WebCAI - AntiCancer Drugs

Question 1

MOA mechlorethamine

Answer 1

alkylating agent - cross links strands of DNA

most common position: N-7 position of guanidine

Question 2

MOA fluorouracil

Answer 2

pyrimidine antagonist that inhibits thymidylate synthesis

Question 3

MOA mercaptopurine

Answer 3

purine antagonist that inhibits purine synthesis

Question 4

is vincristine a plant alkaloid?

Answer 4

yes

Question 5

highest incidence of alopecia?

Answer 5

cyclophosphamide

Question 6

MOA busulfan

what is it used for?

Answer 6

alkylating agent; used for CML

Question 7

MOA cytarabine; what is it used for?

Answer 7

MOA: pyrimidine analog that inhibits DNA synthesis

use: leukemias and lymphomas

Question 8

what drug is used for hair cell leukemia?

Answer 8

cladribine

Question 9

what drugs can cross the BBB?

Answer 9

nitrosoureas: carmustine, lomustine, semustine, streptozotocin

Question 10

what drug is useful in treating functional, malignant pancreatic islet cell tumors?

Answer 10

streptozotocin

Question 11

signature adverese effect of methotrexate

Answer 11

cirrhosis

Question 12

signature adverese effect of bleomycin

Answer 12

pulmonary fibrosis

Question 13

signature adverese effect of cyclophosphamide

Answer 13

cystitis

Question 14

signature adverese effect of alkylating agents

Answer 14

amenorrhea

Question 15

signature adverese effect of cisplatin

Answer 15

nephrotoxicity

Question 16

signature adverese effect of fluorouracil

Answer 16

hand and foot syndrome

Question 17

can you use folic acid to treat methotrexate toxicity?

Answer 17

no - use folinic acid

folic acid -> dihydrofolic acid -> tetrahydrofolic acid -> folinic acid

methothrexate inhibits the first two steps in this pathway

Question 18

what drug does folinic acid potentiate?

Answer 18

fluorouracil - facilitates its binding to thymidylate synthase

Question 19

how is mercaptopurine activated

Answer 19

via purine salvage pathway (HGPRT)

Question 20

what can mercaptopurine be used for?

Answer 20

ALL, crohn’s disease, ulcerative colitis

Question 21

allopurinol would most likely potentiate the pharmacologic actions of….

Answer 21

mercaptopurine:

• purine nucleic acids are converted to uric acid by the enzyme xanthine oxidase resulting in hyperuricemia followed by gouty neuropathy.
• This can be prevented by the use of allopurinol which is an inhibitor of xanthine oxidase.
• Since mercaptopurine is also destroyed by xanthine oxidase, administration of allopurinol potentiates the pharmacological action of mercaptopurine; both its tumoricidal as well as its toxic effects,

the dose of mercaptopurine must be reduced when used with allopurinol

Question 22

azathioprine is usually used in what context

Answer 22

immunosuppression - allograft rejection

is an antimetabolite to purine utilization

Question 23

what is a fungal derived immunosuppressive agent used to prevent allograft rejection?

Answer 23

cyclosporine

Question 24

gefitinib

Answer 24

EGFR - tyrosine kinase inhibitor

used for non-small cell lung cancer

Question 25

alkylating agents

Answer 25

mechlorethamine, nitrosoureas, cyclophosphamide, busulfan, platin drugs

Question 26

drugs that inhibit thymidylate synthetase

Answer 26

fluorouracil, capecitabine

Question 27

causes metaphase arrest

Answer 27

vinca alkaloids, taxanes, colchicine

Question 28

intercalates with DNA

Answer 28

"rubicin", actinomycin (D), mitomycin mitoxantrone

Question 29

inhibits folic acid reductase

Answer 29

methotrexate, premetrexid, pralatrexate

Question 30

dose limiting toxicity of vincristine

Answer 30

peripheral nervous system toxicity

Question 31

dose limiting toxicity of vinblastine

Answer 31

bone marrow toxicity "blast the bone marrow"

Question 32

what drug inhibits DNA-dependent RNA synthesis?

Answer 32

dactinomycin

Question 33

what drug is converted in the body to thioinosinic acid and competes with AMP/GMP?

Answer 33

mercaptopurine

Question 34

name three drugs that have relatively low toxicity to bone marrow

Answer 34

bleomycin, vincristine and cisplatin

Question 35

what cancers are deficient in asparagine synthetase?

Answer 35

leukemias

Question 36

does dactinomycin need to be biotransformed in order to be active in the body?

Answer 36

no

Question 37

name three alkylating drugs that can be administered orally?

Answer 37

cyclophosphamide, chlorambucil, busulfan