Nebivolol


Full Prescribing Info
Dosage/Direction for Use

Oral
Hypertension
Adult: Initially, 5 mg once daily. May increase dose at intervals of 2 wk if needed. Max: 40 mg once daily.
Elderly: >65 yr
Initially, 2.5 mg once daily increased to 5 mg once daily if required.
Renal impairment: Initially, 2.5 mg once daily. Maintenance: Increased to 5 mg once daily if required.

Oral

Heart failure
Adult: Initially, 1.25 mg once daily. May double dose every 1-2 wk if tolerated. Max: 10 mg once daily.
Administration
May be taken with or without food.
Contraindications
Sick sinus syndrome, 2nd or 3rd degree heart block (w/o pacemaker), decompensated cardiac failure, severe bradycardia, cardiogenic shock, untreated phaeochromocytoma, metabolic acidosis, severe peripheral circulatory disturbances, history of bronchospasm and bronchial asthma. Hepatic impairment.
Special Precautions
Patients w/ inadequate cardiac function, well-compensated heart failure, myasthenia gravis. Patients undergoing major surgery involving general anaesth. May mask signs and symptoms of hypoglycaemia and hyperthyroidism. Abrupt withdrawal may exacerbate angina symptoms and/or precipitate MI and ventricular arrhythmias in patients w/ coronary artery disease. Pregnancy and lactation. Monitoring Parameters Monitor ECG, BP and blood glucose in diabetic patients.
Adverse Reactions
Headache, paraesthesia, fatigue, asthenia, dizziness, diarrhoea, nausea, constipation, abdominal pain, insomnia, chest pain, bradycardia, dyspnoea, rash, and peripheral oedema, hypercholesterolaemia, hyperuricaemia, increased BUN, decreased HDL levels.
Overdosage
Symptoms: Bradycardia, hypotension, cardiac failure, dizziness, fatigue, hypoglycaemia, vomiting, bronchospasm, heart block. Management: Symptomatic and supportive treatment. IV atropine may be given for bradycardia, if it persists, admin IV isoproterenol cautiously. For hypotension, admin IV fluids and vasopressors. IV glucagon may also be useful. A β2-agonist and/or aminophylline for bronchospasm. Admin IV glucose for hypoglycaemia and an IV cardiac glycoside and diuretic may be used for CHF.
Drug Interactions
Increased plasma concentrations w/ potent CYP2D6 inhibitors (e.g. paroxetine, fluoxetine, propafenone, thioridazine, quinidine). Concomitant use w/ antiarrhythmic drugs (e.g. amiodarone, disopyramide) or nondihydropyridine Ca channel blockers (e.g. diltiazem, verapamil) may cause conduction disturbance. Additive negative effects on AV conduction and heart rate w/ other β-adrenergic blocking agents or digoxin. Concurrent admin w/ catecholamine-depleting agents (e.g. reserpine) may result in additive hypotension or bradycardia. Abrupt withdrawal of clonidine may increase risk of rebound HTN.
Action
Nebivolol exhibits high selectivity for β1-adrenergic receptors and has vasodilating activity due to a direct action on the endothelium, involving nitric oxide release. It lacks intrinsic sympathomimetic and membrane-stabilising activity.
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: 1.5-4 hr.
Distribution: Volume of distribution: 8-12 L/kg. Plasma protein binding: Approx 98% (mainly to albumin).
Metabolism: Undergoes extensive hepatic metabolism via glucuronidation and via by alicyclic and aromatic hydroxylation, N-dealkylation by CYP2D6 isoenzyme.
Excretion: Via urine and faeces (as metabolites). Elimination half-life: Approx 10 hr (nebivolol); approx 24 hr (hydroxy metabolites).
Storage
Oral: Store between 20-25°C. Protect from light.
CIMS Class
ATC Classification
C07AB12 - nebivolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
Disclaimer: This information is independently developed by CIMS based on nebivolol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 CIMS. All rights reserved. Powered by CIMSAsia.com
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