Amiodarone HCL

---

Product Name :	Amiodarone HCL
Specs :	USP/BP/EP
Cas No.：	19774-82-4
Product Serie：	Cardiovascular & Blood System Drug
Product  Details ：	Molecular Formula: C25H29I2NO3.HCl;C25H30ClI2NO3    Molecular Weight: 681.78

Back      Home

Overview

Belonging to Class III antiarrhythmics, it acts as a multi-channel blocker, inhibiting sodium, potassium, calcium channels, and α/β-adrenergic receptors, thereby prolonging the cardiac action potential duration. This white to off-white crystalline powder is soluble in methanol, slightly soluble in water, and stable under controlled room temperature, making it a cornerstone in treating life-threatening ventricular and supraventricular arrhythmias.

Features

Electrophysiological Actions:

K⁺ Channel Blockade: Primarily inhibits delayed rectifier K⁺ currents (IKr, IKs), prolonging QT interval and effective refractory period, suppressing reentrant arrhythmias.

Non-Competitive α/β-Blockade: Reduces sympathetic tone, useful in catecholamine-mediated arrhythmias, with minimal negative inotropy due to preserved calcium channel activity.

Pharmacokinetic Properties:

Lipophilicity: High lipid solubility (log P = 6.1) leads to extensive tissue distribution (volume of distribution >1000 L), slow onset (clinical effects in 2-3 days), and long half-life (50-60 days), requiring loading doses (800-1600 mg/day) for rapid stabilization.

Hepatic Metabolism: Metabolized by CYP3A4 to desethylamiodarone (active metabolite, half-life 70 days), with 35% excreted in bile (non-renal elimination), ideal for patients with renal impairment.

Therapeutic Advantages:

Broad-Spectrum Efficacy: Effective against atrial fibrillation (AF), ventricular tachycardia (VT), and Wolff-Parkinson-White syndrome, with >80% success in converting AF to sinus rhythm in acute settings.

Low Proarrhythmic Risk: Compared to other Class III agents (e.g., sotalol), it has a lower incidence of torsades de pointes (0.5-1%), attributed to its unique channel-blocking profile.

Applications

Cardiac Arrhythmia Management:

Atrial Fibrillation: First-line for persistent AF (rate control and rhythm conversion), particularly in patients with heart failure (e.g., AMIODARONE in AF trial showed 69% sinus rhythm maintenance at 1 year).

Ventricular Arrhythmias: Used in life-threatening VT/VF (e.g., post-MI, congenital long QT syndrome), often as a bridge to defibrillator implantation.

Post-Operative Arrhythmias: Prophylactic use in cardiac surgery reduces AF incidence by 30-50%, improving post-op outcomes.

Off-Label Uses:

Thyroid Disorders: Investigated for Graves' disease due to iodine content, though restricted by potential thyroid dysfunction (5-10% incidence of hypo/hyperthyroidism).

Cancer Therapy: Preclinical studies suggest anti-angiogenic effects via VEGFR inhibition, though clinical trials remain in early stages.

Safety and Handling

Requires baseline thyroid function tests (TSH, free T4) and LFT monitoring due to iodine-induced thyroiditis and hepatotoxicity risks. Our product meets ICH Q1A stability guidelines, with a shelf life of 36 months when stored at 20-25°C, and complies with USP <797> for sterile compounding in IV formulations.