Common Prodrugs & Their active metabolites Flashcards

1
Q

Codeine

Prodrug

A

Morphine

Active metabolite

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2
Q

Clopidogrel

Prodrug

A

(Active metabolite)

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3
Q

Lisdexamfetamine

Prodrug

A

Dextroamphetamine

Active metabolite

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4
Q

Primidone

Prodrug

A

Phenobarbital

Active metabolite

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5
Q

Capecitabine

Prodrug

A

Fluorouracil

Active metabolite

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6
Q

Fosaprepitant

Prodrug

A

Aprepitant

Active metabolite

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7
Q

Fosphenytoin

Prodrug

A

Phenytoin

Active metabolite

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8
Q

Enalapril

Prodrug

A

Enalaprilat

Active metabolite

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9
Q

Tramadol

Prodrug

A

(Active metabolite)

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10
Q

Valacyclovir

Prodrug

A

Acyclovir

Active metabolite

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11
Q

Valganciclovir

Prodrug

A

Ganciclovir

Active metabolite

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12
Q

Calcifediol

Prodrug

A

Calcitriol

Active metabolite

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13
Q

Colisimethate

Prodrug

A

Colistin

Active metabolite

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14
Q

Isavuconazonium Sulfate

Prodrug

A

Isavuconazole

Active metabolite

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15
Q

Famiciclovir

Prodrug

A

Penciclovir

Active metabolite

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16
Q

Fosamprenavir

Prodrug

A

Amprenavir

Active metabolite

17
Q

Cortisone

Prodrug

A

Cortisol

Active metabolite

18
Q

Predisone

Prodrug

A

Prednisolone

Active metabolite

19
Q

Leflunomide

Prodrug

A

Teriflunomide

Active metabolite

20
Q

Levodopa

Prodrug

A

Dopamine

Active metabolite

21
Q

Codeine, by itself, and in combo products, such as Tylenol #3
What is the safety Consideration?

A
  1. Risk of toxicity with UMs of CYP2D6;
    - higher conversion to morphine
    * *DO NOT USE codeine with UMs of CYP2D6
  2. Risk of poor analgesia with PMs of CYP2D6
    - Use an alternative analgesic in patients identified as PMs of 2D6
22
Q

Clopidogrel (Plavix)

What is the safety consideration?

A
  1. Risk with CYP2C19 inhibitors, which may block conversion to active form:
    * *DO NOT USE with 2C19 inhibitors, including:
    - OMEPRAZOLE
    - ESOMEPROZOLE
  2. Risk with PMs of CYP2C19; low conversion to active form, with reduced effect drug on platelet activity
    - Use alternative P2Y12 inhibitor in patients identified as PMs of 2C19