Amiodarone 200mg tab 30 pc

Description

Composition
Active substance:
1 tablet contains: amiodarone hydrochloride – 200 mg ;.
Excipients:
Ludipress (lactose monohydrate, povidone K30 (Kollidon 30), crospovidone (Kollidon CL)) – 204,2 mg, potato starch – 8.4 mg magnesium stearate – 4.2 mg colloidal silicon dioxide (Aerosil) – 4,2 mg.
Description:
Tablets white or white with kremovatam color ploskotsilindricheskoy forms with the mark and chamfered.
Product form:
Tablets of 200 mg.
10 tablets in blisters.
3 blisters together with instructions for use in a pack.
Contraindications
Increased sensitivity to the drug (including to iodine), sick sinus syndrome (sinus bradycardia, sinoatrial block), in the absence of an artificial pacemaker (risk of cardiac sinus), atrioventricular block II-III degree and di- and Three-beam blockade (without pacemaker), cardiogenic shock, collapse, hypotension, age 18, lactose intolerance, lactase deficiency, glucose-galactose malabsorption, refractory hypokalemia, hypomagnesemia, hypothyroidism, g ipertireoz, interstitial lung disease, congenital or acquired lengthening the interval QT, simultaneous reception of monoamine oxidase inhibitors, pregnancy, lactation.
Simultaneous administration of the drug, prolongs QT interval, and causes paroxysmal tachycardia, a polymorphic ventricular including type “pirouette”: antiarrhythmic drugs of class IA (quinidine, gidrohinidin, disopyramide, procainamide), III class (dofetilide, ibutilide, bretylium tosylate), sotalol; bepridil, vincamine, phenothiazines (Chlorpromazine, tsiamemazin, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultopride, sulpiride, tiapride, veraliprid), butyrophenones (droperidol, haloperidol), sertindole, pimozide; tricyclic antidepressants (doxepin, amitriptyline), maprotiline, cisapride, macrolides (erythromycin / in, spiramycin), azoles, antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, Lumefantrine); pentamidine (parenteral), difemanila methylsulfate, mizolastine, astemizole, terfenadine, fluoroquinolones (including moxifloxacin).
Carefully
Caution should be exercised when using the drug in patients with chronic heart failure (III-IV functional class NYHA classification), atrioventricular block I degree, liver failure, asthma and older (high risk of severe bradycardia).
Dosage
200 mg
Indications
Prevention of relapse of paroxysmal arrhythmias: life-threatening ventricular arrhythmias (including ventricular tachycardia, ventricular fibrillation), supraventricular arrhythmias (including the organic heart disease, and also after failure or inability other antiarrhythmic therapy associated with WPW- syndrome), fibrilloflutter.
Prevention of sudden death due to arrhythmia in patients at high risk: patients with recent myocardial infarction with ventricular extrasystoles amount of more than 10 / h, clinical signs of congestive heart failure and left ventricular ejection fraction less than 40%.
Interaction with other drugs
Contraindicated in combination:
– antiarrhythmic drugs of class IA (quinidine, gidrohinidin, disopyramide, procainamide), III class (dofetilide, ibutilide, bretylium tosylate), sotalol; bepridil, vincamine, phenothiazines (Chlorpromazine, tsiamemazin, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultopride, sulpiride, tiapride, veraliprid), butyrophenones (droperidol, haloperidol), sertindole, pimozide; tricyclic antidepressants (doxepin, amitriptyline), maprotiline, cisapride, macrolides (erythromycin / in, spiramycin), azoles, antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, Lumefantrine); pentamidine (parenteral), difemanila methylsulfate, mizolastine, astemizole, terfenadine, fluoroquinolones (including moxifloxacin), as increases the risk of ventricular tachycardia type “pirouette”.
Deprecated combination:
– beta-blockers, some blockers “slow” calcium channel blockers (verapamil, diltiazem), there is a risk of disturbance of automatism (severe bradycardia) and conduction.
– with laxatives, which may cause hypokalemia, as it increases the risk of ventricular tachycardia type “pirouette”.
