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福辛普利:新一代血管紧张素转换酶抑制剂。

Fosinopril: a new generation of angiotensin-converting enzyme inhibitors.

作者信息

Weber M A

机构信息

Section of Clinical Pharmacology and Hypertension, Long Beach VA Medical Center, California 90822.

出版信息

J Cardiovasc Pharmacol. 1992;20 Suppl 10:S7-12. doi: 10.1097/00005344-199200101-00003.

Abstract

Fosinopril, the first agent in a new chemical class of phosphorus-containing angiotensin-converting enzyme (ACE) inhibitors, has unique pharmacologic properties. Fosinopril administration leads to complete inhibition of plasma ACE activity for 12-24 h. In patients with normal renal function, approximately equal amounts of the drug are eliminated via the hepatic and renal routes. With worsening renal function, increasing amounts of fosinopril are eliminated hepatically. This dual elimination allows for the administration of fosinopril using the same starting dosage to any patient, regardless of renal function. Fosinopril may provide end-organ protection against the effects of hypertension and antihypertensive therapy; this drug potentially protects the kidney by increasing renal functional reserve, while maintaining cardiac left ventricular performance. Moreover, despite marked blood reductions, cerebral blood flow is maintained. Controlled trials show that fosinopril in single daily doses of 10-40 mg is efficacious and safe for the long-term treatment of hypertension. At these doses, favorable responses were seen in up to 80% of patients. Fosinopril is equally effective in elderly as well as younger patients and works in black as well as in nonblack patients. The incidence of adverse events does not differ significantly between fosinopril- and placebo-treated patients. Fosinopril represents a clinically useful agent for the treatment of hypertension.

摘要

福辛普利是新型含磷血管紧张素转换酶(ACE)抑制剂化学类别中的首个药物,具有独特的药理特性。服用福辛普利可使血浆ACE活性完全抑制12 - 24小时。在肾功能正常的患者中,大约等量的药物通过肝脏和肾脏途径消除。随着肾功能恶化,经肝脏消除的福辛普利量增加。这种双重消除方式使得无论肾功能如何,都可以使用相同的起始剂量对任何患者给药福辛普利。福辛普利可能为高血压及抗高血压治疗的影响提供终末器官保护;该药物可能通过增加肾功能储备来保护肾脏,同时维持心脏左心室功能。此外,尽管血压显著降低,但脑血流量得以维持。对照试验表明,每日单次服用10 - 40毫克福辛普利对高血压的长期治疗有效且安全。在这些剂量下,高达80%的患者有良好反应。福辛普利在老年患者和年轻患者中同样有效,在黑人患者和非黑人患者中均起作用。福辛普利治疗组和安慰剂治疗组患者不良事件的发生率无显著差异。福辛普利是治疗高血压的一种临床有用药物。

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