Bupropion

Aka: Bupropion, Wellbutrin, Zyban, Norepinephrine Dopamine Reuptake Inhibitor, NDRI

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II. Background

  1. Cost: $67 per month

III. Indications

  1. Tobacco Cessation (Zyban)
    1. May be used in combination with Nicotine Replacement
    2. Not considered first-line therapy for adolescents
  2. Reasonable second line Antidepressant
    1. Selective Serotonin Reuptake Inhibitor (SSRI) Failure
    2. Adjunctive therapy in combination with SSRI

IV. Precautions

  1. FDA Pregnancy Category C
  2. FDA Black Box Warning
    1. Increased risk of Suicidality in patients with Major Depression

V. Efficacy: Smoking Cessation (with concurrent counseling)

  1. Predictors of quitting with Bupropion
    1. Higher dose (Bupropion 300 mg/day)
    2. Male gender
    3. Prior Tobacco abstinence previously
    4. Abstinence for >2 weeks with current attempt
  2. Quit Rates (Study: n=893 over 10 weeks)
    1. Note these rates are higher than with other studies
    2. Placebo: 20% quit
    3. Transdermal Nicotine (21 mg): 32% quit
    4. Bupropion SR 150 mg bid: 46% quit
    5. Bupropion and Transdermal Nicotine: 51% quit
  3. Reference
    1. (1997) Med Lett Drugs Ther 39(1007):77-8 [PubMed]
    2. Dale (2001) Chest 119:1357-64 [PubMed]

VI. Mechanism

  1. Monocyclic aminoketone
  2. Norepinephrine Dopamine Reuptake Inhibitor (NDRI)
    1. Marked Norepinephrine reuptake inhibitor effect
    2. Some selective Dopamine reuptake inhibitor effect
  3. Smoking Cessation effect
    1. Enhances Dopamine levels in the mesolimbic system
      1. Reduces desire for nicotine dramatically
    2. Affects noradrenergic Neurons in the locus ceruleus
      1. Reduces nicotine withdrawal symptoms

VII. Dosing: Major Depression

  1. Elderly: 100 mg PO bid
  2. Usual dosing
    1. Initial: 100 mg PO bid for 4 days
    2. Next: 100 mg PO tid
    3. Maximum: 150 mg PO tid

VIII. Dosing: Smoking Cessation

  1. Protocol (May substitute 2 of Wellbutrin 75 mg)
    1. Start: Bupropion 150 mg PO qd for 3 days
    2. Then: Bupropion 150 mg PO bid for 7-12 weeks
  2. General
    1. Stop smoking during second week of medication
    2. Stop Bupropion if unable to quit by 7 weeks
    3. Cost: $186/10 week supply (wholesale)
    4. Minimum of 8 hours between doses
    5. More is not better
    6. Swallow pills whole (not crushed, divided or chewed)

IX. Pharmacokinetics

  1. Serum Half Life: 15 hours
  2. Therapeutic Blood Level: 50-100 ng/ml

X. Drug Interactions

  1. Prozac associated with panic and Psychosis
  2. Increased toxicity with:
    1. MAO inhibitor
    2. Ritonavir
  3. Carbamazepine (Tegretol) increases metabolism

XI. Contraindications

  1. Seizure disorder
  2. Concurrent psychiatric medications
    1. MAO inhibitor (allow 14 day interval between these two medication classes)
    2. Ritonavir
    3. Other forms of Bupropion (Wellbutrin, Zyban)
  3. Eating Disorder
    1. Anorexia Nervosa
    2. Bulimia
  4. Pregnancy
  5. Uncontrolled Hypertension

XII. Adverse Effects: Dopaminergic effects

  1. Very Activating, Agitation
    1. Good choice in withdrawn people
    2. Decreases in 1-2 weeks after starting medication
    3. Consider starting with Benzodiazepine and tapering
  2. Insomnia (35-40%)
  3. Dry Mouth (10%)
  4. Restlessness
  5. Tremor
  6. Gastrointestinal upset
  7. Headache
  8. Appetite suppression and weight loss
    1. Avoid in Eating Disorders
  9. Lowers Seizure threshold
    1. Avoid if concurrent Seizure disorder
    2. Seizure Incidence
      1. Regular release: 1%
        1. Increased with dose >150 mg/dose or 450 mg/day
      2. Sustained release: 0.1%
        1. Increased with dose >200 mg/dose or 400 mg/day
    3. Minimize risk by limiting dose to 150 mg q6 hours

