Betaloc. 50 mg. 30 tablets
Betaloc. 50 mg. 30 tablets
Prolonged-release tablets 50 mg: white, round, scored , marked with the symbol A / mo , diameter of 9 mm.
4 . CLINICAL FEATURES
4.1 Therapeutic indikatsiiHipertoniya . Angina pectoris . In the combined treatment of symptomatic chronic heart failure with impaired systolic left ventricular function . Prevention of morbidity and mortality from cardiovascular events and reinfarction after the acute phase of myocardial infarction. Cardiac arrhythmias, including especially supraventricular tachycardia, reduction of ventricular rate in atrial fibrillation and ventricular extrasystoles . Functional heart disorders , hyperkinetic syndrome . Prophylaxis of migraine.
4.2 Posology and method of administration
Betaloc ZOK prolonged-release tablets are intended for once-daily dosing . It is preferable to take the morning . Sustained-release tablets can be divided . Should not be chewed or crushed. The tablets should be swallowed with at least half a cup of liquid. Concomitant food intake does not affect bioavailability . The dosage should be individually adjusted to avoid bradycardia.
The following information is presented in the form of instructions:
The recommended dose in patients with mild to moderate hypertension is 50 mg daily. In patients who do not respond to 50 mg, the dose may be increased up to 100-200 mg per day, and / or combined with other antihypertensive drugs , diuretics and preferably koltsievi antagonists of dihydropyridine type .
100-200 mg as a single dose . The dose may be combined with the nitrate or be increased.
Adjunctive therapy to treatment with ACE- inhibitors , diuretics and possible therapy with digitalis derivatives with symptomatic heart nedostatachnost.Patsientite must have chronic heart failure without acute failure in the last 6 weeks, and substantially unchanged basic therapy in the last 2 to sedmitsi.Lechenieto heart failure with beta -blockers can sometimes cause a temporary exacerbation of symptoms. In some cases it is possible to continue the treatment or reduce the dose and in other cases it may be necessary to discontinue treatment. Appointment of Betaloc ZOK therapy in patients with severe heart failure (NYHA IV) should be done only by physicians trained in the treatment of heart failure ( see section 4.4). Dosage in patients with stable heart failure functional class IIPreporachitelna initial dose the first two weeks, 25 mg once daily . After two weeks may be increased to 50 mg once a day. The target dose for long-term treatment is 200 mg once daily .
Dosage in patients with chronic heart failure functional class III- IVPreporachitelnata initial dose is 12.5 mg ( half a tablet of 25 mg) once daily for the first week . The dose should be individually adjusted and patients should be under close monitoring during dose escalation , because the symptoms of chronic heart failure may worsen in some patients. After 1-2 weeks, the dose can be increased to 25 mg once daily . Then, after two more weeks, the dosage may be increased to 50 mg once daily . In patients . That tolerate higher doses , the dose may be doubled every two weeks up to a maximum of 200 mg per day.
In hypotension and / or bradycardia, it may be necessary to decrease the dose of the concomitant drug or reduction in dose of Betaloc ZOK. Initial hypotension does not necessarily mean that the dosage of Betaloc ZOK can not be tolerated in a chronic treatment , but the dosage should be increased until the patient's condition has stabilized . Simultaneously, other actions may be necessary to monitor renal function .
100-200 mg as a single dose . The dose may be increased if necessary .
Prevention after myocardial infarction
Maintenance dose is usually 200 mg once
Functional heart disorders with palpitations
100 mg daily as a single dose. The dose may be increased if necessary to 200 mg.
Prophylaxis of migraine
100-200 mg daily as a single dose .
Impaired renal function
The elimination rate is only slightly influenced by renal function and therefore there is no need for dosage adjustment in patients with impaired renal function.
Impaired liver function
Generally, the dose of Betaloc ZOK prescribed to patients suffering from liver cirrhosis and those with normal hepatic function is the same as metoprolol has low protein binding (5-10 %). Only when there are many symptoms of severe hepatic impairment (eg shunt-operated patients ) , then you need to take lower dozata.Patsienti Elderly : No dose adjustment required .
Experience in the treatment of children with Betaloc ZOK is limited.
Cardiogenic shock. Sick sinus syndrome . Atrioventricular block second or third degree. ' Patients with uncompensated heart failure (pulmonary edema, hypoperfusion , or hypotension) , and patients with continuous or intermittent inotropic therapy acting through agonism of beta- receptors. Symptomatic bradycardia or hypotension. Metoprolol should not be given to patients with acute myocardial infarction, where heart rate was < 45 beats / min , PQ interval > 0.24 or systolic blood pressure <100 mm Hg. When indications of heart failure should be reassessed the condition of patients with blood pressure sitting below 100 mmHg prior to treatment . Disease , peripheral arterial with risk of gangrene . Hypersensitivity to metoprolol or any of the excipients, or to other beta- blockers.
