Toprol XL
Toprol XL
Toprol XL (Metoprolol)Pharmacological action
The cardioselective blocker of b-adrenoreceptors which are not possessing internal sympathomimetic activity. Antihypertensive, antianginal and antiarrhytmic an effect has.
Blocking in low doses heart b1-adrenoreceptors, reduces intracellular current Ca2 +, renders negative hrono - dromo - batmo - and inotropic action.
Antihypertensive action is caused by reduction of warm emission and renin synthesis, oppression of activity a renin-angiotenzinovoj of system, restoration of sensitivity of baroreceptors of an aortic arch (there is no intensifying of their activity in reply to BP depression) and as a result reduction of peripheric sympathetic influences. Reduces raised by a BP in rest, at a physical strain and stress.
The BP decreases through 15 mines, is maximum - through 2 h; action remains during 6 h. Stable depression is observed after several weeks of regular reception.
The antianginal effect is defined by depression of requirement of a myocardium in oxygen as a result of CARDIAC CONTRACTIONS RATE reduction (elongation of a diastole and improvement of perfusion of a myocardium) and contractilities, and also depression of sensitivity of a myocardium to influence of a sympathetic innervation. Reduces frequency and gravity of attacks of a stenocardia and raises shipping of an exercise stress.
At long-term reception reduces the cholesterol maintenance in blood.
At application in average therapeutic doses has less expressed influence on the organs containing b2-adrenoreceptors (a pancreas, sceletal muscles, smooth muscles of peripheric arteries, bronchuses, uteruses) and on carbohydrate metabolism.
At application in high doses (more than 100 mg/sut) are rendered by blocking effect on both subtypes of b-adrenoreceptors.
Indications
- An arterial hypertensia (in monotherapy or in a combination with other antihypertensive preparations), including hyperkinetic type;
- An ischemic heart disease (secondary preventive maintenance of a myocardial infarction, preventive maintenance of attacks of a stenocardia);
- Disturbances of a rhythm of heart;
- A hyperthyroidism (as a part of complex therapy);
- Preventive maintenance of attacks of a migraine.
Dosage regimen
At an arterial hypertensia prescribe in a daily dose of 50-100 mg/sut in 1 or 2 receptions. At insufficient therapeutic effect probably gradual rising of a daily dose to 100-200 mg.
At a stenocardia, for preventive maintenance of attacks of a migraine prescribe in a dose of 100-200 mg/24h in 2 receptions (in the morning and in the evening).
For secondary preventive maintenance of a myocardial infarction prescribe in an average daily dose of 200 mg in 2 receptions (in the morning and in the evening).
At the functional disturbances of warm activity accompanied by a tachycardia prescribe in a daily dose of 100 mg in 2 receptions (in the morning and in the evening).
At elderly patients, patients with disturbances of function of kidneys, and also in need of carrying out of a hemodialysis of change of a regimen of dosage it is not required.
Tablets should be accepted inside during time or right after food intake. Tablets can be halved, but not to chew.
Side effect
From party TSNS and peripheric nervous system: undue fatigability, delicacy, a headache, retardation of rate of mental and impellent reactions; seldom - paresthesias in extremities, depression, anxiety, depression of ability to concentration of attention, drowsiness, a sleeplessness, dreadful dreamings, confusion of consciousness or short-term disturbance of memory, an asthenic syndrome, muscular delicacy.
From sense organs: seldom - sight depression, depression of secretion of a plaintive liquid, a conjunctivitis, a sonitus.
From cardiovascular system: a sinus bradycardia, palpitation, BP depression, an orthostatic hypotension; seldom - depression of contractility of a myocardium, time aggravation of symptoms of a chronic heart failure, an arrhythmia, intensifying of disturbances of a peripheric circulation (a cold snap of the bottom extremities), disturbances of conductivity of a myocardium; in single instances - AV-blockade, a cardialgia.
