Pharmacokinetics and Pharmacodynamics of Low-, Intermediate-, and High-Dose Landiolol and Esmolol During Long-Term Infusion in Healthy Whites
Language English Country United States Media print
Document type Comparative Study, Journal Article, Randomized Controlled Trial
- MeSH
- Adrenergic beta-1 Receptor Antagonists administration & dosage adverse effects pharmacokinetics MeSH
- White People MeSH
- Adrenergic beta-Antagonists administration & dosage adverse effects pharmacokinetics MeSH
- Adult MeSH
- Double-Blind Method MeSH
- Hemodynamics drug effects MeSH
- Infusions, Intravenous MeSH
- Cross-Over Studies MeSH
- Blood Pressure drug effects MeSH
- Middle Aged MeSH
- Humans MeSH
- Adolescent MeSH
- Young Adult MeSH
- Urea administration & dosage adverse effects analogs & derivatives pharmacokinetics MeSH
- Morpholines administration & dosage adverse effects pharmacokinetics MeSH
- Propanolamines administration & dosage adverse effects pharmacokinetics MeSH
- Prospective Studies MeSH
- Drug Administration Schedule MeSH
- Heart Rate drug effects MeSH
- Therapeutic Equivalency MeSH
- Dose-Response Relationship, Drug MeSH
- Healthy Volunteers MeSH
- Check Tag
- Adult MeSH
- Middle Aged MeSH
- Humans MeSH
- Adolescent MeSH
- Young Adult MeSH
- Male MeSH
- Female MeSH
- Publication type
- Journal Article MeSH
- Randomized Controlled Trial MeSH
- Comparative Study MeSH
- Geographicals
- Czech Republic MeSH
- Names of Substances
- Adrenergic beta-1 Receptor Antagonists MeSH
- Adrenergic beta-Antagonists MeSH
- esmolol MeSH Browser
- landiolol MeSH Browser
- Urea MeSH
- Morpholines MeSH
- Propanolamines MeSH
The pharmacokinetics, pharmacodynamics, safety, and tolerability of long-term administration of esmolol and landiolol, a new fast-acting cardioselective β-blocker, were compared for the first time in Caucasian subjects in a prospective clinical trial. Twelve healthy volunteers received landiolol and esmolol by continuous infusion for 24 hours in a randomized crossover study using a dose-escalation regimen. Blood concentrations of drugs and metabolites, heart rate, blood pressure, ECG parameters, and tolerability were observed for 30 hours and compared. Drug blood concentrations and areas under the curve were dose-proportional. The half life of landiolol (4.5 minutes) was significantly shorter than that of esmolol (6.9 minutes). Volume of distribution and total clearance were lower for landiolol. Heart rate reduction was faster and more pronounced with landiolol and retained throughout the administration period; effects on blood pressure were not different. Landiolol turned out to be superior to esmolol with respect to pharmacokinetic and pharmacodynamic profile and local tolerability.
AOP Orphan Pharmaceuticals AG Vienna Austria
APROVA s r o Brno Czech Republic
Center for Pharmacology and Analysis s r o Plzeň Czech Republic
References provided by Crossref.org
Dobutamine Alters the Pharmacokinetic and Pharmacodynamic Behavior of Esmolol
