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PHRM 864 > L7 Antimetabolites > Flashcards

L7 Antimetabolites Flashcards

1
Q

Which of the following drugs targets Her2?

A. Sirolimus
B. Alectinib
C. Vemurafinib
D. Tucatinib

A

D

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2
Q

Which of the following drugs targets a kinase that is produced by formation of the Philadelphia chromosome?

A. Alectinib
B. Gefitinib
C. Imatinib
D. binimetinib

A

C

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3
Q

Which compound below is not a covalent kinase inhibitor?

	A. Gefitinib
	B. Osimertinib 
	C. Afatinib 
	D. Acalabrutinib
A

A

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4
Q

Which type of kinase inhibitor can bind in the ATP binding site and stabilize the inactive confirmation of a kinase?

	A. Type I
	B. Type II 
	C. Type III
	D. Type IV
A

B

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5
Q

T or F:
Antimetabolites are typically analogs of naturally occurring metabolites

A

true

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6
Q

T or F:
most antimetabolites require biotransformation to a nucleotide analog to be active

A

true

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7
Q

what are the 2 ways pyrimidine analogs can interfere with metabolism?

A

interfere with pyrimidine synthesis
inhibit DNA polymerase

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8
Q

what is the fluorinated uracil analog?

A

5-fluorouracil (5-FU)

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9
Q

what is the significance of 5-FU being converted into fDUMP or fUTP?

A

5-FU has a short half life in plasma, the others get into the cell and persist

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10
Q

in the presence of folates, __________ _________ synthesizes thymidine monophosphate (TMP) from dUMP ***

A

thymidylate synthase

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11
Q

T or F:
upregulation of thymidylate synthase contributes to 5-FU resistance

A

True

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12
Q

what is the enzyme that breaks down 5-FU?

A

dihydropyrimidine dehydrogenase (DPD)

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13
Q

what is the “rescue” for 5-FU overdose?

A

thymidine

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14
Q

what is the connection between 5-FU and leucovorate?

A

leucovorate is a folate cofactor that is converted to tetrahydrofolate in cells, higher levels of tetrahydrofolate increases the efficacy of 5-FU

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15
Q

what do the cytosine analogs primarily inhibit?

A

DNA synthesis

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16
Q

what class is cytarabine?

A

cytosine analog

17
Q

Cytarabine gets converted to ______ intracellularly

A

Ara-CTP

18
Q

what is Ara-CTP

A

the thing cytarabine gets converted into, it is a competitive inhibitor of DNA polymerase alpha

19
Q

what converts cytarabine into non-toxic uracil arabinoside?

A

cytidine deaminase

20
Q

T or F:
Increased levels of cytidine deaminase in the CNS makes Ara-C highly toxic

A

False, decreased levels

21
Q

what class is gemcitabine

A

cytosine analog

22
Q

T or F:
Cytarabine is more potent than the other cytosine analog Gemcitabine

A

false, gem is more

23
Q

what does tetrahydrouridine inhibit?

A

cytidine deaminase (CDA)

24
Q

T or F:
Cytarabine is inactivated by cytidine deaminase

A

True

25
Q

Tetrahydrouridine is given with _____ to increase efficacy and decrease resistance

A

cytarabine

26
Q

Nucleoside analog:
A. 5-FU
B. Cytarabine

A

A. 5-FU

27
Q

6-MP is a _____ analog

A

purine

28
Q

6-MP inhibits multiple enzymes in the __________________________ pathway

A

de novo purine biosynthesis

29
Q

T or F:
6-MP blocks the synthesis of purine nucleotides

A

true

30
Q

6-MP is inactivated by what?

A

thiopurine methyl transferase (TPMT)

31
Q

what common drug has an interaction with 6-MP that is definitely on the exam

A

allopurinol

32
Q

why is there a bad drug reaction between 6-MP and allopurinol

A

xanthine oxidase breaks down 6-MP, allopurinol is a xanthine oxidase inhibitor

33
Q

T or F:
allopurinol blocks the breakdown of both purine analogs, 6-MP and 6-TG

A

false, just 6-MP

34
Q

Which drug primarily interferes with purine biosynthesis?

A. 5-Fluorouracil

B. Capecitabine

C. 6-Mercaptopurine

D. Cytosine arabinoside

A

C

35
Q

make some folic acid flashcards because im brain dead and not getting the slide rn

A

okay later bro

36
Q

stopped at slide 39

A

PHRM 864 (23 decks)

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