Dosing & Uses
Dosage Forms & Strengths
tablet (Wellbutrin - Discontinued)
- 75mg
- 100mg
tablet, sustained-release (Wellbutrin SR)
- 100mg
- 150mg
- 200mg
tablet, extended-release (Wellbutrin XL)
- 150mg
- 300mg
tablet, extended-release (Aplenzin)
- 174mg
- 348mg
- 522mg
tablet, extended-release (Forfivo XL)
- 450mg
tablet, extended-release (Zyban - Discontinued)
- 150mg
Major Depressive Disorder
Immediate-release
- Initial: 100 mg PO q12hr; may increase to 100 mg PO q8hr as early as day 4; may consider increasing dose up to maximum 150 mg q8hr after several weeks if no clinical improvement observed with 100 mg q8hr
- Alternatively, may initiate with 75 mg PO q8hr
Sustained-release
- Initial: 150 mg PO qDay; may increase to 150 mg q12hr after 3 days
- May increase to no more than 200 mg q12hr after more than 4 weeks if no clinical improvement observed with 150 mg q12hr
Extended-release
- Initial: 150 mg PO qDay; may increase to 300 mg qDay on day 4
- May increase not to exceed 450 mg qDay after more than 4 weeks if no clinical improvement observed with 300 mg qDay; Forfivo may be used only after titrating initially with other bupropion products
Aplenzin
- Initial: 174 mg PO qDay; after 4 days, may increase to usual adult target dose of 348 mg PO qDay
- May increase not to exceed 522 mg qDay after more than 4 weeks
Forfivo XL
- 450 mg PO qDay without regard to food
- Can be used in patients who have been receiving 300 mg/day of another bupropion formulation for at least 2 weeks and who require a dosage of 450 mg/day
- Patients who are currently being treated with other bupropion products at 450 mg/day can be switched to equivalent dose of Forfivo XL once daily
Dosing considerations (Depression)
- Extended-release: When switching to XL, give the same total daily dose at the indicated frequencies: 3 times daily for immediate-release, twice daily for sustained-release, and once daily for extended-release
- Forfivo XL: Do not initiate treatment with Forfivo XL; use another bupropion formulation for initial dose titration
- Switching from hydrochloride salt formulation to hydrobromide salt (Aplenzin): 150 mg/day hydrochloride salt = 174 mg/day hydrobromide salt; 300 mg/day hydrochloride salt = 348 mg/day hydrobromide salt; 450 mg/day hydrochloride salt = 522 mg/day hydrobromide salt
Seasonal Affective Disorder
Wellbutrin XL: 150 mg PO qDay; may increase to 300 mg qDay
Aplenzin (bupropion hydrobromide): 174 mg PO qDay initially (equivalent to 150 mg bupropion HCl); after 1 week, may increase to usual target dose of 348 mg/day (equivalent to 300 mg bupropion HCL)
Dosing considerations (SAD)
- Initiate treatment in the autumn prior to onset of seasonal depressive symptoms and continue through the winter season
Smoking Cessation
Zyban (discontinued): 150 mg PO qDay for 3 days, THEN
Increase to 150 mg q12hr; should continue treatment for 7-12 weeks; if patient successfully quits after 7-12 weeks, consider ongoing maintenance therapy based on individual patient risk/benefit
Dosing considerations (Smoking Cessation)
- Begin therapy 1 week before target quit date (usually second week of treatment)
- May be used in combination with nicotine patch
ADHD (Off-label)
Initial: 150 mg/day PO
Titrate to 150-450 mg/day based on tolerability and efficacy; may administer in divided doses or in ER or SR formulations
Neuropathic Pain (Off-label)
150 mg bupropion SR PO twice daily for 6 weeks
Dosing Modifications
Hepatic impairment
- Mild to moderate: Use caution; consider reducing dose or frequency; Fortivo XL not recommended
- Moderate to severe (Buproban, Wellbutrin XL, Zyban): Not to exceed 150 mg every other day
- Moderate to severe (Aplenzin): Not to exceed 174 mg every other day
- Moderate to severe (Wellbutrin SR): 100 mg once daily or 150 mg every other day
- Moderate to severe (Zyban): 150 mg every other day
- Elderly: Lower dose/frequency may be required because of decreased renal/hepatic clearance
Renal impairment
- Use caution; consider dose reduction
Dosage Forms & Strengths
tablet (Wellbutrin - Discontinued)
- 75mg
- 100mg
tablet, sustained-release (Wellbutrin SR)
- 100mg
- 150mg
- 200mg
tablet, extended-release (Wellbutrin XL)
- 150mg
- 300mg
tablet, extended-release (Aplenzin)
- 174mg
- 348mg
- 522mg
tablet, extended-release (Forfivo XL)
- 450mg
ADHD (Off-label)
Immediate-release
- Initial: 3 mg/kg/day or 150 mg/day PO
- Titrate to 6 mg/kg/day or 300 mg/day, maximum
- Single dose should not exceed 150 mg; may administer as divided doses for safety and effectiveness (eg, BID for children and TID for adolescents)
Extended-release
Sustained-release
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (8)
- eliglustat
bupropion increases levels of eliglustat by affecting hepatic enzyme CYP2D6 metabolism. Contraindicated. If coadministered with strong or moderate CYP2D6 inhibitors, reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive and intermediate metabolizers; eliglustat is contraindiated if strong or moderate CYP2D6 inhibitors are given concomitantly with strong or moderate CYP3A inhibitors.
