健康志愿者舌下和口服维拉帕米后的药代动力学和药效学
Pharmacokinetics and pharmacodynamics of verapamil following sublingual and oral administration to healthy volunteers.
作者信息
John D N, Fort S, Lewis M J, Luscombe D K
机构信息
Medicines Research Unit, Welsh School of Pharmacy, University of Wales, Cardiff.
出版信息
Br J Clin Pharmacol. 1992 Jun;33(6):623-7. doi: 10.1111/j.1365-2125.1992.tb04091.x.
Abstract
- The pharmacokinetics and pharmacodynamics of verapamil administered via the oral and sublingual routes were compared in a randomised, two-way cross-over study involving six healthy male volunteers. 2. Administered sublingually, a verapamil 40 mg (Securon) crushed tablet produced a significantly higher peak plasma concentration (P less than 0.05), a greater rate of absorption (P less than 0.05), and greater bioavailability (P less than 0.05) when compared with orally administered verapamil 40 mg (Securon). 3. In comparison with oral dosing, PR intervals were significantly (P less than 0.05) prolonged between 30 and 90 min after sublingual verapamil dosing. 4. Correlations between log plasma verapamil concentration and percentage increase in PR interval were greater after sublingual compared with oral dosing in all volunteers.
摘要
- 在一项涉及六名健康男性志愿者的随机双向交叉研究中，比较了口服和舌下给药维拉帕米的药代动力学和药效学。2. 与口服40毫克维拉帕米（Securon）相比，舌下含服一片碾碎的40毫克维拉帕米（Securon）片剂产生的血浆峰浓度显著更高（P小于0.05），吸收速率更快（P小于0.05），生物利用度更高（P小于0.05）。3. 与口服给药相比，舌下给予维拉帕米后30至90分钟，PR间期显著延长（P小于0.05）。4. 在所有志愿者中，舌下给药后血浆维拉帕米浓度对数与PR间期增加百分比之间的相关性大于口服给药。
相似文献
1
Pharmacokinetics and pharmacodynamics of verapamil following sublingual and oral administration to healthy volunteers.健康志愿者舌下和口服维拉帕米后的药代动力学和药效学
Br J Clin Pharmacol. 1992 Jun;33(6):623-7. doi: 10.1111/j.1365-2125.1992.tb04091.x.
2
[Pharmacokinetics and pharmacodynamics of verapamil in healthy volunteers after single oral and sublingual administration].[单次口服和舌下给药后维拉帕米在健康志愿者体内的药代动力学和药效学]
Arzneimittelforschung. 1982;32(12):1567-71.
3
4
Pharmacokinetics and pharmacodynamics of two formulations of verapamil.维拉帕米两种制剂的药代动力学和药效学
Br J Clin Pharmacol. 1987 Nov;24(5):661-4. doi: 10.1111/j.1365-2125.1987.tb03226.x.
5
Verapamil disposition and effect on PQ-intervals after buccal, oral and intravenous administration.维拉帕米经颊、口服和静脉给药后的处置及其对PQ间期的影响。
Arzneimittelforschung. 1984;34(4):498-502.
6
Chronopharmacology of intravenous and oral modified release verapamil.静脉注射和口服缓释维拉帕米的时辰药理学
Br J Clin Pharmacol. 1999 Apr;47(4):413-9. doi: 10.1046/j.1365-2125.1999.00910.x.
7
A rabbit model for sublingual drug delivery: comparison with human pharmacokinetic studies of propranolol, verapamil and captopril.舌下给药的兔模型：与普萘洛尔、维拉帕米和卡托普利人体药代动力学研究的比较
J Pharm Sci. 2006 Jan;95(1):37-44. doi: 10.1002/jps.20312.
8
Pharmacodynamics of acute intranasal administration of verapamil: comparison with i.v. and oral administration.维拉帕米急性鼻内给药的药效学：与静脉注射和口服给药的比较。
Biopharm Drug Dispos. 1985 Oct-Dec;6(4):447-54. doi: 10.1002/bdd.2510060411.
9
Lormetazepam--plasma concentrations in volunteers following sublingual and oral dosing.氯美扎酮——志愿者舌下给药和口服给药后的血浆浓度
Psychopharmacology Suppl. 1984;1:99-104.
10
R-verapamil: pharmacokinetics and effects on PR interval, blood pressure and heart rate.R-维拉帕米：药代动力学及其对PR间期、血压和心率的影响
Br J Clin Pharmacol. 1993 Aug;36(2):93-8. doi: 10.1111/j.1365-2125.1993.tb04202.x.
