nebivolol hydrochloride: clinical use

Prescribing considerations

• Establish that chronic heart failure is stable and ensure initiation is supervised by a clinician experienced in heart-failure management.
• Avoid abrupt withdrawal; deterioration of heart failure or exacerbation of ischaemic symptoms may occur.
• Use caution with first-degree heart block, peripheral circulatory disease, chronic obstructive pulmonary disease, diabetes, hyperthyroidism, psoriasis and significant allergy history.
• Nebivolol may mask tachycardia associated with hypoglycaemia or hyperthyroidism.
• Evidence in children and adolescents is insufficient; the selected product does not recommend paediatric use.

Contraindications and cautions

• Hypersensitivity to nebivolol or an excipient
• Liver insufficiency or impaired liver function
• Acute or decompensated heart failure requiring intravenous inotropic support, or cardiogenic shock
• Sick sinus syndrome or sinoatrial block
• Second- or third-degree heart block without a pacemaker
• History of bronchospasm or bronchial asthma
• Untreated phaeochromocytoma
• Metabolic acidosis
• Bradycardia or hypotension meeting the product's pretreatment thresholds
• Severe peripheral circulatory disturbance

Monitoring

• Blood pressure, resting pulse and symptoms of bradycardia or hypotension
• Cardiac conduction and signs of worsening heart failure where clinically indicated
• Clinical stability during initiation and adjustment for chronic heart failure
• Blood glucose more carefully in diabetes, particularly with sulfonylureas
• Fetal growth and uteroplacental blood flow if treatment is necessary during pregnancy
• Exposed newborns for bradycardia and hypoglycaemia after birth

Clinical pharmacology

Nebivolol is a racemic mixture. Its SRRR enantiomer provides competitive selective beta-receptor antagonism, while nitric-oxide-pathway activity contributes mild vasodilation. It is extensively metabolised, partly to active metabolites, through genetically variable CYP2D6 metabolism; exposure and elimination are substantially greater in poor metabolisers.

Formulation and product differences

• The selected product is a white, round, cross-scored tablet that can be divided into equal quarters.
• It contains lactose monohydrate and is unsuitable for certain rare hereditary disorders affecting galactose or glucose-galactose handling.
• Tablet appearance, score design, excipients and divisibility may differ between manufacturers; check the specific pack information before splitting.

Tablet

Route: Oral

Strengths: 1.25 mg, 2.5 mg, 5 mg, 10 mg