S3M2 pharm

  1. Heparin
    • - increases AT-III activity==> b/d of IXa, XIIa, XIIa, Xa and IIa
    • - inhibit platelet aggregation
    • - venous thrombosis, Pulm embolism, unstable angina, acute MI, ballon angioplasty
  2. LMWH
    • - Xa inihibitor
    • - no effect on platelets
  3. Fondaparinux
    • - synthetic LMWH
    • - Xa inhibitor
    • - no effect on platelets
  4. Lepirudin
    - thrombin (IIa) inhibitor
  5. Warfarin
    • - VKOR (Vit K epoxide reductase inhibitor
    • - inhibits formation of II, VII, IX and X
    • -  APC inhibitor (necrosis?)
    • - highly protein bound
  6. Drotecogrin- alpha
    • - rAPC
    • - Va and VIIIa inactivator
    • - reduce mortality in septic pts
  7. Dabigatran etixilate
    • - competative thrombin (IIa) inhibitor
    • - no antidote
    • - prevents thrombin induced platelet aggregation and clot formation
  8. Atelpase
    • - plasminogen activator (to plasmin)
    • - leads to fibrin degradation
    • - MI and Ichemic stroke (within 3 hours) and pulmonayry thromboembolism
  9. ASA
    • - irreversible inactivation of COX1
    • - inhibits synthesis of TXA2
  10. Clopidigrel
    - blocks ADP-r on platelets, so fibrin cannot bind, inhibitig aggregation
  11. Abciximab
    - Fab fragment against glucoprotein IIb/IIIa
  12. Vitamin K
    • - cofactor for VKOR
    • - counteract warfarin toxicity, hemorrhagic disease of the newborn, hypoprothrombinemia
  13. Thrombin
    • - rIIa (rThrombin)
    • - intraocular surgeries to control hemorrhaging
  14. EACA/ Aminocaproic acid/ epsilon aminocaproic acid
    • - competatively inhibits plasminogen activation
    • - inhibits fibrinolysis
    • - reduce hemorrhage in CABG
    • - TOTAL C/I: DIC
  15. protamine sulfate
    • - binds heparin tightly, reversing its effect
    • - after cardiac surgery
  16. Proguanil
    • sporontocidal produg
    • effective against hepatic preerythrocytic forms of P falciparum and P vivax
    • used with atovaquone for MDR faaciparum and vivax
  17. Primaquine
    • used for latent tissue (hyponozoite forms of vivax and ovale with chloroquine, gametocytic.
    • can also be used a prophylactic
    • **C/I in G6PD deficiency (==>acute  IV hemolysis and methemoglobinuria)**
  18. chloroquine
    • effective against INTRAerythrocytic forms of plasmodia by preventing heam (parasitic waste product) conversion
    • inhibits actions of TNF-alpha, gametocytic (v, o, m)
    • **A/E: convulsions and, at high doses, retinopathy and ototoxicity** 
    • safe prophylaxis for prego
  19. Quinine
    • prototypical blood schizonticide and gametocytic (vivax and malariae)
    • prevent haem conversion (like chloroquine)
    • **A/E: cinchonism, hypogly, hypoTN, thrombocytopenia**
    • NO PREGO
  20. pyrimethamine and sulfadioxine
    3 uses 
    • prophylaxis of falciparum, combo with quinine to tx MDR falciparum, 2 doses for prego with chloro-R falciparum
    • inhibits pDHFR
  21. drugs that act on asexual erythrocytic stage of malarial infection to interrupt erythrocytic schizogony, thus terminating clinical attacks
    • chloroquine, quinine, quinidine, mefloquine, doxycycline, artermisinin
    • MADQCQ 
  22. Metronidazole
    • tx of certain protozoa- amebiasis, trichomniasis, giadiasis, balantdiasis and hepatic abscess
    • deprive anaerobe of reducing equivalents
    • amplifies warfarin 
    • **metallic aftertaste, No EtOH (disulfiram- like effects) **
  23. Nifurtimox
    • tx of acute Chagas disease (prolonged therapy req'd)
    • **seizures and polyneuritis** 
    • no early prego 
  24. Stibogluconate
    • tx for leishmaniasis
    • becomes highly toxic during therapy (cardiac toxicity!!)
