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硫必利。对其药效学和药代动力学特性以及在老年躁动症治疗潜力的综述。

Tiapride. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in geriatric agitation.

作者信息

Steele J W, Faulds D, Sorkin E M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs Aging. 1993 Sep-Oct;3(5):460-78. doi: 10.2165/00002512-199303050-00007.

Abstract

Tiapride is a substituted benzamide derivative with selective dopamine D2-receptor antagonist properties which appears to have preferential affinity for extrastriatal dopamine receptors. Animal and clinical studies show that tiapride has anxiolytic properties but the mechanism of action is uncertain. Results from limited studies indicate that the clinical efficacy of tiapride in the treatment of agitation, aggressiveness, anxiety and sleep disorders in the elderly appears superior to that of placebo, chlorpromazine, lorazepam and meprobamate. Tiapride also exerts a beneficial effect on vigilance and alertness in elderly patients and causes less sedation than chlorpromazine. Tiapride is well tolerated at the dosages recommended for elderly patients. Further well designed comparative studies with newer drugs are needed to determine the relative place of tiapride in the treatment of geriatric agitation, and such studies should also address the quality-of-life benefits for the patient. Additional clinical experience to determine the efficacy of tiapride in elderly patients with more than one disease condition, receiving concomitant medications, and/or with renal impairment is also required. However, despite these current limitations, tiapride may have potentially important applications in this difficult area of clinical medicine.

摘要

硫必利是一种具有选择性多巴胺D2受体拮抗剂特性的取代苯甲酰胺衍生物,似乎对纹状体以外的多巴胺受体具有优先亲和力。动物和临床研究表明,硫必利具有抗焦虑特性,但其作用机制尚不确定。有限研究的结果表明,硫必利在治疗老年人的激越、攻击性、焦虑和睡眠障碍方面的临床疗效似乎优于安慰剂、氯丙嗪、劳拉西泮和甲丙氨酯。硫必利对老年患者的警觉性和觉醒也有有益作用,且比氯丙嗪引起的镇静作用小。按照推荐给老年患者的剂量使用,硫必利耐受性良好。需要进一步设计良好的与新药的对比研究,以确定硫必利在治疗老年激越方面的相对地位,此类研究还应探讨对患者生活质量的益处。还需要更多的临床经验来确定硫必利在患有多种疾病、正在接受联合用药和/或有肾功能损害的老年患者中的疗效。然而,尽管目前存在这些局限性,硫必利在这一困难的临床医学领域可能有潜在的重要应用。

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