丙戊酸钠可急性抑制拉莫三嗪的代谢。
Sodium valproate acutely inhibits lamotrigine metabolism.
作者信息
Yuen A W, Land G, Weatherley B C, Peck A W
机构信息
Wellcome Research Laboratories, Beckenham, Kent.
出版信息
Br J Clin Pharmacol. 1992 May;33(5):511-3. doi: 10.1111/j.1365-2125.1992.tb04079.x.
Abstract
Concomitant administration of sodium valproate (VPA) reduced lamotrigine (LTG) total clearance by approximately 21% and increased elimination half-life and AUC. Reduced elimination occurred acutely within the first hour. Renal elimination of LTG was not impaired. The most probable explanation for this effect is hepatic competition between VPA and LTG for glucuronidation. Volume of distribution and parameters related to absorption, Cmax and tmax were unchanged.
摘要
丙戊酸钠（VPA）与拉莫三嗪（LTG）同时给药可使拉莫三嗪的总清除率降低约21%，并延长消除半衰期和增加药时曲线下面积（AUC）。在给药后的第一小时内即迅速出现清除率降低的情况。拉莫三嗪的肾排泄未受损害。对此效应最可能的解释是VPA与LTG在肝脏中竞争葡萄糖醛酸化。分布容积以及与吸收相关的参数、最大血药浓度（Cmax）和达峰时间（tmax）均未改变。
相似文献
1
Sodium valproate acutely inhibits lamotrigine metabolism.丙戊酸钠可急性抑制拉莫三嗪的代谢。
Br J Clin Pharmacol. 1992 May;33(5):511-3. doi: 10.1111/j.1365-2125.1992.tb04079.x.
2
Lamotrigine and valproate pharmacokinetics interactions in epileptic patients.拉莫三嗪与丙戊酸盐在癫痫患者中的药代动力学相互作用。
Eur J Drug Metab Pharmacokinet. 2009 Apr-Jun;34(2):93-9. doi: 10.1007/BF03191157.
3
Time course of reversal of valproate-mediated inhibition of lamotrigine.丙戊酸钠介导的拉莫三嗪抑制作用的逆转时间过程。
Seizure. 2018 Apr;57:76-79. doi: 10.1016/j.seizure.2018.03.003. Epub 2018 Mar 7.
4
Lack of an effect of valproate concentration on lamotrigine pharmacokinetics in developmentally disabled patients with epilepsy.丙戊酸盐浓度对发育性残疾癫痫患者拉莫三嗪药代动力学无影响。
Epilepsy Res. 2000 Nov;42(1):23-31. doi: 10.1016/s0920-1211(00)00160-1.
5
Evaluation of VPA dose and concentration effects on lamotrigine pharmacokinetics: implications for conversion to lamotrigine monotherapy.丙戊酸剂量和浓度对拉莫三嗪药代动力学影响的评估：转换为拉莫三嗪单药治疗的意义
Epilepsy Res. 2003 Dec;57(2-3):85-93. doi: 10.1016/j.eplepsyres.2003.09.008.
6
Neurotoxicity following addition of intravenous valproate to lamotrigine therapy.在拉莫三嗪治疗中添加静脉丙戊酸盐后的神经毒性。
Neurology. 2003 Jun 24;60(12):1991-2. doi: 10.1212/01.wnl.0000065915.68602.91.
7
Effects of various antiepileptic drugs on plasma levels of lamotrigine, a novel antiepileptic, in rats.多种抗癫痫药物对新型抗癫痫药拉莫三嗪大鼠血浆水平的影响。
Pharmacology. 1997 Jun;54(6):319-27. doi: 10.1159/000139502.
8
Effect of comedication on lamotrigine clearance in Korean epilepsy patients.合并用药对韩国癫痫患者拉莫三嗪清除率的影响。
Clin Chim Acta. 2015 Jan 1;438:269-73. doi: 10.1016/j.cca.2014.09.004. Epub 2014 Sep 8.
9
Adding valproate to lamotrigine: a study of their pharmacokinetic interaction.在拉莫三嗪基础上加用丙戊酸盐：二者药代动力学相互作用的研究
Neurology. 2000 Aug 22;55(4):588-91. doi: 10.1212/wnl.55.4.588.
10
Bidirectional interaction of valproate and lamotrigine in healthy subjects.丙戊酸盐与拉莫三嗪在健康受试者中的双向相互作用。
Clin Pharmacol Ther. 1996 Aug;60(2):145-56. doi: 10.1016/S0009-9236(96)90130-7.
引用本文的文献
1
UGT2B10 is the Major UDP-Glucuronosyltransferase 2B Isoform Involved in the Metabolism of Lamotrigine and is Implicated in the Drug-Drug Interaction with Valproic Acid.UGT2B10 是参与拉莫三嗪代谢的主要 UDP-葡萄糖醛酸基转移酶 2B 同工酶，与丙戊酸的药物-药物相互作用有关。
AAPS J. 2024 Sep 25;26(6):107. doi: 10.1208/s12248-024-00978-8.
2
UGT1A4*3 polymorphism influences serum concentration and therapeutic effect of lamotrigine for epilepsy treatment: A meta-analysis.UGT1A4*3 多态性影响拉莫三嗪治疗癫痫的血清浓度和疗效：一项荟萃分析。
PLoS One. 2024 Jul 18;19(7):e0307377. doi: 10.1371/journal.pone.0307377. eCollection 2024.