Combinations in which care should be taken:
– diuretics causing hypokalaemia, amphotericin B (w / w), systemic glucocorticosteroids, tetrakozaktid – risk of ventricular arrhythmias, including ventricular tachycardia type “pirouette”;
– procainamide – the risk of side effects procainamide (amiodarone, procainamide increases the plasma concentration and its metabolite N-acetylprocainamide);
– indirect anticoagulants (warfarin) – amiodarone increases the concentration of warfarin in the blood plasma (risk of bleeding) due to the inhibition of isoenzyme CYP2C9; cardiac glycosides – a violation of automatism (severe bradycardia) and conduction atriventrikulyarnoy (increase digoxin plasma concentrations);
– esmolol – violation contraction, automaticity and conduction (suppression of compensatory reactions of the sympathetic nervous system);
– phenytoin, fosphenytoin – the risk of developing neurological disorders (amiodarone increases the concentration of phenytoin in plasma due to the inhibition of isoenzyme CYP2C9);
– flecainide – amiodarone increases its concentration in blood plasma (by inhibiting the isozyme CYP2D6);
– drugs metabolized with isoenzyme CYP3A4 (cyclosporine, fentanyl, lidocaine, tacrolimus, sildenafil, midazolam, triazolam, dihydroergotamine, ergotamine, HMG-CoA reductase) – amiodarone increases their concentration in the blood plasma (the risk of toxicity and / or enhance the pharmacodynamic effects);
– Orlistat reduces the concentration of amiodarone and its active metabolite in plasma;
– clonidine, guanfacine, cholinesterase inhibitors (donepezil, galantamine, rivastigmine, tacrine, ambenonium chloride, pyridostigmine, neostigmine), pilocarpine – the risk of bradycardia;
– cimetidine, grapefruit juice slows down the metabolism of amiodarone and increase its concentration in the blood plasma;
– drugs for inhalation anesthesia – the risk of bradycardia (atropine-resistant), reducing blood pressure, conduction abnormalities, decrease cardiac output, acute respiratory distress syndrome, including fatal, the development of which is associated with high oxygen concentrations;
– radioactive iodine – amiodarone (contains iodine in its composition) may interfere with the absorption of radioactive iodine, which can distort the results of radioisotope studies of the thyroid gland;
– drugs rifampin and Hypericum perforatum (powerful inductors isoenzyme CYP3A4) reduce the concentration of amiodarone in blood plasma;
– HIV protease inhibitors (inhibitors isoenzyme CYP3A4) may increase the amiodarone concentration in blood plasma;
– klopodogrel – may reduce its concentration in blood plasma;
– Dextromethorphan (substrate isoenzymes CYP2D6 and CYP3A4) – may increase its plasma concentration (amiodarone inhibit CYP2D6 isozyme);
– while the use of drugs lithium may develop hypothyroidism;
– while the use of colestyramine decreases amiodarone concentration in blood plasma as a result of its binding to colestyramine and reduced absorption from the gastrointestinal tract;
– while the use of the drug cotrimoxazole possible deterioration of intraatrial conduction.
Overdose
In case of toxicity in the form of pro-arrhythmogenic effect drug overturned.
Symptoms of sinus bradycardia, arrhythmia, atrioventricular block, ventricular tachycardia, paroxysmal tachycardia type “pirouette”, worsening of existing chronic heart failure, liver dysfunction, cardiac arrest.
Treatment: gastric lavage and administration of activated charcoal, if the drug has recently passed (1-2 hours from the time of admission). When tachycardia type “pirouette” – intravenous magnesium salts pacing. Otherwise symptomatic therapy. No specific antidote, hemodialysis is not effective, amiodarone and its metabolites are not removed by dialysis. With the development of bradycardia possible appointment of atropine, beta1-agonists, in severe cases – pacing.
pharmachologic effect
Pharmacological group:
Antiarrhythmics.
Pharmacodynamics:
Class III antiarrhythmic drug (an inhibitor of repolarization). It has also antianginal, vasodilatig, alpha- and beta-adrenoceptor blocking, thyrotropin and antihypertensive action.
Antiarrhythmic effect due to the influence on electrophysiological processes of the myocardium; prolongs the action potential of cardiomyocytes; increases the effective refractory period of the atrial, ventricular, atrioventricular (AV) node, bundle of Hiss and the Purkinje fibers, additional ways of excitation. Blocking “fast” sodium channel has effects characteristic for class I antiarrhythmics. Inhibits slow (diastolic) depolarization of the membrane of the sinus node cells, inducing bradycardia and decreased AV conduction.
Antianginal effect caused koronarorasshiryayuschee and antiadrenergicheskim effect, decreasing myocardial oxygen demand. It has an inhibiting effect on alpha- and beta-adrenergic receptors of the cardiovascular system (without their complete blockade). It reduces sensitivity to hyperstimulation of the sympathetic nervous system, the resistance of coronary vessels; increases coronary blood flow; slows the heart rate; It increases the energy reserves of the myocardium (by increasing the content kreatinsulfata, adenosine and glycogen).
In its structure is similar to the thyroid hormones. The iodine content is about 37% of its molecular weight. Influences the metabolism of thyroid hormones, inhibits the conversion of T4 to TOR (block thyroxine-5-deiodinase) and blocks the capture of these hormones cardiocytes and hepatocytes, which leads to a weakening of the stimulating effect of thyroid hormones on the myocardium (TK deficiency can lead to hyperproduction and hyperthyroidism). The onset of action (even using “stress” doses) – from 2-3 days to 2-3 months, the duration of action ranging from several weeks to months (as determined in the blood plasma during the 9 months following the termination of his reception).
