依巴斯汀在健康受试者中的药代动力学、抗组胺作用及浓度-效应关系。
The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
作者信息
Vincent J, Liminana R, Meredith P A, Reid J L
机构信息
University Department of Materia Medica, Stobhill General Hospital, Glasgow.
出版信息
Br J Clin Pharmacol. 1988 Nov;26(5):497-502. doi: 10.1111/j.1365-2125.1988.tb05288.x.
Abstract
- The kinetics and effects of ebastine 10 and 50 mg were studied after oral dosing in healthy subjects. 2. The parent drug was extensively metabolised during the first pass to its carboxylic acid derivative, carebastine. 3. The pharmacokinetics of carebastine were linear over the dose range studied and the terminal elimination half-life was 10.6 +/- 2.6 and 12.5 +/- 1.9 h respectively after 10 and 50 mg of ebastine. 4. Antihistamine (H1-receptor) activity was examined with intradermal histamine (2 micrograms). Oral ebastine reduced the histamine wheal area for up to 24 h and also reduced subjective local pain. 5. Antihistamine activity correlated well with plasma levels of carebastine in individual subjects. 6. Ebastine appears to have potential as an antihistamine for once a day dosing.
摘要
- 在健康受试者中口服给药后，研究了10毫克和50毫克依巴斯汀的动力学和效应。2. 母体药物在首过代谢过程中广泛代谢为其羧酸衍生物卡瑞巴斯汀。3. 在研究的剂量范围内，卡瑞巴斯汀的药代动力学呈线性，服用10毫克和50毫克依巴斯汀后，终末消除半衰期分别为10.6±2.6小时和12.5±1.9小时。4. 用皮内注射组胺（2微克）检测抗组胺（H1受体）活性。口服依巴斯汀可使组胺风团面积减少长达24小时，还可减轻局部主观疼痛。5. 在个体受试者中，抗组胺活性与卡瑞巴斯汀的血浆水平密切相关。6. 依巴斯汀似乎有潜力作为一种每日一次给药的抗组胺药。
相似文献
1
The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.依巴斯汀在健康受试者中的药代动力学、抗组胺作用及浓度-效应关系。
Br J Clin Pharmacol. 1988 Nov;26(5):497-502. doi: 10.1111/j.1365-2125.1988.tb05288.x.
2
Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.伊曲康唑和利福平显著改变依巴斯汀及其代谢物在健康参与者体内的处置和抗组胺作用。
J Clin Pharmacol. 2010 Feb;50(2):195-204. doi: 10.1177/0091270009348974. Epub 2009 Oct 19.
3
Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects.H1受体拮抗剂依巴斯汀及其活性代谢产物卡瑞斯汀在健康受试者体内的药代动力学。
Arzneimittelforschung. 1994 Jan;44(1):59-64.
4
Effect of age and gender on the pharmacokinetics of ebastine after single and repeated dosing in healthy subjects.年龄和性别对健康受试者单次及重复给药后依巴斯汀药代动力学的影响。
Int J Clin Pharmacol Ther. 2001 Mar;39(3):126-34. doi: 10.5414/cpp39126.
5
Pharmacokinetics and pharmacodynamics of ebastine in children.依巴斯汀在儿童中的药代动力学和药效学
J Pediatr. 1993 Apr;122(4):641-6. doi: 10.1016/s0022-3476(05)83555-3.
6
7
Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.与健康志愿者相比，依巴斯汀在肝功能受损患者中的药代动力学及安全性：一项I期开放标签研究。
Clin Pharmacokinet. 2004;43(2):121-9. doi: 10.2165/00003088-200443020-00004.
8
Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.依巴斯汀在健康受试者和肾功能不全患者中的药代动力学及安全性。
Clin Pharmacokinet. 2007;46(6):525-34. doi: 10.2165/00003088-200746060-00006.
9
Pharmacokinetics and electrocardiographic effect of ebastine in young versus elderly healthy subjects.依巴斯汀在年轻与老年健康受试者中的药代动力学及心电图效应
Am J Ther. 1998 May;5(3):153-8. doi: 10.1097/00045391-199805000-00005.
10
Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats.大鼠单次给药后[14C]依巴斯汀的吸收、分布、代谢和排泄
Arzneimittelforschung. 1994 Apr;44(4):527-38.
引用本文的文献
1
Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation.细胞外信号调节激酶介导依巴斯汀诱导的人毛囊真皮乳头细胞增殖。
Biomed Res Int. 2019 Feb 11;2019:6360503. doi: 10.1155/2019/6360503. eCollection 2019.
2
Comparative Efficacy and Safety of Ebastine 20 mg, Ebastine 10 mg and Levocetirizine 5 mg in Acute Urticaria.依巴斯汀20毫克、依巴斯汀10毫克和左西替利嗪5毫克治疗急性荨麻疹的疗效与安全性比较
J Clin Diagn Res. 2017 Mar;11(3):WC06-WC09. doi: 10.7860/JCDR/2017/23961.9550. Epub 2017 Mar 1.
