Oncology Drugs Flashcards

(83 cards)

1
Q

Name the antimetabolites

A

Azathioprine, 6-mercaptopurine, 6-thioguanine, cladribine, cytarabine, 5-fluorouracil, methotrexate

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2
Q

Mechanism of azathioprine, 6-MP and 6-TG

A

purine (thiol) analogs –> decreased de novo purine synthesis
activated by HGPRT
azathioprine is prodrug to 6-MP

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3
Q

Use of azathioprine, 6-MP and 6-TG

A
preventing organ rejection
RA
IBD
SLE
to wean pts off steroids and to tx steroid-refractory chronic disease
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4
Q

Toxicity of azathioprine, 6-MP and 6-TG

A

MYELOSUPPRESSION

GI, liver

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5
Q

Metabolism of azathioprine and 6-MP

A

metabolized via xanthine oxidase

increased toxicity if used with allopurinol or febuxostat (used to treat gout)

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6
Q

Mechanism of cladribine

A

purine analog –> multiple mechanism (e.g. inhibition of DNA polymerase, DNA strand breaks)

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7
Q

Use of cladribine

A

hairy cell leukemia

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8
Q

Toxicity of cladribine

A

myelosuppression, nephrotoxicity, and neurotoxicity

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9
Q

Mechanism of cytarabine

A

pyrimidine analong –> inhibition of DNA polymerase

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10
Q

Use of cytarabine

A

leukemias (AML), lymphomas

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11
Q

Toxicity of cytarabine

A

leukopenia, thrombocytopenia, megaloblastic anemia

CYTarabine causes panCYTopenia

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12
Q

Mechanism of 5-fluorouracil

A

pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes with folic acid
complex inhibits thymidylate synthase –> decreased dTMP –> decreased DNA synthesis

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13
Q

Use of 5-FU

A

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

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14
Q

Toxicity of 5-FU

A

myelosuppression, which is NOT reversible with leucovorin (folinic acid)

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15
Q

Mechanism of methotrexate

A

folic acid analog that competitively inhibits dihydrofolate reductase –> decreased dTMP –> decreased DNA synthesis

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16
Q

Use of methotrexate

A

cancers: leukemia (ALL), lymphoma, choriocarcinoma, sarcomas

Non-neoplastic: ectopic pregnancy, medical abortion (with misoprostol), RA, psoriasis, IBD, vasculitis

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17
Q

Toxicity of methotrexate

A

myelosuppression (reversible with leucovorin)
hepatotoxicity
mucostitis (e.g. mout ulcers)
pulmonary fibrosis

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18
Q

Name the antitumor antibiotics

A

bleomycin, dactinomycin, doxorubicin, daunorubicin

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19
Q

Mechanism of bleomycin

A

induces free radical formation –> breaks in DNA strands

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20
Q

Use of bleomycin

A

testicular cancer, Hodgkin lymphoma

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21
Q

Toxicity of bleomycin

A

pulmonary fibrosis
skin hyperpigmentation
mucositis

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22
Q

Mechanism of dactinomycin (actinomycin D)

