Betaloc Zok pills coated 50mg N30
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Active ingredients
Metoprolol
Release form
Pills
Composition
Metoprolol succinate 47.5 mg, which corresponds to the content: metoprolol tartrate 50 mg metoprolol 39 mg adjuvants: ethylcellulose - 23 mg, hyprolose - 7 mg, hypromellose - 6.2 mg, microcrystalline cellulose - 120 mg, paraffin - 0.1 mg, macrogol - 1.6 mg, silicon dioxide - 12 mg, sodium stearyl fumarate - 0.3 mg, titanium dioxide - 1.6 mg.
Pharmacological effect
Metoprolol is a beta1-blocker that blocks β1-adrenoreceptors at doses significantly lower than the doses required to block β2-adrenoreceptors. Metoprolol has a slight membrane-stabilizing effect and does not show a partial agonist. released during nervous and physical stress. This means that metoprolol has the ability to prevent an increase in heart rate, minute volume and increased contractility of the heart, as well as an increase in blood pressure caused by an abrupt release of catecholamines. a constant concentration of the drug in the blood plasma is observed and a stable clinical effect (blockade of β1-adrenoreceptors) is ensured for more than 24 hours. Due to the lack of obvious peak plasma concentrations, clinically, Betaloc ZOK is characterized by better selectivity for β1-adrenoreceptors compared with conventional tablet forms of beta1-adrenergic blockers. In addition, the potential risk of side effects observed at peak plasma concentrations of the drug, for example, bradycardia and weakness in the legs when walking, is greatly reduced. Patients with symptoms of obstructive pulmonary disease can be prescribed, if necessary, ZOK Betaloc in combination with beta2-adrenomimetic. When used in combination with beta2-adrenomimetics, Betaloc ZOK at therapeutic doses has less effect on bronchodilation caused by beta2-adrenomimetics than nonselective beta-adrenoblockers. Metoprolol, to a lesser extent than non-selective beta-blockers, affects insulin production and carbohydrate metabolism.The effect of the drug on the reaction of the cardiovascular system in hypoglycemia is much less pronounced compared with non-selective beta-blockers. load. At the beginning of metoprolol therapy, an increase in OPSS is noted. However, long-term use may reduce blood pressure due to a decrease in OPSS with a constant cardiac output. In the MERIT-HF study of survival in chronic heart failure (NYHA classification II-IV functional class) with a reduced ejection fraction (≤0.4) that included 3991 patients ZOK showed an increase in survival and a decrease in the frequency of hospitalizations. With long-term treatment, patients achieved a general improvement in well-being, easing the severity of symptoms (according to NYHA functional classes). Also, therapy with the use of the drug Betaloc ZOK has shown an increase in the left ventricular ejection fraction, a decrease in the final systolic and terminal diastolic volumes of the left ventricle. Improving the quality of life during treatment with the drug Betaloc ZOK was observed in patients after myocardial infarction.
Pharmacokinetics
On contact with liquid, the pills quickly disintegrate, thus dispersing the active substance in the gastrointestinal tract. The rate of release of the active substance depends on the acidity of the medium. The duration of the therapeutic effect after taking the drug in the dosage form of Betaloc ZOK (sustained release pills) is more than 24 hours, while achieving a constant rate of release of the active substance over 20 hours inside. Systemic bioavailability after oral administration of a single dose is approximately 30-40%. Metoprolol undergoes oxidative metabolism in the liver. Three major metabolites of metoprolol did not show a clinically significant β-blocking effect. About 5% of the oral dose of the drug is excreted in the urine unchanged, the rest of the drug is excreted in the form of metabolites. Communication with proteins of a blood plasma low, approximately 5-10%.
Indications
- arterial hypertension; - stenocardia; - stable symptomatic chronic heart failure with impaired left ventricular systolic function (as an adjunct therapy to the main treatment of heart failure); - to reduce mortality and the frequency of recurrent infarction after the acute phase of myocardial infarction; including supraventricular tachycardia, reducing the frequency of ventricular contractions during atrial fibrillation and ventricular extrasystoles; - functional disorders of the heart activities accompanied by tachycardia; - prevention of migraine attacks.
