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Unit 1: Pharm > DNA Intercalating Agents > Flashcards

Flashcards in DNA Intercalating Agents Deck (20)
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1
Q

Name the 5 anthracycline antibiotics. What major mechanistic class do they belong to?

A

Daunorubicin, doxorubicin, epirubicin, idarubicin, and mitoxantrone. DNA intercalating agents.

2
Q

Name the 2 DNA intercalating agents that are not anthracyclines.

A

Dactinomycin/Actinomycin D and Bleomycin

3
Q

Name the DNA intercalating agent that interferes with DNA-dependent RNA polymerase by intercalating G-C pairs.

A

Dactinomycin/Actinomycin D

4
Q

Name the DNA intercalating agent that is derived from copper-chelating peptides and can induce both single- and double-stranded DNA breaks.

A

Bleomycin

5
Q

From what microbe were the DNA intercalating agents derived?

A

Streptomyces

6
Q

What is the common MO for all the “anti-tumor antibiotics”, and are they cell cycle specific?

A

DNA intercalating, CCNS

7
Q

Describe 3 ways DNA intercalating agents fight cancer, without using the word “intercalate”

A

block DNA/RNA synthesis, cause DNA strand breaks, and interfere with cell replication

8
Q

What DNA intercalating agent is used to treat pediatric tumors like Wilms’ tumor, rhabdomyosarcoma, and Ewing’s sarcoma, as well as choriocarcinoma (placenta)?

A

Dactinomycin/Actinomycin D

9
Q

What is a major side effect of treating pediatric tumors with dactinomycin?

A

Hematopoietic suppression with pancytopenia

10
Q

Daunorubicin, doxorubicin/adriamycin, epirubicin, and idarubicin all have what major side effect, and what drug can protect against this effect?

A

Cardiotoxicity; dexrazoxane is cardio-protective

11
Q

What 2 anthracyclines are used only to treat AML?

A

Daunorubicin and idarubicin

12
Q

Which anthracycline has the broadest spectrum of clinical use, including for sarcomas, breast and lung carcinomas, and malignant lymphomas?

A

Doxorubicin

13
Q

What 2 cancers is epirubicin used to treat?

A

Metastatic breast cancer and gastric cancer

14
Q

Name the DNA intercalating anthracycline that has the least cardiotoxicity.

A

Mitoxantrone

15
Q

Epirubicin is used in the combo regimen FEC to treat what kind of cancer?

A

Breast cancer (metastatic)

16
Q

What 2 diseeases is mitoxantrone used to treat?

A

AML and late-stage multiple sclerosis

17
Q

Besides intercalation, what is another mechanism by which the anthracyclines cause DNA damage?

A

They donate electrons to oxygen, forming ROS (reactive oxygen species) like superoxide, hydrogen peroxide, and hydroxyl radicals

18
Q

What are 3 characterically toxic side effects of bleomycin?

A

Pulmonary toxicity (fibrosis), cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema), and hyperthermia

19
Q

In which DNA intercalating agent is myelo- and immunosuppression the least pronounced, making it a good drug to use in combination regimes like PEB and ABVD?

A

Bleomycin

20
Q

Name 3 types of cancer that bleomycin is often used to treat, and the combination regimens associated with 2 of those cancers.

A

Testicular tumor (PEB), Hodgkins lymphoma (ABVD), and squamous cell carcinoma