Chemotherapeutics: Antimetabolites

Question 1

irreversibly and competitively binds DHF reductase

Answer 1

methotrexate

Question 2

brings folate cycle to halt

Answer 2

methotrexate

Question 3

builds up DHF

Answer 3

methotrexate

Question 4

what phase is methotrexate most effective in

Answer 4

S phase

Question 5

what does methotrexate treat

Answer 5

RA and cancer therapy drugs

Question 6

Adverse effects of methotrexate

Answer 6

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

Question 7

what reduces the toxic affects of methotrexate

Answer 7

Leucovorin (called leucovorin rescue)

Question 8

Leucovorin is also called

Answer 8

Folinic acid

Question 9

how does Leucovorin work

Answer 9

restores active folate stores

Question 10

inhibits thymidylate synthase

Answer 10

5-Flourouracil (5-FU)

Question 11

block thymidine production

Answer 11

5-Flourouracil

Question 12

causes increased dUMP

Answer 12

5-Flurouracil

Question 13

what does 5-Flurouracil treat

Answer 13

colon cancer

Question 14

leucovorin rescue works for 5-FU toxicity true/false

Answer 14

false

Question 15

5-Flourouracil side effects

Answer 15

severe diarrhea, photosensitivity, myelosuppression, hyper pigmentation

Question 16

blocks synthesis of IMP

Answer 16

Azathioprine and 6-MP

Question 17

prodrug of 6MP

Answer 17

Azathioprine

Question 18

Azathioprine converted to 6MP by what enzyme

Answer 18

Hypoxanthine-Guanine Phosphoribosyl Transferase (HGPRT)

Question 19

What phase does Azathioprine arrest cells in

Answer 19

S Phase

Question 20

Side effects of Azathioprine

Answer 20

myelosuppression

Question 21

Azathioprine treats

Answer 21

RA and organ transplant

Question 22

6 Mercaptopurine treats

Answer 22

Leukemias

Question 23

6 Mercaptopurine is metabolized by what enzyme

Answer 23

xanthine oxidase

Question 24

What drug does 6MP have a drug interaction with

Answer 24

allopurinol

Question 25

6 mercaptopurine side effects

Answer 25

myelosuppression, n/v/d, hepatotoxicity, jaundice

Question 26

how does allopurinol work

Answer 26

xanthine oxidase inhibitor

Question 27

allopurinol treats

Answer 27

gout and hyperuricemia

Question 28

allopurinol side effects

Answer 28

characteristic rash

Question 29

cladribine works by

Answer 29

inhibiting DNA pol alpha and beta

Question 30

cladribine cell specific true/false

Answer 30

true, S phase

Question 31

Cladribine treats

Answer 31

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

Question 32

Cladribine side effects

Answer 32

myelosuppression, n/v/d and neuropathy

Question 33

Cladribine is a cytotoxic ______ analog

Answer 33

purine

Question 34

Cytarabine is a cytotoxic ________ analog

Answer 34

pyrimidine analog

Question 35

cytarabine treats

Answer 35

Leukemias (AML and NonHL)

Question 36

Cytarabine MOA

Answer 36

inhibits DNA pol alpha and beta

Question 37

cytarabine side effects

Answer 37

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

Question 38

cytarabine unique property

Answer 38

rapaidly degraded; ineffective to solid tumors

Question 39

gemcitabine MOA

Answer 39

inhibits ribonucleotide reductase and DNA pol a and b

Question 40

side effects gemcitabine

Answer 40

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

Question 41

Floxuridine treats

Answer 41

Gi tumor metastases to liver

Question 42

5-FU prodrugs

Answer 42

Floxuridine and Capecitabine

Question 43

Capecitabine treats

Answer 43

breast and colon cancer

Question 44

6-thioguanine (6TG) is similar to

Answer 44

6MP

Question 45

6-thioguanine treats

Answer 45

leukemias

Question 46

6-thioguanine side effects

Answer 46

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

Question 47

6-thioguanine unique properties

Answer 47

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

Question 48

Fludarabine MOA for triphosphate metabolite

Answer 48

inhibits DNA pol a and b

Question 49

Fludarabine MOA for diphosphate metabolite

Answer 49

inhibits ribonucleotide reductase

Question 50

Fludarabine treats

Answer 50

leukemias/lymphomas

Question 51

fludarabine side effects

Answer 51

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

Question 52

fludarabine unique properties

Answer 52

causes apoptosis in susceptible cells