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慢性口服普萘洛尔治疗期间血浆中普萘洛尔和4-羟基普萘洛尔的浓度。

Plasma concentrations of propranolol and 4-hydroxypropranolol during chronic oral propranolol therapy.

作者信息

Wong L, Nation R L, Chiou W L, Mehta P K

出版信息

Br J Clin Pharmacol. 1979 Aug;8(2):163-7. doi: 10.1111/j.1365-2125.1979.tb05815.x.

DOI:10.1111/j.1365-2125.1979.tb05815.x
PMID:486291
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1429768/
Abstract

1 The plasma levels of propranolol and 4-hydroxypropranolol have been measured in 17 hypertensive patients receiving chronic oral therapy with propranolol. 2 The range of plasma propranolol concentrations was from 5.3 to 300 ng/ml, and that of 4-hydroxypropranolol was from 2.1 to 36.0 ng/ml. 3 The mean (+/- s.d.) plasma concentration ratio of 4-hydroxypropranolol to propranolol was 0.130 (+/- 0.005); however, a very wide range was observed with individual values ranging from 0.057 to 0.241. 4 A statistically significant correlation was observed between the plasma concentration of 4-hydroxypropranolol and that of propranolol. 5 Propranolol and 4-hydroxypropranolol plasma concentrations were each significantly, but poorly, correlated with daily propranolol dose. 6 The clinical significance of the results has been discussed.

摘要
  1. 已对17名接受普萘洛尔长期口服治疗的高血压患者测定了其血浆中普萘洛尔和4-羟基普萘洛尔的水平。

  2. 血浆普萘洛尔浓度范围为5.3至300 ng/ml,4-羟基普萘洛尔的浓度范围为2.1至36.0 ng/ml。

  3. 4-羟基普萘洛尔与普萘洛尔的平均(±标准差)血浆浓度比为0.130(±0.005);然而,观察到个体值范围非常宽,从0.057至0.241。

  4. 观察到4-羟基普萘洛尔的血浆浓度与普萘洛尔的血浆浓度之间存在统计学显著相关性。

  5. 普萘洛尔和4-羟基普萘洛尔的血浆浓度各自与每日普萘洛尔剂量显著但相关性较差。

  6. 已讨论了结果的临床意义。

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1
Plasma concentrations of propranolol and 4-hydroxypropranolol during chronic oral propranolol therapy.慢性口服普萘洛尔治疗期间血浆中普萘洛尔和4-羟基普萘洛尔的浓度。
Br J Clin Pharmacol. 1979 Aug;8(2):163-7. doi: 10.1111/j.1365-2125.1979.tb05815.x.
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Clin Pharmacol Ther. 1980 Jan;27(1):22-31. doi: 10.1038/clpt.1980.4.
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Propranolol plasma levels and relief of migraine. Relationship between plasma propranolol and 4-hydroxypropranolol concentrations and clinical effects.
Arch Neurol. 1985 Jan;42(1):46-8. doi: 10.1001/archneur.1985.04060010052015.
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Effects of cholestyramine and colestipol on the plasma concentrations of propranolol.消胆胺和考来替泊对普萘洛尔血浆浓度的影响。
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Fluorometric TLC determination of free and conjugated propranolol, naphthoxylactic acid, and p-hydroxypropranolol in human plasma and urine.荧光薄层色谱法测定人血浆和尿液中游离及结合的普萘洛尔、萘氧乳酸和对羟基普萘洛尔
J Pharm Sci. 1978 Jun;67(6):826-31. doi: 10.1002/jps.2600670626.
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Clin Pharmacol Ther. 1980 Jul;28(1):32-9. doi: 10.1038/clpt.1980.127.
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Br J Clin Pharmacol. 1982 Jul;14(1):79-82. doi: 10.1111/j.1365-2125.1982.tb04937.x.
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Plasma concentrations of propranolol and 4-hydroxy-propranolol at steady-state in neurological patients: intersubject and intrasubject correlations with dose.
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Plasma concentrations of propranolol and 4-hydroxypropranolol in man measured by high pressure liquid chromatography.
Life Sci. 1979 Jan 15;24(3):209-17. doi: 10.1016/0024-3205(79)90221-2.

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本文引用的文献

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Relation of propranolol plasma level to beta-blockade during oral therapy.口服治疗期间普萘洛尔血浆水平与β受体阻滞的关系。
Pharmacology. 1972;7(3):178-84. doi: 10.1159/000136287.
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Studies on the absorption, distribution and excretion of propranolol in rat, dog and monkey.大鼠、犬和猴体内普萘洛尔的吸收、分布及排泄研究。
J Pharmacol Exp Ther. 1971 Feb;176(2):302-11.
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Effect of route of administration on the relationship between -adrenergic blockade and plasma propranolol level.给药途径对β-肾上腺素能阻滞与血浆普萘洛尔水平之间关系的影响。
Clin Pharmacol Ther. 1972 Mar-Apr;13(2):181-5. doi: 10.1002/cpt1972132181.
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Pharmacology of 4-hydroxypropranolol, a metabolite of propranolol.普萘洛尔的代谢产物4-羟基普萘洛尔的药理学
Br J Pharmacol. 1971 Sep;43(1):222-35. doi: 10.1111/j.1476-5381.1971.tb07171.x.
5
Spuriously low plasma propranolol concentrations resulting from blood collection methods.采血方法导致血浆普萘洛尔浓度假性降低。
Clin Pharmacol Ther. 1975 Nov;18(5 Pt 1):535-8. doi: 10.1002/cpt1975185part1535.
6
Studies of the absorption and removal of propranolol in hypertensive patients during therapy.高血压患者治疗期间普萘洛尔吸收与清除情况的研究。
Circulation. 1975 Aug;52(2):313-8. doi: 10.1161/01.cir.52.2.313.
7
Clinical pharmacology of propranolol.普萘洛尔的临床药理学
Circulation. 1975 Jul;52(1):6-15. doi: 10.1161/01.cir.52.1.6.
8
Plasma binding and the affinity of propranolol for a beta receptor in man.
Clin Pharmacol Ther. 1976 Aug;20(2):152-7. doi: 10.1002/cpt1976202152.
9
Fluorometric TLC determination of free and conjugated propranolol, naphthoxylactic acid, and p-hydroxypropranolol in human plasma and urine.荧光薄层色谱法测定人血浆和尿液中游离及结合的普萘洛尔、萘氧乳酸和对羟基普萘洛尔
J Pharm Sci. 1978 Jun;67(6):826-31. doi: 10.1002/jps.2600670626.
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High-pressure liquid chromatographic method for the simultaneous quantitative analysis of propranolol and 4-hydroxypropranolol in plasma.
J Chromatogr. 1978 May 1;145(3):429-36. doi: 10.1016/s0378-4347(00)81372-9.