Adult: As bupropion hydrochloride conventional tab: Initially, 100 mg bid; may increase to usual dose of 100 mg tid after 3 days. If no signs of clinical improvement after several weeks, dose may be increased to Max: 450 mg daily in divided doses (Max: 150 mg/dose). As bupropion hydrochloride 12-hour extended-release (sustained-release) tab: Initially, 150 mg once daily in the morning, may increase to target dose of 150 mg bid after 3 days, if tolerated. If no response to 300 mg daily, increase dose to Max: 200 mg bid (400 mg daily). As bupropion hydrochloride 24-hour extended-release tab: Initially, 150 mg once daily in the morning, may increase to the target dose of 300 mg once daily after 4 days, if tolerated. If no clinical improvement after 2 weeks, may increase dose to 450 mg once daily. As bupropion hydrobromide 24-hour extended-release tab: Initially, 174 mg once daily in the morning, may increase to target dose of 348 mg once daily after 4 days. Max: 522 mg once daily. Treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Oral Smoking cessation
Adult: For nicotine-dependent patients in combination with motivational support: As bupropion hydrochloride modified-release or prolonged-release tab: Initially, 150 mg once daily for 6 days, then increase to 150 mg bid starting Day 7, with a minimum 8-hour interval between successive doses. Max: 150 mg/dose or 300 mg daily. Treatment should be started while the patient is still smoking and a “target stop date” of smoking is set, preferably in the 2nd week of treatment. Continue treatment for 7-9 weeks; discontinue if patient has not been able to stop smoking after 7 weeks of therapy. Do not interchange the brand specifically used for smoking cessation with other available brands used for different indications. Dosage and treatment recommendations may vary among countries and between individual products. Refer to specific product or local treatment guidelines for detailed information. Elderly: As bupropion hydrochloride modified-release or prolonged-release tab: 150 mg once daily.
Oral Seasonal affective disorder
Adult: For the prevention of seasonal major depressive disorder (MDD) episodes: As bupropion hydrochloride 24-hour extended-release tab: Initially, 150 mg once daily in the morning, may increase to target dose of 300 mg once daily in the morning after 7 days, if tolerated. As bupropion hydrobromide 24-hour extended-release tab: Initially, 174 mg once daily in the morning, may increase to the target dose of 348 mg once daily in the morning after 7 days, if tolerated. Initiate treatment in autumn prior to onset of depressive symptoms, continue treatment through winter season. Taper and discontinue in early spring. Timing of treatment initiation and duration of therapy must be individualised according to patient’s historical pattern of seasonal MDD episodes. Treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
What are the brands available for Bupropion in Hong Kong?
Smoking cessation:
Patients with predisposing factors to seizures: Max: 150 mg daily. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Renal Impairment
Smoking cessation:
As bupropion hydrochloride modified-release or prolonged-release tab: 150 mg once daily.
Major depressive disorder:
Reduce dose or dosing frequency. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Seasonal affective disorder:
Reduce dose or dosing frequency.
Hepatic Impairment
Smoking cessation:
As bupropion hydrochloride modified-release or prolonged-release tab: Mild to moderate: 150 mg once daily. Severe hepatic cirrhosis: Contraindicated.
Major depressive disorder:
As bupropion hydrochloride conventional tab: Mild (Child-Pugh score 5-6): Reduce dose or dosing frequency. Moderate to severe (Child-Pugh score 7-15): Max: 75 mg daily. As bupropion hydrochloride 12-hour extended-release (sustained-release) tab: Mild (Child-Pugh score 5-6): Reduce dose or dosing frequency. Moderate to severe (Child-Pugh score 7-15): Max dose: 100 mg daily or 150 mg every other day. As bupropion hydrochloride 24-hour extended-release tab: Mild (Child-Pugh score 5-6): Reduce dose or dosing frequency. Moderate to severe (Child-Pugh score 7-15): Max: 150 mg every other day. As bupropion hydrobromide 24-hour extended-release tab: Mild (Child-Pugh score 5-6): Reduce dose or dosing frequency. Moderate to severe: Max: 174 mg every other day. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Seasonal affective disorder:
As bupropion hydrochloride 24-hour extended-release tab: Mild (Child-Pugh score 5-6): Reduce dose or dosing frequency. Moderate to severe (Child-Pugh score 7-15): Max: 150 mg every other day. As bupropion hydrobromide 24-hour extended-release tab: Mild (Child-Pugh score 5-6): Reduce dose or dosing frequency. Moderate to severe: Max: 174 mg every other day. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Administration
Bupropion hydrochloride May be taken with or without food.
