Brand names: Aplenzin, Forfivo XL, Wellbutrin
Drug class: Antidepressants, Miscellaneous

Medically reviewed by Drugs.com on Jul 10, 2025. Written by ASHP.

Introduction

Antidepressant and smoking deterrent; aminoketone derivative.

Uses for buPROPion

Major Depressive Disorder

Conventional tablets, sustained-release (Wellbutrin SR) tablets, and extended-release (Wellbutrin XL) tablets used for treatment of major depressive disorder as defined by the Diagnostic and Statistical Manual (DSM).

Guidelines from the American Psychiatric Association (APA) and the Department of Veterans Affairs/Department of Defense state that there is no evidence to suggest superiority of one first-line antidepressant over another. Recommended first-line agents for initial treatment of major depressive disorder include bupropion, mirtazapine, an SSRI, an SNRI, trazodone, vilazodone, or vortioxetine. Select an initial antidepressant for treatment based on the following factors: patient preference; nature of prior response to medication; safety, tolerability, and anticipated adverse effects; concurrent psychiatric and medical conditions; specific properties of the medication; and cost.

Seasonal Affective Disorder

Extended-release tablets (Wellbutrin XL, Aplenzin) used for prevention of seasonal major depressive episodes in patients with a diagnosis of seasonal affective disorder.

Smoking Cessation

Extended-release (SR) 150-mg tablets used as an aid to smoking cessation therapy; may be used in combination with a nicotine transdermal system if necessary.

US Preventive Services Task Force (USPSTF) guideline recommends that clinicians ask all adults about tobacco use and provide behavioral interventions. Pharmacotherapy is recommended in all nonpregnant adults who use tobacco. Recommended pharmacotherapy interventions include nicotine replacement therapy (NRT), bupropion hydrochloride SR, and varenicline. The American Thoracic Society (ATS) recommends varenicline over bupropion for adult patients in whom pharmacotherapy is being initiated. US Public Health Service (USPHS) guideline recommends bupropion SR as one of several first-line drugs that may reliably increase long-term smoking abstinence rates.

Depression Associated with Bipolar Disorder

Has been used for treatment of bipolar depression^{† [off-label]} (bipolar disorder, depressive episode).

Legacy guideline from APA considers bupropion one of several second-line agents for use when first-line agents are ineffective or not tolerated. Guidelines from the Department of Veterans Affairs/Department of Defense state there is insufficient evidence to recommend for or against use of antidepressants as monotherapy or to augment treatment with second-generation antipsychotics or mood stabilizers for acute bipolar depression.

Panic Disorder

Has been used in the treatment of panic disorder^{† [off-label]}.

APA legacy guidelines state bupropion may be useful for some patients for the treatment of panic disorder, but cannot be recommended first-line given the limited and mixed data regarding its efficacy.

Stimulant Use Disorder

Has been used for the treatment of specific types of stimulant use disorder including cocaine-use disorder^{† [off-label]} and amphetamine-type stimulant disorder^{† [off-label]}.

American Society of Addiction Medicine (ASAM) and American Academy of Addiction Psychiatry (AAAP) state that bupropion may be considered in patients with cocaine-use disorder to promote abstinence from cocaine use. Bupropion, with or without naltrexone, may be considered in patients with amphetamine-type stimulant use disorder to promote reduced use of amphetamine-type stimulants.

Cancer-related fatigue

Has been used for the treatment of cancer-related fatigue^{† [off-label]}.

American Society of Clinical Oncology (ASCO) guidelines recommend against use of antidepressants to manage symptoms of cancer-related fatigue in adults undergoing cancer treatment based on lack of benefit in studies using SSRIs. However, ASCO states there is interest evaluating other antidepressants with differing mechanisms such as bupropion.

buPROPion Dosage and Administration

General

Pretreatment Screening

• Assess BP before initiating bupropion.

• Screen for history of bipolar disorder and risk factors for bipolar disorder (e.g., family history of suicide, bipolar disorder, or depression) prior to initiating therapy.

Patient Monitoring

• Monitor and closely observe for any indication for clinical worsening, suicidality, or unusual changes in behavior, particularly during initial therapy or following any change (increase or decrease) in dosage.

• Monitor for serious neuropsychiatric symptoms or worsening of preexisting psychiatric illness.

• Monitor BP periodically.

• Consider monitoring renal function in geriatric patients.

