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Heme and Oncology
Pharmacology: Heme & Oncology
| Question | Answer |
|---|---|
| 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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