Chemo Rx

Question 1

CYTOTOXIC Chemotherapeutic agents can be divided into two groups based on their effects at different stages of the cell cycle and have effects on different types of cancer:

Answer 1

1. Cell-cycle specific (CCS): hematologic malignancies, solid tumors high growth fraction
2. Cell-cycle non-specific (CCNS): solid tumors with low or high growth fraction

Question 2

What are the 3 bone-marrow sparing chemotherapy agents?

Answer 2

1. bleomycin
2. cisplatin
3. vincristine

Question 3

Alkylating agents are mutagenic and can lead to _____. Which is the most likely to cause this?

Answer 3

• leukemia
• Procarbazine

Question 4

List the 4 alkylating agents (chemo rx)

Answer 4

1. Cyclophosphamide
2. Procarbazine
3. Cisplatin
4. Carboplatin

Question 5

Which 2 alkylating agents are platinum analogs?

Answer 5

1. cisplatin
2. carboplatin

(-“platin” rx = platinum)

Question 6

The log kill hypothesis says that chemotherapy drugs are ______ kinetics

Answer 6

first order

(3 log kill = 10⁹ -10 ⁶ cancer cells)

Question 7

_______ (3 chemotherapeutic agents) cause pulmonary side effects .

Answer 7

1. Bleomycin
2. Busulfan
3. Procarbazine

(“Bleomycin & Busulfan Block your Breath”)

Question 8

________( 2 chemotherapeutic agents) cause cardiotoxicity.

Answer 8

1. Mitoxantrone (least cardiotoxic)
2. Dexrazoxane (delayed CHF)

Question 9

Which chemo rx cause nephrotoxicity?

Answer 9

1. Cisplatin
2. Methotrexate (Pemetrexed)

Question 10

______ treats nephrotoxicity caused by Cisplatin

Answer 10

Amifostine

Question 11

Side effect shared by vinka alkaloids, -“taxanes” and Procarbazine

Answer 11

neurotoxicity

Question 12

_____ is the chemo rx least likely to cause neurotoxicity

Answer 12

Vinblastine

(does BLAST the Bone marrow though)

Question 13

Hemorrhagic cystitis is an adverse reaction to ________ (chemo rx).

Answer 13

Cyclophosphamide

Question 14

______ is a second generation platinum analog (alkylating agent) and therefore, has less toxicity.

(myelosuppression is the main dose-limiting toxicity)

Answer 14

carboplatin

(second gen. to cisplatin)

Question 15

Neurotoxicity and ototoxicity are the side effects of _______.

Answer 15

cisplatin

(platinum analog - alkylating agent)

Question 16

The MOA for the alkylating agents is the alkyl group forms a _______ leading to DNA strand breakage.

Answer 16

cross-link

(cell-cycle checkpoints will recognize → apoptosis)

Question 17

Hepatic VOD is an adverse effect of the ______ class of chemo rx.

Answer 17

alkylating agents

Question 18

5 Mechanisms of resistance against alkylating agents

Answer 18

1. increase glutathione
2. increase DNA repair
3. decrease permeability to agent
4. degrade rx
5. impair apoptotic pathways

Question 19

Cyclophosphamide is converted into _______ which alkylates DNA → cytotoxicity.

Answer 19

phosphoramide mustard & acrolein

Question 20

Which alkylating agent treats NHL, breast, ovarian, neuroblastoma and leukemia?

Answer 20

cyclophosphamide

Question 21

______ (alkylating agent) makes free radicals and converts CYP into methylating species.

Answer 21

Procarbazine

(inhibits DNA & RNA synthesis)

Question 22

Procarbazine is also a ______ inhibitor.

Answer 22

MAO

(caution w/patients on SSRI/SNRI)

Question 23

______ (alkylating agent) treats Hodgkin and brain tumors

Answer 23

Procarbazine

Question 24

BM suppression, pulmonary toxicity, neurotoxicity are _____ (alkylating agent) side effects

Answer 24

Procarbazine side effects

Question 25

Platinum analogs form intra- and inter-strand cross-links causing cytotoxicity used to treat ________ (5) cancers.

