Brands of Nebivolol in Kenya
Nebi, Galaxy Pharmaceuticals Ltd
Nebibio, Sava Healthcare Ltd
Nebiem, MSN Laboratories Private Limited.
Nebilet, Menarini International Operations Luxembourg S.A
Nebiloc, Universal Corporation Limited
Nebilong, Micro Labs
Nebiring, Ravenbhel Healthcare Pvt. Ltd
Nebtas, Intas Pharmaceuticals Ltd
Nebiton, Medisel Kenya Ltd
Nodon, Cadila Pharmaceuticals (EA) Ltd
NEBIVOLOL MODE OF ACTION:
Nebivolol is a beta-1 adrenergic receptor antagonist with antihypertensive and vasodilatory activity. Nebivolol binds to and blocks the beta-1 adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure.
- Treatment of essential hypertension.
- Chronic heart failure (CHF)
- Treatment of stable mild and moderate chronic heart failure in addition to standard therapies in elderly patients ≥ 70 years.
DOSAGE AND ADMINISTRATION
The dose is 5 mg daily, preferably at the same time of the day.
The blood pressure lowering effect becomes evident after 1-2 weeks of treatment. Occasionally, the optimal effect is reached only after 4 weeks.
Combination with other antihypertensive agents
Beta-blockers can be used alone or concomitantly with other antihypertensive agents. To date, an additional antihypertensive effect has been observed only when Nebivolol 5 mg is combined with hydrochlorothiazide 12.5-25 mg.
Patients with renal insufficiency
In patients with renal insufficiency, the recommended starting dose is 2.5 mg daily. If needed, the daily dose may be increased to 5 mg.
Patients with hepatic insufficiency
Data in patients with hepatic insufficiency or impaired liver function are limited. Therefore the use of Nebivolol in these patients is contra-indicated.
In patients over 65 years, the recommended starting dose is 2.5 mg daily. If needed, the daily dose may be increased to 5 mg. However, in view of the limited experience in patients above 75 years, caution must be exercised and these patients monitored closely.
The efficacy and safety of Nebivolol in children and adolescents aged below 18 years has not been established. No data are available. Therefore, use in children and adolescents is not recommended.
Chronic heart failure (CHF)
The treatment of stable chronic heart failure has to be initiated with a gradual uptitration of dosage until the optimal individual maintenance dose is reached.
Patients should have stable chronic heart failure without acute failure during the past six weeks. It is recommended that the treating physician should be experienced in the management of chronic heart failure.
1.25 mg nebivolol, to be increased to 2.5 mg nebivolol once daily, then to 5 mg once daily and then to 10 mg once daily.
The maximum recommended dose is 10 mg nebivolol once daily.
Initiation of therapy and every dose increase should be done under the supervision of an experienced physician over a period of at least 2 hours to ensure that the clinical status (especially as regards blood pressure, heart rate, conduction disturbances, signs of worsening of heart failure) remains stable.
Patients with renal insufficiency
No dose adjustment is required in mild to moderate renal insufficiency since uptitration to the maximum tolerated dose is individually adjusted. There is no experience in patients with severe renal insufficiency (serum creatinine ≥ 250μmol/L). Therefore, the use of nebivolol in these patients is not recommended.
Patients with hepatic insufficiency
Data in patients with hepatic insufficiency are limited. Therefore the use of Nebivolol in these patients is contra-indicated.
No dose adjustment is required since uptitration to the maximum tolerated dose is individually adjusted.
The efficacy and safety of Nebivolol in children and adolescents aged below 18 years has not been established. Therefore, use in children and adolescents is not recommended. No data are available.
– Hypersensitivity to the active substance or to any of the excipients .
– Liver insufficiency or liver function impairment.
– Acute heart failure, cardiogenic shock or episodes of heart failure decompensation requiring i.v. inotropic therapy.
In addition, as with other beta-blocking agents, Nebivolol is contra-indicated in:
- Sick sinus syndrome, including sino-atrial block.
- Second and third degree heart block (without a pacemaker).
- History of bronchospasm and bronchial asthma.
- Untreated phaeochromocytoma.
- Metabolic acidosis.
- Bradycardia (heart rate < 60 bpm prior to start therapy).
- Hypotension (systolic blood pressure < 90 mmHg).
- Severe peripheral circulatory disturbances.
