Metoprolol

When ATH:
C07AB02

Characteristic.

Metoprolol tartrate: white, practically odorless crystalline powder, soluble in water, methylene chloride, chloroform and alcohol, slightly soluble in acetone, insoluble in ether. Metoprolol succinate: white crystalline powder, easily soluble in water, Soluble in methanol, sparingly soluble in ethanol, slightly soluble in dichloromethane and 2-propanol, practically insoluble in ethyl acetate, acetone, diethyl ether and heptane.

Pharmacological action.
Gipotenzivnoe, antianginalnoe, antiarrhythmic.

Application.

Hypertension mild to moderate (monotherapy or in combination with other antihypertensives), CHD, hyperkinetic cardiac syndrome, irregular heartbeat (sinus tachycardia, ventricular and supraventricular arrhythmias, including paroxysmal tachycardia, supraventrykulyarnuyu tachycardia, extrasystole, atrial flutter and atrial fibrillation, atrial tachycardia), gipertroficheskaya cardiomyopathy, mitral valve prolapse, myocardial infarction (Prevention and treatment), migraine (prevention), thyrotoxicosis (Combination Therapy); treatment of akathisia, neuroleptic-induced.

Contraindications.

Hypersensitivity, AV блокада II и III степени, sinoatrialynaya blockade, acute or chronic (decompensated) heart failure, sick sinus syndrome, vыrazhennaya sinusovaya bradycardia (HR less 60 u. / min), cardiogenic shock, hypotension (Sad less than 100 mm Hg. Art.), expressed by peripheral circulatory disorders, pregnancy, lactation.

Restrictions apply.

Diabetes, gipoglikemiâ, otyahoschennыy allerholohycheskyy history, metabolic acidosis, bronchial asthma, эmfizema, non-allergic bronchitis, hyperthyroidism, psoriasis, pheochromocytoma, liver dysfunction and / or kidney, myasthenia, depression, general anesthesia, the elderly and children's age.

Pregnancy and breast-feeding.

Maybe, if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Side effects.

From the nervous system and sensory organs: no less 10% - Weakness; 1-9.9% - Dizziness and headache; 0,1-0.9% - Decreased concentration, drowsiness / insomnia, nightmares, depression, muscle cramps, paraesthesia; 0,01-0.09% - Nervousness, alarm, the weakening of the libido, blurred vision, xerophthalmia, conjunctivitis; less 0,01% - Lethargy, fatigue, anxiety, confusion, Amnesia / short-term memory loss, hallucinations, noise in ears, dysgeusia.

Cardio-vascular system and blood (hematopoiesis, hemostasis): 1-9.9% - Bradycardia, heartbeat, gipotenziya, cold extremities; to 0.1-0.9% - heart failure, OF блокада, edematous syndrome, chest pain; in 0,01-0,09% - reduction of myocardial contractility, Arrhythmia, less 0,01% - Gangrene (in patients with severe peripheral circulatory disorders); conduction disturbances infarction, syncope, thrombocytopenia, leukopenia, agranulocytosis.

From the digestive tract: 1-9.9% - Nausea, abdominal pain, diarrhea or constipation; 0,1-0.9% - Vomiting; 0,01-0.09% - Dry mouth, abnormal liver function; flatulence, dyspepsia, heartburn, hepatitis.

From the respiratory system: breathlessness (1–9,9%), bronchospasm (0,1–0,9%), vasomotor rhinitis (0,01-0.09%), dyspnoea.

For the skin: 0,1-0.9% - A rash, dystrophic skin changes; 0,01-0.09% - Alopecia obratimaya; less 0,01% - Photosensitivity, exacerbation of psoriasis; itch, эritema, hives, hyperhidrosis.

Other: weight loss (0,1–0,9%), arthralgia, arthritis, myalgia, muscular weakness, Peyronie's disease.

Cooperation.