- isocarboxazid
isocarboxazid and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion
- phenelzine
phenelzine and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion
- pimozide
bupropion will increase the level or effect of pimozide by affecting hepatic enzyme CYP2D6 metabolism. Contraindicated. Both bupropion and hydroxybupropion (major metabolite) are considered strong CYP2D6 inhibitors; additionally, bupropion and pimozide lower seizure threshold
- rasagiline
rasagiline and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion
- selegiline
selegiline and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion
- selegiline transdermal
selegiline transdermal and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion
- tranylcypromine
tranylcypromine and bupropion both increase dopaminergic effects. Contraindicated. Bupropion inhibits reuptake of dopamine and norepinephrine (NE), and MAOIs decrease metabolism of dopamine and NE; coadministration increases risk for hypertensive reactions; allow at least 14 days between discontinuation of MAOI and initiating bupropion
Serious - Use Alternative (26)
- caffeine
caffeine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- chlorpromazine
chlorpromazine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- clomipramine
bupropion will increase the level or effect of clomipramine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug.
- clozapine
clozapine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- cyclobenzaprine
bupropion and cyclobenzaprine both increase serotonin levels. Avoid or Use Alternate Drug.
- duloxetine
duloxetine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- escitalopram
escitalopram increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- fexinidazole
fexinidazole will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Avoid or Use Alternate Drug. Coadministration may decrease plasma concentrations of CYP2B6 substrates owing to fexinidazole inducing CYP2B6.
- fluoxetine
fluoxetine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- fluvoxamine
fluvoxamine increases toxicity of bupropion by Other (see comment). Avoid or Use Alternate Drug. Comment: May lower seizure threshold; keep bupropion dose as low as possible.
- iobenguane I 131
bupropion will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.
- linezolid
bupropion, linezolid. serotonin levels. Avoid or Use Alternate Drug. Linezolid may increase serotonin as a result of MAO-A inhibition. If linezolid must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity. Serotonergic therapy may be resumed 24 hours after last linezolid dose or after 2 weeks of monitoring, whichever comes first.
- lorcaserin
bupropion and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.
- methylene blue
bupropion and methylene blue both increase serotonin levels. Avoid or Use Alternate Drug. Methylene blue may increase serotonin as a result of MAO-A inhibition. If methylene blue must be administered, discontinue serotonergic drug immediately and monitor for CNS toxicity. Serotonergic therapy may be resumed 24 hours after last methylene blue dose or after 2 weeks of monitoring, whichever comes first.
- metoclopramide intranasal
bupropion will increase the level or effect of metoclopramide intranasal by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Concurrent use of metoclopramide intranasal and strong CYP2D6 inhibitors is not recommended since the metoclopramide intranasal dose cannot be adjusted.
- milnacipran
milnacipran increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- nefazodone
nefazodone increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- olopatadine intranasal
bupropion and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- ozanimod
ozanimod increases toxicity of bupropion by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug. Because the active metabolite of ozanimod inhibits MAO-B in vitro, there is a potential for serious adverse reactions, including hypertensive crisis. Therefore, coadministration of ozanimod with drugs that can increase norepinephrine or serotonin is not recommended. Monitor for hypertension with concomitant use.
- paroxetine
bupropion will increase the level or effect of paroxetine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug.
paroxetine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible. - tedizolid
tedizolid, bupropion. Either increases levels of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- theophylline
theophylline increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- thioridazine
bupropion will increase the level or effect of thioridazine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug.
- trazodone
trazodone increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- venlafaxine
venlafaxine increases toxicity of bupropion by unspecified interaction mechanism. Avoid or Use Alternate Drug. May lower seizure threshold; keep bupropion dose as low as possible.
- vortioxetine
bupropion, vortioxetine. Either increases effects of the other by serotonin levels. Avoid or Use Alternate Drug.
Monitor Closely (117)
- amantadine
amantadine, bupropion. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Potential CNS toxicity d/t synergistic central dopamine effect.
- amifampridine
bupropion increases toxicity of amifampridine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Amifampridine can cause seizures. Coadministration with drugs that lower seizure threshold may increase this risk.
