哌罗匹隆代谢的广泛变异性及对精神科患者催乳素的影响。
The wide variability of perospirone metabolism and the effect of perospirone on prolactin in psychiatric patients.
机构信息
Department of Psychiatry, Niigata University Graduate School of Medical and Dental Sciences, Niigata, Japan.
出版信息
Prog Neuropsychopharmacol Biol Psychiatry. 2010 Aug 16;34(6):830-3. doi: 10.1016/j.pnpbp.2010.03.027. Epub 2010 Apr 2.
BACKGROUND
Perospirone was developed in Japan and is used for the treatment of schizophrenia and related illnesses. The authors investigated the relationship between the dosage of perospirone and the plasma levels of perospirone and its active metabolite, ID15036, and also evaluated the impact of the plasma concentrations of perospirone and ID15036 on the plasma prolactin level to examine whether perospirone or ID15036 affected the dopamine D(2) blockade, in psychiatric patients treated with perospirone.
METHODS
The subjects consisted of 21 adults treated with perospirone (4-60 mg/day). The plasma perospirone and ID15036 levels were measured in 21 patients and serum prolactin levels were investigated in 10 male patients with schizophrenia.
RESULTS
The plasma ID15036 level was higher than the plasma perospirone, and a positive correlation was observed between the dosage of perospirone and the ID15036 levels (p=0.032). The 10 male patients showed a positive correlation between the plasma perospirone levels and plasma prolactin levels (r=0.688, p=0.028) and between the plasma ID15036 levels and prolactin levels (r=0.775, p=0.009).
CONCLUSION
The plasma levels of ID15036 may have a greater impact on the dopamine D(2) blockade than perospirone in patients treated with perospirone.
背景
哌罗匹隆由日本研发，用于治疗精神分裂症及相关疾病。作者研究了哌罗匹隆剂量与哌罗匹隆及其活性代谢物 ID15036 的血浆浓度之间的关系，并评估了哌罗匹隆和 ID15036 的血浆浓度对催乳素水平的影响，以考察哌罗匹隆或 ID15036 是否会影响接受哌罗匹隆治疗的精神科患者的多巴胺 D2 阻断作用。
方法
本研究的对象为 21 例接受哌罗匹隆（4-60mg/天）治疗的成年人。21 例患者检测了血浆哌罗匹隆和 ID15036 浓度，10 例男性精神分裂症患者检测了血清催乳素浓度。
结果
ID15036 的血浆浓度高于哌罗匹隆，哌罗匹隆剂量与 ID15036 浓度呈正相关（p=0.032）。10 例男性患者的血浆哌罗匹隆浓度与催乳素浓度呈正相关（r=0.688，p=0.028），血浆 ID15036 浓度与催乳素浓度也呈正相关（r=0.775，p=0.009）。
结论
与哌罗匹隆相比，接受哌罗匹隆治疗的患者中 ID15036 的血浆浓度可能对多巴胺 D2 阻断作用的影响更大。
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