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口服给药后醋丁洛尔的剂量依赖性处置。

Dose-dependent acebutolol disposition after oral administration.

作者信息

Meffin P J, Winkle R A, Peters F A, Harrison D C

出版信息

Clin Pharmacol Ther. 1978 Nov;24(5):542-7. doi: 10.1002/cpt1978245542.

DOI:10.1002/cpt1978245542
PMID:699478
Abstract

The relationship between dose and area under the blood concentration-time curve has been studied in 6 healthy subjects following both oral and intravenous doses of acebutolol. There is a more than proportional increase in area with increasing oral doses, and the area over a dosing interval following multiple oral doses is greater than the total area after a single dose of the same size. The role of an acetyl metabolite in producing these effects is discussed, as is the relevance of these observations to the clinical use of acebutolol.

摘要

在6名健康受试者中,研究了醋丁洛尔口服和静脉给药后的剂量与血药浓度-时间曲线下面积之间的关系。随着口服剂量增加,曲线下面积呈超比例增加,多次口服给药后一个给药间隔内的曲线下面积大于相同剂量单次给药后的总面积。文中讨论了乙酰代谢产物在产生这些效应中的作用,以及这些观察结果与醋丁洛尔临床应用的相关性。

相似文献

1
Dose-dependent acebutolol disposition after oral administration.口服给药后醋丁洛尔的剂量依赖性处置。
Clin Pharmacol Ther. 1978 Nov;24(5):542-7. doi: 10.1002/cpt1978245542.
2
The influence of renal function on plasma levels and urinary excretion of acebutolol and its main N-acetyl metabolite.肾功能对醋丁洛尔及其主要N-乙酰代谢产物的血浆水平和尿排泄的影响。
Clin Nephrol. 1982 Aug;18(2):88-94.
3
Circulatory effects of intravenous and oral acebutolol in acute myocardial infarction.静脉注射与口服醋丁洛尔对急性心肌梗死的循环系统影响
Clin Pharmacol Ther. 1985 Sep;38(3):266-72. doi: 10.1038/clpt.1985.169.
4
Observations on the pharmacokinetics of acebutolol.醋丁洛尔的药代动力学观察
Clin Pharmacol Ther. 1976 Apr;19(4):416-20. doi: 10.1002/cpt1976194416.
5
Acebutolol disposition after intravenous administration.静脉注射后醋丁洛尔的处置情况。
Clin Pharmacol Ther. 1977 Nov;22(5 Pt 1):557-67. doi: 10.1002/cpt1977225part1557.
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Acebutolol metabolite plasma concentration during chronic oral therapy.慢性口服治疗期间醋丁洛尔代谢物的血浆浓度
Br J Clin Pharmacol. 1977 Oct;4(5):519-22. doi: 10.1111/j.1365-2125.1977.tb00779.x.
7
The pharmacokinetics of acebutolol in man, following the oral administration of acebutolol HCl as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d.).盐酸醋丁洛尔单次口服给药(400毫克)后,以及多次口服给药期间和之后(400毫克,每日两次)在人体中的药代动力学。
Biopharm Drug Dispos. 1981 Apr-Jun;2(2):103-14. doi: 10.1002/bdd.2510020202.
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Quantitation in plasma and urine of acebutolol and a major metabolite with preliminary observations on their disposition kinetics in man.醋丁洛尔及其主要代谢产物在血浆和尿液中的定量分析以及对其在人体处置动力学的初步观察。
Res Commun Chem Pathol Pharmacol. 1976 Sep;15(1):31-51.
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Plasma and urine concentrations of acebutolol and its acetyl metabolite in patients with renal functional impairment.肾功能损害患者中醋丁洛尔及其乙酰代谢物的血浆和尿液浓度。
N Z Med J. 1980 Apr 23;91(658):289-91.
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Once-daily dosing of acebutolol in hypertension.
J Cardiovasc Pharmacol. 1983 Jan-Feb;5(1):157-61. doi: 10.1097/00005344-198301000-00024.

引用本文的文献

1
Pharmacokinetics of acebutolol in patients with all grades of renal failure.醋丁洛尔在各程度肾衰竭患者中的药代动力学
Eur J Clin Pharmacol. 1980 May;17(5):339-48. doi: 10.1007/BF00558446.
2
A single and multiple dose pharmacokinetic and pharmacodynamic comparison of conventional and slow-release metroprolol.常规释放与缓释美托洛尔的单剂量和多剂量药代动力学及药效学比较。
Eur J Clin Pharmacol. 1980 Feb;17(2):87-92. doi: 10.1007/BF00562615.
3
Observations on the clinical pharmacology and plasma concentrations of diacetolol, the major human metabolite of acebutolol.
醋丁洛尔的主要人体代谢物双醋洛尔的临床药理学及血药浓度观察
Br J Clin Pharmacol. 1981 Oct;12(4):561-5. doi: 10.1111/j.1365-2125.1981.tb01265.x.
4
Pharmacokinetics and bioavailability of diacetolol, the main metabolite of acebutolol.醋丁洛尔的主要代谢产物双醋洛尔的药代动力学和生物利用度。
Eur J Clin Pharmacol. 1981 Mar;19(4):287-92. doi: 10.1007/BF00562806.
5
Comparison of the pharmacodynamic and pharmacokinetic profiles of single and multiple doses of a commercial slow-release metoprolol formulation with a new Oros delivery system.采用新型渗透泵给药系统的市售缓释美托洛尔制剂单剂量与多剂量的药效学和药代动力学特征比较。
Br J Clin Pharmacol. 1982 Mar;13(3):393-8. doi: 10.1111/j.1365-2125.1982.tb01391.x.
6
Pharmacokinetics in man of acebutolol and hydrochlorothiazide as single agents and in combination.醋丁洛尔和氢氯噻嗪单药及联合用药在人体中的药代动力学。
Eur J Clin Pharmacol. 1983;24(6):801-6. doi: 10.1007/BF00607091.
7
Comparative pharmacokinetic profiles of metoprolol and chlorthalidone administered alone or in combination to healthy volunteers.美托洛尔和氯噻酮单独或联合给药于健康志愿者的比较药代动力学特征。
Eur J Clin Pharmacol. 1983;24(5):655-60. doi: 10.1007/BF00542217.
8
A multiple dose comparative study of the pharmacodynamic and pharmacokinetic behaviour of polymer-matrix and Oros dosage forms of oxprenolol in healthy volunteers.在健康志愿者中进行的氧烯洛尔聚合物基质剂型和渗透泵控释剂型的药效学及药代动力学行为的多剂量对比研究。
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):177S-184S. doi: 10.1111/j.1365-2125.1985.tb02759.x.
9
Acebutolol. A review of its pharmacological properties and therapeutic efficacy in hypertension, angina pectoris and arrhythmia.醋丁洛尔。其药理学特性及在高血压、心绞痛和心律失常治疗中的疗效综述。
Drugs. 1985 Jun;29(6):531-69. doi: 10.2165/00003495-198529060-00003.
10
Pharmacokinetics of sustained-release verapamil after a single administration and at steady state.单次给药及稳态下缓释维拉帕米的药代动力学
Eur J Drug Metab Pharmacokinet. 1985 Apr-Jun;10(2):133-8. doi: 10.1007/BF03189707.