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49 Cards in this Set
- Front
- Back
Stimulates erythroid production and differentiation. Stimulates release of reticulocytes from the marrow
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Erythropoietin
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Thrombopoietin peptide mimetic binds to TPOR --> JAK/STAT activation --> increased platelet counts
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Romiplostim (Nplate) Thrombopoietin receptor agonists
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Promotes proliferation of megakaryocte progenitors & maturation of megakaryocytes --> increased platelet and neutrophil production
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IL-11 (Oprelvekin)
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Recombinant G-CSF binds to G-CSFR --> JAK/STAT activation --> production, maturation and activation of PMNs
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Filgrastim (Neupogen)
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Recombinant GM-CSF binding GM-CSFR --> JAK/STAT activation --> proliferation and differentiation of PMNs, eosinophils, monocytes & macrophages
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Sargramostim (Leukine)
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Binds to ATIII and accelerates inhibition of factor Xa, factor IIa (thrombin), and factor IXa
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Heparin (Unfractionated, UFH)
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Binds to ATIII and accelerates inhibition of factor Xa, minor inhibition of factor IIa (thrombin),but NOT factor IXa
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Enoxaparin (Lovenox) (Low Molecular Weight Heparin, LMWH)
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Highly basic protein that is used to terminate the action of heparin and LMWH
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Protamine Sulfate
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(Selective Factor Xa Inhibitor) Synthetic pentasacchride that promotes AT-III mediated inhibition of factor Xa
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Fondaparinux (Arixtra)
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Directly inhibit thrombin (Factor IIa) & prevents conversion of fibrinogen to fibrin
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Lepirudin (Refludan)
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Vitamin K antagonist which blocks synthesis of factors II, VII, IX, and X
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Warfarin (Coumadin)
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Promotes conversion of plasminogen to plasmin therby stimulating clot lysis
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Alteplase (Activase)
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Blocks conversion of plasminogen to plasmin, reverses fibrinolysis and attenuates bleeding
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Aminocaproic acid
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Inhibits DHFR --> inhibition of DNA synthesis
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Methotrexate
(Folate Antagonist) |
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Inhibits Purine Synthesis and purine recycling --> inhibition of DNA synthesis. Incorporated into DNA as a fradulent nucleotide --> chain termination
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Mercaptopurine
(Purine Antagonists ) |
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Inhibits DNA Polymerase -->Inhibition of DNA replication, Incorporated into DNA as a fradulent nucleotide causing chain termination
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Cytarabine
(Pyrimidine Antagonists) |
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1) Inhibition of thymidylate synthase leading to decreased production of dTMP 2)Incorporation into DNA and RNA leading to strand breaks
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5-FU (5- Fluorouracil)
(Pyrimidine Antagonists) |
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Once activated, forms covalent bonds between adjacent guanine residues, Cross links DNA --> Inhibition of DNA replication and transcription
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Cyclophosphamide
(Nitrogen Mustards) |
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Alkylates DNA -->Crosslinking DNA --> Inhibition of DNA replication and transcription
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Carmustine
(Nitrosourea Drugs) |
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Cross links DNA between adjacent guanine residues --> Inhibition of DNA replication and transcription
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Cisplatin
(Platinum Compounds) |
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1)Non-specificially Intercalates DNA --> DNA strand breaks, inhibits DNA replication and transcription
2)Inhibits Topoisomerase II --> DS breaks 3)Promotes free radical formation --> Strand breaks |
Doxorubicin
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Binds to tubulin --> Blocks polymerization of tubulin --> mitotic arrest --> cell death
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Vincristine
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Binds to tubulin & Blocks de-polymerization of tubulin --> stabilizes tubules --> mitotic arrest & cell death
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Paclitaxel
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Inhibits topoisomerase II --> permanent double strand DNA breaks
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Etoposide
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Monoclonal antibody --> binds EGFR Her-2 => growth inhibition of cells expressing the receptor
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Trastuzumab (Herceptin)
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Protein TK Inhibitor that inhibits Bcr-Abl TK by binding to the active site of this mutated protein --> decrease in constitutive activity
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Imatinab (Gleevac)
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Recombinant, humanized IgG1 monoclonal antibody that binds VEGF and inhibits VEGF/receptor interaction
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Bevacizumab (Avastin)
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Small molecule inhibitor of EGFR (HER-1) TK activity which prevents receptor autophosporylation
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Erlotinib (Tarceva)
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Promotes differentiation of promyelocytes to PMNs by facilitating the activity of the mutant PML-RARα
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Retinoic Acid (Vesanoid, aka ATRA)
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mTOR inhibitors
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Everolimus
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RAF inhibitors
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Sorafenib
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Estrogen antagonist (ERα) in breast tissue and estrogen agonist (ERβ) in non-breast tissue (uterine, endometrium) Inhibits estrogen signaling
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Tamoxifen
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Estrogen antagonist (ERα) and (ERβ)I in all tissues (represses trans-activation of both isoforms); promotes proteolytic degradation of ER but preserves ERβ
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Fulvestrant (Faslodex)
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Block the conversion of androgens to estrogens by competing with androstenediones for the active site of aromatase -->Inhibits Aromatase
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Anastrozole (Arimidex)
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Gonadotropin-releasing hormone (GNRH) agonist which causes an intial surge in LH and FSH followed by inhibition of gonadotropin release
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Leuprolide (Lupron)
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Non-steroidal anti-androgen (Inhibits the AR)
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Flutamide (Eulexin)
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Antidote to Alteplase/Thrombolytics
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Aminocaproic acid
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Antidote of sorts for Methotrexate (Protects normal cells from too much killing by methotrexate, cancer cells still targeted by MTX) DFHR converts dietary folate into the tetrahydrofolate form required for thymidine and pyrine synthesis
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Leucovorin
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Like an antidote for Heparin
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Protamine Sulfate
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Side effects for these two drugs lead to Gout
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Mercaptopurine, Vincristine
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These anti-neoplastic agents can penetrate the CNS
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Methotrexate (only intrathecal), Carmustine (readily penetrates),
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These anti-neoplastic agents have CNS toxicitiy as a side-effect
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side effects of : 5-FU, Vincristine, paclitaxel,
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Pulmonary Toxicity
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Carmustine side effects
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Dose dependent cardio-tox
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Doxorubicin side effects
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Hypertension
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Bevacizumab side effects
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Oral, rapid CYP2C8 metabolism
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Retinoic Acid (Vesanoid, aka ATRA) metabolism
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Increased risk of diabetes & cadiovascular disease
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Leuprolide (Lupron) side effects
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SEVERE persistent vomiting 1 hr. after administration, dose dependent. Nephrotox
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Cisplatin side effects
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*Acrolein (toxic) is a metabolite , and prevention of hemorrhagic cystitis
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Cyclophosphamide side effects --> use Mensa to counteract
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