cancer

Question 1

antimetabolites

Answer 1

azathioprine, 6 mercaptopurine, cladribine, cytarabine (arabinofuranosyl cytidine), 5-florouracil, methotrexat

Question 2

azathioprine, 6 mercaptopurine mechanism

Answer 2

purine (thiol) analogs. decreae de novo purine sytnhesis. activated by HGPRT.

Question 3

what is azathioprine metabolized into

Answer 3

6MP

Question 4

use of azathioprine, 6 mercaptopurine

Answer 4

prevents organ rejection, RA, IBD, SLE;

used to wean patients off steroids in chronic disease and to treat steroid refractory chronic disease

Question 5

SE of azathioprine, 6 mercaptopurine

Answer 5

myelosupression, GI liver.
azathioprine and 6MP are metabolized by xanthine oxidase; thus both have increase toxicity with allopurinol or febuxostat

Question 6

antimetabolites block what phase of cellcycle

Answer 6

S phase

Question 7

cladribine mechanism

Answer 7

purine analog; multiple mechanisms ( inhibiton of dna polymerase, dna strand breaks)

Question 8

use of cladibrine

Answer 8

hairy cell leukemia

Question 9

hairy cell leukemia treated by

Answer 9

cladibrine

Question 10

se of cladibrine

Answer 10

myelosuppression, nephrotoxciity, neurotoxicity

Question 11

an antimetaboilte that is a pyrimidein analog; causes inhibtion of dna polymerase

Answer 11

cytarabine

Question 12

use of cytaribne

Answer 12

leukemias (AML), lymphomas

Question 13

SE of cytarabine

Answer 13

myelosuppression with megaloblastic anemia. cytarabine causes pancytopenia
CYTarabine: panCYTopenia

Question 14

5 fluorouracil mechanism

Answer 14

pyrimidine analog bioactivated to 5-FdUMP, which covalently complexes with thimidylate synthase and folic acid.

Question 15

prodrug with similar activity to 5 fluorouracil

Answer 15

capecitabine

Question 16

5 fluorouracil continued mechaism

Answer 16

complex inhibits thimydlate synthase : decrease dTMP and decreasing DNA syntehsis

Question 17

use of 5 fluorouracil

Answer 17

colon cancer, pancreatic cancer, basal cell carcionma

Question 18

the addition of leucovorin enhacnces the effect of

Answer 18

5 fluooruacila

Question 19

SE of 5 fluoroucail

Answer 19

myelosuppression, palmar plantar erythrodysesthesia (hand foot syndrome)

Question 20

methotrexate mechanism

Answer 20

folic acid analog that competitvely inhibits dihydrofolate reductase: decreasing dTMP; decreasing DNA synthesis

Question 21

use of methotrexate

Answer 21

leukemias (ALL), lymphomas, choriocarcinoma, sarcomas;

non-neoplastic: ectopic pregnancy; medical abortion (with misoprostol), RA, psoriasis, IBD, vasculitis

Question 22

ectopic pregnancy treamtnet

Answer 22

methotrexat (inhibits trophoblast division, therefore decreses trophoblast survival, hindering implantation, and encouraging expulsion

Question 23

leucovorin rescue

Answer 23

methotrexate

Question 24

se of methotrexate

Answer 24

myelosuppression (reversible w leucovorin), hepatotoxcicity (cirrhosis), mucositis, pulmonary fibrosis, bone marrow (pancytopenia, hair follicles (alopecia), GI mucosa (ulcerations - apthous - death of mucsoa)

Question 25

after entering target cell, Methotrexate undergoes ____ which prevents movement ofe methotrexatioe out of cell

Answer 25

polyglutamation; which prevents movement of methotrexate

Question 26

antitumor antiboitcs

Answer 26

bleomycin, dactinomycin (actinomycin D), doxorubicin, daunorubicin)

Question 27

bleomycin mechanism

Answer 27

induces free radical formation: breaks in DNA strands

Question 28

use of bleomycin

Answer 28

testicular cancer, hodgkin lymphoma

Question 29

se of bleomycin

Answer 29

pulmonary fibrosis, skin hyperpigmentation. minimal myelosuppression

Question 30

dactinomycin (actinomycin D) mechanism

Answer 30

intercalates in DNA

Question 31

use of dactinomycin

Answer 31

wilms tumor, ewing sarcoma, rhabdomyosarcoma. used for childhood tumors

Question 32

SE of dactinomycin

Answer 32

myelosuppression

Question 33

doxorubicin, | daunorubicin mechainsm

Answer 33

generates free radicals | intercaltes in DNA -> breaks in DNA -> decrease replication

