NEBILET

What it is

Nebilet is nebivolol hydrochloride tablets. Each tablet contains 1.25 mg, 5 mg or 10 mg nebivolol (as hydrochloride salt). Nebivolol is a selective β1-receptor antagonist in extensive metabolisers at doses less than or equal to 10 mg. The d-enantiomer is largely responsible for the β-receptor antagonist activity whilst the l-enantiomer has mild vasodilating properties attributable to an interaction with the L-arginine/nitric oxide pathway.

Approved indications

— Essential hypertension. — Stable chronic heart failure as an adjunct to standard therapies in patients 70 years or older.

Dosing overview

For hypertension, the blood pressure lowering effect becomes evident after 2 weeks of treatment, with the optimal effect occasionally reached only after 4 weeks. For chronic heart failure, patients should have stable disease without acute failure during the past six weeks, treatment should be initiated by an experienced physician, and dosing of concomitant cardiovascular drugs should be stabilised during the past two weeks prior to nebivolol initiation. 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 clinical stability.

Key safety warnings

Abrupt cessation of nebivolol should not be done abruptly unless clearly indicated. In patients with coronary artery disease, severe exacerbation of angina, precipitation of myocardial infarction and ventricular arrhythmias have occurred following abrupt discontinuation of β-blockade. The dosage should be reduced gradually over a period of about 1–2 weeks. Prior to surgery, the anaesthetist should be informed that the patient is receiving nebivolol because of the potential for interactions with other drugs, resulting in severe bradyarrhythmias and hypotension, decreased reflex ability to compensate for blood loss, hypovolaemia and regional sympathetic blockade. Nebivolol does not affect glucose levels in diabetic patients, but care should be taken as nebivolol may mask certain symptoms of hypoglycaemia (tachycardia, palpitations). β-blockers could further increase the risk of severe hypoglycaemia when used concurrently with sulfonylureas. In patients with chronic obstructive pulmonary disorders, β-adrenergic antagonists should be used with caution as airway constriction may be aggravated. β-adrenergic antagonists may increase the sensitivity to allergens and the severity of anaphylactic reactions, and adrenaline treatment does not always give the expected therapeutic effect. This medicinal product contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp-lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.

Contraindications

— Hypersensitivity to nebivolol hydrochloride or to any of the excipients. — Liver insufficiency or liver function impairment. — Acute heart failure, cardiogenic shock or episodes of heart failure decompensation requiring intravenous inotropic therapy. — Sick sinus syndrome (including sino-atrial block), and second and third degree heart block (without a pacemaker). — History of bronchospasm (including in chronic obstructive pulmonary disease) and/or asthma. — Untreated phaeochromocytoma. — Metabolic acidosis. — Bradycardia (heart rate less than 60 bpm prior to starting therapy). — Hypotension (systolic blood pressure less than 100 mmHg). — Severe peripheral circulatory disturbances.

PBS listing

Nebilet 1.25 mg tablet is listed on the PBS with a restriction type of restricted and an ex-manufacturer price of A$8.59.

Regulatory history

Nebilet nebivolol (as hydrochloride) 1.25 mg, 5 mg and 10 mg tablets were first listed on the ARTG on 2009-06-26.