红霉素对卡马西平转化为其活性10,11 - 环氧化代谢物的抑制作用。
Inhibition by erythromycin of the conversion of carbamazepine to its active 10,11-epoxide metabolite.
作者信息
Barzaghi N, Gatti G, Crema F, Monteleone M, Amione C, Leone L, Perucca E
机构信息
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
出版信息
Br J Clin Pharmacol. 1987 Dec;24(6):836-8. doi: 10.1111/j.1365-2125.1987.tb03257.x.
Abstract
The serum levels of carbamazepine (CBZ) and its 10,11-epoxide metabolite (CBZ-E) were determined in seven subjects after a single dose of CBZ (400 mg) in the control state and during co-administration of erythromycin (500 mg three times daily for 10 days). Erythromycin treatment was associated with a decrease in CBZ clearance and a prolongation of CBZ half-life, while CBZ-E levels were markedly reduced. These data provide evidence that erythromycin inhibits the conversion of CBZ to its epoxide metabolite.
摘要
在7名受试者中，测定了他们在对照状态下单次服用卡马西平（CBZ，400mg）以及在联合使用红霉素（每日3次，每次500mg，共10天）期间血清中卡马西平（CBZ）及其10,11 - 环氧化代谢物（CBZ - E）的水平。红霉素治疗与卡马西平清除率降低及卡马西平半衰期延长有关，而CBZ - E水平则显著降低。这些数据证明红霉素可抑制卡马西平向其环氧化代谢物的转化。
相似文献
1
Inhibition by erythromycin of the conversion of carbamazepine to its active 10,11-epoxide metabolite.红霉素对卡马西平转化为其活性10,11 - 环氧化代谢物的抑制作用。
Br J Clin Pharmacol. 1987 Dec;24(6):836-8. doi: 10.1111/j.1365-2125.1987.tb03257.x.
2
Effect of flurithromycin, a new macrolide antibiotic, on carbamazepine disposition in normal subjects.新型大环内酯类抗生素氟红霉素对正常受试者卡马西平处置的影响。
Int J Clin Pharmacol Res. 1988;8(2):101-5.
3
Interaction of carbamazepine-10,11-epoxide, an active metabolite of carbamazepine, with valproate: a pharmacokinetic study.
Epilepsia. 1990 May-Jun;31(3):339-42. doi: 10.1111/j.1528-1157.1990.tb05385.x.
4
5
Autoinduction and steady-state pharmacokinetics of carbamazepine and its major metabolites.卡马西平及其主要代谢产物的自动诱导和稳态药代动力学
Br J Clin Pharmacol. 1992 Jun;33(6):611-5. doi: 10.1111/j.1365-2125.1992.tb04089.x.
6
Carbamazepine-10,11-diol steady-state serum levels and renal excretion during carbamazepine therapy in adults and children.卡马西平治疗成人和儿童期间卡马西平 -10,11 -二醇的稳态血清水平及肾脏排泄情况
Ther Drug Monit. 1984;6(3):259-65. doi: 10.1097/00007691-198409000-00001.
7
Single-dose kinetics and metabolism of carbamazepine-10,11-epoxide.卡马西平-10,11-环氧化物的单剂量动力学与代谢
Clin Pharmacol Ther. 1983 Jan;33(1):58-65. doi: 10.1038/clpt.1983.8.
8
Kinetics of carbamazepine and its 10,11-epoxide metabolite in children.儿童体内卡马西平及其10,11-环氧化代谢物的动力学
Clin Pharmacol Ther. 1976 Mar;19(3):276-83. doi: 10.1002/cpt1976193276.
9
Pharmacokinetic study of carbamazepine and its epoxide metabolite in humans.
J Pharmacobiodyn. 1987 Nov;10(11):652-61. doi: 10.1248/bpb1978.10.652.
10
Carbamazepine metabolism in man. Induction and pharmacogenetic aspects.人类体内的卡马西平代谢。诱导作用及药物遗传学方面。
Clin Pharmacokinet. 1985 Jan-Feb;10(1):80-90. doi: 10.2165/00003088-198510010-00004.