Question 34

bleomycin and doxorubicin work at what phase

Answer 34

G2

Question 35

use of doxorubicin, daunorubicin

Answer 35

solid tumors, leukemias, lymphomas

Question 36

SE of doxorubicin, daunorubicin

Answer 36

cardiotoxicity (dilated cardiomyopathy, myelosuppression, alopecia) cardiotoxicity forms from anthracyte : topoisomerase II complex that forms in healthy cardiomycoytes

Question 37

iron chelating agent used to prevent cardiotoxicty in doxorubicin

Answer 37

dexrazoxane

Question 38

alkylating agents

Answer 38

busulfan, cyclophosphamide, ifosfamide nitrosureas

Question 39

busulfan mechanism

Answer 39

cross links DNA

Question 40

use of busulfan

Answer 40

CML. also used to ablate bone marrow before bone marrow transplatntion

Question 41

SE of busulfan

Answer 41

severe myelosuppression (in almost all clses); pulmonary fibrosis, hyperpigmentation

Question 42

cyclophosphamide, ifosfamide mechanism

Answer 42

cross-link DNA at guanine N-7; require bioactivation by liver; a nitrogen mustard

Question 43

use of cyclopshopahmide, ifosfamide

Answer 43

solid tumors, leukkemai, lymphomas

Question 44

SE of cyclophosphamide, ifosfamide

Answer 44

myelosuppression; hemorraghich cystitis,

Question 45

hemorraghic cystiits in cyclophsomaide toxicity prevented with

Answer 45

mesna or n-acetylcysteine

Question 46

thiol group of ___ binds toxic metaboits in hemorraghich cystiits

Answer 46

mesna

Question 47

nitrosoureas mechanism

Answer 47

require bioactviation; cross BBB -> CNS. Cross link DNA

Question 48

use of nitrosoureas

Answer 48

brain tumors (including glioblastoma multiforme)

Question 49

SE of nitrosoureas

Answer 49

CNS toxicity (convulsions, dizziness, ataxia)

Question 50

microtubule inhibitors

Answer 50

paclitaxel, vincristine, vinblastine

Question 51

paclitaxel mechanism

Answer 51

hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)

Question 52

microtuuble inhibitors work in

Answer 52

M phase

Question 53

use of paclitaxel

Answer 53

ovarian and breast carcinomas

Question 54

SE of paclitaxel

Answer 54

myelosuppression, neuropathy, hypersenstiivty

Question 55

vincristine , vinblatine mechanism

Answer 55

vinca alkaloids that bind B-tubulin and inhibit its polymerization into microtubules -> prevent mitotic spindle formation (M-phase arrest)

Question 56

use of vincristine vinblastine

Answer 56

solid tumors, leukemias, hodgkin (vinblastine) and non-hodgkin (vincristine) lymphomas

Question 57

vincristine SE

Answer 57

neurotoxicity (areflexia, peripheral neuritis), constipation (including paralytic ileus)

Question 58

cisplatin, carboplatin use

Answer 58

testicular bladder ovary lung carcinomas

Question 59

cisplatin carboplatin mechainsm

Answer 59

crross link DNA

Question 60

se of cisplatin, carboplatin

Answer 60

nephrotoxicity, peripihreal neuropathy, ototoxicity. prevent nephrotoxicity with amifostine (free radical scavenger) and chloride (saline) diuresis

Question 61

etoposide, teniposide mechanism

Answer 61

etoposide, teniposide inhibits sealing activity of topoisomerase II: increasing DNA degradation

Question 62

SE of etoposide , teniposide

Answer 62

myelosuppression, alopecia

Question 63

mechanism of etoposide, teniposide

Answer 63

solid tumors (particularly testicular and small cell lung cancer), leukemia lymphomas

Question 64

irinotecan, topotecan

Answer 64

inhibit topoisomerase I and prevent dna unwinding and replication

Question 65

use of irinotecan, topotecan

Answer 65

colon cancer (irinotecan); ovarian and small cell lung cancer (topotecan)

Question 66

SE of irinotecan, topotecan

Answer 66

severe myelosuppression, diarrhea

Question 67

hydroxyurea mechanism

Answer 67

inhibits ribonucleotide reductase : decrease DNA syntehsis (S phase specific)

Question 68

use of hydroxyurea

Answer 68

myeloproliferative disorders (CML, poly vera), sickle cell (increase HbF); melanoma

Question 69

se of hydroxurea

Answer 69

myelosuppresion