bupropion

ROUTE	ONSET	PEAK	DURATION
PO	1–3 wk	unknown	unknown

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 (↑ risk of seizures).

Use Cautiously in:

Renal/hepatic impairment (↓ dose recommended) (Forfivo XL not recommended in patients with renal or hepatic impairment);
Recent history of MI;
History of suicide attempt;
Unstable cardiovascular status;
May ↑ risk 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 during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: May ↑ risk of suicide attempt/ideation especially during early treatment or dose adjustment in children/adolescents; safety and effectiveness not established in children;
Geri: ↑risk of drug accumulation and ↑ sensitivity to effects in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension

Derm: photosensitivity

Endo: hyperglycemia, hypoglycemia, syndrome of inappropriate antidiuretic hormone secretion

GI: dry mouth, nausea, vomiting, change in appetite, weight gain, weight loss

Neuro: agitation, headache, tremor, aggression, anxiety, delusions, depression, hallucinations, HOMICIDAL THOUGHTS/BEHAVIOR, hostility, insomnia, mania, panic, paranoia, psychoses, SEIZURES, SUICIDAL THOUGHTS/BEHAVIOR

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with MAO-inhibitors may ↑ risk 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 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 isoenzyme and may ↑ levels and risk of toxicity of antidepressants (SSRIs and tricyclic), haloperidol, risperidone, thioridazine, beta blockers, flecainide, and propafenone.
May ↓ levels and efficacy of tamoxifen.
May ↓ the efficacy of tamoxifen.
May ↓ digoxin levels.

Route/Dosage ⬆ ⬇

Depression

PO (Adults ): Immediate-release: 100 mg twice daily initially; after 3 days may ↑ to 100 mg 3 times daily; after at least 4 wk of therapy, may ↑ up 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). 12–hr sustained-release: 150 mg once daily in the morning; after 3 days, may ↑ to 150 mg twice daily with at least 8 hr between doses; after at least 4 wk of therapy, may ↑ to a maximum daily dose of 400 mg given as 200 mg twice daily. 24–hr extended-release (Wellbutrin XL): 150 mg once daily in the morning, may be ↑ after 4 days to 300 mg once daily; some patients may require up to 450 mg/day as a single daily dose. 24–hr extended-release (Aplenzin): 174 mg once daily in the morning, may be ↑ after 4 days to 348 mg once daily; some patients may require up to 522 mg/day as a single daily dose. 24–hr 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 ): 24–hr extended-release (Wellbutrin XL): 150 mg/day in the morning; if dose is well tolerated, ↑ to 300 mg/day in one wk. Doses should be tapered to 150 mg/day for 2 wk before discontinuing; 24–hr extended-release (Aplenzin): 174 mg once daily in the morning, may be ↑ after 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 ): 12–hr sustained release: 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)

Immediate-release tablets: 75 mg; 100 mg
12–hour sustained-release tablets: 100 mg; 150 mg; 200 mg
24–hour extended-release tablets (Wellbutrin XL): 150 mg; 300 mg
24–hour extended-release tablets (Aplenzin): 174 mg; 348 mg; 522 mg
24–hour extended-release tablets (Forfivo XL): 450 mg
In combination with: dexamethasone (Auvelity); naltrexone (Contrave). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess mental status and mood changes in all patients, especially during initial few mo 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/homicidal ideation). If so, 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.

Implementation ⬆ ⬇

Do not confuse bupropion with buspirone. Do not confuse Wellbutrin SR with Wellbutrin XL.
- Administer doses in equally spaced time increments during the day to minimize the risk of seizures. Risk of seizures increases fourfold in doses >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 hydrochloride, 348 mg/day Aplenzin is equivalent to 300 mg/day bupropion hydrochloride, and 174 mg/day Aplenzin is equivalent to 150 mg/day bupropion hydrochloride.
PO: DNC: 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.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take bupropion as directed at the same time each day. Missed doses 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. Advise patient to read Medication Guide before starting and with each Rx refill in case of changes.
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.
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.
Rep: Instruct females of reproductive potential to inform health care professional if pregnancy is planned or suspected or if breastfeeding. Inform patient about pregnancy exposure registry to monitor pregnancy outcomes in women exposed to antidepressants during pregnancy. Register patients by calling the National Pregnancy Registry for Antidepressants at 1-844-405-6185 or visiting online at https://womensmentalhealth.org/clinical-and-researchprograms/pregnancyregistry/antidepressants/.
Emphasize the importance of follow-up exams to monitor progress.
Smoking Cessation: Smoking should be stopped during the 2nd wk 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.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