• Closely monitor patients with renal impairment (Cl_cr <90 mL/minute) for adverse reactions that could indicate high exposures of bupropion or its metabolites.

• Monitor for development of seizures.

Dispensing and Administration Precautions

• The Institute for Safe Medication Practices (ISMP) includes Wellbutrin SR and Wellbutrin XL, and buPROPion and busPIRone on their List of Confused Drug Names, and recommends using special safeguards to ensure the accuracy of prescriptions for these drugs; these may include strategies such as using both brand and generic names on prescriptions/labels, using tall-man (mixed case) letters, and including the purpose of the medication on prescriptions.

Other General Considerations

• Increase dosage gradually to minimize risk of seizure.

• If a patient is being transitioned to bupropion therapy from an MAOI, allow at least 14 days to elapse between discontinuation of the MAOI and initiation of bupropion; conversely, if switching from bupropion to an MAOI, allow at least 14 days to elapse between discontinuation of bupropion therapy and initiation of the MAOI.

• When switching patients from bupropion hydrochloride conventional tablets or bupropion hydrochloride sustained-release film-coated tablets (e.g., Wellbutrin SR) to bupropion hydrochloride extended-release tablets (Wellbutrin XL), give the same total daily dose when possible.

• Do not initiate treatment with bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL). For initial dosage titration, use another bupropion formulation; 450-mg tablets can be used in patients who are receiving 300 mg per day for at least 2 weeks and require a dosage of 450 mg per day. If a patient is currently treated with another bupropion formulation at 450 mg per day, the patient can be switched to an equivalent dosage of the 450-mg tablets once daily.

• When discontinuing treatment of bupropion hydrochloride extended-release tablets (Wellbutrin XL) 300 mg once daily, decrease dosage to 150 mg once daily prior to discontinuation.

• When discontinuing treatment with bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL), use another bupropion formulation for tapering the dosage prior to discontinuation.

• When discontinuing treatment with bupropion hydrobromide extended-release tablets (Aplenzin) 348 mg once daily, decrease dosage to 174 mg bupropion hydrobromide once daily prior to discontinuation.(227)

• When used for smoking cessation, bupropion extended-release tablets (SR) may be used with a nicotine transdermal system.

• When used for smoking cessation, patients receiving bupropion extended-release tablets (SR) should be advised of behavioral interventions, counseling services, and other support services to be used to increase likelihood of quitting smoking and remaining abstinent. If a patient fails an attempt to quit, the patient may benefit from interventions and/or NRT to improve chances for success on subsequent attempts.

Administration

Oral Administration

Administer orally with or without food.

Conventional Bupropion Hydrochloride Tablets

Initially, administer orally twice daily in the morning and evening, then increase to 3 times daily, with ≥6 hours separating doses.

Dosages ≥300 mg should be administered as divided doses ≤150 mg per dose.

Avoid bedtime administration of evening dose to decrease incidence of insomnia.

Do not chew, divide, or crush tablets; swallow tablets whole.

Extended-release Tablets

Sustained-release (SR), film-coated bupropion hydrochloride tablets (e.g., Wellbutrin SR): Initially, administer orally once daily in the morning, then increase to twice daily, in the morning and evening. Dosages >150 mg should be administered as divided doses twice daily, with ≥8 hours separating the doses. Avoid bedtime administration of evening dose to decrease incidence of insomnia.

Extended-release (SR) bupropion hydrochloride tablets: Administer orally once daily for the first 3 days, then usually increase to twice daily administration with ≥8 hours separating the doses. Avoid bedtime administration of evening dose to decrease incidence of insomnia.

Extended-release bupropion hydrobromide (Aplenzin) or bupropion hydrochloride (Wellbutrin XL) tablets: Administer orally once daily in the morning.

Extended-release bupropion hydrochloride 450-mg film-coated tablets (Forfivo XL): Administer orally once daily in the morning.

Do not chew, divide, or crush extended-release tablets; tablets should be swallowed whole.

The shell of some extended-release tablets (e.g., Aplenzin, Wellbutrin XL) does not dissolve and may be passed in the stool.

Dosage

Available as bupropion hydrochloride or bupropion hydrobromide; dosage expressed in terms of the salt.

Bupropion hydrobromide doses of 174, 348, and 522 mg are equivalent to bupropion hydrochloride doses of 150, 300, and 450 mg, respectively.

