RX 422 final exam drugs for cards.txt

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HUSOP2014
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150780
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RX 422 final exam drugs for cards.txt
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2012-04-29 12:45:40
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HUSOP 2014 DRUG ACTION FINAL
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DRUGS FOR DA4 FINAL
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  1. insulin aspartate
    • rapid acting insulin analog
    • B28 proline replaced by aspartic acid
    • injected 30 min. before a meal
  2. insulin glargine
    • long acting insulin analog
    • 2 arginine residues added to the B-chain C-terminus and an asparagine residue replaces glycine at A21
  3. Humulin
    • recombinant human regular insulin
    • insulin monomers associated in hexameric aggregates
  4. insulin glulysine
    • rapid acting analog
    • B29 lysine replaced by glutamic acid and B23 asparagine replaced by lysine
    • shortest duration of action: 1-2.5 hours
    • clear - no Zn, buffer, or protein added
  5. insulin lispro
    • rapid acting insulin analog
    • B28 (Pro) and B29 (Lys) have been reversed, impairs hexamer formation for faster action
    • injected 30 min before a meal
  6. NPH insulin
    • neutral protamine Hagedorn (isophane)
    • intermediate acting insulin
  7. tolbutamide
    • 1st gen; short acting sulfonylurea
    • Stimulates insulin release from b-islet cells, binds SUR1 receptor
    • For Type 2 DM
  8. Rosiglitazone
    • Insulin sensitizer, PPAR-gamma (peroxisome proliferator activated receptor) agonist
    • Nuclear TF, regulates carb and lipid metabolism
    • requires insulin for its action
    • ADR: liver toxicity, edema, weight gain
  9. Pioglitazone
    • Insulin sensitizer, PPAR-gamma agonist
    • Nuclear TF, regulates carb and lipid metabolism
    • requires insulin for its action
    • ADR: liver toxicity, edema, weight gain
  10. chlorpropramide
    • 1st generation sulfonylurea; long acting
    • Stimulates insulin release from b-islet cells, binds SUR1 receptor
    • For Type 2 DM
  11. troglitazone
    • insulin sensitizer, binds PPAR-gamma
    • d/c because of liver toxicity
  12. glyburide
    • 2nd generation sulfonylurea; short acting
    • Stimulates insulin release from b-islet cells, binds SUR1 receptor
    • For Type 2 DM
    • ADR: hypoglycemia
  13. glipizide
    • 2nd generation sulfonylurea; long acting
    • Stimulates insulin release from b-islet cells, binds SUR1 receptor
    • For Type 2 DM
    • ADR: hypoglycemia
  14. Acarbose
    • Alpha-glucosidase inhibitor for Type 2 DM
    • Reduces intestinal absorption of starch, dextrin, disacch.
    • reduces post-prandial glucose spike
    • does NOT produce hypoglycemia
  15. miglitol
    • Alpha-glucosidase inhibitor for type 2 DM
    • Reduces intestinal absorption of starch, dextrin, disacch.
    • reduces post-prandial glucose spike
    • does NOT produce hypoglycemia
  16. repaglinide
    • meglitinide secretagogue
    • short acting
    • block ATP/K channels, prevent postprandial glucose spike
  17. nateglinide
    • Phenylalanine secretagogue
    • short acting
    • block ATP/K channels, prevent postprandial glucose spike
  18. exendin-4
    • incretin for type 2 DM, BID injection