Special warnings and precautions for use
In patients treated with beta- blockers should be administered parenteral products with verapamil. Metoprolol may intensify symptoms of circulatory disorders of the peripheral arteries such as intermittent claudication . Severely impaired renal function. Acute conditions with metabolic acidosis. Treatment in combination with digitalis.
In patients with angina Prinzmetal frequency and duration of relapses can be increased due to the contraction of the coronary arteries induced by alpha receptor . Therefore, non-selective beta- blockers must be used in such patients. Beta1 - selective blockers should be used with caution .
Patients with bronchial asthma and other chronic obstructive pulmonary disease to be administered concomitantly with appropriate bronchodilators ( / 32 - agonists ) such as tablets or inhalation . The dose of beta2- stimulants may be increased when starting treatment with metoprolol.
During treatment with metoprolol risk of interfering with carbohydrate metabolism or masked hypoglycemia is less than non-selective beta- blokeri.Mnogo rarely aggravate existing moderate in severity disturbance of AV conduction ( possibly reach AV block).
Treatment with beta-blockers may aggravate the treatment of anafilaktachna reaction. Treatment with adrenaline in normal doses does not always provide the desired therapeutic effect. If Betaloc ZOK is prescribed to a patient with phaeochromocytoma should be made with alpha - bloker.Dannite efficacy and safety of controlled clinical trials in patients with severe symptomatic heart failure (NYHA class IV) are limited. Treatment of heart failure in these patients should be undertaken only by physicians experienced in this area (see section 4.2).
Patients with chronic ( compensated ) heart failure associated with acute myocardial infarction and angina pectoris were excluded from the study Betaloc Zok in heart failure . In these conditions the efficiency and safety in the treatment of acute myocardial infarction have not been documented . Use in uncompensated heart failure is contraindicated ( see section 4.3). Before surgery should inform the anesthetist that the patient is receiving metoprolol. It is not recommended to stop treatment blocker in patients for operative lechenie.Vnezapnoto discontinuation of beta- blockade is dangerous , especially in high - risk patients and may worsen chronic heart failure and increase the risk of myocardial infarction and sudden death. Any discontinuation of Betaloc ZOK, if possible, should be done gradually over at least two weeks, the dose should be reduced by half with each step until the last dose when 25 mg tablet be split . The last dose should be taken at least four days prior to termination. If symptoms suggested a slow rate of break lechenieto.Ako taking Betaloc ZOK should be discontinued before surgery it should be done at least 48 hours before the procedure except in special cases such as thyrotoxicosis and patients phaeochromocytoma.Pri B- blocker anaphylactic shock is a major burden .
4.5 Interaction with other medicinal products and upset anyone else forms of interaction
The following combinations with Betaloc ZOK to avoid : Derivatives of barbituric acid Barbituriti ( tested for pentobarbital ) induction of the metabolism of metoprolol by enzyme induction.
Propafenone: after taking propafenone four patients treated with metoprolol plasma concentrations of metoprolol increased from two to five times and in two patients side effects were typical of metoprolol. The reaction was confirmed in eight healthy volunteers. This interaction can be explained by the fact that, propafenone, quinidine inhibited similarly to the metabolism of metoprolol by cytochrome P450 2D6. This combination is likely intractable as propafenone and also beta- blocking properties .
Verapamil: in combination with beta- receptor blocking agents ( such as atenolol, propranolol and pindolol) verapamil can cause bradycardia and decrease of blood pressure . Verapamil and beta- blockers have additive suppressive effect on AV conduction and sinus node function .
The following combination of Betaloc ZOK may require dosage adjustment : Amiodarone: According to a report of a similar case patients treated with amiodarone may develop severe sinus bradycardia, concomitant treatment with metoprolol. Amiodarone has an extremely long half-life ( approximately 50 days) , suggesting that the interaction may occur long after discontinuation of the drug.
Antiarrhythmics , class I: class I- and antiarrhythmics beta- receptor blockers have additive negative inotropic effect , which can lead to serious side effects in hemodynamics in patients with impaired left ventricular . This combination should be avoided and " sick sinus syndrome " and abnormal AV conduction. This interaction is best found in the drug disopyramide.
Nonsteroidal antiinflammatory / antirheumatic drugs: it was found that NSAIDs reduce the antihypertensive effect of beta -blockers . Indomethacin is the most studied. This interaction probably not observed with sulindac. A study of the adverse reaction with diclofenac.
Dipkenhydramin: Diphenhydramin decreased clearance (2.5 times) of metoprolol to alpha-hydroximetoprolol by CYP 2D6 -speed hidroksilatori . The effect of metoprolol is increased. Diphenhydramine may inhibit metabolism by CYP 2D6 substrati.Diltiazem : Diltiazem and beta- blockers have an additional depressing effect on AV conduction and sinus node function . Pronounced bradycardia was observed ( case report ) in combination therapy with diltiazem.
Elpinephrine: Approximately ten messages from the treatment of patients with non-selective beta-blockers ( including pindolol and -propranolol) show that patients develop pronounced hypertension and bradycardia after administration of epinephrine (adrenaline). These clinical observations have been confirmed in studies in healthy volunteers. Done is suggested that epinephrine with local anesthetics can cause these reactions after intravascular administration . This risk is probably lower in cardioselective beta-blockers.
