Topoisomerase Inhibitors Flashcards

1
Q

What do topoisomerase enzymes regulate?

A

The winding states of DNA

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2
Q

When does the winding of DNA occur?

A

During DNA replications and transcription into mRNA

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3
Q

What is the first step for topoisomerase enzymes?

A

Act as molecular scissors and cuts the DNA phosphate backbone

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4
Q

What is the second step for the topoisomerase enzymes?

A

DNA strands pass through the nick or cut in the DNA phosphate backbone

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5
Q

What is the third step for the topoisomerase enzymes?

A

Acts as molecular glue and reseals the DNA phosphate backbone

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6
Q

What step do the topoisomerase inhibitors prevent?

A

Step 3

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7
Q

What is the bacterial type II of topoisomerase called?

A

DNA gyrase

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8
Q

What is the MOA for irinotecan?

A

Topoisomerase I Inhibitor

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9
Q

What is a unique concern with irinotecan?

A

IICS (irinotecan-induced choline this syndrome)

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10
Q

If caught early enough, what would you treat the ADR caused by irinotecan with?

A

Atropine

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11
Q

What is the boxed warning for irinotecan?

A

Diarrhea

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12
Q

If caught later, what would you treat the ADR caused by irinotecan with?

A

Loperamide

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13
Q

What is a distant cousin of morphine?

A

Loperamide

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14
Q

What does the gene UGT1A1 code for?

A

UGT Enzyme

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15
Q

What does the UGT enzyme do?

A

Inactivate/detoxify irinotecan drug phase II drug metabolism

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16
Q

Patients with a mutated and dysfunctional UGT enzyme are at an increase risk of what two things?

A
  1. Diarrhea
  2. Neutropenia
17
Q

Topoisomerase II inhibitors that act at the G2 phase

A

Epipodophylltoxins

18
Q

Etoposide IV

A

TOPSAR

19
Q

What is an ADR of etoposide IV?

A

Infusion rate related hypotension

20
Q

When should you infuse etoposide?

A

Over 30-60 minutes

21
Q

What concentration should you dilute etoposide to?

A

< 0.4 mg/mL

22
Q

What must you avoid when using etoposide?

A

DEHP as a plasticizer

23
Q

When is etopophos used?

A

If the concentration needs to be > 0.4 mg/mL

24
Q

What patients is etopophos useful in?

A

Ones with fluid retention

25
Q

True or false: etopophos does not have concern when using DEHP as a plasticizer

A

True