bupropion hydrochloride: clinical use

Prescribing considerations

• Assess motivation and access to behavioural or motivational support.
• Review seizure risk, alcohol use, mental-health history and all medicines.
• Use caution in older adults and in renal or mild-to-moderate hepatic impairment because bupropion or active metabolites may accumulate.
• Consider CYP2D6 inhibition, CYP2B6-mediated interactions and medicine-level changes caused by smoking cessation.
• Some rapid urine drug screens may produce false-positive amphetamine results.

Contraindications and cautions

• Current seizure disorder or any previous seizure
• Current or previous bulimia or anorexia nervosa
• Known central nervous system tumour
• Abrupt withdrawal from alcohol, benzodiazepines or similar medicines associated with withdrawal seizures
• Severe hepatic cirrhosis
• Current or previous bipolar disorder
• Concurrent monoamine oxidase inhibitor use without the required washout
• Concurrent use of another bupropion-containing product
• Hypersensitivity to bupropion or an excipient

Monitoring

• Blood pressure, especially with pre-existing hypertension or concurrent nicotine patches
• New or worsening depression, suicidal thinking, mania, psychosis or other neuropsychiatric symptoms
• Symptoms of seizure, hypersensitivity, severe skin reaction or serotonin syndrome
• Adverse effects suggesting accumulation in renal or hepatic impairment
• Interacting-medicine effects, including digoxin toxicity after bupropion withdrawal

Clinical pharmacology

Bupropion selectively inhibits neuronal noradrenaline and dopamine reuptake, with minimal direct effect on serotonin reuptake and no monoamine oxidase inhibition. It is extensively metabolised, principally through CYP2B6, to active metabolites; bupropion and hydroxybupropion inhibit CYP2D6.

Formulation and product differences

• The selected product is an oral prolonged-release tablet.
• The tablet must remain intact; cutting, crushing or chewing defeats its release characteristics and increases adverse-effect risk.
• The selected product is licensed for smoking cessation with motivational support, not for depression.

Modified-release tablet

Route: Oral

Strengths: 150 mg