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Flashcards in Cancer Drugs Deck (70):
1

8 antimetabolites drugs

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

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

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

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

HGPRT

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Azathioprine is metabolized into

6-MP

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Azathioprine, 6-mercaptopurine, 6-thioguanine clinical use

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

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Azathioprine, 6-mercaptopurine, 6-thioguanine side effects

1. Myelosuppresion 2. GI. 3. Liver

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Azathioprine and MP-6 are metabolized by

Xantine oxidase

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Azathioprine and MP-6 has increased toxicity if administrated with

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

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Cladribine (2-CDA) mechanism of action

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

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Cladribine (2-CDA) clinical use

Hairy cell leukemia

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Cladribine (2-CDA) toxicity

1. Myelosupression
2. Nephrotoxicity
3. Neurotoxicity

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Cytarabine (arabinofuranosyl cytidine) mechanism of action

Pyrimidine analog --> Dna polymerase inhibitor

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Cytarabine (arabinofuranosyl cytidine) clinical use

AML
LYMPHOMAS

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Cytarabine (arabinofuranosyl cytidine) toxicity

1. Leukopenia
2. Thrombocytopenia
3. Megaloblastic anemia

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Methotrexate (MTX) mechanism of action

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

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Methotrexate (MTX) clinical use

1. Cancers (ALL, lymphomas, choriocarcinoma, sarcomas)
2. Non-neoplastic: ectopic pregnant, medical abortion (with misoprostol), RA, psoriasis, IBD, vasculitis

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Methotrexate (MTX) toxicity

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

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Antimetabolites drugs action

Inhibit DNA synthesis (S phase)

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5-fluorouracil toxicity

Myelosupression (NOT REVERSIBLE WITH LEUCOVORIN)

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5-fluorouracil clinical use

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

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5-fluorouracil mechanism of action

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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Hydroxyurea mechanism of action

Inhibits ribonucleatide reductase

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Antitumor antibiotics

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

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Bleomycin mechanism of action

Induce free radicals --> breaks in DNA strands

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Bleomycin clinical use

Testicular cancer
Hodgkin lymphoma

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Bleomycin side effects

1. Pulmonary fibrosis
2. MINIMAL myelosupression
3. Skin hyperpigmentation

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What part of cycle does bleomycin inhibit

G2 (double check repair)

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Dactinomycin (actinomycin D) side effects

Myelosuppression

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Dactinomycin (actinomycin D) mechanism of action

Intercalates in DNA

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Dactinomycin (actinomycin D) clinical use

Used for childhood tumors
1. Wilms
2. Ewing sarcoma
3. Rhabdomyosacroma

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Doxorubicin,
Daunorubicin mechanism of action

1. Generates free radicals
2. Intercalate in DNA--> breaks in DNA--> decreased replication

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Doxorubicin,
Daunorubicin clinical uses

1. Solid tumors
2. Leukemias
3. Lymphomas

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Doxorubicin,
Daunorubicin side effects

Toxic to tissues following extravasation
1. Dilated cardiomyopathy
2. Alopecia
3. Myelosuppression

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How to prevent dilated cardiomyopathy with doxorubicin or daunorubicin administration

Dexrazoxane, an iron chelatin agent

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Alkylating agents

Busulfan
Cyclophosphamide, isosfamide
Nitrosoureas (carmustine, iomustine, semustine, streptozocin)

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Busulfan mechanism of action

Cross-links DNA

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Busulfan clinical use

1. CML
2. To ablate patient's bonipe marrow before bone marrow transplantation

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Busulfan side effects

1. Severe myelosuppression (almost always)
2. Pulmonary fibrosis
3. Hyperpigmentation

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Nitrosoureas toxicity

Cns: 1. Dizziness 2. Ataxia 3. Convulsion

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Nitrosoureas clinical use

Brain tumors (including glioblastoma multiforme)

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Nitrosoureas mechanism of action

Require bioactivation
Cross BBB
cross link DNA

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Cyclophosphamide, ifosfamide mechanism of action

Cross link DNA at guanine N-7
Require bioactivation by liver

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Cyclophosphamide, ifosfamide clinical use

1. Solid tumors
2. Leukemia
3. Lymphomas

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Cyclophosphamide, ifosfamide toxicity

1. Myelosuppresion
2. Hemorrhagic cystitis

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Partially Prevent hemorrhagic cystitis in Cyclophosphamide, ifosfamide by:

Mesna (thiol group of mesna binds toxic metabolitis)

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Microtubule inhibitors

1. Paclitaxel, and others taxols
2. Vincristine
3. Vinblastine

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Paclitaxel toxicity

1. Myelosuppression
2. Alopecia
3. Hypersensitivity
4. Neuropathy

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Paclitaxel clinical use

1. Ovarian ca
2. Breast ca

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Paclitaxel mechanism of action

Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)

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Vinblastine clinical use

1. Solid tumor
2. Leukemia
3. Hodgkin

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Vincristine clinical use

1. Solid tumor
2. Leukemias
3. Non-hodgkin

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Vincristine vs. vinblastine clinical uses

Both: solid tumor, leukemia
Vinblastine: Hodgkin
Vincristine: non-Hodgkin

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Vinblastin toxicity

Myelossupression

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Vincristine toxicity

1.Neurotoxicity: (areflexia, peripheral neuritis)
2. Paralytic ileus

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Vincristine, vinblastine mechanism of action

Vinca alkaloids that bind β-tubulin and inhibit its polymerization into microtubules (prevent mitotic spindle formation (M-phase arrest)

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Hydroxyurea mechanism of action

Inhibits ribonucleotide reductase (inhibits dna synthesis-S phase)

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Vinca alkaloids

Vincristine
Vinblastine

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Hydroxyurea clinical use

1. Melanoma
2. CML
3. Sickle cell anemia (increases HbF)

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Hydroxyurea toxicity

1. SEVERE myelosuppression
2. GI upset

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Vemurafenib clinical use

Metastatic melanoma

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Vemurafenib mechanism of action

Small molecule inhibitor of BRAF oncogene (melanoma)

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BRAF oncogene is (+) in

MELANOMA

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Erlotinib toxicity

Rash

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Erlotinib clinical use

Non small cell lung carcinoma

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Erletonib mechanism of action

EGFR tyrosine kinase inhibitor

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Cetuximab - mechanism of action

Monoclonal antibody against EGFR

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Cetuximab - clinical use

1. stage IV CRC (wild-typeKRAS)
2. head and neck cancer

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Cetuximab - adverse effects

1. rash
2. elevated LFTs
3. Diarrhea

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Etoposide tenoposide toxicity

1. Myelosuppression
2. Gi upset
3. Alopecia

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Irinotecan, topotecan toxicity

1. Severe myelosuppression
2. Diarrhea