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普萘洛尔剂量、血浆浓度与β受体阻滞

Propranolol dosage, plasma concentration, and beta blockade.

作者信息

Mullane J F, Kaufman J, Dvornik D, Coelho J

出版信息

Clin Pharmacol Ther. 1982 Dec;32(6):692-700. doi: 10.1038/clpt.1982.225.

DOI:10.1038/clpt.1982.225
PMID:7140135
Abstract

One hundred sixty-nine normal men received varying propranolol dosage regimens and placebo. Dose level and frequency were compared with plasma propranolol levels and beta blockade, as assessed by reduction of exercise tachycardia. Propranolol levels above 20 ng/ml induced significant beta blockade. An average daily propranolol dose slightly in excess of 160 mg led to a minimum plasma level above 20 ng/ml. Approximately 50% of subjects achieved 20 bpm or greater decrease in exercise tachycardia with 160 mg per day. The degree of beta blockade at the daily minimum propranolol level was related to dose and not dose frequency. The relation of propranolol dose and plasma levels to beta blockade in normal subjects appears to reflect observations in large clinical trials.

摘要

169名正常男性接受了不同的普萘洛尔给药方案及安慰剂治疗。将剂量水平和给药频率与血浆普萘洛尔水平及β受体阻滞作用进行了比较,β受体阻滞作用通过运动性心动过速的降低来评估。普萘洛尔水平高于20 ng/ml时会引起显著的β受体阻滞。每日普萘洛尔平均剂量略超过160 mg会使血浆最低水平高于20 ng/ml。约50%的受试者每日服用160 mg时运动性心动过速降低20 bpm或更多。每日最低普萘洛尔水平时的β受体阻滞程度与剂量有关,而非给药频率。正常受试者中普萘洛尔剂量和血浆水平与β受体阻滞的关系似乎反映了大型临床试验中的观察结果。

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Propranolol dosage, plasma concentration, and beta blockade.普萘洛尔剂量、血浆浓度与β受体阻滞
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J Pharmacokinet Biopharm. 1987 Dec;15(6):569-82. doi: 10.1007/BF01068413.
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Clin Pharmacokinet. 1987 Jul;13(1):51-64. doi: 10.2165/00003088-198713010-00003.
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Eur J Clin Pharmacol. 1985;29(2):131-47. doi: 10.1007/BF00547412.
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Effect of diltiazem on the pharmacokinetics of propranolol, metoprolol and atenolol.地尔硫䓬对普萘洛尔、美托洛尔和阿替洛尔药代动力学的影响。
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