Major depressive disorder (unipolar), Seasonal affective disorder, Smoking cessation
#仿單變更2022
藥理
Antidepressant, Dopamine/Norepinephrine-Reuptake Inhibitor
Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the reuptake of serotonin. Metabolite inhibits the reuptake of norepinephrine.
藥動學
Absorption:
1. Onset of action: 1 to 2 weeks
2. Duration of action: 1 to 2 days Distribution:
1. Vd: ~20 to 47 L/kg
2. Protein binding: 84% Metabolism:
Extensively hepatic via CYP2B6 to hydroxybupropion; non-CYP-mediated metabolism to erythrohydrobupropion and threohydrobupropion. Metabolite activity ranges from 20% to 50% potency of bupropion. Bupropion also undergoes oxidation to form the glycine conjugate of meta-chlorobenzoic acid, the major urinary metabolite. Excretion:
Urine (87%, primarily as metabolites); feces (10%, primarily as metabolites)
禁忌症
1. Hypersensitivity to bupropion or any component of the formulation
2. Seizure disorder
3. History of anorexia/bulimia
4. Patients undergoing abrupt discontinuation of ethanol or sedatives(benzodiazepines, barbiturates, or antiepileptic drugs)
5. Use of MAO inhibitors (concurrently or within 14 days of discontinuing either bupropion or the MAO inhibitor)
6. Initiation of bupropion in a patient receiving linezolid or intravenous methylene blue
懷孕分類
Pregnancy Risk Factor C (FDA)
哺乳分類
Bupropion and its active metabolites are present in breast milk.
Seizures and sleep disturbances have been reported in breastfeeding infants following bupropion exposure via breast milk.
副作用
Common:
Tachycardia, insomnia, headache, agitation, dizziness, diaphoresis, weight loss, xerostomia, constipation, nausea and vomiting, nausea, tremor, blurred vision, nasopharyngitis, pharyngitis, rhinitis Warnings: 1. Serotonin syndrome: Serotonin syndrome has been reported in patients combining Bupropion and other drugs such as selective serotonin reuptake inhibitors (SSRIs) and serotonin norepinephrine re-uptake inhibitors (SNRIs). <20220127>
劑量和給藥方法
Major depressive disorder (unipolar):
Initial 150 mg once daily in the morning; if tolerated, may increase as early as day 4 of dosing to 300 mg once daily; if no clinical improvement after 2 weeks, may increase to 450 mg once daily Seasonal affective disorder (SAD):
Initial 150 mg once daily in the morning; if tolerated, may increase after 7 days to 300 mg once daily in the morning Smoking cessation: Note: Therapy should begin at least 1 week before target quit date. Target quit dates are generally in the second week of treatment. If patient successfully quits smoking, continue treatment for at least 12 weeks.
(Monotherapy or in combination with nicotine replacement therapy) Initial 150 mg once daily for 3 days; increase to 150 mg twice daily (maximum dose: 300 mg/day).
小兒調整劑量
Limited data available
腎功能調整劑量
Use with caution; manufacturer's labeling suggests a reduction in dose and/or frequency be considered but does not provide specific dosing recommendations.
肝功能調整劑量
1. Mild impairment (Child-Pugh score 5 to 6): Use with caution; manufacturer's labeling suggests a reduction in dose and/or frequency
2. Moderate to severe impairment, including severe hepatic cirrhosis (Child-Pugh score 7 to 15): Use with extreme caution; maximum 150 mg every other day