13 - Cancer Chemotherapy Flashcards

1
Q

Drugs acting on S phase

A

CHEM 665

  • cytarabine
  • hydroxyurea
  • etoposide
  • methotrexate
  • 6 - thioguanine
  • 6 - mercaptopurine
  • 5-FU
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2
Q

Drug acting on G2 phase

A

Bleomycin

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3
Q

Drugs acting on M phase

A
  • Vincristine
  • Vinblastine
  • Paclitaxel (Taxane)
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4
Q

Drugs that for DNA cross-links

A

CCCB

  • Cyclophosphamide
  • Cisplatin
  • Carmustin
  • Busulfan
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5
Q

Drugs that form hydrogen peroxide which generate free radicals

A
  • Procarbazine

- Dacarbazine

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6
Q

Rescue agent for Cyclophosphamide

A

MESNA

Cystitis can be prevented by adequate hydration

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7
Q

Rescue agent for Cisplatin

A

Amifostine

Decrease nephrotoxicity by administering mannitol with forced hydration

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8
Q

Has a wider spectrum of coverage in solid tumors and has less renal and GI side effects

A

Carboplatin

- widely used in transplant regimen

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9
Q

Part of FOLFOX and FOLFIRI regimen (solid tumors) that are resistant to Cisplatin and Carboplatin

A

Oxaliplatin

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10
Q

Ototoxic medications

A
  • aspirin
  • ibuprofen
  • cisplatin
  • kanamycin (most ototoxic aminoglycoside)
  • Gentamycin
  • Lasix
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11
Q

Highest carcinogenic potential among alkylating agents

A

Procarbazine

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12
Q

Alkylating agent used for CML

A

Busulfan

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13
Q

Drugs causing pulmonary fibrosis

A

BBBAN Me

  • Busulfan
  • Bleomycin
  • Bromocriptine
  • Amiodarone
  • Nitrofurantoin
  • Methotrexate
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14
Q

Special alkylating agent that is for brain tumors

A

Carmustine
- highly lipophilic

SE: CNS toxicity

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15
Q

Alkylating agents

A
  • cyclophosphamide
  • cisplatin
  • procarbazine
  • dacarbazine
  • carmustine
  • busulfan
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16
Q

Antimetabolites

A
  • methotrexate
  • 6 - mercaptopurine
  • 5 - fluorouracil
  • cytarabine
  • gemcitabine
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17
Q

inhibits dihydrofolate reductase

A

Methotrexate

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18
Q

rescue therapy for Methotrexate

A

Leucovorin (Folinic acid)

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19
Q

Inhibits de novo purine nucleotide synthesis

A

6 - mercaptopurine

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20
Q

6-MP metabolism is inhibited by

A
  • Allopurinol

- Febuxostat

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21
Q

MOA of Pemetrexed

A

inhibits:

  • thymidylate synthase
  • dihydrofolate reductase
  • purine nucleotide synthesis
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22
Q

Inhibits thymidylate synthase causing thymineless death of cells

A

5-Fluorouracil

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23
Q

Prodrug of 5-FU

A

Tegafur

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24
Q

Inhibits:

  • DNA repair and synthesis
  • ribonucleotide reductase with reduced formation of dNTPs
A

