DNA intercalating agents Flashcards
What is the mechanism of action of DNA interacalating agents?
bind DNA through intercalation btwn specific bases
- block DNA, RNA synthesis
- Cause DNA strands to break and interferes with replication
Are DNA intercalating agents cell cycle specific or nonspecific?
nonspecific
What is the mechanism of action of Dactinomycin?
- intercalates G-C base pairs of DNA
- interferes with DNA dependent RNA polymerase
- also causes ssDNA breaks
What is Dactinomycin used to treat?
pediatric tumors:
- wilms tumor
- rhabdomyosarcoma
- ewings sarcoma
- choriocarcinoma
What is an important side effect of Dactinomycin?
hematopoietic supression with pancytopenia
Name four anthracyclines?
- daunorubicin
- idarubicin
- doxorubicin
- epirubicin
What is the mechanism of action daunorubicin, idarubicin, doxorubicin, epirubicin?
- intercalate btwn DNA BPs and donate e- to O2 to form superoxide
- superoxide reacts with itself to form H202
- cleaved in the presence of Fe to form OH radical which cleaves DNA
what is daunorubicin used to treat?
AML
What is an important side effect of daunorubicin?
- irreversible dose -dependent cardiotoxicity
- alopecia
What is idarubicin used to treat?
AML
What is doxorubicin used to treat?
- sarcomas
- breast and lung carcinomas
- malignant lymphomas
What drug is given to patients to prevent cardiotoxicity by DNA intercalating agents?
dexrazoxane
What is epirubicin used to treat?
- metastatic breast cancer
- gastric cancer
What is the mechanism of action of bleomycin?
2 copper cheating peptides , Forms free radicals
Is bleomycin cell cycle specific or nonspecific?
Specific - G2
