bupropion WELLBUTRIN

Class: NDRI
FDA Indications: MDD, SAD (XL Only), Smoking Deterrent
Off-Label Use: PMDD, Pathological Gambling, Neuropathic Pain, ADHD, Weight Loss, Migraines, Chronic Fatigue Syndrome, Methamphetamine Dependence, Hypoactive Sexual Desire Disorder, SSRI-induced Sexual Dysfunction
Prescribing
Forms: 75, 100mg IR tablet; 100, 150, 200mg SR tablet; 150, 300mg XL tablet
Dose 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

NAMI drug fact sheet

Precautions
Contraindications: Concomitant use of MAOIs, seizure disorder, anorexia or bulimia
Serious Side Effects: Seizure risk: 0.1% at ≤300mg/day; ~0.4% at 450mg/day; almost 4% at 600mg/day
Side Effects: headache, dizziness, confusion, visual changes, constipation, xerostomia, tremor, nausea, insomnia, weight loss, agitation, rash, tachycardia, hostility
Pharmacodynamics
1° MOA: Norepinephrine dopamine reuptake inhibitor
2° 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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Last updated August 27 2018 18:45:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.