Cytarabine
- most specific for the S phase in cell cycle

Gemcitabine

  • used for pancreatic CA
  • can be used for solid tumors

*-BINE - inhibits ribonucleotide reductase

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25
Drugs that inhibit ribonucleotide reductase
- Fludarabine - Cladribine - Cytarabine - Gemcitabine
26
Drugs that have SE of hand-foot syndrome - "Palmar-plantar erythrodysesthesia" - redness, swelling and pain sometimes with blistering
- Capecitabine | - Pemetrexed
27
Natural Product Anti-cancer drugs
- Vincristine - Vinblastine - Etoposide - Topotecan - Paclitaxel
28
Prevents microtubule assembly
- Vincristine (crispy nerves: peripheral neuropathy) | - Vinblastine (BM suppression)
29
Prevents microtubule disassembly
Taxane - Paclitaxel - Docetaxel - Cabazitaxel
30
- Inhibits Topoisomerase II (DNA Gyrase) | - inhibits mitochondrial electron transport
Etoposide E2poside
31
Inhibits Topoisomerase I
Topotecan
32
Camptothecin that is used for advanced ovarian CA (2nd line) and small cell lung CA
Topotecan
33
Camptothecin that is used for metastatic colon CA
Irinotecan
34
- Intercalates between base pairs - inhibits topoisomerase II - generates free radicals
Doxorubicin SE: - ruby red: red urine - Cardiomyopathy
35
Rescue therapy for Doxorubicin
Dexrazoxane
36
Anthracycline
- Doxorubicin - Daunorubicin - Idarubicin - Epirubicine - Mitoxantrone
37
Anthracycline used for ALL
Daunorubicin
38
Anthracycline used for AML
Idarubicine
39
Antitumor drug that generates free radicals causing DNA strand breaks - also intercalates with DNA
Bleomycin
40
- Binds to double-stranded DNA | - inhibits DNA-dependent RNA synthesis
Actinomycin other name: dactinomycin - oldest antitumor antibiotic
41
Inhibits tyrosine kinase activity of: - BCR-ABL oncogene in CML - cKit tyrosine kinase in GIST
Imatinib Gleevec - imatinib mesylate - GIST
42
Tyrosine kinase inhibitor that is also used for idiopathic pulmonary fibrosis
Nintedanib
43
Acts on breast CA cells that overexpress Her-2/neu
Trastuzumab / Pertuzumab / Lapatinib - monoclonal antibody Use: metastatic breast CA
44
SE of Trastuzumab
Cardiomyopathy like doxorubicin
45
Monoclonal antibody that inhibits binding of VEGF to VEGFR. - inhibits tumor vascular permeability - enhances tumor blood flow and drug delivery
Bevacizumab - inhibits angiogenesis
46
Drug that acts a multiple kinase inhibitor against VEGFR1 to 3 kinases and is used for thyroid cancer
Levatinib
47
Binds to surface protein in NHL cells inducing complement-mediated lysis, direct toxicity and induction of apoptosis
Rituximab
48
Binds to EGFR inhibiting downstream EGFR signaling, enhances response to chemo and radiotherapy
Cetuximab Bevacizumab - inhibits binding of VEGF
49
Inhibits EGFR tyrosine kinase
Erlotinib Cetuximab - binds to EGFR
50
MOA is endogenous glycoproteins with antineoplastic, immunosuppressive and antiviral actions
Interferon-alpha
51
hydrolyzes circulating L-asparaginase leading to rapid inhibition of protein synthesis
Asparaginase | - used for ALL
52
Vitamin derivative that allows DNA transcription and differentiation of immature leukemic promyelocytes into mature granulocytes
All-trans retinoic acid
53
Antifolate analog
Pralatrexate
54
Inhibits polymerase alpha and beta (DNA)
- Fludarabine | - Cladribine
55
DNA hypomethylating agent used for myelodysplastic syndrome
Decitabine
56
Alkylating agent used for brain tumors (astrocytoma and glioblastoma multiforme)
Temozolomide
57
Mitotic inhibitor (microtubule) used for metastatic breast CA
Eribulin
58
CD30 used for Hodgkin Lymphoma
Brentuximab
59
mTOR inhibitor used as an immunosuppressant in organ transplantation
Everolimus | Sirolimus
60
anti-CD20 used for CLL and Follicular lymphoma
Obinutuzumab
61
IgG4 isotype antibody that blocks protective mechanism of CA | targets PD-1
Pembrolizumab
62
EGFR-TK inhibitor for advanced non-small cell lung CA
Osimertinib
63
First therapeutic proteasome inhibitor used for multiple myeloma and mantle cell lymphoma
Bortezomib