Contraindications
- AV block II and III degree; - heart failure in the stage of decompensation; - permanent or intermittent therapy with inotropic drugs acting on β-adrenoreceptors; - clinically significant sinus bradycardia; - SSSU; - cardiogenic shock; - severe violations of peripheral circulation (in including with the threat of gangrene); - hypotension; - patients with suspected acute myocardial infarction with heart rate less than 45 beats / min, PQ interval more than 0.24 s or systolic blood pressure less than 100 mm Hg; - hypersensitivity to metoprolol and others to the drug's applicants or to other beta-blockers; - intravenous introduction of slow calcium channel blockers (like verapamil); - age up to 18 years (efficacy and safety have not been established). With caution, use the drug in stage I AV-blockade, Prinzmetal angina, bronchial asthma, COPD, diabetes mellitus, severe renal failure, metabolic acidosis, together with cardiac glycosides.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Like most drugs, Betaloc ZOK should not be prescribed during pregnancy and during breastfeeding, unless the expected benefits to the mother outweigh the potential risk to the fetus and / or the baby. As with other antihypertensive drugs, beta-adrenergic blockers may cause side effects for example, bradycardia in the fetus, newborns or babies who are breastfed. The amount of metoprolol excreted in breast milk and the beta-blocking effect in a breastfed baby (when the mother takes metoprolol in therapeutic doses) is insignificant.
Dosage and administration
Betaloc ZOK is intended for daily intake of 1 time / day, it is recommended to take the drug in the morning. The tablet Betaloc ZOK should be swallowed, washed down with a liquid. Tablets (or pills divided in half) should not be chewed or crushed. Food intake does not affect the bioavailability of the drug. When selecting a dose, the development of bradycardia should be avoided. Arterial hypertension 50-100 mg 1 time / day. If necessary, the dose can be increased to 100 mg 1 time / day or use Betaloc ZOK in combination with other antihypertensive agents, preferably a diuretic and a calcium channel blocker derived dihydropyridine. Stenocardia 100-200 mg Betaloc ZOK 1 time / day. If necessary, another antianginal medication may be added to the therapy. Stable symptomatic chronic heart failure with impaired left ventricular systolic function Patients must be in a stage of stable chronic heart failure without exacerbations of the exacerbation during the last 6 weeks and without changes in the main therapy during the last 2 weeks. Therapy of heart failure with beta-blockers can sometimes lead to a temporary worsening of the symptomatic picture. In some cases, it is possible to continue therapy or reduce the dose, in some cases it may be necessary to discontinue the drug. Stable chronic heart failure, functional class II Recommended initial dose Betaloc AOC for the first 2 weeks 25 mg 1 time / day. After 2 weeks of therapy, the dose can be increased up to 50 mg 1 time / day, and then it can double every 2 weeks. A maintenance dose for long-term treatment is 200 mg of Betaloc ZOK 1 time / day. Stable chronic heart failure, III-IV functional class Recommended initial dose the first 2 weeks 12.5 mg of Betaloc ZOK (half a tablet of 25 mg) 1 time / day.The dose is selected individually. During the period of increasing the dose, the patient should be under observation, since in some patients, the symptoms of heart failure may worsen. After 1-2 weeks, the dose may be increased to 25 mg of Betaloc ZOK 1 time / day. Then after 2 weeks, the dose may be increased to 50 mg 1 time / day. Patients who tolerate the drug, you can double the dose every 2 weeks to reach the maximum dose of 200 mg of Betaloc ZOK 1 time / day. In case of arterial hypotension and / or bradycardia, you may need a decrease in concomitant therapy or a decrease in dose of Betaloc ZOK. Hypotension at the beginning of therapy does not necessarily indicate that this dose of Betaloc ZOK will not be tolerated with further long-term treatment. However, the dose should not be increased until the condition stabilizes. Control of renal function may be required. Heart rhythm disorders 100-200 mg of ZAK Betaloc 1 time / day. Maintenance treatment after myocardial infarction 200 mg of ZOK Betaloc 1 time / day. Functional disturbances of cardiac activity, followed by tachycardia 100 mg. can be increased to 200 mg / day. Prevention of migraine attacks 100-200 mg Betaloc ZOK 1 time / day. Kidney dysfunctions There is no need to adjust the dose in patients with impaired renal function. Liver dysfunction. Usually due to low the degree of communication with plasma proteins dose adjustment metoprolol is not required. However, in severe impaired liver function (in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required. Older age There is no need to adjust the dose in elderly patients. The experience with the use of the drug OTC Betaloc in children is limited.
