静脉注射红霉素后的个体间差异及剂量相关变异性。
Intersubject and dose-related variability after intravenous administration of erythromycin.
作者信息
Austin K L, Mather L E, Philpot C R, McDonald P J
出版信息
Br J Clin Pharmacol. 1980 Sep;10(3):273-9. doi: 10.1111/j.1365-2125.1980.tb01755.x.
Abstract
1 It is well-known that considerable variability and unpredictability in serum concentrations results from orally administered erythromycin. 2 Disposition kinetics and their variability were studies in 24 healthy subjects after a single dose of erythromycin lactobionate and four doses were studied to evaluate dose-related variability in five other subjects. 3 Erythromycin kinetics were adequately described by a classical two compartment open model with little intersubject variability. 4 Dose-related variability occurred. Clearance was independent of dose but T1/2 beta and Vdss increased with dose. 5 Data are presented to show that non-invasive sampling of urine and saliva are of limited value in studying erythromycin pharmacokinetics.
摘要
众所周知，口服红霉素后血清浓度会有相当大的变异性和不可预测性。
对24名健康受试者单次给予乳糖酸红霉素后研究了处置动力学及其变异性，并对另外5名受试者给予四剂药物以评估剂量相关变异性。
红霉素动力学可用经典的二室开放模型充分描述，个体间变异性较小。
出现了剂量相关变异性。清除率与剂量无关，但T1/2β和Vdss随剂量增加。
所提供的数据表明，尿液和唾液的非侵入性采样在研究红霉素药代动力学方面价值有限。
相似文献
1
Intersubject and dose-related variability after intravenous administration of erythromycin.静脉注射红霉素后的个体间差异及剂量相关变异性。
Br J Clin Pharmacol. 1980 Sep;10(3):273-9. doi: 10.1111/j.1365-2125.1980.tb01755.x.
2
Dose-related pharmacokinetics after oral administration of a new formulation of erythromycin base.口服新剂型红霉素碱后的剂量相关药代动力学。
Br J Clin Pharmacol. 1982 May;13(5):685-91. doi: 10.1111/j.1365-2125.1982.tb01437.x.
3
Absorption and bioavailability of oral erythromycin.口服红霉素的吸收与生物利用度。
Br J Clin Pharmacol. 1981 Aug;12(2):131-40. doi: 10.1111/j.1365-2125.1981.tb01191.x.
4
Pharmacokinetics of intravenous erythromycin lactobionate.
J Int Med Res. 1980;8 Suppl 2:15-23.
5
Pharmacokinetics of a new, microencapsulated erythromycin base after repeated oral doses.新型微囊化红霉素碱重复口服给药后的药代动力学
Chemotherapy. 1982;28(3):176-84. doi: 10.1159/000238073.
6
Biliary excretion of erythromycin after parenteral administration.静脉注射后红霉素的胆汁排泄
Br J Clin Pharmacol. 1979 Sep;8(3):233-5. doi: 10.1111/j.1365-2125.1979.tb01007.x.
7
Pharmacokinetics of intravenous erythromycin.静脉注射红霉素的药代动力学
J Pharm Sci. 1978 Aug;67(8):1057-9. doi: 10.1002/jps.2600670809.
8
Plasma and saliva concentrations for a new formulation of erythromycin stearate.硬脂酸红霉素新制剂的血浆和唾液浓度。
Curr Med Res Opin. 1979;6(2):118-23. doi: 10.1185/03007997909109408.
9
Pharmacokinetics of erythromycin on repetitive dosing.红霉素重复给药的药代动力学
J Clin Pharmacol. 1977 Oct;17(10 Pt 1):592-600. doi: 10.1177/009127007701701006.
10
Reversible sensorineural hearing loss with intravenous erythromycin lactobionate.静脉注射乳糖酸红霉素导致的可逆性感音神经性听力损失。
Ann Otol Rhinol Laryngol. 1977 Jan-Feb;86(1 Pt 1):9-11. doi: 10.1177/000348947708600103.
引用本文的文献
1
Impact of sex and pregnancy on hepatic CYP3A4 expression and activity in a humanized mouse model.性别和妊娠对人源化小鼠模型中肝脏CYP3A4表达及活性的影响
Drug Metab Dispos. 2025 Feb;53(2):100025. doi: 10.1016/j.dmd.2024.100025. Epub 2024 Nov 29.
2
Pregnane X Receptor and the Gut-Liver Axis: A Recent Update.孕烷 X 受体与肠-肝轴：最新进展。
Drug Metab Dispos. 2022 Apr;50(4):478-491. doi: 10.1124/dmd.121.000415. Epub 2021 Dec 3.
