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恩屈嗪,一种新型外周血管扩张剂。三年期间安全性和有效性评估。

Endralazine, a new peripheral vasodilator. Evaluation of safety and efficacy over a 3 year period.

作者信息

Bogers W A, Meems L

出版信息

Eur J Clin Pharmacol. 1983;24(3):301-5. doi: 10.1007/BF00610045.

DOI:10.1007/BF00610045
PMID:6861845
Abstract

Nineteen out-patients with moderate to severe essential hypertension were treated daily for 3 years, with an average dose of 13 mg endralazine, a new peripheral vasodilator, in free combination with pindolol 3 x 5 mg. The blood pressure showed a statistically significant reduction from 172/110 mmHg to 154/92 mmHg after treatment for 3 years. Tachyphylaxis was not observed during the 3 years period. Oedema was the most frequent side-effect, but it disappeared spontaneously. No difference in efficacy and tolerance between slow and fast acetylators was found. Only 2 patients developed a weak positive antinuclear antibody titre, which disappeared spontaneously from one during continued treatment. No clinical evidence of a systemic lupus erythematosus-like syndrome was noted. It is concluded that the differences between endralazine and hydralazine in dosage and metabolism may explain the lower immunogenic activity of endralazine.

摘要

19例中重度原发性高血压门诊患者接受了为期3年的治疗,每日服用平均剂量为13毫克的恩屈嗪(一种新型外周血管扩张剂),并与3×5毫克的吲哚洛尔自由联合使用。治疗3年后,血压从172/110毫米汞柱降至154/92毫米汞柱,具有统计学显著差异。在这3年期间未观察到快速耐受性。水肿是最常见的副作用,但会自行消失。慢乙酰化者和快乙酰化者在疗效和耐受性方面未发现差异。只有2例患者抗核抗体滴度呈弱阳性,其中1例在持续治疗期间自行消失。未发现系统性红斑狼疮样综合征的临床证据。结论是,恩屈嗪和肼屈嗪在剂量和代谢方面的差异可能解释了恩屈嗪较低的免疫原活性。

相似文献

1
Endralazine, a new peripheral vasodilator. Evaluation of safety and efficacy over a 3 year period.恩屈嗪,一种新型外周血管扩张剂。三年期间安全性和有效性评估。
Eur J Clin Pharmacol. 1983;24(3):301-5. doi: 10.1007/BF00610045.
2
Endralazine, a new peripheral vasodilator--a randomized cross-over trial against dihydralazine.恩屈嗪,一种新型外周血管扩张剂——与双肼屈嗪对比的随机交叉试验。
J Cardiovasc Pharmacol. 1982 Jul-Aug;4(4):562-6. doi: 10.1097/00005344-198207000-00006.
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Clinical evaluation of endralazine (BO22708), a new vasodilator, in essential hypertension.新型血管扩张剂恩屈嗪(BO22708)治疗原发性高血压的临床评估
Clin Exp Hypertens A. 1982;4(8):1409-18. doi: 10.3109/10641968209060798.
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Endralazine, a new peripheral vasodilator: absence of effect of acetylator status on antihypertensive effect.恩屈嗪,一种新型外周血管扩张剂:乙酰化状态对其降压效果无影响。
Lancet. 1983 Mar 26;1(8326 Pt 1):670-1. doi: 10.1016/s0140-6736(83)91967-0.
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Evaluation of once daily endralazine in hypertension.每日一次服用恩屈嗪治疗高血压的疗效评估。
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Pharmacodynamic and pharmacokinetic studies with the vasodilator endralazine.血管扩张剂恩屈嗪的药效学和药代动力学研究。
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引用本文的文献

1
Clinical pharmacological studies with the vasodilator endralazine in patients with renal impairment.
Eur J Clin Pharmacol. 1984;27(2):159-63. doi: 10.1007/BF00544039.
2
Evaluation of once daily endralazine in hypertension.每日一次服用恩屈嗪治疗高血压的疗效评估。
Eur J Clin Pharmacol. 1986;30(5):553-7. doi: 10.1007/BF00542414.
3
Comparison of once daily endralazine with placebo in the treatment of hypertension uncontrolled by a beta-blocker and diuretic.每日一次服用恩屈嗪与安慰剂治疗β受体阻滞剂和利尿剂控制不佳的高血压的比较。

本文引用的文献

1
Effect of dose on acetylator phenotype distribution of hydralazine.
Clin Pharmacol Ther. 1981 Mar;29(3):337-43. doi: 10.1038/clpt.1981.46.
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Kinetics of hydralazine and its main metabolites in slow and fast acetylators.慢乙酰化者和快乙酰化者中肼屈嗪及其主要代谢物的动力学
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Hydrallazine-induced lupus erythematosus-like syndrome in a patient of the rapid acetylator phenotype.一名快速乙酰化酶表型患者出现肼屈嗪诱导的类红斑狼疮综合征。
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Genetically determined variability in acetylation and oxidation. Therapeutic implications.乙酰化和氧化的基因决定变异性。治疗意义。
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Hydralazine-pyrimidine interactions may explain hydralazine-induced lupus erythematosus.肼屈嗪与嘧啶的相互作用可能解释肼屈嗪诱发的红斑狼疮。
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[Management of treatment-resistant hypertension: comparison of the antihypertensive effect of endralazine and minoxidil (author's transl)].
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Sensitive high-performance liquid chromatographic assay for endralazine and two of its metabolites in human plasma.人血浆中恩屈嗪及其两种代谢物的灵敏高效液相色谱测定法。
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Further evidence for an acetylator phenotype difference in the metabolism of hydralazine in man.关于人体内肼屈嗪代谢中乙酰化表型差异的进一步证据。
Br J Clin Pharmacol. 1981 Apr;11(4):345-51. doi: 10.1111/j.1365-2125.1981.tb01131.x.
8
Acetylator phenotype and lupus erythematosus.乙酰化酶表型与红斑狼疮
Clin Pharmacokinet. 1981 Mar-Apr;6(2):118-34. doi: 10.2165/00003088-198106020-00003.
9
Hydrallazine in hypertension: is there a safe dose?肼屈嗪治疗高血压:是否存在安全剂量?
Br Med J. 1980 Aug 2;281(6236):353-4. doi: 10.1136/bmj.281.6236.353.
10
Antinuclear antibodies and cardiovascular drugs.抗核抗体与心血管药物
Drugs. 1980 Apr;19(4):292-305. doi: 10.2165/00003495-198019040-00004.