Metoprolol - instructions for use, dose, side effects, contraindications

Selective β₁-blocker, which does not have internal sympathomimetic activity. Has antihypertensive, antiarrhythmic, antianginal action. In therapeutic doses does not affect the tone of peripheral arteries.

Reduces the effect of catecholamines on the heart muscle, thereby reducing the heart rate, minute and shock volumes of blood within 24 hours.

Eliminates the effects of arrhythmogenic factors: tachycardia, arterial hypertension, increased content of cyclic AMP.

Antianginal action is due to a decrease in myocardial oxygen demand with prolonged diastole and improved perfusion of the heart muscle.

Pharmacokinetics:

The maximum concentration is achieved in 2-4 hours.

It binds to plasma proteins up to 16%. Poorly penetrates the blood-brain barrier, penetrates the placenta.

The half-life is 3-7 hours. Partially metabolized in the liver, eliminated by the kidneys: 5% unchanged and 95% - in the form of metabolites. When hemodialysis is not excreted from the blood plasma.

Indications:

It is used for the treatment of arterial hypertension, as well as for the prevention of arrhythmia and migraine attacks.

ICD-10

V.F40-F48.F45 Somatoform disorders

VI.G40-G47.G43 Migraine

IX.I20-I25.I21.90 Acute myocardial infarction, unspecified with hypertension

IX.I10-I15.I10 Essential [primary] hypertension

IX.I30-I52.I47.1 Nadzheludochkovaya tachycardia

IX.I30-I52.I49.4 Other and unspecified depolarization

Contraindications:

Cardiogenic shock, atrioventricular blockade of II-III degree, bradycardia, chronic cardiac insufficiency, resistant to the action of cardiac glycosides, bronchial asthma, renal and hepatic insufficiency.

Individual intolerance.

Carefully:

Chronic bronchitis with an asthmatic component, obliterating arterial diseases, atrioventricular blockade of the 1st degree, disturbance of the water-electrolyte balance.

Pregnancy and lactation:

Recommendations for FDA - Category D without teratogenicity. Not applicable in pregnancy and lactation.

Dosing and Administration:

Inside: on 100 mg / day in 1-2 reception. If necessary, the dose increases to 200 mg / day.

Intravenous injection: 2-5 mg, repeated administration is possible after 5 minutes.

The highest daily dose: inside - 400 mg; intravenously - 20 mg.

The highest single dose: inside - 200 mg; intravenously - 5 mg.

Side effects:

Central nervous system: dizziness, insomnia, asthenia.

Respiratory system: shortness of breath, rarely - bronchospasm

The cardiovascular system: bradycardia, atrioventricular blockage, cold extremities.

Blood System: neutropenia, thrombocytopenia.

Sense organs: "dry eye syndrome", transient visual impairment.

Gastrointestinal tract: dyspepsia, diarrhea, or constipation.

Reproductive system: lowering the potency.

Leather: hyperhidrosis.

Allergic reactions.

Overdose:

Symtomas: pronounced bradycardia, arterial hypotension.

Treatment: intravenously 1-2 mg. atropine, 2.5 μg / kg dobutamine, intravenously bolus 10 mg glucagon, intravenously drop 10-20 μg isoprenaline at a rate of not more than 5 μg / min.

Interaction:

Increases the concentration of ethanol in the blood and lengthens its excretion.

Potentiates the effect of lidocaine in systemic application.

Negative dromo-, foreign, chromotropic influences are intensified with simultaneous admission with amiodarone, anesthetics, antiarrhythmics, digoxin, diltiazem, verapamil.

Increases the bioavailability of metoprolol together with cimetidine.

Special instructions:

Discontinue taking the drug gradually (for 8-10 days).

Before an operative intervention it is necessary to inform the anesthesiologist about taking the drug by the patient.

Instructions

Metoprolol (Metoprololum)