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培哚普利。对其药理特性及在心血管疾病治疗中的应用综述。

Perindopril. A review of its pharmacological properties and therapeutic use in cardiovascular disorders.

作者信息

Todd P A, Fitton A

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1991 Jul;42(1):90-114. doi: 10.2165/00003495-199142010-00006.

Abstract

Perindopril is a long acting angiotensin converting enzyme (ACE) inhibitor, which displays similar pharmacodynamic properties to other agents in this class. In common with enalapril, it is also a prodrug. After absorption, perindopril is hydrolysed to the active metabolite, perindoprilat, and with once daily administration adequate 24-hour inhibition of ACE is obtained. Perindopril 4 to 8mg once daily is usually effective for blood pressure control in patients with mild to moderate essential hypertension. Those patients who do not respond adequately to monotherapy with perindopril usually respond with the addition of a second agent, such as a thiazide diuretic. General practice trials indicate that perindopril is at least as effective and as well tolerated as usual therapeutic dosages of captopril, atenolol or hydrochlorothiazide plus amiloride in mild to moderate essential hypertension. Preliminary results indicate that perindopril may also be effective in patients with severe hypertension or congestive heart failure. Perindopril is generally well tolerated and has an adverse effect profile similar to that of other ACE inhibitors. It further clinical experience confirms initial findings, perindopril is likely to represent a useful alternative to other members of the ACE inhibitor class in all grades of hypertension and congestive heart failure.

摘要

培哚普利是一种长效血管紧张素转换酶(ACE)抑制剂,其药理动力学特性与该类其他药物相似。与依那普利一样,它也是一种前体药物。吸收后,培哚普利被水解为活性代谢产物培哚普利拉,每日给药一次即可实现对ACE的24小时充分抑制。培哚普利每日一次4至8毫克通常对轻度至中度原发性高血压患者的血压控制有效。那些对培哚普利单一疗法反应不佳的患者通常加用第二种药物(如噻嗪类利尿剂)后会有反应。全科医学试验表明,在轻度至中度原发性高血压中,培哚普利至少与卡托普利、阿替洛尔或氢氯噻嗪加阿米洛利的常规治疗剂量一样有效且耐受性良好。初步结果表明,培哚普利对重度高血压或充血性心力衰竭患者可能也有效。培哚普利一般耐受性良好,不良反应情况与其他ACE抑制剂相似。如果进一步的临床经验证实了初步发现,那么在所有级别的高血压和充血性心力衰竭中,培哚普利可能是ACE抑制剂类其他药物的一种有用替代药物。

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