Amiodarone hydrochloride

What is Amiodarone hydrochloride?

• Amiodarone hydrochloride (Nexterone) is an antiarrhythmic agent used for treatment and prophylaxis of ventricular fibrillation (VF) and hemodynamically unstable ventricular tachycardia (VT).

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What are the uses of this medicine?

• Amiodarone hydrochloride (Nexterone) is used for treatment and prophylaxis of ventricular fibrillation (VF) and hemodynamically unstable ventricular tachycardia (VT) in patients refractory to other therapy.

How does this medicine work?

• Amiodarone (a" mee oh' da rone) is an iodinated benzofuran derivative that is a structural analogue of thyroid hormone.
• Amiodarone may interact with thyroid nuclear receptors, but its antiarrhythmic effects are believed to be mediated by its action in blocking membrane ion channels via perturbation of the lipid environment in the membrane bilayer.
• Amiodarone is highly lipophilic and is concentrated in many tissues and cells, including hepatocytes in the liver.
• It has a slow onset of action and a long but variable elimination half life (up to 6 months) and can accumulate in tissues including hepatocytes.
• Amiodarone is highly effective in suppressing ventricular arrhythmias and in maintaining sinus rhythm in patients with atrial fibrillation.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Known hypersensitivity to any of the components of NEXTERONE Premixed Injection, including iodine.
• Cardiogenic shock.
• Marked sinus bradycardia.
• Second- or third-degree atrioventricular (AV) block unless a functioning pacemaker is available.

What drug interactions can this medicine cause?

• Avoid concomitant use with QT Prolonging Drugs (eg: class I and III antiarrhythmics, lithium, certain phenothiazines, tricyclic antidepressants, certain fluoroquinolone and macrolide antibiotics, azole antifungals, halogenated inhalation anesthetic agents).
• Avoid concomitant use with CYP450 Inhibitors (eg: Grapefruit juice, certain fluoroquinolone and macrolide antibiotics, azole antifungals, cimetidine).
• Amiodarone is a substrate for CYP3A and CYP2C8, so inhibitors and inducers affect amiodarone exposure.
• Amiodarone inhibits p-glycoprotein and CYP1A2, CYP2C9, CYP2D6, and CYP3A, increasing exposure to other drugs.

Is this medicine FDA approved?

• Amiodarone was first approved for use in the United States in 1985 and it is still widely used with several million prescriptions written yearly. Approved indications are limited to recurrent ventricular arrhythmias which have not responded to other available antiarrhythmics. Amiodarone is also used off-label for suppression of atrial fibrillation and maintenance of normal sinus rhythm after cardioversion.

How should this medicine be used?

Recommended dosage: The recommended starting dosing regimen is:

• Initial Load: 150 mg in 100 mL infused over 10 minutes
• Followed by: 1 mg/min for 6 hours
• Followed by: 0.5 mg/min thereafter
• For breakthrough episodes of VF or hemodynamically unstable VT, repeat the Initial Load.

Administration:

• NEXTERONE Premixed Injection is available in GALAXY containers as a single-use, ready-to-use, iso-osmotic solution in dextrose for intravenous administration.
• No further dilution is required.
• Discard any unused portion after use.
• Inspect parenteral drug products for particulate matter and discoloration prior to administration, whenever solution and container permit, solution should be clear.
• Visually inspect the container.
• Administer NEXTERONE, whenever possible, through a central venous catheter dedicated to that purpose.
• Use an in-line filter during administration.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection, 1.5 mg/mL (150 mg/100 mL) Premixed in Dextrose
• Injection, 1.8 mg/mL (360 mg/200 mL) Premixed in Dextrose

This medicine is available in fallowing brand namesː

• NEXTERONE

What side effects can this medication cause?

The most common side effects of this medicine include:

• hypotension
• asystole/cardiac arrest/pulseless electrical activity
• VT
• cardiogenic shock

• Other important adverse reactions are torsade de pointes, congestive heart failure, and liver function test abnormalities.

What special precautions should I follow?

