Heme/Lymph Module Drug Lists

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  1. 3 classes of Anticoagulants
    • Anticoagulants
    • Fibrinolytics
    • Antiplatelets
  2. 6 Anticoagulants
    • Heparins: aka HMWH; activates antithrombinIII
    • LMWH/Enoxoparin: specific inhibition of factorXa
    • Lepirudin: binds soluble and bound thrombin
    • Warfarin/coumadin: inhibits vitK epoxide reductase
    • Drotrecogin-α: recomb human Activated Protein C; cleaves fVa,VIIa
    • Dabigatran etexilate: novel oral anticoag; stroke; direct competitive inhibition of thrombin
  3. 4 Fibrinolytics (anticoag)
    • Streptokinase: activates plasmin; not available in US
    • Alteplase: converts fibrin-bound plasminogen to plasmin
    • Reteplase: same as alteplase, also binds fibrin
    • Tenecteplase: same as reteplase
  4. 3 antiplatelet drugs (anticoag)
    • Aspirin: blocks thromboxane A2 synth via irreversible COX inhibition
    • Clopidogrel: blocks platelet ADP receptors, preventing fibrinogen-based activation
    • Abciximab: inhibiting MAB against IIb/IIIa, preventing activation
  5. 6 drugs that facilitate clotting
    • VitK: essential clotting cofactor; coumarin tox
    • Factor VIII: clotting factor replacement
    • Factor IX: clotting factor replacement
    • Desmopressin: increases plasma [clotting factors]
    • Aminocaproic acid: not on US market
    • Protamine sulphate: binds heparin, blocks anticoag effect
  6. 9 drugs against Plasmodial infection (malaria)
    • Proguanil: prophylaxis/suppression of P. falciparum, acute suppression of P. vivax
    • Primaquine: Gametocytocidal for all Plasmodium; hypnozoitocidal for P. vivax and ovale
    • Chloroquine: schizonticidal for all sensitive Plasmodium spp
    • Quinine: same as chloroquine
    • Quinidine: Tx of non-immune persons and multidrug resistant falciparum,
    • Mefloquine: prophylaxis for multidrug resistant falciparum
    • Doxycycline: same as mefloquine
    • Artemisinin: Tx of non-immune persons for falciparum
    • all of the above have same MoA - buildup of free radicals in microbe
    • Antifolates: Pyrimethamine+sulfadioxine; inhibits parasite dihydrofolate reductase
  7. 8 drugs against other protozoal (non-Plasmodial) infections
    • Metronidazole: Entamoeba hystolytica, Giardia lamblia, and Trichomonas vaginalis; only approved nitroimidazole in US; prodrug that acts as e- sink for parasite
    • Diloxanide furoate: given with metronidazole
    • Tinidazole: same as metronidazole
    • Nifurtimox: Trypanosoma cruzi; free radical production
    • Stilbogluconate Na: Leishmania donovani;
    • Paromomycin: same as stilbo; also Cryptosporidium
    • Suramin: Trypanosoma cruzi
    • Tetracyclines: Balantidium coli
  8. 4 classes of Immunosuppressive drugs
    • Toxic to all dividing cells
    • Toxic to lymphocytes
    • Toxic to a subpopulation of immune cells
    • Molecular targeted MABs against cytokines w/ toxic outcomes
  9. 1 Pan-Cytotoxic immunosuppressive\
    • Azathioprine: de novo purine synth, acts in S phase; also antimalignant/arthritic
    • Mercaptopurine: downstream metabolite of azathioprine, same MoA
    • Allopurinol: given concomittantly; can increase mercaptopurine tox
  10. 6 Lymphotoxic immunosuppressives
    • ALG: antilymphocytic globulin; activates complement against T-cells
    • IV Ig: pooled Ig's from healthy donors
    • Rho (D) Ig: anti-Rh IgG to prevent newborn hemolysis
    • Muromonab-CD3: blocks T-cell antigen recognition; acute renal allograft rejection
    • Asparaginase: cleaves Asn to Asp, robbing from AA pool; anticancer
    • Glucocorticoids: genetic immunosuppression
  11. 4 immunosuppressives toxic to subpopulations of immune cells
    • Cyclosporine: binds cyclophillin-A (blocks calcineurin), suppresses IL-2
    • Tacrolimus: 10-100x as potent as cyclosporine; binds FKBP12 (blocks calcineurin) to suppress IL-2
    • Sirolimus: inhibits mTOR, stopping G1->S progression
    • Mycophenylate mofetil: inhibits IMP dehydrogenase (de novo guanine synth), selective for B/T-cells
  12. 4 molecular-targeting immunosuppressives
    • Etanercept: TNF-α receptor
    • Infliximab: TNF-α antibody
    • Abciximab: non-specific MAB (IIb/IIIa, others)
    • Daclizumab: IL-2 receptor antibody, prevents CD4 activation
  13. 2 main Immunostimulant "classes"
    • Bacillus Calmette-Guerin (BCG): non-specific immunostimulant
    • Recombinant Cytokines
  14. 3 classes of immunostimulant Cytokines
    • Interferons
    • Interleukins
    • Colony-stimulating factors
  15. 3 immunostimulant Interferons
    • Interferon-α: upreg MHC-I, downreg MHC-II; hairy cell leuk, hepB/C
    • Interferon-β-1a/1b: multiple sclerosis
    • Interferon-γ: phagocytes; chronic granulomatosis disease
  16. 2 immunostimulant Interleukins
    • Aldesleukin: IL-2; metastatic renal carcinoma, melanoma
    • Oprelvekin: IL-11; stimulates platelet formation