Side effects
Betaloc ZOK is well tolerated by patients, the side effects are mostly mild and reversible. To assess the incidence of cases, the following criteria were used: very often (> 10%), often (1-9.9%), infrequently (0.1-0.9%), rarely (0.01 -0.09%), very rarely (<0.01%). From the side of the cardiovascular system: often - bradycardia, orthostatic arterial hypotension (very rarely accompanied by fainting), cold extremities, palpitations; infrequently - a temporary increase in heart failure symptoms,AV degree I blockade, cardiogenic shock in patients with acute myocardial infarction, edema, pain in the region of the heart; rarely - other conduction disorders, arrhythmias; very rarely - gangrene (in patients with severe disorders of the peripheral circulation). From the side of the central nervous system: very often - increased fatigue; often - dizziness, headache; infrequently - paresthesias, convulsions, depression, loss of concentration, drowsiness or insomnia, nightmares; rarely, increased nervous irritability, anxiety; very rarely - memory impairment, amnesia, depression, hallucinations. On the part of the digestive system: often - nausea, abdominal pain, diarrhea, constipation; infrequently - vomiting; rarely, dryness of the oral mucosa. From the side of the liver: rarely, abnormal liver function; very rarely - hepatitis. Dermatological reactions: infrequently - skin rash (such as psoriasis-like urticaria), increased sweating; rarely - hair loss; very rarely - photosensitivity, exacerbation of psoriasis. On the part of the respiratory system: often - shortness of breath on exertion; infrequently - bronchospasm; rarely - rhinitis. From the senses: rarely - visual disturbances, dryness and / or eye irritation, conjunctivitis; very rarely - tinnitus, taste disturbances. From the musculoskeletal system: very rarely - arthralgia. From the metabolism: infrequently - weight gain. From the hematopoietic system: very rarely - thrombocytopenia. Other: rarely - impotence, sexual dysfunction.
Overdose
Metoprolol at a dose of 7.5 g in an adult caused fatal intoxication. A 5-year-old child who took 100 mg of metoprolol did not show signs of intoxication after gastric lavage. Acceptance of 450 mg of metoprolol by a teenager of 12 years has led to moderate intoxication. Acceptance of 450 mg of metoprolol by a teenager of 12 years has led to moderate intoxication. Admission of 1.4 g and 2.5 g of metoprolol in adults caused moderate and severe intoxication, respectively. Acceptance of 7.5 g for adults has resulted in extremely severe intoxication. Symptoms: With an overdose of metoprolol, the symptoms of the cardiovascular system are the most serious, however, sometimes, especially in children and adolescents, symptoms of the central nervous system and suppression of pulmonary functionAV-blockade I-III degree, asystole, pronounced decrease in blood pressure, weak peripheral perfusion, heart failure, cardiogenic shock; depression of lung function, apnea, as well as increased fatigue, impaired consciousness, loss of consciousness, tremor, convulsions, increased sweating, paresthesias, bronchospasm, nausea, vomiting, esophagial spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia possible; effects on the kidneys; transient myasthenic syndrome; concomitant use of alcohol, antihypertensive drugs, quinidine, or barbiturates may worsen the patient's condition. The first signs of overdose can be observed 20 min-2 h after taking the drug. Treatment: the appointment of activated carbon, if necessary, gastric lavage. Important! Atropine (0.25-0.5 mg IV for adults, 10-20 µg / kg for children) should be prescribed before gastric lavage (due to the risk of stimulating the vagus nerve). If necessary, maintain the airway (intubation) and adequate ventilation of the lungs. Restoration of circulating blood volume and glucose infusion. ECG monitoring. Atropine 1.0-2.0 mg IV, if necessary, repeat the introduction (especially in the case of vagal symptoms). In the case of (suppression) myocardial depression, infusion of dobutamine or dopamine is indicated. You can also use glucagon 50-150 µg / kg i.v. with an interval of 1 min. In some cases, adding adrenaline to therapy may be effective. In case of arrhythmias and dilated ventricular (QRS) complex, sodium solutions (chloride or bicarbonate) are injected with infusion. Installation of an artificial pacemaker is possible. When a cardiac arrest due to an overdose, resuscitation may be necessary for several hours. Terbutaline can be used to relieve bronchospasm (injection or by inhalation). Symptomatic treatment is carried out.