引用本文的文献
1
Pharmacokinetics of the CYP3A4 and CYP2B6 Inducer Carbamazepine and Its Drug-Drug Interaction Potential: A Physiologically Based Pharmacokinetic Modeling Approach.CYP3A4和CYP2B6诱导剂卡马西平的药代动力学及其药物相互作用潜力：基于生理的药代动力学建模方法
Pharmaceutics. 2021 Feb 17;13(2):270. doi: 10.3390/pharmaceutics13020270.
2
Interactions Between Antiepileptic and Antibiotic Drugs: A Systematic Review and Meta-Analysis with Dosing Implications.抗癫痫药与抗生素药物相互作用：系统评价和荟萃分析及其给药影响。
Clin Pharmacokinet. 2019 Jul;58(7):875-886. doi: 10.1007/s40262-018-0720-z.
3
Macrolide - induced clinically relevant drug interactions with cytochrome P-450A (CYP) 3A4: an update focused on clarithromycin, azithromycin and dirithromycin.大环内酯类药物与细胞色素P-450A（CYP）3A4的临床相关药物相互作用：聚焦于克拉霉素、阿奇霉素和地红霉素的最新进展
Br J Clin Pharmacol. 2000 Oct;50(4):285-95. doi: 10.1046/j.1365-2125.2000.00261.x.
4
Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition.细胞色素P450 3A4抑制的药代动力学-药效学后果及临床相关性
Clin Pharmacokinet. 2000 Jan;38(1):41-57. doi: 10.2165/00003088-200038010-00003.
5
Macrolide antibacterials. Drug interactions of clinical significance.大环内酯类抗菌药物。具有临床意义的药物相互作用。
Drug Saf. 1995 Aug;13(2):105-22. doi: 10.2165/00002018-199513020-00005.
本文引用的文献
1
Simultaneous liquid-chromatographic determination of carbamazepine and its epoxide metabolite in plasma.
Clin Chem. 1982 Oct;28(10):2127-30.
2
Carbamazepine intoxication due to triacetyloleandomycin administration in epileptic patients.
Epilepsia. 1980 Oct;21(5):489-96. doi: 10.1111/j.1528-1157.1980.tb04300.x.
3
Effect of erythromycin on carbamazepine kinetics.
Clin Pharmacol Ther. 1983 Apr;33(4):460-4. doi: 10.1038/clpt.1983.62.
4
Carbamazepine--erythromycin-base interaction.卡马西平与红霉素碱的相互作用。
Med J Aust. 1984 Jan 21;140(2):81. doi: 10.5694/j.1326-5377.1984.tb103896.x.
5
Carbamazepine--erythromycin interaction leading to carbamazepine toxicity in four epileptic children.卡马西平与红霉素相互作用导致4名癫痫患儿出现卡马西平中毒
Ther Drug Monit. 1983;5(4):405-7. doi: 10.1097/00007691-198312000-00005.
6
Carbamazepine toxicity induced by concurrent erythromycin therapy.同时使用红霉素治疗引起的卡马西平中毒。
Arch Neurol. 1985 Feb;42(2):187-8. doi: 10.1001/archneur.1985.04060020105023.
7
Erythromycin-carbamazepine interaction.红霉素-卡马西平相互作用
Neurology. 1986 Apr;36(4):594-5. doi: 10.1212/wnl.36.4.594b.
8
A case of erythromycin-induced carbamazepine toxicity.一例红霉素诱发的卡马西平中毒病例。
J Clin Psychiatry. 1986 Mar;47(3):147.
9
Carbamazepine-erythromycin interaction. Case studies and clinical significance.卡马西平与红霉素的相互作用。病例研究及临床意义。
JAMA. 1986 Mar 7;255(9):1165-7. doi: 10.1001/jama.255.9.1165.
10
Carbamazepine-danazol drug interaction: its mechanism examined by a stable isotope technique.
Ther Drug Monit. 1986;8(4):387-92.
Zotero 插件