引用本文的文献
1
Verapamil Improves the Activity of Bedaquiline against Mycobacterium abscessus In Vitro and in Macrophages.维拉帕米可提高贝达喹啉对脓肿分枝杆菌的体外和巨噬细胞内活性。
Antimicrob Agents Chemother. 2019 Aug 23;63(9). doi: 10.1128/AAC.00705-19. Print 2019 Sep.
2
Improved Predictions of Drug-Drug Interactions Mediated by Time-Dependent Inhibition of CYP3A.时间依赖性抑制 CYP3A 介导的药物相互作用的预测能力得到改善。
Mol Pharm. 2018 May 7;15(5):1979-1995. doi: 10.1021/acs.molpharmaceut.8b00129. Epub 2018 Apr 10.
3
Acceleration of tuberculosis treatment by adjunctive therapy with verapamil as an efflux inhibitor.维拉帕米作为外排抑制剂辅助治疗加速结核病治疗。
Am J Respir Crit Care Med. 2013 Sep 1;188(5):600-7. doi: 10.1164/rccm.201304-0650OC.
4
Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic applications.口腔黏膜给药：临床药代动力学与治疗应用。
Clin Pharmacokinet. 2002;41(9):661-80. doi: 10.2165/00003088-200241090-00003.
5
Verapamil: a review of its pharmacological properties and therapeutic use in coronary artery disease.维拉帕米：其药理特性及在冠状动脉疾病中的治疗应用综述
Drugs. 1996 May;51(5):792-819. doi: 10.2165/00003495-199651050-00007.
6
Preliminary investigation of the efficacy of sublingual verapamil in the management of acute atrial fibrillation and flutter.舌下含服维拉帕米治疗急性房颤和房扑疗效的初步研究。
Br J Clin Pharmacol. 1994 May;37(5):460-3. doi: 10.1111/j.1365-2125.1994.tb05715.x.
本文引用的文献
1
Effects of intravenous and chronic oral verapamil administration in patients with supraventricular tachyarrhythmias.静脉注射和长期口服维拉帕米对室上性快速心律失常患者的影响。
Circulation. 1980 Nov;62(5):996-1010. doi: 10.1161/01.cir.62.5.996.
2
Intravenous verapamil for termination of re-entrant supraventricular tachycardias: intracardiac studies correlated with plasma verapamil concentrations.静脉注射维拉帕米终止折返性室上性心动过速：心内研究与血浆维拉帕米浓度的相关性
Ann Intern Med. 1980 Nov;93(5):682-9. doi: 10.7326/0003-4819-93-5-682.
3
Comparison of intravenous and oral verapamil dosing.
Clin Pharmacol Ther. 1982 Dec;32(6):711-20. doi: 10.1038/clpt.1982.227.
4
The pharmacology of verapamil. IV. Kinetic and dynamic effects after single intravenous and oral doses.
Clin Pharmacol Ther. 1982 Apr;31(4):418-26. doi: 10.1038/clpt.1982.54.
5
Clinical use of oral verapamil in chronic and paroxysmal atrial fibrillation.口服维拉帕米在慢性和阵发性心房颤动中的临床应用。
Chest. 1982 Mar;81(3):308-11. doi: 10.1378/chest.81.3.308.
6
7
[Pharmacokinetics and pharmacodynamics of verapamil in healthy volunteers after single oral and sublingual administration].[单次口服和舌下给药后维拉帕米在健康志愿者体内的药代动力学和药效学]
Arzneimittelforschung. 1982;32(12):1567-71.
8
Pharmacokinetics of (+)-, (-)- and (+/-)-verapamil after intravenous administration.静脉注射后（+）-、（-）-和（±）-维拉帕米的药代动力学
Br J Clin Pharmacol. 1984 Apr;17(4):453-8. doi: 10.1111/j.1365-2125.1984.tb02371.x.
9
Inter- and intra-subject variation in the first-pass elimination of highly cleared drugs during chronic dosing. Studies with deuterated verapamil.慢性给药期间高清除率药物首过消除的个体间和个体内差异。氘代维拉帕米的研究。
Eur J Clin Pharmacol. 1984;26(1):47-53. doi: 10.1007/BF00546708.
10
Verapamil disposition and effect on PQ-intervals after buccal, oral and intravenous administration.维拉帕米经颊、口服和静脉给药后的处置及其对PQ间期的影响。
Arzneimittelforschung. 1984;34(4):498-502.
Zotero 插件