Interaction with other drugs
Metoprolol is a substrate of CYP2D6, and therefore, CYP2D6 inhibitory drugs (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone, and diphenhydramine) can affect the metoprolol plasma concentration. Combinations of metoprolol. Combinations with metoprolol. metoprolol,due to the induction of enzymes (the study was conducted with phenobarbital). Propafenone: when prescribing propafenone to 4 patients treated with metoprolol, there was an increase in plasma concentration of metoprolol by 2-5 times, while 2 patients had side effects characteristic of metoprolol. This interaction was confirmed during the study on 8 volunteers. Probably, the interaction is due to the inhibition by propafenone, like quinidine, of the metabolism of metoprolol by the isoenzyme CYP2D6. Taking into account the fact that propafenone has the properties of beta-blocker, co-administration of metoprolol and propafenone does not seem appropriate. Verapamil: a combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on AV conduction and sinus node function. Combinations that may require a dose adjustment of Betaloc ZOK-antarrhythmic drugs of class I: when combined with beta-blockers, the negative inotropic effect may develop; side effects in patients with impaired left ventricular function. Similar combinations should also be avoided in patients with SSS and AV conduction disorders. The interaction is described on the example of disopyramide. Amiodarone: combined with metoprolol can lead to severe sinus bradycardia. Taking into account the extremely long T1 / 2 of amiodarone (50 days), a possible interaction should be considered after a long time after the cancellation of amiodarone. Diltiazem: diltiazem and beta-blockers mutually enhance the inhibitory effect on AV conduction and the function of the sinus node. When metoprolol was combined with diltiazem, there were cases of severe bradycardia. NSAIDs: NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction was registered with the combination with indomethacin and probably will not be observed with the combination with sulindac. Negative interaction was noted in studies with diclofenac. Diphenhydramine: diphenhydramine reduces the biotransformation of metoprolol to α-hydroxymetoprolol 2.5 times.At the same time, there is an increase in the action of metoprolol. Epinephrine (adrenaline): 10 cases of severe arterial hypertension and bradycardia were reported in patients taking non-selective beta-adrenergic blockers (including pindolol and propranolol) and receiving epinephrine. Interaction is also noted in the group of healthy volunteers. It is assumed that such reactions can be observed with the use of epinephrine in conjunction with local anesthetics in case of accidental contact with the vascular bed. Apparently, this risk is much lower when using cardio-selective beta-blockers. Phenylpropanolamine: phenylpropanolamine (norephedrine) in a single dose of 50 mg can increase diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents an increase in blood pressure caused by phenylpropanolamine. However, beta-blockers can cause reactions of paradoxical hypertension in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported in patients receiving phenylpropanolamine. Quinidine: quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (approximately 90% of the population in Sweden), causing a significant increase in the plasma concentration of metoprolol and increased β-adrenoreceptor blockade . It is believed that this interaction is also characteristic of other beta-blockers, the metabolism of which is involved in the CYP2D6 isoenzyme. Clonidine: hypertensive reactions with the abrupt cancellation of clonidine may be enhanced while taking beta-blockers. When used together, if clonidine is to be discontinued, discontinuation of beta-blockers should be started a few days before clonidine is discontinued. Rifampicin: rifampicin can increase the metabolism of metoprolol, reducing its concentration in plasma. Patients who simultaneously take metoprolol and other beta-blockers (eye drops) or MAO inhibitors should be carefully monitored. When taking beta-blockers, inhalation anesthetics increase the cardio-depressive effect.Plasma concentration of metoprolol may increase when taking cimetidine or hydralazine. Cardiac glycosides when used together with beta-blockers may increase the time of AV conduction and cause bradycardia.