  17. 4 immunostimulant Colony-Stimulating Factors
    • Filgrastim: G-CSF, stimulates bone marrow recovery during chemo and PMN proliferation
    • Sargramostim: GM-CSF, non-lineage specific; myeloid recovery after chemo
    • Epoetin-α: recombinant EPO; given with cisplatin
    • Thrombopoietin: either molecule or fusion protein of GM-CSF and IL-3
  18. 7 major classes of Antimalignant drugs
    • Antimetabolites: rob cells of products necessary for division; e.g. methotrexate, blocks THF synth
    • Alkylating Agents: x-links DNA to prevent transcription/translation
    • Cytotoxic antibiotics: Cell-Cycle NonSpecific (CCNS), generally break or otherwise interfere with DNA
    • Natural Products: depending, either topoisomerase or tubule activity
    • Hormones: depends on cancer
    • Immunosuppresants: name says it all
    • Others: interferon, ILs, antibodies, platinums
  19. 2*, 2** Antimetabolite antineoplastics
    • *Methotrexate: blocks DiHydroFolate Reductase
    • *5-Fluorouracil: incorporated into RNA, rendering it useless
    • **Capecitabine: prodrug of 5-FU, non-responsive colorectal and breast
    • **Cytarabine: blocks DNA elong; AML drug
    • Azathioprine/mercaptopurine - anti-PRPP stuff
  20. 2*, 2** Alkylating antineoplastics
    • *Cyclophosphamide: prodrug -> nitrogen mustard, acrolein that x-links DNA; SIADH
    • *Cisplatin: directly x-links DNA
    • **Carmustine: CNS tox, CNS cancers
    • **Temozolamide: success against malignant gliomas
  21. 2*, 2** Cytotoxic Antibiotic antineoplastics
    • *Doxorubicin: topoII poison; free radical formation
    • *Bleomycin: Cu-chelating peptides; fragments DNA
    • **Daunorubicin: leukemia
    • **Dactinomycin: suppress hematopoiesis to pancytopenia
  22. 3*, 2** Natural antineoplastics
    • *Vincristine, *Vinblastine: alkaloids, bind tubulin preventing microtubule assembly
    • **Etoposide: stabilizes topoII-DNA complex, breaking dsDNA
    • **Topotecan: topoI inhibitor
    • *Paclitaxel/docetaxel: taxanes; inhibit microtubule disassembly
  23. 3*, 4**, Hormone/Antihormone antineoplastics
    • *Tamoxifen: anti-estrogen
    • *Prednisone: replacement
    • *Prednisolone: replacement
    • **Anastrazole: aromatase inhibitor
    • **Finasteride: DHT inhibitor (5-α reductase)
    • **Flutamide: antiandrogen
    • **Leuprolide: GRH; inhibits LH/FSH
  24. 6 Immunosuppressant antineoplastics
    azathioprine, prednisolone, antilymphocytic globulin, cyclosporine, tacrolimus, mycophenolate
  25. 1*, 5** "other" antineoplastics
    • *Cisplatin: binds DNA, nephrotox
    • **Asparaginase: prevents Asn synth; ALL
    • **Rituximab: chimeric anti-CD20, facilitating complement; add w/ CHOPS
    • **Trastuzumab: tx of HER2 breast cancer
    • **Hydroxyurea: inhibits ribonucleotide reductase (no ribo -> deoxy)
    • **Imatinib mesylate: inhibits BCR-ABL tyr-kin in CML
  26. 5 classes of Antiretroviral (HIV) Drugs
    • NRTI: nucleotide reverse-transcriptase inhibitors (ZELDAS)
    • NNRTI: non-nucleotide reverse transcriptase inhibitors (DEN)
    • PI: protease inhibitors (NEVER = navir)
    • Integrase Inhibitors: prevent viral genome from entering host genome (STOP = ralt, Spanish for stop)
    • Entry Inhibitors: block viral entry (SMOKING = fumar, enfu and marav)
    • Zeldas Den Never Stop Smoking!
  27. 6 NRTIs
    • Zidovudine: front-runner in control, reduces vert transmit; cx lamivudine, myelosuppressives
    • Emtricitabine: HIV+hepB; fluorinated lamivudine
    • Lamivudine: HIV1+hepB (potent); pancreatitis and high resistance risk
    • Didanosine: pancreatic tox, blindness; cx delavirdine, indinavir, atazanavir
    • Abacavir: general NRTI
    • Stavudine: cx advanced immunosuppression
  28. 3 NNRTIs
    • Delavirdine: skin rash and Stevens-Johnson; cx pregnancy
    • Efavirenz: depression, mania, psychosis; cx pregnancy
    • Nevirapine: Stevens-Johnson, fulminant hepatitis; single dose vert transmit protection
    • binds HIV1 reverse transcriptase, inhibiting viral DNA pols
  29. 5 antiretroviral PIs
    • Atazanavir: no Cushings; Cx indinavir (CYP3A4 inhibitor)
    • Indinavir: CYP3A4 inhibitor
    • Lopinavir: combos with ritonavir
    • Ritonavir: potent CYP3A4 inhibitor, combos with other PIs for lower effective dose
    • Saquinavir: Cx delavirdine
    • all of the above are also Cx with same as NNRTIs
  30. 1 antiretroviral Integrase Inhibitor
    Raltegravir: binds integrase; Tx-experienced, multi-drug resistant HIV1
  31. 2 antiretroviral Entry Inhibitors
    • Enfuvirtide: binds gp41, preventing conf. change required for fusion to cell (f = 41)
    • Maraviroc: binds host CCR5, preventing viral adhesion (specific to R5 strain)
Card Set
Heme/Lymph Module Drug Lists
Lists all the major types, classes, and drugs for the Heme/Lymph module of semester 3, along with primary drug facts; use for name recognition
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