LOBIVON ® is a nebivolol-based drug
THERAPEUTIC GROUP: Beta-blockers
Indications LOBIVON ® Nebivolol
LOBIVON ® is used in the treatment of essential hypertension and chronic heart failure of mild, moderate and stable degrees.
Mechanism of action LOBIVON ® Nebivolol
Nebivolol, taken through LOBIVON ® is absorbed in the gastrointestinal tract and readily metabolized in the liver by cytochromial enzymes. The metabolic processes that this active ingredient undergoes depend on the CYP2D6 enzyme, whose activity is strictly influenced by gene variants of the same protein. For this, bioavailability, time to reach maximum plasma concentration and half-life will vary between slow and rapid metabolisers. although the "rapid" polymorphism appears to be the most frequent in the population.
Nebivolol is a latest generation cardioselective beta-blocker, which combines the classic mechanism of selective inhibition of beta 1 adrenergic receptors expressed in the heart with an evident vasodilating action, determined by the induction of the arginine-nitric oxide pathway, with increased concentrations of this last molecule at the level of the intimate arteriolar tunic.
The reduction of the frequency and intensity of myocardial contraction, the improved coronary perfusion, the reduction of cardiac action and the innovative vasodilatory action make nebivolol one of the most effective beta-blockers in antihypertensive therapy.
The metabolites of nebivolol, both hydroxylated and glucuronated, are eliminated in more or less similar parts in the urine and faeces.
Studies carried out and clinical efficacy
NEBIVOLOLO, A NEW GENERATION BETA-BLOCKER
Eur J Pharmacol. 2005 Jan 31; 508 (1-3): 159-66. Epub 2005 Jan 7.
The cellular mechanisms involved in the vasodilator effect of nebivolol on the renal artery.
Georgescu A, Pluteanu F, Flonta ML, Badila E, Dorobantu M, Popov D.
Nebivolol represents one of the new generation beta blockers, as it associates an important vasodilatory action with the inhibitory effect on cardiac beta 1 adrenergic receptors. The study of the molecular mechanisms of vasodilation, which make this active ingredient one of the most effective beta blockers in the treatment of high blood pressure, has shown an "activation of the beta 1 receptors of vascular smooth muscle and an increase in the activity of nitric oxide synthetase with a consequent increase in nitric oxide concentrations.
2.L "ANTIPERTENSIVE EFFECTIVENESS OF NEBIVOLOLO
Ther Adv Cardiovasc Dis. 2010 Dec; 4: 349-57.
Efficacy and safety of nebivolol in Hispanics with stage I-II hypertension: a randomized placebo-controlled trial.
Punzi H, Lewin A, Lukic T, Goodin T, Wei Chen.
This study tests the efficacy of nebivolol in the treatment of hypertension in about 300 patients. The data obtained show a reduction in diastolic pressure of about 11mmHg and of systolic pressure of 14mmHg, in patients with grade I and II hypertension, treated for 8 weeks with nebivolol.
3.NEBIVOLOLO: PROTECTIVE EFFECT
J Hum Hypertens. 2010 Apr 8.
Effects of nebivolol in obese African Americans with hypertension (NOAAH): markers of inflammation and obesity in response to exercise-induced stress. Merchant N, Rahman ST, Ferdinand KC, Haque T, Umpierrez GE, Khan BV.
Very interesting study conducted on obese patients subjected to intense physical exercise, useful for observing the protective effects of nebivolol on the patient's health. More precisely, the administration of this active ingredient for 8 weeks, at therapeutic doses, guaranteed a reduction in pro-inflammatory cytokines and leptin, and an increase in adiponectin, exerting a protective effect against the inflammatory stress induced by exercise. intense physique.
Method of use and dosage
LOBIVON ® 5mg tablets of nebivolol in racemic form: the standard dosage for the treatment of hypertension is one tablet per day, preferably taken at the same time. For elderly patients or patients with reduced renal function the starting dosage should be halved. The therapeutic effect appears 1-2 weeks after " start of treatment, while maximum effectiveness is observed only after 4 weeks.
