Bupropion

Indications
 Oral
Smoking cessation
Adult: Modified-release preparation: Initially, 150 mg once daily for 6 days then increased to 150 mg bid. Period of treatment: 7-12 wk. To discontinue treatment if abstinence is not achieved by 7th wk. Max: 300 mg/day.
Elderly: 150 mg/day.
Oral
Depression
Adult: Initially, 100 mg bid increased to 100 mg tid after 3 days if necessary. Increased further to 150 mg tid if no improvement has been observed after several wk of therapy. Max: 150 mg tid. As a 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.
Contraindications
 Epilepsy; eating disorders (e.g. bulimia or anorexia nervosa); hypersensitivity.
Warnings / Precautions
 History of seizure disorders, bipolar disorders; MI or unstable heart disease; pregnancy; renal or hepatic impairment. Monitor BP before and after treatment; monitor wkly if used with nicotine products. May impair ability to drive and operate machinery. Avoid use within 2 wk of MAO inhibitor withdrawal.
Adverse Reactions
 Facial oedema; nausea, dry mouth, constipation, diarrhoea, anorexia; mouth ulcer; thirst; myalgia, arthralgia; insomnia, dream, abnormality, anxiety, disturbed concentration, dizziness, nervousness, tremor, dysphoria; rhinitis, increased cough, pharyngitis, sinusitis; dyspnoea, epistaxis, agitation, insomnia, tremor, headache, weight loss, vomiting, skin rash.
Potentially Fatal: Stevens-Johnson syndrome.
Overdose Reactions
 Symptoms include hallucinations, loss of consciousness, sinus tachycardia, and ECG changes such as conduction disturbances or arrhythmias. Maintain an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. EEG monitoring is also recommended for the first 48 hr post-ingestion. General supportive and symptomatic measures are also recommended. Induction of emesis is not recommended.
Drug Interactions
 Neuroleptics, lithium and TCAs, benzodiazepine, alcohol, drugs that lower seizure threshold. Increased risk of side effects when co-admin with levodopa. Reduced hepatic clearance with fluoxetine. Caution when administering with agents that will affect hepatic drug metabolizing enzymes. Increased risk of toxicity when used with ritonavir.
Potentially Fatal: Concurrent use with MAO inhibitors may cause acute toxicity symptoms and increased risk of fatality.
See Below for More bupropion hydrochloride Drug Interactions
Mechanism of Actions
 Bupropion HCl is a relatively weak inhibitor of the neuronal uptake of norepinephrine, serotinin and dopamine. The mechanism by which it aids in smoking cessation is presumed to be mediated by its noradrenergic and/or dopaminergic actions.
Absorption: Well absorbed from the GI tract but undergoes extensive first pass effect.
Distribution: ≥80% bound to plasma proteins. Crosses the placenta and distributed into breast milk.
Excretion: Terminal half-life of immediate-release preparation: about 14 hr. Mainly excreted in the urine as metabolites.
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 15-25°C.
Storage
 Oral: Store at 15-25°C.
Available As
  • Bupropion 100 mg
  • Bupropion 150 mg
  • Bupropion 300 mg

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