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原发性高血压长期治疗后停用胍法辛。关于血压、血浆和尿去甲肾上腺素的观察。

Withdrawal of guanfacine after long-term treatment in essential hypertension. Observations on blood pressure and plasma and urinary noradrenaline.

作者信息

Zamboulis C, Reid J L

出版信息

Eur J Clin Pharmacol. 1981 Jan;19(1):19-24. doi: 10.1007/BF00558376.

DOI:10.1007/BF00558376
PMID:7007059
Abstract
  1. Guanfacine (2-6 mg/day) a centrally acting antihypertensive drug, was effective in controlling blood pressure in 5 essential hypertensives and lowered plasma noradrenaline and urinary catecholamine excretion. 2. Withdrawal of guanfacine by blind substitution of identical placebo tablets under observation in hospital led to a gradual recovery of blood pressure over 2-4 days. 3. Salivary flow, which was reduced on guanfacine, returned to pretreatment levels by 2 days after withdrawal and significantly exceeded control for the next two days. 4. Urinary catecholamine excretion returned to pretreatment levels by 3 days but did not exceed control levels during the period of study. 5. Plasma noradrenaline returned gradually to pretreatment levels, and by day 4 significantly exceeded them. 6. No patient experienced symptoms suggesting catecholamine excess although four out of five reported a headache from the second day onwards. 7. Guanfacine, a centrally acting drug which pharmacologically resembles clonidine, has a slow offset of hypotensive effect over 2-3 days. Symptoms or biochemical evidence of catecholamine excess were not encountered within 48 h of withdrawal, possibly reflecting the longer duration of action and plasma half-life of guanfacine.
摘要
  1. 胍法辛(2 - 6毫克/天),一种中枢性抗高血压药物,对5例原发性高血压患者控制血压有效,并降低了血浆去甲肾上腺素和尿儿茶酚胺排泄量。2. 在医院观察下,通过盲目替换为相同的安慰剂片剂停用胍法辛,导致血压在2 - 4天内逐渐恢复。3. 胍法辛使唾液分泌减少,停药后2天恢复到治疗前水平,并在接下来的两天显著超过对照组。4. 尿儿茶酚胺排泄量在3天内恢复到治疗前水平,但在研究期间未超过对照组水平。5. 血浆去甲肾上腺素逐渐恢复到治疗前水平,到第4天显著超过该水平。6. 尽管五分之四的患者从第二天起报告头痛,但没有患者出现提示儿茶酚胺过量的症状。7. 胍法辛是一种中枢性药物,药理作用类似于可乐定,其降压作用在2 - 3天内缓慢消退。停药后48小时内未出现儿茶酚胺过量的症状或生化证据,这可能反映了胍法辛作用持续时间较长和血浆半衰期较长。

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Withdrawal of guanfacine after long-term treatment in essential hypertension. Observations on blood pressure and plasma and urinary noradrenaline.原发性高血压长期治疗后停用胍法辛。关于血压、血浆和尿去甲肾上腺素的观察。
Eur J Clin Pharmacol. 1981 Jan;19(1):19-24. doi: 10.1007/BF00558376.
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本文引用的文献

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Improved technique for the fluorimetric estimation of catecholamines.儿茶酚胺荧光测定的改进技术。
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Changes in blood pressure, heart rate, and sympathetic activity on abrupt withdrawal of tiamenidine (HOE 440) in essential hypertension.原发性高血压患者突然停用噻美尼定(HOE 440)后血压、心率及交感神经活动的变化
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Some observations on the inhibition of salivation by St 155 [2-(2,6-dichlorophenylamine)-2-imidazoline hydrochloride, Catapres, Catapresan].
Guanfacine and clonidine: antihypertensive and withdrawal characteristics after continuous infusion and its interruption in the spontaneously hypertensive and normotensive rat.
胍法辛和可乐定:连续输注及其中断后在自发性高血压大鼠和正常血压大鼠中的降压及撤药特征
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Guanfacine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of hypertension.胍法辛。对其药效学、药代动力学特性及治疗高血压疗效的综述。
Drugs. 1986 Apr;31(4):301-36. doi: 10.2165/00003495-198631040-00003.
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Clinical consequences of abrupt drug withdrawal.突然停药的临床后果。
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Central nervous system mechanisms in blood pressure control.血压控制中的中枢神经系统机制。
Eur J Clin Pharmacol. 1985;28 Suppl:3-11. doi: 10.1007/BF00543703.
关于St 155[2-(2,6-二氯苯胺)-2-咪唑啉盐酸盐,可乐定,氯压定]对唾液分泌抑制作用的一些观察
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4
Studies on catecholamines, renin and aldosterone following Catapresan (2-(2,6-dichlor-phenylamine)-2-imidazoline hydrochloride) in hypertensive patients.高血压患者服用可乐宁(2-(2,6-二氯苯胺)-2-咪唑啉盐酸盐)后儿茶酚胺、肾素和醛固酮的研究。
Eur J Pharmacol. 1970;10(3):389-97. doi: 10.1016/0014-2999(70)90212-8.
5
Effects of clonidine withdrawal: possible mechanisms and suggestions for management.可乐定撤药的影响:可能机制及处理建议
Br Med J. 1973 Apr 28;2(5860):209-11. doi: 10.1136/bmj.2.5860.209.
6
Pharmacological actions of the antihypertensive agent N-amidino-2-(2,6-dichlorophenyl)acetamide hydrochloride (BS 100-141).抗高血压药物盐酸N-脒基-2-(2,6-二氯苯基)乙酰胺(BS 100-141)的药理作用
Arzneimittelforschung. 1975 Oct;25(10):1483-91.
7
A sensitive radioenzymatic assay for norepinephrine in tissues and plasma.一种用于检测组织和血浆中去甲肾上腺素的灵敏放射酶分析法。
Life Sci. 1975 Feb 1;16(3):375-84. doi: 10.1016/0024-3205(75)90258-1.
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Effects of clonidine on biochemical indices of sympathetic function and plasma renin activity in normotensive man.
Clin Sci Mol Med. 1977 Jul;53(1):45-53. doi: 10.1042/cs0530045.
9
Comparison of the actions of central and peripheral administration of clonidine and BS 100-141 in the rabbit [proceedings].可乐定和BS 100 - 141经中枢和外周给药对家兔作用的比较[会议论文集]
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Pharmacokinetic and concentration-effect relationships of clonidine in essential hypertension.可乐定在原发性高血压中的药代动力学及浓度-效应关系
Eur J Clin Pharmacol. 1977 Dec 28;12(6):463-9. doi: 10.1007/BF00561067.