From the alimentary system: a nausea, vomiting, abdominal pains, a diarrhoeia, a constipation, dryness in a mouth, taste change; rising of activity of hepatic transaminases; seldom - a hyperbilirubinemia.
Dermatological reactions: an urticaria, a dermal itch, an eruption, a psoriasis exacerbation, psoriasiform changes of a skin, a dermahemia, an exanthema, a photodermatosis, diaphoresis intensifying, a reversible alopecia.
From respiratory system: difficulty of an exhalation (a bronchospasm at appointment in high doses or at predisposed patients), a dyspnea.
From endocrine system: a hypoglycaemia (at the patients receiving insulin); seldom - a hyperglycaemia.
From hemopoiesis system: a thrombocytopenia, an agranulocytosis, a leukopenia.
The other: a dorsodynia or joints, insignificant augmentation of mass of a body.
Contraindications
- A cardiogenic shock;
- AV-blockade II and III degrees;
- Sinuatrial blockade;
- The expressed bradycardia (the CARDIAC CONTRACTIONS RATE less than 50 ud./mines);
- A heart failure in a decompensation stage;
- An angiospastic stenocardia;
- The expressed arterial hypotension (a systolic BP below 100 mm hg);
- The lactemia period;
- Simultaneous reception of inhibitors MAO;
- Simultaneous i.v. verapamil introduction;
- A hypersensibility to Metoprolol and to other ingredients of a preparation.
With care it is necessary to prescribe a preparation at a diabetes, a metabolic acidosis, a bronchial asthma, chronic obstructive illness of lungs (an emphysema of lungs, a chronic obstructive bronchitis), obliterating diseases of peripheric vessels (an alternating lameness), hepatic insufficiency, chronic renal insufficiency, a myasthenia, a pheochromocytoma, AV-blockade of I degree, a thyrotoxicosis, depressions (including in the anamnesis), a psoriasis, and also at children and teenagers are elderly till 18 years and at patients of advanced age.
Pregnancy and lactemia
Application Toprol XL at pregnancy is possible only in that case when the prospective advantage for mother exceeds potential risk for a foetus. In need of preparation appointment during this period careful observation over a condition of a foetus and the newborn during 48-72 h after sorts as are possible a pre-natal growth inhibition, a bradycardia, an arterial hypotension, a respiratory depression, a hypoglycaemia is necessary.
Metoprolol influence on the newborn at feeding by a breast is not studied, therefore to the women Toprol XL accepting, it is necessary to stop thoracal feeding.
Special indicatings
At appointment of Toprol XL preparation is necessary to supervise the CARDIAC CONTRACTIONS RATE and a BP regularly. The patient should be warned, that at the CARDIAC CONTRACTIONS RATE less than 50 ud./mines are necessary consultation of the doctor.
At patients with a diabetes it is necessary to supervise regularly glucose level in blood and if necessary to spend correction of a dose of insulin or peroral hypoglycemic preparations.
Toprol XL appointment as the patient with a chronic heart failure probably only after achievement of a stage of indemnification.
At the patients Toprol XL accepting, intensifying of expression of reactions of hypersensitivity (against the burdened allergological anamnesis) and absence of effect from introduction of usual doses of Epinephrinum (adrenaline) is possible.
Against Toprol XL application aggravation of symptoms of disturbance of a peripheric circulation is possible.
Toprol XL is necessary to cancel gradually, consistently reducing its dose within 10 days. At the sharp termination of treatment there can be a withdrawal (intensifying of attacks of a stenocardia, BP rising). In cancellation of a preparation with a stenocardia it is necessary for patients to be under careful medical observation.
At an angina of exertion the picked up dose of a preparation should provide the CARDIAC CONTRACTIONS RATE in rest within 55-60 ud./mines, at a load - no more than 110 ud./minutes
The patients using contact lenses, should consider, that against treatment by beta adrenoblockers probably reduction of production of a plaintive liquid.
Metoprolol can mask some clinical implications of a hyperthyroidism (tachycardia). Sharp cancellation at patients with a thyrotoxicosis is contraindicative, as is capable to strengthen semiology.