3
Hepatic Cytochrome P450 Abundance and Activity in the Developing and Adult Göttingen Minipig: Pivotal Data for PBPK Modeling.发育中和成年哥廷根小型猪肝脏细胞色素P450的丰度和活性：用于生理药代动力学（PBPK）建模的关键数据。
Front Pharmacol. 2021 Apr 15;12:665644. doi: 10.3389/fphar.2021.665644. eCollection 2021.
4
Relationship between primary eradication of and drinking habits in women: collaborative research between a pharmacy and a clinic.与女性饮酒习惯之间的关系：药房与诊所之间的合作研究。
Epidemiol Infect. 2019 Oct 22;147:e292. doi: 10.1017/S0950268819001730.
5
The Role of Macrolides in Chronic Rhinosinusitis (CRSsNP and CRSwNP).大环内酯类药物在慢性鼻-鼻窦炎（非鼻息肉型慢性鼻-鼻窦炎和鼻息肉型慢性鼻-鼻窦炎）中的作用
Curr Allergy Asthma Rep. 2017 May;17(5):30. doi: 10.1007/s11882-017-0696-z.
6
Systemic exposure of topical erythromycin in comparison to oral administration and the effect on cytochrome P450 3A4 activity.与口服给药相比，局部用红霉素的全身暴露情况及其对细胞色素P450 3A4活性的影响。
Br J Clin Pharmacol. 2014 Dec;78(6):1433-40. doi: 10.1111/bcp.12497.
7
Microphysiological modeling of the reproductive tract: a fertile endeavor.生殖道的微生理建模：一项富有成效的努力。
Exp Biol Med (Maywood). 2014 Sep;239(9):1192-202. doi: 10.1177/1535370214529387. Epub 2014 Apr 15.
8
Macrolide antibiotics and the risk of cardiac arrhythmias.大环内酯类抗生素与心律失常风险。
Am J Respir Crit Care Med. 2014 May 15;189(10):1173-80. doi: 10.1164/rccm.201402-0385CI.
9
Indinavir Pharmacokinetics during Different Phases of the Menstrual Cycle in HIV-Infected Women.感染 HIV 的女性在月经周期不同阶段的茚地那韦药代动力学。
Clin Drug Investig. 2002;22(2):125-34. doi: 10.2165/00044011-200222020-00007.
10
Nano-bio-technology and sensing chips: new systems for detection in personalized therapies and cell biology.纳米生物技术和传感芯片：个性化治疗和细胞生物学检测的新系统。
Sensors (Basel). 2010;10(1):526-43. doi: 10.3390/s100100526. Epub 2010 Jan 12.
本文引用的文献
1
Factors affecting the absorption and biliary excretion of erythromycin and two of its derivatives in humans.影响红霉素及其两种衍生物在人体中吸收和胆汁排泄的因素。
Clin Pharmacol Ther. 1961 May-Jun;2:308-12. doi: 10.1002/cpt196123308.
2
Demethylation of erythromycins by rabbit tissues in vitro.
Biochem Pharmacol. 1965 Jul;14(7):1049-58. doi: 10.1016/0006-2952(65)90033-x.
3
Variations in absorption of erythromycin.红霉素吸收的差异。
Med J Aust. 1969 Mar 1;1(9):449-51. doi: 10.5694/j.1326-5377.1969.tb92211.x.
4
Serum protein binding of erythromycin and erythromycin 2'-propionate ester.红霉素及红霉素2'-丙酸酯的血清蛋白结合情况。
J Pharm Sci. 1972 Mar;61(3):425-8. doi: 10.1002/jps.2600610322.
5
Serum protein binding of erythromycin, lincomycin, and clindamycin.红霉素、林可霉素和克林霉素的血清蛋白结合情况。
J Pharm Sci. 1973 Jul;62(7):1074-7. doi: 10.1002/jps.2600620704.
6
Intestinal secretion of erythromycin base.
J Pharm Sci. 1976 Mar;65(3):417-9. doi: 10.1002/jps.2600650325.
7
Erythromycin symposium: introduction.
Scott Med J. 1977 Dec;22(5):349-51. doi: 10.1177/00369330770220S101.
8
Complications of intravenous therapy: reduction by buffering of intravenous fluid preparation.静脉治疗的并发症：通过缓冲静脉输液制剂来减少
Med J Aust. 1977 Oct 15;2(16):528-31. doi: 10.5694/j.1326-5377.1977.tb114619.x.
9
Influence of sex on drug kinetics in man.性别对人体药物动力学的影响。
Clin Pharmacokinet. 1977 May-Jun;2(3):157-66. doi: 10.2165/00003088-197702030-00001.
10
Pharmacokinetics of Erythromycin in man.红霉素在人体中的药代动力学
Antibiot Chemother (1971). 1978;25:181-203.
Zotero 插件