ალიმენტური ტრაქტი და მეტაბოლიზმი
სისტემური გამოყენების ინფექციის საწინააღმდეგო
სისხლი და სისხლ-წარმომქმნელი ორგანოები
სამომავლოდ დაგეგმილი პროდუქტები
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
- 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.