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First Aid > Hem Onc Drugs > Flashcards

Hem Onc Drugs Flashcards

1
Q

Methotrexate (MTX) mech:

A

Folic acid analog that inhibits dihydrofolate reductase, which leads to dTMP -> decreased DNA and decreased protein synthesis

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2
Q

Methotrexate Clinical use:

A

Cancers: Leukemias, Lymphomas, Choriocarcinoma, Sarcomas. Non-neoplastic: abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis, IBD

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3
Q

Methotrexate Toxicity:

A

Myelosuppression, which is reverible with leucovorin (folinic acid) ‘rescue’. Macrovesicular fatty change in liver. Mucositis. Teratogen

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4
Q

5-FU Mech:

A

Pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase which leads to a decrease in dTMP,, leading to decrease DNA and protein synthesis

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5
Q

5-FU Clinical Use:

A

Colon cancer, pancreatic cancer, basal cell carcinoma (topical)

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6
Q

5-FU Toxicity:

A

Myelosuppression, which is not reversible with leucovorin. OD: rescue with uridine. Photosensitivity.

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7
Q

Cytarabine mech:

A

pyrimidine analog that inhibits DNA polymerase

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8
Q

Cytarabine Clinical Use:

A

Leukemias, Lymphomas

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9
Q

Cytarabine Toxicity:

A

Leukopenia, thrombocytopenia, megaloblastic anemia, CYTarabine causes panCYTopenia

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10
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine (6-TG) mech:

A

purine (thiol) analogs lead to decreased de novo purine synthesis. Activated by HGPRT

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11
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine (6-TG) Clinical Use:

A

Preventing organ rejection, RA, SLE (azathioprine). Leukemia, IBD (6-MP, 6TG).

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12
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine (6-TG) Toxocity:

A

Bone marrow, GI, liver. Azathioprine and 6-MP are metabolized by xanthine oxidase; thus both have increased toxicity with allopurinol, which inhibits their metabolism.

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13
Q

The antimetabolites inlcude

A

MTX, 5-FU, Cytarabine, Azathioprine/6-MP

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14
Q

What are the antitumor antibiotics?

A

Dactinomycin, Doxorubicin (Adriamycin), Daunorubicin, Bleomycin

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15
Q

Dactinomycin (Actinomycin D) mech:

A

intercalates in DNA

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16
Q

Dactiomycin (Actinomycin D) use:

A

Wilms tumor, Ewing sarcoma, rhabdomyosarcoma. Used for childhood rumors (children act out)

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17
Q

Dactinomycin (Actinomycin D) Toxicity:

A

Myelosuppression

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18
Q

Doxorubicin (Adriamycin), Daunorubicin mech:

A

Generate free radicals. Intercalate in DNA which leads to breaks in DNA and decrease in replication.

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19
Q

Doxorubicin (Adriamycin), Daunorubicin use:

A

Solid tumors, Leukemias, Lymphomas

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20
Q

Doxorubicin (Adriamycin), Daunorubicin Toxicity:

A

Cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia. Toxic to tissues following extravasation. Dexrazoxane (iron chelating agent), used to prevent cardiotoxicity

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21
Q

Bleomycin mech:

A

Induces free radical formation, which causes breaks in DNA strands.

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22
Q

Bleomycin use:

A

Testicular cancer, Hodgkin lymphoma

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23
Q

Bleomycin Toxicity:

A

Pulmonary fibrosis, skin changes, mucositis. Minimal myelosuppression.

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24
Q

What are the alkylating agents?

A

1) Cyclophosphamide/ifosfamide 2) Nitrosoureas: (carmustine, lomustine, semustine, streptozocin) 3) Busulfan

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25
Q

Cyclophosphamide, ifosfamide mech:

A

Covalently X-linked (interstrand) DNA at guanine N-7. Require bioactivation by liver.

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26
Q

Cyclophosphamide, ifosfamide use:

A

Solid tumors, leukemia, lymphomas, and some brain cancers

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27
Q

Cyclophosphamide, ifosfamide toxicity:

A

Myelosuppression; hemorrhagic cystitis, partially prevented with mesna (thio group of mesna binds toxic metabolites)

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28
Q

Nitrosoureas (carmustine, lomustine, semustine, streptozocin) mech:

A

Require bioactivation. Cross blood-brain barrier to CNS. Cross-Links DNA

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29
Q

Nitrosoureas (carmustine, lomustine, semustine, streptozocin) clinical use:

A

brain tumors (including glioblastoma multiforme)

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30
Q

Nitrosoureas (carmustine, lomustine, semustine, streptozocin) toxicity:

A

CNS toxicity (convulsions, dizziness, ataxia)

31
Q

Busulfan mech:

A

Cross-links DNA

32
Q

Busulfan clinical use:

A

CML. Also used to ablate patient’s bone marrow before bone marrow transplantation

33
Q

Bustulfan toxicity:

A

Severe myelosuppression (in almost all cases), pulmonary fibrosis, hyperpigmentation.

34
Q

What are the microtubule inhibitors?

A

Vincristine/Vinblastine & paclitaxel and other taxols.

