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Cardioselective beta1-blocker without internal sympathomimetic activity. It has a hypotensive, antianginal and antiarrhythmic effect. It lowers the automatism of the sinus node, reduces heart rate, slows AV conductivity, reduces contractility and myocardial excitability, reduces cardiac output, reduces myocardial need for oxygen. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.
It causes a hypotensive effect, which stabilizes by the end of the 2nd week of course application. With exertional angina, metoprolol reduces the frequency and severity of seizures. Normalizes heart rhythm with supraventricular tachycardia and atrial fibrillation. When myocardial infarction contributes to the limitation of the ischemic zone of the heart muscle and reduces the risk of fatal arrhythmias, reduces the possibility of recurrence of myocardial infarction. When used in moderate therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.
♦ arterial hypertension;
♦ stable symptomatic chronic heart failure
in violation of the systolic function of the left ventricle (as
adjuvant therapy to the primary treatment of chronic heart
♦ reduction of mortality and frequency of recurrent infarction after the acute phase
♦ heart rhythm disorder, including supraventricular tachycardia,
a decrease in the frequency of ventricular contraction during atrial fibrillation and
♦ functional disorders of cardiac activity, accompanied by
♦ prevention of migraine attacks.
1 tab. metoprolol 100 mg
Excipients: lactose monohydrate 180 mg, microcrystalline cellulose 72 mg, potato starch 12 mg, carboxymethyl starch sodium 16 mg, povidone 16 mg, magnesium stearate 4 mg.
Metoprolol is marketed under different brands and generic names, and comes in different dosage forms:
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Dosage and Administration
When ingested, the average dose is 50-100 mg / day. in 1-2 doses. If necessary, the daily dose is gradually increased to 200 mg.
Maximum doses: when ingestion daily dose is 400 mg.
Since the cardiovascular system: possible bradycardia, arterial hypotension, AV-conduction disorders, the appearance of symptoms of heart failure.
On the part of the digestive system: at the beginning of therapy, dry mouth, nausea, vomiting, diarrhea, constipation; in some cases - abnormal liver function.
On the part of the central nervous system and peripheral nervous system: at the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, feeling of cold and paresthesia in the limbs; reduction of secretion of the tear fluid, conjunctivitis, rhinitis, depression, sleep disturbances, nightmarish dreams are possible.
From the hemopoietic system: in some cases - thrombocytopenia.
On the part of the endocrine system: hypoglycemic states in patients with diabetes mellitus.
On the part of the respiratory system: symptoms of bronchial obstruction are possible in predisposed patients.
Allergic reactions: skin rash, itching.
Hypersensitivity, cardiogenic shock, AV block II and III degree, sinoatrial block, chronic (decompensated) heart failure, sick sinus syndrome, severe sinus bradycardia (HR less than 60 beats / min), Prinzmetal angina, acute myocardial infarction less than 45 udmin, PQ interval more than 0.24 sec, systolic blood pressure less than 100 mm RT.st).
Pregnancy, lactation. Simultaneous intravenous administration of blockers of "slow" calcium channels like verapamil. Age up to 18 years. Pheochromocytoma. patients receiving long-term or intermittent therapy with inotropic drugs and acting on beta-adrenoreceptors.
With simultaneous use with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of severe arterial hypotension, bradycardia, AV blockade.
With simultaneous use with barbiturates, metabolism of metoprolol is accelerated, which leads to a decrease in its effectiveness.
With simultaneous use with hypoglycemic agents may increase the action of hypoglycemic agents.
With simultaneous use with NSAIDs, it is possible to reduce the hypotensive effect of metoprolol.
With simultaneous use with opioid analgesics, the cardiodepressive effect is mutually enhanced.
With simultaneous use with peripheral muscle relaxants may increase neuromuscular blockade.
With simultaneous use with agents for inhalation anesthesia increases the risk of inhibition of myocardial function and the development of arterial hypotension.
With simultaneous use with oral contraceptives, hydralazine, ranitidine, cimetidine concentration of metoprolol in the blood plasma increases.