- amitriptyline
amitriptyline increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
bupropion will increase the level or effect of amitriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - amobarbital
amobarbital, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- amoxapine
amoxapine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
bupropion will increase the level or effect of amoxapine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - aripiprazole
bupropion will increase the level or effect of aripiprazole by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- atomoxetine
bupropion will increase the level or effect of atomoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- benzhydrocodone/acetaminophen
bupropion will increase the level or effect of benzhydrocodone/acetaminophen by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Hydromorphone (<3% of the circulating parent hydrocodone [benzhydrocodone is prodrug of hydrocodone]) is mainly formed by CYP2D6 mediated O-demethylation of hydrocodone. Hydromorphone may contribute to the total analgesic effect of hydrocodone.
benzhydrocodone/acetaminophen, bupropion. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment. - betaxolol
bupropion will increase the level or effect of betaxolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- brexpiprazole
bupropion will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.
- butabarbital
butabarbital, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- butalbital
butalbital, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- cannabidiol
cannabidiol, bupropion. affecting hepatic enzyme CYP2B6 metabolism. Modify Therapy/Monitor Closely. Owing to the potential for both CYP2B6 induction and inhibition with the coadministration of CYP2B6 substrates and cannabidiol, consider reducing dosage adjustment of CYP2B6 substrates as clinically appropriate.
- carbamazepine
carbamazepine will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.
- carvedilol
bupropion will increase the level or effect of carvedilol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- cenobamate
cenobamate will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP2B6 substrate, as needed, when coadministered with cenobamate.
- chloroquine
bupropion will increase the level or effect of chloroquine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- chlorpromazine
bupropion will increase the level or effect of chlorpromazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- cinacalcet
bupropion will increase the level or effect of cinacalcet by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- citalopram
bupropion will increase the level or effect of citalopram by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- clomipramine
clomipramine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- clopidogrel
clopidogrel will increase the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Plasma concentrations of bupropion may be significantly increased when coadministered with clopidogrel or other CYP2B6 inhibitors. The increase in plasma bupropion concentrations may cause an increase in adverse reactions including tremor, headache, insomnia, dry mouth, nausea, or seizures.
- codeine
bupropion will decrease the level or effect of codeine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Prevents the conversion of codeine to its active metabolite morphine.
- cyclosporine
cyclosporine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- daridorexant
bupropion and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- desipramine
bupropion will increase the level or effect of desipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
desipramine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - deutetrabenazine
bupropion will increase the level or effect of deutetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Strong CYP2D6 inhibitors increase the systemic exposure to the active dihydro-metabolites of deutetrabenazine by approximately 3-fold. Do not exceed 18 mg/dose and 36 mg/day of deutetrabenazine if coadministered with strong CYP2D6 inhibitors.
- dextroamphetamine
bupropion will increase the level or effect of dextroamphetamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
dextroamphetamine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - dextroamphetamine transdermal
bupropion will increase the level or effect of dextroamphetamine transdermal by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Initiate with lower doses and monitor patients for signs and symptoms of serotonin syndrome, particularly during dextroamphetamine initiation and after a dosage increase. If serotonin syndrome occurs, discontinue dextroamphetamine transdermal and CYP2D6 inhibitor.
- dextromethorphan
bupropion will increase the level or effect of dextromethorphan by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- diazepam intranasal
diazepam intranasal, bupropion. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may potentiate the CNS-depressant effects of each drug.
- difelikefalin
difelikefalin and bupropion both increase sedation. Use Caution/Monitor.
- digoxin
bupropion will decrease the level or effect of digoxin by Other (see comment). Use Caution/Monitor. Monitor for decreased digoxin concentrations; bupropion may induce OATP4C1 transporter, which is involved in digoxin renal elimination
- doxepin
bupropion will increase the level or effect of doxepin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
doxepin increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - duloxetine
bupropion will increase the level or effect of duloxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- efavirenz
efavirenz will decrease the level or effect of bupropion by increasing metabolism. Use Caution/Monitor. Coadministration with hepatic inducers reduced bupropion AUC and Cmax; hydroxybupropion (active metabolite) Cmax was increased
- eluxadoline
bupropion increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of bupropion by unknown mechanism. Use Caution/Monitor.
- fenfluramine
fenfluramine, bupropion. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration with drugs that increase serotoninergic effects may increase the risk of serotonin syndrome.
- fesoterodine
bupropion will increase the level or effect of fesoterodine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- flecainide
bupropion will increase the level or effect of flecainide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Coadministration of bupropion and flecainide should be approached with caution and should be initiated at the lower end of the dose range of flecainide. If bupropion is added to the treatment regimen of a patient already receiving flecainide, consider decreasing the dose of flecainide.