35
Q

Vincristine/Vinblastine mech:

A

Vinca alkaloid that bind beta tubulin, inhibit its polymerization into microtubules, thereby preventing mitotic spindle formation (M-phase arrest)

36
Q

Vincristine/Vinblastine use:

A

Solid tumors, leukemias, and lymphomas

37
Q

Vincristine/Vinblastine toxicity:

A

1) Vincristine - neurotoxicity (areflexia, peripheral neuritis), paralytic ileus. 2) Vinblastine blasts bone marrow (suppression)

38
Q

Paclitaxel, other taxols mech

A

Hyperstabalize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur). ‘It is taxing to stay polymerized’

39
Q

Paclitaxel clinical use

A

Ovarian and breast carcinomas

40
Q

Paclitaxel toxicity:

A

Myelosupression, alopecia, hypersensitivity

41
Q

Cisplatin, carboplatin mech:

A

cross-link DNA

42
Q

Cisplatin, carboplatin use:

A

Testicular, bladder, ovary, lung carcinoma

43
Q

Cisplatin, carboplatin toxicity:

A

Nephrotoxicity and acoustic nerve damage. Prevent nephrotoxicity with amifostine (free radial scavenger) and chloride diuresis.

44
Q

Etoposide, teniposide mech:

A

eTOPOside inhibits TOPOisomerase II which increases DNA degradation.

45
Q

Clinical use of etoposide, teniposide:

A

Solid tumors (particularily testicular and small cell lung cancer), leukemias, lumphomas.

46
Q

Etopoise, teniposide toxicity:

A

myelosuppression, GI irritation, alopecia

47
Q

Irinotecan, topotecan mech:

A

Inhibit topoisomerase I and prevent DNA unwinding and replication

48
Q

Irinotecan, topotecan clinical use:

A

Colon cancer (irinotecan); ovarian and small cell lug cancers (topotecan)

49
Q

Irinotecan topotecan toxicity:

A

Severe myelosuppression, diarrhea

50
Q

Hydroxyurea mech:

A

Inhibits ribonucleotide reductase which leads to decreased DNA Synthesis (S-phase specific)

51
Q

Hydroxyurea use:

A

Melanoma, CML, sickle cell disease (increased HbF)

52
Q

Hodoxyurea toxicity:

A

Bone marrow suppression, GI upset

53
Q

Prednisone, prednisolone mech:

A

may trigger apoptosis. may even work on nondividing cells.

54
Q

prednisone, prednisolone use:

A

most commonly used glucocorticoid in cancer chemo. used in CLL, non-hodgkin lymphomas (part of combination chemo regimen). Also used as imunosuppressants (i.e autoimmune diseases).

55
Q

Prednisone, prednisolone toxicity:

A

Cushing-like symptoms; weight gain, central obesity, muscle breakdown ,cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycmia, psychosis

56
Q

Tamoxifen, raloxifene mech

A

SERMS - receptor antagonists in breast and agonists in bone. Block the binding of estrogen to ER + cells

57
Q

Tamoxifen, raloxifene clinical use

A

breast cancer treatment (tamoxifen only) and prevention. Raloxifene for osteoporosis.

58
Q

Tamoxifen toxicity

A

partial agonist in endometrium, which increases the risk of endometrial cancer; ‘hot flashes’

59
Q

Raloxifene toxicity

A

no increase in endometrial carcinoma because it is an endometrial antagonist

60
Q

Trastuzumab (herceptin) mech

A

monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase receptor. Helps kill breast cancer cells that overexpress HER-2, through inhibition of HER2 initiated cellular signaling and antibody dependent cytotoxicity

61
Q

Trastuzumab (herceptin) clinical use:

A

HER-2 + breast cancer and gastric cancer (tras2zumab)

62
Q

Trastuzumab toxicity:

A

Cardiotoxicity. “HEARTceptin’ damages the heart

63
Q

Imatinib (Gleevac) mech:

A

Tyrosine Kinase inhibitor of bcr-abl (Philadelphia chromosome fusion gene in CML) and c-Kit (common in GI stromal tumors)

64
Q

Imatinib use:

A

CML, GI stromal tumors

65
Q

Imatinib toxicity:

A

fluid retention

66
Q

Rituximab mech:

A

monoclonal antibody against CD20, which is found on most B-cell neoplasms

67
Q

Rituximab use:

A

non-hodgkin lymphoma, rheumatoid arthritis (with MTX); ITP

68
Q

Rituximab toxicity:

A

increased risk of progressive multifocal leukoencephalopathy

69
Q

Vemurafenib mech:

A

Small molecule inhibitor to forms of the B-Raf kinase with the V600E mutation

70
Q

Vemurafenib use:

A

Metastatic melanoma

71
Q

Bevacizumab mech:

A

monoclonal antibody against VEGF, inhibits angiogenesis

72
Q

Bevacizumab clinical use:

A

Solid tumors (colorectal cancer, renal cell carcinoma)

73
Q

Bevacizumab toxicity:

A

Hemorrhage and impaired wound healing

First Aid (33 decks)

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