Week 2: alkylators

Question 1

Name the 5 alkylators

Answer 1

Cyclophosphamide, bendamustine, temozolomide, cisplatin, carboplatin

Question 2

Where is DNA usually alkylated?

Answer 2

N7 of guanine leading to breakage of the glycosidic bond

Question 3

What kind of agents are more effective at creating lesions that are difficult to repair?

Answer 3

Bifunctional agents

Question 4

Are drugs typically nucleophilic or electrophilic?

Answer 4

electrophilic

Question 5

Name 2 nitrogen mustards?

Answer 5

cyclophosphamide, bendamustine

Question 6

Name two platinum compounds

Answer 6

Cisplatin, Carboplatin

Question 7

What is bendamustine used for? Side effect?

Answer 7

B cell malignancies, can cause prolonged neutropenia

Question 8

What drug is the most important cytotoxic drug ever discovered?

Answer 8

Cyclophosphamide

Question 9

What are side effects with cyclophosphamide? How do you treat them?

Answer 9

Acrolein can cause hemorrhages in the stomach and 5q-; treat with MESNa

Question 10

what is the most prescribed cytotoxic drug?

Answer 10

cyclophosphamide

Question 11

What is so great about mustard use in a clinical setting?

Answer 11

Broad therapeutic index without obvious “ceiling” makes them useful for high-dose chemotherapy with stem-cell rescue

Question 12

What is the downside of mustard use?

Answer 12

hemorrhagic cystitis, bladder cancer and myelodysplasia (5q-)

Question 13

What drug class is cisplatin?

Answer 13

Platinum drug

Question 14

T/F: cisplatin is myelosuppressive

Answer 14

False, not very myelosuppressive at all

Question 15

What are the toxicities of cisplatin?

Answer 15

damage to 8th CN and long sensory nerves; kidney damage, nausea and vomiting

Question 16

What is cisplatin used to treat?

Answer 16

germ cell tumors, bladder, head and neck

Question 17

What is carboplatin used to treat?

Answer 17

lung, GYN and breast cancers

Question 18

What is the advantage of carboplatin over cisplatin?

Answer 18

much less neurotoxic, emetogenic and neprotoxic

Question 19

What is the downside of carboplatin?

Answer 19

myelosuppressive, causing thrombocytopenia

Question 20

T/F: cisplatin is unmatched in broad-spectrum anti-cancer activity, and unmatched in toxicity as well

Answer 20

True

Question 21

What is the most important toxicity of platinum drugs?

Answer 21

neuropathy

Question 22

What platinum has the most favorable therapeutic index?

Answer 22

carboplatin

Question 23

What is the number one side effect of oxaliplatin?

Answer 23

causes extreme cold intolerance

Question 24

Where do non-classical alkylators do their thing at?

Answer 24

N7 and O6 of guanine, and A3 on adenine

Question 25

What is temozolomide useful in treating?

Answer 25

CNS tumors

Question 26

What should be checked before treatment with temozolomide?

Answer 26

expression of MGMT which will remove methylation

Question 27

What else can non-classical alkylators be used for?

Answer 27

bone marrow transplant conditioning regimens (very toxic to stem cells)