With simultaneous use with amiodarone arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.
With simultaneous use with verapamil Cmax increases in plasma and AUC of metoprolol. Minute and stroke volume of the heart, pulse rate, arterial hypotension are reduced. Perhaps the development of heart failure, dyspnea and blockade of the sinus node.
With the on / in the introduction of verapamil in patients receiving metoprolol there is a threat of cardiac arrest.
With simultaneous use may increase bradycardia caused by digitalis glycosides.
With simultaneous use with dextropropoxifene, the bioavailability of metoprolol is increased.
With simultaneous use with diazepam may decrease clearance and increase the AUC of diazepam, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions.
With simultaneous use with diltiazem, the concentration of metoprolol in the blood plasma increases due to inhibition of its metabolism under the influence of diltiazem. The effect on the activity of the heart is additively inhibited due to the slowing down of impulse conduction through the AV node caused by diltiazem. There is a risk of severe bradycardia, a significant decrease in stroke and minute volume.
With simultaneous use of lidocaine, a violation of lidocaine may be possible.
With simultaneous use with mibefradil in patients with low CYP2D6 isoenzyme, it is possible to increase plasma plasma concentration of metoprolol and increase the risk of toxic effects.
With simultaneous use with norepinephrine, epinephrine, other adreno-and sympathomimetics (including in the form of eye drops or as part of antitussives), some increase in blood pressure is possible.
With simultaneous use with propafenone, the concentration of metoprolol in the blood plasma increases and the toxic effect develops. It is believed that propafenone inhibits the metabolism of metoprolol in the liver, reducing its clearance and increasing serum concentrations.
With simultaneous use with reserpine, guanfacine, methyldopa, clonidine, the development of severe bradycardia is possible.
With simultaneous use of rifampicin decreases the concentration of metoprolol in the blood plasma.
Metoprolol may cause a slight decrease in theophylline clearance in smoking patients.
Fluoxetine inhibits the CYP2D6 isoenzyme, this leads to inhibition of the metabolism of metoprolol and its accumulation, which can enhance the cardiodepressive effect and cause bradycardia. The case of the development of lethargy is described.
Fluoxetine and mainly its metabolites are characterized by a long T1 / 2, so the likelihood of drug interaction persists even a few days after discontinuing fluoxetine.
There are reports of a decrease in the clearance of metoprolol from the body with simultaneous use with ciprofloxacin.
With simultaneous use with ergotamine may increase peripheral circulatory disorders.
With simultaneous use with estrogen decreases the antihypertensive effect of metoprolol.
With simultaneous use of metoprolol increases the concentration of ethanol in the blood and prolongs its excretion.
It is used with caution in patients with chronic obstructive airway diseases, diabetes mellitus (especially when labile), Raynaud's disease and obliterating diseases of the peripheral arteries, pheochromocytoma (should be used in combination with alpha-adrenergic blockers), marked impaired renal function and liver.
With metoprolol treatment, a reduction in tear fluid production is possible, which is important for patients using contact lenses.
The completion of a long course of treatment with metoprolol should be carried out gradually (for at least 10 days) under the supervision of a physician.
The simultaneous use of metoprolol with MAO inhibitors is not recommended.
In combination therapy with clonidine, the latter should be stopped several days after the cancellation of metoprolol, in order to avoid a hypertensive crisis. At simultaneous use with hypoglycemic agents correction of their dosing regimen is required.
A few days before undergoing anesthesia, it is necessary to stop taking metoprolol or to choose a remedy for anesthesia with minimal negative inotropic effects.
Influence on ability to drive motor transport and control mechanisms
In patients whose activities require increased attention, the question of the use of metoprolol on an outpatient basis should be addressed only after evaluating the patient's individual response.
Symptoms: severe sinus bradycardia, dizziness, AV blockade (up to the development of complete transverse blockade and cardiac arrest), marked reduction in blood pressure, syncope, arrhythmia / ventricular premature beats, acute heart failure; cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma, nausea, vomiting, cyanosis, hypoglycemia, convulsions. The first signs of overdose appear 20 minutes -2 hours after taking the drug.