  25. Levamisole
    • antiparasitic drug that stimulates maturation/proliferation of T cells- Dukes Stage C colon cancer
    • **A/E: agranulocytosis**
  26. BCG
    non specific immunostimulant for the treatment of bladder cancer
  27. Thalidomide
    • used in leprosum and Chrons disease
    • inhibits TNF-alpha production
  28. INF- alfa
    • enhances expression of MHC-I, decreases expression of MHC-II
    • hairy cell leukemia, Hep B and C, HPV(imiquimod)
  29. INF- beta
    approved for MS
  30. INF- gamma
    • promotes CTL response
    • tx CGD
    • antiviral, proinflammatory, influences T cell subset differentiation 
  31. Aldesleukin
    • r-IL-2
    • promotes lymphoid cell differentiation-->CTLs and NK
    • metastatic melanoma and metastatic renal cell carcinoma
  32. Oprelvekin
    • r- IL-11
    • tx thrombocytopenia
  33. Filgrastim
    • G-CSF (granulocyte colony stimulating factor)
    • increase n0 production
    • stimulates bone marrow recovery during chemo 
  34. Sargramostim
    • non lineage specific hematopoetic agent
    • promotes myeloid recovery in high dose chemo patients:
    • - Non-Hodgkins lymphoma
    • - acute lymphoblastic leukemia (ALL)
    • - Hodkins pts undergoing BM transplant
    • - AIDS neutropenia
    • **C/I in HF, pulm edema, yeast allergy**
  35. Epoetin-alfa
    • r- erythropoetin
    • tx of anemia
    • adequate Fe intake is required 
  36. Thrombopoetin
    • selectively stimulates megakaryocytopoesis
    • tx anemia, neutropenia and thrombocytopenia in high dose chemo and platelet recovery in hematopeitic stem cell transplant
  37. Azathiprine
    • antimetabolite of purine synthesis that is indiscriminately toxic to dividing cells, PRPP inhibitor
    • tx to prevent graft rejection, AID (SLE, RA,etc), T4HS 
    • prevents clonal expansion (B and T), prevent de novo purine syn, inhibit S phase in all cells
    • **interaction with allopurinol** (mercaptopurine accum)
  38. mercaptopurine
    • PRPP inhibitor
    • tx some cancers and as an immunosuppressant
    • utilizes XO, so concaminent use of allopurinol may result in toxic levels of MP
  39. antilymphocytic globulin (ALG)
    • anti-Tcell horse Ig
    • used to treat acute rejection of kidney t/p, prevent rejection following kidney t/p, prevent GVHD in BM t/p, treat aplastic anemia 
    • **A/E: anaphylaxis (T1HS) and serum sickness: T3HS- fever, rash, joint pain
  40. Rho (D) Ig
    • prevention of hemolytic disease of the newborn
    • given to Rh- pregos
  41. Immune Globulin (IVIG)
    • polyclonal human Ig (mostly IgG)
    • tx Kawasaki's disease, subacute SLE, thrombocytopenic purpure
  42. Muronab
    • - anti-CD3 Ig of thymocytes and primed T-cells
    • - use: acute renal allograft rejection, esp when corticosteroid therapy is not working
    • **A/E: cytokine release syndrome, pulmonary edema (avoid in hypervolemic pt), blood dyscrasias**
  43. cyclosporine
    • calcineurin inhibitor (prevents activation (de-P of TF NF-AT-------X----> IL-2 t/s) (binds cyclophilin)
    •  use: prevent t/p rejection (must be used before t/p performed), treat GVHD, uveitis, severe psoriasis
    • very hydrophobic and hard to solublize
    • **nephrotoxic**
  44. Tacrolimus
    • -macrolide Abx that prevents IL-2 t/s
    • - used as cyclosporine substitue to prevent transplant rejection, also used topically for atopic dermatitis
    • **seizures, nephro/neuro-toxicity**
  45. Sirolimus
    • macrocytic lactone- immunosuppressive
    • acts like cyclosporine by preventing IL-2 t/s
    • inhibits mammalian kinase mTOR (molecular tgt of rapamycin)
    • NOT nephroxic
  46. mycophenolate
    • prodrug converted to mycophenolic acid 
    • inhibitor of inosine monophosphate dehydrogenase (guanine synthese RLS)
    • prevent allogenic graft rejection, SLE
    • selectively inhibits T and B proliferation and function 
    • **A/E: leukopenia, neutropenia, cytomegalo sepsis
    • used INSTEAD of azothoiprine in immunosuppression
  47. Etanercept
    • TNF-alpha FUSION PROTEIN (prevents action) 
    • tx: RA, cancer (with methotrexate), psoriasis, immunosupp
  48. Infliximab
    • anti-TNF-alpha Ig (prevents binding)
    • tx: RA and Chrons
    • **C/I: infections, sepsis, chronically immunosuppressed**
  49. Daclizumab
    • binds IL-2 receptor, preventing CD4 Tcell activation
    • tx: acute transplant rejection
    • **A/E: dyspnea, fever, GI distress, hypoTN, HTN, angina** 
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S3M2 pharm
S3M2 pharm