For the treatment of chronic heart failure, it is not possible to define an optimal dosage a priori, as close medical supervision is necessary, useful for defining the effective therapeutic dose based on the physio-pathological characteristics of the patient.
IN ANY CASE, BEFORE TAKING LOBIVON ® Nebivolol - YOU NEED THE PRESCRIPTION AND CONTROL OF YOUR DOCTOR.
LOBIVON ® Nebivolol warnings
The "intake of LOBIVON ® must" be preceded by careful anamnestic and clinical evaluations, in order to avoid the onset of unpleasant side effects.
In detail, the bradycardic action of nebivolol could be accentuated by the concomitant administration of drugs active on the cardiovascular system or anesthetics, so as to require the suspension of therapy; it could also mask some important signs, such as tachycardia in pathologies of endocrine interest such as diabetes. and "hyperthyroidism.
Furthermore, even considering this active ingredient a cardioselective beta-blocker, at high concentrations it could interact with the adrenergic receptors of the respiratory tract, inducing bronchial constriction and aggravating the symptoms in patients with bronchopathies.
Particular attention should also be paid to patients suffering from particular cardiac pathologies or not properly treated (first degree heart block, peripheral circulatory pathologies, Prinzmetal's angina).
Nebivolol appears to increase sensitivity to allergens, worsening symptoms in predisposed patients.
If it is necessary to suspend the therapy, this should take place gradually, especially in patients with various types of heart disease.
LOBIVON ® contains lactose, therefore it is not recommended for use in patients with glucose / galactose malabsorption or lactase enzyme deficiency.
PREGNANCY AND BREASTFEEDING
The haemodynamic effects induced by LOBIVON ®, in particular the reduced placental perfusion, could compromise the normal embryonic and fetal development, and cause clinically relevant metabolic decompensations; for these reasons it is not recommended to take LOBIVON ® during pregnancy.
The same indication also applies to the lactation period, given the presence of nebivolol in breast milk at significant concentrations.
Interactions
To the common interactions observed for the category of cardioselective beta-blockers - such as class II and III antiarrhythmics, calcium antagonists of the verapamil / diltiazem type, centrally acting antihypertensives, halogenated volatile anesthetics, digitalis glycosides, antipsychotics and antidepressants, capable of determining a increase in the biological effects of the drug - others are added, important in the variation of the pharmacokinetic properties of nebivolol. In particular, given the role of the hepatic enzyme CYP2D6, its inhibitors such as paroxetine, fluoxetine, thioridazine and quinidine could increase the plasma levels of nebivolol resulting in a greater risk of side effects.
Contraindications LOBIVON ® Nebivolol
Like other Beta-blockers, LOBIVON ® is contraindicated in case of hypersensitivity to one of its components, in case of hypotension, circulatory disorders, metabolic acidosis, inadequately treated pheochromocytoma, heart block or heart failure not adequately treated. , cardiogenic shock and liver failure.
Undesirable Effects - Side Effects
The most common side effects of LOBIVON ® include headache, dizziness, paraesthesia, dyspnoea, constipation, nausea, diarrhea, fatigue and edema.
Rarer, and observed mainly in particular categories of patients at risk, were side effects such as nightmares, vision changes, bradycardia, heart failure, slowed AV conduction / AV block, hypotension, bronchospasm, dyspepsia, flatulence, vomiting, pruritus, rash skin, impotence and depression.
The literature also describes some episodes of hallucinations, psychosis, confusion, cold / cyanotic extremities, Raynaud's phenomena, dry eyes and oculo-muco-cutaneous toxicity associated with nebivolol therapy.
Note
LOBIVON ® can only be sold under medical prescription.
"use of LOBIVON ® by athletes, in the absence of therapeutic need, to reduce the physiological response to stress and related symptoms (tremor of the limbs, increase in blood pressure, increase in emotional tension, etc.) constitutes a DOPANTE practice.
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