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阿立必利,一种新型取代苯甲酰胺,用作癌症化疗期间的止吐药。

Alizapride, a new substituted benzamide, as an antiemetic during cancer chemotherapy.

作者信息

Joss R A, Galeazzi R L, Bischoff A K, Brunner K W

出版信息

Eur J Clin Pharmacol. 1985;27(6):721-5. doi: 10.1007/BF00547056.

DOI:10.1007/BF00547056
PMID:3987777
Abstract

In early clinical trials alizapride showed a better antiemetic activity with fewer side effects than metoclopramide. Alizapride has now been evaluated in an open dose-ranging study in 24 patients receiving strongly emetic chemotherapy. Alizapride 4-8 mg/kg was given as a 15 min infusion 0.5 h before and 1.5, 3.5, 5.5 and 8.5 h after the chemotherapy. At the dose levels of 6 and 8 mg/kg x 5, respectively 6 out-of 9 and 4 of 4 patients experienced side effects (hypotension, dizziness, profuse sweating, general malaise and diarrhoea). At 4 mg/kg x 54 of 15 patients experienced side effects due to alizapride (dyspnoea 1, diarrhoea 2, extrapyramidal syndrome 1 patient). Overall, 9 of 24 patients were partially or completely protected from nausea and vomiting. Based on this experience alizapride has antiemetic activity and few side effects in the dose of 4 mg/kg x 5.

摘要

在早期临床试验中,阿立必利显示出比甲氧氯普胺更好的止吐活性,且副作用更少。阿立必利现已在一项开放性剂量范围研究中进行评估,该研究纳入了24名接受强效致吐化疗的患者。阿立必利4 - 8mg/kg在化疗前0.5小时以及化疗后1.5、3.5、5.5和8.5小时以15分钟输注的方式给药。在剂量水平分别为6mg/kg×5和8mg/kg×5时,9名患者中有6名以及4名患者中的4名出现了副作用(低血压、头晕、大量出汗、全身不适和腹泻)。在4mg/kg×5的剂量水平时,15名患者中有4名因阿立必利出现了副作用(呼吸困难1例、腹泻2例、锥体外系综合征1例)。总体而言,24名患者中有9名在一定程度上或完全免受恶心和呕吐的困扰。基于这一经验,阿立必利在4mg/kg×5的剂量下具有止吐活性且副作用较少。

相似文献

1
Alizapride, a new substituted benzamide, as an antiemetic during cancer chemotherapy.阿立必利,一种新型取代苯甲酰胺,用作癌症化疗期间的止吐药。
Eur J Clin Pharmacol. 1985;27(6):721-5. doi: 10.1007/BF00547056.
2
The antiemetic activity of high-dose alizapride and high-dose metoclopramide in patients receiving cancer chemotherapy: a prospective, randomized, double-blind trial.
Clin Pharmacol Ther. 1986 Jun;39(6):619-24. doi: 10.1038/clpt.1986.109.
3
[Evaluation of a new antiemetic, alizapride, in cancerology (author's transl)].
Sem Hop. 1982 Jun 3;58(22):1370-3.
4
Antiemetic efficacy of escalating doses of alizapride against chemotherapy-induced emesis.递增剂量阿立必利对化疗所致呕吐的止吐疗效。
Oncology. 1989;46(4):235-7. doi: 10.1159/000226723.
5
Anti-emetic effect of high-dose metoclopramide vs alizapride--a randomised crossover study.高剂量甲氧氯普胺与阿立必利的止吐效果比较——一项随机交叉研究。
Br J Clin Pharmacol. 1994 Sep;38(3):282-4. doi: 10.1111/j.1365-2125.1994.tb04355.x.
6
[Antiemetic and antinauseant effect of alizapride in patients subjected to antiblastic infusion chemotherapy in a day-hospital regime].[阿立必利在日间医院模式下接受抗恶性肿瘤灌注化疗患者中的止吐和抗恶心作用]
G Ital Oncol. 1989 Jan-Mar;9(1):18-21.
7
[Phase I study of alizapride in cancer patients treated with cisplatin].阿立必利在接受顺铂治疗的癌症患者中的Ⅰ期研究
Sem Hop. 1983 Sep 8;59(31):2161-5.
8
[Alizapride in the treatment of vomiting induced by cytostatic agents].[阿立必利治疗细胞抑制剂所致呕吐]
Fortschr Med. 1983 Apr 14;101(14):662-4.
9
Activity of a new antiemetic agent: alizapride. A randomized double-blind crossover controlled trial.
Cancer Chemother Pharmacol. 1988;22(4):316-20. doi: 10.1007/BF00254238.
10
[Comparative double-blind study: alizapride-metoclopramide].[对照双盲研究:阿立必利-甲氧氯普胺]
Ann Gastroenterol Hepatol (Paris). 1984 Jan-Feb;20(1):59-61.

引用本文的文献

1
A randomized trial comparing alizapride alone or with dexamethasone vs a metoclopramide-dexamethasone combination for emesis induced by moderate-dose cisplatin.
Cancer Chemother Pharmacol. 1987;19(4):335-8. doi: 10.1007/BF00261484.
2
Does parenteral magnesium sulfate have an antiemetic effect during chemotherapy with cis-platinum?肠胃外硫酸镁在顺铂化疗期间有止吐作用吗?
Cancer Chemother Pharmacol. 1989;24(2):109-12. doi: 10.1007/BF00263130.
3
Rational pharmacotherapy of gastrointestinal motility disorders.胃肠动力障碍的合理药物治疗。

本文引用的文献

1
The course of nausea and vomiting after high-dose cyclophosphamide.大剂量环磷酰胺治疗后恶心呕吐的病程。
Cancer Treat Rep. 1982 Jul;66(7):1487-93.
2
Intravenous metoclopramide. An effective antiemetic in cancer chemotherapy.静脉注射胃复安。癌症化疗中一种有效的止吐药。
JAMA. 1982 May 21;247(19):2683-6. doi: 10.1001/jama.247.19.2683.
3
Antiemetic efficacy of high-dose metoclopramide: randomized trials with placebo and prochlorperazine in patients with chemotherapy-induced nausea and vomiting.大剂量甲氧氯普胺的止吐疗效:在化疗引起的恶心和呕吐患者中与安慰剂和丙氯拉嗪的随机试验
Eur J Pediatr. 1989 Apr;148(6):489-95. doi: 10.1007/BF00441540.
N Engl J Med. 1981 Oct 15;305(16):905-9. doi: 10.1056/NEJM198110153051601.
4
The control of chemotherapy-induced emesis.化疗引起的呕吐的控制
Ann Intern Med. 1981 Sep;95(3):352-9. doi: 10.7326/0003-4819-95-3-352.
5
Gastrointestinal toxicity of cis-diamminedichloroplatinum (II).
Neth J Med. 1982;25(8):270-4.
6
Continuous infusion of high-dose metoclopramide for the prevention of nausea and vomiting in patients receiving cancer chemotherapy.
Eur J Clin Pharmacol. 1983;25(1):35-9. doi: 10.1007/BF00544011.
7
[Evaluation of a new antiemetic, alizapride, in cancerology (author's transl)].
Sem Hop. 1982 Jun 3;58(22):1370-3.
8
[Pharmacokinetics and bioavailability of alizapride (author's transl)].
Sem Hop. 1982 Feb 11;58(6):339-44.
9
[Pharmacodynamics of alizapride (author's transl)].阿立必利的药效学(作者译)
Sem Hop. 1982 Feb 11;58(6):323-31.