Dosing & Uses
Dosing Forms & Strengths
bupropion/naltrexone
extended release tablet
- 90mg/8mg
Obesity
For use as adjunct to reduced-calorie diet and increased physical activity for long-term weight management in adults with initial body mass index of ≥30 kg/m² (obese) or ≥27 kg/m² (overweight) in presence of at least 1 weight-related comorbidity (eg, hypertension, type 2 diabetes, or dyslipidemia)
1 tablet (90mg/8mg) initially week 1; increase by 1 tablet/day each subsequent week until daily maintenance dose of 2 tablets twice daily (360 mg bupropion/32 mg naltrexone) is achieved at the start of week 4
Dosage Modifications
Coadministration with CYP2B6 inhibitors (eg, ticlopidine or clopidogrel): Not to exceed 1 tablet BID
Hepatic impairment
- Mild to moderate: 2 tablets (one tablet each morning and evening)
- Severe hepatic impairment: Not recommended
Renal impairment
- Mild: Not studied
- Moderate-to-severe: Not to exceed 1 tablet BID
- End-stage renal disease: Not recommended
Dosing Considerations
Clinical response should be observed by 4 months of treatment
Discontinue therapy if clinically meaningful weight loss (≥5%) not exhibited after 4 months; other weight management strategies should be considered
Effect on cardiovascular morbidity not established
Safety and efficacy when used in combination with other weight-loss products, including over-the-counter drugs and herbal preparations, not established
Do not administer within 14 days of taking a monoamine oxidase inhibitor for depression
Recommendations to reduce risk of seizure
- Bupropion component may increase the risk of seizures
- Do not exceed 360 mg bupropion component (4 tablets daily)
- Administer daily dose in divided doses (twice daily)
- Escalate dose gradually
- Do not take more than 2 tablets at one time
- Avoid coadministration with high-fat meals
- If dose is missed, wait until next scheduled dose to resume regular dosing schedule
Safety and efficacy not established
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 (21)
- 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.
- bremelanotide
bremelanotide will decrease the level or effect of naltrexone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid using bremelanotide with an orally administered naltrexone-containing product that is intended to treat alcohol and opioid addiction due to the potential for naltrexone treatment failure.
- 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.
- naldemedine
naldemedine, naltrexone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Potential for additive opioid receptor anatagonism and increased risk of opioid withdrawal.
- naloxegol
naloxegol, naltrexone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration; potential for additive effect of opioid receptor anatagonism and increased risk of opioid withdrawal.
- 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.
Monitor Closely (65)
- acamprosate
naltrexone increases levels of acamprosate by unspecified interaction mechanism. Use Caution/Monitor. No dosage adjustment is needed.
- 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. - apalutamide
apalutamide will decrease the level or effect of naltrexone by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.
- 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. - dronabinol
naltrexone increases effects of dronabinol by Other (see comment). Use Caution/Monitor. Comment: Naltrexone may enhance therapeutic effects of cannabinoids. .
- 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.
lofexidine will decrease the level or effect of naltrexone by unknown mechanism. Modify Therapy/Monitor Closely. Coadministration of lofexidine with oral naltrexone resulted in statistically significant differences in the steady-state pharmacokinetics of naltrexone. The efficacy of oral naltrexone may be reduced if administered within 2 hours of taking lofexidine. Interaction not expected with other naltrexone routes of administration. - loratadine
bupropion will increase the level or effect of loratadine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.
- nabilone
naltrexone increases effects of nabilone by Other (see comment). Use Caution/Monitor. Comment: Naltrexone may enhance therapeutic effects of cannabinoids. .
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%
Nausea (32.5%)
Constipation (19.2%)
Headache (17.6%)
Vomiting (10.7%)
1-10%
Dizziness (9.9%)
Insomnia (9.2%)
Dry mouth (8.1%)
Diarrhea (7.1%)
Anxiety (4.2%)
Hot flash (4.2%)
Fatigue (4%)
Tremor (4%)
Upper abdominal pain (3.5%)
Viral gastroenteritis (3.5%)
Influenza (3.4%)
Tinnitus (3.3%)
Urinary tract infection (3.3%)
Hypertension (3.2%)
Abdominal pain (2.8%)
Hyperhidrosis (2.6%)
Irritability (2.6%)
Increased blood pressure (2.4%)
Dysgeusia (2.4%)
Rash (2.4%)
Muscle strain (2.2%)
Palpitations (2.1%)
Frequency Not Defined
Tachycardia
Myocardial infarction
Vertigo
Motion sickness
Lower abdominal pain
Eructation
Lip swelling
Hematochezia
Hernia
Feeling jittery
Thirst
Feeling hot
Asthenia
Cholecystitis
Pneumonia
Staphylococcal infection
Kidney infection
Increased creatinine clearance
Increased hepatic enzymes
Decreased hematocrit
Dehydration
Intervertebral disc protrusion
Jaw pain
Disturbance in attention
Lethargy
Intention tremor
Balance disorder
Memory impairment
Amnesia
Mental impairment
Presyncope
Abnormal dreams
Nervousness
Dissociation (feeling spacy)
Tension
Agitation
Mood swings
Vaginal hemorrhage
Irregular menstruation
Erectile dysfunction
Vulvovaginal dryness
Alopecia
Postmarketing Reports
Loss of consciousness, malaise
Warnings
Black Box Warnings
Not approved for treatment of major depressive disorder or psychiatric disorders
Antidepressants like bupropion increase the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials but were not seen in patients ≥24 years and a lower risk was seen in patients ≥65 years; patients of all ages should be monitored closely for suicidal thoughts and behaviors
Serious neuropsychiatric reactions reported in patients taking bupropion for smoking cessation that occurred during therapy or while discontinuing therapy; patients should be monitored for neuropsychiatric reactions
Contraindications
Uncontrolled hypertension
Seizure disorder or a history of seizures
Use of other bupropion-containing products