- fluoxetine
bupropion will increase the level or effect of fluoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- fluphenazine
bupropion will increase the level or effect of fluphenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- fluvoxamine
fluvoxamine will increase the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.
- gabapentin
gabapentin, bupropion. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- gabapentin enacarbil
gabapentin enacarbil, bupropion. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- galantamine
bupropion will increase the level or effect of galantamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- ganaxolone
bupropion and ganaxolone both increase sedation. Use Caution/Monitor.
- haloperidol
bupropion will increase the level or effect of haloperidol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- hydrocodone
bupropion will increase the level or effect of hydrocodone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Hydromorphone (<3% of the circulating parent hydrocodone) is mainly formed by CYP2D6 mediated O-demethylation of hydrocodone. Hydromorphone may contribute to the total analgesic effect of hydrocodone.
hydrocodone, bupropion. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment. - hydromorphone
bupropion will increase the level or effect of hydromorphone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- iloperidone
bupropion will increase the level or effect of iloperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- imipramine
bupropion will increase the level or effect of imipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
imipramine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - ioflupane I 123
bupropion decreases effects of ioflupane I 123 by receptor binding competition. Use Caution/Monitor. Drugs that bind to dopamine transporter receptor with high affinity may interfere with the image following ioflupane I 123 administration.
- lasmiditan
lasmiditan, bupropion. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.
- lemborexant
lemborexant will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Modify Therapy/Monitor Closely. Monitor CYP2B6 substrate for adequate clinical response. Consider increasing the CYP2B6 substrate dose according to specific prescribing recommendations.
lemborexant, bupropion. Either increases effects of the other by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects. - levodopa
bupropion increases effects of levodopa by pharmacodynamic synergism. Use Caution/Monitor. There is a higher incidence of adverse reactions with concurrent use of bupropion with levodopa. Use small initial dosages and small, gradual dosage increases of bupropion.
- lisdexamfetamine
lisdexamfetamine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- lofepramine
bupropion will increase the level or effect of lofepramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
lofepramine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - lofexidine
bupropion will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.
- loratadine
bupropion will increase the level or effect of loratadine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor, bupropion. affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2B6 substrates. .
- lurasidone
lurasidone, bupropion. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Potential for increased CNS depressant effects when used concurrently; monitor for increased adverse effects and toxicity.
- maprotiline
maprotiline increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
bupropion will increase the level or effect of maprotiline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - metformin
bupropion increases levels of metformin by Other (see comment). Use Caution/Monitor. Comment: Bupropion may inhibit OCT2 mediated renal excretion of metformin.
- methamphetamine
bupropion will increase the level or effect of methamphetamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
methamphetamine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - methylenedioxymethamphetamine
methylenedioxymethamphetamine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- metoprolol
bupropion will increase the level or effect of metoprolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- mexiletine
bupropion will increase the level or effect of mexiletine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- mifepristone
mifepristone will increase the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.
- mipomersen
mipomersen, bupropion. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.
- mirtazapine
bupropion will increase the level or effect of mirtazapine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- morphine
bupropion will increase the level or effect of morphine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- nebivolol
bupropion will increase the level or effect of nebivolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- nelfinavir
nelfinavir, bupropion. decreasing metabolism. Use Caution/Monitor. Incr levels of bupropion, but decr levels of active metabolites. .
- nilotinib
nilotinib, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- nirmatrelvir
nirmatrelvir will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Buproion extensively metabolized by CYP2B6 to active metabolite. Monitor for adequate clinical response to bupropion when coadministered with CYP2B6 inhibitors.
- nirmatrelvir/ritonavir
nirmatrelvir/ritonavir will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Bupropion is extensively metabolized by CYP2B6 to active metabolite. Monitor for adequate clinical response to bupropion when coadministered with CYP2B6 inhibitors.
- nortriptyline
bupropion will increase the level or effect of nortriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
nortriptyline increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - oliceridine
bupropion will increase the level or effect of oliceridine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.
bupropion, oliceridine. Either increases effects of the other by serotonin levels. Modify Therapy/Monitor Closely. - oxycodone
bupropion will increase the level or effect of oxycodone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- pentobarbital
pentobarbital, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- perphenazine
bupropion will increase the level or effect of perphenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
perphenazine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - phenobarbital
phenobarbital will decrease the level or effect of bupropion by increasing metabolism. Use Caution/Monitor. Decrease levels of bupropion.
- pitolisant
bupropion will increase the level or effect of pitolisant by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If coadministered with strong CYP2D6 inhibitors, initiate pitolisant at 8.9 mg/day and increase after 7 days to maximum of 17.8 mg/day. For patients currently taking pitolisant, reduce pitolisant dose by half upon initiating strong CYP2D6 inhibitors.
