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Cancer Drugs Flashcards

1
Q

8 antimetabolites drugs

A
  1. Azathioprine 2. Cladribine 3. Cytarabine 4. 5-fluorouracil 5. Hydroxyurea 6. Methotrexate 7. 6-mercaptopurine 8. 6-thioguanine
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2
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine mechanism of action

A

Purine (thiol) analogs–> decrease de novo purine synthesis

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3
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine are activated by

A

HGPRT

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4
Q

Azathioprine is metabolized into

A

6-MP

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5
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine clinical use

A
  1. Prevent organ rejection
  2. RA. 3. SLE. 4. IBD. 5 wean patients off steroids in chronic disease
  3. Treat steroid-refractory chronic disease
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6
Q

Azathioprine, 6-mercaptopurine, 6-thioguanine side effects

A
  1. Myelosuppresion 2. GI. 3. Liver
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7
Q

Azathioprine and MP-6 are metabolized by

A

Xantine oxidase

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8
Q

Azathioprine and MP-6 has increased toxicity if administrated with

A
  1. Allopurinol
  2. Febuxostat
    (Both xanthine oxidase inhibitors,for lynch nyhan syndrome
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9
Q

Cladribine (2-CDA) mechanism of action

A

Purine analog –> inhibition of dna polymerase, dna strand breaks)

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10
Q

Cladribine (2-CDA) clinical use

A

Hairy cell leukemia

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11
Q

Cladribine (2-CDA) toxicity

A
  1. Myelosupression
  2. Nephrotoxicity
  3. Neurotoxicity
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12
Q

Cytarabine (arabinofuranosyl cytidine) mechanism of action

A

Pyrimidine analog –> Dna polymerase inhibitor

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13
Q

Cytarabine (arabinofuranosyl cytidine) clinical use

A

AML

LYMPHOMAS

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14
Q

Cytarabine (arabinofuranosyl cytidine) toxicity

A
  1. Leukopenia
  2. Thrombocytopenia
  3. Megaloblastic anemia
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15
Q

Methotrexate (MTX) mechanism of action

A

Folic acid analog that inhibits dihydropholate reductase–> decreases dTMP–>decreases DNA synthesis

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16
Q

Methotrexate (MTX) clinical use

A
  1. Cancers (ALL, lymphomas, choriocarcinoma, sarcomas)

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

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17
Q

Methotrexate (MTX) toxicity

A
  1. Myelosupression (REVERSIBLE WITH LEUCOVORIN)
  2. Hepatotoxicity
  3. Mucositis (mount ulcers)
  4. Pulmonary fibrosis
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18
Q

Antimetabolites drugs action

A

Inhibit DNA synthesis (S phase)

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19
Q

5-fluorouracil toxicity

A

Myelosupression (NOT REVERSIBLE WITH LEUCOVORIN)

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20
Q

5-fluorouracil clinical use

A
  1. Colon cancer
  2. Pancreatic cancer
  3. Basal cell carcinoma (topical)
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21
Q

5-fluorouracil mechanism of action

A

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

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22
Q

Hydroxyurea mechanism of action

A

Inhibits ribonucleatide reductase

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23
Q

Antitumor antibiotics

A
  1. Bleomycin
  2. Dactinomycin (actinomycin D)
  3. Doxorubicin, daunorubicin
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24
Q

