Anti-cancer Drugs

Question 1

How does methotrexate work

Answer 1

it’s an antimetabolite - inhibits dihydrofolate reductase, which inhibits the conversion of dUMP to dTMP, which decreases DNA and decreases protein synthesis

Question 2

What are the 3 uses for methotrexate

Answer 2

1. Solid cancer: leukemia, lymphoma, sarcomas, choriocarcinoma 2. Abortion, ectopic pregnancy 3. Immunosuppression: rheumatoid arthritis, psoriasis

Question 3

Methotrexate toxicity

Answer 3

myleosuppresion that is reversible with folinic acid “rescue” (Leucovorin) and fibrotic lung

Question 4

Mechanism of 5 flourouracil

Answer 4

a pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid - this inhibits thymidylate synthase, which decreases dTMP, which decreases DNA and protein synthesis

Question 5

5FU has synergy with

Answer 5

Methotrexate

Question 6

How is 5FU myelosuppression different from MTX

Answer 6

Myelosuppression is not reversible with leucocorin in 5-FU, but is with MTX. neeed thymidine rescue with 5-FU

Question 7

What is the mechanism of 6-Mercaptopurine (6-MP)

Answer 7

A purine analogue (just like allopurinol) that decrease de novo synthesis. Activated by HGPRTase.

Question 8

What is the toxicity of 6-MP increased with

Answer 8

It’s metabolized by xanthine oxidase, so toxicity increases with allopurinol

Question 9

What is 6-Thioguanate (6-TG)

Answer 9

The same as 6-MP except it can be given with allopurinol

Question 10

Cytarabine

Answer 10

A pyrimidine analog - inhibition of DNA polymerase

Question 11

All anti metabolites work in

Answer 11

S phase

Question 12

Dactinomyocin

Answer 12

Intercalates DNA

Question 13

Dactinomyocin is used for

Answer 13

Children’s tumors: wilm’s tumor, ewing’ sarcoma, rhabdomyosarcoma

Question 14

How does doxorubicin work

Answer 14

It generates free radicals by noncovalently (dactinomyocin covalently) intercalating DNA, causing breaks in DNA, which decreases replication

Question 15

Doxorubicin toxicity and Rx for that

Answer 15

cardiotoxicity - because the heart lack superoxide dismutase, causing cardiomyopapthy; Dexrazoxane is used to prevent it

Question 16

Bleomycin MOA

Answer 16

Induces free radical formation, which causes breaks in DNA strands

Question 17

Eradicated Ball Cancer

Answer 17

Etoposide, Bleomycin, Cisplatin

Question 18

Bleomycin toxicity

Answer 18

Pulmonary fibrosis

Question 19

Etoposide (VP16) MOA

Answer 19

Inhibits topoisomerase 2, causing increased DNA degradataion - forms a complex between topoisomerase and 2 and DNA

Question 20

Which antibiotics work like etoposide

Answer 20

Flouroquinolones

Question 21

Etoposide is used for

Answer 21

Small cell carcinoma of the lung and prostate, testicular cancer

Question 22

This drug alkylates DNA and causes pulmonary fiborsis

Answer 22

Busulfan

Question 23

This drug fragments DNA and causes pulmonary fibrosis

Answer 23

Bleomycin

Question 24

This drug blocks purine synthesis, and is metabolized by xanthine oxidase

Answer 24

6-mercaptopurine: antimetabolite

Question 25

This drug cross links DNA and is neprho and oto toxic

Answer 25

Cisplatin, carboplatin, oxaliplatin

Question 26

Nitrogen mustard that alkylates DNA (electrophile that binds DNA)

Answer 26

Cyclophosphamide (DMARD)

Question 27

Folic acid analog that inhibits dihydrofolate reductase

Answer 27

Methotrexate

Question 28

Prevent tubulin dissasembly

Answer 28

Paclitaxel and other taxols P

Question 29

Pyrimidine analog that is bio-activated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase, which decreases dTMP and decreases DNA and protein synthesis

Answer 29

5-FU

Question 30

Intercalates DNA, produces free oxygen radicals, and cardiotoxic

Answer 30

Doxorubicin

Question 31

DNA alkylating agent used in brain cancer

Answer 31

Nitrosureas cross blood brain bar

Question 32

Prevents Tubulin assembly

Answer 32

Vincristine and vinblastine

Question 33

Inhibits thymidylate synthase - leading to decrease nucleotide synthesis

Answer 33

5-FU

Question 34

SERM - blocking estrogen binding receptors

Answer 34

Tamoxifen, raloxifene: antagonist in breat and agonist in bone. tamoxifen may increase the risk of endometrial carcinoma via partial agonist effects - raloxifen is an endometrial antagonists

Question 35

Mechanism similar to antiviral acyclovir and foscarnet

Answer 35

Cytarabine (pyrimidine analog = inhibition of DNA polymerase)

Question 36

Mechanisms similar to flouroquionlones

Answer 36

Etoposide

Question 37

mechanisms similar to trimethoprim

Answer 37

methotrexate (folic acid analog that inhibits dihydrofolate reductase = dec dTMP = dec DNA = dec. protein synthesis

Question 38

monoclonal antibody against HER2 (erb-2)

Answer 38

Trastuzumab

Question 39

Free radical induced DNA strand breakage

Answer 39

Bleomycin, Doxorubicin, Daunorubicin

Question 40

Inhibitor of PRPP synthetase

Answer 40

6-MP: purine thiol analog = dec de novo purine synthesis, activated by HGPRtase

Question 41

Reversible with Leucovorin

Answer 41

Methotrexate

Question 42

Treatment for choriocarcinoma

Answer 42

Methotrexate, vinblastine, vincristine

Question 43

Treatment for AML

Answer 43

Cytarabine

Question 44

Treatment to CLL

Answer 44

Busulfan, Imatinib

Question 45

Prevents breast cancer

Answer 45

tamoxifen and raloxifene

Question 46

Treatment for testicular cancer

Answer 46

"Eradicate Ball Cancer" 1. Etoposide 2. Bleomycin 3. Cisplatin

Question 47

Applied topically for AKs and basal cell cancers

Answer 47

5-FU

Question 48

Treatment for childhood tumors (ewing sarcoma, wilms tumor, rhabdomyosarcoma)

Answer 48

Dactinomcyin

Question 49

Inhibits ribonucleotide reductase

Answer 49

Hydroxyurea: dec DNA synthesis ( s phase specific)

Question 50

Side effect of hemorrhagic cystitis

Answer 50

Acrolein produced by cyclophophamide

Question 51

Antibody against Philadelphia chromsome

Answer 51

Imatinib

Question 52

Side Effects of prednisone

Answer 52

Immunosuppression - osteoporosis - acne - catarcts - cushingoid features - peptic ulcers - hypertension -hyperglycemia - insomnia - psychosis