Heme:Onc Pharm Flashcards
(101 cards)
1
Q
Mech: Inhibits dihydrofolate reductase.
A
Methotrexate mechanism of action?
2
Q
Used for Leukemia, lymphomas, choriocarcinoma, sarcoma, rheumatoid arthritis.
A
Methotrexate
3
Q
Side Effects: Myelosuppression. Reversible with leucovorin (folinic acid). Hepatotoxicity (fatty liver), muscositis, teratogenic.
A
Methotrexate side effects?
4
Q
Mech: Inhibits thymidylate synthase.
A
5-fluorouracil mechanism of action?
5
Q
Used for: Colon cancer and other solid tumors, basal cell carcinoma.
A
5-fluorouracil uses?
6
Q
Side Effects: Myelosuppresion. Treat overdose with thymidine. Photosensitivity.
A
5-fluorouracil side effects?
7
Q
Mech: Activated by HGPRTase, decreases de novo purine synthesis.
A
6-mercaptopurine (azathioprine), 6-thioguanine mechanism of action?
8
Q
Used for: Leukemia, lymphomas (not CLL or Hodgkin’s.)
A
6-mercaptopurine (azathioprine) uses?
9
Q
SE: Myelosuppression. Decrease dose with allopurinol use (metabolized by xanthine oxidase).
A
6-mercaptopurine (azathioprine) side effects?
10
Q
Used for:Acute lymphoid leukemia.
A
6-thioguanine uses?
11
Q
Myelosuppression. Don’t need to decrease dose with allopurinol use.
A
6-thioguanine side effects?
12
Q
Mech: Pyrimidine antagonist; inhibits DNA polymerase.
A
Cytarabine mechanism of action?
13
Q
Used for: AML, ALL, non-Hodgkin’s lymphoma.
A
Cytarabine uses?
14
Q
SE: Myelosuppression, megaloblastic anemia.
A
Cytarabine side effects?
15
Q
Mech: Intercalates in DNA.
A
Dactinomycin (actinomycin D) mechanism of action?
16
Q
Used for: Wilms’ tumor, Ewing’s sarcoma, rhabdomyosarcoma. Used for childhood tumors.
A
Dactinomycin (actinomycin D) uses?
17
Q
SE: Myelosuppression.
A
Dactinomycin (actinomycin D) side effects?
18
Q
Mech: Generates free radicals; noncovalently intercalases in DNA. Inhibits topoisomerase II.
A
Doxorubicin, daunorubicin (adriamycin) mechanism of action?
19
Q
Used for: Hodgkin’s lymphoma, multiple myeloma, sarcomas, and solid tumors (breast,ovary, lung).
A
Doxorubicin, daunorubicin (adriamycin) uses?
20
Q
SE: Dilated cardiomyopathy, myelosuppression, marked alopecia. Toxic to tissues with extravasation. Prevent cardiotoxicity with dexrazoxane.
A
Doxorubicin, daunorubicin (adriamycin) side effects?
21
Q
Mech: G2 phase specific. Induces formation of free radicals resulting in DNA strand breaks.
A
Bleomycin mechanism of action?
22
Q
Used for: Testicular cancer, Hodgkin’s lymphoma.
A
Bleomycin uses?
23
Q
SE: Pulmonary fibrosis, skin changes, but minimal myelosuppression.
A
Bleomycin side effects?
24
Q
Mech: Late S to G2 phase specific. Inhibits topoisomerase II.
A
Etoposide (VP-16), teniposide mechanism of action?
25
Used for: Small cell carcinoma of the lung and prostate, testicular carcinoma.
Etoposide (VP-16), teniposide uses?
26
SE: Myelosuppression, GI irritation, alopecia.
Etoposide (VP-16), teniposide side effects?
27
Mech: Covalently X-link (interstrand) DNA at guanine N-7. Requires bioactivation by liver.
Cyclophosphamide, ifosfamide mechanism of action?
28
Used for: Non-Hodgkin's lymphoma, neuroblastoma, breast and ovarian carcmomas.
Cyclophosphamide, ifosfamide uses?
29
SE: Myelosuppression, hemorrhagic cystitis, which can be partially prevented with mesna. SIADH.
Cyclophosphamide, ifosfamide side effects?
30
Mech: Prodrug, crosses BBB into CNS.
Nitrosureas (carmustine, lomustine, semustine, streptozocin) mechanism of action?
31
Used for: CNS tumors (including glioblastoma multiforme).
Nitrosureas (carmustine, lomustine, semustine, streptozocin) uses?
32
SE: CNS toxicity (dizziness, ataxia).
Nitrosureas (carmustine, lomustine, semustine, streptozocin) side effects?
33
Mech: Alkylates DNA.
Busulfan mechanism of action?
