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纳必隆。其药理特性与治疗用途的初步综述。

Nabilone. A preliminary review of its pharmacological properties and therapeutic use.

作者信息

Ward A, Holmes B

出版信息

Drugs. 1985 Aug;30(2):127-44. doi: 10.2165/00003495-198530020-00002.

Abstract

Nabilone is a new orally active cannabinoid for the treatment of severe gastrointestinal toxicity associated with cancer chemotherapy. The pharmacological profile of nabilone suggests that it acts primarily by preventing emesis controlled by the medulla oblongata, although its secondary mild anxiolytic activity may contribute to the overall efficacy. Nabilone 2mg twice daily starting 12 hours prior to, and continued for the duration of, chemotherapy produces significant reduction in the severity and duration of nausea and the frequency of vomiting in about 50 to 70% of patients with severe symptoms refractory to conventional therapy. Nabilone has proven to be more effective in controlling symptoms and preferred by more patients than prochlorperazine 10mg 2 to 4 times daily in a limited number of studies, despite a higher incidence of side effects. Comparative trials against other new antiemetic agents, such as high dose metoclopramide, and use of nabilone in combination with other antiemetics remain to be undertaken. The incidence of side effects is high with nabilone; drowsiness, dizziness and/or vertigo occur in 60 to 70% of patients, but rarely lead to drug withdrawal, although more troublesome effects, such as postural hypotension, ataxia, vision disturbance and toxic psychoses, may cause discontinuation of therapy. Thus, nabilone offers an effective alternative to the treatment options available in a difficult therapeutic area - those patients with severe gastrointestinal side effects from cancer chemotherapy who are refractory to conventional therapy.

摘要

纳布啡是一种新型口服活性大麻素,用于治疗与癌症化疗相关的严重胃肠道毒性。纳布啡的药理特性表明,它主要通过预防延髓控制的呕吐起作用,尽管其继发的轻度抗焦虑活性可能有助于整体疗效。在化疗前12小时开始,每天两次服用2毫克纳布啡,并持续整个化疗期间,可使约50%至70%有严重症状且对传统治疗无效的患者的恶心严重程度和持续时间以及呕吐频率显著降低。在有限的研究中,尽管副作用发生率较高,但已证明纳布啡在控制症状方面比每日2至4次服用10毫克氯丙嗪更有效,且更受患者青睐。与其他新型止吐药(如高剂量甲氧氯普胺)的对比试验以及纳布啡与其他止吐药联合使用的研究仍有待开展。纳布啡的副作用发生率较高;60%至70%的患者会出现嗜睡、头晕和/或眩晕,但很少导致停药,尽管更麻烦的影响,如体位性低血压、共济失调、视力障碍和中毒性精神病,可能会导致治疗中断。因此,对于癌症化疗导致严重胃肠道副作用且对传统治疗无效的患者这一治疗困难领域,纳布啡为现有的治疗选择提供了一种有效的替代方案。

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