DNA Intercalating Agents

Question 1

dactinomycin general/MOA

Answer 1

DNA intercalating agent
intercalates between G-C base pairs
interferes with RNA polymerase, inhibiting transcription
causes single-strand DNA breaks

Question 2

dactinomycin TU

Answer 2

mainly pediatric tumors - Wilm’s tumor, rhabdomyosarcoma, Ewing’s sarcoma
advanced choriocarcinoma in women

Question 3

dactinomycin Tox

Answer 3

anorexia, nausea, vomiting

hematopoietic suppression with pancytopenia

Question 4

anthracyclines

Answer 4

daunorubicin, doxorubicin, epirubicin, idarubicin

Question 5

anthracycline MOA

Answer 5

intercalate between DNA base pairs

reduced to intermediates that work through free radicals to create strand breaks

Question 6

anthracycline TU

Answer 6

dauno- and idarubicin - used with Ara-C in Tx of AML
doxorubicin - broad clinical spectrum; sarcomas, breast, lung, lymphomas
epirubicin - in combo FEC for breast; gastric

Question 7

anthracycline Tox

Answer 7

dose-dependent cardiomyopathy

neutropenia, stomatitis, alopecia

Question 8

bleomycin MOA

Answer 8

DNA intercalating agent
mixture of 2 peptides from Streptomyces
binds to DNA, induces single and double stranded breaks following oxidation and free radical formation

Question 9

bleomycin TU

Answer 9

in PEB for testicular carcinoma
in ABVD for Hodgkins
also effective against squamous cell carcinoma

Question 10

bleomycin Tox

Answer 10

severe, dose-related pulmonary fibrosis
cutaneous toxicity (hyperpigmentation, hperkeratosis, erythema)
minimally myeolsuppressive
hyperthermia, headache, nausea, vomiting