METOPROLOL

Active material: Metoprolol
When ATH: C07AB02
CCF: Beta₁-adrenoblokator
When CSF: 01.01.01.02
Manufacturer: HEMOFARM A.D. (Serbia)

Pharmaceutical form, composition and packaging

Pills, covered with a film shell pinkish, round, lenticular, with Valium on one side.

[Ring] Colloidal anhydrous silica, microcrystalline cellulose, sodium carboxymethyl (Type A), magnesium stearate.

The composition of the shell: gipromelloza, polysorbate 80, talc, Titanium dioxide (E171), carmine dye (Ponceau 4R).

14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.

Pills, Film-coated white to yellowish-white, round, lenticular, with Valium on one side.

[Ring] Colloidal anhydrous silica, microcrystalline cellulose, sodium carboxymethyl (Type A), magnesium stearate.

The composition of the shell: gipromelloza, polysorbate 80, talc, Titanium dioxide (E171).

10 PC. – blisters (3) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Cardioselective beta₁-blocker without intrinsic sympathomimetic activity. It has hypotensive, antianginalnoe and antiaritmicescoe action. Lowers automaticity sinus node, reduces heart rate, slows AV-conduction, reduces airway and anxiety attack, reduces cardiac output, reducing myocardial oxygen demand. Suppresses the stimulating effect of Catecholamines on the heart during physical and psychoemotional exertion.

Causes gipotenzivny effect, that is stabilized by the end of the 2-week course application. When strokes voltage metoprolol reduces the frequency and severity of attacks. Normalizes heart rhythm when najeludockova tachycardia and atrial fibrillation. Myocardial infarct zone constraining ischemia of cardiac muscle and reduces the risk of fatal arrhythmias, reduces possibility of recurrence of myocardial infarction. When used in therapeutic doses has average less pronounced effect on the smooth muscles of the bronchi and peripheral arteries, than selective beta-adrenoblokatora.

Pharmacokinetics

After intake of metoprolol quickly and almost completely absorbed from the digestive tract, C_max the active substance in plasma is achieved by 1-2 no. Intensive metabolised in the liver with the formation of active metabolites.

T_1/2 metoprolol plasma is 3-4 h and during the course of treatment does not change. More 95% the dose secreted by the kidneys, of these, only 3% – in unchanged form.

Testimony

Arterial hypertension, prevention of angina attacks, heart rhythm disturbances (supraventricular tachycardia, arrythmia), secondary prophylaxis of post-myocardial infarction, hyperkinetic cardiac syndrome (incl. hyperthyroidism, NDCS). Preventing attacks of migraine.

Dosage regimen

If ingestion is the average dose is 100 mg / day 1-2 admission. If necessary, the daily dose gradually increased to 200 mg. The on / in a single dose – 2-5 mg; in the absence of effective re-introduction possible through 5 m.

The maximum dose: the ingestion dose – 400 mg, the on/in a single dose – 15-20 mg.

Side effect

Cardio-vascular system: possible aetiology, hypotension, violations AV conduction, symptoms of heart failure.

From the digestive system: at the beginning of therapy, there may be dryness in the mouth, nausea, vomiting, diarrhea, constipation; in some cases – abnormal liver function.

From the central and peripheral nervous system: at the beginning of therapy possible weakness, fatiguability, dizziness, headache, muscle cramps, feeling cold and paresthesias in the extremities; possible reduced secreta slezna fluid, conjunctivitis, rhinitis, depression, sleep disorders, nightmares.

From the hematopoietic system: in some cases – thrombocytopenia.

On the part of the endocrine system: gipoglikemicakie State in patients with diabetes mellitus.

The respiratory system: prone patients may cause symptoms of bronchial obstruction.

Allergic reactions: skin rash, itch.

Contraindications

AV-blockade II and III degrees, sinoatrialynaya blockade, bradycardia (HR less 50 beats / min), SSS, hypotension, chronic heart failure II B-III stage, acute heart failure, cardiogenic shock, metabolic acidosis, expressed by peripheral circulatory disorders, hypersensitivity to metoprololu.

Pregnancy and lactation

Pregnancy may only, when the intended benefits to the mother outweighs the potential risk to the fetus. Metoprolol penetrates through the placental barrier. In connection with the possible development of bradycardia in the newborn, hypotension, Hypoglycemia and stop breathing you need to cancel for metoprolol 48-72 hours before the planned period of delivery. After delivery you must ensure strict monitoring of the newborn child during the 48-72 no.

