Indications
Treatment of depression (with psychotherapy). Depression
with seasonal affective disorder (Aplenzin and
Wellbutrin XL only). Smoking cessation (Zyban only).
Unlabeled Use: Treatment of ADHD in adults (SR
only). To increase sexual desire in women.
Action
Decreases neuronal reuptake of dopamine in the CNS.
Diminished neuronal uptake of serotonin and norepinephrine
(less than tricyclic antidepressants). Therapeutic
Effects: Diminished depression. Decreased
craving for cigarettes.
Pharmacokinetics
Absorption: Although well absorbed, rapidly and extensively
metabolized by the liver.
Distribution: Unknown.
Metabolism and Excretion: Extensively metabolized
by the liver into 3 active metabolites (CYP2B6 involved
in formation of one of the active metabolites).
Half-life: 14 hr (active metabolites may have longer
half-lives).
TIME/ACTION PROFILE (antidepressant effect)
ROUTE ONSET PEAK DURATION
PO 1–3 wk unknown unknown
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Concurrent
use of MAO inhibitors or MAO-like drugs (linezolid or
methylene blue); Concurrent use of ritonavir; Seizure
disorders; Arteriovenous malformation, severe head injury,
CNS tumor, CNS infection, severe stroke, anorexia
nervosa, bulimia, or abrupt discontinuation of alcohol,
benzodiazepines, barbiturates, or antiepileptic drugs
(qrisk of seizures); Lactation: Potential for serious adverse
reactions in nursing infants.
Use Cautiously in: Renal/hepatic impairment (p
dose recommended) (Forfivo XL not recommended in
patients with renal or hepatic impairment); Recent history
of MI; History of suicide attempt; Unstable cardiovascular
status; Mayqrisk of suicide attempt/ideation
especially during early treatment or dose adjustment;
this risk appears to be greater in adolescents or children;
Psychiatric illness; Angle-closure glaucoma; OB:
Use only if benefit to patient outweighs potential risk to
fetus; Geri:qrisk of drug accumulation;qsensitivity to
effects.
Exercise Extreme Caution in: Severe hepatic
cirrhosis (pdose required); Pedi:qrisk of suicidal
thinking and behavior. Observe carefully, especially at
initiation of therapy and duringqorpin dose.
Adverse Reactions/Side Effects
CNS: HOMICIDAL THOUGHTS/BEHAVIOR, SEIZURES, SUICIDAL
THOUGHTS/BEHAVIOR, agitation, headache, aggression,
anxiety, delusions, depression, hallucinations,
hostility, insomnia, mania, panic, paranoia, psychoses.
CV: hypertension. GI: dry mouth, nausea, vomiting,
change in appetite, weight gain, weight loss. Derm:
photosensitivity. Endo: hyperglycemia, hypoglycemia,
syndrome of inappropriate ADH secretion. Neuro:
tremor.
Interactions
Drug-Drug: Concurrent use with MAO-inhibitors
mayqrisk of hypertensive reactions; concurrent use
contraindicated; at least 14 days should elapse between
discontinuation of MAO inhibitor and initiation of bupropion
(or visa versa). Concurrent use with MAO-inhibitor
like drugs, such as linezolid or methylene
blue mayqrisk 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).qrisk of adverse reactions
when used with amantadine or levodopa.qrisk 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 mayplevels; may
need toqbupropion dose. Mayqcitalopram levels.
Carbamazepine maypblood levels and effectiveness.
Concurrent use with nicotine replacement may cause
hypertension.qrisk of bleeding with warfarin. Bupropion
and one of its metabolites inhibit the CYP2D6 enzyme
system and mayqlevels and risk of toxicity from
antidepressants (SSRIs and tricyclic), haloperidol,
risperidone, thioridazine, haloperidol, beta
blockers, flecainide, and propafenone. Mayplevels
and efficacy of tamoxifen. Maypthe efficacy of tamoxifen.
Maypdigoxin levels.
Route/Dosage
Depression
PO (Adults): Immediate-release—100 mg twice
daily initially; after 3 days mayqto 100 mg 3 times
daily; after at least 4 wk of therapy, mayqup to 450
mg/day in divided doses (not to exceed 150 mg/dose;
wait at least 6 hr between doses at the 300 mg/day dose
or at least 4 hr between doses at the 450-mg/day dose).
Sustained-release—150 mg once daily in the morning;
after 3 days, mayqto 150 mg twice daily with at
least 8 hr between doses; after at least 4 wk of therapy,
mayqto a maximum daily dose of 400 mg given as 200
mg twice daily. Extended-release (Wellbutrin XL)—
150 mg once daily in the morning, may beqafter 4
days to 300 mg once daily; some patients may require
up to 450 mg/day as a single daily dose. Extended-release
(Aplenzin)—174 mg once daily in the morning,
may beqafter 4 days to 348 mg once daily; some patients
may require up to 522 mg/day as a single daily
dose. Extended-release (Forfivo XL)—450 mg once
daily (should NOT be used as initial therapy; it should
only be used in patients who have been receiving 300 mg/day of another bupropion formulation for at least 2
wk and require titration up to 450 mg/day or in those
patients receiving 450 mg/day of another bupropion
formulation).
Hepatic Impairment
PO (Adults): Moderate-to-severe hepatic impairment
(Aplenzin)—Max dose: 174 mg every other
day.
Seasonal Affective Disorder
PO (Adults): Extended-release (Wellbutrin XL)—
150 mg/day in the morning; if dose is well tolerated,q
to 300 mg/day in one wk. Doses should be tapered to
150 mg/day for 2 wk before discontinuing; Extendedrelease
(Aplenzin)—174 mg once daily in the morning,
may beqafter 7 days to 348 mg once daily.
Hepatic Impairment
PO (Adults): Moderate-to-severe hepatic impairment
(Aplenzin)—Max dose: 174 mg every other
day.
Smoking cessation
PO (Adults): Zyban—150 mg once daily for 3 days,
then 150 mg twice daily for 7–12 wk (doses should be
at least 8 hr apart).
Availability (generic available)
Tablets: 75 mg, 100 mg. Cost: Generic—75 mg
$79.43/100, 100 mg $106.01/100. Sustained-release
tablets: 100 mg, 150 mg, 200 mg. Cost: Generic—
100 mg $51.12/180, 150 mg $59.60/180, 200
mg $52.33/180. Extended-release tablets (Wellbutrin
XL): 150 mg, 300 mg. Cost: Generic—150 mg
$74.84/90, 300 mg $63.94/90. Extended-release
tablets (Aplenzin): 174 mg, 348 mg, 522 mg. Cost:
174 mg $359.09/30, 348 mg $473.36/30, 522 mg
$1,077.23/30. Extended-release tablets (Forfivo
XL): 450 mg. Cost: $176.40/30.
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