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bupropion (Rx)Brand and Other Names:Wellbutrin, Zyban, more...Budeprion SR, Aplenzin, Buproban, Wellbutrin SR, Wellbutrin XL, Forfivo XL

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet (Wellbutrin)

  • 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
more...

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): 75 mg once daily
  • 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

Administration

Swallow extended-release tablets whole; do not chew, crush, or split

Dosage Forms & Strengths

tablet (Wellbutrin)

  • 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
more...

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

bupropion and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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

            Parkinsonism

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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

            Use for smoking cessation

            • Serious neuropsychiatric events, including, but not limited to, depression, suicidal ideation, suicide attempt, and completed suicide, have been reported in patients taking bupropion for smoking cessation

            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

            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 disorder or condition that increases risk of seizure (see Contraindications)

            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

            SR and XL tablets: Do not chew, divide, or crush tablets, as this may lead to an increased risk of adverse effects, including seizures

            Discontinue permanently in patients who experience seizures

            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

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Enters breast milk; use caution

            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.

            more...
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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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            Images

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            Formulary

            FormularyPatient Discounts

            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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