    • GLP-1 (glucagon like peptide) receptor (Gs) agonist, increase GLUT2 expression which increases insulin release
    • proconvertase convertes proglucan to GLP-1, degraded by dipeptidyl peptidase IV
  19. aminoguanide
    agent used successfully in trials to prevent oxidation of nonenzymatic glycosylated proteins (which can undergo oxidation and cause cell damage)
  20. liraglutide
    • incretin for type 2 DM, QD injection
    • GLP-1 (glucagon like peptide) receptor agonist (Gs), increases GLUT2 expression which increases insulin release
    • proconvertase convertes proglucan to GLP-1, degraded by dipeptidyl peptidase IV
    • More effective than exendin-4
  21. metformin
    • oral biguanide for type 2 DM
    • activates AMP- activated protein kinase
    • decreases hepatic glucose production, enhances insulin action in muscle and adipose, reduces TGs
    • does NOT produce hypoglycemia
  22. phenformin
    • d/c, biguanide similar to metformin
    • activates AMPK
    • produced too much lactic acidosis
  23. tretinoin
    • 1st generation retinoid (Retin-A)
    • Reduces hyperkeratinization/acne vulgaris
    • Used with anthracycline for APL (acute promyelocytic leukemia)
  24. Isotretinoin
    • AKA accutane
    • 1st generation retinoid
    • Normalizes keratinization, reduces P. acnes
    • For nodulocystic acne vulgaris
  25. Alitretinoin
    • 1st generation retinoid, binds all RAR and RXRs
    • For Kaposi's sarcoma
  26. Acitretin
    • 2nd generation retinoid
    • For plaque psoriasis
    • T1/2= 2-3 days, stored in fat
  27. Bexarotene
    • 3rd generation retinoid
    • Selectively binds RXR
    • For Tcell lymphoma
    • ADR: hypothyroidism
  28. Adapalene
    • Similar to tretinoin, naphthoic acid derivative, retinoid-like (3rd generation)
    • More anti-inflammatory, more stable to sunlight
  29. Calcipotriene (dermatologic)
    • Vitamin D analog
    • Binds VDR which then associates with RXR-alpha
    • Enhances differentiation
    • For mild/moderate psoriasis
  30. Methotrexate (dermatologic)
    • Decreases expression of CLA positive T-cells and endothelial E-selectin
    • 3 doses once a week
    • For moderate/severe psoriasis
    • ADR: hepatic fibrosis
  31. Mycophenolate Mofetil (dermatologic)
    • Inhibits IMPDH (type 2) in B and T cells
    • For moderate/severe psoriasis
  32. Alefacept (dermatologic)
    • anti-CD2 - recombinant fusion protein (LFA3 + IgG1 Fc domain)
    • blocks memory T-cell costimulation
    • ADR: reduction in CD4+ cells
    • For moderate/severe psoriasis
  33. Tacrolimus (dermatologic)
    • Calcineurin inhibitor ,binds FK506-BP12
    • stops NFAT from initiating IL-2 production in T-cells
    • Also binds langerhans cells, mast cells, keratinocytes
    • ADR: HTN and renal dysfunction, NO epidermal thinning
    • For moderate/severe psoriasis, also rosacia
  34. Cyclosporine (dermatologic)
    • Calcineurin inhibitor, which stops NFAT from initiating IL-2 production in T-cells
    • Also binds langerhans cells, mast cells, keratinocytes
    • ADR: HTN and renal dysfunction
    • For moderate/severe psoriasis
  35. Etanercept (dermatologic)
    • Recombinant anti-TNF-?
    • Fusion protein (TNF binding domain + IgG1 fc domain)
    • ADR: increased risk of infection
  36. Betamethasone (dermatologic)
    • Fluorinated topical GC, most potent
    • For psoriasis, not for face or genitals
    • ADR: skin atrophy (GCs)
