Chapter 38: Pharm of Cancer

Question 1

This drug inhibits thymidylate synthase, thus decreasing availability of dTMP = “thymineless death”

Answer 1

Fluorouracil (5-FU)

Question 2

What is the orally available prodrug of 5-FU?

Answer 2

Capecitabine

Question 3

GI cancers, breast cancer, skin cancer like basal cell carcinoma can be treated by this inhibitor of thymidylate synthase….

Answer 3

5-FU

Question 4

What are the major adverse effects of 5-FU?

Answer 4

myelosuppression

photosensitivity

(atherosclerosis, cerebellar syndrome, vision changes, alopecia, GI probs)

Question 5

6-MP effectiveness and toxicity is increased by ______?

Answer 5

allopurinol

Question 6

6-MP MOA?

Answer 6

inhibit IMP dehydrogenase to prevent formation of GMP/AMP by IMP

Question 7

6-MP and Azathioprine have the same MOA - which one is used mainly for immunosuppression and which is used mainly for ALL/AML?

Answer 7

Immunosupression - azathioprine

ALL/AML - 6-MP

Question 8

What drug inhibits ribonucleotide reductase? (thus decreasing DNA synthesis…S phase specificty)

Answer 8

Hydroxyurea

Question 9

What does hydroxyurea do in the treatment of sickle cell disease?

Answer 9

increases HbF

Question 10

Drug used in the treatment of myeloprolierative disorders like essential thrombocytosis or polycythemia vera

Answer 10

hydroxyurea

Question 11

What are the major adverse effects of hydroxyurea?

Answer 11

myelosuppression

GI disturbance

Question 12

MOA of cyclophosphamide

Answer 12

covalently binds DNA…

directly modify DNA structure - alkylating agent

Question 13

What are the major adverse effects of cyclophosphamide?

Answer 13

Myelosuppression, hemorrhagic cystitis (BLADDER!!!)

Question 14

An alkylating agent that is one of the most versatile nitrogen mustards in clinical use. It is a prodrug that must be first activated by hepatic P-450 to produce its active metabolites.

Answer 14

Cyclophosphamide

Question 15

What potentiates the action of 5-FU?

Answer 15

Folinic acid

Question 16

Super versatile, broad spectrum agent used to treat autoimmune disease, leukemias, lymphomas, mycosis fungoides, neuroblastoma, malignant histiocytosis, and more.

Answer 16

cyclophosphamide

Question 17

Alkylating agent that directly binds DNA and is used for the treatment of brain cancer

Answer 17

Carmustine

Question 18

Agents that cross link intra-strand guanine bases used in the tx of genitourinary cancers (including testicular), lung cancer….

Answer 18

Cisplatin

Carboplatin

Question 19

What are the major adverse effects of cisplatin and carboplatin? Which of these is exclusive to cisplatin?

Answer 19

Myelosuppresion, peripheral neuropathy, ototoxicity, nephrotoxicity

Nephrotoxicity - cisplatin only

Question 20

How do you limit the nephrotoxicity of cisplatin?

Answer 20

co admin with amifostine

Question 21

Bleomycin MOA?

Answer 21

Binds oxygen and chelates iron ….binds DNA –> STRAND BREAKS via generating oxidative intermediates

Question 22

What is the dose limiting side effect of bleomycin?

Answer 22

pulmonary fibrosis

irreversible

Question 23

What types of cancers is bleomycin used to treat? Why?

Answer 23

Potentially curable cancers because pulmonary fibrosis effect can be so bad

testicular cancer, hodgkins disease, non hodg lymphoma, squamous cell carcinoma

Question 24

Doxorubicin and daunorubicin made adverse effect? MOA?

Answer 24

heart failure

inhibit top II - G2 phase of cell cycle

Question 25

What top I inhibitor can cause life threatening diarrhea?

Answer 25

TECANS - irinoTECAN topoTECAN

Question 26

In giving doxorubicin to a pt with hepatic dysfxn, what must you keep in mind?

Answer 26

reduce dosing bc drug is excreted in bile

Question 27

Vinblastine MOA and dose limiting effect?

Answer 27

binds tubulin subunits and prevents microtubule polymerization bone marrow suppression is dose limiting

Question 28

Vincristine MOA and dose limiting effect?

Answer 28

binds tubulin subunits and prevents microtubule polymerization peripheral neuropathy is dose limiting

Question 29

Which drugs come from the peri-winkle plant?

Answer 29

vincristine & vinblastine

Question 30

What drug inhibits microtubule DEpolymerization? What is this drug's dose limiting effect?

Answer 30

paclitaxel peripher neuropathy - stocking/glove sensory loss

Question 31

AIDS related Kaposi sarcoma can be treated by this drug that comes from a western yew tree

Answer 31

paclitaxel