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Block 8 drugs > Chemotherapeutics: Antimetabolites > Flashcards

Chemotherapeutics: Antimetabolites Flashcards

1
Q

irreversibly and competitively binds DHF reductase

A

methotrexate

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2
Q

brings folate cycle to halt

A

methotrexate

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3
Q

builds up DHF

A

methotrexate

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4
Q

what phase is methotrexate most effective in

A

S phase

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5
Q

what does methotrexate treat

A

RA and cancer therapy drugs

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6
Q

Adverse effects of methotrexate

A

megaloblastic anemia, myelosuppression, pulmonary fibrosis, hepatotoxicity, alopecia, mucositis

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7
Q

what reduces the toxic affects of methotrexate

A

Leucovorin (called leucovorin rescue)

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8
Q

Leucovorin is also called

A

Folinic acid

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9
Q

how does Leucovorin work

A

restores active folate stores

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10
Q

inhibits thymidylate synthase

A

5-Flourouracil (5-FU)

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11
Q

block thymidine production

A

5-Flourouracil

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12
Q

causes increased dUMP

A

5-Flurouracil

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13
Q

what does 5-Flurouracil treat

A

colon cancer

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14
Q

leucovorin rescue works for 5-FU toxicity true/false

A

false

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15
Q

5-Flourouracil side effects

A

severe diarrhea, photosensitivity, myelosuppression, hyper pigmentation

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16
Q

blocks synthesis of IMP

A

Azathioprine and 6-MP

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17
Q

prodrug of 6MP

A

Azathioprine

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18
Q

Azathioprine converted to 6MP by what enzyme

A

Hypoxanthine-Guanine Phosphoribosyl Transferase (HGPRT)

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19
Q

What phase does Azathioprine arrest cells in

A

S Phase

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20
Q

Side effects of Azathioprine

A

myelosuppression

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21
Q

Azathioprine treats

A

RA and organ transplant

22
Q

6 Mercaptopurine treats

23
Q

6 Mercaptopurine is metabolized by what enzyme

A

xanthine oxidase

24
Q

What drug does 6MP have a drug interaction with

A

allopurinol

25
Q

6 mercaptopurine side effects

A

myelosuppression, n/v/d, hepatotoxicity, jaundice

26
Q

how does allopurinol work

A

xanthine oxidase inhibitor

27
Q

allopurinol treats

A

gout and hyperuricemia

28
Q

allopurinol side effects

A

characteristic rash

29
Q

cladribine works by

A

inhibiting DNA pol alpha and beta

30
Q

cladribine cell specific true/false

A

true, S phase

31
Q

Cladribine treats

A

Leukemia/Lymphomas (Chronic Lymphocytic Leukemia and Non hodgekin Lymphoma)

32
Q

Cladribine side effects

A

myelosuppression, n/v/d and neuropathy

33
Q

Cladribine is a cytotoxic ______ analog

34
Q

Cytarabine is a cytotoxic ________ analog

A

pyrimidine analog

35
Q

cytarabine treats

A

Leukemias (AML and NonHL)

36
Q

Cytarabine MOA

A

inhibits DNA pol alpha and beta

37
Q

cytarabine side effects

A

myelosuppression, n/v/d, neurotoxicity (at high doses)

38
Q

cytarabine unique property

A

rapaidly degraded; ineffective to solid tumors

39
Q

gemcitabine MOA

A

inhibits ribonucleotide reductase and DNA pol a and b

40
Q

side effects gemcitabine

A

myelosuppression, n/v, flu like symptoms, hemolytic-uremic syndrome, thrombotic thrombocytopenic purpura

41
Q

Floxuridine treats

A

Gi tumor metastases to liver

42
Q

5-FU prodrugs

A

Floxuridine and Capecitabine

43
Q

Capecitabine treats

A

breast and colon cancer

44
Q

6-thioguanine (6TG) is similar to

45
Q

6-thioguanine treats

46
Q

6-thioguanine side effects

A

myelosuppression, n/v/d, neurological (at high doses)

47
Q

6-thioguanine unique properties

A

not metabolized by XO like 6MP. dose modified in pts with thiopurine methyltransferase (TPMT)

48
Q

Fludarabine MOA for triphosphate metabolite

A

inhibits DNA pol a and b

49
Q

Fludarabine MOA for diphosphate metabolite

A

inhibits ribonucleotide reductase

50
Q

Fludarabine treats

A

leukemias/lymphomas

51
Q

fludarabine side effects

A

myelosupression, n/v/d, neurological (at high doses)

52
Q

fludarabine unique properties

A

causes apoptosis in susceptible cells

Block 8 drugs (12 decks)

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