Chemical Property of Landiolol
Edit
Chemical Property:
- Appearance/Colour:White crystalline powder
- Melting Point:125.4oC
- Boiling Point:727.513 °C at 760 mmHg
- Flash Point:393.786 °C
- PSA：127.82000
- Density:1.201 g/cm3
- LogP:1.40470
- XLogP3:0.1
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:9
- Rotatable Bond Count:14
- Exact Mass:509.27371521
- Heavy Atom Count:36
- Complexity:666
- Purity/Quality:
-
99% *data from raw suppliers
LANDIOLOL 95.00% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:CC1(OCC(O1)COC(=O)CCC2=CC=C(C=C2)OCC(CNCCNC(=O)N3CCOCC3)O)C
- Isomeric SMILES:CC1(OC[C@H](O1)COC(=O)CCC2=CC=C(C=C2)OC[C@H](CNCCNC(=O)N3CCOCC3)O)C
- Recent ClinicalTrials:Beta-blockade With Landiolol in Out-of-hospital Cardiac Arrest
- Recent EU Clinical Trials:A prospective, randomized, double- blind, placebo- controlled study to evaluate the efficacy of Landiolol hydrochloride for prevention of atrial fibrillation in patients undergoing cardiac surgery
- Recent NIPH Clinical Trials:General Drug Use-Results Survey of Onoact [ ventricular fibrillation and hemodynamically ventricular tachycardia]
-
Description
Landiolol was launched as iv infusion for the treatment of tachyarrhythmia
during surgery. This structurally related derivative of esmolol can be synthesized in 3 linear
steps from 3-(4-hydroxyphenyl)propionic acid by successive esterification followed by
alkylation of the phenol function with (2S)-glycidyltosylate and opening of the resulting
epoxide by the appropriate amine. Landiolol is an ultra short acting PI-adrenergic blocker
more cardioselective (βI/β2 = 255) than esmolol (βi/β2 = 32). It showed 6-8 times greater
efficiency compared to esmolol in reducing isoproterenol-induced increase in heart rate
and ventricular contraction in anesthetized dogs. In clinical trials, landiolol was effective
against a variety of arrhythmias with efficacy seen in patients with atrial fibrillation,
proxysmal supraventricular tachycardia, ventricular tachycardia and premature complexes.
Landiolol produced a doserelated pharmacokinetic behavior, has a rapid onset of action
(10 min.) and is rapidly hydrolyzed to inactive acidic metabolites by esterases after iv
administration. This results in an ultra-short half-life (approx. 3 min.) and p-blocade,
allowing rapid termination of the drug effect by termination of infusion if side effects occur.
Hypertension was the most frequent adverse event and resolved in less than 30 min. after
drug withdrawal.
