Antimetabolites Flashcards

1
Q

antimetabolites destroy cells during what phase of the cell cycle

A

S phase- when DNA is synthesized

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2
Q

poorly lipid soluble folate analogue refers to which medication (folic acid antagonist)

A

methotrexate

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3
Q

what enzyme does methotrexate inhibit

A

dihydrofolate reductase

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4
Q

what form is methotrexate administerad

A

oral

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5
Q

what is methotrexate used for in children but not adults

A

acute lymphoblastic leukemia in children but not adults

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6
Q

other uses of methotrexate

A

rheumatoid arthritis

psoriasis

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7
Q

what three ways do resistance to methotrexate develop

A

impaired transport into cells

production of altered forms of dihydrofolate reductase (lacking affinity to the drug)

increased concentrations of intracellular dihydrofolate reductase

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8
Q

what are the most important side effects of methotrexate

A

GI- ulcerative stomatitis and diarrhea

bone marrow suppression -leukopenia and thrombocytopenia

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9
Q

what does the methotrexate pulmonary toxicity take form as

A

fulminant non cariogenic pulmonary edema
or
more progressive inflammation with interstitial infiltrates and pleural effusions

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10
Q

what should we measure preoperatively if the patient has had recent methotrexate

A

liver enzymes

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11
Q

what is the rescue technique used for methotrexate

A

protecting normal cells from lethal damage by folate antagonist by administration of folinic acid (leucovorin), thymidine, or both

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12
Q

how does fluorouracil work

A

by blocking production of thymine nucleotide by inhibiting thymidlyate synthase

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13
Q

T/F

flurouracil readily enters the CSF

A

True

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14
Q

clinical uses of fluorouracil

A

breast Ca, GI ca, keratoses of the skin and superficial basal cell carcinoma

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15
Q

this can occur up to one week after administration of fluorouracil

A

MI

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16
Q

what is the early warning sign of fluorouracil toxicity

A

stomatitis manifesting as a white patchy membrane that ulcerates and becomes necrotic - may warn of similar lesions in the esophagus and GI tract

17
Q

what occurs 9-14 days following therapy and is a serious side effect of fluorouracil

A

myelosuppression manifesting as leukopenia and thrombocytopenia

18
Q

what is capecitabine metabolized to, why do we administer capecitabine

A

metabolized to fluorouracil and has the potential to be more selective than fluorouracil (breast ca)

19
Q

what is pemetrexed used for

A

mesothelioma and lung ca

20
Q

cytarabine clinical use

A

acute leukemia in children and adults

21
Q

side effects of cytarabine at high doses

A

cerebellar toxicity and ataxia can occur at high doses

22
Q

what is gemcitabine used for

A

pancreas ca
breast ca
lung ca

23
Q

common side effects of gemcitabine

A
bone marrow suppression
flulike symptoms
fever
fatigue
mild nausea and vomiting
diarrhea
24
Q

mercaptopurine is incorporated into DNA or RNA strands how does it work

A

block further strand synthesis or causes structural alterations that damage DNA

25
Q

what is mercaptopurine clinical use

A

acute leukemia in children.

26
Q

why do we give allopurinol with mercaptopurine

A

allopurinol blocks xanthine (which oxidizes mercaptopurine)
able to decrease mercaptopurine dose 1/3 when combined with allopurinol.

*hyperuricemia and hyperuricosuria also occur

27
Q

with administration of mercaptopurine- what happens in 1/3 of patients

A

jaundice associated with bile stasis and occasional hepatic necrosis

28
Q

what is the principle side effect of mercaptopurine

A

bone marrow suppression-thrombocytopenia, granulocytopenia or anemia.

29
Q

what is thioguanine administered for

A

acute myelogenous leukemia

30
Q

thioguanine must be administered with ___drug but we do not decrease the dose

A

allopurinol-

31
Q

side effects of thioguanine

A

bone marrow suppression

gi effects

32
Q

pentostatin and cladribine clinical uses

A

hairy cell leukemia

33
Q

what is a side effect of cladribine

A

fever due to cytokines

34
Q

pentostatin and cladribine both have recovery from immunosuppression- which drug has faster recovery

A

cladribine

35
Q

hydroxurea clinical uses

A

chronic myelogenous leukemia