3
Clinical utility and patient adherence with ebastine for allergic rhinitis.依巴斯汀治疗变应性鼻炎的临床效用及患者依从性
Patient Prefer Adherence. 2010 Oct 14;4:389-95. doi: 10.2147/PPA.S8186.
4
A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults.10毫克依巴斯汀速溶片与口服地氯雷他定及安慰剂在抑制健康成年人组胺引起的皮肤反应方面的比较。
Clin Drug Investig. 2007;27(7):453-61. doi: 10.2165/00044011-200727070-00002.
5
Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.依巴斯汀在健康受试者和肾功能不全患者中的药代动力学及安全性。
Clin Pharmacokinet. 2007;46(6):525-34. doi: 10.2165/00003088-200746060-00006.
6
Small molecular drug transfer across the blood-brain barrier via carrier-mediated transport systems.小分子药物通过载体介导的转运系统穿过血脑屏障。
NeuroRx. 2005 Jan;2(1):54-62. doi: 10.1602/neurorx.2.1.54.
7
Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.与健康志愿者相比，依巴斯汀在肝功能受损患者中的药代动力学及安全性：一项I期开放标签研究。
Clin Pharmacokinet. 2004;43(2):121-9. doi: 10.2165/00003088-200443020-00004.
8
Differential cognitive effects of ebastine and (+)-chlorpheniramine in healthy subjects: correlation between cognitive impairment and plasma drug concentration.依巴斯汀和（+）-氯苯那敏对健康受试者认知功能的差异影响：认知障碍与血浆药物浓度之间的相关性。
Br J Clin Pharmacol. 2002 Mar;53(3):296-304. doi: 10.1046/j.0306-5251.2001.01183.x.
9
Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine.通过正电子发射断层扫描（PET）对人脑组胺H1受体占有率进行神经成像：第二代抗组胺药依巴斯汀与经典抗组胺药（+）-氯苯那敏的比较研究。
Br J Clin Pharmacol. 2001 Nov;52(5):501-9. doi: 10.1046/j.1365-2125.2001.01471.x.
10
Ebastine: an update of its use in allergic disorders.依巴斯汀：其在过敏性疾病中应用的最新进展
Drugs. 2000 Apr;59(4):981-1006. doi: 10.2165/00003495-200059040-00018.
本文引用的文献
1
The quantitative comparison of histamine antagonists in man.人体内组胺拮抗剂的定量比较。
Proc R Soc Med. 1949 Aug;42(8):615-23. doi: 10.1177/003591574904200818.
2
CIRCADIAN REACTIVITY RHYTHMS OF HUMAN SKIN TO HISTAMINE OR ALLERGEN AND THE ADRENAL CYCLE.人体皮肤对组胺或变应原的昼夜反应节律与肾上腺周期
J Allergy. 1965 May-Jun;36:273-83. doi: 10.1016/0021-8707(65)90086-9.
3
Influence of liver disease and environmental factors on hepatic monooxygenase activity in vitro.肝脏疾病和环境因素对体外肝单加氧酶活性的影响。
Eur J Clin Pharmacol. 1981;20(1):39-46. doi: 10.1007/BF00554665.
4
Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy.阿司咪唑。对其药效学特性和治疗效果的综述。
Drugs. 1984 Jul;28(1):38-61. doi: 10.2165/00003495-198428010-00003.
5
The effects of astemizole on histamine-induced weal and flare.阿司咪唑对组胺诱导的风团和潮红的影响。
Eur J Clin Pharmacol. 1983;25(4):547-51. doi: 10.1007/BF00542126.
6
Sedation and antihistaminics.
Arzneimittelforschung. 1982;32(9a):1193-5.
7
Performance studies with the H1-histamine receptor antagonists, astemizole and terfenadine.使用H1组胺受体拮抗剂阿司咪唑和特非那定的性能研究。
Br J Clin Pharmacol. 1982 Feb;13(2):199-202. doi: 10.1111/j.1365-2125.1982.tb01356.x.
8
Relationship between antihistamic activity and plasma level of diphenhydramine.
Eur J Clin Pharmacol. 1974 Aug 23;7(5):393-5. doi: 10.1007/BF00558213.
9
Ebastine: the effect of a new antihistamine on psychomotor performance and autonomic responses in healthy subjects.依巴斯汀：一种新型抗组胺药对健康受试者精神运动表现和自主神经反应的影响。
Br J Clin Pharmacol. 1988 Nov;26(5):503-8. doi: 10.1111/j.1365-2125.1988.tb05289.x.
10
Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines).H1受体拮抗剂（抗组胺药）的临床药代动力学
Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97. doi: 10.2165/00003088-198510060-00002.
Zotero 插件