- pivmecillinam
pivmecillinam increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- pregabalin
pregabalin, bupropion. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.
- primidone
primidone, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- prochlorperazine
bupropion will increase the level or effect of prochlorperazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
prochlorperazine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible. - promethazine
bupropion will increase the level or effect of promethazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- propafenone
bupropion will increase the level or effect of propafenone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- propranolol
bupropion will increase the level or effect of propranolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- protriptyline
protriptyline increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
bupropion will increase the level or effect of protriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - remimazolam
remimazolam, bupropion. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.
- rifampin
rifampin will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor.
- risperidone
bupropion will increase the level or effect of risperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- ritonavir
ritonavir decreases levels of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Ritonavir decreases levels of bupropion by inducing CYP2B6. Bupropion levels decreased by 20-80%, increased doses of bupropion may be required .
- secobarbital
secobarbital, bupropion. increasing metabolism. Use Caution/Monitor. Decr levels of bupropion, but incr levels of active metabolites. .
- sertraline
sertraline increases levels of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Sertraline may inhibit hydroxylation of bupropion to its major active metabolite hydroxybupropion.
bupropion will increase the level or effect of sertraline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - solriamfetol
bupropion and solriamfetol both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- sorafenib
sorafenib, bupropion. decreasing metabolism. Use Caution/Monitor. Incr levels of bupropion, but decr levels of active metabolites. .
- sparsentan
sparsentan will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Sparsentan (a CYP2B6 inducer) decreases exposure of CYP2B6 substrates and reduces efficacy related to these substrates.
- stiripentol
stiripentol, bupropion. affecting hepatic enzyme CYP2B6 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP2B6 inhibitor and inducer. Monitor CYP2B6 substrates coadministered with stiripentol for increased or decreased effects. CYP2B6 substrates may require dosage adjustment.
- sufentanil SL
sufentanil SL, bupropion. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.
- tamoxifen
bupropion decreases effects of tamoxifen by decreasing metabolism. Use Caution/Monitor. Inhibition of CYP2D6 metabolism to tamoxifen's active metabolite, endoxifen.
bupropion will decrease the level or effect of tamoxifen by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Inhibition of CYP2D6 decreases metabolism of tamoxifen to active metabolite, endoxifen - tamsulosin
bupropion increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- tapentadol
bupropion and tapentadol both increase serotonin levels. Modify Therapy/Monitor Closely.
- telotristat ethyl
telotristat ethyl will decrease the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Use Caution/Monitor. Consider increasing dosage of interacting drug, if necessary
- temocillin
temocillin increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- ticarcillin
ticarcillin increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
- timolol
bupropion will increase the level or effect of timolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- tolterodine
bupropion will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- tramadol
bupropion will increase the level or effect of tramadol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- trifluoperazine
bupropion will increase the level or effect of trifluoperazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- trimipramine
trimipramine increases toxicity of bupropion by unspecified interaction mechanism. Use Caution/Monitor. May lower seizure threshold; keep bupropion dose as low as possible.
bupropion will increase the level or effect of trimipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. - valbenazine
bupropion will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- venlafaxine
bupropion will increase the level or effect of venlafaxine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
Minor (19)
- armodafinil
armodafinil, bupropion. increasing metabolism. Minor/Significance Unknown. Decr levels of bupropion, but incr levels of active metabolites. .
- carbamazepine
carbamazepine decreases levels of bupropion by increasing metabolism. Minor/Significance Unknown.
- cefamandole
cefamandole increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- cefpirome
cefpirome increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- dexfenfluramine
bupropion will increase the level or effect of dexfenfluramine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.
- donepezil
bupropion will increase the level or effect of donepezil by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.
- encainide
bupropion will increase the level or effect of encainide by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.
- ethanol
ethanol, bupropion. Either increases toxicity of the other by pharmacodynamic synergism. Minor/Significance Unknown. Additive CNS depression.
- fluphenazine
fluphenazine increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- meperidine
meperidine increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- modafinil
modafinil, bupropion. increasing metabolism. Minor/Significance Unknown. Decr levels of bupropion, but incr levels of active metabolites. .
- nicotine inhaled
bupropion, nicotine inhaled. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypertension.
- nicotine intranasal
bupropion, nicotine intranasal. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypertension.
- perhexiline
bupropion will increase the level or effect of perhexiline by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.
- promazine
bupropion will increase the level or effect of promazine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.
promazine increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible. - promethazine
promethazine increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- thioridazine
thioridazine increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- trifluoperazine
trifluoperazine increases toxicity of bupropion by unspecified interaction mechanism. Minor/Significance Unknown. May lower seizure threshold; keep bupropion dose as low as possible.
