bupropion WELLBUTRIN
Class: NDRIFDA Indications: MDD, SAD (XL Only), Smoking Deterrent
Off-Label Use: Neuropathic Pain, Weight Loss, ADHD, Migraines, PMDD, Chronic Fatigue Syndrome, Pathological Gambling, Methamphetamine Dependence, Hypoactive Sexual Desire Disorder, SSRI-induced Sexual Dysfunction
Prescribing
Forms: 75, 100mg IR tablet; 100, 150, 200mg SR tablet; 150, 300mg XL tabletDose Range: 150-450 mg/day
Starting: 150 mg QAM; may increase to usual dose of 300 mg QAM if adequately tolerated after at least 4 days; maximum dose 450 mg QAM
Precautions
Contraindications: Concomitant use of MAOIs, seizure disorder, anorexia or bulimiaSerious Side Effects: Seizure risk: 0.1% at ≤300mg/day; ~0.4% at 450mg/day; almost 4% at 600mg/day
Side Effects: agitation, xerostomia, constipation, headache, nausea, dizziness, tremor, visual changes, insomnia, confusion, tachycardia, rash, hostility, weight loss
Pharmacodynamics
1° MOA: Norepinephrine dopamine reuptake inhibitor2° MOA: Noncompetitive nicotinic acetylcholine receptor antagonist
Target: NET, DAT, nAChR
Pharmacokinetics
t½: 21 (12-30)° TMAX: 2h(IR), 3(SR), 5(XL)°Substrate of: 2B6
Inhibits: 2D6; Induces: ∅
Active Metabolites: Hydroxybupropion (50% as potent as bupropion); threohydrobupropion & erythrohydrobupropion (20% as potent)
DDIs
- - DO NOT CO-PRESCRIBE WITH MAOIs
- - use extreme caution when coadministering with other drugs that lower seizure threshold
- - 2B6 inhibitors can ↑ serum levels
Misc
- - effective for depression with pronounced anergia & anhedonia
- - may improve cognitive slowing/pseudodementia
- - ∅ weight gain; ↓ rates of sexual side effects
- - least chance of triggering mania
- - anxious/agitated patients need lower starting doses & slower titrations & may need a concomitant anxiolytic agent
- - to ↓ seizures risk, don't exceed a dosage increase of 100 mg/day in a 3-day period, 150 mg as a single dose, or total daily dose of 450 mg
Special Populations
Category C—Some animal studies show adverse effects; no controlled studies in humans
RID 0.2-2%; ∅ AE's have been reported
May be at risk of accumulation of bupropion and its metabolites
Recommend only 150mg/day in patients with GFR <50 mL/min; in hemodialysis patients 150 mg every 3 days
Mean t½ for active metabolites ↑ 2-vto 5-fold in patients with severe hepatic impairment
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