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Pharmacologic class: Aminoketone
Therapeutic class: Second-generation antidepressant, smoking-cessation aid
Pregnancy risk category C
FDA Box Warning
• Antidepressants increase risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders. Risk must be balanced with clinical need, as depression itself increases suicide risk. With patient of any age, observe closely for clinical worsening, suicidality, or unusual behavior changes. Advise family or caregiver to observe patient closely and communicate with prescriber as needed.
• Bupropion hydrobromide (Aplenzin) and bupropion hydrochloride (Budeprion SR, Budeprion XL, Buproban, Wellbutrin, Wellbutrin SR, and Wellbutrin XL) aren't approved for smoking cessation treatment, but bupropion hydrochloride under the names of Buproban and Zyban is approved for this use. Serious neuropsychiatric events, including but not limited to depression, suicidal ideation, suicide attempt, and completed suicide, have been reported in patients taking Buproban and Zyban for smoking cessation. Some cases may have been complicated by the signs and symptoms of nicotine withdrawal in patients who stopped smoking. Risks should be weighed against benefits of their use in smoking cessation.
• Drug isn't approved for use in pediatric patients.
Unclear. Thought to decrease neuronal reuptake of dopamine, serotonin, and norepinephrine in CNS. Action as smoking-cessation aid may result from noradrenergic or dopaminergic activity.
Tablets (extended-release): 174 mg, 348 mg, 522 mg
Tablets: 75 mg, 100 mg
Tablets (extended-release): 150 mg, 300 mg
Tablets (sustained-release): 100 mg, 150 mg, 200 mg
Indications and dosages
Adults: Initially, 100 mg P.O. immediate-release tablet b.i.d. (morning and evening). After 3 days, may increase to 100 mg t.i.d. After 4 weeks, may increase to a maximum dosage of 450 mg/day in divided doses. No single dose should exceed 150 mg. With total daily dosage of 300 mg, wait at least 6 hours between doses; with total daily dosage of 450 mg, wait at least 4 hours between doses. Alternatively, give one 150-mg sustained-release tablet daily; increase to 150-mg sustained-release tablet b.i.d. based on clinical response. Or initially, 174 mg P.O. extended-release tablet daily in the morning; if 174-mg dose is adequately tolerated, increase to 348 mg extended-release tablet daily as early as day 4. An increase in dosage to maximum of 522 mg extended-release tablet daily, given as a single dose, may be considered for patients in whom no clinical improvement is noted after several weeks of treatment at 348 mg/day. Don't exceed single dose of 150 mg for immediate-release tablets, 522 mg for extended-release tablets, or 200 mg for sustained-release tablets.
➣ Smoking cessation
Adults: 150 mg P.O. sustained-release tablet (Zyban) or 150 mg extended-release tablet (Buproban) once daily for 3 days, then 150-mg sustained-release tablet b.i.d. for 7 to 12 weeks. Space doses at least 8 hours apart. Don't exceed maximum dosage of 300 mg daily.
• Hypersensitivity to drug
• Anorexia nervosa or bulimia
• MAO inhibitor use within past 14 days
• Acute alcohol or sedative withdrawal
• Use of other bupropion products
Use cautiously in:
• renal or hepatic impairment, unstable cardiovascular status
• patients with cranial trauma or other predispositions toward seizures, patients treated with other agents that lower seizure threshold (such as antipsychotics, other antidepressants, theophylline, systemic steroids)
• patients with recent history of myocardial infarction or unstable heart disease
• elderly patients
• pregnant or breastfeeding patients
• Be aware that patients should swallow extended- and sustained-release tablets whole and not crush or chew them.
• Be aware that treatment for smoking cessation should start while patient is still smoking, since approximately 1 week of treatment is required to achieve steady-state blood levels of bupropion.
• Avoid bedtime doses because they may worsen insomnia.
☞ Know that drug shouldn't be withdrawn abruptly when used for depression.
