Alprazolam: Pharmacokinetics, Clinical Efficacy, and Mechanism of Action

Alprazolam: Pharmacokinetics, Clinical Efficacy, and Mechanism of Action
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阿普唑仑:药代动力学、临床疗效和作用机制

DOI:
10.1002/j.1875-9114.1982.tb03191.x
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发表时间:
1982
期刊:
Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy
影响因子:
--
通讯作者:
H. Kravitz
H. Kravitz
中科院分区:
--
文献类型:
--
作者:
J. Fawcett;H. Kravitz

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阿普唑仑是一种三唑苯并二氮类药物,是第一种在美国和加拿大上市的这类新的苯二氮卓类药物。它在0.7至2.1小时内达到血药浓度峰值,血清半衰期为12至15小时。在推荐的每日剂量为0.5-4.0毫克时,它与安定和氯氮卓酮一样有效,是一种抗焦虑药物。它目前被批准的适应症是用于治疗焦虑症和焦虑症状,包括与抑郁相关的焦虑。尽管目前还没有被批准用于治疗抑郁症,但迄今为止发表的研究表明,阿普唑仑与标准的三环抗抑郁药相比具有更好的疗效。阿普唑仑在治疗恐慌症方面的潜在作用也在调查中。阿普唑仑已用于老年患者,效果良好,不良反应发生率低。它的主要副作用,嗜睡,比同等剂量的安定产生的要少。关于毒性、耐受性和停药情况的数据有限,但阿普唑仑似乎至少与其他苯二氮类药物相当。药物相互作用的数据也是有限的,在给服用其他精神药物的患者开阿普唑仑时应该小心,因为潜在的附加抑郁效应。
Alprazolam, a triazolobenzodiazepine, is the first of this new class of benzodiazepine drugs to be marketed in the United States and Canada. It achieves peak serum levels in 0.7 to 2.1 hours and has a serum half‐life of 12 to 15 hours. When given in the recommended daily dosage of 0.5 to 4.0 mg, it is as effective as diazepam and chlordiazepoxide as an anxiolytic agent. Its currently approved indication is for the treatment of anxiety disorders and symptoms of anxiety, including anxiety associated with depression. Although currently not approved for the treatment of depressive disorders, studies published to date have demonstrated that alprazolam compares favorably with standard tricyclic antidepressants. Also undergoing investigation is the potential role of alprazolam in the treatment of panic disorders. Alprazolam has been used in elderly patients with beneficial results and a low frequency of adverse reactions. Its primary side effect, drowsiness, is less than that produced by diazepam at comparable doses. Data on toxicity, tolerance, and withdrawal profile are limited, but alprazolam seems to be at least comparable to other benzodiazepines. Drug interaction data are also limited, and care should be exercised when prescribing alprazolam for patients taking other psychotropic drugs because of potential additive depressant effects.
DOI: 10.1001/archpsyc.1983.01790030057007
发表时间: 1983
影响因子: --
作者:
Greenblatt,DJ;Divoll,M;Abernethy,DR;Moschitto,LJ;Smith,RB;Shader,RI
通讯作者: Shader,RI
内源性抑郁症的睡眠和治疗预测。
DOI: 10.1176/ajp.138.4.429
发表时间: 1981
期刊: The American journal of psychiatry
影响因子: --
作者:
Kupfer,DJ;Spiker,DG;Coble,PA;Neil,JF;Ulrich,R;Shaw,DH
通讯作者: Shaw,DH
DOI: 10.1073/pnas.78.3.1939
发表时间: 1981
影响因子: 11.1
作者:
Gavish,M;Snyder,SH
通讯作者: Snyder,SH