• Hypotension, the most common adverse reaction seen with intravenous amiodarone.
• NEXTERONE causes bradycardia and AV block which may require slowing the infusion rate or discontinuing NEXTERONE. In some patients, inserting a pacemaker is required. Have a temporary pacemaker available when treating a patient predisposed to bradycardia or AV block.
• Acute hepatocellular necrosis leading to hepatic coma, acute renal failure, and death has been associated with the administration of intravenous amiodarone. Carefully monitor patients receiving NEXTERONE for evidence of progressive hepatic injury. Consider reducing the rate of administration or withdrawing NEXTERONE if hepatic injury occurs.
• NEXTERONE may cause a worsening of existing arrhythmias or precipitate a new arrhythmia, sometimes leading to fatal outcomes. Correct hypokalemia, hypomagnesemia or hypocalcemia whenever possible before initiating treatment with NEXTERONE. Give special attention to electrolyte and acid-base balance in patients experiencing severe or prolonged diarrhea or in patients receiving concomitant diuretics and laxatives.
• There have been postmarketing reports of acute-onset (days to weeks) pulmonary injury in patients treated with intravenous amiodarone. Monitor for new respiratory symptoms and evaluate appropriately. Obtain a baseline chest X-ray and pulmonary function tests in patients who are expected to be receiving amiodarone chronically.
• Cases of optic neuropathy and optic neuritis, usually resulting in visual impairment, have been reported in patients treated with oral amiodarone or intravenous amiodarone. Perform an ophthalmic examination if symptoms of visual impairment appear, such as changes in visual acuity and decreases in peripheral vision.
• Nexterone inhibits peripheral conversion of throxine (T4) to triiodothyronine (T3) and may cause increased T3 levels, and increased levels of inactive reverse T3 (rT3) in clinically euthyroid patients. Monitor thyroid function prior to treatment and periodically thereafter.
• Amiodarone can cause fetal harm when administered to a pregnant woman. Inform the patient of the potential hazard to the fetus if NEXTERONE is administered during pregnancy or if the patient becomes pregnant while taking NEXTERONE.
• Anaphylactic/anaphylactoid reactions have been reported with intravenous amiodarone including shock (sometimes fatal), cardiac arrest, and the following manifestations: hypotension, tachycardia, hypoxia, cyanosis, rash, Stevens-Johnson syndrome, flushing, hyperhidrosis and cold sweat.
• Infusion site phlebitis has occured in patients receiving intravenous amiodarone.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypotension, cardiogenic shock, bradycardia, AV block, and hepatotoxicity.

Management of overdosage:

• Treat hypotension and cardiogenic shock by slowing the infusion rate or with standard therapy: vasopressor drugs, positive inotropic agents, and volume expansion.
• Bradycardia and AV block may require temporary pacing.
• Monitor hepatic enzyme concentrations closely. Neither amiodarone nor DEA is dialyzable.

Can this medicine be used in pregnancy?

• Amiodarone can cause fetal harm when administered to a pregnant woman.
• Fetal exposure may increase the potential for adverse experiences including cardiac, thyroid, neurodevelopmental, neurological and growth effects in neonate.

Can this medicine be used in children?

• The safety and effectiveness of amiodarone in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• AMIODARONE HYDROCHLORIDE

Inactive ingredients:

• BETADEX SULFOBUTYL ETHER SODIUM
• ANHYDROUS CITRIC ACID
• TRISODIUM CITRATE DIHYDRATE
• ANHYDROUS DEXTROSE
• SODIUM HYDROXIDE
• HYDROCHLORIC ACID
• WATER

Who manufactures and distributes this medicine?

• Baxter Healthcare Corporation

Deerfield, IL

What should I know about storage and disposal of this medication?

• Store at 20° - 25°C (68° - 77°F); excursions permitted to 15° - 30°C (59° - 86°F).
• Protect from light and excessive heat.
• Protect from freezing.
• Use carton to protect contents from light until used.

• Dailymed label info on Amiodarone hydrochloride
• FDA Amiodarone hydrochloride

Amiodarone hydrochloride Resources
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List of antiarrhythmic agents:

• Amiodarone
• Disopyramide
• Dofetilide
• Dronedarone
• Flecainide
• Ivabradine
• Mexiletine
• Procainamide
• Propafenone
• Quinidine