Contraindications
CNS tumour, current or history of anorexia nervosa or bulimia; current or history of seizure disorder; history of bipolar disorder (when used for smoking cessation). Severe hepatic cirrhosis. Abrupt withdrawal of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs. Concomitant use with linezolid or methylthioninium chloride (also known as methylene blue). Concomitant use with or within 14 days of discontinuing MAOIs.
Special Precautions
Patient with CV disease, CAD, history of hypertension; hepatic encephalopathy; predisposing factors to seizures (e.g. history of severe head trauma, arteriovenous malformation, CNS infection, CNS tumour, severe stroke), metabolic disorders (e.g. hypoglycaemia, hyponatraemia, hypoxia); diabetes mellitus (treated with oral hypoglycaemics or insulin); bipolar disorders or risk factors for bipolar disorder, history of psychiatric illness. Patient for whom weight loss is inappropriate. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Increased risk of suicidal thoughts and behaviour (in children, adolescents and young adults); dose-related seizures, activation of mania or hypomania; CNS stimulation (e.g. increased energy, insomnia, agitation, nervousness); anaphylactoid/anaphylactic reactions (e.g. angioedema, bronchospasm, dyspnoea); hypertension, acute angle-closure glaucoma, motor or cognitive impairment, weight loss. Rarely, neuropsychiatric effects (e.g. delusions, hallucinations, psychosis, concentration disturbance, abnormality in thinking, paranoia, confusion, homicidal ideation); anaphylactic shock, erythema multiforme, and Stevens-Johnson syndrome. Cardiac disorders: Tachycardia, arrythmia, palpitations. Ear and labyrinth disorders: Tinnitus, auditory disturbance. Eye disorders: Visual disturbance, blurred vision. Gastrointestinal disorders: Dry mouth, nausea, vomiting, abdominal pain, constipation, taste disorders. General disorders and administration site conditions: Fever, chest pain, asthenia. Metabolism and nutrition disorders: Anorexia, hyponatraemia. Musculoskeletal and connective tissue disorders: Arthralgia, myalgia. Nervous system disorders: Headache, dizziness, migraine, tremor. Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, pharyngitis, rhinitis, sinusitis, cough. Skin and subcutaneous tissue disorders: Urticaria, rash, pruritus, hyperhidrosis. Vascular disorders: Flushing.
This drug may cause dizziness, light-headedness, and motor or cognitive impairment, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure (at baseline and periodically); renal and hepatic function (at baseline and as clinically indicated); body weight. Closely monitor for signs of suicidal ideation and behavioural changes during initiation and dose adjustment.
Overdosage
Symptoms: Drowsiness, hallucinations, mental status changes, loss of consciousness, ECG changes (e.g. conduction disturbance [including QRS prolongation], arrythmia, tachycardia); clonus, myoclonus, hyperreflexia, seizure and serotonin syndrome. Management: Supportive treatment. Secure adequate airway, ventilation and oxygenation. Use of activated charcoal is recommended. Monitor ECG and vital signs.