Phenylpropranolamine: Phenylpropranolamine ( norephedrine ) in single doses of 50 mg may increase diastolic pressure to pathological levels in healthy volunteers. Propranolol generally stops the rise in blood pressure caused by phenylpropranolamine. However, beta-blockers can cause paradoxical hypertensive reactions in patients taking high doses phenylpropranolamine. Hypertensive crisis during treatment with phenylpropranolamine only been described in two sluchaya.Quinidine : Quinidine inhibits the metabolism of metoprolol in a so- called fast hidroksilatori (more than 90% in Sweden ) with a significant increase in plasma levels , and as a result, an increased beta- blockade . Such an interaction may occur for other beta -blockers metabolized by the same enzyme ( cytochrome P450 2D6). If you stop co-administered Quinidine, B- blocker should be discontinued several days before Quinidine.Clonidine: hypertensive reaction to sudden withdrawal of clonidine may be increased by beta-blockers.
Rifampicine: Rifampicine may induce the metabolism of metoprolol, resulting in reduced plasma levels.
The plasma concentrations of metoprolol may be increased by concomitant administration of cimetidine, hydralazine , selective inhibitors of serotonin reuptake (SSRI) such as paroxetine , fluoxetine and sertraline. Patients taking other beta-blockers (eg eye drops ) or MAO inhibitors should be closely monitored . Patients on beta- blockade therapy for inhaled anesthetics enhance cardio - depressive patients efekt.Pri B- blockers should be adapted dose of oral antidiabetic agents .
Use in pregnancy and lactation
Metoprolol CR / ZOK should not be used during pregnancy and lactation unless its use is not considered vazhna.Kakto all antihypertensive drugs p- blockers can cause side effects such as bradycardia in the fetus and newborn. You need to pay attention to especially if these drugs are given in the last three months of pregnancy and during labor.
Metoprolol passes into breast milk , but the risk that affect your child is unlikely at therapeutic doses.
4.7 Effects on ability to drive and use machines
When treated with Betaloc ZOK may occur dizziness and fatigue. This should be taken into account when driving or operating machinery .
4.8 Undesirable effects
Metoprolol CR / ZOK is well tolerated in most cases side effects are mild and reversible. The following events have been reported as adverse reactions during clinical trials or from use in clinical practice , most often with conventional metoprolol (metoprolol tartrate). In many cases, no association was found with the use of metoprolol. The following definitions of frequency of reactions : Very common (> 10% ), common ( 1-9.9 %) , uncommon ( 0.1-0.9 % ), rare ( 0:01 to 00:09 %) and very rare ( <0.01 %).
Common: bradycardia, orotostatichni disorders ( rarely syncope) , cooling of the peripheral parts of the body , palpitation .
Uncommon: worsening heart failure , heart block first degree, edema, atrial pain.
Rare: cardiac conduction disorders , cardiac arrhythmia
Very rare: Gangrene in patients with vascular disorders .
Central nervous system:
Very common: fatigue. Common: headache, dizziness.
Uncommon: paraesthesia , muscle cramps.
Common: abdominal pain , nausea , diarrhea, and finding.
Rare: dry mouth .
Very rare: thrombocytopenia.
Rare: abnormal results of liver function tests .
Very rare: hepatitis.
Uncommon: increase tegloto.S
Very rare: arthralgia .
Uncommon: depression , impaired concentration , somnolence or sleep disturbances, nightmares .
Rare: nervousness , anxiety , impotence / sexual dysfunction
Very rare: amnesia / impaired memory , confusion , hallucinations
Common: dyspnoea on exertion .
Uncommon : bronchospasm .
Rare: Abnormal vision , dry and / or irritated eyes , conjunctivitis .
Very rare : tinnitus , taste disturbance .
Uncommon: rash ( in the form of urticaria and psoriasiform skin lesions induced dystrophy ), increased sweating. Rare: alopecia .
Very rare: photosensitivity reactions , worsening psoriasis.
Overdose : 7.5 g caused lethal intoxication in adults. 100 mg in 5 year old child does not cause symptoms after gastric lavage. 450 mg in 12-year and 1.4 g in an adult led to moderate intoxication , 2.5 g in adults cause severe intoxication and 7.5 g in an adult causing severe intoxication.
cardiac symptoms are most important , but in some cases, especially in children and young adults the symptoms of CNS and respiratory depression may prevail . Bradycardia , AV- block I-III, asistolichno decrease in blood pressure , poor peripheral perfusion , cardiac failure, cardiogenic shock . Respiratory depression, apnea . Other : fatigue , confusion , unconsciousness, fine tremor, seizures , sweating, paresthesia , bronchospasm , nausea , vomiting, possible esophageal spasms , hypoglycemia (especially in children) and hyperglycemia , hyperkalemia. Effects on the kidneys.