NEBIVOLOL-WGR

What it is

NEBIVOLOL-WGR contains nebivolol hydrochloride, available in tablet strengths of 1.25 mg, 5 mg and 10 mg. Nebivolol is a selective β1-receptor antagonist at doses of 10 mg or less. The d-enantiomer is largely responsible for the β-receptor antagonist activity while the l-enantiomer has mild vasodilating properties attributable to an interaction with the L-arginine/nitric oxide pathway.

Approved indications

— To treat essential hypertension. — To treat stable chronic heart failure as an adjunct to standard therapies in patients 70 years or older.

Dosing overview

The blood pressure lowering effect becomes evident after 2 weeks of treatment, with the optimal effect sometimes reached only after 4 weeks. Initiation of therapy and every dose increase for heart failure should be done under the supervision of an experienced physician over a period of at least 2 hours to ensure that the clinical status remains stable.

Key safety warnings

The cessation of therapy with NEBIVOLOL-WGR should not be done abruptly unless clearly indicated. Severe exacerbation of angina and precipitation of myocardial infarction and ventricular arrhythmias have occurred following abrupt discontinuation of β-blockade in patients with ischaemic heart disease. The dosage should be reduced gradually over a period of about 1–2 weeks. β-adrenergic antagonists may induce bradycardia; if the pulse rate drops below 50–55 bpm at rest and/or the patient experiences symptoms suggestive of bradycardia, the dosage should be reduced or treatment gradually withdrawn. NEBIVOLOL-WGR may mask certain symptoms of hypoglycaemia in diabetic patients (tachycardia, palpitations). β-blockers could further increase the risk of severe hypoglycaemia when used concurrently with sulfonylureas. Diabetic patients should be advised to carefully monitor blood glucose levels. In patients with chronic obstructive pulmonary disorders, β-adrenergic antagonists should be used with caution as airway constriction may be aggravated.

Contraindications

NEBIVOLOL-WGR is contraindicated in: hypersensitivity to nebivolol hydrochloride or 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; 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 < 60 bpm prior to starting therapy); hypotension (systolic blood pressure < 100 mmHg); and severe peripheral circulatory disturbances.

Regulatory history

NEBIVOLOL-WGR received ARTG registration on 16 November 2023 for strengths of 1.25 mg, 5 mg and 10 mg as tablet blister packs. The date of first approval for the NEBIVOLOL-WGR variant (APO-Nebivolol) was 21 February 2018.