Cancer Chemotherapeutic- Alkylating Agents

Question 1

Alkylating Agents are:

Answer 1

1) bischlorethylamines
2) nitrosoureas
3) aziridines
4) alkylsulfonate
5) procarbazine, dacarbazine
6) Altretamine
7) Cisplatin, Carboplatin, Oxaliplatin

Question 2

What do alkylating agents do?

Answer 2

add alkyl groups to bases in the DNA, predom on G. They cause either alkylation at the O-6 or N-7 positions of G.

Question 3

Bases that are alkylated to a lesser extent are:

Answer 3

N1, N3 of A and N3 of C

Question 4

Bifunctional alkylating agents can cause…

Answer 4

intra and interstrand crosslinking in DNA

Question 5

Mispairing of bases results in

Answer 5

mutations in replicating DNA

Question 6

N7 alkylation of G could cause…

Answer 6

depurination

Question 7

Resistance to alkylating drugs may be due to:

Answer 7

1) Increased efficiency of DNA repair
2) Decreased cellular permability to drug
3) increased glutathione production
4) increased glutathione S-transferase activity

Question 8

Toxicity is

Answer 8

dose related

Question 9

Toxicity affects:

Answer 9

rapidly proliferating tissues such as: 
bone marrow
GI
reproductive system
hair follicles

Question 10

Emetogenic effect (nausea) can be reduced by

Answer 10

pretreatment with 5HT3 (serotonin) receptor blockers such as ondansetron or granisetron