Metoprolol

Chemical name

({+})-1-[4-(2-Метоксиэтил)ф��нокси]-3-[(1-метилэтил)а мино]-2-пропанол (in the form of tartrate or succinate)

Gross

C15-H25-N-O3

Characteristics

Metoprolola tartrat : white, almost odourless crystalline powder dissolves easily in water, metilenhloride, chloroform and alcohol, poorly soluble in acetone, nerastvorim broadcast. Metoprolola succinate : white crystalline powder, readily soluble in water, soluble in methanol, sparingly soluble in ethanol - poorly soluble in dihlormetane and 2-propanole almost nerastvorim in etilazette, acetone, ether dietilovom and geptane.

Of drugs

The drugs-gipotenzivne, antianginalnoe, antiaritmicescoe. Does mostly бета_1-адренорецептор�� Heart does not have internal and simpatomimeticescoy �ембраностабилизирую��ей activity. Decreases heart and release Sad, slow heart rhythm, weakens the incentive effect on the rest miocard in physical activity and mental surges, warns fence ortostaticescuu tachycardia. Antihypertensive effect of a decrease in heart release and synthesis of renin, oppression activity ренин-ангиотензиново�� system and the central nervous system, the restoration of the sensitivity baroretseptorov and eventually reduced peripheral sympathetic influences. Gipotenzivny effect develops quickly (Sad lowered in 15 minutes, as in 2 hrs) and continued for six hours; to the reception metoprolola succinate-clinical effects blockade �ета_1-адренорецепторо в a 24-hour Dad slowly changing : a steady decline after a few weeks of regular admission. Antianginalny effect is a consequence of reducing the frequency and force of heart, energy costs and the needs of attack of oxygen. Down the frequency and severity of heart attacks, the death rate in patients with diagnostirovannam myocardial infarction increases the portability loads. Metoprolola succinate reducyruet risk of fatal outcome (including sudden death) re-emergence of a heart attack (eg, patients with diabetes mellitus), and improves the quality of life of patients with acute myocardial infarction and idiopathic cardiomiopatiei dilatation. Antiaritmicescoe activity is manifested in the removal of aritmogennah sympathetic affects the vascular system of the heart, sinusovogo slow rhythm and the speed of bringing the AV node, automatic braking and refrakternogo extension period. Provides moderate inotroponoe negative effect. Cardioseleguosti remains in the use of daily doses of less than 200 mg. The distinguishing between бета_1-адренорецептор�� theoretically reduces the risk of bronchospasm (in patients with bronchial asthma decreased less vital function of the lung), gipoglikemii and narrow peripheral Sosudov.v experiments on dogs (up to 105 mg / kg / day, for 1 year), rats (up to 800 mg / kg / day, within 2 years), and mice (up to 750 mg / kg / day, for 21 months) signs of carcinogenicity is detected, but identified histological changes in the type hyperplasia of liver cells and induration macrofagami lung tissue. In imposing masham-albinosm in doses up to 750 mg / kg / day for 21 months increased with the females frequency sound development Adenomas lungs, but repetition of the experience of the increase in the frequency of tumors has been noted. Test results dominant lethal mutations in mice, the study of chromosomes somatic cells test abnormalities somatic cell nuclear transfer interfaze et al showed no mutagenic properties. In rats receiving doses of 55.5 times the maximum daily dose for humans (450 mg) influence fertility and increased rates postimplantatini death and decreased survival of newborn animals (signs teratogenicity �тсутствовал).Метопро��ола tartrat quickly and almost entirely (95%) absorbed by ingestion, under heavy presistemnomu metabolizmu. Bioavailability is about 50% in the first reception and rises to 70% during the second application. About 12% of contact albuminami blood plasma. Quickly distributed in the tissues, permeates through GEB (level in the central nervous system is 78% plasma concentration), placental barrier breast milk (concentrations higher than plasma). The volume of 5.5 l / mm C_max achieved in 1-2 h after administration, the level in the blood varies considerably. T_1/2, from 3 to 7 p.m. Biotransformiroetsa in liver, with the formation of two active metabolites. Report the news is in the form of metabolites, Cl-1 l /