3
Drug hypersensitivity reactions: review of the state of the science for prediction and diagnosis.药物过敏反应：预测和诊断的科学现状综述。
Toxicol Sci. 2024 Jun 26;200(1):11-30. doi: 10.1093/toxsci/kfae046.
4
Lamotrigine Drug Interactions: Ignorance is not Bliss.拉莫三嗪的药物相互作用：无知并非幸事。
Kans J Med. 2022 Mar 15;15(1):109-111. doi: 10.17161/kjm.vol15.15798. eCollection 2022.
5
Effect of permeation enhancers on in vitro release and transdermal delivery of lamotrigine from EudragitRS100 polymer matrix-type drug in adhesive patches.渗透促进剂对拉莫三嗪从Eudragit RS100聚合物基质型药物贴剂中的体外释放及经皮递送的影响。
Prog Biomater. 2019 Jun;8(2):91-100. doi: 10.1007/s40204-019-0114-9. Epub 2019 May 8.
6
A Physiologically Based Pharmacokinetic Model for Optimally Profiling Lamotrigine Disposition and Drug-Drug Interactions.一种基于生理学的药代动力学模型，用于优化拉莫三嗪处置及药物相互作用的分析。
Eur J Drug Metab Pharmacokinet. 2019 Jun;44(3):389-408. doi: 10.1007/s13318-018-0532-4.
7
Expert Opinion on the Management of Lennox-Gastaut Syndrome: Treatment Algorithms and Practical Considerations.关于伦诺克斯-加斯东综合征管理的专家意见：治疗算法与实际考量
Front Neurol. 2017 Sep 29;8:505. doi: 10.3389/fneur.2017.00505. eCollection 2017.
8
Pharmacokinetics of lamotrigine and its metabolite N-2-glucuronide: Influence of polymorphism of UDP-glucuronosyltransferases and drug transporters.拉莫三嗪及其代谢产物N-2-葡萄糖醛酸苷的药代动力学：尿苷二磷酸葡萄糖醛酸转移酶和药物转运体多态性的影响
Br J Clin Pharmacol. 2016 Aug;82(2):399-411. doi: 10.1111/bcp.12984. Epub 2016 May 29.
9
Antecedent Drug Exposure Aetiology and Management Protocols in Steven-Johnson Syndrome and Toxic Epidermal Necrolysis, A Hospital Based Prospective Study.史蒂文斯-约翰逊综合征和中毒性表皮坏死松解症的既往药物暴露病因及管理方案：一项基于医院的前瞻性研究
J Clin Diagn Res. 2016 Jan;10(1):FC01-4. doi: 10.7860/JCDR/2016/16430.7047. Epub 2016 Jan 1.
10
New genetic findings lead the way to a better understanding of fundamental mechanisms of drug hypersensitivity.新的基因研究结果为更好地理解药物超敏反应的基本机制指明了方向。
J Allergy Clin Immunol. 2015 Aug;136(2):236-44. doi: 10.1016/j.jaci.2015.06.022.
本文引用的文献
1
Mechanism of anticonvulsant action of valproate.丙戊酸盐的抗惊厥作用机制。
Prog Neurobiol. 1982;19(4):315-59. doi: 10.1016/0301-0082(82)90010-7.
2
Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: I. Anticonvulsant profile in mice and rats.新型潜在抗癫痫药物拉莫三嗪的药理学研究：I. 对小鼠和大鼠的抗惊厥作用谱
Epilepsia. 1986 Sep-Oct;27(5):483-9. doi: 10.1111/j.1528-1157.1986.tb03572.x.
3
Acute effects of lamotrigine (BW430C) in persons with epilepsy.
Epilepsia. 1986 May-Jun;27(3):248-54. doi: 10.1111/j.1528-1157.1986.tb03536.x.
4
Lamotrigine, a new anticonvulsant: pharmacokinetics in normal humans.
Clin Pharmacol Ther. 1987 Nov;42(5):535-41. doi: 10.1038/clpt.1987.193.
5
Depletion of hepatic UDP-glucuronic acid by drugs that are glucuronidated.被葡萄糖醛酸化的药物导致肝脏UDP-葡萄糖醛酸的耗竭。
J Pharmacol Exp Ther. 1986 Mar;236(3):610-4.
6
The pharmacokinetics of lamotrigine (BW430C) in healthy subjects with unconjugated hyperbilirubinaemia (Gilbert's syndrome).拉莫三嗪（BW430C）在患有非结合性高胆红素血症（吉尔伯特综合征）的健康受试者中的药代动力学。
Br J Clin Pharmacol. 1989 Jul;28(1):117-20. doi: 10.1111/j.1365-2125.1989.tb03514.x.
7
Double-blind crossover trial of lamotrigine (Lamictal) as add-on therapy in intractable epilepsy.
Epilepsy Res. 1989 Nov-Dec;4(3):222-9. doi: 10.1016/0920-1211(89)90007-7.
8
Alteration of zidovudine pharmacokinetics by probenecid in patients with AIDS or AIDS-related complex.
Clin Pharmacol Ther. 1989 Nov;46(5):494-500. doi: 10.1038/clpt.1989.176.
9
Controlled trial of lamotrigine (Lamictal) for refractory partial seizures.
Epilepsia. 1989 May-Jun;30(3):356-63. doi: 10.1111/j.1528-1157.1989.tb05309.x.
10
A randomised double-blind placebo-controlled add-on trial of lamotrigine in patients with severe epilepsy.
Epilepsy Res. 1990 Aug;6(3):221-6. doi: 10.1016/0920-1211(90)90077-9.
Zotero 插件