Bupropion as an Antidote for Serotonin Reuptake Inhibitor-Induced Sexual Dysfunction

Ashton, Adam Keller; Rosen, Raymond C.

doi:10.4088/jcp.v59n0304

Cited by 116 publications

(52 citation statements)

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“…Bupropion has greater affinity for DAT, with IC 50 (mM) values of 58 for serotonin, 2.0 for dopamine and 5.0 for noradrenaline (Ascher et al, 1995). We examined the effects of citalopram and bupropion, both separately and in combination, since the addition of bupropion to an SSRI has been reported to alleviate the sexual dysfunction caused by SSRIs (Ashton and Rosen, 1998;Clayton et al, 2001). We also report the effects of a potent SSRI, paroxetine, on DAT and SERT levels in depressed patients.…”

Section: Introductionmentioning

confidence: 99%

Changes in Human In vivo Serotonin and Dopamine Transporter Availabilities during Chronic Antidepressant Administration

Kugaya

Seneca

Snyder

et al. 2002

Neuropsychopharmacol

152

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Few studies have demonstrated in vivo alterations of human serotonin and dopamine transporters (SERTS and DATS) during antidepressant treatment. The current study measured these transporter availabilities with [123 I]b-CIT single photon emission computed tomography (SPECT) during administration of selective serotonin reuptake inhibitors (SSRIs) or a non-SSRI, bupropion. A total of 17 healthy human subjects were randomly assigned to two different treatment protocols: (1) citalopram (40 mg/day) followed by augmentation with bupropion (100 mg/day) or (2) bupropion (100-200 mg/day) for 16 days. Citalopram significantly inhibited [123 I]b-CIT binding to SERT in brainstem (51.4%) and diencephalon (39.4%) after 8 days of administration, which was similarly observed after 16 days. In contrast, citalopram significantly increased striatal DAT binding by 15-17% after 8 and 16 days of administration. Bupropion and its augmentation to citalopram did not have a significant effect on DAT or SERT. In 10 depressed patients who were treated with paroxetine (20 mg/day), a similar increase in DAT and inhibition of SERT were observed during 6 weeks treatment. The results demonstrated the inhibition of SERT by SSRI in human in vivo during the chronic treatment and, unexpectedly, an elevation of DAT. This apparent SSRI-induced modulation of the dopamine system may be associated with the side effects of these agents, including sexual dysfunction.

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Section: Introductionmentioning

confidence: 99%

Changes in Human In vivo Serotonin and Dopamine Transporter Availabilities during Chronic Antidepressant Administration

Kugaya

Seneca

Snyder

et al. 2002

Neuropsychopharmacol

152

View full text Add to dashboard Cite

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“…[29][30][31][32][33][34][35][36] Bupropion is also an efficacious adjunct treatment option in counteracting SSRI associated sexual dysfunction. [36][37][38][39][40][41] Certainly bupropion and SSRIs are co-prescribed in mentally ill patients; however it is not known if these drugs interact in vivo.…”

Section: Discussionmentioning

confidence: 99%

Drug Interaction Study between Bupropion and Ticlopidine in Male CF-1 Mice

Molnari

Hassan

Moeller

et al. 2011

Biological & Pharmaceutical Bulletin

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Bupropion is an atypical antidepressant that is biotransformed in humans to its major active metabolite hydroxybupropion by cytochrome P450 2B6 (CYP2B6). Co-administration of bupropion with an inhibitor of CYP2B6 can result in a serious drug interaction, leading to bupropion related adverse effects (e.g. seizures). The antiplatelet agent ticlopidine has been identified as a potent in vitro inhibitor of bupropion hydroxylation, however it is unknown if it interacts in vivo in rodents. In this study we investigated the potential pharmacokinetic (PK) drug interaction between bupropion and ticlopidine in mice. Using a destructive sampling design, male CF-1 mice were administered ticlopidine 1.0 mg/kg daily for 5 d, followed by single-dose bupropion 50 mg/kg. Bupropion and hydroxybupropion levels were measured by HPLC-UV in plasma and brain tissues at 30, 60, 90, 120 and 180 min post-dose, and compared between treatment groups. There was a strong trend in both plasma and brain data towards greater bupropion levels and smaller hydroxybupropion levels in ticlopidine treated mice. Analysis of variance indicated statistical differences (pϽ Ͻ0.05) at many time points. The variance associated with the area under the curve was calculated using Bailer's method and significant differences were found between treatment groups. Taken together, the concentration time point statistical analysis followed by PK modeling demonstrate a significant PK drug interaction between bupropion and ticlopidine. To our knowledge, this is the first study to document an in vivo drug interaction between these drugs in mice. Our findings support future in vivo drug interaction studies in mice between bupropion and CYP2B6 inhibitors.

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“…Tilleggsbehandling med bupropion har vaert forsøkt i ulike regimer. I en åpen studie hadde en av tre pasienter nytte av enkeltdoser på 75-150 mg 1-2 timer før samleie (9). Det ble sett effekt både på libido, ereksjon/lubrikasjon og orgasme/ ejakulasjon.…”

Section: Praktisk Håndteringunclassified