Tablets. Tablet contains amiodarone hydrochloride 200 mg.
PHARMACODYNAMICS. Rotaritmil is a main representative of class III antiarrhythmic drugs and has antianginal, coronary vasodilative a- and p-blocking effect. Mechanism of amiodarone action is conditioned by block of ionic channels of cardiomyocyte cell membranes (mainly potassium ones), decrease in automaticity of the sinoatrial node and non-competitive inhibition of a- and p-adrenergic activity. Antiarrhythmic action of amiodarone is related to its ability to prolong the action potential and refractory period, and to reduction in excitability of myocardium. Antianginal action of the drug is determined by the decrease in myocardial demand for oxygen (due to heart beat reduction HR and moderate decrease in peripheral resistance) and increase in coronary blood flow due to direct influence on coronary artery smooth muscles. It maintains cardiac output lowering pressure in aorta and peripheral vascular resistance. Absence of negative inotropic effect permits to use Rotaritmil in cardiac insufficiency. PHARMACOKINETICS. After oral administration the drug is slowly absorbed with bioavailability 30-80%. After single dose the highest concentration in blood plasma is achieved in 3-7 hours. Onset of therapeutic action usually takes place in a week. Elimination begins within several days and stable concentration in plasma is achieved within one or several months. Amiodarone is metabolized in liver. It has pharmacologically active metabolite. Amiodarone has long half-life elimination period with large individual variability. Amiodarone is generally eliminated in urine and feces. Excretion in urine is insignificant that allows prescribing the drug in usual doses for patients with renal insufficiency. To obtain the therapeutic effect it is necessary to use initial saturating dose for accumulation of the drug in tissues. Presence of cumulative effect ensures the duration of action within 10-45 days after treatment cessation.
Treatment and prophylaxis of heart rhythm disorders, including arrhythmias resistant to other antiarrhythmic drugs:
ventricular arrhythmias including ventriculartachycardia and ventricularfibrillation; supraventricular paroxysmal tachycardias: documented attacks of recurrent stable supraventricular paroxysmal tachycardia in patients with organic heart diseases; documented attacks of recurrent stable supraventricular paroxysmal tachycardia in patients without organic heart diseases when antiarrhythmic drugs of other classes are inefficient orthere are contraindications fortheiradministration; documented episodes of recurrent stable supraventricular paroxysmal tachycardia in patients with Wolff- Parkinson-White syndrome; atrial fibrillation and atrial flutter;
rehabilitation period after myocardial infarction, if there are evidences of arrhythmic episodes before.
Amiodaron can be used in treatment of rhythm disorders in patients with ischemic heart disease and/or left ventriculardysfunction.
- high sensitivity to the drug components and iodine;
- sick sinus syndrome, atrioventricular heart block of degree I l-l 11 and His bundle block;
- congenital or acquired prolongation of QTinterval;
- severe cardiac insufficiency;
- manifested arterial hypotension, collapse, shock;
- concomitant administration of drugs able to prolong QT interval;
- concomitant administration of MAO inhibitors;
- thyroid gland disfunction (hypo-and hyperthyrosis);
- hypokaliemia, hypomagnesemia;
- age under 18 years old, ll-lll trimester of pregnancy.
DOSAGE AND ADMINISTRATION:
Rotaritmil should be administered orally before the meals with the sufficient quantity of water. Loading dose: in hospital is 600-800 mg daily (up to maximal 1200 mg) up to achieving the summary dose of 10 g. Ambulatory it is from 600 to 800 mg daily up to achieving the summary dose of 10 g (usually within 10-14 days). Maintainance dose: from 100 to 400 mg/daily (3 mg/kg of body weight daily). Amiodarone can be administered in a day or with intervals in administration of 2 days a week. Average therapeutic single dose: 200 mg. Average therapeutic daily dose: 400 mg. Maximal single dose: 400 mg. Maximal daily dose: 1200 mg.
10 tablets in blister.
3 blisters with an enclosed leaflet in a carton box.