Drug Interactions
Increased risk of seizures with drugs that lower seizure threshold (e.g. antipsychotics, antidepressants, antimalarials, quinolones, systemic corticosteroids, sedating antihistamines, tramadol, theophylline, anorexiants, hypoglycaemic drugs). May reduce the clinical efficacy of prodrugs that are CYP2D6-dependent for metabolic activation (e.g. tamoxifen). Increased serum concentration with CYP2B6 inhibitors (e.g. ticlopidine, clopidogrel). Enhanced metabolism and decreased exposure with CYP2B6 inducers (e.g. ritonavir, lopinavir, efavirenz), carbamazepine, phenobarbital, phenytoin. May increase the exposure of CYP2D6 substrates including certain antidepressants (e.g. venlafaxine, fluoxetine, sertraline), antipsychotics (e.g. haloperidol, risperidone, thioridazine), β-blockers (e.g. metoprolol), type 1C antiarrhythmics (e.g. propafenone, flecainide). Increased risk of CNS toxicity with levodopa and amantadine. May decrease the plasma levels of digoxin. Potentially Fatal: Increased risk of hypertensive reactions with MAOIs. Increased risk of serotonin syndrome with SSRIs and SNRIs.
Food Interaction
Concurrent consumption of alcohol may cause adverse neuropsychiatric events or reduced alcohol tolerance.
Lab Interference
May interfere with urine immunoassay screening tests for amphetamine or methamphetamine which may lead to false-positive results.
Action
Description: Mechanism of Action: Bupropion is an aminoketone-derivative antidepressant. Its exact mechanism of action has not been fully understood; however, it is known to inhibit the neuronal uptake of norepinephrine and dopamine with minimal effect on the serotonin reuptake. Presumably, the noradrenergic and/or dopaminergic effects are involved in smoking cessation. Onset: Depression: Within 1-2 weeks. Duration: 1-2 days. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: Bupropion: Within 2 hours (conventional tab); within 3 hours (12-hour extended-release [sustained-release] or modified-release tab); approx 2.5-3 hours (prolonged-release tab); approx 5 hours (24-hour extended-release tab). Hydroxybupropion: Approx 3 hours (conventional tab); approx 6-7 hours (extended-release tab). Distribution: Widely distributed. Crosses the placenta and enters breast milk. Volume of distribution: Approx 2,000 L. Plasma protein binding: 84% (bupropion); 77% (hydroxybupropion). Metabolism: Extensively metabolised in the liver primarily by CYP2B6 isoenzyme into hydroxybupropion (major active metabolite) and via reduction forming threohydrobupropion and erythrohydrobupropion (active metabolites); may undergo extensive first-pass metabolism. Excretion: Mainly via urine (approx 87%, mainly as metabolites; <1% as unchanged drug); faeces (approx 10%, mainly as metabolites). Terminal plasma half-life: Bupropion: Approx 14 hours (single dose); approx 21 hours (multiple doses).
Chemical Structure
Bupropion Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 444, Bupropion. https://pubchem.ncbi.nlm.nih.gov/compound/Bupropion. Accessed July 29, 2024.
Storage
Store between 15-30°C. Protect from light and moisture.
N06AX12 - bupropion ; Belongs to the class of other antidepressants.
References
Anon. Bupropion. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 24/04/2024.Aplenzin Tablet, Extended Release (Bausch Health US, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/05/2024.Buckingham R (ed). Bupropion. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/04/2024.Bupropion Hydrochloride Tablet, Film Coated (Apotex Corp). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/04/2024.Bupropion. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 24/04/2024.Forfivo XL Tablet, Film Coated Extended Release (TWi Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/05/2024.GlaxoSmithKline NZ Limited. Zyban 150 mg Modified Release Film-coated Tablets data sheet 22 March 2024. Medsafe. http://www.medsafe.govt.nz. Accessed 24/04/2024.Joint Formulary Committee. Bupropion Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/04/2024.Wellbutrin SR Tablet, Film Coated (GlaxoSmithKline LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/05/2024.Wellbutrin XL Tablet, Extended Release (Bausch Health US, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/05/2024.Zyban 150 mg Prolonged Release Tablets (Glaxo Wellcome UK Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 24/04/2024.
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