Nebivolol

Oral
Hypertension

Oral
Heart failure

Hypertension: Initially, 2.5 mg once daily. Maintenance: Increase to 5 mg daily if required.

May be taken with or without food.

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.

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.

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.

PO: C

Monitor ECG, BP and blood glucose in diabetic patients.

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.

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.

Description: 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.
Pharmacokinetics:
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 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).

Store between 20-25°C. Protect from light.

Beta-Blockers

Anon. Nebivolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com.

Buckingham R (ed). Nebivolol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com.

Bystolic Tablet (Cardinal Health). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/.

Bystolic Tablet (Cardinal Health). U.S. FDA. https://www.fda.gov/.

McEvoy GK, Snow EK, Miller J et al (eds). Nebivolol. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com.

Wickersham RM. Nebivolol HCl. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/.