The following interactions apply to beta-adrenergic antagonists in general.
Combinations not recommended:
Class I antiarrhythmics (quinidine, hydroquinidine, cibenzoline, flecainide, disopyramide, lidocaine, mexiletine, propafenone): effect on atrio-ventricular conduction time may be potentiated and negative inotropic effect increased .
Calcium channel antagonists of verapamil/diltiazem type: negative influence on contractility and atrio-ventricular conduction. Intravenous administration of verapamil in patients with ß-blocker treatment may lead to profound hypotension and atrio-ventricular block .
Centrally-acting antihypertensives (clonidine, guanfacin, moxonidine, methyldopa, rilmenidine): concomitant use of centrally acting antihypertensive drugs may worsen heart failure by a decrease in the central sympathetic tonus (reduction of heart rate and cardiac output, vasodilation) . Abrupt withdrawal, particularly if prior to beta-blocker discontinuation, may increase risk of “rebound hypertension”.
Combinations to be used with caution
Class III antiarrhythmic drugs (Amiodarone): effect on atrio-ventricular conduction time may be potentiated.
Anaesthetics – volatile halogenated: concomitant use of beta-adrenergic antagonists and anaesthetics may attenuate reflex tachycardia and increase the risk of hypotension . As a general rule, avoid sudden withdrawal of beta-blocker treatment. The anaesthesiologist should be informed when the patient is receiving Nebivolol.
Insulin and oral antidiabetic drugs: although nebivolol does not affect glucose level, concomitant use may mask certain symptoms of hypoglycaemia (palpitations, tachycardia).
Baclofen (antispastic agent), amifostine (antineoplastic adjunct): concomitant use with antihypertensives is likely to increase the fall in blood pressure, therefore the dosage of the antihypertensive medication should be adjusted accordingly.
Combinations to be considered
Digitalis glycosides: concomitant use may increase atrio-ventricular conduction time. Clinical trials with nebivolol have not shown any clinical evidence of an interaction. Nebivolol does not influence the kinetics of digoxin.
Calcium antagonists of the dihydropyridine type (amlodipine, felodipine, lacidipine, nifedipine, nicardipine, nimodipine, nitrendipine): concomitant use may increase the risk of hypotension, and an increase in the risk of a further deterioration of the ventricular pump function in patients with heart failure cannot be excluded.
Antipsychotics, antidepressants (tricyclics, barbiturates and phenothiazines): concomitant use may enhance the hypothensive effect of the beta-blockers (additive effect).
Non steroidal anti-inflammatory drugs (NSAID): no effect on the blood pressure lowering effect of nebivolol.
Sympathicomimetic agents: concomitant use may counteract the effect of beta-adrenergic antagonists. Beta-adrenergic agents may lead to unopposed alpha-adrenergic activity of sympathicomimetic agents with both alpha- and beta-adrenergic effects (risk of hypertension, severe bradycardia and heart block).
As nebivolol metabolism involves the CYP2D6 isoenzyme, co-administration with substances inhibiting this enzyme, especially paroxetine, fluoxetine, thioridazine and quinidine may lead to increased plasma levels of nebivolol associated with an increased risk of excessive bradycardia and adverse events.
Co-administration of cimetidine increased the plasma levels of nebivolol, without changing the clinical effect. Co-administration of ranitidine did not affect the pharmacokinetics of nebivolol. Provided Nebilet is taken with the meal, and an antacid between meals, the two treatments can be co-prescribed.
Combining nebivolol with nicardipine slightly increased the plasma levels of both drugs, without changing the clinical effect. Co-administration of alcohol, furosemide or hydrochlorothiazide did not affect the pharmacokinetics of nebivolol. Nebivolol does not affect the pharmacokinetics and pharmacodynamics of warfarin.
Immune system disorders
angioneurotic oedema, hypersensitivity
Nervous system disorders
headache, dizziness, paraesthesia
bradycardia, heart failure, slowed AV conduction/AV-block
hypotension, (increase of) intermittent claudication
Respiratory, thoracic and mediastinal disorders
constipation, nausea, diarrhoea
dyspepsia, flatulence, vomiting
Skin and subcutaneous tissue disorders
pruritus, rash erythematous
Reproductive system and breast disorders
General disorders and administration site conditions
Reporting of suspected adverse reactions:
The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, email@example.com or clicking below button:
Clinical | Pharmacokinetic data
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