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Bupropion appears to enhance monoaminergic neurotransmission via its effects on both the NE and DA transporterswith subsequent reuptake inhibition of these 2 neurotransmittersBupropion and 2 of its metaboliteshydroxybupropion and threohydrobupropionwere shown to decrease the uptake of NE and DA into rat and mouse synaptosomes9 Bupropion’s activity as a DA transporter inhibitor is further supported by a recent study showing approximately a 3-fold increase in expression of the immediate early gene c-fos in human DA transporter cellsandif coincubated with DAan attenuation of the DA-induced c-fos in human DA transporter cells14 Acute administration of bupropion reduces firing of brain stem NE and DA neuronsdata on fileGlaxoSmithKlineResearch Triangle ParkN.CAdditionallyfiring rates of NE neurons in the locus ceruleus are inhibited after acute bupropion administration9 Microdialysis studies following acute administration of bupropion demonstrate that extra-cellular NE and DA concentrations are increased in the nucleus accumbensdata on fileGlaxoSmithKlineResearch Triangle ParkN.CFurther evidence of the NDRI action of bupropion was found when administration of NEor DA-blocking drugs was shown to reduce the efficacy of bupropionand hydroxybupropionin animal models of depression15.
FDA pregnancy category CIt is not known whether bupropion will harm an unborn babyTell your doctor if you are pregnant or plan to become pregnant while using this medicine.
Studies in rodents and primates have shown that bupropion exhibits some pharmacologic actions common to psychostimulantsIn rodentsit has been shown to increase locomotor activityelicit a mild stereotyped behavioral responseand increase rates of responding in several schedule-controlled behavior paradigmsIn primate models to assess the positive reinforcing effects of psychoactive drugsbupropion was self-administered intravenouslyIn ratsbupropion produced amphetamine-like and cocaine-like discriminative stimulus effects in drug discrimination paradigms used to characterize the subjective effects of psychoactive drugs.
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