CNS: agitation, headache, insomnia, mania, psychoses, depression, dizziness, drowsiness, tremor, anxiety, nervousness, seizures
CV: hypertension, hypotension, tachycardia, palpitations, severe hypertension, complete AV block
EENT: blurred vision, amblyopia, auditory disturbances, epistaxis, rhinitis, pharyngitis
GI: nausea, vomiting, dyspepsia, abdominal pain, flatulence, mouth ulcers, dry mouth
GU: urinary retention, urinary frequency, nocturia, vaginal irritation, testicular swelling
Metabolic: hyperglycemia, changes in libido, hypoglycemia, syndrome of inappropriate antidiuretic hormone secretion
Musculoskeletal: arthralgia, myalgia, leg cramps, twitching, neck pain
Respiratory: bronchitis, increased cough, dyspnea
Skin: photosensitivity, dry skin, pruritus, rash, urticaria, diaphoresis, skin temperature changes, erythema multiforme, Stevens-Johnson syndrome
Other: altered taste, increased or decreased appetite, weight gain or loss, hot flashes, fever, allergic reaction, flulike symptoms, anaphylactoid reactions, anaphylaxis
Drug-drug. Benzodiazepine withdrawal, corticosteroids, other antidepressants, over-the-counter stimulants, phenothiazines, theophylline: increased risk of seizures
Cimetidine: inhibited bupropion metabolism
CYP2B6 substrates or inhibitors (such as clopidogrel, cyclophosphamide, orphenadrine, thiotepa, ticlopidine), efavirenz, fluvoxamine, nelfinavir, nor-fluoxetine, paroxetine, ritonavir, sertraline: increased bupropion activity
Despiramine, paroxetine, ritonavir, sertraline: possibly increased bupropion blood level
Levodopa, MAO inhibitors: increased risk of adverse reactions
Nicotine transdermal system: increased risk of severe hypertension
Drug-diagnostic tests. Glucose: increased level
Drug-behaviors. Alcohol use or cessation: increased risk of seizures
Sun exposure: increased risk of photo-sensitivity
• Monitor blood pressure, ECG, CBC, and renal and hepatic function. Monitor tricyclic antidepressant (TCA) blood level if patient's taking TCAs concurrently.
• Be aware that if patient is also on nicotine patch for smoking cessation, the combination may cause or increase risk of hypertension.
• Check for oral and dental problems.
☞ Instruct patient to seek immediate medical attention if itching, hives, swelling of the throat, or difficulty breathing occurs.
☞ Instruct patient taking drug for smoking cessation to immediately notify prescriber if agitation, hostility, depressed mood, changes in thinking or behavior, suicidal ideation, or suicidal behavior occurs.
• Advise patient to set a "target quit date" within first 2 weeks of treatment for smoking cessation.
• Instruct patient to swallow extendedor sustained-release tablets without crushing or chewing.
☞ Caution patient not to discontinue drug abruptly when taking drug for depression.
• Emphasize importance of frequent oral hygiene. (Dry mouth increases risk of caries and dental problems.)
• Caution patient to avoid alcohol, because it may increase risk of seizures.
• Advise patient to keep regular appointments for periodic blood tests and hepatic and renal studies.
• Advise breastfeeding patient that she should decide whether to discontinue breastfeeding or discontinue drug, taking into account the importance of drug for her treatment.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.
Forfivo XL(trade name),
Wellbutrin SR(trade name),
Wellbutrin XL(trade name),
Time/action profile (antidepressant effect)
Adverse Reactions/Side Effects
Central nervous system
- seizures (life-threatening)
- suicidal thoughts/behavior (life-threatening)
- agitation (most frequent)
- headache (most frequent)
- dry mouth (most frequent)
- nausea (most frequent)
- vomiting (most frequent)
- change in appetite
- weight gain
- weight loss
- syndrome of inappropriate ADH secretion
- tremor (most frequent)
Drug-Drug interactionConcurrent use with MAO-inhibitor like drugs, such as linezolid or methylene blue may ↑ risk of hypertensive reactions; concurrent use contraindicated; do not start therapy in patients receiving linezolid or methylene blue ; if linezolid or methylene blue need to be started in a patient receiving bupropion, immediately discontinue bupropion and monitor for 2 wk or until 24 hr after last dose of linezolid or methylene blue, whichever comes first (may resume bupropion therapy 24 hr after last dose of linezolid or methylene blue)↑ risk of adverse reactions when used with amantadine, or levodopa.↑ risk of seizures with phenothiazines, antidepressants, theophylline, corticosteroids, OTC stimulants/anorectics, or cessation of alcohol or benzodiazepines (avoid or minimize alcohol use).Ritonavir, lopinavir/ritonavir, and efavirenz may ↓ levels; may need to ↑ bupropion dose.May ↑ citalopram levels.Carbamazepine may ↓ blood levels and effectiveness.Concurrent use with nicotine replacement may cause hypertension.↑ risk of bleeding with warfarin.Bupropion and one of its metabolites inhibit the CYP2D6 enzyme system and may ↑ levels and risk of toxicity from antidepressants (SSRIs and tricyclic), haloperidol, risperidone, thioridazine, haloperidol, beta blockers, flecainide, and propafenone.May ↓ levels and efficacy of tamoxifen.May ↓ the efficacy of tamoxifen.
