Antibiotics Cancer Flashcards

1
Q

Anthracyclines and Anthracenediones?

A

Doxorubicin, Idarubicin, Daunorubicin, Epirubicin, Valrubicin, and Mitoxantrone
(Do, I, Dance, E,V,M)

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2
Q

Antibitotics

A

Dactinomycin, Bleomycin, Mitomycin

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3
Q

Antineoplastic Antibiotics Vs. Antibitoics?

A

Antineoplastic ABX act on tumerous or cancer cells while the other on bacterial cells.
-Microbial origin

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4
Q

What gives Dactinomycin their biological activity and cytotoxicity?

A

Binding to double-helical DNA

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5
Q

Formation of a Dactinomycin-DNA complex….

A

stability sufficient to block the transcription of DNA by RNA polymerase

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6
Q

Phenoxazone ring intercalates between _____

A

adjacent guanine-cytosine base pairs of DNA

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7
Q

Dactinomycin is much more effective in ______

A

blocking transcription of RNA due to the DNA-dependent RNA polymerases being much more sensitive.

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8
Q

Dactinomycin causes single strand breaks in DNA due to ?

A

Free-radical intermediate (topoisomerase II)

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9
Q

Treatment for Rhabdomyosarcoma and Wilms Tumor in children?

A

Dactinomycin + Vincristine and Cyclophosphamide with surgery and radiotherapy
(Do, Children, Vibe)

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10
Q

Choriocarcinoma treatment?

A

Dactinomycin and MTX
(Chronic——>D, M)

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11
Q

Dactinomycin is extremely _____?

A

corrosive to soft tissues

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12
Q

What are your naturally producing anthracyclines?

A

Idarubicin, Epiruubicin, Doxorubicin, Daunorubicin
(Do, I, Dance, Easy)

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13
Q

Which anthracycline is a semisynthetic analogue of Doxorubicin?

A

Valrubicin

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14
Q

Mitoxatrone is a synthetic anthracenedione derivative of ________?

A

Topoisomerase II Inhibitor

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15
Q

Anthracyclines and Anthreacenediones MOA?

A

Intercalate with DNA, directly affecting transciption (RNA) and replication (DNA)

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16
Q

main important activity of anthracyclines is to?

A

form a heterotrimeric complex with topoisomerase II and DNA

17
Q

What is topoisomerase II for?

A

essential for DNA replication and repair
-produces double strand breaks at the 3’ phosphate backbone, allowing uncoiling of supercoiled DNA)

18
Q

Topoisomerase II + Anthracyclines

A

make a ternary complex which inhibits reliagtion of broken DNA, leading to apoptosis

19
Q

Quinone moieties of anthracyclines can?

A

form radical intermediates that react with O2 to produce superoxide anion radicals, this attacks DNA (oxidizes) and leads to damage and apoptosis

20
Q

Resistance to anthracylcines?

A

-decreased/mutation of topoisomerase II
-Increased glutathione
-Enhanced ability to repair DNA strand breaks

21
Q

Anthracyclines cross the BBB?

A

No they do NOT

22
Q

Anthracyclines cause?

A

Cardiomyopathy (long term) and congestive heart failure (chronic, dose related)

23
Q

Doxorubicin is effective in which cancer?

A

malignant lymphoma when used in combo with other agents

24
Q

Bleomycin MOA?

A

generates free radicals, oxidative damage to the deoxyribose of thymidylate and other nucleotides leading to single and double stranded breaks in DNA

25
Q

Bleomycin radicals?

A

Fe 2+ to oxygen radicals

26
Q

Bleomycin accumulates where in the cell cycle?

A

G2 phase

27
Q

Bleomycin is degraded by?

A

Hydrolase
activity of hydrolase is low in skin and lung (leading to toxcity)

28
Q

Bleomycin resistance is due to ?

A

high levels of hydrolase activity

29
Q

treatment of testicular cancer?

A

Bleomycin + cisplatin and Vinblastine or Etoposide

30
Q

Bleomycin is part of the ABVD regimen for

A

Hodgkin Disease: Adriamycin (Doxorubicin), Bleomycin, Vinblastine, Darcarbazine

31
Q

Bleomycin can be used for local treatment of?

A

bladder cancer
(reduce dose if renal impairment)

32
Q

Mitomycin is part of?

A

family of aziridine containing natural products

33
Q

Mitomycin MOA?

A

Bifunctional or trifunctional alkylating agent
-it inhibits DNA synthesis and cross-links DNA at the N6 position of Adenine and at the O6 and N7 position of guanine, leading to DNA break

34
Q

Mitomycine Adverse effects?

A

Myelosuppression (major), CHF, potentiate cardiotoxicity when used with Doxorubicin

35
Q

Mitomycin usage?

A

superficial transitional cell carcinoma (direct instillation into baldder)
-combo with 5FU and Cisplatin for anal cancer