
    • :( bleeding
    • Interacts with CYP450 drugs
    • Transient protein C deficiency can be induced (---> dermal vascular thrombosis/skin necrosis)
    • Contraind: pg, bleeding, aneurysm, recent surgery, hypersensitivity
    • Reverse with vitamin K
  32. Thrombin inhibitor
    • Dabigatran
    • No monitoring (better than warfarin)
    • Oral Prodrug
  33. Anti-10a inhibitors
    • Rivaroxaban, Apixaban, Fondiparinux (diff structure)
    • Like LMWhep
    • Inhibit CYP450
    • No blood monitoring needed
    • No reversing agent
  34. Fibrinolytic drugs (thrombolytics)
    • Streptokinase
    • Recombinant tPA (alteplase, reteplase, tenecteplase)
    • Urokinase
    • Anistreplase
    • Timing is important to prevent intracerebral bleed, esp if pt >75
  35. Recombinant tissue-plasminiongen activator (tPA)
    • Alteplase=tPA (widely used, DVT, PE, MI, TIA)
    • -better than streptokinase bc no allergic rxn, more specific to fibrin, shorter half life
    • Reteplase, tenecteplase (STEMI)
    • Potentiates plasminogen to plasmin conversion (which breaks down clot)
  36. Antistreplase
    Streptokinase and plasminogen as complex
  37. Plasminogen Inhibitor
    • Aminocaproic acid, Tranexamic acid
    • Bleeding emergencies
  38. Antiplatelet drugs
    • Aspirin
    • ADP antagonists (Clopidogrel, ticlopidine, prasugrel)
    • Dipyridamole
    • Glycoprotein IIb/IIIa R inh (Abciximab, eptifibatide, tirofiban)
  39. Aspirin (Acetylsalicylic acid)
    • Irrev inhibits COX-1 (low TXA2)
    • Effects last 5 days after d/c drug
    • :( GI bleed, OD=salicylism (vomiting, tinnitus, dizziness)
    • Uses: pts with iscemic heart disease/stroke, angina prophylaxis, MI tx, TIA tx
  40. ADP Inh/P2Y12 inh
    • Interferes with ADP binding to R --> inh GPIIb/IIIa act
    • Can be alternatives to aspirin, used after coronary-stent procedure
    • Works for a week after d/c
    • :( GI bleed, neutropenia/purpura(ticlopidine-immune)
  41. Dipyridamole
    • Vasodilator
    • Increased intracellular cAMP, inhibiting PDE (dec TXA1)
    • Potentiates PGI2 to dec platelet adhesion
    • Uses - w/ warfarin, after TIA
  42. GPIIb/IIIa R antagonist
    • Abciximab
    • -(for cath lab) Long acting, acts on VWF too, given w hep or aspirin too
    • Eptifibatide (for cath lab or non-invasive management)
    • Tirofiban
    • Acute coronary event, unstable angina
  43. SERMs: Selective Estrogen R Modulators
    • Raloxifene, Tamoxifen, Toremifene
    • Nonsteroidal
    • Agonist in bone/endometrium
    • Antagonist in breast
    • :( hot flashes, n/v, vaginal discharge, thrombosis, endometrial cancer
    • Bones okay :)
  44. Tamoxifen
    • Combines SERM/R, translocates to nucleus, Inhibits DNA syn
    • Increase inhibitory growth F, dec growth F
    • Oral
    • Uses - tx metastatic breast ca, aduvant tx, prophylactic in high risk pts
    • CYP2D6 biotransformation to metabolite active = endoxifen
  45. Raloxifene
    • Equal to tamoxifene in trials, but not as popular
    • lower incidence of thrombosis
  46. Toremifene
    • Like tamoxifene
    • Not popular
    • Lower estrogenic/anti-estrogenic ratio
  47. Aromatase inhibitors
    • Non-steroidal - Anastrozole, Letrozle
    • Steroidal - exemestane (irrev)
    • Inh androstenedione to estrone, testosterone to estradiol
    • Tx of POSTmenopausal only bc only act on peripheral production of estrogen
    • (in premenopausal F, would stim ovaries to make more)
    • :( arthralgia/myalgia, fatigue, osteopenia, osteoporosis (use bisphosphonate), hot flashes, vag dryness
  48. Premenopausal breast ca treatment
    • Early:
    • Chemo then SERM (tamoxifen)
    • Ovarian ablation
    • Tamoxifen alone

    • Advanced:
    • Tamoxifen
    • Ovarian ablation
    • chemo + tamoxifen

    NEVER give chemo and hormone tx at same time
  49. Postmenopausal breast ca treatment
    • Tamoxifen OR aromatase inhibitor
    • NEVER give chemo and hormone tx at same time
  50. Gonadotropin Releasing Hormone Agonist (GnRHag or LH/FSHag)
    • Goserelin, Histrelin, Leuprolide, Triptorelin
    • First- sex steroid spikes, then negative feedback takes over
    • Uses - prostrate/breast ca
    • Results - women to post menopausal estrogen levels, men to castration testosterone levels
    • All long acting
    • :( hot flashes, men gynecomastia/breast tenderness, osteoporosis long term, TUMOR FLARE
  51. Goserelin
    • GnRH ag
    • subQ q1-3mo
    • :( HA, vaginitis
  52. Histrelin
    • GnRH ag
    • Implant (q12mo)
    • :( urinary retention
  53. Leuprolide
    • GnRH ag
    • Depot injections (q1-3mo)
  54. Triptorelin
    • GnRH ag
    • IM inj (1-6mo)
  55. Anti-androgenic agents
    • Nilutamide, bicalutamide, flutamide
    • Nonsteroidal. bind androgen R, competitievely inh dhTestosterone and testosterone
    • Treat tumor flare from GnRH agonist and hot flashes
    • Combined tx with GnRH agonist for ca
  56. Ketoconazole
    • Antifungal which inhibits 5% testosterone production
    • Last line androgen blockade
  57. Abiraterone
    • Anti-androgen
    • Tx metastatic castration-resisant prostate ca
    • Irrev inh CYP17 which processes androgens
    • :( thrombocytopenia
  58. Fulvestrant
    • Estrogen antagonist
    • Second line agents
    • Competitively binds estrogen R - works like SERM but antag only
    • :( hot flashes, n, weakness
  59. Degarelix
    • LHRH antagonist
    • Dec testosterone
    • No tumor flare
    • :( hot flashes, injection site rxn

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