Piloerection induced by replacing fluvoxamine with milnacipran
Piloerection induced by replacing fluvoxamine with milnacipran
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DOI：
10.1111/j.1365-2125.2006.02838.x
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发表时间：
2007-06-01
影响因子：
3.4
通讯作者：
Sawada, Yasufumi
中科院分区：
文献类型：
--
作者：
Hori, Satoko;Matsuo, Nobuko;Sawada, Yasufumi
目的报道1例盐酸米那西普兰替代马来酸氟伏沙明后出现勃起的病例，并根据受体占用理论分析其影响。方法40岁女性，3年惊恐障碍病史，在氯硝西酯双钾和舒必利的基础上给予氟伏沙明50 mg d（-1）。抑郁症没有改善，她抱怨疲劳，缺乏精力和困倦。将氟伏沙明剂量增加到50毫克，每日两次，这些症状在几天内恶化。由于怀疑氟伏沙明和替扎尼定（另一家诊所开的处方）之间存在相互作用，因此氟伏沙明被米那西普兰（milnacpran）代替，每天50mg（-1）。虽然她的睡意有所改善，但她抱怨全身都有勃起的感觉。该症状在一周内逐渐减轻，当milnacpran剂量在2个月时增加到100mg /天（-1）时，不再发生勃起。我们利用从文献中获得的药代动力学和药效学参数，计算了内源性去甲肾上腺素在常用剂量米那西普兰、氟伏沙明和丙咪嗪治疗期间α(1)-肾上腺素受体占用率的变化。结果内源性去甲肾上腺素对米那西普兰、氟伏沙明和丙咪嗪治疗组α(1)-肾上腺素受体的占据比分别为7.13、1.00和4.12。内源性去甲肾上腺素对α(1)-肾上腺素受体的占用以剂量依赖性的方式增加，而氟伏沙明基本上没有影响。结论该患者用米那西普兰替代氟伏沙明后出现的阴茎勃起，可能是由于米那西普兰诱导内源性去甲肾上腺素增加了α(1)-肾上腺素受体的占据。
Aims To present a case of piloerection after replacing fluvoxamine maleate with milnacipran hydrochloride, and to analyse this effect based on receptor occupancy theory.Methods A 40-year-old female with a 3-year history of panic disorder was prescribed fluvoxamine 50 mg day(-1) in addition to clorazepate dipotassium and sulpiride. Depression was not improved and she complained of fatigue, lack of energy and drowsiness. These symptoms worsened within a few days of an increase in the dose of fluvoxamine to 50 mg twice daily. Since an interaction between fluvoxamine and tizanidine, prescribed by another clinic, was suspected, fluvoxamine was replaced with milnacipran 50 mg day(-1). Although her drowsiness improved, she complained of piloerection throughout her body. This symptom gradually abated within a week and when the dosage of milnacipran was increased to 100 mg day(-1) at 2 months, no further piloerection occurred. We calculated the changes in alpha(1)-adrenoceptor occupancy by endogenous norepinephrine during treatment with the usual doses of milnacipran, fluvoxamine and imipramine by using pharmacokinetic and pharmacodynamic parameters obtained from the literature.Results The ratios of alpha(1)-adrenoceptor occupancy by endogenous norepinephrine during the treatment with milnacipran, fluvoxamine and imipramine to that without drug were estimated to be 7.13, 1.00 and 4.12, respectively. The alpha(1)-adrenoceptor occupancy by endogenous norepinephrine was increased in a dose-dependent manner by milnacipran, whereas fluvoxamine had essentially no effect.Conclusions The piloerection observed after the replacement of fluvoxamine with milnacipran in this patient appears to have been due to an increase in the alpha(1)-adrenoceptor occupancy by endogenous norepinephrine induced by milnacipran.