Drug Table - DNA Intercalating Agents

Question 1

DNA Intercalating Agents

General Mechanism

Answer 1

Bind DNA through intercalation between
specific bases, blocking DNA, RNA or both
synthesis; cause DNA strands to break and
interfere with cell replication; CCNS

Question 2

Dactinomycin (Actinomycin D, Cosmegen) Mech

Answer 2

Intercalates G-C base pairs of DNA,
interfering with DNA-dependant RNA
polymerase; also causes ssDNA breaks

Question 3

Dactinomycin (Actinomycin D, Cosmegen) Therapeutics

Answer 3

Pediatric tumors (Wilms' tumor,
rhabdomyosarcoma Ewing's sarcoma);
choriocarcinoma in women

Question 4

Dactinomycin (Actinomycin D, Cosmegen) Imp Side effects

Answer 4

Hematopoietic suppression with

pancytopenia

Question 5

Dactinomycin (Actinomycin D, Cosmegen) Other side effects

Answer 5

Anorexia, nausea, vomiting

Question 6

Daunorubicin (Cerubidine) Class

Answer 6

Anthracyclines

Question 7

Daunorubicin (Cerubidine) Mech

Answer 7

Intercalate between DNA base pairs and
donate electrons to O2 to form superoxide;
superoxide reacts with itself to form H2O2 –
> cleaved in the presence of Fe to form OH
radical, which cleaves DNA

Question 8

Daunorubicin (Cerubidine) Therapeutics

Answer 8

AML

Question 9

Daunorubicin (Cerubidine) Imp Side effects

Answer 9

Irreversible dose-dependent

cardiotoxicity; alopecia

Question 10

Daunorubicin (Cerubidine) Other side effects

Answer 10

Myelosuppression
(neutropenia), stomatitis, GI
disturbances

Question 11

Daunorubicin (Cerubidine) Misc

Answer 11

Dexrazoxane is cardio-protective

Question 12

Idarubicin (Idamycin) Class

Answer 12

Anthracyclines

Question 13

Idarubicin (Idamycin) Mech

Answer 13

Intercalate between DNA base pairs and
donate electrons to O2 to form superoxide;
superoxide reacts with itself to form H2O2 –
> cleaved in the presence of Fe to form OH
radical, which cleaves DNA

Question 14

Idarubicin (Idamycin) Therapeutics

Answer 14

AML

Question 15

Idarubicin (Idamycin) Imp Side effects

Answer 15

Irreversible dose-dependent

cardiotoxicity; alopecia

Question 16

Idarubicin (Idamycin) Other side effects

Answer 16

Myelosuppression
(neutropenia), stomatitis, GI
disturbances

Question 17

Idarubicin (Idamycin) Misc

Answer 17

Dexrazoxane is cardio-protective

Question 18

Doxorubicin (Adriamicin, Doxil) class

Answer 18

Anthracyclines

Question 19

Doxorubicin (Adriamicin, Doxil) Mech

Answer 19

Intercalate between DNA base pairs and
donate electrons to O2 to form superoxide;
superoxide reacts with itself to form H2O2 –
> cleaved in the presence of Fe to form OH
radical, which cleaves DNA

Question 20

Doxorubicin (Adriamicin, Doxil) Therapeutics

Answer 20

Sarcomas, breast and lung carcinomas,

malignant lymphomas

Question 21

Doxorubicin (Adriamicin, Doxil) Imp side effects

Answer 21

Irreversible dose-dependent

cardiotoxicity; alopecia

Question 22

Doxorubicin (Adriamicin, Doxil) Other side effects

Answer 22

Myelosuppression
(neutropenia), stomatitis, GI
disturbances

Question 23

Doxorubicin (Adriamicin, Doxil) Misc

Answer 23

Dexrazoxane can be used to prevent

cardiotoxic effects

Question 24

Epirubicin (Ellence) Class

Answer 24

Anthracyclines

Question 25

Epirubicin (Ellence) Mech

Answer 25

Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 -- > cleaved in the presence of Fe to form OH radical, which cleaves DNA

Question 26

Epirubicin (Ellence) Therapeutics

Answer 26

Metastatic breast cancer, gastric | cancer

Question 27

Epirubicin (Ellence) Imp side effects

Answer 27

Irreversible dose-dependent | cardiotoxicity; alopecia

Question 28

Epirubicin (Ellence) Other side effects

Answer 28

Myelosuppression (neutropenia), stomatitis, GI disturbances

Question 29

Epirubicin (Ellence) Misc

Answer 29

Dexrazoxane can be used to prevent | cardiotoxic effects

Question 30

Bleomycin (Blenoxane) Mech

Answer 30

Acts in G2 phase of cell cycle. Binds to | DNA, producing ss- and dsDNA breaks

Question 31

Bleomycin (Blenoxane) Therapeutics

Answer 31

Combination therapy for testicular tumors or Hodgkin's disease; squamous cell carcinomas and lymphomas

Question 32

Bleomycin (Blenoxane) Imp side effects

Answer 32

``` Pulmonary toxicity (pulmonary fibrosis); cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema); hyperthermia ```

Question 33

Bleomycin (Blenoxane) Other side effects

Answer 33

Minimally myelo- and immunosuppressive (often used in combo therapy); headache, nausea, vomiting

Question 34

Bleomycin (Blenoxane) Misc

Answer 34

Dexrazoxane can be used to prevent | cardiotoxic effects