Pharmacokinetics:
Absorption Slow and variable – 30-50% bioavailability – 30-50%. Maximum plasma concentration (Cmax) observed after 4-7 hours. The range of therapeutic plasma concentration – 1-2.5 mg / L (but in determining the dose should be borne in mind and the clinical picture). The time to reach an equilibrium concentration in plasma – from one to several months. The volume of distribution – 60 liters, indicating the intensity distribution in the tissue. It has high lipid solubility, high concentrations stored in fatty tissue and organs with a good blood supply (concentration in adipose tissue, liver, kidney, myocardium than in plasma – respectively 300, 200, 50 and 34 times). Pharmacokinetics of amiodarone necessitate the use of the drug in high doses load. Penetrates the blood-brain barrier (BBB) ​​and placenta (10-50%), is secreted from breast milk (25% of the dose received by the mother). Communication with plasma proteins – 95% (62% – with albumin, 33.5% – with the beta-lipoproteins). It is metabolized in the liver, is an inhibitor of isozyme CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver. The major metabolite – dezetilamiodaron – a pharmacologically active and can enhance the antiarrhythmic effect of a basic compound. Possibly also by deiodination (at a dose of 300 mg is released about 9 mg of elemental iodine). Prolonged treatment concentration of iodine may reach 60-80% of amiodarone concentrations.
Given the ability to cumulation and related greater variability of pharmacokinetic parameters, data on half-life (T1 / 2) are contradictory. Excretion after oral administration of amiodarone is carried out in two phases: the initial period – 4-21 h, during the second phase, the T1 / 2 – 25-110 days. After prolonged oral average T1 / 2 – 40 days (this is important when selecting a dose, as may be necessary, at least one month in order to stabilize the new plasma concentrations, while complete removal might last for more than 4 months ).
Excreted in the bile (85-95%), kidneys displayed less than 1% of an oral dose (therefore with impaired renal function is not required in changing dosing). Amiodarone and its metabolites do not undergo dialysis.
Pregnancy and breast-feeding
Amiodarone is contraindicated during pregnancy, but for health reasons Amiodarone can be used if the expected benefit to the mother outweighs the potential risk to the fetus.
Amiodarone is excreted in breast milk in significant amounts, and the drug is contraindicated for use during lactation.
Conditions of supply of pharmacies
On prescription.
side effects
Frequency: very frequently (10% or more), often (1% or more, less than 10%), rare (0.1% or more, less than 1%), rare (0.01% or more, less than 0.1 %), very rarely (less than 0.01%, including some cases), the frequency is not known (from the available data rate can not be determined).
With the cardiovascular system: often – moderate bradycardia (dose-dependent); infrequently – sinoatrial and atrioventricular block of various degrees, proaritmogennoe action (the emergence of new or worsening of existing arrhythmias, including cardiac arrest); very rarely – bradycardia, sinus arrest (in patients with sinus node dysfunction and elderly patients); frequency is unknown – the progression of chronic heart failure (with prolonged use).
From the digestive system: very often – nausea, vomiting, decreased appetite, dulling or loss of taste, feeling of heaviness in the epigastric pain, isolated increased activity of “liver” transaminases (1.5-3 times above normal); often – acute toxic hepatitis with increased activity of “liver” transaminases and / or jaundice, including hepatic failure, including fatal; very rare – chronic liver failure (psevdoalkogolny hepatitis, cirrhosis), including fatal.
The respiratory system: often – or alveolar interstitial pneumonitis, bronchiolitis obliterans with pneumonia, including fatalities, pleural effusion, pulmonary fibrosis; very rarely – bronchospasm in patients with severe respiratory failure patients (especially in patients with bronchial asthma), acute respiratory distress syndrome, including fatalities; the frequency is unknown – pulmonary hemorrhage.
From the senses: very often – microcalcifications in the corneal epithelium, consisting of complex lipids, including lipofuscin (complaints on color appearance of ghosting or fuzziness of contours of objects in bright light); very rarely – optic neuritis, visual neuropathy.
From a metabolism: often – Hypothyroidism, hyperthyroidism; very rarely – a syndrome of inappropriate secretion of antidiuretic hormone.
For the skin: very often – photosensitivity; often – grayish or bluish skin pigmentation (with prolonged use; disappear after cessation of drug administration); very rarely – erythema (with simultaneous radiotherapy), skin rash, exfoliative dermatitis (connection with drug intake is not inserted), alopecia; frequency is unknown – angioedema, urticaria.