At a diabetes Toprol XL reception can mask hypoglycaemia symptoms (a tachycardia, a sweating, BP rising).
At Metoprolol appointment with a bronchial asthma simultaneous application beta2-adrenomimetikov is necessary for patients.
At patients with pheochromocytoma Toprol XL is necessary to apply in a combination to alpha adrenoblockers.
Before carrying out of any surgical intervention it is necessary to inform the anaesthesiologist on spent Toprol XL therapy (a choice of a preparation for the general anaesthesia with the minimum negative inotropic action); preparation cancellations it is not required.
At preparation appointment elderly patients should supervise liver function regularly. Correction of a regimen of dosage is required only in case of occurrence in elderly patients of the accruing bradycardia, the expressed depression of a BP, AV-blockade, a bronchospasm, ventricular arrhythmias, serious disturbances of function of a liver. Sometimes it is necessary to stop treatment.
It is necessary to carry out the special control of a condition of patients with depressive disorders in the anamnesis. In a case development of depression Toprol XL is necessary to cancel.
Use in pediatrics
Efficiency and safety of Toprol XL application at children and teenagers is elderly till 18 years are not defined.
Influence on ability to driving of motor transport and to management of mechanisms
At the patients which activity demands special attention, a question on preparation appointment it is out-patient it is necessary to solve only after an estimation of individual reaction of the patient.
Overdosage
Symptoms: the expressed sinus bradycardia, giddiness, a nausea, vomiting, a cyanosis, an arterial hypotension, an arrhythmia, a bronchospasm, a syncope; at an acute overdosage - a cardiogenic shock, a loss of consciousness, a coma, AV-blockade up to development of full cross-section blockade and a cardiac standstill.
Overdosage first signs appear through 20 mines-2 h after reception.
Treatment: a gastric lavage, appointment of adsorbents, symptomatic therapy: at the expressed depression of a BP, in case of an acute arterial hypotension, a bradycardia and a menacing heart failure - i.v. (with an interval of 2-5 mines) introduction beta-adrenostimuljatorov or i.v. introduction of Atropini sulfas of 0 mg, in the absence of a positive effect - Dopaminum, Dobutaminum or Norepinephrinum. As the subsequent measures probably appointment of a glucagon of 1-10 mg. At a bronchospasm - i.v. introduction beta2-adrenostimuljatorov, at cramps - slow i.v. Diazepamum introduction. Metoprolol it is badly deduced by means of a hemodialysis.
Medicinal interaction
At simultaneous Toprol XL application with inhibitors MAO probably appreciable intensifying of hypotensive action. Between reception of inhibitors MAO and Toprol XL should make a break not less than 14 days.
Simultaneous i.v. verapamil introduction can provoke a cardiac standstill, simultaneous appointment of nifedipine leads to appreciable depression of a BP.
At simultaneous Toprol XL application with ergot alkaloids the risk of disturbances of a peripheric circulation amplifies.
At simultaneous Toprol XL application raises effect of peroral hypoglycemic preparations and insulin and raises risk of development of a hypoglycaemia.
At simultaneous Toprol XL application with antihypertensive agents, Sodium nitritums, blockers of calcium channels the risk of development of an arterial hypotension raises.
At simultaneous Toprol XL application with verapamil, antiarrhytmic preparations (Amiodaronum), Reserpinum, Clonidinum, agents for the general anaesthesia.
At simultaneous Toprol XL application strengthens action of curariform relaxants.
Toprol XL at simultaneous application reduces a clearance of xanthines, especially at patients with initially raised clearance of Theophyllinum under the influence of smoking.
At simultaneous Toprol XL application with the clearance of lidocaine decreases and concentration of lidocaine in plasma raises.
At joint application with ethanol the risk of the expressed depression of a BP is enlarged.
Conditions and periods of storage
B.Preparat's list should be stored in a place inaccessible to children at temperature from 15 to 25 C. The Period of validity - 5 years.
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