A

intercalates in DNA

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23
Q

Use of dactinomycin

A

Wilms tumor
Ewing sarcoma
Rhabdomyosarcoma

CHILDHOOD TUMORS - Kids ACT out

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24
Q

Toxicity of dactinomycin

A

myelosuppression

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25
Mechanism of doxorubicin/daunorubicin
generate free radicals | intercalate in DNA --> breaks in DNA --> decreased replication
26
Use of doxorubicin/daunorubicin
solid tumors leukemias lymphomas
27
Toxicity of doxorubicin/daunorubicin
CARDIOTOXICITY (dilated cardiomyopathy) myelosuppression alopecia toxic to tissues following extravasation
28
Agent given with doxorubicin/daunorubicin to prevent cardiotoxicity
Dexrazoxane - iron chelating agent
29
Name the alkylating agents
busulfan, cyclophosphamide, ifosfamide, nitrosureas (carmustine, lomustine, semustine, streptozocin)
30
Mechanism of busulfan
cross-links DNA
31
Use of busulfan
CML | used to ablate bone marrow before transplant
32
Toxicity of busulfan
SEVERE MYELOSUPPRESSION pulmonary fibrosis hyperpigmentation
33
Mechanism of cyclophosphamide/ifosfamide
cross-link DNA at guanine N-7 | require bioactivation by liver
34
Use of cyclophosphamide/ifosfamide
solid tumors leukemia lymphoma
35
Toxicity of cyclophosphamide/ifosfamide
``` myelosuppression HEMORRHAGIC CYSTITIS (partially prevented with MESNA and hydration) ```
36
Mechanism of nitrosureas
require bioactivation cross BBB --> CNS cross link DNA
37
Use of nitrosureas
brain tumors (including glioblastoma multiforme)
38
Toxicity of nitrosureas
CNS toxicirty (convulsions, dizziness, ataxia)
39
Name the microtubule inhibitors
paclitaxel (other taxols), vincristine, vinblastine
40
Mechanism of paclitaxel/taxols
hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)
41
Use of paclitaxel/taxol
ovarian and breast carcinomas
42
Toxicity of paclitaxel/taxol
myelosuppression alopecia hypersensitivity
43
Mechanism of vincristine/vinblastine
vinea alkaloids that bind beta-tubulin and inhibit its polymerization into MTs --> prevent mitotic spindle formation (M-phase arrest)
44
Use of vincristine/vinblastine
solid tumors leukemias Hodgkin (vinblastine) lymphoma Non-Hodgkin (vincristine) lymphoma
45
Toxicity of vincristine
neurotoxicity (areflexia, peripheral neuritis) | paralytic ileus
46
Toxicity of vinblastine
bone marrow supression
47
Mechanism of cisplatin/carboplatin
cross-link DNA
48
Use of cisplatin/carboplatin
testicular bladder ovary lung carcinomas
49
Toxicity of cisplatin/carboplatin
nephrotoxicity, ototoxicity
50
How can prevent nephrotoxicity of cisplatin/carboplatin
use with amifostine (free radical scavenger) and chloride (saline) diuresis
51
Mechanism of etoposide/teniposide
etoposide inhibits topoisomerase II --> increased DNA degradation
52
Use of etoposide/teniposide
solid tumors (testicular and small cell lung) leukemia lmyphoma
53
Toxicity of etoposide/teniposide
myelosuppression, GI upset, alopecia
54
Mechanism of irinotecan, topotecan
inhibit topoisomerase I and prevent DNA unwinding and replication
55
Use of irinotecan, topotecan
``` colon cancer (irinotecan) ovarian and small cell lung (topotecan) ```
56
Toxicity of irinotecan, topotecan
severe myelosuppression | diarrhea
57
Mechanism of hydroxyurea
inhibits ribonucleotide reductase --> decreased DNA synthesis (S-phase specific)
58
Use of hydroxyurea
melanoma, CML, sickle cell disease (increase HbF)
59
Toxicity of hydroxyurea
severe myelosupression | GI upset
60
Mechanism of prednisone/prednisolone
various; bind intracytoplasmic receptor; alter gene transcription
61
Use of prednisone/prednisolone
CLL non-Hodgkin lymphoma (part of combo) immunosuppressants (autoimmune diseases)
62
Toxicity of prednisone/prednisolone
Cushing like symptoms
63
Mechanism of bevacizumab
monoclonal antibody against VEGF inhibiting angiogenesis
64
Use of bevacizumab
colon cancer and renal cell carcinoma | age related macular degeneration
65
Toxicity of bevacizumab
hemorrhage blood clots impaired wound healing
66
Mechanism of erlotinib
EGFR tyrosine kinase inhibitor
67
Use of erlotinib
non small cell lung carcinoma (adenocarcinoma if EGF positive)
68
Toxicity of erlotinib
rash
69
Mechanism of imatinib
tyrosine kinase inhibitor of BCR-ABL (philadelphia chromosome fusion gene) and c-kit (GI stromal tumors)
70
Use of imatinib
CML, GI stromal tumors
71
Toxicity of imatinib
fluid retention
72
Mechanism of rituximab
Ab against CD20 on B cells
73
Use of rituximab
Non-Hodgkin lymphoma CLL IBD RA
74
Toxicity of rituximab
increased risk of progressive multifocal leukoencephalopathy (PML) from JC virus
75
Mechanism of tamoxifen/raloxifene
selective estrogen receptor modulators - antagonists in breast and agonists in bone - block binding of estrogen to ER + cells in breast
76
Use of tamoxifen/raloxifene
breast cancer treatment (tamoxifen only) and prevention | osteoporosis for raloxifene
77
Toxicity of tamoxifen
partial agonist in endometrium --> increased risk of endometrial hyperplasia and cancer increased risk for hot flashes
78
Toxicity of raloxifene
no increase in endometrial cancer because antagonist in endometrial tissue
79
Mechanism of trastuzumab
Ab against Her-2, a tyrosine kinase receptor (through interrupted cellular signaling and antibody-dependent cytotoxicity)
80
Use of trastuzumab
HER2 + breast cancer and gastric cancer
81
Toxicity of trastuzumab
cardiotoxicity
82
Mechanism of vemurafenib
small molecule inhibitor of BRAF oncogene + melanoma
83
Use of vemurafenib
metastatic melanoma