bupropion (Rx)

>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

Nervous system: Abnormal electroencephalogram (EEG), aggression, akinesia, aphasia, completed suicide, delirium, delusions, dysarthria, extrapyramidal syndrome (dyskinesia, dystonia, hypokinesia, parkinsonism), hallucinations, increased libido, manic reaction, neuralgia, neuropathy, paranoid ideation, restlessness, suicide attempt, and unmasking tardive dyskinesia

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

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 risk is dose-related; can minimize risk by limiting daily dose to 522 mg and gradually increasing dose; discontinue permanently in patients who experience seizures

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

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

Some patients who stopped smoking reported to have experienced symptoms of nicotine withdrawal, including depressed mood; depression, rarely including suicidal ideation, reported in smokers undergoing a smoking cessation attempt without medication; however, some of these adverse events occurred in patients taking bupropion who continued to smoke

Neuropsychiatric adverse events reported in patients without and with pre-existing psychiatric disease; some patients experienced worsening of their psychiatric illnesses; observe patients for occurrence of neuropsychiatric adverse events; patient should stop therapy and contact healthcare provider immediately if agitation, depressed mood, or changes in behavior or thinking that are not typical for patient are observed, or if patient develops suicidal ideation or suicidal behavior; symptoms may persist after discontinuation of therapy; in some cases; monitoring and supportive care should be provided until symptoms resolve

Bupropion hydrobromide extended-release tablets are intended for oral use only; inhalation of crushed tablets or injection of dissolved bupropion reported; seizures and/or cases of death reported when administered intranasally or by parenteral injection

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%)

Oral Administration

Swallow extended/sustained-release tablets whole; do not chew, crush, or split; this may lead to adverse effects including seizures