Drug Metabolism and Pharmacokinetics
Online ISSN : 1880-0920
Print ISSN : 1347-4367
ISSN-L : 1347-4367
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Pharmacokinetics and Pharmacodynamics of Landiolol Hydrochloride, an Ultra Short-acting β1-Selective Blocker, in a Dose Escalation Regimen in Healthy Male Volunteers
Makoto MURAKAMIHidetoshi FURUIEKyoko MATSUGUMAAtsuko WANIBUCHIShinichi KIKAWAShin IRIE
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2005 年 20 巻 5 号 p. 337-344

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  Objectives: We conducted a randomized, double-blind, placebo-controlled study to evaluate the pharmacokinetics and pharmacodynamics of landiolol hydrochloride in a dose escalation regimen in healthy male volunteers.
   Methods: We set two-dose escalation regimen (LM and MH groups) using three different doses [L (low): 0.03 mg/kg/min (1 min) loading→0.01 mg/kg/min (10 min) continuous, M (medium): 0.06 mg/kg/min (1 min) loading→0.02 mg/kg/min (10 min) continuous, H (high): 0.125 mg/kg/min (1 min) loading→0.04 mg/kg/min (10 min) continuous]. Sixteen subjects were allocated randomly to the LM, MH, and placebo groups (n=6, 6, and 4, respectively).
   Results: In both the LM and MH groups, the blood concentration of landiolol hydrochloride changed within a constant range from 2 minutes after initiation of administration to just before the higher dose escalation. By 2 minutes following the higher dose escalation, the concentration of landiolol hydrochloride reached Cmax, and reached almost steady state levels until 6 minutes following administration of the higher dose. The t1/2 of landiolol hydrochloride was 3.5 minutes. The heart rates and blood pressures of subjects administered landiolol hydrochloride decreased, but there were no adverse events in any subject.
   Conclusions: The concentration of landiolol hydrochloride rapidly reached steady state levels, and rapidly dissipated after completion of administration.
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© 2005 by The Japanese Society for the Study of Xenobiotics
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