Metoprolol in small quantities is the breast milk. Use during lactation is not recommended.

Cautions

To apply caution in patients with chronic obstructive respiratory diseases, diabetes (especially when labil'nom reaches), Raynaud's disease and obliterating diseases of peripheral arteries, pheochromocytoma (should be used in conjunction with alpha-adrenergic), acute violations of the kidney and the liver.

Treatment with metoprolol may reduce slezna fluid, that has implications for patients, using contact lenses.

The completion of a lengthy course of treatment, metoprolol should be gradually (at least 10 days) under the supervision of a physician.

Not recommended simultaneous application of metoprolol with MAO inhibitors.

In combination therapy with clonidine last admission should continue a few days after the lifting of metoprolol, to avoid gipertoniceski kriza. Together with the use of means of correction required their hypoglycemic dosage.

A few days before the anesthesia should stop taking metoprolol or choose for narcosis tool with minimal negative inotropic effect.

Effects on ability to drive vehicles and management mechanisms

Patients, activities that require increased attention, the question of the application of metoprolol in the outpatient setting should be addressed only after an assessment of the individual reactions of the patient.

Drug Interactions

If you are applying with antigipertenzivei means, Diuretics, antiarrhythmics, nitratami, raises the risk of arterial expressed hypotension, ʙradikardii, AV-blockade.

If you are applying with barbituratami accelerates the metabolism of metoprolol, which reduces its effectiveness.

Together with the use of hypoglycemic means strengthening of gipoglikemicakih funds.

Together with the use of NSAIDS may reduce gipotenzivnogo actions metoprolol.

Together with the use of opioid analgesics mutually reinforced kardiodepressivnyj effect.

If you are applying with perifericescimi miorelaxanthami possible increase neuromuscular blockade.

If you are applying to means of inhalation narcosis increases the risk of myocardial function and development of oppression, arterial hypotension.

In an application with oral contraceptives, gidralazinom, ranitidine, cimetidine increases concentration metoprolola plasma.

Together with the use of amiodarone possible arterial gipotenzia, bradycardia, ventricular fibrillation, asistolija.

Together with the use of Verapamil increases (C)_max in the blood plasma and the AUC of metoprolol. Dropping a minute and impact of the heart, pulse rate, hypotension. May develop heart failure, Dyspnea and blockade of sinus node.

The on/in the introduction against the backdrop of the admission verapamila metoprolol there is a threat of cardiac arrest.

If you are applying may increase bradycardia, caused by Digitalis glycosides.

Together with the use of dextrapropoxiphen increases the bioavailability of metoprolol.

Together with the use of diazepam may reduce clearance and an increase in AUC of diazepam, that could lead to the strengthening of its effects and reduce the speed psychomotor reactions.

Together with the use of diltiazem increases concentration metoprolola plasma blood as a result of the inhibiting its metabolism under the influence of diltiazem. Additively oppressed heart operations in connection with the slowdown in spending momentum through the AV node, caused by diltiazem. Raises the risk of bradycardia, significant impact reduction and minute volume.

Together with the use of lidocaine may impair excretion of lidocaine.

Together with the use of mibefradilom in patients with low activity of CYP2D6 may increase the concentration of izofermenta metoprolola plasma and increase the risk of toxic effects.

Together with the application norapinefrinom, epinephrine, other adreno- and sympathomimetic (incl. in the form of eye drops or in a protivokashlevykh funds) Perhaps some ad.

Together with the use of propafenonom increases concentration metoprolola plasma and develops toxic effect. It is believed, that inhibits the metabolism of propafenone metoprolol in the liver, reducing the clearance and increasing serum concentrations.

If you are applying with rezerpinom, guanfacinom, methyldopa, clonidine may develop bradycardia.

Together with the use of rifampicin reduced the concentration metoprolola plasma.

Metoprolol may cause a slight decrease in clearance of theophylline in smokers patients.

Fluoxetine inhibits CYP2D6 CYP, This leads to the oppression of the metabolism of metoprolol and its cumulation, that could increase and cause action cardiodepressivne bradycardia. Case development lethargy.

Fluoxetine and mainly its metabolites are characterized by long T_1/2, so the likelihood of drug interaction is preserved even after a few days after fluoksetina.

There had been reports of a decrease in clearance of metoprolol from the body together with the use of ciprofloxacin.

If you are applying with ergotaminom possibly increasing violations of peripheral blood circulation.

Together with the use of estrogen diminishes antihypertensive activity metoprolol.

While applying metoprolol increases the concentration of ethanol in blood and lengthens its excretion.