Pharm
Bupropion
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Bupropion
, Wellbutrin, Zyban, Norepinephrine Dopamine Reuptake Inhibitor, NDRI
Background
Cost: $67 per month
Indications
Tobacco Cessation
(Zyban)
May be used in combination with
Nicotine Replacement
Not considered first-line therapy for adolescents
Reasonable second line
Antidepressant
Selective Serotonin Reuptake Inhibitor
(
SSRI
) Failure
Adjunctive therapy in combination with
SSRI
Precautions
FDA Pregnancy Category C
FDA Black Box Warning
Increased risk of
Suicidality
in patients with
Major Depression
Efficacy
Smoking Cessation
(with concurrent counseling)
Predictors of quitting with Bupropion
Higher dose (Bupropion 300 mg/day)
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
(1997) Med Lett Drugs Ther 39(1007):77-8 [PubMed]
Dale (2001) Chest 119:1357-64 [PubMed]
Mechanism
Monocyclic aminoketone
Norepinephrine Dopamine Reuptake Inhibitor (NDRI)
Marked
Norepinephrine
reuptake inhibitor effect
Some selective
Dopamine
reuptake inhibitor effect
Smoking Cessation
effect
Enhances
Dopamine
levels in the mesolimbic system
Reduces desire for nicotine dramatically
Affects noradrenergic
Neuron
s in the locus ceruleus
Reduces nicotine withdrawal symptoms
Dosing
Major Depression
Elderly: 100 mg PO bid
Usual dosing
Initial: 100 mg PO bid for 4 days
Next: 100 mg PO tid
Maximum: 150 mg PO tid
Dosing
Smoking Cessation
Protocol (May substitute 2 of Wellbutrin 75 mg)
Start: Bupropion 150 mg PO qd for 3 days
Then: Bupropion 150 mg PO bid for 7-12 weeks
Gene
ral
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)
Pharmacokinetics
Serum Half Life: 15 hours
Therapeutic Blood Level: 50-100 ng/ml
Drug Interactions
Prozac
associated with panic and
Psychosis
Increased toxicity with:
MAO inhibitor
Ritonavir
Carbamazepine
(
Tegretol
) increases metabolism
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
Anorexia Nervosa
Bulimia
Pregnancy
Uncontrolled Hypertension
Adverse Effects
Dopamine
rgic 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 Disorder
s
Lowers
Seizure
threshold
Avoid if concurrent
Seizure
disorder
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
Minimize risk by limiting dose to 150 mg q6 hours
Management
Overdose
Findings
Tachycardia
(23%)
Nausea
and
Vomiting
(14%)
Seizure
s (11%)
Occur up to 14 hours after ingestion (esp. sustained release products)
May occur with
Overdose
>600 mg (but typically occurs with
Overdose
>2500 mg)
Prolonged and recurrent
Seizure
s may occur with extended release preparations
Treat
Seizure
s with
Benzodiazepine
s (other antiepileptics in
Status Epilepticus
are not indicated)
If intubated,
Propofol
is preferred for sedation
Intraventricular conduction abnormalities (
Wide QRS
,
Prolonged QT
c)
May occur with large
Overdose
s
Give 1-2 ampules bicarbonate IV frequently until QRS narrows (goal pH 7.45-7.55)
Management
Consider
Intravenous Lipid Emulsion
(
Intralipid
) in severe cases (e.g. cardiac toxicity)
Supportive care
References
Nordt and Shoenberger in Herbert (2019) EM:Rap 19(3): 8-9
Yen (2015) Crit Dec Emerg Med 29(10):18-23
Advantages
No
Anticholinergic Toxicity
No
Antihistamine
rgic activity
No cardiac toxicity
No sexual side effects
Resources
Tobacco Cessation
Counseling
Zyban Advantage Plan
Free 3 month program to users of product
Tobacco Cessation
counseling course
References
Sundberg (1995) Depression Primary Care, PGM, p. 45-57
Mallin (2002) Am Fam Physician 65(6):1107-17 [PubMed]
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