Indications

Arterial hypertension temperate and moderate (monotherapy or in combination with other hypotensive drugs), disease, giperkineticeski cardialny syndrome, the heart rhythm (sinusova tachycardia, and ventricular supraventrikuliarnaya Already, including paroxysmal tachycardia, tachycardia supraventrikuljarnuu, ekstrasistoliu, fibrillation and began predserdy, predserdnuu tachycardia), gipertrofica cardiomyopathy, mitral prolapse valve myocardial infarction (prevention and treatment), migraine (prevention), thyrotoxicosis (complex therapy); akatizia treatment, by neiroleptikami.

Restrictions on the use of

Diabetes mellitus, hypoglycaemia, coupled allergic history, metabolic disorders, bronchial asthma, emphysema, bronchitis neallergicaki, Ray, psoriasis, feohromotsytoma, of the liver and / or kidneys, male, depression, a general anaesthesia, elderly and child.

Pregnancy and lactation

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

Contraindications

Hypersensitivity, AV blockade II and III extent sinoatrialnaya blockade acute or chronic (under decompensation) cardiac failure, syndrome weakness sinusnogo hub expressed sinusova aetiology (HR least 60 u. / min), cardiogenny shock Arterial gipotenzia (Sad less than 100 mm Hg), expressed human peripheral blood circulation, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : not less than 10% weakness; 1-9,9% dizziness and headache; 0.1-0.9% decrease in concentration, drowsiness / insomnia, nightmares, depression, muscular convulsions, paresthesia; 0,01-0,09% nervousness, anxiety, relaxation Yeah, impaired vision, xeroftalmia, conjunctivitis; less than 0.01% lethargy, increased fatigue, anxiety, sputannosti consciousness, �мнезия/кратковременн ая memory loss, hallucinations, noise in the winter, the taste Oshchutmeni.so the circulatory system and blood (blood, gemostaz) : 1-9,9% aetiology, heart, gipotenzia, cooling limbs; in the 0.1-0.9% cardiac insufficiency, AV blockade otechny syndrome, pain in the chest; in 0,01-0,09% decline sokratimosti infarction, arrhythmia, less than 0.01% gangrene (in patients with severe human peripheral blood circulation); the conductivity attack sinkope, thrombocytopenia, lakopenia, Agranulozitoz.so part of the intestine : 1-9,9% nausea, pain in the abdomen, diarrhoea or constipation; 0.1-0.9% vomiting; 0,01-0,09% dryness in the mouth, a breach of the liver; flatulence, neuralgia, aches, Gepatit.so the respiratory system : smoking (1-9,9%), bronhospazm (0.1-0.9%), rhinitis vazomotornyi (0,01-0,09%), Despnoe.so the Skin : 0.1-0.9% rashes, dystrophic skin lesions; 0,01-0,09% obratimaya alopecia; less than 0.01% photosensitization, and the exacerbation of psoriasis; itch, erythema, urticaria, Gipergidros.prochie : reducing body mass index (0.1-0.9%), artralgia, arthritis, mialgia, muscle weakness, Peyroni disease.

Specific guidance

The treatment may change the results of tests in the laboratory (more urea transaminaz, phosphatases, LDG).

Patient interaction

Hypotension potenziruut simpatolitiki, nifedipin, nitroglycerin, dioretiki, apressin etc. gipotenzivee drugs. Antiarrhythmic and anaesthetic to increase the risk of developing bradikardii, adults, hypotension. Anti naperstanki potenziruut slower AV conduction. Also in / in the introduction and verapamila diltiazema could trigger stops the heart. Beta-adrainomimetiki, eufillin, cocaine, estrogena, indometacin, etc. NPVS weaken antigipertenzivny effect. Enhance and prolong the antidepoliarizuth miorelaksantov. The combination with alcohol leads to the mutual reinforcement of depressive effect on the central nervous system. Allergens increase the risk of severe systemic allergic reactions or arginine. Changes effectiveness of insulin and oral protivodiabeticakih and increases the risk of gipoglikemii. Antatsida, gidralazina, oral contraceptives, zimetidin, ranitidine, fenotiazina raise metoprolola level in the blood, rifampicin - reduces. Cl reduces lidocaine, efficiency бета_2-адреномиметико�� (to increase the dose). Incompatible with MAO inhibitors type A.

