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2nd U1 Pharm > DNA intercalating agents > Flashcards

DNA intercalating agents Flashcards

1
Q

What is the mechanism of action for DNA intercalating agents?

A

Bind DNA through intercalation btwn specific bases–block DNA and/or RNA synthesis

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2
Q

Through which mechanisms does Dactinomycin work?

A

Intercalates G-C base pairs–interfering with DNA-dependent RNA polymerase

Breaks ssDNA

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3
Q

What does Dactinomycin interfere with?

A

DNA dependent RNA polymerase

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4
Q

Dactinomycin is used in the treatment of…

A 
Pediatric tumors
-Wilms tumor
-rhabdomyosarcoma
-Ewings sarcoma
Choriocarcinoma in women
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5
Q

What are the side effects seen with Dactinomycin?

A

Hematopoietic suppression with pancytopenia
Anorexia
N/V

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6
Q

Name the 4 DNA intercalating agents that fall in the anthracycline class

A

Daunorubicin
Idarubicin
Doxorubicin
Epirubicin

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7
Q

The Anthracycline DNA intercalating agents, Daunorubicin, Idarubicin, Doxorubicin, and Epirubicin, all work through the same mechanism. Describe this mechanism…

A

Intercalate btwn DNA base pairs–donate electrons to O2 forming a superoxide–these react forming H2O2—> in presents of Fe will be cleaved to OH radical which cleaves DNA

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8
Q

What two DNA intercalating agents are used in the treatment of AML?

A

Daunorubicin and Idarubicin

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9
Q

Daunorubicin and Idarubicin are both used in the treatment of…

A

AML

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10
Q

What are the side effects seen with the Anthracycline DNA intercalating agents, Daunorubicin, Idarubicin, Doxorubicin, and Epirubicin?

A 
Irreversible dose-dependent cardiotoxicity
Alopecia
Myelosuppression-neutropenia
stomatitis 
GI disturbances
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11
Q

What drug can be given to prevent cardiotoxic effects caused by the Anthracycline DNA intercalating agents, Daunorubicin, Idarubicin, Doxorubicin, and Epirubicin?

A

Dexrazoxane

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12
Q

What intercalating agent acts in G2 phase of the cell cycle–binds to DNA-breaking dsDNA and producing ssDNA?

A

Bleomycin

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13
Q

Which Anthracycline DNA intercalating agent is used to treat sarcomas, breast and lung carcinomas and malignant lymphomas?

A

Doxorubicin

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14
Q

Metastatic breast cancer and gastric cancer are treated with the use of which anthracycline DNA intercalating agent?

A

Epirubicin

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15
Q

Bleomycin is used for combination therapy in what cancers?

A

testicular tumors or Hodgkin’s disease

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16
Q

Which DNA intercalating agent is used in the treatment of squamous cell carcinomas and lymphomas?

A

Bleomycin

17
Q

What are the side effects seen with Bleomycin?

A 
Pulmonary toxicity--pulmonary fibrosis 
Cutaneous toxicity
-Hyperpigmentation
-hyperkeratosis
-erythema 
-hyperthermia
Myelo and immunosuppressive
Headache
N/V

2nd U1 Pharm (11 decks)

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