Anthracyclines Flashcards

1
Q

What type of drugs are the anthracyclines?

A

CCNS

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2
Q

What are the 3 distinct mechanisms of the anthracyclines?

A
  1. DNA intercalation (DNA cants unwind)
  2. Topisomerase II (-) (prevents resealing of “cut” DNA)
  3. Oxygen based radical (mediated damage of DNA)
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3
Q

What is the main ADR of anthracyclines?

A

Cardiotoxicity

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4
Q

What reaction can lead to cardiotoxicity?

A

Fenton reaction

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5
Q

Where do the anthracyclines tend to distribute to?

A

The heart

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6
Q

What is the chemical trigger to cardiotoxicity?

A

Fe2+

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7
Q

In cells without catalase, what does H2O2 react with? What does it form?

A

Fe2+; highly destructive hydroxyl radical

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8
Q

What are heart muscle cells relatively deficient in?

A

Catalase

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9
Q

What is the risk for cardiotoxicity related to?

A

The cumulative anthracyclines dose a patient receives over their lifetime

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10
Q

What is the lifetime cumulative dose for doxorubicin?

A

450-550 mg/m2

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11
Q

What should you monitor patients for before and after treatment with doxorubicin?

A

LVEF

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12
Q

What may be considered when doxorubicins dose exceeds 300 mg/m2?

A

Chemoprotectant

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13
Q

What is the chemoprotectant that can be given 30 minutes before doxorubicin?

A

Zinecard

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14
Q

What is the MOA of Dexrazoxane?

A

Chelates/neutralizes the Fe2+ chemical trigger in heart muscle cells

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15
Q

What is the boxed warning for anthracyclines?

A

Vesicants: cause skin blistering via extravasation

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16
Q

What type of anthracyclines are not considered vesicants?

A

Liposomal formulations

17
Q

What are liposomal formulations of anthracyclines less toxic to?

A

Cardiac tissue

18
Q

What is the antidote for doxorubicin extravasation?

A

Totect

19
Q

Why aren’t the liposomal formulations toxic to the heart?

A

Less anthracycline is delivered to the heart via a different PK Profile

20
Q

What color are the anthracyclines?

A

RED