Overdosing

Symptoms : arterial gipotenzia, acute cardiac insufficiency, aetiology, cardiac arrest, AV blockade cardiogenny shock bronhospazm, breathing problems and consciousness / coma, nausea, vomiting, Generalized convulsions, zianoz (seen in 20 min to 2 h after administration). Treatment : washing stomach, symptomatic therapy : introduction of atropine sulfate (in / in a rapidly 0.5-2 mg), with bradikardii and violating AV conduction; glukagona (1-10 mg in / in, then / in drip 2-2.5 mg / h) and dobutamina, in the case of reducing sokratimosti attack; adrenomimetikov (noradrenalin, adrenaline, etc.), with arterial hypotension; diazepam (in / in slowly) for the convulsing; beta-adrainomimetikov inhalation or / with the introduction of jet eufillina for cupping bronhospasticeskih reactions; cardiostimulyatsia.

Precautions

In patients with chronic heart failure may deterioration of uterine diseases, requiring the use of cardiac glycosides and / or dioretikov with close monitoring gemodinamicheski status. In the case of a growing bradikardii or AV blockade, it is necessary to reduce dose or / with a atropine. Against the backdrop of diabetes mellitus and hyperthyroidism metoprolol may mask tachycardia caused gipoglikemiei or thyrotoxicosis. In patients with diabetes need a correction protivodiabeticakih doses of drugs, and close monitoring of the fast. In the background, the treatment of surgical intervention, to the choice should be an anaesthetic with the least negative effect inotrope. Perhaps a stronger reaction of гиперчувствительност и and the lack of therapeutic effect of conventional doses of epinephrine in the face aggravated allergologicaki history. In a simultaneous treatment of Clonidine, metoprolol thus gradually, a few days before the clonidine because of the risk of developing heavy gipertoniceski kriza. Patients who are feohromotsytoma use only in conjunction with alfa-adrainolitikami. Admission metoprolola out for 2-3 days before (the risk of bradikardii, hypotension and gipoglikemii their baby), exceptionally newborn after delivery should be within 48 to 72 hours under medical supervision. It should refrain from the use in paediatric practice, since safety and efficacy of their use in children has not been quantified. Denial of medical treatment to reduce the dose to be phased in over 10 to 14 days. Patients with the disease should that period be under the close supervision of a physician. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside (during or after delivery, with liquid squeezed liquid one morning, or the morning and evening (with dwurazovom admission), in / 386/1989 As antianginalnogo, antigipertenzivnogo and antiaritmicski funds in giperkineticescom syndrome metoprolola tartrat appointed interior in the dose of 100-200 mg 2-3 admission, as appropriate, dose increases with weekly intervals up to 450 mg / sut. The acute period of myocardial infarction on monitoring AD heart rhythm and ECG are three bolusnykh in / with injections of 5 mg to dvukhmintnami interruptions (total dose 15 mg) with good endurance in 15 minutes after the last injection appointed to the interior of 25-50 mg every 6 h for 48 p, then on the 100 mg twice a day (morning and evening) for a period of 3 months to 3 years. You can use metoprolola succinate dose remains the same. To prevent migraine attacks, the interior of 50-100 mg 2-4 every Sutki.metoprolola succinate in heart, hypertension, aritmiah, functional disorders of the heart, accompanied by shortness appointed interior in the dose of 50 mg once a day, for the prevention of migraines and 200 mg once a day. dose increase no earlier than one hour, after development maximum effect.

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