Chemotherapy III Antitumor Agents

Question 1

Doxorubicin MOA

Answer 1

Intercalation between base pairs of DNA leading to strand breaks due to inhibition of topoisomerase II

Question 2

Doxorubicin SE

Answer 2

• Cardiac toxicity : congestive cardiomyopathy.
• Nausea and vomiting and hair loss, stomatitis.
• Myelosuppression is dose limiting toxicity.

Question 3

Topoisomerase I

Answer 3

Single strand DNA breaks: relaxation of the strand and re-anneal the strands.

Question 4

Topoisomerase II

Answer 4

Double strand breaks in the DNA: relaxation and re-anneal the strands of DNA.

Question 5

Doxorubicin Indications

Answer 5

Breast cancer, leukemia, sarcoma, Hodgkin’s and Non- Hodgkin’s lymphoma

Question 6

What is thought to be the mechanism behind cardiotoxicity of doxorubicin?

Answer 6

Free radical damage

Question 7

Irinotecan MOA

Answer 7

Topoisomerase I inhibition leading to single strand breaks in the DNA.

Question 8

Irinotecan SE

Answer 8

• Nausea, vomiting and myelosuppression (dose limiting), stomatitis and hair loss
• Early cholinergic diarrhea
• Late secretory diarrhea

Question 9

Irinotecan Indications

Answer 9

GI tract cancers

Question 10

Bleomycin MOA

Answer 10

Binds to DNA, free radical production leading to single and double strand DNA breaks. The bleomycin-iron form is the active species.

Question 11

Bleomycin SE

Answer 11

Pulmonary toxicity is a cumulative toxicity

Question 12

Bleomycin Indications

Answer 12

Testicular cancer

Question 13

What phase of the cell cycle does bleomycin act in?

Answer 13

G2-M phase

Question 14

What are the uses of prednisone in chemotherapy?

Answer 14

Prednisone in high doses for lymphoma and multiple myeloma

Question 15

What is the use of tamoxifen in chemotherapy?

Answer 15

It can be used to treat and prevent breast cancer

Question 16

Anastrozole Indications

Answer 16

Hormone receptor positive breast cancer

Question 17

Flutamide MOA

Answer 17

Flutamide inhibits the uptake and binding of the testosterone to specific receptors in hormonally sensitive prostate cancer cells

Question 18

Flutamide Indications

Answer 18

Metastatic Prostate Cancer

Question 19

Leuprolide MOA

Answer 19

GnRH agonist that leads to inhibition of LH and FSH via negative feedback

Question 20

Leuprolide Indications

Answer 20

Prostate cancer

Question 21

What confers multi drug resistance to topoisomerase II inhibitors and tubular inhibitors?

Answer 21

P glycoprotein efflux pump

Question 22

How is doxorubicin eliminated?

Answer 22

Via bile - dose must be reduced in jaundice

Question 23

What infusion times are more cardiotoxic for doxorubicin?

Answer 23

Shorter times

Question 24

What is the max lifetime dose of doxorubicin?

Answer 24

400 mg/m^2

Question 25

What should be avoided with bleomycin administration?

Answer 25

Do NOT co-administer high concentration oxygen