UMMC Pharm I Drug List

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UMMC Pharm I Drug List
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2012-09-08 16:12:52
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UMMC Pharm I Drug List
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  1. Acetaminophen:(Tylenol)
    • reversible analgesic/fever reducer (similar effects to Aspirin). Inhibits COX-PG synthesis in brain. Not anti-inflammatory. Can be safely used if allergies to aspirin.
    • OD causes HEPATOTOXICITY in 4 days.
    • Acetaminophen specifically works against both Prostaglandin H2 synthases.
    • Metabolized by CYP-450-2E1.
  2. Aspirin: (Salacylic Acid)
    • irreversible COX inhibitor. Anti-fever/anti-platelet/analgesic/anti-inflammatory.
    • Also down regulates leukocyte adhesion molecules.
    • Used in treatment of Rheumatoid arthritis, Rheumatic Fever, & prophylactically for platelet aggregation prevention.
    • Adverse Effects: can cause gastric bleeding (ulcers) from COX-1 inhibition & can disable immune system (contraindicated in young people for this purpose.)
    • PG’s needed for Diuretic action, so Aspirin contraindicated when in use.
    • Don’t use aspirin while pregnant or if you have Gout. 200mg/kg = toxic dose.
    • OD causes metabolic/respiratory acidosis. Can cause internal bleeding w/ warfarin/heparin/ethanol. Hinders effects of insulin, ACE inhibitors, & Probenecid (Gout).
  3. Colchicine:
    • Anti-mitotic drug (binds tubulin); reduces inflammation by PMN’s in joints.
    • Used sparingly in to treat GOUT acutely b/c of its severe toxic effects.
  4. Etanercept :
    • anti-inflammatory drug. Links TNF receptor to IgG FC portion.
    • IgG prevents inflammation from occurring.
    • ADVERSE EFFECTS: serious infections can occur by inhibiting inflammatory process.
  5. Ibuprofen:
    • reversible analgesic/fever reducer/anti-inflammatory.
    • Works equally on COX1 &2. 2-hr half life.
    • Highest pain relief score (above aspirin + codeine)
  6. Indomethacin:
    • highly ANTI-INFLAMMATORY (not routine use); some analgesia related to inflammation. HIGH TOXICITY:
    • gastric bleeding as well as esophageal/stomach perforations.
  7. Ketorolac:
    • injectable NSAID. Potent COX-1 inhibitor--lots of GI problems.
    • Use for patients who can’t take oral meds.
  8. Febuxostat:
    • selective Xanthine Oxidase inhibitor.
    • Well tolerated in Gout patients who can’t use Allopurinol.
    • Metabolically inactivated, so no need for adjustment for the renally impaired.
  9. Probenecid :
    • Gout treatment. Decreases Uric Acid by blocking tubular reabsorption.
    • But only works at sub-therapeutic levels??? Aspirin negatively interacts with it.
  10. Thalidomide:
    • highly TERATOGENIC drug.
    • Reduces levels of TNF-a. (anti-inflammatory).
    • Treat Mult. Myeloma/AI skin diseas.
  11. Cyclophosphamide :
    • alkylating drug that slows/stops cell growth.
    • Acts by cross-linking DNA/RNA/proteins in S-phase.
    • Is a Prodrug. Used as a chemotherapy drug for lymphomas & leukemias.
    • Also used to treat AI diseases (Lupus nephritis).
    • ADVERSE EFFECTS: bone marrow suppression (Trombocytopenia & Neutropenia). Bladder Cancer.
  12. Cyclosporine:
    • immunosuppressive drug. Inhibits dephosphorylation of Calcineurin (secondary messenger needed for T-cell DIFFENTIATION);
    • prevents secretion of IL-2 . Lack of T-cell proliferation affects B-cells.
    • Used in treating Grafts & autoimmune diseases.
    • ADVERSE EFFECTS: Nephrotoxicity & Recurrent infections.
  13. Methotrexate:
    • immunosuppressive drug. Treats inflammatory disease.
    • Inhibits Dihydrofolate-Reductase (folate metabolism)-required for DNA synthesis-
    • greater toxicity on rapidly proliferating cells, so inhibits proliferation of lymphocytes.
    • Used as a CHEMO drug—affective against cancer & Rheumatoid A.
    • Adverse: immune-suppressive/Teratogen.
  14. Mycophenolate Mofetil:
    • immunosuppressive PROdrug.
    • Selectively inhibits lymphocyte purine synthesis.
    • Often used in treatment of Lupus Nephritis.
    • Adverse = (increased infection)
  15. Muromonab:
    • immunosuppressive anti-CD3 MAB (CD3= TCR receptor complex)—targets T-cells.
    • Rho(D) immune Globulin : injectable anti-D IgG AB’s; attaches to and kills Rh+ RBC’s in maternal blood.
    • Prevents mother from mounting immune response to Rh+ RBC’s & forming her own anti-D+ Ab’s.
