Adult: Initially, 100 mg bid for at least 3 days, may increase to 100 mg tid if necessary. Increased further to 150 mg tid if no improvement has been observed after several wk of therapy. Max: 150 mg tid. As modified-release preparation: 150 mg once daily in the morning, increased to 150 mg bid after 3 days if necessary, may further increase to 200 mg bid after several wk if needed. Max: 450 mg as a single dose. Elderly: As immediate-release tab: Initially, 37.5 mg bid. As sustained-release tab: Initially, 100 mg daily. Dose may be increased by 37.5-100 mg every 3-4 days as tolerated. Max: 300 mg daily in divided doses.
Oral Smoking cessation
Adult: As modified-release preparation: Initially, 150 mg once daily for 6 days then increased to 150 mg bid, give 8 hr between doses for 7-9 wk. Discontinue treatment if abstinence is not achieved by 7th wk. Max: 300 mg daily. Elderly: 150 mg once daily for 7-9 wk.
Renal Impairment
Smoking cessation: 150 mg once daily. Depression: Reduce dose or dosing frequency.
Hepatic Impairment
Smoking cessation: Mild to moderate: 150 mg once daily. Severe hepatic cirrhosis: Contraindicated. Depression: Mild to moderate: Reduce dose or dosing frequency. Severe: As immediate-release preparation: Max: 75 mg once daily. As modified-release preparation: Max: 100 mg once daily or 150 mg every other day.
Contraindications
Current or history of seizure disorder, eating disorders (e.g. bulimia or anorexia nervosa); CNS tumour, epilepsy; history of bipolar disorder (when used as an aid in smoking cessation). Abrupt withdrawal of alcohol, benzodiazepines, barbiturates, antiepileptic drugs. Severe hepatic cirrhosis. Concomitant admin or w/in 14 days of MAOIs withdrawal.
Special Precautions
Patient w/ bipolar disorders (in the treatment of depression); recent history of MI or unstable heart disease; other risk factors for seizures (e.g. alcohol abuse, diabetes, history of head trauma). Renal or mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
This drug may cause dizziness and lightheadedness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor BP and LFT before and during treatment; monitor wkly if used with nicotine products. Monitor for worsening and emergence of suicidal thoughts and behaviours.
Overdosage
Symptoms: Hallucinations, nausea and vomiting, loss of consciousness, tachycardia, seizures. Management: Supportive treatment. Ensure adequate airway, ventilation and oxygenation. Administer activated charcoal for a dose >450 mg w/in 1 hr of ingestion. Perform gastric lavage to decrease absorption. May give benzodiazepine for seizures.
Drug Interactions
Observe extreme caution w/ concurrent admin of drugs that lower seizure threshold (e.g. other antidepressants, antipsychotics, theophylline, systemic corticosteroids). Increased risk of side effects w/ levodopa or amantadine. Decreased exposure w/ CYP2B6 inducers (e.g. ritonavir, lopinavir, efavirenz). May increase exposure of CYP2D6 substrates (e.g. venlafaxine, fluoxetine, antipsychotics, β-blockers, type 1C antiarrhythmics. Potentially Fatal: Concurrent use w/ MAOIs may cause acute toxicity symptoms and increased risk of fatality.
Food Interaction
Avoid alcohol.
Lab Interference
False positive result for amphetamine urine rapid test.
Action
Description: Mechanism of Action: Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, w/ minimal effect on serotonin reuptake. The mechanism by which it aids in smoking cessation is presumed to be mediated by its noradrenergic and/or dopaminergic actions. Onset: 1-2 wk. Duration: 1-2 days. Pharmacokinetics: Absorption: Well absorbed from the GI tract. Distribution: Widely distributed. Volume of distribution: Approx 2,000 L. Plasma protein binding: ≥80%. Crosses the placenta and distributed into breast milk. Metabolism: Metabolised hepatically by CYP2B6 isoenzyme to hydroxybupropion as major metabolite; may undergo extensive first-pass metabolism. Excretion: Via urine (mainly as metabolites, <1% as unchanged drug). Terminal plasma half-life: Approx 14 hr (immediate-release); approx 20 hr (modified-release).
Chemical Structure
Bupropion Source: National Center for Biotechnology Information. PubChem Database. Bupropion, CID=444, https://pubchem.ncbi.nlm.nih.gov/compound/Bupropion (accessed on Jan. 22, 2020)
N06AX12 - bupropion ; Belongs to the class of other antidepressants.
References
Anon. Bupropion. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 24/05/2016.Buckingham R (ed). Bupropion . Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/05/2016.Bupropion Hydrochloride SR Tablet, Film-Coated, Extended Release (ScieGen Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 24/05/2016.Joint Formulary Committee. Bupropion Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/05/2016.McEvoy GK, Snow EK, Miller J et al (eds). Bupropion Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 24/05/2016.
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