Composition: Bupropion (as hydrochloride) 150mg.
Presentation: Film-coated, prolonged release, white tablets.
Storage and stability: Do not store above 25C. Store in original package.
Action: Selective inhibitor of neuronal re-uptake of catecholamines (noradrenaline and dopamine).
Indications: Aid to smoking cessation in combination with motivational support in nicotine-dependent patients.
Contraindications: Hypersensitivity to bupropion or excipients; current or previous seizure disorder; current or previous diagnosis of bulimia or anorexia nervosa; severe hepatic cirrhosis; history of bipolar disorder. Concomitant use of bupropion and monoamine oxidase inhibitors (MAOIs). At least 14 days should elapse between discontinuation of irreversible MAOIs and initiation of treatment with bupropion. For reversible MAOIs the period depends on the plasma elimination half-life of the specific product.
Dosage and administration: Patients should be treated for seven to nine weeks. If no effect is seen at seven weeks, treatment should be discontinued. Although discontinuation reactions are not expected, a tapering-off period may be considered.
Adults, treatment should be started while the patient is still smoking and a "target stop date" set within the first two weeks of treatment, preferably in the second week. Initial dose 150mg daily for three days, increasing to 150mg twice daily. There should be an interval of at least eight hours between successive doses. Maximum single dose should not exceed 150mg and total daily dose should not exceed 300mg.
Children and adolescents under 18 years, not recommended.
Elderly, use with caution. Recommended dose 150mg once daily. Greater sensitivity in some elderly patients cannot be ruled out.
Hepatic impairment, use with caution. The recommended dose in patients with mild to moderate impairment is 150mg once daily.
Renal insufficiency, use with caution. Recommended dose 150mg once daily.
Pregnancy and lactation, should not be used. Mothers should be advised not to breast feed while taking bupropion.
Overdosage: Overdose has resulted in drowsiness, hallucinations and loss of consciousness. Although most patients recovered without sequelae, deaths associated with overdoses have been reported rarely in patients ingesting massive doses. Hospitalisation is advised in the event of an overdose (see SPC for details).
Precautions: The recommended dose should not be exceeded since bupropion is associated with a dose-related risk of seizure. Zyban should be administered with extreme caution to patients with one or more conditions predisposing to a lowered seizure threshold. Bupropion should be discontinued if patients experience hypersensitivity or anaphylactic reactions. Symptoms such as arthralgia, myalgia and fever have been reported in association with rash and other symptoms suggestive of delayed hypersensitivity. If combination therapy with a nicotine transdermal system is used, caution must be exercised and weekly monitoring for potential treatment-emergent elevations of blood pressure is recommended.
Patients should exercise caution before driving or operating machinery until reasonably certain their performance is not adversely affected.
Drug interactions: Medicinal products with narrow therapeutic indices which are predominantly metabolised by CYP2D6 isoenzyme, including certain antidepressants, antipsychotics, beta-blockers and type 1C antiarrhythmics, when administered concomitantly with bupropion should be initiated at the lower end of the dose range. Care should be taken when bupropion is co-administered with products known to affect the CYP2B6 isoenzyme (eg, orphenadrine, cyclophosphamide, ifosfamide). Caution is advised when bupropion is co-administered with medicinal products known to induce (eg, carbamazepine, phenobarbital, phenytoin) or inhibit (eg, valproate) metabolism. Use with caution in patients receiving levodopa as a higher incidence of undesirable effects may occur. See SPC for effect of smoking cessation on drug blood levels.
Side effects: Common side effects (incidence greater than 1 per cent): fever, dry mouth, gastrointestinal disturbance including nausea and vomiting, abdominal pain, constipation, insomnia, tremor, headache, concentration disturbance, dizziness, depression, agitation, anxiety, rash, pruritus, sweating, hypersensitivity reactions such as urticaria, taste disorders. See SPC for less common and rare adverse events. The incidence of seizures is approximately 0.1 per cent.
Net price: 60 tablets £42.85.
Supplier: Glaxo Wellcome UK, Stockley Park West, Uxbridge, Middlesex UB11 1BT. Tel 0800 221441, fax 020 8990 4328.
Legal class: POM.
Marketing date: June 22.