Bulimia or anorexia nervosa, which may increase risk of seizures
Long-term opioid or opiate agonists use or acute opiate withdrawal
Patients undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs
Within 14 days of monoamine oxidase inhibitor therapy
Hypersensitivity
Pregnancy
Cautions
Monitor patients for suicidal ideation or behavior and for unusual changes in behavior (see black box warning)
Discontinue therapy and do not restart if seizure occurs while on therapy; use caution when prescribing to patients with predisposing risk factors for seizures
Not for administration to patients receiving long-term opioids, owing to naltrexone component (opioid antagonist); discontinue therapy if long-term opiate therapy required
Following therapy, patients may be more sensitive to opioids, even at lower doses
A patient should not attempt to overcome naltrexone opioid blockade by administering large amounts of exogenous opioids; may lead to fatal overdose
Opioid-dependent patients, including those being treated for alcohol dependence, should be opioid-free (including tramadol) before therapy is initiated; opioid-free interval of a minimum of 7-10 days is recommended for patients previously dependent on short-acting opioids; patients transitioning from buprenorphine or methadone may need as long as 2 weeks
Blood pressure and pulse should be measured prior to starting therapy and should be monitored at regular intervals, particularly among patients with controlled hypertension prior to treatment
Discontinue therapy if symptoms or signs of acute hepatitis occur
Screen patients for a history of bipolar disorder and the presence of risk factors for bipolar disorder; therapy was not studied in patients receiving antidepressant medications patients with a history of bipolar disorder or recent hospitalization foor psychiatric illness were excluded from clinical trials
Angle-closure attack may occur in patients with anatomically narrow angles that do not have a patent iridectomy
Measure blood glucose levels prior to and during therapy; patients who develop hypoglycemia after initiating Contrave therapy should adjust antidiabetic drug regimen
Use caution in patients with history of tumor or infection of the brain or spine
Initiation of therapy in patients receiving linezolid or intravenous (IV) methylene blue
Use caution in hepatic impairment
May precipitate a manic, mixed, or hypomanic episode; risk higher in patients with bipolar disorders or have risk factors for bipolar disorder, including family history of bipolar disorder, suicide, or depression; not FDA approved for bipolar depression
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
Pregnancy & Lactation
Pregnancy
Weight loss offers no benefit to a pregnant patient and may cause fetal harm; when a pregnancy is recognized, advise pregnant patient of risk to fetus, and discontinue therapy; available pharmacovigilance data and data from clinical trials with individual components of combination drug use in pregnant patients have not demonstrated a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes
Bupropion
- Data from epidemiological studies of pregnant patients exposed to bupropion in first trimester have not identified an increased risk of congenital malformations overall
- When bupropion was administered to pregnant rats during organogenesis, there was no evidence of fetal malformations at doses up to approximately 20 times maximum recommended human dose (MRHD) of 360 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 twice the MRHD and greater; decreased fetal weights were seen at doses 5 times MRHD and greater
Naltrexone
- Limited case report data of pregnant patients exposed to naltrexone in first trimester have not identified an increased risk of congenital malformations overall; daily oral administration of naltrexone during period of organogenesis has been shown to increase incidence of early fetal loss in rats and rabbits at doses ≥15 times and ≥60 times MRHD of 32 mg/day respectively
- There was no evidence of fetal malformations in rats and rabbits at doses up to approximately 100 and 200 times the MHRD, respectively
- Appropriate weight gain based on pre-pregnancy weight is currently recommended for all pregnant patients, including those who are already overweight or obese, due to obligatory weight gain that occurs in maternal tissues during pregnancy
Lactation
Data from published literature report the presence of bupropion and its metabolites in human milk
Limited data from postmarketing reports with bupropion use during lactation have not identified a clear association of adverse effects on a breastfed infant
Naltrexone and its major metabolite, 6 β-naltrexol, are present in human milk; there are no data on bupropion, naltrexone, or their metabolites on milk production; the developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug combination or from mother’s underlying 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
Bupropion: Increases dopamine activity in the brain, which appears to lead to a reduction in appetite and increase in energy expenditure by increasing activity of pro-opiomelanocortin (POMC) neurons
Naltrexone: Blocks opioid receptors on the POMC neurons, preventing feedback inhibition of these neurons and further increasing POMC activity
Combination may regulate activity in the dopamine reward system of the brain that helps control food cravings and overeating behaviors
Absorption
Naltrexone
- Peak time: 2 hr
Bupropion
- Peak time: 3 hr
Metabolism
Naltrexone
- Hepatic
Bupropion
- Hepatic, via CYP2B6
Distribution
Naltrexone
- Protein bound: 21%
Bupropion
- Protein bound: 84%
Elimination
Naltrexone
- Excretion: Urine (53-79%)
- Half-life: 5 hr
Bupropion
- Excretion: Urine (87%); feces (10%)
- Half-life: 21 hr
Administration
Oral Administration
Take by mouth in the morning and evening
Do not crush, chew, or cut tablets
Doses >32 mg/360 mg per day not recommended
Do not administer with high-fat meal as it may result in significant increase in bupropion and naltrexone exposure
Therapy may cause elevation in blood pressure or heart rate, especially during initial 3 months of therapy; patients with hypertension should be monitored closely
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Formulary
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