SELOKEN ® is a drug based on metoprolol tartrate
THERAPEUTIC GROUP: Beta-blockers
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications SELOKEN ® Metoprolol tartrate
SELOKEN ® is indicated for the treatment of arterial hypertension, angina pectoris, acute myocardial infarction and arrhythmias, with the exception of bradyarrhythmias.
SELOKEN ® can also be used as a therapeutic support in hyperthyroidism.
Mechanism of action SELOKEN ® Metoprolol tartrate
Metoprolol, the active ingredient contained in SELOKEN ® taken orally, is rapidly and completely absorbed at the gastro-enteric level, reaching its maximum plasma peak after about an hour and a half, with concentrations halved compared to the total dose taken (for important first-pass metabolism suffered by the drug).
The remaining share acts, at therapeutic concentrations, selectively on cardiac Beta 1 receptors, inhibiting them and reducing the activation induced by catecholamines. This biological mechanism takes the form of the negative inotropic and chronotropic effect, which guarantees a reduction in the heart rate, the intensity of contraction of the myocardium and in general of cardiac work. These assumptions are the basis of the therapeutic action of SELOKEN ® which, in addition to guaranteeing a reduction in angina attacks, a regulation of the heart rate, a better tolerance to physical effort and a better coronary perfusion, also allows a significant lowering of blood pressure both in orthostatic and clinostatic position.
After its action, given the half-life of about 3/5 hours, the metoprolol is eliminated in hydroxylated form mainly through the urine.
Studies carried out and clinical efficacy
METOPROLOL AND SIBUTRAMINE
Sibutramine is a drug traditionally used in the treatment of obesity, but often associated with palpitations and hypertension. The data show that the concomitant administration of metoprolol can significantly reduce the incidence of hypertension and palpitations, increasing patients' compliance with treatment.
2.METOPROLOL IN THE TREATMENT OF HYPERTENSION
This study, performed on almost 22, 000 patients with moderate hypertension, tested the efficacy of administering 100 mg daily metoprolol for four weeks. The results, quite positive, show that in 85% of cases an average pressure drop was observed from 162/95 mmHg to 148/87 mmHg, with excellent tolerability for about 94% of patients.
3.LIMITES OF NON-VASODILATING BETABLOCCANTS
The antihypertensive and cardioprotective effects of cardioselective beta-blockers, not vasodilators, such as metoprolol are known. Despite this therapeutic role, these active ingredients do not guarantee a significant reduction in the thickness of the intimate and medium tunic, much less a vasoprotective effect. Also for this reason, the need arose to experiment with third-generation beta-blockers in clinical practice, which in addition to the aforementioned effects seem to guarantee an important antioxidant action necessary for vascular protection.
Method of use and dosage
SELOKEN ® 100 mg tablets of metoprolol tartrate or 200 mg of prolonged release metoprolol: in the treatment of hypertension, the recommended dosages involve the use of one or two 100mg tablets of metoprolol per day. The precise dose and the treatment period should be established by the physician based on the physio-pathological conditions of the patient and his response to therapy.
In the treatment of cardiac arrhythmias, angina pectoris and infarct, the expected daily dosage varies from one to three tablets, and it is the duty of the doctor to establish the useful dose.
The injectable preparation of metoprolol is exclusively pertinent to the hospital, and should be subsequently followed by a maintenance carried out with tablets.
IN ANY CASE, BEFORE TAKING SELOKEN ® Metoprolol Tartrate - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.
Warnings SELOKEN ® Metoprolol tartrate
Given the high selectivity to the normal therapeutic dosage, and the moderate lipophilicity that prevents SELOKEN ® from reaching the respiratory tract, it is possible to extend its use also to patients with airway diseases, subjected to beta 2 agonist drug therapy.
Similarly, SELOKEN ® could be used in patients with heart failure, as long as they are adequately treated before and during therapy.
Although metoprolol is a cardioselective antagonist of Beta 1 receptors, it is possible, albeit minimally, that the active ingredient interferes with glucose metabolism, masking some signs and symptoms of hypoglycemia.
Particular attention is required before surgery, as the anesthetic drugs used in the operating room could accentuate the negative inotropic effect of metoprolol, and seriously jeopardize the patient's health. Therefore, it would be advisable to promptly notify the anesthesiologist or arrange for the suspension of therapy in useful times. It is necessary to remember that in case of suspension of therapy, it is advisable to provide for a gradual decrease in dosage, in order to avoid reactive reactions, potentially harmful.
SELOKEN ® contains lactose, therefore it may cause side reactions of gastrointestinal interest in patients suffering from intolerance to glucose / galactose or from lactase enzyme deficiency.
Metoprolol does not seem to interfere with normal driving and motor vehicle use skills.
PREGNANCY AND BREASTFEEDING
Like other antihypertensive drugs, even in the absence of adequate clinical literature, it is advisable to avoid the administration of metoprolol during the entire pregnancy, in order to avoid the appearance of hemodynamic and cardiovascular effects dangerous for the health of the fetus.
Although therapeutic doses of SELOKEN ® do not appear to reach concentrations of metoprolol harmful to the newborn in breast milk, it is advisable to suspend breast-feeding during therapy with this drug.
Interactions
Metoprolol undergoes a hepatic first pass metabolism, supported by particular cytochrome P450 isoforms; therefore, molecules capable of interacting with this enzyme could alter the normal concentrations of metoprolol and make the therapeutic response unpredictable. More precisely, antiarrhythmics, antidepressants, antipsychotics, COX-2 inhibitors, alcohol and hydralazine could increase metoprolol concentrations, while rifampicin may decrease them.
Calcium channel blockers such as verapamil or diltiazem, and antiarrhythmics could increase the negative inotropic and chronotropic effect, while concomitant administration of digitalis glycosides could increase atrioventricular conduction time and determine bradycardia.
In patients receiving concomitant hypoglycemic therapy, the dosage may need to be adjusted, given the effect of metoprolol on carbohydrate metabolism.
Contraindications SELOKEN ® Metoprolol tartrate
SELOKEN ® is contraindicated in case of hypersensitivity to one of its components, in case of bradycardia, high-grade atrioventricular block, heart failure not responsive to digital therapy or inadequately treated, cardiogenic shock, in therapy with beta-receptor agonists, and in case of renal failure or impaired renal function.
Undesirable effects - Side effects
SELOKEN ® seems to be well tolerated, even if especially during the initial phase of treatment increases the incidence of gastro-intestinal disorders, sleep disorders, fatigue, fatigue, bradycardia and cold extremities.
Less frequent were cases of thrombocytopenia, hypotension, bradycardia, granulocytopenia, bronchospasm, reduction of cardiac function and hypersensitivity reactions, for which it was necessary to suspend therapy. In any case the suspension of treatment should take place gradually, especially in those patients with deterioration of cardiac function.
Note
SELOKEN ® can be sold only under medical prescription.
The use of SELOKEN ® in athletes, in the absence of therapeutic necessity, to reduce the physiological response to stress and the related symptoms (tremor of the limbs, increase in blood pressure, increase in emotional tension, etc.) is a DOPANT practice.
