mefloquine hydrochloride: clinical use

Prescribing considerations

• Base prophylaxis on destination-specific malaria risk and resistance patterns plus the traveller's medical, psychiatric and medication history.
• Discuss the distinctive neuropsychiatric risk and provide clear instructions to stop prophylactic mefloquine and obtain immediate review if mental-state changes occur.
• Assess cardiac conduction disease, hepatic or renal impairment, neurological symptoms, visual problems and activities requiring balance or fine coordination.
• The presence of lactose may matter in rare hereditary disorders of galactose metabolism.

Contraindications and cautions

• Hypersensitivity to mefloquine, related compounds such as quinine or quinidine, or formulation excipients.
• For chemoprophylaxis: current or previous depression, anxiety disorder, psychosis, schizophrenia, suicidal behaviour, other psychiatric disorder or convulsions of any origin.
• Halofantrine use during mefloquine exposure or its prolonged post-treatment elimination period.
• History of blackwater fever.
• Severe hepatic impairment.

Monitoring

• Actively review new psychiatric, neurological, vestibular, visual, cardiac, respiratory or hypersensitivity symptoms.
• Consider antiseizure medicine concentrations where concurrent treatment is unavoidable.
• For prolonged use, undertake periodic liver-function and ophthalmic assessment.
• Refer visual disturbance for medical assessment; stop and assess new peripheral neuropathy symptoms.

Clinical pharmacology

Mefloquine is highly protein-bound, extensively metabolised in the liver mainly through CYP3A4 and has a long elimination half-life. Food increases absorption. It acts against susceptible asexual intraerythrocytic Plasmodium forms but not dormant hypnozoites.

Formulation and product differences

• The selected products are white to off-white, cross-scored oral tablets supplied in moisture-protective foil packaging.
• The formulation contains lactose monohydrate.

Tablet

Route: Oral

Strengths: 250 mg