Drugs - Hematology and Oncology Flashcards Preview

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Flashcards in Drugs - Hematology and Oncology Deck (42):
1

Unfractionated heparin

MOA: activates antithrombin, decreasing thrombin and factor Xa; short half life

Use: immediate anticoagulation for PE, MI, DVT; used during pregnancy because does not cross placenta

Adverse effects: bleeding, heparin-induced thrombocytopenia (higher risk that LMWH or fondapurinix), osteoporosis; level increased with simultaneous isoniazid treatment

Antidote: protamine sulfate

2

Protamine sulfate

MOA: positively charged molecule that binds to negatively charged heparin

Use: heparin toxicity

3

Low molecular weight heparin

MOA: activates antithrombin, decreaseing factor Xa; better bioavailability than unfractionated and longer half life; admistered SC and requires less monitoring but not easily reversible

Use: immediate anticoagulation for PE, MI, DVT

Adverse effects: bleeding, heparin-induced thrombocytopenia, osteoporosis; level increased with simultaneous isoniazid treatment

4

Fondaparinux

MOA: synthetic factor that activates antithrombin, decreaseing factor Xa; better bioavailability than unfractionated and longer half life; admistered SC and requires less monitoring but not easily reversible

Use: immediate anticoagulation for PE, MI, DVT

Adverse effects: bleeding, heparin-induced thrombocytopenia, osteoporosis; level increased with simultaneous isoniazid treatment

5

Warfarin

MOA: interferes with gamma carboxylation of vitamin K dependent clotting factors (II, VII, IX, X, C, S) by affecting vitamin K epoxide reductase complex; increases PT through effect on extrinsic pathway; long half life and takes a few days to take effect, a few weeks to find proper therapeutic dose

Use: chronic anticoagulation to prevent thromboembolism; prevent stroke in setting of atrial fibrillation or mechanical valve; avoided in pregnancy; monitored with MT/INR

Adverse effects: bleeding, teratogenic, skin/tissue necrosis, early transient hypercoagulability due to faster effect on proteins C and S (often do heparin bridging to prevent); interactions with certain foods

Antidote: vitamin K

6

Apixaban and rivaroxaban

MOA: direct factor Xa inhibitors

Use: treat and prevent DVT and PE, superior for stroke prophylaxis in atrial fibrillation patients compared with warfarin; does not require coagulation monitoring

Adverse effects: bleeding with no available reversal agent

7

Thrombolytics

Drugs: tPA, rPA, streptokinase

MOA: aid conversion of plasminogen to plasmin, increasing both PT and PTT

Use: used in early MI, early ischemic stroke, and severe PE (within 3 hours)

Toxicity: bleeding

Antidote: toxicity treated with aminocaproic acid which prevents conversion of plasminogen to plasmin; can also use fresh frozen plasma and cryoprecipitate to correct associated factor deficiencies

8

Aspirin

MOA: irreversibly inhibits COX 1 and COX 2 preventing TXA2 formation; platelets can't synthesize a new enzyme; increases bleeding time, decreases TXA2 and prostaglandins

Use: antipyretic, analgesic, anti-inflammatory, decreases platelet aggregation; used post MI and post thrombotic stroke for secondary prevention

Adverse effects: gastric ulceration, tinnitus, acute renal failure, interstitial nephritis, upper GI bleeding, Reye syndrome in kids with viral infection

Overdose: hyperventilation and respiratory alkalosis that transitions to mixed metabolic acidosis-respiratory alkalosis

Antidote: alkalinize urine with sodium bicarbonate to promote renal excretion

9

ADP receptor inhibitors

Drugs: Clopidogrel, prasugrel, ticagrelor, ticlopidine

MOA: inhibit platelet aggregation by blocking ADP receptors; prevents GIIb/IIIa expression and prevents alpha granule secretion

Use: acute coronary syndrome, coronary stenting, decrease thrombotic stroke; used alongside aspirin

Adverse effects: neutropenia, TTP

10

cilostazol and dipyridamole

MOA: phosphodiesterase III inhibitors that inhibit platelet aggregation and vasodilate

Use: intermittent claudication, coronary vasodilation, prevent stroke or TIA when used in combo with aspirin, angina prophylaxis

Adverse effects: headache, facial flushing, hypotension, abdominal pain

11

GP IIb/IIIa inhibitors

Drugs: abciximab, eptifibatide, tirofiban

MOA: bind to GIIb/IIIa on activated platelets and prevent aggregation; prevents fibrin cross linking

Use: unstable angina, percutaneous transluminal coronary angioplasty

Adverse effects: bleeding, thrombocytopenia

12

Azathioprine, 6-mercaptopurine (6-MP), and 6-thioguanine (6-TG)

MOA: antimetabolite that inhibits DNA synthesis; purine analogs that decrease de novo purine synthesis

Use: prevent organ rejection, RA, IBD, SLE, steroid-refractory chronic disease

Adverse effects: myelosuppression, GI, liver; metabolized by xanthine oxidase and so have increased toxicity with allopurinol or febuxostat

13

Cladribine (2-CDA)

MOA: antimetabolite; purine analog

Use: hairy cell leukemia

Adverse effects: myelosuppression, nephrotoxicity, neurotoxicity

14

Cytarabine

MOA: antimetabolite; pyrimiding analog that inhibits DNA polymerase

Use: AML, lymphomas

Adverse effects: leukopenia, thrombocytopenia, megaloblastic anemia

15

5-fluorouracil

MOA: antimetabolite; pyrimidine analog; complexes with folic acid and inhibits thymidylate synthesis

