CONCOR ® is a bisoprolol emifumarato drug.
THERAPEUTIC GROUP: Beta-blockers
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications CONCOR ® Bisoprolol
CONCOR ® is used in the treatment of high blood pressure and angina pectoris.
Mechanism of action CONCOR ® Bisoprolol
Bisoprolol, taken through CONCOR ®, is absorbed for more than 90% in the intestine, and metabolized only to a small extent in the liver. Linked to 30% of the total plasma protein intake, it reaches the heart, where it has a high affinity for Beta 1 adrenergic receptors.
This active ingredient, in fact, is a classic cardioselective beta-blocker that does not present any type of activity on vascular and bronchial smooth muscle, nor intrinsic sympathomimetic activity.
Its therapeutic action is therefore mainly due to the inhibitory action on the cardiac Beta 1 receptors, with a consequent negative inotropic and chronotropic effect, which allows both to reduce the cardiac work and to improve the coronary reperfusion. The antihypertensive action for this pharmaceutical category has not yet been well characterized, although experimental evidence shows a significant reduction in plasma renin activity (enzyme involved in the renin-angiotensin-aldosterone pathway), while the antianginal action would be sustained precisely by the reduction of cardiac work and coronary circulation optimization.
After a somewhat prolonged half-life (10/12 hours), the drug is eliminated in equal parts through feces and urine.
Studies carried out and clinical efficacy
THE ANTIPERTENSIVE EFFECT OF BISOPROLOL
This study, conducted on 273 hypertension patients treated with 5 mg bisoprolol for 16 weeks, demonstrates the antihypertensive efficacy of this active ingredient. More precisely, the reduction in the observed systolic pressure was 16mmHg, with a responsiveness of 90% and an insignificant incidence of side effects.
2. THE EFFECTIVENESS OF BISOPROLOL IN INFLAMMATORY PATHOLOGY
Bisoprolol appears to be effective not only in the treatment of hypertension, but also in inflammatory pathology. This study, conducted on 67 patients, showed that the secretion of inflammatory cytokines could significantly decrease during therapy with this active ingredient. The described action could be particularly important in the prevention of systemic and non-systemic pathologies on an inflammatory basis.
3.THE COMBINED HYPERTENSION THERAPY
Several studies support the particular efficacy of the low-dose combination of bisoprolol and hydrochlorothiazide. In particular, the combined therapy seems not only more effective than monotherapy, but also able to guarantee the achievement of the therapeutic standard in less time without clinically relevant side effects.
Method of use and dosage
CONCOR ® 5mg / 10mg bisoprolol emifumarato tablets: the standard dose used in the treatment of arterial hypertension and angina pectoris is that of 5mg a day. In the event of reduced efficacy, and after a careful clinical evaluation, the doctor may decide to double the daily dose.
The intake should be carried out on a full stomach, whereas discontinuation of therapy should be done by gradually reducing the dose.
IN ANY CASE, BEFORE TAKING CONCOR ® Bisoprololo - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.
Warnings CONCOR ® Bisoprolol
CONCOR ®, like other beta-blockers, has important metabolic and cardiovascular effects that could be potentially dangerous for particular categories of patients at risk. For example, the bradycardic action of bisoprolol could mask some side effects of hypoglycemia and hyperthyroidism, hiding important signs for diagnostic and therapeutic purposes. The same action could be accentuated and become dangerous in the case of concomitant administration of anesthetic and muscle relaxants; therefore, it would be advisable to suspend therapy before surgery.
The suspension of CONCOR ® therapy should be carried out gradually, in order to avoid particularly evident reactive responses in cardiac patients and those suffering from first degree heart block, peripheral circulatory diseases or Prinzmetal angina.
Although bisiprolol is a selective beta-blocker, high concentrations may also have an effect on bronchial smooth muscle beta 2 receptors, causing bronchospasm in patients with bronchopathy.
Bisoprolol appears to increase sensitivity to allergens, worsening the symptoms in predisposed patients.
Unexpected reactions and side effects such as dizziness, drowsiness and headache, could reduce the patient's normal perceptual abilities and make the use of machinery or driving vehicles dangerous.
PREGNANCY AND BREASTFEEDING
CONCOR ® is contraindicated during the entire period of pregnancy, as it could be responsible for hemodynamic events that could compromise normal placental perfusion and cause problems with the development of the fetus. Moreover, at the time of delivery, the metabolic effects of bisopropole could determine hypoglycemia and bradycardia, with serious repercussions on the health of the fetus.
The absence of data on the possible secretion of this active ingredient in breast milk suggests avoiding intake even during lactation, or suspending it in the event of therapy.
Interactions
The cardioselective Beta blockers, therefore also the bisoprolol, can interact with numerous other active principles, determining a significant variation of the therapeutic efficacy.
More precisely, class II and III antiarrhythmics, calcium antagonists such as verapamil / diltiazem, centrally acting antihypertensives, halogenated anesthetics-volatiles, digitalis glycosides, clonidine, antipsychotics and antidepressants, are able to determine an increase in the biological effects of the drug with possible hypotension.
In the case of diabetic patients undergoing hypoglycemic therapy, it may be necessary to resort to a dosage adjustment following constant monitoring of blood glucose.
CONCOR ® could also cause an increase in the depressive action of alcohol, analgesics and antihistamines.
Contraindications CONCOR ® Bisoprolol
CONCOR ® is contraindicated in cases of hypotension, respiratory diseases and bronchopathies, pheochromocytoma, metabolic acidosis, cardiogenic shock, bradycardia, acute or chronic inadequately treated heart failure and hypersensitivity to one of its active ingredients.
Undesirable effects - Side effects
Studies in the literature and data from clinical experience highlight the appearance of side effects especially in the initial phase of therapy. Among the most frequent adverse reactions were fatigue, fatigue, dizziness, headache, feeling of cold and tingling in the extremities, nausea, vomiting, diarrhea and constipation. There were less frequent cases of weakness, cramps, bradycardia, hypotension, depression.
Changes in haemato-clinical parameters have been observed only in a few cases, for which the suspension of therapy has rebalanced these values.
Note
CONCOR ® is salable only under medical prescription.
The use of CONCOR ® in athletes, in the absence of therapeutic need, 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.