Gipotenziю potenciruюt sympatholytic, nifedipine, nitroglycerin, Diuretic, hydralazine and other antihypertensive drugs. Antiarrhythmic and anesthetic agents increase the risk of bradycardia, Arrhythmia, gipotenzii. Digitalis drugs potentiate slow AV conduction. Simultaneous I / verapamil and diltiazem administration can cause cardiac arrest. Beta-adrenergic agonist, aminofillin, cocaine, Estrogens, indomethacin, and other NSAIDs weaken the antihypertensive effect. Boosts and prolongs the effect of muscle relaxants antidepolyarizuyuschih. The combination of alcohol leads to a mutual reinforcement of inhibitory effect on the CNS. Allergens increase the risk of severe systemic allergic reactions or anaphylaxis. It changes the effectiveness of insulin and oral antidiabetic agents and increases the risk of hypoglycemia. Antacids, oral contraceptives, cimetidine, ranitidine, phenothiazines - increase in blood levels of metoprolol, rifampicin - reduces. It decreases the clearance of lidocaine, effectiveness of beta₂-adrenomimetikov (necessary to increase the dose of the latter). Incompatible with MAO inhibitors type A.

Overdose.

Symptoms: hypotension, acute heart failure, bradycardia, cardiac arrest, OF блокада, cardiogenic shock, bronchospasm, respiratory failure and consciousness / coma, nausea, vomiting, generalized seizures, cyanosis (manifested through 20 min - 2 h after administration).

Treatment: gastric lavage, simptomaticheskaya therapy: atropine sulfate (I / fast 0.5-2 mg) - Bradycardia and AV conduction disorders; glucagon (1-10 Mg / in, then / drip 2-2.5 mg / h) dobutamine, and - in the case of reduction of myocardial contractility; adrenomimetikov (noradrenaline, adrenaline and others.) - With hypotension; diazepam (in / slow) - To eliminate seizures; inhaled beta-agonists or / bolus of aminophylline for relief bronchospastic reactions; kardiostimuljaцija.

Dosing and Administration.

Inside, I /. As antianginalnogo, antihypertensive and antiarrhythmic, hyperkinetic syndrome when metoprolol tartrate administered orally at a dose of 100-200 mg 2-3 reception, if necessary, dose increased at weekly intervals until 450 mg / day. In the acute phase of myocardial infarction under the monitoring of blood pressure, heart rate and ECG carried out 3 bolus in / on injection 5 at two-minute intervals mg (total dose 15 mg), with good endurance through 15 minutes after the last injection designate the interior of 25-50 mg every 6 h for 48 no, and then - 50-100 mg 2 once a day (in the morning and in the evening) during 3 Months - 3 years. When moving to metoprolol succinate dose remains the same. For the prevention of migraine attacks - inside of 50-100 mg 2-4 times a day.

Metoprolol succinate in CAD, hypertension, aritmijax, functional disorders of cardiac activity, accompanied by palpitations administered orally at a dose of 50-100 mg 1 once a day, for the prevention of migraine - 200 mg 1 once a day. The dose is increased not earlier, than 1 Sun, ie. after the development of maximum effect.

Precautions.

In patients with chronic heart failure may deteriorate myocardial contractility, necessitating the use of cardiac glycosides and / or diuretics, with close monitoring of hemodynamic status. In the case of increasing bradycardia or AV block is necessary to reduce the dose or / atropine. Diabetes mellitus and hyperthyroidism Metoprolol may mask tachycardia, cause hypoglycemia or hyperthyroidism. Patients with diabetes need dose adjustment of antidiabetic drugs, and careful monitoring of blood glucose levels. During the on-treatment surgery, the drug of choice should be the anesthetic with the least negative inotropic effects. Perhaps more significant development of hypersensitivity reactions and lack of therapeutic effect of conventional doses of epinephrine with aggravated allergic history. Upon termination of simultaneous treatment with clonidine, metoprolol lifted gradually, several days before clonidine, because of the risk of severe hypertensive crisis. In patients with pheochromocytoma application is possible only together with alpha-adrenolytics. Metoprolol stop for 2-3 days before delivery (the risk of bradycardia, hypotension and hypoglycemia in the newborn), in exceptional cases, newborns after birth have 48-72 hours to be under medical supervision. It should refrain from the use in pediatric practice, because the safety and efficacy of its use in children is not identified. If you cancel the treatment is necessary to reduce the dosage gradually over a period of 10-14 days. Patients with coronary artery disease in this period should be under close medical supervision. Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention.

Cautions.

During treatment may change the test results in laboratory studies (increase in urea, transaminases, fosfataz, LDH).

Cooperation