Bleomycin mechanism of action

A

Induce free radicals –> breaks in DNA strands

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25
Bleomycin clinical use
Testicular cancer | Hodgkin lymphoma
26
Bleomycin side effects
1. Pulmonary fibrosis 2. MINIMAL myelosupression 3. Skin hyperpigmentation
27
What part of cycle does bleomycin inhibit
G2 (double check repair)
28
Dactinomycin (actinomycin D) side effects
Myelosuppression
29
Dactinomycin (actinomycin D) mechanism of action
Intercalates in DNA
30
Dactinomycin (actinomycin D) clinical use
Used for childhood tumors 1. Wilms 2. Ewing sarcoma 3. Rhabdomyosacroma
31
Doxorubicin, | Daunorubicin mechanism of action
1. Generates free radicals | 2. Intercalate in DNA--> breaks in DNA--> decreased replication
32
Doxorubicin, | Daunorubicin clinical uses
1. Solid tumors 2. Leukemias 3. Lymphomas
33
Doxorubicin, | Daunorubicin side effects
Toxic to tissues following extravasation 1. Dilated cardiomyopathy 2. Alopecia 3. Myelosuppression
34
How to prevent dilated cardiomyopathy with doxorubicin or daunorubicin administration
Dexrazoxane, an iron chelatin agent
35
Alkylating agents
Busulfan Cyclophosphamide, isosfamide Nitrosoureas (carmustine, iomustine, semustine, streptozocin)
36
Busulfan mechanism of action
Cross-links DNA
37
Busulfan clinical use
1. CML | 2. To ablate patient's bonipe marrow before bone marrow transplantation
38
Busulfan side effects
1. Severe myelosuppression (almost always) 2. Pulmonary fibrosis 3. Hyperpigmentation
39
Nitrosoureas toxicity
Cns: 1. Dizziness 2. Ataxia 3. Convulsion
40
Nitrosoureas clinical use
Brain tumors (including glioblastoma multiforme)
41
Nitrosoureas mechanism of action
Require bioactivation Cross BBB cross link DNA
42
Cyclophosphamide, ifosfamide mechanism of action
Cross link DNA at guanine N-7 | Require bioactivation by liver
43
Cyclophosphamide, ifosfamide clinical use
1. Solid tumors 2. Leukemia 3. Lymphomas
44
Cyclophosphamide, ifosfamide toxicity
1. Myelosuppresion | 2. Hemorrhagic cystitis
45
Partially Prevent hemorrhagic cystitis in Cyclophosphamide, ifosfamide by:
Mesna (thiol group of mesna binds toxic metabolitis)
46
Microtubule inhibitors
1. Paclitaxel, and others taxols 2. Vincristine 3. Vinblastine
47
Paclitaxel toxicity
1. Myelosuppression 2. Alopecia 3. Hypersensitivity 4. Neuropathy
48
Paclitaxel clinical use
1. Ovarian ca | 2. Breast ca
49
Paclitaxel mechanism of action
Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)
50
Vinblastine clinical use
1. Solid tumor 2. Leukemia 3. Hodgkin
51
Vincristine clinical use
1. Solid tumor 2. Leukemias 3. Non-hodgkin
52
Vincristine vs. vinblastine clinical uses
Both: solid tumor, leukemia Vinblastine: Hodgkin Vincristine: non-Hodgkin
53
Vinblastin toxicity
Myelossupression
54
Vincristine toxicity
1. Neurotoxicity: (areflexia, peripheral neuritis) | 2. Paralytic ileus
55
Vincristine, vinblastine mechanism of action
Vinca alkaloids that bind β-tubulin and inhibit its polymerization into microtubules (prevent mitotic spindle formation (M-phase arrest)
56
Hydroxyurea mechanism of action
Inhibits ribonucleotide reductase (inhibits dna synthesis-S phase)
57
Vinca alkaloids
Vincristine | Vinblastine
58
Hydroxyurea clinical use
1. Melanoma 2. CML 3. Sickle cell anemia (increases HbF)
59
Hydroxyurea toxicity
1. SEVERE myelosuppression | 2. GI upset
60
Vemurafenib clinical use
Metastatic melanoma
61
Vemurafenib mechanism of action
Small molecule inhibitor of BRAF oncogene (melanoma)
62
BRAF oncogene is (+) in
MELANOMA
63
Erlotinib toxicity
Rash
64
Erlotinib clinical use
Non small cell lung carcinoma
65
Erletonib mechanism of action
EGFR tyrosine kinase inhibitor
66
Cetuximab - mechanism of action
Monoclonal antibody against EGFR
67
Cetuximab - clinical use
1. stage IV CRC (wild-typeKRAS) | 2. head and neck cancer
68
Cetuximab - adverse effects
1. rash 2. elevated LFTs 3. Diarrhea
69
Etoposide tenoposide toxicity
1. Myelosuppression 2. Gi upset 3. Alopecia
70
Irinotecan, topotecan toxicity
1. Severe myelosuppression | 2. Diarrhea

Hematology And Oncology (21 decks)

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