lofepramine hydrochloride: clinical use

Prescribing considerations

• Assess suicide risk and monitor clinical worsening, particularly early in treatment and after treatment changes.
• Review cardiovascular disease, QT-risk factors, seizure history, mania, glaucoma, urinary retention, constipation, porphyria, thyroid disease and hepatic or renal impairment.
• Avoid abrupt withdrawal unless clinically essential.
• Inform anaesthetic teams because anaesthetics may increase arrhythmia and hypotension risk.

Contraindications and cautions

• Hypersensitivity to lofepramine, dibenzazepines or formulation excipients
• Mania
• Severe hepatic or renal impairment
• Heart block, cardiac arrhythmias or recovery after myocardial infarction
• Untreated narrow-angle glaucoma
• Prostatic hypertrophy with urinary retention or risk of paralytic ileus
• Acute alcohol, hypnotic, analgesic or psychotropic poisoning, or acute delirium
• Concomitant or recent monoamine oxidase inhibitor treatment
• Avoid concomitant amiodarone or terfenadine

Monitoring

• Check blood pressure before treatment.
• Monitor mood, suicidal thinking and unusual behavioural change.
• Consider baseline and periodic full blood counts, particularly with a history of blood dyscrasia.
• Assess sodium if drowsiness, confusion or convulsions develop.
• Consider ECG and electrolyte assessment when cardiac disease, QT prolongation or hypokalaemia risk is present.
• Investigate symptoms suggesting hepatic injury.

Clinical pharmacology

Lofepramine is extensively metabolised during first passage through the liver, principally to the active metabolite desipramine. It inhibits monoamine reuptake and potentiates serotonergic transmission; elimination is mainly through urinary and biliary excretion of metabolites.

Formulation and product differences

• The selected product is a white to pale yellow-orange, cherry-scented oral suspension.
• Shake before use and protect from light.
• The suspension contains ethanol, sorbitol, maltitol, propylene glycol and methyl and propyl hydroxybenzoates.
• It is essentially sodium-free but is unsuitable for people with hereditary fructose intolerance.

Oral suspension

Route: Oral

Strengths: 70 mg/5 mL