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49 Cards in this Set

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