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Heme and Oncology

Pharmacology: Heme & Oncology

1. Which chemotherapeutic agents have the greatest efficacy against treating gliomas? 2. Why? 1. nitrosureas (carmustine, lomustine) 2. ability to cross the blood-brain barrier
How do alkylating agents induce death in cells? p53-dependent apoptosis
1. Metabolite of cyclophosphamide that leads to hemorrhagic cystitis 2. What is given to prevent this toxicity? 1. acrolein 2. mesna (binds the toxic metabolite acrolein)
Cyclophosphamide antitumor mechanism Cyclophosphamide is metabolized by cytochrome P450 to phosphoramide mustard which forms DNA crosslinks
Side effects associated with drugs: 1. hemorrhagic cystitis 2. cardiotoxicity 3. peripheral neuritis 4. pulmonary fibrosis 5. ototoxicity 1. cyclophosphamide 2. doxorubicin 3. vincristine 4. busulfan, bleomycin 5. cisplatin
1. Antimetabolite associated with increased toxicity with allopurinol 2. Why is this interaction seen 1. 6-mercaptopurine (azathioprine which is metabolized to 6-MP) 2. the drug is metabolized by xanthine oxidase, the enzyme inhibited by allopurinol
Cancer drug that: 1. inhibits topoisomerase II 2. intercalates DNA 3. inhibits microtubule formation 4. inhibits microtubule disassembly 1. etoposide 2. dactinomycin/doxorubicin 3. vincristine 4. paclitaxel
Used to reverse myelosuppression cause from Methotrexate toxicity Leucovorin
Clinical use of retinoic acid as an antineoplastic: acute promyelocytic leukemia (AML M3)
Imatinib 1. Mechanism of action 2. Clinical use 1. inhibits the bcr-Abl tyrosine kinase (philadelphia chromosome) 2. chronic myelogenous leukemia
Avastin mechanism of action monoclonal antibody to endothelial growth factor (VEGF) to inhibit tumor angiogenesis
1. Folic acid analog that inhibits dihydrofolate reductase 2. Pyrimidine analog that inhibits thymidylate synthase 3. Inhibits ribonucleotide reductase 1. Methotrexate 2. 5-fluorouracil 3. Hydroxyurea
Alkylating agent capable of crossing blood brain barrier Nitrosureas (carmustine, lomustine)
1. Anti-neoplastic that causes nephrotoxicity and acoustic nerve damage 2. GnRH agonist used for treatment of metastatic prostate carcinoma 1. Cisplatin, carboplatin 2. Leuprolide, Goserelin, Naferelin
Monoclonal antibody against HER-2 Trastuzumab
1. Androgen receptor antagonist 2. Monoclonal antibody against CD20 1. Flutamide 2. Rituximab (CD20 functions in the immunre response)
Mechanism of action: 1. 6-mercaptopurine, 6-thioguanine 2. Cytarabine (ara-C) 1. inhibits de novo purine synthesis 2. Pyrimidine antagonist
Used for childhood tumors (Wilm's tumor, Ewing's sarcoma, rhabdomyosarcoma) Dactinomycin (ACTinomycin D) - children ACT out
1. SERM that may ↑ the risk of endometrial carcinoma 2. SERM that does not present a risk for endometrial carinoma 1. Tamoxifen 2. Raloxifene
Heparin: 1. site of action 2. antidote 3. mechanism of action 4. monitoring 1. blood 2. protamine 3. activates antithrombin III which ↓ thrombin (factor II) and factor X 4. PTT
Warfarin 1. site of action 2. antidote 3. mechanism of action 4. monitoring 1. liver 2. fresh frozen plasma and vitamin K 3. vitamin K antagonist 4. PT/INR
Which coagulation factors are degraded by: 1. heparin 2. LWMH 3. Lepirudin 4. Rivaroxaban 1. factor X & II (thrombin) equally 2. factor X > factor II 3. factor II (thrombin) 4. factor X
1. Which anticoagulation drug is initially prothrombotic? 2. How does warfarin effect other drugs metabolized by cytochrome P450 1. warfarin 2. warfarin is metabolized by cytochrome P450 and causes buildup of other drugs that use it for metabolism as well
Mechanism of action 1. abciximab 2. clopidogrel 3. eptifibatide 1. gpIIb/IIIa receptor inhibitor 2. ADP receptor antagonist 3. gpIIb/IIIa receptor inhibit
1. Pharmacological treatment of peripheral vascular disease? 2. Action of Alteplase 1. cilostazol 2. converts plasminogen to plasmin
Cilostazol mechanism and effects: inhibits phosphodiesterase → ↑cAMP → vasodilation & inhibition of platelet aggregation
1. thrombin inhbitor given to patients with heparin-induced thrombocytopenia 2. anticoagulation given to pregnant patients 1. bivalirudin, lepirudin 2. heparin
1. warfarin-induced digital necrosis is associated with what deficiency? 2. Which cytochrome isoenzyme metabolizes clopidogrel and warfarin? 1. protein C 2. CYP2C9
1. Which heparinoid has the lowest incidence of causing heparin induced thrombocytopenia 2. mechanism of action of dipyridamole 1. fondaparinux 2. ↓ adenosine uptake, phosphodiesterase inhibitor
1. Which thrombolytic forms a complex with plasminogen to work? 2. Which thrombolytic acts specifically on fibrin-bound plasminogen? 1. streptokinase 2. alteplase
How does aspirin effect: 1. prothrombin time 2. PTT 3. bleeding time 1. no effect 2. no effect 3. increase
tPA antagonist Aminocaproic acid
Mechanism of action: 1. Clopidogrel 2. Enoxaparin 3. Aspirin 1. inhibits platelet aggregation by irreversibly blocking ADP receptors 2. low molecular weight heparin acts more on Xa 3. irreversibly inhibits COX to prevent conversion of arachidonic acid to thromboxane A2
How does heparin cause thrombocytopenia? heparin binds platelet factor IV, causing antibody production
Drug used in ischemic stroke prevention and causes neutropenia. Ticlopidine
What activates 6-mercaptopurine? HGPRTase
Created by: amichael87



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