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依诺昔酮。对其药理特性及治疗潜力的综述。

Enoximone. A review of its pharmacological properties and therapeutic potential.

作者信息

Vernon M W, Heel R C, Brogden R N

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1991 Dec;42(6):997-1017. doi: 10.2165/00003495-199142060-00008.

Abstract

Enoximone is an imidazolone derivative currently undergoing trials in patients with congestive heart failure refractory to conventional therapy. It is a phosphodiesterase inhibitor with both positive inotropic and vasodilator properties, and is active by both oral and intravenous routes of administration. While pharmacodynamic studies have documented beneficial haemodynamic effects after short term oral administration, and objective and subjective improvement relative to placebo during some short term trials, its clinical efficacy during continuous longer term therapy remains uncertain. Enoximone is of potential benefit as an adjunct in short term management of patients with end-stage cardiac failure awaiting cardiac transplantation. In the usually small studies reported to date enoximone was generally better tolerated at oral dosages of less than 2 mg/kg than at higher dosages. Thus, while its pharmacodynamic profile holds potential promise in a difficult therapeutic area, the long term clinical efficacy and tolerability of enoximone remain yet to be determined in controlled trials of adequate size and duration.

摘要

依诺昔酮是一种咪唑啉酮衍生物,目前正在对常规治疗无效的充血性心力衰竭患者进行试验。它是一种磷酸二酯酶抑制剂,具有正性肌力和血管舒张特性,口服和静脉给药均有效。虽然药效学研究记录了短期口服给药后有益的血流动力学效应,以及在一些短期试验中相对于安慰剂的客观和主观改善,但其在持续长期治疗中的临床疗效仍不确定。依诺昔酮作为等待心脏移植的终末期心力衰竭患者短期管理的辅助药物可能有益。在迄今为止报道的通常规模较小的研究中,依诺昔酮口服剂量低于2mg/kg时通常比高剂量时耐受性更好。因此,虽然其药效学特征在一个困难的治疗领域具有潜在前景,但依诺昔酮的长期临床疗效和耐受性仍有待在足够规模和持续时间的对照试验中确定。

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