Treatment: gastric lavage and prescription of adsorbent drugs, symptomatic therapy: with a marked decrease in blood pressure - the patient should be in the Trendelenburg position; in case of excessive reduction of blood pressure, bradycardia and heart failure - in / in the introduction with an interval of 2-5 minutes of beta-adrenostimulyatorov to achieve the desired effect or in / in the introduction of 0.5-2 mg of atropine sulfate. In the absence of a positive effect, dopamine, dobutamine or norepinephrine. As a follow-up, a transvenous intracardiac pacemaker can be set. In case of bronchospasm, beta-adrenomimetics should be introduced. With convulsions, slow i.v. administration of diazepam. Hemodialysis is ineffective.
- Brand name: Metoprolol
- Active ingredient: Metoprolol
- Dosage form: pills are white or white with a grayish shade of color, round, flat, risky on one side and chamfered on both sides.
- Manufacturer: Akrikhin
Studies and clinical trials of Metoprolol (Click to expand)
- Effect of chiral enhancers on the permeability of optically active and racemic metoprolol across hairless mouse skin
- Chiral analysis of metoprolol and its by-products by capillary electrophoresis
- Influence of acebutolol and metoprolol on cardiac output and regional blood flow in rats
- Evaluation of “external” predictability of an in vitro–in vivo correlation for an extended-release formulation containing metoprolol tartrate
- Cardioprotective effect of metoprolol and enalapril in doxorubicin-treated lymphoma patients: A prospective, parallel-group, randomized, controlled study with 36-month follow-up
- Catalytic asymmetric synthesis of propranolol and metoprolol using a La–Li–BINOL complex
- Pharmacokinetics of Atenolol and Metoprolol Administered together with Piroxicam
- Determination of Metoprolol Tartrate by Ion-Pair Extraction with Bromothymol Blue
- The effect of antacid, metoclopramide, and propantheline on the bioavailability of metoprolol and atenolol
- The effect of hydralazine on the pharmacokinetics of three different beta adrenoceptor antagonists: Metoprolol, nadolol, and acebutolol
- Influence of inflammatory disease on the clinical pharmacokinetics of atenolol and metoprolol
- Rapid chiral separation of metoprolol in plasma—application to the pharmacokinetics/pharmacodynamics of metoprolol enantiomers in the conscious goat
- Enantioselective bioanalysis of beta-blocking agents: Focus on atenolol, betaxolol, carvedilol, metoprolol, pindolol, propranolol and sotalol
- Development, validation and analytical error function of two chromatographic methods with fluorimetric detection for the determination of bisoprolol and metoprolol in human plasma
- Direct enantiomeric resolution of (±)-atenolol, (±)-metoprolol, and (±)-propranolol by impregnated TLC using L-aspartic acid as chiral selector
- HPLC quantiﬁcation of metoprolol with solid-phase extraction for the drug monitoring of pediatric patients
- High-performance liquid chromatography method development and validation for simultaneous determination of five model compounds, antipyrine, metoprolol, ketoprofen, furosemide and phenol red, as a tool for the standardization of rat in situ intestinal permeability studies using timed wavelength detection
- Selected ion monitoring of metoprolol and two metabolites in plasma and urine using deuterated internal standards
- Analysis of α-hydroxy metabolites of metoprolol in human urine after phosgene/trimethylsilyl derivatization
- ChemInform Abstract: Synthesis and Biological Evaluation of a Fluorinated Analogue of the . beta.-Adrenergic Blocking Agent Metoprolol.
- ChemInform Abstract: Synthesis, NMR Studies and Conformational Analysis of Oxazolidine Derivatives of the β-Adrenoreceptor Antagonists Metoprolol, Atenolol, and Timolol.
- Synthesis and Cardiovascular Activity of Metoprolol Analogues.
- Influence of input rate on the stereospecific and nonstereospecific first pass metabolism and pharmacokinetics of metoprolol extended release formulations
- Stereoselective metabolism of metoprolol: Enantioselectivity of α-hydroxymetoprolol in plasma and urine