Adults

Major Depression

Optimum duration of treatment not established; however, acute depressive episodes thought to require several months or longer of sustained antidepressant therapy.

Unknown whether dosage required for initial response is identical to dosage needed to maintain response.

Periodically reevaluate usefulness and appropriate dosage of drug in patients receiving prolonged therapy with conventional, SR, or extended-release tablets.

Therapy with Conventional Bupropion Hydrochloride Tablets

Oral

Initially, 100 mg twice daily.

To minimize risk of seizures, do not increase dosage by >100 mg daily every 3 days.

If clinical improvement not apparent after >3 days, may increase to 100 mg 3 times daily.

Dosages >300 mg should not be considered until completion of several weeks of therapy; if no improvement is apparent, then the dosage may be increased to a maximum of 150 mg 3 times daily.

Therapy with Sustained-release and Extended-release Bupropion Hydrochloride Tablets

Oral

Sustained-release, film-coated tablets (e.g., Wellbutrin SR): Initially, 150 mg once daily in the morning. If tolerated, may increase to target dosage of 150 mg twice daily (with ≥8 hours between doses) as early as day 4 of therapy. Dosages >300 mg daily should not be considered until completion of several weeks of therapy; then, if no apparent improvement, may increase dosage to maximum of 200 mg twice daily (with ≥8 hours between doses).

Extended-release tablets (Wellbutrin XL): Initially, 150 mg once daily. If tolerated, may increase to target dosage of 300 mg once daily after 4 days of therapy.

Extended-release tablets (Forfivo XL): 450 mg once daily in patients who have received another bupropion hydrochloride formulation at a dosage of 300 mg daily for ≥2 weeks and require a dosage of 450 mg daily, or in patients currently receiving bupropion hydrochloride 450 mg daily of another bupropion formulation.

Therapy with Extended-release Bupropion Hydrobromide Tablets

Oral

Extended-release tablets (e.g., Aplenzin): Initially, 174 mg once daily in the morning. After day 4 of therapy, may increase to target dosage of 348 mg once daily in the morning.

Seasonal Affective Disorder

Therapy with Extended-release Bupropion Hydrochloride Tablets

Oral

Extended-release tablets (Wellbutrin XL): Initiate therapy in autumn prior to onset of depressive symptoms; continue treatment through the winter and taper and discontinue in early spring. Individualize timing of initiation and duration of therapy based on patient’s historical pattern of seasonal depressive episodes.

Initially, 150 mg once daily in the morning. If tolerated, increase dosage after 7 days to target dosage of 300 mg once daily.

For patients receiving 300 mg once daily during the autumn-winter period, taper dosage to 150 mg once daily prior to discontinuance.

Therapy with Extended-release Bupropion Hydrobromide Tablets

Oral

Extended-release tablets (Aplenzin): Initiate therapy in autumn prior to onset of depressive symptoms; continue treatment through the winter and taper and discontinue in early spring. Individualize timing of initiation and duration of therapy based on patient’s historic pattern of seasonal depressive episodes.

Initially, 174 mg once daily. After 7 days of dosing, may increase to target dose of 348 mg once daily in the morning.

For patients receiving 348 mg once daily during the autumn-winter period, taper dosage to 174 mg once daily prior to discontinuance.

Smoking Cessation

Therapy with Extended-release (SR) Bupropion Hydrochloride Tablets

Oral

Initially, 150 mg daily for the first 3 days of therapy. Initiate 1–2 weeks prior to discontinuance of cigarette smoking.

Maintenance, 150 mg twice daily (with ≥8 hours between doses). Continue therapy for 7–12 weeks; evaluate need for prolonged therapy after that period based on individual patient assessment.

Cessation of smoking is unlikely in patients who do not show substantial progress toward abstinence after 7 weeks of therapy, so such therapy generally should be discontinued at that time in these patients.

Special Populations

Hepatic Impairment

Smoking cessation in patients with severe hepatic cirrhosis: Maximum 150 mg every other day as extended-release (SR) tablets .

Major depression, seasonal affective disorder, or smoking cessation in patients with mild hepatic impairment (Child-Pugh score: 5–6): Reduce dosage and/or frequency of administration as required.

Bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL) are not recommended for patients with hepatic impairment.

Renal Impairment

Active metabolites may accumulate; reduce dosage and/or frequency of administration as required for patients with a Cl_cr < 90 mL/minute.

Bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL) are not recommended for patients with renal impairment.

Geriatric Patients

Use caution when administering bupropion to geriatric patients; consider dosage reduction and monitor renal function due to age-related decreases in renal function.

Cautions for buPROPion

Contraindications

• Seizure disorders.

• Current or past diagnosis of anorexia nervosa or bulimia.

• Patients receiving any other bupropion formulation because risk of seizures is dose-dependent.

• Patients undergoing abrupt discontinuance of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs.

• Patients currently receiving, or having recently received (i.e., within 14 days), MAOI therapy.

• Patients currently receiving a reversible MAOI (e.g., linezolid, IV methylene blue).

• Hypersensitivity to the drug or any ingredient in the formulation.

Warnings/Precautions

Warnings

Suicidal Thoughts and Behaviors in Children, Adolescents, and Young Adults

Increased risk of suicidal thoughts and behavior in adolescent and young adult patients taking antidepressants (See Boxed Warning). Depression itself is a risk factor for suicidal thoughts and behaviors.

Monitor all patients treated with bupropion for any indication for clinical worsening and emergence of suicidal thoughts and behaviors, particularly during initiation of therapy (i.e., the first few months) and during periods of dosage adjustments.

Counsel families and caregivers to monitor for changes in the patient's behavior, and to report such symptoms to a clinician. Consider changing the therapeutic regimen or discontinuing therapy in patients whose depression is persistently worse or in patients experiencing emergent suicidal thoughts or behaviors. .

Other Warnings and Precautions

Neuropsychiatric Symptoms and Suicidality in Smoking Cessation Treatment

Serious neuropsychiatric symptoms, including mood changes (e.g., depression, mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, hostility, agitation, aggression, anxiety, and panic as well as suicidal ideation, suicide attempt, and completed suicide, reported.

Monitor patients for neuropsychiatric symptoms or for worsening of preexisting psychiatric conditions. Discontinue bupropion in patients who develop agitation, hostility, depressed mood, or changes in behavior or thinking that are not typical for the patient or who develop suicidal ideation or suicidal behavior.

Seizures

Dose-related increase in risk of seizures reported; increase dose gradually and avoid exceeding recommended daily and single doses. Do not exceed a total daily dosage of 450 mg (as 150 mg 3 times daily) of bupropion hydrochloride as conventional tablets; 400 mg daily (as 200 mg twice daily) of bupropion hydrochloride as sustained-release, film-coated tablets (e.g., Wellbutrin SR); 300 mg daily (as 150 mg twice daily) of bupropion hydrochloride as extended-release (SR) tablets for smoking cessation; 300 mg once daily of bupropion hydrochloride as extended-release tablets (e.g., Wellbutrin XL); 450 mg once daily of bupropion hydrochloride as extended-release, 450-mg tablets (Forfivo XL); or 522 mg once daily of bupropion hydrobromide as extended-release tablets (Aplenzin).

Bupropion is contraindicated in patients with a seizure disorder, anorexia nervosa or bulimia, or undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs.

If patients experience a seizure during therapy, discontinue medication and do not restart.

Hypertension

Hypertension (sometimes severe) has occurred with bupropion therapy. Risk of hypertension is increased with concomitant use of MAOIs (contraindicated) or other dopaminergic or noradrenergic drugs; also increased with concomitant transdermal nicotine therapy.

Safety in patients with recent history of MI or unstable heart disease not established.

Assess blood pressure before initiating bupropion and monitor periodically during therapy, especially in patients receiving concomitant NRT.

Activation of Mania or Hypomania

Possible precipitation of manic, mixed, or hypomanic manic episodes; risk appears increased in patients with bipolar disorder or who have risk factors for bipolar disorder.

Bupropion is not FDA-labeled for use in treating bipolar depression. Screen for history of bipolar disorder and risk factors for bipolar disorder (e.g., family history of suicide, bipolar disorder, depression) prior to initiating therapy.

Psychosis and Other Neuropsychiatric Effects in Patients Treated for Depression

Neuropsychiatric manifestations, including confusion, delusions, hallucinations, psychosis, disturbances in concentration, and paranoia, reported in patients receiving bupropion in depression trials. Some of these patients had a diagnosis of bipolar disorder. In some cases, symptoms diminished with dosage reduction or withdrawal of therapy. Similar types of neuropsychiatric manifestations reported during postmarketing experience in patients receiving the medication for smoking cessation.

