Amiodarone
Amiodarone
Cordarone, Pacerone, Nexterone (IV)
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Summary
Common uses
Recurrent ventricular fibrillation or hemodynamically unstable VT0, Atrial fibrillation rhythm control (when structural heart disease limits other options)0, Electrical storm / VT storm0
Pharmacy
Starting dose
Oral load 800-1600 mg/d in divided doses for 1-3 weeks, then 600-800 mg/d for 1 month, then 200-400 mg/d maintenance; IV 150 mg over 10 min then 1 mg/min for 6 hours then 0.5 mg/min
Preparations
100, 200, 400 mg tablets; 50 mg/mL IV (with polysorbate 80 in older formulations causing hypotension); 1.5 mg/mL Nexterone IV (PVC-free, lower hypotension risk)
US FDA Max
Oral maintenance 400 mg/d typical; higher in refractory cases
Pharmacology
Routes
Oral, IV
Onset
IV: minutes; oral: weeks to load
Duration
Weeks after discontinuation (extremely long half-life)
Half-life
~58 days (parent); ~61 days (desethylamiodarone, active metabolite)[1]
Bioavailability
~50% (oral; highly variable)[1]
Pregnancy
Generally avoided; fetal goiter/hypothyroidism risk (iodine load). Used only for life-threatening arrhythmia.[citation needed]
Legal status
Purported mechanism
Amiodarone is a multi-class antiarrhythmic with primary class III (K+ channel blocker, prolongs action potential and refractoriness) action plus class I (Na+ channel blocker), class II (β-adrenergic antagonist), and class IV (Ca²⁺ channel blocker) effects.0 Heavily iodinated (37% iodine by weight); cumulative tissue burden underlies the constellation of organ toxicities: pulmonary fibrosis, thyroid (hyper- or hypothyroidism), hepatic, corneal microdeposits, blue-gray skin discoloration (slate-blue, especially sun-exposed), peripheral neuropathy, optic neuropathy. Routine monitoring: TSH, LFTs, CXR/PFTs, ECG (QT). Numerous drug interactions via CYP3A4, CYP2C9, and P-gp inhibition[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Cordarone (amiodarone HCl), Wyeth/Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/018972s055lbl.pdf