瑞莫必利：药代动力学及对血浆催乳素的影响
Remoxipride: pharmacokinetics and effect on plasma prolactin.
作者信息
Movin-Osswald G, Hammarlund-Udenaes M
机构信息
Department of Clinical Pharmacology, Astra Research Centre AB, Södertlje, Sweden.
出版信息
Br J Clin Pharmacol. 1991 Sep;32(3):355-60. doi: 10.1111/j.1365-2125.1991.tb03911.x.
Abstract
- The pharmacokinetics of remoxipride, a new neuroleptic, were investigated in 15 healthy subjects after an intravenous infusion of 50 mg, an intramuscular injection of 100 mg and after administration of two immediate release capsules (A and B), each of 100 mg, in a cross-over study. The effect of the different remoxipride formulations on plasma prolactin concentrations was also studied. 2. The volume of distribution of remoxipride was 0.65 +/- 0.11 kg-1 (mean +/- s.d.). Total plasma clearance was 119 +/- 39 ml min-1, of which 31 +/- 13 ml min-1 was due to renal clearance. The absolute bioavailability after the i.m. and oral formulations was greater than 90%, indicating a small extent of first-pass metabolism. The mean elimination half-life was 4.8 +/- 1.4 h. The unbound fraction of remoxipride and the blood/plasma ratio were 0.19 +/- 0.03 and 0.64 +/- 0.06, respectively. 3. The transient increase in plasma prolactin was similar after all four remoxipride administrations and independent of the given dose.
摘要
- 在一项交叉研究中，对15名健康受试者静脉输注50毫克、肌内注射100毫克以及服用两粒每粒100毫克的速释胶囊（A和B）后，研究了新型抗精神病药物瑞莫必利的药代动力学。还研究了不同瑞莫必利制剂对血浆催乳素浓度的影响。2. 瑞莫必利的分布容积为0.65±0.11千克/升（平均值±标准差）。总血浆清除率为119±39毫升/分钟，其中31±13毫升/分钟为肾清除率所致。肌内注射和口服制剂后的绝对生物利用度大于90%，表明首过代谢程度较小。平均消除半衰期为4.8±1.4小时。瑞莫必利的游离分数和血/浆比分别为0.19±0.03和0.64±0.06。3. 所有四种瑞莫必利给药后，血浆催乳素的短暂升高相似，且与给药剂量无关。
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本文引用的文献
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Remoxipride, a new potential antipsychotic compound with selective antidopaminergic actions in the rat brain.瑞莫必利，一种在大鼠脑中具有选择性抗多巴胺能作用的新型潜在抗精神病化合物。
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Remoxipride--a new potential antipsychotic drug. Pharmacological effects and pharmacokinetics following repeated oral administration in male volunteers.
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Psychopharmacology (Berl). 1989;98(3):304-9. doi: 10.1007/BF00451679.
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Clinical profile of remoxipride--a combined analysis of a comparative double-blind multicentre trial programme.
Acta Psychiatr Scand Suppl. 1990;358:92-8. doi: 10.1111/j.1600-0447.1990.tb05297.x.
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Safety evaluation in both short- and long-term treatment of schizophrenia with remoxipride.瑞莫必利治疗精神分裂症的短期和长期安全性评估。
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