  37. Hydrocortisone (dermatologic)
    • Least potent topical GC
    • For mild/moderate psoriasis
    • ADR: skin atrophy
  38. Prednisone (dermatologic)
    • Systemic GC for severe psoriasis
    • Extensive ADRs, pustular flares if rapidly tapered
  39. Infliximab (derm.)
    • anti-TNF-alpha (bound and unbound) - complement dependent
    • ADR: reactivate TB, exacerbate CHF
    • For moderate/severe psoriasis
  40. efalizumab (dermatologic)
    • anti-CD11a of LFA1, blocks binding to ICAM-1 on APCs
    • For moderate/severe psoriasis
  41. 8-methoxypsoralen
    • photosensitizer used in combo with UVA for severe psoriasis
    • type 1 rxn O2 independent, type 2 rxn O2 dependent
    • Better GI absorption than 4,5,8 TMP
  42. Aminolevulinic acid (ALA)
    • Photosensitizer, used in combo with PDT
    • Converted to protoporphyrin
    • For actinic keratoses and non-melanoma cancer
  43. Avobenzone, Oxybenzone, titanium oxide, zinc oxide
    UVA sunscreen, reduce deeply penetrating light
  44. 4,5,8-trimethylpsoralen
    • photosensitizer used in combo with UVA for severe psoriasis
    • type 1 rxn O2 independent, type 2 (melanogenesis) rxn O2 dependent
    • Less GI absorption than 8-MOP
  45. Methoxsalen
    • Photosensitizer used in combo with UVA
    • For psoriasis, vitiligo, atopic dermatitis, cutaneous lymphoma
    • ADR: blistering, erythema. Chronic= actinic keratoses
  46. PABA esters, cinnamates, salicylates
    UVB sunscreen agents
  47. minoxidil
    • originally for HTN, opens K+ channels, hyperpolarizes, relaxation
    • for alopecia, enhances follicle size
  48. Finasteride
    • Inhibits type 2 5-alpha-reductase, decreases DHT
    • for alopecia for men
    • ADR: ED, decrease libido
  49. Timolol
    • nonselective beta antagonist
    • decreases aqueous humor production
    • 1st line OAG
  50. apraclonidine
    • selective alpha-2 agonist for OAG
    • decreases aqueous humor production, maybe more meshwork outflow
  51. pilocarpine
    • M3 agonist,2nd/3rd line OAG
    • Increases trabecular outflow
  52. levobunolol
    • nonselective beta antagonist for OAG
    • decreases aqueous humor production
  53. Clonidine
    • alpha-2 agonist for OAG
    • decreases aqueous humor production, maybe more meshwork outflow
  54. carbachol
    • M3 agonist, 2nd/3rd line OAG
    • Increases trabecular outflow
  55. metipranolol
    • nonselective beta antagonist 1st line OAG
    • decreases aqueous humor production
  56. brimonidine
    • selective alpha-2 agonist for OAG
    • decreases aqueous humor production
    • preferred over apraclonidine
  57. echothiophate
    • AchE-I, 2nd/3rd line OAG
    • Increases trabecular outflow
  58. carteolol
    • nonselective beta antagonist
    • decreases aqueous humor production
    • 1st line for OAG
  59. betaxolol
    • Beta antagonist (Beta-1-selective), not as effective in OAG
    • Decreases aqueous humor production
  60. dorzalamide
    • topical carbonic anhydrase-I for OAG
    • decreases aqueous humor production
  61. brinzolamide
    • topical carbonic anhydrase-I for OAG
    • decreases aqueous humor production
  62. latanoprost
    • PG analog, 1st line OAG
    • Increases uveoscleral outflow
  63. Acetazolamide
    • oral carbonic anhydrase-I for OAG
    • decreases aqueous humor production
  64. travoprost
    • PG analog, for OAG
    • Increases uveoscleral outflow
    • 2nd line, ADR: pigmentation, CV effects
  65. Methazolamide
    • oral carbonic anhydrase-I for OAG
    • decreases aqueous humor production
  66. bimatoprost
    • PG analog, 1st line OAG
    • Increases uveoscleral outflow
  67. Tafluprost
    • PG analog, 1st line OAG
    • Increases uveoscleral outflow
    • Ester prodrug, no preservative
  68. Dipivefrin
    • Epinephrine prodrug converted by esterases in cornea
    • Stimulates alpha-2, increases outflow for OAG
  69. 3 classes of drugs used for CAG
    • Ach agonist
    • Hyperosmotic
    • Beta blocker
  70. verteporfin
    • Deposits in new vessels, used with photodynamic therapy
    • Produces ROS to damage and occlude new vessels
    • For exudative (neovascular) AMD
  71. Pegaptanib
    • PEG anti-VEGF aptamer
    • Single mRNA strand that binds VEGF
  72. vit-E, vit-C, vit-B2, ZnO, CuO
    supplements recommended for those at risk for AMD
  73. Ranibizumab
    • rh monoclonal igG1 - binds VEGF-A
    • for neovascular AMD
  74. bevacizumab (for AMD)
    • murine-mAb against VEGF-A
    • most widely used for neovascular AMD(low cost), off-label
  75. lutein
    caratenoid, antioxidant for AMD
  76. zeaxanthin
    caratenoid, antioxidant for AMD
  77. lycopene
    caratenoid, powerful antioxidant
  78. aflibercept
    • fusion protein (VEGFR-1/2 + IgG1 Fc)
    • binds VEGF-A
    • for neovascular AMD
  79. restasis
    • topical cyclosporin
    • increases tear production, decreases inflammation

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