34
Used for: Chronic myelogenous leukemia, bone marorow ablation prior to bone marrow transplant.
Busulfan uses?
35
SE: Pulmonary fibrosis, hyperpigmentation.
Busulfan side effects?
36
Mech: Destabilize microtubules in M-phase.
Vincristine, vinblastine mechanism of action?
37
Used for: Hodgkin's lymphoma, Wilm's tumor, choriocarcinoma.
Vincristine, vinblastine uses?
38
SE: Peripheral neuropathy (vincristine), myelosuppression (vinblastin.)
Vincristine, vinblastine side effects?
39
Mech: Hyperstabilize microtubules in M-phase.
Paclitaxel mechanism of action?
40
Used for: Ovarian and breast carcinomas.
Paclitaxel uses?
41
SE: Myelosuppression and hypersensitivity.
Paclitaxel side effects?
42
Mech: Alkylating agent; cross-links DNA.
Cisplatin, carboplatin mechanism of action?
43
Used for: Testicular, bladder, ovary, and lung carcinomas.
Cisplatin, carboplatin uses?
44
SE: Severe nephrotoxicity and acoustic nerve damage. Amifostine and chloride diuresis decreases nephrotoxicity. Strong emetic. Ondansetron decreases nausea/vomiting.
Cisplatin, carboplatin side effects?
45
Mech: Inhibits ribonucleotide reductase (decreasing DNA synthesis; S-phase).
Hydroxyurea mechanism of action?
46
Used for: Melanoma, CML/essential thrombocythemia/polycythemia vera (myeloproliferative disorders), sickle cell disease.
Hydroxyurea uses?
47
SE: Myelosuppression.
Hydroxyurea side effects?
48
Mech: Induces apoptosis.
Prednisone mechanism of action?
49
Used for: CLL, Hodgkin's lymphoma, and autoimmune disease.
Prednisone uses?
50
SE: Cushing-like symptoms; immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis.
Prednisone side effects?
51
Mech: SERMs- receptor antagonists in breast, agonists in bone; block the binding of estrogen to estrogen receptor-positive cells.
Tamoxifen, raloxifene mechanism of action?
52
Used for: Treats estrogen receptor positive breast cancer. Can be used to prevent breast cancer and osteoporosis.
Tamoxifen, raloxifene uses?
53
SE: Tamoxifen may increase the risk of endometrial carcinoma via partial agonist effects; "hot flashes." Raloxifene does not cause endometrial carcinoma because it is an endometrial antagonist.
Tamoxifen, raloxifene side effects?
54
Mech: Monoclonal antibody against HER-2 (erb-B2). Helps kill breast cancer cells that overexpress HER-2, possibly through antibody-dependent cytotoxicity.
Trastuzumab (Herceptin) mechanism of action?
55
Used for: Metastatic breast cancer.
Trastuzumab (Herceptin) uses?
56
SE: Cardiotoxicity.
Trastuzumab (Herceptin) side effects?
57
Mech: Philadelphia chromosome bcr-abl tyrosine kinase inhibitor.
Imatinib (Gleevec) mechanism of action?
58
Used for: CML, GI stromal tumors.
Imatinib (Gleevec) uses?
59
SE: Fluid retention.
Imatinib (Gleevec) side effects?
60
Mech: Inhibits topisomerase I.
Topotecan, irinotecan mechanism of action?
61
Used for: Ovarian, small cell lung cancer (topotecan); metastatic colorectal cancer (irinotecan)
Topotecan, irinotecan uses?
62
SE: Myelosuppression.
Topotecan, irinotecan side effects?
63
Mech: Alkylating agent; cross-links DNA. MAOI.
Procarbazine mechanism of action?
64
Used for: Hodgkin's lymphoma.
Procarbazine uses?
65
SE: Can cause secondary leukemias. Myelosupression. Avoid tyramine rich foods.
Procarbazine side effects?
66
Mech: Anti-CD20 monoclonal antibody.
Rituximab mechanism of action?
67
Used for: B-cell non-Hodgkin's lymphoma, rheumatoid arthritis (with methrotrexate).
Rituximab uses?
68
Small molecule inhibitor of forms of the BRAF kinase with the V600E mutation used for Metastatic Melanoma.
Vemurafenib
69
Monoclonal antibody against VEGF that inhibits angiogenesis and is used for Solid Tumors.
Bevacizumab
70
Chemotoxicity of Cisplatin/Carboplatin
Acoustic Nerve Damage and Nephrotoxicity
71
Chemotoxicity of Vincristine
Peripheral Neuropathy
72
Chemotoxicity of Bleomycin, Busulfan
Pulmonary Fibrosis
73
Chemotoxicity of Doxorubicin, Trastuzumab
Cardiotoxicity
74
Chemotoxicity of Cyclophosphamide
Hemorrhagic Cystitis
75
Chemotoxicity of 5-FU, 6-MP, and Methotrexate
Myelosuppression
76
Mech: Cofactor for the activation of antithrombin --> decreased thrombin and decreased factor Xa.
