bupropion (Rx)

Brand and Other Names:Zyban, Budeprion SR, more...Aplenzin, Buproban, Wellbutrin SR, Wellbutrin XL, Forfivo XL
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Dosing & Uses

AdultPediatric

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)

  • 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: 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

  • Initial: Up to 3 mg/kg/day or 150 mg/day PO  
  • Titrate to 6 mg/kg/day or 300 mg/day, maximum

Sustained-release

  • Initial: Up to 3 mg/kg/day or 150 mg/day PO  
  • Titrate to 6 mg/kg/day or 300 mg/day, maximum
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Interactions

Interaction Checker

and bupropion

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            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)

            • abametapir

              abametapir will increase the level or effect of bupropion by affecting hepatic enzyme CYP2B6 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP2B6 substrates. If not feasible, avoid use of abametapir.

            • 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.

            • 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 (111)

            • 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.

            • 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.

            • 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.

            • 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.

            • 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. .

            • 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. .

            • 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.

            • warfarin

              bupropion increases effects of warfarin by unknown mechanism. Use Caution/Monitor. Altered PT/INR infrequently associated with hemorrhagic or thrombotic complications were observed when bupropion was administered with warfarin. Monitor INR when bupropion is added to existing warfarin regimen.

            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.

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            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

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            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
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            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.

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            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%)

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            Administration

            Oral Administration

            Swallow extended/sustained-release tablets whole; do not chew, crush, or split; this may lead to adverse effects including seizures

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            bupropion HCl oral
            -
            300 mg tablet
            bupropion HCl oral
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            150 mg tablet
            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            bupropion HCl oral
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            75 mg tablet
            bupropion HCl oral
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            200 mg tablet
            bupropion HCl oral
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            100 mg tablet
            Wellbutrin XL oral
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            150 mg tablet
            Wellbutrin XL oral
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            300 mg tablet
            Wellbutrin SR oral
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            150 mg tablet
            Wellbutrin SR oral
            -
            100 mg tablet
            Wellbutrin SR oral
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            200 mg tablet
            Forfivo XL oral
            -
            450 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            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.Do not crush or chew extended-release tablets. Doing so can release all of the drug at once, increasing the risk of side effects. Also, do not split the tablets unless they have a score line and your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing or chewing.The dosage is based on your medical condition, liver function, 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 persist or worsen, 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.Stop taking bupropion and 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), painful sores in the mouth/around the eyes, 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 include: 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/laboratory tests (including brain scan for Parkinson's disease, urine screening for amphetamines), possibly causing false results. Tell laboratory personnel and all your doctors 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.Keep all regular medical and psychiatric appointments. Laboratory and/or medical tests (such as blood pressure, liver function) may be performed periodically to monitor your progress or check for side effects. 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 September 2021. Copyright(c) 2021 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.

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            Formulary

            FormularyPatient Discounts

            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.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.