Exam 3 from his study guide Flashcards
Amiodarone LD
1.2-1.8 g/d divided doses up to 10 grams
Amiodarone MD
200-400 mg/d
Amiodarone + Warfarin
Decrease dose by 25%
Amiodarone + Dig
Decrease dose by 50%
Amiodarone + HMG-CoA reductase inhibitors
Interactions
Amiodarone + Phenytoin
Increase Phenytoin 50%
Grapefruit juice may increase oral absorption
Separate 2 hours
Drugs that cause QT prolongation
Azoles
Macrolides
FQ
Haloperidol
Drugs that delay AV nodal conduction
Non-DHP CCB
BB
Dig
Amiodarone Absorption
Very slow and incomplete orally (50-70%)
Food increases rate and extent
Has enterohepatic circulation
Amiodarone Distribution
Mainly lipophilic tissues
Tissue concentration 10-400x higher than serum concentration levels
Uses 2 compartment model
Amiodarone Metabolism
Major site: Liver 3A4
Minor sites: 1A2, 2C19, 2D6
Active metabolite: desmethylamiodarone
Amiodarone is a major inhibitor of these enzymes
3A4
2D6
2C9
P-gp in the gut
Amiodarone excretion/elimination
Major route: biliary
Half-life - dependent on time taking amiodarone
-Chronic dosing = 53 day half-life
IV therapy = variable (9-36 days)
Factors that change amiodarone elimination
Cirrhosis
Elderly