Pharmacokinetics of verapamil: Experience with a sustained intravenous infusion regimen☆

作者: Michael J. Reiter , David G. Shand , Linda M. Aanonsen , Robert Wagoner , Elizabeth Mccarthy

DOI: 10.1016/0002-9149(82)91224-3

关键词: Intravenous doseHeart rateBolus (medicine)TachycardiaAnesthesiaRegimenBlood pressureMedicinePharmacokineticsVerapamil

摘要: Disappearance kinetic characteristics of verapamil were determined in 9 patients after a single intravenous dose. From the pharmacokinetic variables determined, we designed an regimen to maintain plasma concentration 150 ng/ml consisting (1) loading bolus (10 mg over 2 minutes), followed by (2) rapid infusion (0.375 mg/min) for 30 minutes, and finally (3) maintenance (0.125 mg/min). We tested this 7 12 hours, found it be safe produce stable prolongation P-R interval. Verapamil was highest immediately administration prevented from falling below 67 infusion. Maintenance remained between 77 156 all patients, averaged 122 ng/ml. Transient slight decreases brachial blood pressure sinus cycle length occurred coincident with maximum concentration. Maximum lagged behind peak but sustained duration Prolongation interval not significantly different at end that 90 minutes start regimen. No patient demonstrated significant side effects, arrhythmia, or clinically important hypotension. Although specified produced final averaging 125 ng/ml, is predicted regimens producing other concentrations can similarly devised changing bolus, infusion, doses proportion desired

参考文章(26)
G Remberg, M Ende, M Schomerus, H J Dengler, M Eichelbaum, The metabolism of DL-[14C]verapamil in man. Drug Metabolism and Disposition. ,vol. 7, pp. 145- 148 ,(1979)
R G McAllister, D W Bourne, L W Dittert, The pharmacology of verapamil. I. Elimination kinetics in dogs and correlation of plasma levels with effect on the eletrocardiogram. Journal of Pharmacology and Experimental Therapeutics. ,vol. 202, pp. 38- 44 ,(1977)
Jerome A. Dominic, David W. A. Bourne, Tiong G. Tan, Edward B. Kirsten, R. G. McAllister, The pharmacology of verapamil. III. Pharmacokinetics in normal subjects after intravenous drug administration. Journal of Cardiovascular Pharmacology. ,vol. 3, pp. 25- 38 ,(1981) , 10.1097/00005344-198101000-00003
Deborah L. Keefe, Sandra R. Harapat, Robert E. Kates, Relationship between pharmacodynamics and myocardial concentration of verapamil American Journal of Cardiology. ,vol. 47, pp. 406- ,(1981) , 10.1016/0002-9149(81)90697-4
L. Schamroth, D. M. Krikler, C. Garrett, Immediate Effects of Intravenous Verapamil in Cardiac Arrhythmias BMJ. ,vol. 1, pp. 660- 662 ,(1972) , 10.1136/BMJ.1.5801.660
RUEY J. SUNG, Intravenous Verapamil for Termination of Re-Entrant Supraventricular Tachycardias Annals of Internal Medicine. ,vol. 93, pp. 682- 689 ,(1980) , 10.7326/0003-4819-93-5-682
Ming K. Heng, Bramah N. Singh, Anthony H.G. Roche, Robin M. Norris, Christopher J. Mercer, Effects of intravenous verapamil on cardiac arrhythmias and on the electrocardiogram. American Heart Journal. ,vol. 90, pp. 487- 498 ,(1975) , 10.1016/0002-8703(75)90431-7
Christopher Y.C. Chew, Harvey S. Hecht, John T. Collett, Russell G. Mcallister, Bramah N. singh, Influence of severity of ventricular dysfunction on hemodynamic responses to intravenously administered verapamil in ischemic heart disease The American Journal of Cardiology. ,vol. 47, pp. 917- 922 ,(1981) , 10.1016/0002-9149(81)90194-6
R L Rinkenberger, E N Prystowsky, J J Heger, P J Troup, W M Jackman, D P Zipes, Effects of intravenous and chronic oral verapamil administration in patients with supraventricular tachyarrhythmias. Circulation. ,vol. 62, pp. 996- 1010 ,(1980) , 10.1161/01.CIR.62.5.996