- tropisetron
bupropion will increase the level or effect of tropisetron by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Headache (25-34%)
Dry mouth (17-28%)
Nausea (1-18%)
Weight loss (15-20%)
Insomnia (11-20%)
Agitation (2-32%)
Dizziness (6-22%)
Pharyngitis (3-13%)
1-10%
Constipation (5-10%)
Infection (8-9%)
Abdominal pain (2-9%)
Anxiety (5-7%)
Diarrhea (5-7%)
Tinnitus (3-6%)
Tremor (3-6%)
Nervousness (3-5%)
Anorexia (3-5%)
Palpitation (2-6%)
Myalgia (2-6%)
Sweating (2-5%)
Rash (1-5%)
Sinusitis (1-5%)
Weight gain (4%)
Chest pain (3-4%)
Urinary frequency (2%)
Vaginal hemorrhage (2%)
Pruritus (2-4%)
Vomiting (2-4%)
Arthralgia (1-4%)
Flushing (1-4%)
Migraine (1-4%)
Decreased memory (<3%)
Irritability (2-3%)
Somnolence (2-3%)
Dysphagia (<2%)
Arthritis (2%)
Paresthesia (1-2%)
Fever (1-2%)
Twitch (1-2%)
Seizures (0.4% [<450 mg/day], >3% [>450 mg/day]; may be increased risk with concomitant ECT)
Frequency Not Defined
Confusion
Cystitis
Erythema
Ataxia
Coma
EEG abnormality
Euphoria
Gastric reflux
Postmarketing reports
Hyperglycemia
Hypoglycemia
Hyponatremia
Syndrome of inappropriate antidiuretic hormone secretion
Nervous system: Abnormal electroencephalogram (EEG), aggression, akinesia, aphasia, completed suicide, delirium, delusions, dysarthria, extrapyramidal syndrome (dyskinesia, dystonia, hypokinesia, parkinsonism), hallucinations, increased libido, manic reaction, neuralgia, neuropathy, paranoid ideation, restlessness, suicide attempt, and unmasking tardive dyskinesia
Skin reactions: Maculopapular rash, alopecia, angioedema, exfoliative dermatitis, hirsutism, Stevens-Johnson syndrome, urticaria, and acute generalized exanthematous pustulosis
Warnings
Black Box Warnings
Not FDA approved for bipolar depression
Suicidality
- In short-term studies, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults (<24 years) taking antidepressants for major depressive disorders and other psychiatric illnesses; this increase was not seen in patients >24 years
- Slight decrease in suicidal thinking was seen in adults >65 years
- In children and young adults, risks must be weighed against the benefits of taking antidepressants
- Patients should be monitored closely for changes in behavior, clinical worsening, and suicidal tendencies; this should be done during initial 1-2 months of therapy and dosage adjustments
- The patient’s family should communicate any abrupt changes in behavior to the healthcare provider
- Worsening behavior and suicidal tendencies that are not part of the presenting symptoms may require discontinuation of therapy; this drug is not approved for use in pediatric patients
Contraindications
Hypersensitivity to bupropion or other ingredients
History of anorexia/bulimia; patients undergoing abrupt discontinuation of ethanol or sedatives including anticonvulsants, barbiturates, or benzodiazepines
Coadministration of any other medications that contain bupropion, because seizures are dose dependent
Aplenzin contraindications
- Seizure disorder or conditions that increase seizure risk (arteriovenous malformation, severe head injury, CNS tumor, CNS infection, severe stroke, anorexia nervosa or bulimia (current or prior diagnosis)
Coadministration with MAOIs
- Coadministration may cause serotonin syndrome
- Do not use concomitantly or initiate bupropion within 14 days of stopping an MAOI
- Conversely, at least 14 days should be allowed after stopping bupropion before starting an MAOI antidepressant
- Starting bupropion in a patient who is being treated with linezolid or IV methylene blue is contraindicated because of an increased risk of serotonin syndrome
- If linezolid or IV methylene blue must be administered, discontinue bupropion immediately and monitor for CNS toxicity; may resume 24 hr after last linezolid or methylene blue dose or after 2 weeks of monitoring, whichever comes first
Cautions
Caution in severe hepatic cirrhosis (do not exceed 150 mg every other day), mild-moderate hepatic impairment, head trauma and prior seizure history, CNS tumor, concomitant meds lowering seizure threshold
Observe patients for neuropsychiatric symptoms, such as changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide (see Black Box Warnings); therapy may cause delusions, hallucinations, psychosis, paranoia, confusion, and concentration disturbance; symptoms may abate with dose reduction
Healthcare provider should evaluate severity of adverse events and extent to which patient is benefiting from treatment, and consider options including continued treatment under closer monitoring, or discontinuing treatment; in many postmarketing cases, resolution of symptoms after discontinuation of bupropion reported; however, symptoms persisted in some cases; ongoing monitoring and supportive care should be provided until symptoms resolve
Potential risk of hepatotoxicity
Assess blood pressure before initiating treatment with sustained release formulation, and monitor periodically during treatment; risk of hypertension is increased if sustained release formulation is used concomitantly with MAOIs or other drugs that increase dopaminergic or noradrenergic activity; use caution in patients with cardiovascular disease
May cause weight loss; use caution if weight loss not desirable
May cause CNS depression and impair ability to operate heavy machinery
Extended-release: Do not administer less than 8 hr apart
Seizure risk is dose-related; can minimize risk by limiting daily dose to 522 mg and gradually increasing dose; discontinue permanently in patients who experience seizures
May cause sexual dysfunction