Answer 25

solid tumor: breast, lung, bladder, testicular, ovarian

Question 26

Antimetabolite chemo rx are considered \_\_\_\_(CCS/CCNS)

Answer 26

CCS

Question 27

Antimetabolic chemo rx inhibit DNA and RNA synthesis by interfering with \_\_\_\_\_\_\_\_.

Answer 27

purine or pyrimidine nucleotide precursors

Question 28

\_\_\_\_\_\_\_\_ MOA: inhibits dihydrofolate reductase → decreased thymidylate, purine nucleotides and amino acids.

Answer 28

methotrexate & pemetrexed

Question 29

Decreased rx transport into cell, increased dihydrofolate reductase & decreased sensitivity to rx are the mechanisms of resistance to _______ (antimetabolite chemo rx)

Answer 29

methotrexate & pemetrexed

Question 30

Which 2 antimetabolite chemo rx treat leukemia, lymphoma & breast cancer?

Answer 30

1. methotrexate & pemetrexed 2. mercaptopurine & thioguanine (5-fluorouracil also treats breast cancer)

Question 31

Which antimetabolite chemo rx are pyrimidine ***_antagonists***_ and which are pyrimidine _***analogs_***?

Answer 31

* antagonists: cytarabine, capecitabine * analog: fluorouracil (not to be confused w/the *purine* antagonist: Fludarabine)

Question 32

\_\_\_\_\_\_\_ (antimetabolite chemo rx) is a DNA polymerase inhibitor → terminates chain elongation.

Answer 32

Cytarabine | (tx for AML)

Question 33

Cytarabine is the only antimetabolite chemo rx that treats \_\_\_\_\_.

Answer 33

AML

Question 34

Fluorouracil has no antineoplastic activity, but ***_is converted_*** to \_\_\_\_\_→ inhibits DNA synthesis by inhibiting \_\_\_\_\_. How does it inhibit RNA synthesis?

Answer 34

* 5-FdUMP * thymidylate synthase * conversion to 5-FdUTP

Question 35

Fluorouracil treats solid tumors, such as : (3)

Answer 35

1. breast 2. colon 3. gastric (can cause life-threatening diarrhea)

Question 36

2 Resistance mechanisms of 5-FU

Answer 36

1. increase thymidylate synthase levels 2. increase DPD (dihydropyrimidine) → catabolize 5-FU (pts w/decreased DPD → toxicity)

Question 37

Caution in combo therapy: cisplatin & ______ have a drug interaction

Answer 37

methotrexate

Question 38

Capecitabine is a prodrug that is converted into \_\_\_\_\_\_.

Answer 38

5-FU | (same MOA & target cancers)

Question 39

\_\_\_\_\_\_ is a unique side-effect of Capecitabine (antimetabolite chemo rx).

Answer 39

Hand-foot syndrome | (erythema of hands and feet)

Question 40

\_\_\_\_\_\_ inhibits ribonucleotide reductase → decreasing the pool of nucleotides for DNA synthesis

Answer 40

Gemcitabine (antimetabolite chemo rx) | (must be phosphorylated first)

Question 41

Which antimetabolite chemo rx treats pancreatic, non-small cell lung and bladder cancer?

Answer 41

Gemcitabine

Question 42

Which antimetabolite chemo rx treats low-grade NHL & CLL?

Answer 42

Fludarabine

Question 43

\_\_\_\_\_\_\_\_ (2) are converted to TIMP by HGPRT → blocks purine synthesis

Answer 43

1. Mercaptopurine (6MP) 2. Thioguanine (6TG) (antimetabolite chemo rx)

Question 44

Doses of 6MP must be reduced in patients taking \_\_\_\_\_\_.

Answer 44

allopurinol

Question 45

Skin pigmentation, adrenal insufficiency, and pulmonary fibrosis are side effects of \_\_\_\_\_\_.

Answer 45

Busulfan