Advise patients to contact a clinician if adverse neuropsychiatric effects occur.

Angle-closure Glaucoma

Pupillary dilation (mydriasis) occurs with many antidepressants, including bupropion, and may trigger an acute attack of angle-closure glaucoma (narrow-angle glaucoma) in patients with anatomically narrow angles who do not have a patent iridectomy.

Hypersensitivity Reactions

Anaphylactoid/anaphylactic reactions (e.g., pruritus, urticaria, angioedema, dyspnea) reported. Postmarketing reports include erythema multiforme, Stevens-Johnson syndrome, and anaphylactic shock.

Possible arthralgia, myalgia, and fever with rash and other symptoms suggestive of delayed hypersensitivity.

Advise patients to discontinue bupropion and contact their clinician if symptoms of a possible hypersensitivity reaction occur.

Specific Populations

Pregnancy

Data from epidemiologic studies have not shown an overall increased risk for congenital malformations with bupropion. International bupropion pregnancy registry was not designed or powered to evaluate specific defects; however, possible increase in cardiac malformations identified.

National Pregnancy Registry for Antidepressants at 1-844-405-6185 or [Web].

Consider the risks to the female of untreated depression and potential effects on the fetus when discontinuing or changing treatment with antidepressant medications during pregnancy and postpartum.

Encourage pregnant smokers to attempt cessation using educational and behavioral interventions before using medication approaches. Use bupropion extended-release (SR) tablets during pregnancy only if potential benefit justifies potential risk to the fetus.

Lactation

Distributed into milk. Effects of bupropion or its metabolites on milk production not known.

Limited data from postmarketing reports of bupropion use in nursing females have not identified a clear association of adverse reactions in the breast-fed infant. Postmarketing reports of seizures in breast-fed infants; however, causal relationship not established.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

FDA warns that a greater risk of suicidal thinking or behavior (suicidality) occurred during first few months of antidepressant treatment compared with placebo in children and adolescents with major depressive disorder, obsessive-compulsive disorder (OCD), or other psychiatric disorders based on pooled analyses of 24 short-term, placebo-controlled trials of 9 antidepressant drugs (SSRIs and others). However, a later meta-analysis of 27 placebo-controlled trials of 9 antidepressants (SSRIs and others) in patients <19 years of age with major depressive disorder, OCD, or non-OCD anxiety disorders suggests that the benefits of antidepressant therapy in treating these conditions may outweigh the risks of suicidal behavior or suicidal ideation. No suicides occurred in these pediatric trials.

Carefully consider these findings when assessing potential benefits and risks of bupropion in a child or adolescent for any clinical use.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults; however, possibility of increased sensitivity to the medication in some older patients cannot be ruled out.

Consider increased possibility of impaired renal function, which may increase risk of adverse effects, when selecting dosage; may be useful to monitor renal function.

In pooled data analyses, a reduced risk of suicidality was observed in adults ≥65 years of age with antidepressant therapy compared with placebo.

Hepatic Impairment

Reduced dosage required in patients with severe hepatic impairment (Child-Pugh score: 7–15). In patients with severe hepatic impairment, maximum plasma concentration increased by 70% and mean half-life increased (29 hours versus 19 hours in healthy patients).

In patients with mild hepatic impairment (Child-Pugh score: 5–6), consider reduced dosage and/or frequency.

Use of bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL) not recommended for patients with hepatic impairment.

Renal Impairment

Use with caution; parent drug and active metabolites may accumulate. Monitor closely for adverse effects that could indicate high bupropion or metabolite exposures; consider reduced dosage and/or frequency. Compared to patients with normal renal function, patients with moderate-to-severe renal impairment (Cl_cr 30.9 +/- 10.8 mL/minute) were found to have about an approximately 2-fold higher exposure to bupropion when administered a single 150 mg dose of SR bupropion.

Use of bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL) not recommended for patients with renal impairment.

Common Adverse Effects

Adverse effects (≥5%) in patients receiving conventional bupropion hydrochloride tablets: Agitation, dry mouth, constipation, headache/migraine, nausea/vomiting, dizziness, excessive sweating, tremor, insomnia, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmias, auditory disturbance.