- Short Half-life
Heparin
77
Derivatives of hirudin, the anticoagulant used by leeches; inhibit thrombin.
- Alternative to heparin for anticoagulating pts with HIT.
Lepirudin, Bivalirudin
78
Mech: Interferes with normal synthesis and gamma-carboxylation of Vit K-dependent clotting factors II, VII, IX, X, and proteins C and S.
- Metabolized by cytochrome P-450, increases PT (Extrinsic pathway) and has long half-life.
Warfarin (Coumadin)
| The EX-PresidenT went to WAR(farin
79
Used for Immediate anticoagulation for pulmonary embolism, acute coronary syndrome, MI, DVT.
- Used during pregnancy (does NOT cross placenta). Follow PTT
Heparin
80
Used for Chronic anticoagulation (after STEMI, venous thromboembolism prophylaxis, and prevention of stroke in atrial fibrillation).
- Not used in pregnant women (crosses placenta) Follow PT/INR values.
Warfarin
81
SE: Bleeding, teratogenic, skin/tissue necrosis, drug-drug interactions.
- What do you give for overdose?
Warfarin
| - Vitamin K or for rapid reversal give fresh, frozen plasma.
82
Low molecular weight heparins act more on factor Xa, have better bioavailability and 2-4 times longer half-life. Administered subcutaneously and without lab monitoring but not easily reversible.
Enoxaparin, Dateparin
83
SE: Bleeding, thrombocytopenia (HIT), osteoporosis, drug-drug interactions.
- What do you give for overdose?
Heparin
| - Protamine Sulfate (positively charged so it binds the negatively charged heparin)
84
Development of IgG antibodies against heparin bound to platelet factor 4 (PF4). Antibody-heparin-PF4 complex activates platelets --> thrombosis and thrombocytopenia.
Heparin-induced Thrombocytopenia
85
Thombolytics
Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)
86
Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots.
- Increases PT and PTT with no change in platelet count.
Thrombolytics
| - Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)
87
Irreversibly inhibits COX1 and COX2 by covalent acetylation. Platelets cannot synthesize new enzyme, so effect lasts until new platelets are produced which increases bleeding time, decreases TXA2 and prostaglandins with no effect on PT or PTT.
Aspirin
88
Produced by activated platelets and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation. This is achieved by mediating expression of the glycoprotein complex GP IIb/IIIa in the cell membrane of platelets.
Thromboxane A2
89
Inhibit platelet aggregation by irreversibly blocking ADP receptors. Inhibit fibrinogen binding by preventing glycoprotein IIb/IIIa from binding to fibrinogen.
ADP receptor Inhibitors (Clopidogrel, ticlopidine, prasugrel, ticagrelor)
90
Phosphodiesterase III inhibitor; increases cAMP in platelets, thus inhibiting platelet aggregation; vasodilators.
Cilostazol, dipyridamole
91
Bind to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation. One of which is made from monoclonal antibody Fab fragments.
GP IIb/IIIa Inhibitors (Abciximab, eptifibatide, tirofiban)
92
Used for acute coronary syndromes, percutaneous transluminal coronary agioplasty
GP IIb/IIIa Inhibitors (Abciximab, eptifibatide, tirofiban)
93
Used for intermittent claudication, coronary vasodilation, prevention of stroke or TSA (combined with aspirin), angina prophylaxis.
Cilostazol, dipyridamole
94
Used for acute coronary syndrome, coronary stunting. Decrease incidence or recurrence of thrombotic stroke.
ADP receptor Inhibitors (Clopidogrel, ticlopidine, prasugrel, ticagrelor)
95
Used as antipyretic, analgesic, anti-inflammatory, antiplatelet (decreases aggregation)
Aspirin
96
Used for early MI, early ischemic stroke, direct thrombolysis of severe pulmonary embolism
Thrombolytics
| - Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)
97
SE: Bleeding. CI in pts with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diatheses, or severe hypertension.
- Treat toxicity with aminocaproic acid, an inhibitor of fibrinolysis.
Thrombolytics
| - Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)
98
SE: Gastic ulceration, tinnitus (CN VIII). Chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleeding. Reye's syndrome in children with viral infection.
- Overdose can cause resp alkalosis and metabolic acidosis.
Aspirin
99
SE: Neutropenia
Ticlopidine
100
SE: Nausea, headache, facial flushing, hypotension, abdominal pain
Cilostazol, dipyridamole
101
SE: Bleeding, thrombocytopenia
GP IIb/IIIa Inhibitors
