Bupropion
Other CNS Drugs · Dopamine-reuptake inhibitor, antidepressant
Indications
Aid to smoking cessation.
Dosage
Adults: Initially 150 mg daily for 6 days, increase to 150 mg twice daily allowing minimum 8 hr between doses. Max single dose, 150 mg; max daily dose, 300 mg. Start treatment while still smoking. A target date to stop smoking should be set within the first 2 wk and treatment should be continued for 7-9 wk. Discontinue if no effect is seen by 7 wk. Elderly: 150 mg daily. Children: Not recommended.
Adverse Effects
Insomnia, headache, fever, dry mouth, GI upset, CNS effects, skin/hypersensitivity reactions, taste disorders, tremor, dizziness, concentration disturbance, depression.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: History of seizures, bipolar disorder, bulimia, anorexia nervosa, CNS tumour, patients experiencing abrupt withdrawal of alcohol or benzodiazepines. Severe hepatic cirrhosis. Precautions: Risk of seizure increased in patients with history of head trauma, alcohol abuse or diabetes; only use if compelling clinical justification and use a lower dose of 150 mg daily throughout treatment period. Mild to moderate hepatic or renal impairment. Monitor BP before and during treatment, especially in patients with pre-existing hypertension. Monitor BP weekly if using concomitant transdermal nicotine. History of psychiatric illness. Elderly.
Interactions
MAOIs, antipsychotics, antidepressants, antimalarials, tramadol, theophylline, systemic steroids, sedating antihistamines, quinolones, beta-blockers, classic antiarrhythmics. Alcohol or benzodiazepine withdrawal. Central stimulants, anorectic agents, drugs metabolised by CYP2D6, 1A2 or 2B6. Carbamazepine, phenytoin, valproate, levodopa, citalopram, amantadine, digoxin, ritonavir, lopinavir, efavirenz, insulin, oral hypoglycaemics, tamoxifen, other drugs that lower seizure threshold.
Advice to Patient
Take with or without meals. Do not chew or crush film-coated tablets, swallow whole. Do not stop taking medication abruptly, gradually lower the dose and then stop. Contact prescriber if you experience lack of sleep, psychosis, hallucinations, anxiety, seizures, confusion, agitation, restlessness, abnormal thoughts, depression, skin rash, skin irritation, chest pain, palpitations, muscle weakness or tremors, yellowing of skin or eyes, difficulty in breathing, abdominal pain or blood in stools, bronchitis, unusual cough. Avoid alcohol during therapy. If you are using it for smoking cessation, do not combine nicotine patches without consulting prescriber.
Pharmacokinetics
Onset of action: 1 to 2 weeks. Duration of action: 1 to 2 days. Absorption: Rapid. Metabolism: Extensively hepatic. Half-life: Distribution: 3 to 4 hours. Elimination: Approx. 21 hours after chronic dosing (range: 12 to 30 hours); Metabolites (after a single dose): Hydroxybupropion: 20 ± 5 hours; Erythrohydrobupropion: 33 ± 10 hours; Threohydrobupropion: 37 ± 13 hours. Extended release: 21 ± 7 hours; Metabolites: Hydroxybupropion: 24 ± 5 hours; Erythrohydrobupropion: 31 ± 8 hours; Threohydrobupropion: 51 +9 hours. Time to peak, serum: Bupropion: Immediate release: Within 2 hours; Sustained release: Within 3 hours; Extended release: Approx. 5 hours. Metabolite: Hydroxybupropion: Immediate release: Approx. 3 hours; Extended release, sustained release: Approx. 6 to 7 hours. Excretion: Urine, feces.
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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