Adverse effects (≥5%) in patients receiving bupropion hydrochloride sustained-release, film-coated tablets (e.g., Wellbutrin SR): Headache, dry mouth, nausea, insomnia, dizziness, pharyngitis, constipation, agitation, anxiety, abdominal pain, tinnitus, tremor, palpitation, myalgia, sweating, rash, anorexia.

Adverse effects (≥5%) in patients receiving bupropion hydrochloride extended-release (SR) tablets for smoking cessation: Insomnia, rhinitis, dry mouth, dizziness, nervous disturbance, anxiety, nausea, constipation, arthralgia.

Adverse effects (≥5%) in patients receiving bupropion hydrochloride extended-release tablets (e.g., Wellbutrin XL, Forfivo XL): Dry mouth, nausea, insomnia, dizziness, pharyngitis, abdominal pain, agitation, anxiety, tremor, palpitation, sweating, tinnitus, myalgia, anorexia, urinary frequency, rash.

Adverse effects (≥5%) in patients receiving bupropion hydrobromide extended-release tablets (e.g., Aplenzin): Dry mouth, nausea, insomnia, dizziness, pharyngitis, abdominal pain, agitation, anxiety, tremor, palpitation, sweating, tinnitus, myalgia, anorexia, urinary frequency, rash.

Drug Interactions

Metabolized to hydroxybupropion, principally by CYP2B6; CYP isoenzymes not involved in the formation of other bupropion metabolites.

Bupropion and its metabolites inhibit CYP2D6.

Drugs Affecting Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (altered serum concentrations of bupropion) with medications that induce or inhibit CYP2B6.

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP2D6: Potential pharmacokinetic interaction (increased plasma substrate concentrations). Dosage reduction of the CYP2D6 substrate may be necessary, particularly for medications with a narrow therapeutic index.

Prodrugs dependent on CYP2D6 for activation (e.g., tamoxifen): Possible reduced clinical efficacy of the prodrug. An increase in dosage of the prodrug may be necessary.

Drugs Affecting the Seizure Threshold

Use extreme caution with concomitant use of other medications (e.g., other antidepressants, other bupropion-containing drugs, antipsychotic agents, theophylline, systemic corticosteroids) or treatment regimens (e.g., abrupt discontinuation of benzodiazepines) that lower the seizure threshold.

Smoking Cessation

Cessation of smoking (with or without adjunctive use of bupropion) may result in decreased enzyme induction and altered metabolism of some medications (e.g., theophylline, warfarin, insulin); consider dosage adjustment.

Specific Drugs

buPROPion Pharmacokinetics

Absorption

Bioavailability

Peak plasma concentrations usually occur within 2, 3, or 5 hours after oral administration of conventional, sustained-release film-coated (e.g., Wellbutrin SR) or extended-release (Wellbutrin XL) bupropion hydrochloride tablets, respectively. Peak plasma concentrations occur within approximately 5 or 12 hours under fasted or fed conditions, respectively, after oral administration of extended-release, 450-mg bupropion hydrochloride tablets (Forfivo XL). Peak plasma concentrations occur within approximately 5 hours after oral administration of extended-release bupropion hydrobromide tablets (Aplenzin).

Steady-state plasma concentrations of bupropion achieved within 8 days.

At steady state, conventional and extended-release tablets (Wellbutrin SR, Wellbutrin XL) are essentially bioequivalent.

Bupropion hydrochloride extended-release, 450-mg tablets (Forfivo XL) and bupropion hydrobromide extended-release tablets (Aplenzin) are bioequivalent to bupropion hydrochloride extended-release tablets (e.g., Wellbutrin XL), Bupropion hydrobromide doses of 174, 348, or 522 mg are equivalent to bupropion hydrochloride doses of 150, 300, or 450 mg, respectively.

Food

Food does not appear to substantially affect the peak plasma concentration or extent of absorption achieved with extended-release tablets.

Distribution

Extent

Bupropion and its metabolites are distributed into milk.

Plasma Protein Binding

84% bound to human albumin.

Elimination

Metabolism

Extensively metabolized in the liver to 3 active metabolites: hydroxybupropion (principally by CYP2B6), threohydrobupropion, and erythrohydrobupropion. CYP isoenzymes not involved in the formation of threohydrobupropion and erythrohydrobupropion metabolites.

Elimination Route

Excreted in urine (87%) and feces (10%), principally as metabolites.

Half-life

The half-life in the terminal phase (t_½β) averages about 21 hours after chronic dosing.

