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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.