From the nervous system: often – tremor and other extrapyramidal symptoms, sleep disturbance, including the “nightmarish” dream; rarely – peripheral neuropathy (sensory, motor, mixed) and / or myopathy; very rarely – cerebellar ataxia, benign intracranial hypertension (pseudotumor of the brain), headache.
Laboratory findings: rare – long-term use – thrombocytopenia, hemolytic and aplastic anemia.
Other: very rarely – vasculitis, epididymitis, impotence (connection with administration of the drug has not been established), thrombocytopenia, hemolytic and aplastic anemia.
special instructions
Before therapy is recommended to perform an ECG study to assess thyroid function (concentration of hormones), and the content of potassium in the blood plasma. Hypokalemia must be corrected before the start of treatment. During treatment should regularly monitor the ECG (every 3 months) and the activity of “liver” transaminases and other liver function tests and thyroid function (including within a few months after its cancellation), X-ray examination of the lungs (every 6 months ) and pulmonary function tests.
If there in the treatment of dyspnoea and dry cough with or without a deterioration of the general condition (fatigue, fever) necessary to carry out X-ray thorax for possible development of interstitial pneumonitis. In the case of the development of drug overturned. При ранней отмене (с или без лечения глюкостероидами) эти явления, как правило, обратимы. Клинические проявления обычно исчезают через 3-4 нед, восстановление рентгенологической картины и функции легких происходит более медленно (несколько месяцев).
При применении Амиодарона на фоне искусственной вентиляции легких (в том числе при проведении хирургических вмешательств) отмечались редкие случаи развития острого респираторного дистресс-синдрома, в том числе с летальным исходом (вероятность взаимодействия с высокими дозами кислорода), поэтому рекомендуется осуществлять строгий контроль состояния таких пациентов.
Перед проведением хирургического вмешательства необходимо поставить в известность врача-анестезиолога о приеме Амиодарона (риск усиления гемодинамического эффекта общих и местных анестетиков).
У пациентов длительно получающих лечение по поводу нарушений ритма сообщалось о случаях повышения частоты фибрилляции желудочков и/или увеличения порога срабатывания кардиостимулятора или имплантированного дефибриллятора, что может снижать их эффективность. Поэтому перед началом и во время лечения Амиодароном следует регулярно проверять правильность их функционирования.
Вследствие удлинения периода реполяризации желудочков сердца, фармакологическое действие Амиодарона вызывает определенные изменения на ЭКГ: удлинение интервала QT, QTс (корригированного), возможно появление U-волн. Допустимое удлинение интервала QT – не более 450 мс или не более чем на 25 % от исходной величины. Эти изменения не являются проявлением токсического действия препарата, однако, требуют контроля для коррекции дозы и оценки возможного проаритмогенного действия.
При развитии атриовентрикулярной блокады II-III степени, синоатриальной блокады или двухпучковой внутрижелудочковой блокады, лечение должно быть прекращено. При возникновении атриовентрикулярной блокады I степени необходимо усилить наблюдение за пациентом.
При возникновении нарушения зрения (нечеткость зрительного восприятия, снижение остроты зрения) необходимо провести офтальмологическое обследование, включая исследование глазного дна. При развитии нейропатии или неврита зрительного нерва, лечение прекращают (риск развития слепоты).
Безопасность и эффективность применения у детей не определены, начало и продолжительность эффекта у них могут быть меньше, чем у взрослых.
Препарат содержит йод, поэтому может оказывать влияние на результаты тестов накопления радиоактивного йода в щитовидной железе.
Effects on ability to drive vehicles and management mechanisms
В период лечения Амиодароном следует воздерживаться от вождения автотранспорта и занятий потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций.
Storage conditions
Store in a dry, dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Таблетки принимают внутрь целиком до приема пищи, запивая достаточным количеством жидкости.
Режим дозирования устанавливается индивидуально и корректируется врачом.
Нагрузочная («насыщающая») доза: в стационаре – начальная доза (разделенная на несколько приемов) составляет 600-800 мг/сут (3 таблетки), максимальная – 1200 мг/сут до достижения суммарной дозы 10 г (обычно в течение 5-8 дней). Амбулаторно – начальная доза (разделенная на несколько приемов) 600-800 мг/сут – до достижения суммарной дозы 10 г (обычно в течение 10-14 дней).
Поддерживающая доза. При поддерживающем лечении применяется минимальная эффективная доза в зависимости от индивидуальной реакции больного и обычно составляет от 100 до 400 мг/сут (1/2-2 таблетки). Вследствие длительного T1/2 препарат можно принимать через день или делать перерыв в приеме препарата – 2 дня в неделю.
Средняя терапевтическая разовая доза – 200 мг.
Средняя терапевтическая суточная доза – 400 мг.
Максимальная разовая доза – 400 мг.
Максимальная суточная доза – 1200 мг.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist