Ctrl

K

Bupropion hydrochloride SR

Class
Antidepressants
Subclass
Norepinephrine-dopamine reuptake inhibitors
Substance name
buPROPion SR
Brand names
Wellbutrin SR®, Zyban®
Common formulations
Film-coated tablet, Tablet
See also
Bupropion hydrochloride
Bupropion hydrochloride XL (Forfivo XL®, Wellbutrin XL®)
Bupropion hydrobromide ER (Aplenzin®)
Dosage and administration
Adults patients
Symptomatic relief
Neuropathic pain • Off-label
•
150-300 mg PO daily
Treatment
Major depressive disorder
•
Start at: 150 mg PO qAM for 3 days
•
Maintenance: 150 mg PO BID
•
Maximum: 400 mg per day
ADHD • Off-label
•
Start at: 100 mg PO daily for 1 week
•
Maintenance: 100-150 mg PO BID
Alternative
•
Start at: 150 mg PO daily for 3 days
•
Maintenance: 150 mg PO BID
•
Maximum: 400 mg per day
Amphetamine use disorder • Off-label
•
150 mg PO BID for 12 weeks
Cocaine use disorder • Off-label
•
150 mg PO BID for 12-25 weeks
Drug-induced sexual dysfunction in females • SSRIs • Off-label
•
150 mg PO BID
Facilitation
Facilitation of smoking cessation • Off-label
•
Start at: 150 mg PO daily for 3 days
•
Maintenance: 150 mg PO BID for 7-12 weeks
•
Maximum: 300 mg per day
Consider continuing 150 mg daily in patients not tolerating titration to the full dose.
Other off-label uses
•
Treatment of binge eating disorder
•
Treatment of bipolar disorder (depressive episodes)
Indications for use
Labeled indications
Adults
•
Treatment of major depressive disorder
Off-label indications
Adults
•
Symptomatic relief of neuropathic pain
•
Treatment of amphetamine use disorder
•
Treatment of ADHD
•
Treatment of binge eating disorder
•
Treatment of bipolar disorder (depressive episodes)
•
Treatment of cocaine use disorder
•
Treatment of drug-induced sexual dysfunction in females (SSRIs)
•
Facilitation of smoking cessation
Safety risks
Boxed warnings
Suicidal ideation
•
Use extreme caution in patients with major depressive disorder or other psychiatric disorders, particularly in children, adolescents, and young adults. Monitor closely for suicidality and unusual changes in behavior.
Contraindications
Hypersensitivity to bupropion or its components
Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs
Concomitant use of MAOIs
•
Do not use bupropion with or within 14 days of stopping MAOIs, including reversible MAOIs, such as linezolid and methylene blue.
Warnings and precautions
Acute angle-closure glaucoma
•
Use caution in patients with untreated anatomically narrow angles.
Delusions, hallucinations, psychosis, paranoid ideation
•
Maintain a high level of suspicion, as bupropion has been associated with an increased risk for these adverse events.
Hypertension
•
Maintain a high level of suspicion, as bupropion has been associated with an increased risk of hypertension, especially when used with drugs increasing dopaminergic or noradrenergic activity. Assess BP before initiating treatment and monitor periodically during treatment.
•
Recognize that the combination of bupropion with nicotine replacement therapy has not been associated with an increase in BP and is safe to use.
Manic or mixed episodes
•
Use caution in patients with bipolar disorder or risk factors for bipolar disorder, such as family history of bipolar disorder, depression, or suicidal thoughts.
Seizure
•
Use extreme caution in patients with metabolic disorders or using illicit drugs, medications lowering the seizure threshold, or misusing or abusing prescription medications. Discontinue if seizures occur.
Specific populations
Renal impairment
CrCl > 60 mL/min
•
Use acceptable. No dose adjustment required.
CrCl 15-60 mL/min
•
Use with caution. Consider a maximum daily dose of 150 mg/day.
CrCl < 15 mL/min
•
Use with caution. Start at dose of 100 mg q48h or 150 mg q72h. Maximal dose of 150 mg/d. Use of alternative agent may be preferred. Use with caution; to limit accumulation of active metabolites. Titrate gradually based on tolerability and response to a maximum daily dose of 150 mg/day.
Renal replacement therapy
Intermittent hemodialysis
•
Use with caution. Reduce dose. Maximal dose of 150 mg. Maximal frequency of daily. Titrate slowly.
Peritoneal dialysis
•
Use with caution. Reduce dose. Maximal dose of 150 mg. Maximal frequency of daily. Titrate slowly.
Hepatic impairment
Child-Pugh A (mild)
•
Reduce dose. Monitor serum aminotransferases. Administer 50% of the usual indication-specific dose and/or extend the usual frequency .
Child-Pugh B (moderate)
•
Reduce dose. Maximal dose of 100 mg per day or 150 mg every other day. Monitor serum aminotransferases. Administer 50% of the usual indication-specific dose and/or extend the usual frequency.
Child-Pugh C (severe)
•
Reduce dose. Maximal dose of 100 mg per day or 150 mg every other day. Monitor serum aminotransferases.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: B2
•
Use only if benefits outweigh potential risks. Consider safer alternatives. Evidence of fetal harm in animals. Enroll patients in a dedicated pregnancy outcome monitoring registry.
Breastfeeding
Consider alternative agents that may be safer.
•
Use with caution during breastfeeding.
Very low levels in breastfed infants (< 5%).
May potentially cause adverse effects in breastfed infants.
Some adverse effects on lactation reported.
Adverse reactions
Very common > 10%
•
Agitation, hyperhidrosis, lethargy, migraine, pharyngitis, anorexia, blurred vision, constipation, dry mouth, headache, insomnia, nausea, vomiting, weight gain, weight loss, rhinitis, tachycardia, tremor
Common 1-10%
•
Acne vulgaris, ataxia, drug-induced parkinsonism, dysarthria, dystonia, ecchymosis, gingivitis, glossitis, gynecomastia, hyperkinesia, hypertension, hypertonia, hypotension, ↑ liver enzymes, influenza, jaundice, myoclonus, oral ulcers, orthostatic hypotension, peripheral edema, photosensitivity of skin, psychosis, abdominal pain, acid reflux, akathisia, anejaculation, anxiety, arthralgia, asthenia, back pain, bruxism, chest pain, chills, confusion, cough, dental pain, diarrhea, diplopia, dizziness, dysgeusia, dysmenorrhea, dyspareunia, dyspepsia, dysphagia, dyspnea, emotional lability, euphoria, fatigue, fever, flatulence, hair loss, hallucinations, hostility, hot flashes, hypersalivation, impotence, ↑ appetite, ↑ libido, irritability, itching, mania, memory impairment, menstrual irregularity, muscle cramps, myalgia, nasal congestion, nightmares, nocturia, nosebleed, palpitations, paranoid ideation, paresthesia, polydipsia, polyuria, restlessness, skin flushing, skin rash, somnolence, suicidal ideation, syncope, tinnitus, urinary retention, urinary urgency, vaginal bleeding, vaginal irritation, vertigo, sinusitis, skin dryness, stomatitis, testicular swelling, urticaria, xerophthalmia
Uncommon < 1%
•
Acute cystitis, aphasia, bronchospasm, coma, gastrointestinal perforation, hirsutism, maculopapular rash, myocardial infarction, neuropathic pain, pallor, phlebitis, body odor, hair discoloration, malaise, memory impairment, seizure, stroke
Unknown frequency
•
AV block, acute generalized exanthematous pustulosis, acute pancreatitis, anaphylactoid reactions, anaphylaxis, angioedema, DRESS syndrome, ↓ blood glucose, ↓ platelet count, ↓ serum sodium, erythema multiforme, esophagitis, exfoliative dermatitis, gastrointestinal bleeding, hearing loss, ↑ WBC count, ↑ blood glucose, ↑ intraocular pressure, ↑ urine glucose, lymphadenopathy, myasthenia gravis, mydriasis, pulmonary embolism, pancytopenia, akinesia, depression, urinary incontinence, rhabdomyolysis, syndrome of inappropriate antidiuretic hormone secretion, serum sickness, Stevens-Johnson syndrome, tardive dyskinesia
Interactions
Drug(s)
Check Interactions
Reset

What did you think about this content?

Create free account

Sign up for free to access the full drug resource