II. Indications
-
Tobacco Cessation (Zyban)
- May be used in combination with Nicotine Replacement
- Not considered first-line therapy for adolescents
- Reasonable second line Antidepressant in Major Depression
- Selective Serotonin Reuptake Inhibitor (SSRI) Failure
- Adjunctive therapy in combination with SSRI
- Other uses (off label)
- Attention Deficit Disorder
- Obesity Management
- Sexual Dysfunction
- Abuse potential (recreational drug use)
III. Precautions
- FDA Pregnancy Category C
- FDA Black Box Warning
- Increased risk of Suicidality in patients with Major Depression
IV. Efficacy: Smoking Cessation (with concurrent counseling)
- Predictors of quitting with Bupropion
- Higher dose (Bupropion 300 mg/day divided twice daily)
- Male gender
- Prior Tobacco abstinence previously
- Abstinence for >2 weeks with current attempt
- Quit Rates (Study: n=893 over 10 weeks)
- Note these rates are higher than with other studies
- Placebo: 20% quit
- Transdermal Nicotine (21 mg): 32% quit
- Bupropion SR 150 mg bid: 46% quit
- Bupropion and Transdermal Nicotine: 51% quit
- Reference
V. Mechanism
- Monocyclic aminoketone
- Structurally similar to Amphetamine
- Norepinephrine Dopamine Reuptake Inhibitor (NDRI)
- Marked Norepinephrine reuptake inhibitor effect
- Also has Dopamine reuptake inhibitor activity
- Some selective Dopamine reuptake inhibitor effect
- Smoking Cessation effect
VI. Dosing: Major Depression
- Elderly: 100 mg orally twice daily
- Usual dosing
- Initial: 100 mg orally twice daily for 4 days
- Next: 100 mg orally three times daily
- Maximum: 150 mg orally three times daily
VII. Dosing: Smoking Cessation
- Protocol (May substitute 2 of Wellbutrin 75 mg)
- Start: Bupropion 150 mg XR orally daily for 3 days
- Then: Bupropion 150 mg XR orally twice daily for 7-12 weeks
-
General
- Stop smoking during second week of medication
- Stop Bupropion if unable to quit by 7 weeks
- Cost: $186/10 week supply (wholesale)
- Minimum of 8 hours between doses
- More is not better
- Swallow pills whole (not crushed, divided or chewed)
VIII. Pharmacokinetics
- Rapid gastrointestinal absorption
- Peak Concentration at 3-5 hours
- Serum Half Life: >15-20 hours
- Therapeutic Blood Level: 50-100 ng/ml
IX. Drug Interactions
- Prozac associated with panic and Psychosis
- Increased toxicity with:
- Carbamazepine (Tegretol) increases metabolism
X. Contraindications
- Seizure Disorder
- Concurrent psychiatric medications
- MAO inhibitor (allow 14 day interval between these two Medication Classes)
- Ritonavir
- Other forms of Bupropion (Wellbutrin, Zyban)
- Eating Disorder
- Pregnancy
- Uncontrolled Hypertension
XI. Adverse Effects: Dopaminergic effects
- Very Activating, Agitation
- Good choice in withdrawn people
- Decreases in 1-2 weeks after starting medication
- Consider starting with Benzodiazepine and tapering
- Insomnia (35-40%)
- Dry Mouth (10%)
- Restlessness
- Tremor
- Gastrointestinal upset
- Headache
- Appetite suppression and weight loss
- Avoid in Eating Disorders
- Lowers Seizure threshold
- Avoid if concurrent Seizure Disorder
- Avoid in abrupt cessation of Alcohol, Barbiturates, Benzodiazepines or antiepileptics (risk of withdrawal Seizure)
- Seizure Incidence
- Regular release: 1%
- Increased with dose >150 mg/dose or 450 mg/day
- Sustained release: 0.1%
- Increased with dose >200 mg/dose or 400 mg/day
- Regular release: 1%
- Minimize risk by limiting dose to 150 mg q6 hours
XII. Management: Overdose
XIII. Advantages
- No Anticholinergic Toxicity
- No Antihistaminergic activity
- No cardiac toxicity
- No sexual side effects
XIV. Resources: Tobacco Cessation Counseling
- Zyban Advantage Plan
- Free 3 month program to users of product
- Tobacco Cessation counseling course
XV. References
- Sundberg (1995) Depression Primary Care, PGM, p. 45-57
- Mallin (2002) Am Fam Physician 65(6):1107-17 [PubMed]
Images: Related links to external sites (from Bing)
Related Studies
| 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 |
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 |
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 |
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) |
