Heme/Lymph Module Drug Lists

Author:	blakegoodman08
ID:	113156
Filename:	Heme/Lymph Module Drug Lists
Updated:	2011-11-01 11:18:11
Description:	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

3 classes of Anticoagulants
Anticoagulants
Fibrinolytics
Antiplatelets

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

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

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

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

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

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

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

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

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

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

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

2 main Immunostimulant "classes"
Bacillus Calmette-Guerin (BCG): non-specific immunostimulant
Recombinant Cytokines

3 classes of immunostimulant Cytokines
Interferons
Interleukins
Colony-stimulating factors

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

2 immunostimulant Interleukins
Aldesleukin: IL-2; metastatic renal carcinoma, melanoma
Oprelvekin: IL-11; stimulates platelet formation

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

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

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

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

2*, 2** Cytotoxic Antibiotic antineoplastics
*Doxorubicin: topoII poison; free radical formation
*Bleomycin: Cu-chelating peptides; fragments DNA
**Daunorubicin: leukemia
**Dactinomycin: suppress hematopoiesis to pancytopenia

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

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

6 Immunosuppressant antineoplastics
azathioprine, prednisolone, antilymphocytic globulin, cyclosporine, tacrolimus, mycophenolate

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

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!

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

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

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

1 antiretroviral Integrase Inhibitor
Raltegravir: binds integrase; Tx-experienced, multi-drug resistant HIV1

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)