Special Populations

Hepatic impairment can decrease elimination of bupropion.

Renal impairment may decrease elimination of major metabolites.

Stability

Storage

Oral

Conventional Bupropion Hydrochloride Tablets

20–25°C in tight container; protect from light and moisture.

Extended-release Bupropion Hydrochloride Tablets

Sustained-release (e.g., Wellbutrin SR): 20–25°C (excursions permitted to 15–30°C); protect from light and moisture.

Extended-release tablets (Wellbutrin XL): 25°C (excursions permitted to 15–30°C).

Extended-release 450-mg tablets (Forfivo XL): 20–25°C.

Extended-release Bupropion Hydrobromide Tablets

Extended-release tablets (Aplenzin): 25°C (excursions permitted to 15–30°C).

Actions

• Chemically unrelated to tricyclic, tetracyclic, or other currently available antidepressants (e.g., SSRIs); also chemically unrelated to nicotine or other agents currently used in treatment of nicotine dependence.

• Mechanism of antidepressant action is unclear; noradrenergic and/or dopaminergic pathways appear to be principally involved. Relatively weak inhibitor of the neuronal reuptake of norepinephrine and dopamine; does not inhibit monoamine oxidase or reuptake of serotonin.

• Mechanism of action as an adjunct in the cessation of smoking is unclear; noradrenergic and/or dopaminergic effects presumably are involved.

Advice to Patients

• Advise patients to read the FDA-approved patient labeling (medication guide).

• Advise patients to swallow tablets whole and not to crush, chew, or divide the tablets.

• Advise patients to take conventional bupropion hydrochloride tablets in 3–4 divided doses daily, with ≥6 hours between subsequent doses.

• Instruct patients to take bupropion hydrochloride extended-release tablets in two divided doses, preferably with ≥8 hours between successive doses, when doses are >150 mg daily to minimize the risk of seizures.

• Instruct patients to take bupropion hydrochloride extended-release tablets (e.g., Wellbutrin XL) once daily in the morning.

• Instruct patients that if they miss a dose, they should not take an extra tablet to make up for the missed dose and should take the next tablet at the regular time because of the dose-related risk of seizure.

• Advise patients and caregivers to monitor for the emergence of suicidal thoughts and behaviors, especially during the first few months of therapy or during periods of dosage adjustment. Advise families and caregivers of patients to observe for the emergence of such symptoms on a day-to-day basis, since changes may be abrupt; such symptoms should be reported to the patient’s clinician, especially if they are severe, abrupt in onset, or were not part of the patient’s presenting symptoms.

• Inform patients of the risk of serious neuropsychiatric symptoms, including changes in mood (e.g., depression, mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic as well as suicidal ideation, suicide attempt, and completed suicide, when used for smoking cessation. Instruct patients to discontinue bupropion and contact a clinician if they experience such symptoms.

• Inform patients of the risk of hypersensitivity reactions. Advise patients to stop taking bupropion and notify their clinician if they develop signs of a severe allergic reaction.

• Inform patients of the risk of seizures. Advise patients to permanently stop taking the drug and immediately notify their clinician if they have a seizure. Advise patients to minimize or avoid use of alcohol.

• Advise patients that bupropion can cause mild pupillary dilation, which can lead to an episode of angle-closure glaucoma in susceptible individuals.

• Advise patients to avoid concomitant therapy with any other preparations containing bupropion.

• Advise patients of the potential for impaired ability to perform tasks requiring judgment or motor and cognitive skills. Advise patients to avoid operating machinery or driving a motor vehicle until the effects on the individual are known. Inform patients that bupropion may decrease alcohol tolerance.

• Instruct patients to minimize or avoid consumption of alcohol; excessive use of alcohol or abrupt cessation of use may alter the seizure threshold.

• Advise patients that Wellbutrin SR and WellbutrinXL may have an odor.

• Advise patients to store conventional bupropion hydrochloride tablets, film-coated sustained-release tablets (e.g., Wellbutrin SR) at room temperature (20–25ºC) and to keep the tablets dry and out of light.

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as concomitant illnesses.

• Advise females to inform their clinicians if they are or plan to become pregnant or plan to breast-feed. Advise patients of any pregnancy exposure registry that monitors pregnancy outcomes in females exposed to bupropion during pregnancy. Advise patients that bupropion in distributed into milk in small amounts.

• Advise patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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