pharmacology

Last reviewed 11/2020

• bupropion was developed originally as an antidepressant - it is structurally similar to diethylpropion (an appetite suppressant)
  
  
• in vitro studies suggest that bupropion is a weak inhibitor of re-uptake of dopamine and noradrenaline; also in vitro studies suggest that bupropion is, in addition, a much weaker inhibitor of serotonin re-uptake. Bupropion does not inhibit monoamine oxidase (1)
  
  
• other in vitro studies suggest that bupropion acts as a non-competitive antagonist at nicotine acetylcholine receptors (2)
  
  
• bupropion has a half-life of about 20 hours; steady-state plasma concentrations of bupropion and its metabolites occur within 8 days

Reference:

• 1) Ascher JA et al (1995). Bupropion: a review of its mechanism of antidepressant activity. J Clin Psychiatry, 56, 395-401.
• 2) Fryer JD, Lukas RJ (1999). Noncompetitive functional inhibition at diverse, human nicotinic acetylcholine receptor subtypes by bupropion, phencyclidine, and ibogaine. J Pharmacol Exp Ther, 288, 88-92.