Chemotherapy

Question 1

Major categories/ mechanisms of chemotherapy agents? (4)

Answer 1

DNA-damaging agents
- Coss-linking
- Free radical creators

DNA repair inhibitors
- anthracyclines
- topoisomerase inhibitors

Anti-metabolites
- pyramidine, purine antagonists
- anti folates

Anti-tubulin agents
- tubilin binding
- taxanes

Other
- bleomycin, mitomycin

Question 2

Main types of DNA damaging chemotherapy drugs

Answer 2

Alkylating agents
Platinum compounds
Free radicals

Question 3

Main types of Anti-tubulin chemotherapy agents?

Answer 3

Tubulin binding/ Vinka alkaloids (cincristine, vinorelbine)
Taxanes: paclitaxel, docetaxel

Question 4

Main types of anti-metabolite chemotherapy drugs

Answer 4

Pyramidine antagonists
- 5-FU,
- capecitabine,
- cytarabine

Purine Antagonists
- mercaptopurine
- tioguanine

Folic acid antagonists
- methotrexate
- pemetrexed

Question 5

How do alkylating agents work (in chemotherapy)

Answer 5

covalently bind alkyl groups,

major effect is to cross-link DNA

Question 6

Example(s) of alkylating agents?

Answer 6

bendamustine
cyclophosphamide

Question 7

How do platinum compund agents work (in chemotherapy)

Answer 7

cause interstand cross-links of DNA

Question 8

Example(s) of platinum compound agent in chemotherapy?

Answer 8

cisplatin, carboplatin, oxaliplatin

Question 9

How do antimetabolites work (in chemotherapy)?

Answer 9

usually structural analogues of naturally occurring metabolites that interfere with normal synthesis of nucleic acids by falsely substituting purines and pyrimidines in metabolic pathways.

Question 10

Example(s) of Folic Acid antagonists (in chemotherapy)?

Answer 10

methotrexate
pametrexate

Question 11

What is normally given with Folic Acid antagonists?

Answer 11

Folinic Acid.

To rescue normal tissue from the effect of high dose methotrexate.

Question 12

Example(s) of Pyrimidine antagonists (in chemotherapy)?

Answer 12

5-Fluorouracil (5-FU)

Oral capecitabine is metabolized to 5-FU, as is tegafur with uracil.

Question 13

Example(s) of Purine antagonists (in chemotherapy)?

Answer 13

6-mercaptopurine
6-tioguanine

Question 14

Example(s) of Arabinosides (in chemotherapy)?

Answer 14

Cytarabine (used almost exclusively in the treatment of acute myeloid leukaemia)

Question 15

What type of agents are anthracyclines?

Answer 15

Cytotoxic antibodies, (DNA repair inhibitors)

act by intercalating adjoining nucleotide pairs on the same strand of DNA and by inhibiting topoisomerase-II DNA repair

Question 16

What type of agents are vincristine, vinblastine and vinorelbine?

Answer 16

Vinca Alkaloids (Anti-tubulin agents)

Question 17

How do Vinca Alkaloids work (in chemotherapy)

Answer 17

binding to tubulin and inhibiting microtubule formation during mitosis

Question 18

What type of chemotherapy agent is bendamustine and cyclophosphamide?

Answer 18

alkylating agents

Question 19

What type of chemotherapy agent is cisplatin?

Answer 19

platinum compound

Question 20

What type of chemotherapy agent is methetrexane a pametrexate?

Answer 20

Folic Acid antagonists

Question 21

What type of chemotherapy agent is 5-Fluorouracil (5-FU)?

Answer 21

Pyrimidine antagonists

Question 22

What type of chemotherapy agent is 6-mercaptopurine,
6-tioguanine?

Answer 22

Purine antagonists

Question 23

How do arabinosides work (in chemotherapy)? E.g cytarabine

Answer 23

inhibit DNA synthesis by inhibiting DNA polymerase

Question 24

What are the 5 most common chemotherapy side effects?

Answer 24

• CTZ targeted (chemoreceptor trigger zone) -> nausea
• Hair targeted (alopecia)
• Endothelial cells targeted (mucosal lining)
• Myelosuppression
• Ovaries/ gonads targeted

Also fatigue/ chemo brain

Question 25

Folfox combination?

Answer 25

Oxaliplatin, 5-fluorouracil, folinic acid

Question 26

Chemo particularly associated with cardiotoxicity?

Answer 26

anthracyclines (e.g. daunorubicin, doxorubicin, epirubicin)

This is a rare side-effect of chemotherapy and is usually associated with anthracyclines such as doxorubicin;

effects can present as an acute arrhythmia during administration or cardiac failure due to cardiomyopathy after chronic exposure. This effect is dose-related and can largely be prevented by restricting the cumulative total dose of anthracyclines within the safe range

5 FU and its prodrug, capecitabine, can cause cardiac ischaemia.

Question 27

How do taxanes work? (In Chemo)

Answer 27

bind to tubulin dimers and prevent their assembly into microtubules.

(e.g. paclitaxel and docetaxel)

Question 28

Which chemo agents are particularly associated with nausea?

Answer 28

platinum agents

Question 29

Chemo agents particularly associated with skin toxicity?

Answer 29

5-FU, capecitabine and docetaxel

Question 30

Agent to ameliorate severe chemotherapy- and radiotherapy-induced mucositis.

Answer 30

Palifermin (Kepivance), a recombinant keratinocytederived growth factor

Question 31

Particular anti-emetic used in chemotherapy?

Answer 31

Aprepitant, a neurokinin receptor antagonist, is helpful in preventing acute and delayed nausea and vomiting.

used with dexamethasone and a 5-HT 3 antagonist.

Drugs such as cyclizine, olanzapine and levomepromazine, and benzodiazepines, can be used to control persistent nausea.

Question 32

Chemo agents associated with neurotoxicity?

Answer 32

Vinca alkaloids, taxanes and platinum analogues (but not carboplatin).

It is dose-related and cumulative.

Vinca alkaloids, such as vincristine, must never be given intrathecally, as the neurological damage is progressive and fatal.

Question 33

Chemo agents associated with nephrotoxicity?

Answer 33

Cisplatin (but not oxaliplatin or carboplatin), methotrexate and ifosfamide can potentially cause renal damage.

Avoid with hydration

Question 34

Chemo agents associated with sterility?

Answer 34

• alkylating agents
• anthracyclines
• docetaxel

Question 35

Chemo agents particularly associated with secondary malignancies?

Answer 35

The alkylating agents, anthracyclines and epipodophyllotoxins are particularly implicated.