Screen patients for bipolar disorder and monitor for these symptoms; may precipitate manic, hypomanic or mixed episodes in patients with bipolar disorder
Instruct patients to contact a healthcare professional if neuropsychiatric reactions occur
Perform thorough cardiovascular assessment to identify risk factors of sudden cardiac death in pediatric ADHD patients
Risk of mydriasis; may trigger angle closure attack in patients with angle closure glaucoma with anatomically narrow angles without a patent iridectomy; use caution
False-positive urine immunoassay screening tests for amphetamines have been reported; confirmatory test (eg, gas chromatography, mass spectrometry) will distinguish bupropion from amphetamines
Some patients who stopped smoking reported to have experienced symptoms of nicotine withdrawal, including depressed mood; depression, rarely including suicidal ideation, reported in smokers undergoing a smoking cessation attempt without medication; however, some of these adverse events occurred in patients taking bupropion who continued to smoke
Neuropsychiatric adverse events reported in patients without and with pre-existing psychiatric disease; some patients experienced worsening of their psychiatric illnesses; observe patients for occurrence of neuropsychiatric adverse events; patient should stop therapy and contact healthcare provider immediately if agitation, depressed mood, or changes in behavior or thinking that are not typical for patient are observed, or if patient develops suicidal ideation or suicidal behavior; symptoms may persist after discontinuation of therapy; in some cases; monitoring and supportive care should be provided until symptoms resolve
Bupropion hydrobromide extended-release tablets are intended for oral use only; inhalation of crushed tablets or injection of dissolved bupropion reported; seizures and/or cases of death reported when administered intranasally or by parenteral injection
Abuse warning
- XL and SR tablets are intended for oral use only
- Inhaling crushed tablets or injecting dissolved tablets has been reported to cause seizures and/or death
Pregnancy & Lactation
Pregnancy
There is an independent pregnancy exposure registry that monitors pregnancy outcomes in women exposed to any antidepressants during pregnancy; healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-844-4056185 or visiting online at https://womensmentalhealth.org/clinical-and-researchprograms/pregnancyregistry/antidepressants
Data from epidemiological studies of pregnant women exposed to bupropion in first trimester have not identified an increased risk of congenital malformations overall; there are risks to the mother associated with untreated depression in pregnancy
A prospective, longitudinal study followed 201 pregnant women with a history of major depressive disorder who were euthymic and taking antidepressants during pregnancy at beginning of pregnancy; the women who discontinued antidepressants during pregnancy were more likely to experience a relapse of major depression than women who continued antidepressants; consider risks to the mother of untreated depression and potential effects on tfetus when discontinuing or changing treatment with antidepressant medications during pregnancy and postpartum
Animal data
- When bupropion was administered to pregnant rats during organogenesis, there was no evidence of fetal malformations at doses up to approximately 10 times maximum recommended human dose (MRHD) of 450 mg/day; when given to pregnant rabbits during organogenesis, non-dose–related increases in incidence of fetal malformations and skeletal variations were observed at doses approximately equal to the MRHD and greater; decreased fetal weights were seen at doses twice the MRHD and greater
Lactation
Data from published literature report presence of drug and its metabolites in human milk; there are no data on effects of bupropion or metabolites on milk production; limited data from postmarketing reports have not identified a clear association of adverse reactions in the breastfed infant; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Not well understood; structurally unrelated to SSRIs, TCAs, MAOIs; does not inhibit the activity of monoamine oxidase or the reuptake of serotonin
Norepinephrine dopamine reuptake inhibitor; may act through dopaminergic or noradrenergic pathways
Absorption
Peak serum time: 2 hr (immediate-release); 3 hr (extended-release)
Distribution
Protein bound: 84%
Vd: 20-47 L/kg
Metabolism
Hepatic, via CYP2B6
Metabolites: Hydroxybupropion (50% potency of parent compound)
Elimination
Half-life: 8-24 hr (immediate-release); 21 +/- 7 hr (extended-release)
Excretion: Urine (87%); feces (10%)
Administration
Oral Administration
Swallow extended/sustained-release tablets whole; do not chew, crush, or split; this may lead to adverse effects including seizures
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Forfivo XL oral - | 450 mg tablet |  | |
| Wellbutrin SR oral - | 150 mg tablet |  | |
| Wellbutrin SR oral - | 100 mg tablet |  | |
| Wellbutrin SR oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| bupropion HCl oral - | 450 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 300 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 150 mg tablet |  | |
| bupropion HCl oral - | 450 mg tablet |  | |
| bupropion HCl oral - | 200 mg tablet |  | |
| bupropion HCl oral - | 100 mg tablet |  | |
| bupropion HCl oral - | 75 mg tablet |  | |
| Wellbutrin XL oral - | 150 mg tablet |  | |
| Wellbutrin XL oral - | 300 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
bupropion HCl oral
BUPROPION HCL EXTENDED-RELEASE (ANTIDEPRESSANT) - ORAL
