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Pharmacology > Anticancer Drugs > Flashcards

Anticancer Drugs Flashcards

1
Q

Alkylating drugs (mitomycin & cisplatin) MOA

A

carbonium ion –> covalent bonds w/ DNA –>impedes replication

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2
Q

Antimetabolites MOA

A

block or subvert one or more metabolic pathways in DNA synthesis

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3
Q

Cytotoxic antibiotics MOA

A

blocks mammalian cell division

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4
Q

Vinca Alkaloids MOA

A

binds to tubulin –> prevents formation of mitotic spindles–> arrests cell at metaphase

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5
Q

Protein kinase inhibitor MOA

A

blocks tyrosine kinases that tranduce growth signals

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6
Q

Methotrexate MOA (2)

A

inhibits dihydrofolate reduction,

block DTMP & purine synthesis

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7
Q

Doxorubicin MOA

A

blocks topoisomerase II fxn

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8
Q

5-fluorouracil MOA

A

inhibits DTMP synthesis (DNA only)

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9
Q

L-asparaginase MOA

A

catalyses hydrolysis of l-asparagine to l-aspartic acid & ammonia –> deaminates asparagine & inhibits protein synthesis

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10
Q

Paclitaxel & Docetaxel (Taxanes) MOA

A

Stabilizes microtubules in the polymerized state

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11
Q

What is commonly seen w/ BM toxicity due to chemotherapuetics?

A

leukopenia

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12
Q

BCG MOA

A

stimulates immune system to recognize tumor cells

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13
Q

What molecule dissociates once Cisplatin enters the cell?

A

Cl

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14
Q

Methotrexate is a _____ ANTagonist.

A

folate

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15
Q

Solubility of methotrexate

A

low lipid solubility

actively taken up by cells via folate transport system

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16
Q

4 reasons for using combos of cancer drugs on a TX schedule (TQ)

A
  1. Incr. cytotoxicity w/o increasing gen. toxicity
  2. Decr. resistance to individual agents
  3. Permit BM regeneration
  4. More effective when given as 1 or 2 LG doses
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17
Q

Main problem of alkylating agents

A

Strong cross-resistance

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18
Q

What enzyme activates Cyclophosphamide in the liver? (it’s a pro-drug) (TQ)

A

CYP450

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19
Q

Slowest working alkylating agent? Benefits?

A

Chlorambucil

lowest toxicity

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20
Q

Do NOT use cytotoxic antibiotics w/ what other form of therapy?

A

radiotherapy (toxicity)

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21
Q

Doxorubicin & dactinomycin inhibit DNA synthesis by interferring w/ _____.

A

Topoisomerase II

22
Q

What type of cells does bleomycin work on?

A

non-dividing cells

23
Q

Depletion of EXTRAcellular stores of _____ lead to inhibition of protein synthesis.

A

L-asparaginase

24
Q

L-asparaginase only attacks cells lacking what enzyme?

A

L-asparagine synthetase

25
Q

List 2 taxanes derived from Taxus spp plants (bark of yew tree).

A

Paclitaxel

Docetaxel

26
Q

Which drugs should you NEVER give to horses (death!)?

A

Paclitaxel

Docetaxel

27
Q

List the 3 tyrosine kinase inhibitors

A

Imatinib
Toceranib
Mastinib

28
Q

Tyrosine kinase inhibitors block _______.

A

angiogenesis (slows down tumor growth)

29
Q

Bevacizumab blocks the ______ receptor.

A

vascular endothelial growth factor receptor

30
Q

Cetuximab blocks the _____ receptor.

A

epidermal growth factor receptor

31
Q

Trastuzumab blocks the _____ receptor.

A

human epithelial R2

32
Q

Imatinib blocks the ______ receptor.

A

platelet derived growth factor receptor

33
Q

List the 3 antibodies that target epidermal growth factor receptors.

A

Cetuximab
Trastuzumab
Bevacizumab

34
Q

Which antibody works on ErbB-1 expressing tumors?

A

Cetuximab

35
Q

Which anitbody works on ErbB-2 expressing tumors?

A

Trastuzumab

36
Q

Which antibody works on VEGFR in mastocytoma cells?

A

Bevacizumab

37
Q

Possible problem when using glucocorticoids & chemotherapeutics together.

A

Mutli-drug resistance

via induction of PgP (permeability glycoprotein)

38
Q

Which 3 drugs have demonstrated resistance due to decreased accumulation of cytotoxic drugs? (TQ)

A

Doxorubicin
Vinblastine
Dactinomycin

39
Q

Mode of resistance for methotrexate? (TQ)

A

Decreased drug uptake by the cell

40
Q

Mode of resistance for 5-fluorouracil? (TQ)

A

Insufficient activation of the drug

41
Q

Mode of resistance for antimetabolites. (TQ)

A

Increased utilization of alternative metabolic pathways

42
Q

Mode of resistance for alkylating agents. (TQ)

A

Rapid repair of drug induced lesions

43
Q

Mode of resistance for Doxorubicin? (TQ)

A

Altered activity of the drug’s target (topoisomerase II)

44
Q

Active metabolite of Cyclophosphamide

A

Acrolein

45
Q

List 5 nitrogen mustards (alkylating agents).

A

Cyclophosphamide
Melphalan
Chlorambucil
Ifosfamide

46
Q

Alkyl sulfonate alkylating agent

A

Busulfan

47
Q

Non-classical alkylating agent

A

Dacarbazine

48
Q

Nitrosurea alkylating agent

A

Lomustine

49
Q

List 2 platinum coordination complex alkylating agents

A

Cisplatin

Carboplatin

50
Q

List 4 cytotoxic antibiotics

A

Doxorubicin
Dactinomycin
Bleomycin
Mitomycin

Pharmacology (21 decks)

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