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. Dosing: Combination - Auvelity (Bupropion/Dextromethorphan)
- Auvelity taken orally twice daily
- Bupropion 105 mg/tablet
- Dextromethorphan 45 mg/tablet
- Mechanism
- Bupropion, in addition to Antidepressant effects, also increases Dextromethorphan levels via CYP2D6 inhibition
- Dextromethorphan is proposed to have Antidepressant effect
- Precautions
- See Dextromethorphan Toxicity (including Serotonin Syndrome)
- New combination released in 2022, with limited efficacy data, and a monthly cost > $1000
- References
- (2022) Presc Lett 29(12): 69-70
IX. Pharmacokinetics
- Rapid gastrointestinal absorption
- Peak Concentration at 3-5 hours
- Serum Half Life: >15-20 hours
- Therapeutic Blood Level: 50-100 ng/ml
X. Drug Interactions
- Prozac associated with panic and Psychosis
- Increased toxicity with:
- Carbamazepine (Tegretol) increases metabolism
XI. 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
XII. 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
XIII. Management: Overdose
XIV. Advantages
- No Anticholinergic Toxicity
- No Antihistaminergic activity
- No cardiac toxicity
- No sexual side effects
XV. Resources: Tobacco Cessation Counseling
- Zyban Advantage Plan
- Free 3 month program to users of product
- Tobacco Cessation counseling course
XVI. 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 |