Use: colon cancer, pancreatic cancer, BCC

Adverse effects: myelosuppression

16

Methotrexate

MOA: folic acid analog; inhibits dihydrofolate reductase which is nevessary for making tymadine and thus DNA

Use: ALL, lymphomas, choriocarcinoma, sarcoma, ectopic pregnancy, medical abortion, RA, psoriasis, IBD, vasculitis

Adverse effects: myelosuppression, hepatotoxicity, mucositis, pulmonary fibrosis

Antidote: leucovorin can reverse the myelosuppression

17

Bleomycin

MOA: induces free radical formation resulting in DNA strand breaks

Use; testicular cancer, Hodgkin lymphoma

Adverse effects: pulmonary fibrosis, skin hyperpigmentation, minimal myelosuppression

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Dactinomycin

MOA: intercalates in DNA

Use: childhood tumors: Wilms tumor, Ewing sarcoma, rhabdomyosarcoma

Adverse effects: myelosuppression

19

Doxorubicin and daunorubicin

MOA: generates free radicals and intercalates in DNA

Use: sold tumors, leukemias, and lymphomas

Adverse effects: dilated cardiomyopathy (can prevent to some degree with chelators- dexrazoxane), myelosuppression, alopecia

20

Leucovorin

used to reverse the myelosuppression seen with methotrexate therapy

21

dexrazoxane

chelator used to prevent the cardiotoxicity seen with doxorubicin therapy

22

Busulfan

MOA: alkylating agent- cross links DNA

Use: CML

Adverse effects: severe myelosuppression, pulmonary fibrosis

23

Cyclophosphamide and ifsosfamide

MOA: alkylating agent that cross links DNA; requires activation by liver

Use: solid tumors, leukemia, lymphoma

Adverse effects: myelosuppression, hemorrhagic cystitis, partically prevented with mesna

24

Mesna

used to prevent the myelosuppression and hemorrhagic cystitis of cyclophosphamide therapy by binding to toxic metabolites

25

Nitrosoureas

Drugs: carmustine, lomustine, semustine, streptozocin

MOA: alkylating agent- cross link DNA; cross the BBB

Use: brain tumors

Adverse effects: CNS toxicity

26

G-CSF (filgrastim)

used in conjunction with myelosuppressive chemotherapeutics to stimulate neutrophil production and maturation

27

Allopurinol

MOA: xanthine oxidase inhibitor

Use: used to prevent acute tumor lysis syndrome where a bunch of cells all die at once and release toxic substances

28

Oprelvekin (IL-11)

MOA: thrombopoeitic growth factor

Use: combat thrombocytopenia seen with chemotherapy

29

Paclitaxel

MOA: microtubule inhibitor; stabilizes MTs in M phase so that the mitotic spindle can't break down

Use: ovarian and breast carcinoma

Adverse effects: myelosuppression, alopecia, hypersensitivity

30

Vincristine and vinblastine

MOA: microtubule inhibitors; inhibit beta tubulin polymerization preventing mitotic spindle formation

Use: solid tumors, leukemias, hodgkin and non-hodgkin lymphoma

Adverse effects: neurotoxicity for vincristine, myelosuppression for vinblastine

31

Cisplatin and carboplatin

MOA: cross links DNA

Use: testicular, bladder, ovary, lung carcinomas

Adverse effects: nephrotoxicity, ototoxicity; prevented with amifostine and chloride diuresis

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Etoposide and teniposide

MOA: inhibits topoisomerase II increasing DNA degradation

Use: solid tumors, leukemias, lymphomas

Adverse effects: myelosuppression, GI upset, alopecia

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Irinotecan and topotecan

MOA: inhibits topoisomerase I; prevents DNA unwinding and replication

Use: colon cancer, ovarian and small cell lung cancer

Adverse effects: severe myelosuppression, diarrhea

34

Hydroxyurea

MOA: inhibits ribonucleotide reductase, decreasing DNA synthesis; also increases fetal hemoglobin

Use: melanoma, CML, sickle cell disease

Adverse effects: severe myelosuppression, GI upset

35

Prednisone and prednisolone

MOA: alters gene transcription

Use: in cancer used to treat CLL, non-Hodgkin lymphoma; also used as immunosuppressants for autoimmune disease

Adverse effects: Cushing-like symptoms, weight gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis

36

Bevacizumab

MOA: monoclonal against VEGF; inhibits angiogenesis

Use: colorectal cancer, renal cell carcinoma

Adverse effects: hemorrhage, blood clots, impaired wound healing

37

Erlotinib

MOA: inhibitor of EGFR tyrosine kinase

Use: non-small cell lung cancer

Adverse effects: rash

38

Imatinib

MOA: tyrosine kinase inhibitor of BCR-ABL

Use: CML, GI stromal tumors

Adverse effects: fluid retention

39

Rituximab

MOA: monoclonal antibody against CD20 which is on most B cell neoplasms

Uses: non-hodgkin lymphoma, CLL, IBD, RA

Adverse effects: increased risk of progressive multifocal leukoencephalopathy

40

Tamoxifen and raloxifene

MOA: selective estrogen receptor modulators; block estrogen binding to ER+ cells

Uses: breast cancer treatment and prevention, prevention of osteoporosis

Adverse effects: increased risk of endometrial cancer for tamoxifen only due to partial agonist activity in endometrium

41

Trastuzumab (Herceptin)

MOA: monoclonal against HER-2 tyrosine kinase receptor; kills cancer cells that overexpress HER-2

Uses: HER-2 positive breast cancer and gastric cancer

Adverse effects: cardiotoxicity

42

Vermurafenib

MOA: small molecule inhibitor of BRAF oncogene positive melanoma

Use: metastatic melanoma