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Clinical PK > Amiodarone > Flashcards

Amiodarone Flashcards

1
Q

What two formulations can amiodarone be absorbed with?

A

IV and PO

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2
Q

What percent is IV absorbed?

A

100%

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3
Q

Is amiodarone PO absorbed fast or slow?

A

Very slow - incomplete absorption

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4
Q

Is it best to take PO amiodarone with food or without food?

A

With food - it increases the rate of absorption

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5
Q

Where is amiodarone mainly distributed?

A

To lipophilic tissues

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6
Q

(T/F) - Amiodarone has enterohepatic circulation

A

TRUE - long half life

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7
Q

How is amiodarone metabolized?

A

By CYP3A4 in the liver

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8
Q

Does amiodarone inhibit any enzymes and/or transporters?

A

CYP3A4, 2D6, 2C9 and P-gp

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9
Q

Which drugs need to be automatically decreased when amiodarone is concomitantly given with them?

A

Digoxin

Warfarin

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10
Q

By how much percent should digoxin be adjusted when given with amiodarone?

A

Decrease by 50%

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11
Q

By how much percent should warfarin be adjusted when given with amiodarone?

A

Decrease by 25%

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12
Q

Phenytoin is a drug that interacts with amiodarone. What will happen to the levels of amiodarone when given with phenytoin, increase or decrease? By how much percent?

A

Increase by 50%

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13
Q

In which route is amiodarone mainly eliminated/excreted?

A

Biliary

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14
Q

What is the chronic half-life of amiodarone?

A

53 days

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15
Q

What are some factors that can affect the elimination of amiodarone?

A
  • Elderly

- Cirrhosis

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16
Q

The onset of action for amiodarone is when?

A

Variable - 1 to 3 weeks

17
Q

What are the therapeutic levels for amiodarone? Why is it a questionable clinical value?

A

0.5 to 2 mg/mL

It’s questionable because amiodarone does not hang out in the blood as much - it likes fatty tissue

18
Q

What is the loading dose (LD) of amiodarone in an oral formulation? How many grams should it get up to for it to be effective?

A

1.2 to 1.8 g/day - divided doses

10 grams

19
Q

What is the LD of amiodarone in an IV formulation? How many grams should it get up to for it to be effective?

A

5 to 7 mg/kg over 30-60 mins followed by 1.2 to 1.8 g/day

10 grams

20
Q

What is the maintenance dose (MD) of amiodarone?

A

200 to 400 mg/day

21
Q

How is amiodarone IV converted to PO if it has been less than or equal to 1 week of usage?

A

800 to 1600 mg/day for 1-2 weeks then MD 200 to 400 mg/day

22
Q

How is amiodarone IV converted to PO if it has been 1 week to less than 3 weeks of usage?

A

600 to 800 mg/day for 1-2 weeks then MD 200 to 400 mg/day

23
Q

How is amiodarone IV converted to PO if it has been more than 3 weeks of usage?

A

Begin MD 200 to 400 mg/day

24
Q

How is amiodarone PO converted to IV?

A

PO MD will be 30 to 70%

25
Q

What are some cardiac toxicities involved with amiodarone?

A
  • Bradycardia

- AV block or torsades de pointes

26
Q

What factors affect cardiac toxicities of amiodarone in an IV form?

A

Rate and concentration of drug

27
Q

(T/F) - If amiodarone has a concentration > 2 mg/mL, it should be administered in a peripheral line to avoid phlebitis

A

FALSE - in a central line

28
Q

To reduce the risk of cardiac toxicities of amiodarone in an IV form, how should IV be administered?

A

With an IV filter and mixed in glass

29
Q

What are some pulmonary toxicities involved with amiodarone?

A
  • Pulmonary fibrosis
  • Hypersensitivity pneumonitis
  • Pulmonary inflammation
  • Interstitial and alveolar pneumonitis
30
Q

What are some hepatic toxicities involved with amiodarone?

A
  • Transient elevation in LFT (15-30%)

- Clinical hepatitis and cirrhosis (< 3%)

31
Q

What are some thyroid toxicities involved with amiodarone?

A

Hypothyroidism (20%)

Hyperthyroidism (3%)

32
Q

What are some ocular toxicities involved with amiodarone?

A
  • Corneal microdeposits (70-100%)

- Optic neuropathy (< 1%)

33
Q

What are some dermatologic toxicities involved with amiodarone?

A
  • Photosensitivity (25-75%)
34
Q

What tests should be done in patients w/ amiodarone at baseline?

A
  • EKG
  • Pulmonary function tests
  • Chest X-ray
  • LFT
  • Thyroid function
  • Eye exam
35
Q

What tests should be done in patient w/ amiodarone every 6 months?

A
  • LFT
  • Thyroid function
  • Eye exam
36
Q

What tests should be done yearly in patients w/ amiodarone?

A
  • Chest X-ray
  • EKG
  • Pulmonary function tests (if symptoms occur)
37
Q

Is dronedarone a better option than amiodarone?

A

No - causes more potential harm than benefits

Clinical PK (11 decks)

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