Anticancer Drugs Flashcards Preview

Pharmacology > Anticancer Drugs > Flashcards

Flashcards in Anticancer Drugs Deck (50):
1

Alkylating drugs (mitomycin & cisplatin) MOA

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

2

Antimetabolites MOA

block or subvert one or more metabolic pathways in DNA synthesis

3

Cytotoxic antibiotics MOA

blocks mammalian cell division

4

Vinca Alkaloids MOA

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

5

Protein kinase inhibitor MOA

blocks tyrosine kinases that tranduce growth signals

6

Methotrexate MOA (2)

inhibits dihydrofolate reduction,
block DTMP & purine synthesis

7

Doxorubicin MOA

blocks topoisomerase II fxn

8

5-fluorouracil MOA

inhibits DTMP synthesis (DNA only)

9

L-asparaginase MOA

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

10

Paclitaxel & Docetaxel (Taxanes) MOA

Stabilizes microtubules in the polymerized state

11

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

leukopenia

12

BCG MOA

stimulates immune system to recognize tumor cells

13

What molecule dissociates once Cisplatin enters the cell?

Cl

14

Methotrexate is a _____ ANTagonist.

folate

15

Solubility of methotrexate

low lipid solubility
actively taken up by cells via folate transport system

16

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

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

17

Main problem of alkylating agents

Strong cross-resistance

18

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

CYP450

19

Slowest working alkylating agent? Benefits?

Chlorambucil
lowest toxicity

20

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

radiotherapy (toxicity)

21

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

Topoisomerase II

22

What type of cells does bleomycin work on?

non-dividing cells

23

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

L-asparaginase

24

L-asparaginase only attacks cells lacking what enzyme?

L-asparagine synthetase

25

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

Paclitaxel
Docetaxel

26

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

Paclitaxel
Docetaxel

27

List the 3 tyrosine kinase inhibitors

Imatinib
Toceranib
Mastinib

28

Tyrosine kinase inhibitors block _______.

angiogenesis (slows down tumor growth)

29

Bevacizumab blocks the ______ receptor.

vascular endothelial growth factor receptor

30

Cetuximab blocks the _____ receptor.

epidermal growth factor receptor

31

Trastuzumab blocks the _____ receptor.

human epithelial R2

32

Imatinib blocks the ______ receptor.

platelet derived growth factor receptor

33

List the 3 antibodies that target epidermal growth factor receptors.

Cetuximab
Trastuzumab
Bevacizumab

34

Which antibody works on ErbB-1 expressing tumors?

Cetuximab

35

Which anitbody works on ErbB-2 expressing tumors?

Trastuzumab

36

Which antibody works on VEGFR in mastocytoma cells?

Bevacizumab

37

Possible problem when using glucocorticoids & chemotherapeutics together.

Mutli-drug resistance
via induction of PgP (permeability glycoprotein)

38

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

Doxorubicin
Vinblastine
Dactinomycin

39

Mode of resistance for methotrexate? (TQ)

Decreased drug uptake by the cell

40

Mode of resistance for 5-fluorouracil? (TQ)

Insufficient activation of the drug

41

Mode of resistance for antimetabolites. (TQ)

Increased utilization of alternative metabolic pathways

42

Mode of resistance for alkylating agents. (TQ)

Rapid repair of drug induced lesions

43

Mode of resistance for Doxorubicin? (TQ)

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

44

Active metabolite of Cyclophosphamide

Acrolein

45

List 5 nitrogen mustards (alkylating agents).

Cyclophosphamide
Melphalan
Chlorambucil
Ifosfamide

46

Alkyl sulfonate alkylating agent

Busulfan

47

Non-classical alkylating agent

Dacarbazine

48

Nitrosurea alkylating agent

Lomustine

49

List 2 platinum coordination complex alkylating agents

Cisplatin
Carboplatin

50

List 4 cytotoxic antibiotics

Doxorubicin
Dactinomycin
Bleomycin
Mitomycin