(bue-PROE-pee-on HYE-droe-KLOR-ide)
COMMON BRAND NAME(S): Wellbutrin XL
WARNING: Bupropion hydrochloride (HCL) is an antidepressant used for smoking cessation and to treat a variety of conditions, including depression and other mental/mood disorders. Antidepressants can help prevent suicidal thoughts/attempts and provide other important benefits. However, a small number of people (especially people younger than 25) who take antidepressants for any condition may experience new or worsening depression, other mental/mood symptoms, or suicidal thoughts/attempts. It is very important to talk with the doctor about the risks and benefits of antidepressant medication, even if treatment is not for a mental/mood condition.Tell the doctor right away if you notice new or worsening depression/other psychiatric conditions, unusual behavior changes (including possible suicidal thoughts/attempts), or other mental/mood changes (including new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings, impulsive actions, severe restlessness, very rapid speech). Be especially watchful for these symptoms when a new antidepressant is started or when the dose is changed.If you are using bupropion to quit smoking and experience any of these symptoms, stop taking it and contact your doctor right away. Also, tell your doctor right away if you have any of these symptoms after stopping treatment with bupropion.
USES: This medication is used to treat depression. It may also be used to prevent seasonal affective disorder (SAD), a type of depression that occurs each year at the same time (for example, during winter). This medication can improve your mood and feelings of well-being. It may work by restoring the balance of certain natural substances (dopamine, norepinephrine) in the brain.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using bupropion and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily in the morning. If you have stomach upset, you may take this medication with or after a meal or snack. Taking this medication late in the day may cause trouble sleeping (insomnia). Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Swallow the tablets whole. Do not crush or chew the tablets. Doing so can release all of the drug at once, increasing the risk of side effects.The dosage is based on your medical condition and response to treatment. To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.Do not stop taking this medication without consulting your doctor. Your dose may need to be gradually decreased.It may take 4 weeks or longer before you get the full benefit of this drug. Tell your doctor if your condition does not improve or if it worsens.
SIDE EFFECTS: See also Warning section.Dry mouth, sore throat, dizziness, nausea, vomiting, ringing in the ears, headache, decreased appetite, weight loss, constipation, trouble sleeping, increased sweating, or shaking (tremor) may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.An empty tablet shell may appear in your stool. This effect is harmless because your body has already absorbed the medication.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high.Tell your doctor right away if you have any serious side effects, including: fast/pounding/irregular heartbeat, mental/mood changes (such as anxiety, agitation, confusion, unusual behavior/thinking, memory loss), unusual weight loss or gain.Get medical help right away if you have any very serious side effects, including: seizure, eye pain/swelling/redness, widened pupils, vision changes (such as seeing rainbows around lights at night, blurred vision).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking bupropion, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, heart disease, high blood pressure, kidney problems, liver disease, use/abuse of drugs/alcohol, seizures or conditions that increase your risk of seizures (including brain/head injury, brain tumor, eating disorders such as bulimia/anorexia nervosa), personal or family history of glaucoma (angle-closure type).This medication should not be used if you are suddenly stopping regular use of sedatives (including benzodiazepines such as lorazepam), drugs used to treat seizures, or alcohol. Doing so may increase your risk of seizures.This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). Alcohol can also increase your risk of seizures.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially dizziness and memory loss. Dizziness can increase the risk of falling.During pregnancy, this medication should be used only when clearly needed. Since untreated mental/mood problems (such as depression, seasonal affective disorder, bipolar disorder) can be a serious condition, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.This drug passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also Precautions section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: codeine, pimozide, tamoxifen, thioridazine.Taking MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Avoid taking MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before and after treatment with this medication. Ask your doctor when to start or stop taking this medication.This medication may interfere with certain medical/lab tests (such as brain scan for Parkinson's disease, urine screening for amphetamines), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: seizures, severe confusion, hallucinations, rapid heart rate, loss of consciousness.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood pressure, liver function) may be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised June 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
