donepezil hydrochloride monohydrate: clinical use

Prescribing considerations

• Confirm an appropriate dementia diagnosis and arrange treatment supervision by a clinician experienced in Alzheimer’s dementia.
• Ensure adequate support for adherence, including carer involvement where appropriate.
• Reassess cognitive, functional, global or behavioural benefit and treatment tolerability regularly.
• Review concurrent medicines for anticholinergic burden, bradycardic effects, QT prolongation and gastrointestinal bleeding risk.
• Exposure may be increased in mild to moderate hepatic impairment; evidence is lacking in severe hepatic impairment.

Contraindications and cautions

• Hypersensitivity to donepezil, piperidine derivatives or formulation excipients.
• Selected lactose-containing film-coated products are unsuitable for certain rare hereditary disorders of galactose metabolism or absorption.

Monitoring

• Clinical benefit, adherence and adverse effects.
• Pulse and symptoms such as syncope; investigate possible heart block or sinus pauses when indicated.
• Consider ECG monitoring with cardiac disease, bradyarrhythmia, electrolyte disturbance, personal or family QT prolongation, or concurrent QT-prolonging treatment.
• Watch for ulcer or gastrointestinal bleeding symptoms in higher-risk patients, including those taking NSAIDs.
• Review unexplained liver dysfunction, seizures, new extrapyramidal symptoms, severe muscle symptoms or features of neuroleptic malignant syndrome.

Clinical pharmacology

Donepezil is a selective, reversible acetylcholinesterase inhibitor. It is highly protein-bound, is metabolised partly through CYP3A4 and CYP2D6, and has a long terminal elimination half-life. Food does not materially affect absorption.

Formulation and product differences

• Film-coated tablets are swallowed and the selected products contain lactose.
• The selected orodispersible tablet is placed on the tongue to disintegrate before swallowing, with or without water.
• Excipients differ between manufacturers and formulations; check current product information when allergy, intolerance or swallowing difficulty is relevant.

Dispersible tablet

Route: Oral

Strengths: 5 mg, 10 mg

Tablet

Route: Oral

Strengths: 10 mg