Flashcards in Drug Table - DNA Intercalating Agents Deck (34)
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1
DNA Intercalating Agents
General Mechanism
Bind DNA through intercalation between
specific bases, blocking DNA, RNA or both
synthesis; cause DNA strands to break and
interfere with cell replication; CCNS
2
Dactinomycin (Actinomycin D, Cosmegen) Mech
Intercalates G-C base pairs of DNA,
interfering with DNA-dependant RNA
polymerase; also causes ssDNA breaks
3
Dactinomycin (Actinomycin D, Cosmegen) Therapeutics
Pediatric tumors (Wilms' tumor,
rhabdomyosarcoma Ewing's sarcoma);
choriocarcinoma in women
4
Dactinomycin (Actinomycin D, Cosmegen) Imp Side effects
Hematopoietic suppression with
pancytopenia
5
Dactinomycin (Actinomycin D, Cosmegen) Other side effects
Anorexia, nausea, vomiting
6
Daunorubicin (Cerubidine) Class
Anthracyclines
7
Daunorubicin (Cerubidine) Mech
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
8
Daunorubicin (Cerubidine) Therapeutics
AML
9
Daunorubicin (Cerubidine) Imp Side effects
Irreversible dose-dependent
cardiotoxicity; alopecia
10
Daunorubicin (Cerubidine) Other side effects
Myelosuppression
(neutropenia), stomatitis, GI
disturbances
11
Daunorubicin (Cerubidine) Misc
Dexrazoxane is cardio-protective
12
Idarubicin (Idamycin) Class
Anthracyclines
13
Idarubicin (Idamycin) Mech
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
14
Idarubicin (Idamycin) Therapeutics
AML
15
Idarubicin (Idamycin) Imp Side effects
Irreversible dose-dependent
cardiotoxicity; alopecia
16
Idarubicin (Idamycin) Other side effects
Myelosuppression
(neutropenia), stomatitis, GI
disturbances
17
Idarubicin (Idamycin) Misc
Dexrazoxane is cardio-protective
18
Doxorubicin (Adriamicin, Doxil) class
Anthracyclines
19
Doxorubicin (Adriamicin, Doxil) Mech
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
20
Doxorubicin (Adriamicin, Doxil) Therapeutics
Sarcomas, breast and lung carcinomas,
malignant lymphomas
21
Doxorubicin (Adriamicin, Doxil) Imp side effects
Irreversible dose-dependent
cardiotoxicity; alopecia
22
Doxorubicin (Adriamicin, Doxil) Other side effects
Myelosuppression
(neutropenia), stomatitis, GI
disturbances
23
Doxorubicin (Adriamicin, Doxil) Misc
Dexrazoxane can be used to prevent
cardiotoxic effects
24
Epirubicin (Ellence) Class
Anthracyclines
25
Epirubicin (Ellence) Mech
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
26
Epirubicin (Ellence) Therapeutics
Metastatic breast cancer, gastric
cancer
27
Epirubicin (Ellence) Imp side effects
Irreversible dose-dependent
cardiotoxicity; alopecia
28
Epirubicin (Ellence) Other side effects
Myelosuppression
(neutropenia), stomatitis, GI
disturbances
29
Epirubicin (Ellence) Misc
Dexrazoxane can be used to prevent
cardiotoxic effects
30
Bleomycin (Blenoxane) Mech
Acts in G2 phase of cell cycle. Binds to
DNA, producing ss- and dsDNA breaks
31
Bleomycin (Blenoxane) Therapeutics
Combination therapy for testicular
tumors or Hodgkin's disease;
squamous cell carcinomas and
lymphomas
32
Bleomycin (Blenoxane) Imp side effects
Pulmonary toxicity (pulmonary
fibrosis); cutaneous toxicity
(hyperpigmentation,
hyperkeratosis, erythema);
hyperthermia
33
Bleomycin (Blenoxane) Other side effects
Minimally myelo- and
immunosuppressive (often used
in combo therapy); headache,
nausea, vomiting
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