Plot 3, Billings Way, Oregun Industrial Est, Alausa, Ikeja
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Tel: 234-805-729-2700, 234-803-778-8997
MICRO LABS LIMITED 92, SIPCOT, HOSUR-635 126. INDIA.
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN: A4-8257): Each uncoated tablet contains: Amiodarone Hydrochloride BP 100 mg/200 mg
Pack Size: 3 x 10's
Amiodarone HCl is a benzofuran derivative: 2-butyl-3-benzofuranyl 4-[2-(diethylamino)-ethoxy]-3-5-diiodophenyl ketone, hydrochloride.
Amiodarone Hydrochloride is a member of antiarrhythmic drugs with predominantly class Ill (Vaughan Willlams'classification) effects.
Mechanism of action: The antiarrhythmic effect of Amiodarone HCI may be due to at least two major properties. 1) a prolongation of the myocardial cell-action potential duration and refractory period and 2) non-competitive alpha- and beta-adrenergic inhibition.
Absorption: Following oral administration in man, Amiodarone HCI is slowly and variably absorbed. The bioavailability of Amiodarone HCI is approximately 50%, but varies between 35 and 65% in various studies. Maximum plasma concentrations are attained 3 to 7 hours after a single dose.
Distribution: Amiodarone HCI has a very large but variable volume of distribution, averaging about 60 L/kg because of extensive accumulation in various sites, especially adipose tissue and highly perfused organs, such as the liver, lung, and spleen.
Metabolism: One major metabolite of Amiodarone HCI, desethylamiodarone, has been identified in man.
Elimination: The main route of elimination is via hepatic excretion into bile, and some enterohepatic recirculation may occur.
INDICATIONS AND USES:
Amiodarone HCI is mainly indicated in life threatening recurrent ventricular arrhythmias.
1. Recurrent ventricular fibrillation. 2. Recurrent hemodynamically unstable ventricular tachycardia.
Amiodarone HCI is contraindicated in severe sinus-node dysfunction, causing marked sinus bradycardia; second and third-degree atrioventricular block; and when episodes of bradycardia have caused syncope (except when used in conjunction with a pacemaker). Amiodarone HCI is contraindicated in patients with a known hypersensitivity to the drug.
PRECAUTIONS AND WARNINGS:
Impairment of Vision: Corneal micro-deposits appear in the majority of adults treated with Amiodarone HCI.
Photosensitivity: Amiodarone HCI has induced photosensitization in about 10% of patients. Some protection may be afforded by the use of sun-barrier creams or protective clothing.
Thyroid Abnormalities: Amiodarone HCI may cause increased thyroxine levels. If any new signs of arrhythmia appear, the possibility of hyperthyroidism should be considered.
Pediatric use: The safety and effectiveness of Amiodarone HCI in children have not been established. Amiodarone HCI is intended for use only in patients with the indicated life-threatening arrhythmias because its use is accompanied by substantial toxicity. Amiodarone HCI has several potentially fatal toxicities, the most important of which is pulmonary toxicity.
Even in patients at high risk of arrhythmic death, in whom the toxicity of Amiodarone HCI is an acceptable risk; amiodarone HCI poses major management problems that could be life-threatening in a population at risk of sudden death, so that every effort should be made to utilize alternative agents first.
Digitalis: Administration of Amiodarone HCI to patients receiving digoxin therapy regularly results in an increase in the serum digoxin concentration that may reach toxic levels with resultant clinical toxicity.
Anticoagulants: Potentiation of warfarin-type anticoagulant response is almost always seen in patients receiving Amiodarone HCI and can result in serious or fatal bleeding.
USE IN PREGNANCY AND LACTATION:
Amiodarone HCI should be used during pregnancy if the potential benefit to the mother justifies the unknown risk to the fetus. When Amiodarone HCI therapy is indicated, the mother should be advised to discontinue nursing.
Neurologic problems are extremely common, including malaise and fatigue, tremor and involuntary movements and peripheral neuropathy, gastrointestinal complaints, as vomiting, constipation, and anorexia. Rarely hepatitis may occur.
Endocrine: Testicular swelling and gynecomastia in the male; breast enlargement and galactorrhea in the female
Dosage & Administration
DOSAGE AND ADMINISTRATION:
For Life-Threatening Ventricular Arrhythmias, such as Ventricular Fibrillation or Hemodynamically Unstable Ventricular Tachycardia: Close monitoring of the patients is indicated during the loading phase, particularly until risk of recurrent ventricular tachycardia or fibrillation has abated.
Loading doses of 800 to 1,600 mg/day are required for 1 to 3 weeks (occasionally longer) until initial therapeutic response occurs. When adequate arrhythmia control is achieved, or if side effects become prominent, Amiodarone HCI dose should be reduced to 600 to 800 mg/day for one month and then to the maintenance dose, usually 400 mg/day.
OVERDOSAGE, SYMPTOMS AND ANTIDOTE:
There have been few reported cases of Amiodarone HCI overdose in which 3 to 8 grams were taken. There were no deaths or permanent sequelae. In addition to general supportive measures, the patient's cardiac rhythm and blood pressure should be monitored, and if bradycardia ensues, a beta adrenergic agonist or a pacemaker may be used.
STORAGE: Store below 30°