special instructions
Patients receiving beta-blockers should not be given IV blockers of slow calcium channels (similar to verapamil). Patients with bronchial asthma or COPD should be given concomitant beta 2-adrenomimetic therapy. It is necessary to prescribe the minimum effective dose of the drug Betaloc ZOK, thus it may be necessary to increase the dose of beta2-adrenomimetic. It is not recommended to prescribe non-selective beta-blockers to patients with Prinzmetal angina pectoris. Beta-blockers should be prescribed selective beta-blockers for this group of patients. When beta1-blockers are used, the risk of their influence on carbohydrate metabolism or the possibility of masking symptoms of hypoglycemia is much lower than when using non-selective beta-blockers. In patients with chronic heart failure, decompensation should be achieved stages of compensation, both before and during drug treatment. It is very rare for patients with impaired AV conduction to worsen ( th outcome - AV-block). If bradycardia has developed during treatment, the drug dose must be reduced or the drug should be gradually discontinued. Betaloc ZOK can aggravate the course of the existing peripheral circulatory disorders mainly due to a decrease in blood pressure. Care should be taken when prescribing the drug to patients with severe renal insufficiency, metabolic acidosis, simultaneous use with cardiac glycosides. Patients taking beta-blockers, anaphylactic shock occurs in a more severe form. The use of epinephrine (adrenaline) in therapeutic doses does not always lead to the achievement of the desired clinical effect in patients receiving metoprolol. Patients suffering from pheochromocytoma, along with the drug Betaloc ZOK, should be prescribed alpha-adrenergic blocking agent. , therefore it should be avoided.If you need to cancel the drug, it should be made gradually over a period of at least 2 weeks, with a twofold decrease in the dose of the drug at each stage, until the final dose of 12.5 mg (1/2 tab. 25 mg) is reached, which should be taken as at least 4 days until complete withdrawal of the drug. When symptoms appear (for example, increased symptoms of angina, increased blood pressure), a slower withdrawal regimen is recommended. Abrupt cancellation of the beta-adrenergic blocker can lead to worsening of the course of chronic heart failure and increase the risk of myocardial infarction and sudden death. In case of surgical intervention, the anesthesiologist should be informed that the patient is taking Betaloc ZOK. Patients who are to undergo surgical intervention are not recommended to discontinue therapy with beta-blockers. It is necessary to avoid prescribing the drug in high doses without prior titration of doses of the drug to patients with cardiovascular risk factors undergoing non-cardiological operations, due to the increased risk of bradycardia, arterial hypotension and stroke, including fatal. Clinical studies on efficacy and safety in patients with severe stable symptomatic chronic heart failure (NYHA class IV) are limited. The treatment of such patients should be carried out by doctors with special knowledge and experience. Patients with symptomatic heart failure in combination with acute myocardial infarction and unstable angina pectoris were excluded from the studies on the basis of which indications for administration were determined. The efficacy and safety of the drug for this group of patients is not described. Use in unstable heart failure in the decompensation stage is contraindicated. Effect on the ability to drive motor vehicles and control mechanisms