    • prevents Erythroblastosis Fatalis.
  16. Sirolimus:
    Immunosuppressive drug. Binds FK (needed for intracellular T & B cell PROLIFERATION signal from IL-2)
  17. Tacrolimus:
    • Immunosuppressive drug. Binds to FKBP(responsible for dephosphorylating Calcineurin)-same as cyclosporine
    • ---used to Treat ATOPIC DERMATITIS (Exzema)
  18. Aldesleukin:
    synthetic IL-2… upregulates activity of NK & T cells. used to treat metastatic Renal Cell Carcinoma
  19. Alefacept:
    immunosuppressive: blocks LFA/CD2 costimulation signal on T-cells—APOPTOSIS. Used to treat Psoriasis & T-cell Lymphomas
  20. Requirements for Glucocorticoid anti-inflammatory effects:
    • C-11 Hydroxyl group,
    • C-20-21 side chain,
    • C-4,5 dbl bond
  21. General Glucocorticoid method of action via intracellular receptor interaction:
    • -Directly by: TRANSREPRESSION (decreased transcription)of NF-kB & AP-1 genes (pro-inflammatory secondary messengers)
    • -Indirectly: upregulating ANNEXINS, lipocortin, that in turn down-regulates PLA2, COX, & NO expression
    • -also upregulates IkB-----another inhibitor of NF-kB transcription
    • -reduce tissue histamine levels
  22. Physiologic Effects caused by Glucocorticoids:
    • -increased gluconeogenesis & decreased glucose use in peripheral tissues (vital organ survival).
    • -protein & bone degradation
    • -high amounts can affects salt/water balance (bind to mineralocorticoid receptors)
    • *Suppress Inflammatory/Immune responses
    • -increase RBC’s, but Decrease WBC’s
    • -delays wound healing (Fibroblast proliferation decreased)
  23. Common Uses for Glucocorticoids:
    • -prevent Septic Shock & Fetal Distress Syndrome (long acting cross placenta better)
    • -Arthritis & organ transplants
    • -skin diseases (ATOPIC DERMATITIS---EXZEMA) & allergies
  24. Side Effects & Contraindications:
    • -Hypertension & Hyperglycemia (insulin resistance)
    • -myopathay & osteoporosis
    • -increases opportunistic infections & Glaucoma
    • *contraindications: Growth retardation, Peptic Ulcers, Osteoporosis
    • To Minimize Side-Effects:
    • -Timing (w/circadian rhythm), pulse dosing, use other drugs adjunctively, regional administration, use of short/medium acting steroids, or alternate days of treatment.
  25. Cortisol:
    • short acting interacts w/ glucocorticoid receptors (affinity for Mineralocorticoid receptors, but converted to
    • Cortisone which can be considered inactive metabolite or prodrug); formed in the adrenal cortex.
  26. Cortisone:
    • Pro-drug of cortisol (lacks 11-OH group)-activated in body. short acting anti-inflammatory (usually topical).
    • Higher efficacy than cortisol (inc. gluco-receptor affinity, dec. mineralo-receptor affinity, longer duration of action, longer half-life, etc.)
  27. Budesonide: (Rhinocort)
    • short acting anti-inflammatory (usually topical for asthma and intranasally). (10% bioavailability!)
    • Addition of 16,17-butylidenbid[oxy] moiety increases absorption (lipophilic)
  28. Fluticasone: (Flonase)
    • short acting anti-inflammatory (intranassally & Topically). (0% Bioavailability!)
    • Adding lipophilic side chain (proprianate) enhances efficacy especially when applied topically and is used for asthma and dermatology.
  29. Prednisolone:
    Medium-acting steroid. 1-2 double bond slows liver metabolism increasing glucocorticoid effect
  30. Methylprednisolone:
    Medium-acting steroid. Only differs from prednisolone by 6-methyl
  31. Prednisone:
    • Prodrug of Prednisolone. (11-OH missing).
    • Converted in body to active (replaces 11 ketone with 11-OH).
    • Differs from cortisol only by 1-2 double bond
  32. Triamcinolone:
    • Medium-acting steroid. Differs from prednisolone with 9-flouride.
    • 16-17 acetonide analog used topically for dermatological disorders
  33. Beclomethasone:
    • long acting steroid. 9-Chloride and 16-methyl.
    • Requires esterase cleavage of side-chain for activation.
    • Diproprianate beclamethasone can be used in asthma treatment.
  34. Betamethasone:
    • only difference from beclomethasone is 9-flouride.
    • Diproprianate betamethasone used for dermatology.
  35. Dexamethasone: (Decadron)
    • long acting steroid. Requires esterase cleavage of side-chain for activation.
    • Can be used in asthma treatment. Same structure as betamethasone?
  36. Dinoprostone:
    marketed PGE2 for uterine contraction
  37. Mifepristone:
    combo of antiprogestins & PGE2 (Dinoprostone); causes abortion.