Seasonal Affective Disorder
Availability (generic available)
- Monitor mood changes. Inform health care professional if patient demonstrates significant increase in anxiety, nervousness, or insomnia.
- Assess mental status and mood changes, especially during initial few months of therapy and during dose changes. Risk may be increased in children, adolescents, and adults ≤24 yrs. Inform health care professional if patient demonstrates significant increase in signs of depression (depressed mood, loss of interest in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, suicide attempt or suicidal ideation). Restrict amount of drug available to patient.
- Lab Test Considerations: Monitor hepatic and renal function closely in patients with kidney or liver impairment to prevent ↑ serum and tissue bupropion concentrations.
- May cause false-positive urine test for amphetamines.
Potential Nursing DiagnosesIneffective coping (Indications)
- Do not confuse bupropion with buspirone. Do not confuse Wellbutrin SR with Wellbutrin XL. Do not confuse Zyban with Diovan. Do not administer bupropion (Wellbutrin) with Zyban, which contain the same ingredients.
- Administer doses in equally spaced time increments during the day to minimize the risk of seizures. Risk of seizures increases fourfold in doses greater than 450 mg per day.
- May be initially administered concurrently with sedatives to minimize agitation. This is not usually required after the 1st wk of therapy.
- Insomnia may be decreased by avoiding bedtime doses. May require treatment during 1st wk of therapy.
- Nicotine patches, gum, inhalers, and spray may be used concurrently with bupropion.
- When converting from other brands of bupropion to Aplenzin 522 mg/day Aplenzin is equivalent to 450 mg/day bupropion HCl, 348 mg/day Aplenzin is equivalent to 300 mg/day bupropion HCl and 174 mg/day Aplenzin is equivalent to 150 mg/day bupropion HCl.
- Oral: Swallow sustained-release or extended-release tablets whole; do not break, crush, or chew.
- May be administered with food to lessen GI irritation.
- Seasonal Affective Disorder: Begin administration in autumn prior to the onset of depressive symptoms. Continue therapy through winter and begin to taper and discontinue in early spring.
- Instruct patient to take bupropion as directed. Take missed doses as soon as possible and space day’s remaining doses evenly at not less than 4-hr intervals. Missed doses for smoking cessation should be omitted. Do not double doses or take more than prescribed. May require 4 wk or longer for full effects. Do not discontinue without consulting health care professional. May require gradual reduction before discontinuation.
- May impair judgment or motor and cognitive skills. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
- Advise patient, family, and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide, new or worse depression or anxiety, agitation or restlessness, panic attacks, insomnia, new or worse irritability, aggressiveness, acting on dangerous impulses, mania, or other changes in mood or behavior occur.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken, to avoid alcohol during therapy and to consult with health care professional before taking other medications with bupropion, such as Zyban.
- Inform patient that frequent mouth rinses, good oral hygiene, and sugarless gum or candy may minimize dry mouth. If dry mouth persists for more than 2 wk, consult health care professional regarding use of saliva substitute.
- Advise patient to notify health care professional if rash or other troublesome side effects occur.
- Inform patient that unused shell of XL tablets may appear in stool; this is normal.
- Advise patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
- Advise patient to notify health care professional of medication regimen before treatment or surgery.
- Instruct female patients to inform health care professional if pregnancy is planned or suspected or if breast feeding or planning to breast feed.
- Emphasize the importance of follow-up exams to monitor progress. Encourage patient participation in psychotherapy.
- Smoking Cessation: Smoking should be stopped during the 2nd week of therapy to allow for the onset of bupropion and to maximize the chances of quitting.
- Advise patient to stop taking bupropion and contact a health care professional immediately if agitation, depressed mood, and any changes in behavior that are not typical of nicotine withdrawal, or if suicidal thoughts or behavior occur.
- Increased sense of well-being.
- Renewed interest in surroundings. Acute episodes of depression may require several months of treatment.
- Cessation of smoking.