XIII. Management: Overdose

  1. Findings
    1. Tachycardia (23%)
    2. Nausea and Vomiting (14%)
    3. Seizures (11%)
      1. Occur up to 14 hours after ingestion (esp. sustained release products)
      2. May occur with Overdose >600 mg (but typically occurs with Overdose >2500 mg)
      3. Prolonged and recurrent Seizures may occur with extended release preparations
      4. Treat Seizures with Benzodiazepines (other antiepileptics in Status Epilepticus are not indicated)
      5. If intubated, Propofol is preferred for sedation
    4. Intraventricular conduction abnormalities (Wide QRS, Prolonged QTc)
      1. May occur with large Overdoses
      2. Give 1-2 ampules bicarbonate IV frequently until QRS narrows (goal pH 7.45-7.55)
  2. Management
    1. Consider Intravenous Lipid Emulsion (Intralipid) in severe cases (e.g. cardiac toxicity)
    2. Supportive care
  3. References
    1. Nordt and Shoenberger in Herbert (2019) EM:Rap 19(3): 8-9
    2. Yen (2015) Crit Dec Emerg Med 29(10):18-23

XIV. Advantages

  1. No Anticholinergic Toxicity
  2. No Antihistaminergic activity
  3. No cardiac toxicity
  4. No sexual side effects

XV. Resources: Tobacco Cessation Counseling

  1. Zyban Advantage Plan
    1. Free 3 month program to users of product
  2. Tobacco Cessation counseling course

XVI. References

  1. Sundberg (1995) Depression Primary Care, PGM, p. 45-57
  2. Mallin (2002) Am Fam Physician 65(6):1107-17 [PubMed]

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Cost: Medications

bupropion (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
BUPROPION HCL 100 MG TABLET Generic $0.31 each
BUPROPION HCL 75 MG TABLET Generic $0.25 each
BUPROPION HCL SR 100 MG TABLET Generic $0.20 each
BUPROPION HCL SR 150 MG TABLET Generic $0.15 each
BUPROPION HCL SR 200 MG TABLET Generic $0.30 each
BUPROPION HCL XL 150 MG TABLET Generic $0.40 each
BUPROPION HCL XL 300 MG TABLET Generic $0.50 each
wellbutrin (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
WELLBUTRIN SR 100 MG TABLET Generic $0.20 each
WELLBUTRIN SR 150 MG TABLET Generic $0.15 each
WELLBUTRIN SR 200 MG TABLET Generic $0.30 each
WELLBUTRIN XL 150 MG TABLET Generic $0.40 each
WELLBUTRIN XL 300 MG TABLET Generic $0.50 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Ontology: Bupropion (C0085208)

Definition (CHV) a kind of depression treatment drug
Definition (CHV) a kind of depression treatment drug
Definition (NCI) An aminoketone with antidepressant activity. The molecular mechanism of the antidepressant effect of bupropion is unknown. This agent does not inhibit monoamine oxidase and, compared to classical tricyclic antidepressants, is a weak blocker of the neuronal uptake of serotonin and norepinephrine. Buproprion also weakly inhibits the neuronal re-uptake of dopamine.
Definition (NCI_NCI-GLOSS) A substance that is used to treat depression, and to help people quit smoking. It belongs to the family of drugs called antidepressants.
Definition (MSH) A unicyclic, aminoketone antidepressant. The mechanism of its therapeutic actions is not well understood, but it does appear to block dopamine uptake. The hydrochloride is available as an aid to smoking cessation treatment.
Definition (CSP) unicyclic, aminoketone antidepressant; appears to block dopamine uptake; the hydrochloride is used as an aid to smoking cessation treatment.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D016642
SnomedCT 323344001, 387564004, 96199001
LNC LP17172-5, MTHU022987
English 1-Propanone, 1-(3-chlorophenyl)-2-((1,1-dimethylethyl)amino)-, Amfebutamone, Bupropion, 1-Propanone, 1-(3-Chlorophenyl)-2-((1,1-dimethylethyl)amino)-, amfebutamone, bupropion (medication), Bupropion [Chemical/Ingredient], BUPROPION, Amfebutamon, buPROPion, bupropion, (+-)-1-(3-Chlorophenyl)-2-((1,1-dimethylethyl)amino)-1-propanone, Bupropion (product), Bupropion (substance), BUP, Bupropion [dup] (substance)
Swedish Bupropion
Spanish bupropiona, bupropiona (producto), bupropiona (sustancia), bupropión (producto), bupropión (sustancia), bupropión, Bupropion
Czech bupropion
Finnish Bupropioni
Italian Amfebutamone, Bupropione
Russian AMFEBUTAMON, BUPROPION, АМФЕБУТАМОН, БУПРОПИОН
Japanese アンフェブタモン, ブプロピオン
Polish Bupropion
French Bupropione, Amfébutamone
German Bupoprion
Portuguese Bupropiona
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Wellbutrin (C0085934)

Definition (CHV) a depression treatment drug
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D016642
English bupropion (Wellbutrin), wellbutrin, Glaxo Wellcome Brand 2 of Bupropion Hydrochloride, GlaxoSmithKline Brand 2 of Bupropion Hydrochloride, Wellbutrin
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Zyban (C0751626)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D016642
English zyban, Glaxo Wellcome Brand 1 of Bupropion Hydrochloride, GlaxoSmithKline Brand 1 of Bupropion Hydrochloride, Zyban, Zyban (Anti-Smoking)
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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