  38. Alprostadil:
    PGE1 used to treat Erectile Dysfunction; also used to maintain Patent Ductus Arteriosus
  39. Epoprostenol:
    PGI2 used to treat hypertension (vasodilatory effects)
  40. Zileuton:
    5-LOX inhibitor; treats asthma (Leukotrienes D4 & C4 mainly responsible for asthma effects)
  41. Misoprostol:
    • analogue of PGE1; used to treat/prevent gastric ulcers (from NSAIDS);
    • PG’s protect stomach
  42. A. Alprostadil
    • (PGE1) relaxes smooth muscle.
    • Maintains the ductus arterosus patent in some neonates awaiting cardiac surgery.
    • This counteracts the decrease in PGE2 levels that lead to closure.
    • In delayed closure of the ductus arteriosus, COX inhibitors are often used to inhibit synthesis of PGE2 and close the ductus.
    • Also used in the treatment of erectile dysfunction.
  43. B. Misoprostol
    • (PGE1 derivative) is a cytoprotective prostaglandin used in preventing peptic ulcers in those taking dose NSAID therapy.
    • Also used in combination with mifepristone (RU486) for terminating early pregnancies.
  44. C. Dinoprostone
    • (PGE2) PGE2 and PGF2α are used in obstetrics to induce labor.
    • Theoretically, PGE2 and PGF2α should be superior to oxytocin for inducing labor in women with preeclampsia-eclampsia
    • or cardiac and renal diseases because they have no antidiuretic effect.
    • In addition, PGE2 has natriuretic effects.
    • In cases of intrauterine fetal death, the prostaglandins alone or with oxytocin seem to cause delivery effectively.
    • These prostaglandins appear to soften the cervix by increasing proteoglycan content and
    • changing the biophysical properties of collagen.
  45. D. Epoprostenol
    • (PGI2) : prostacyclin used to treat pulmonary hypertension;
    • decreases bronchial and vascular tone; decreases platelet aggregation in dialysis machines.
  46. E. Latanoprost/Travoprost
    Topically active PGF2α derivatives used in ophthalmology to treat open angle glaucoma.
  47. F. Zafirlukast/Montelukast
    • (leukotriene receptor antagonists): potent bronchodilators used to treat asthma;
    • Leukotrienes (LTC4, LTD4 and LTE4) are heavily involved in asthmatic constriction;
    • montelukast does not inhibit CYPs 2C9 and 3A4 so would not affect elimination of other drugs as much as Zafirlukast.
  48. G. Zileuton
    (5-LOX inhibitor): Inhibits leukotriene synthesis; used in asthma treatment; not as effective as the leukotriene receptor antagonists.
  49. Anti-Histamines:
    • *can cross placenta
    • *young eliminate more rapidly than old
    • *H1 = constriction (large vessels/bronchioles); H2 = dilation (precapillary arterioles)
    • General H1 antagonists: block broncho/vasoconstriction, edema, flare, itch, & rhinitis associated w/ H1 receptors
    • -hypotensive effect still not controlled b/c H2 dilation involvement
    • *1st Generation = sedating (lipophilic); 2nd Generation = non-sedating normally; (Ethanol can compound sedative effect)
    • *H1 antagonists not indicated for common cold, but do relieve symptoms (rhinitis, conjunctivitis); “drying” effect.
    • *H1 antagonist Side Effects: sedation, GI problems, dry mouth/cough/dysuria (anti-Ach-drying),tachycardia, allergic
  50. diphenhydramine (Benadryl):
    • 1st Generation is an Ethanolamine; lipophilic, so can cross BBB---SEDATIVE effects.
    • Also inhibits sodium channels at high doses (anesthetic.)
  51. dimenhydrinate (Dramamine):
    • 1st Generation an Ethanolamine; lipophilic, so crosses BBB (sedative).
    • Also antagonizes the muscarinic Ach receptors (treats vertigo/motion sickness)
  52. chlorpheniramine:
    1st Generation an Alkylamine; known to have side effects of CNS stimulation.
  53. promethazine (Phenergan):
    1st Generation anti-cholinergic (muscarinic); ANTI-EMESIS. Anesthetic @ high doses (Na channels).
  54. Acrivastine:
    2nd gen. H1 antagonist.
  55. fexofenadine (Allegra):
    2nd Generation excreted in feces. (Piperadine)
  56. loratadine (Claritin):
    2nd Generation prodrug that is activated by p450 to desloratidine (Piperadine)
  57. desloratadine (Clarinex):
    2nd Generation already active form of Loratidine (Claritin)---(Piperadine)
  58. cetirizine (Zyrtec):
    2nd gen H1 antagonist. Piperazine family
  59. cromolyn sodium:
    2nd Generation inhibits mast cell degranulation by stabilizing their membrane. Prophylactic for asthma.
  60. Nedocrimil:
    has same effect as cromolyn sodium

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