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Landiolol hydrochloride is an ultrashort-acting highly selective beta-1 blocker that primarily antagonizes beta1 receptors present in the heart and improves tachycardia by inhibiting catecholamine-induced increased cardiac beats.
Landiolol hydrochloride is used for the emergency treatment of tachycardia arrhythmias (including atrial fibrillation, atrial flutter, sinus tachycardia) during surgery.
| Items | Specifications | Results |
| Appearance | White powder | Conforms |
| Assay | ≥99.0% | 99.31% |
Items | Specifications | Results |
Appearance | White crystalline powder | White crystalline powder |
Identification | IR/UV | Conform |
Chloride identification(1) | The aqueous solution of this product shows the reaction of chloride identification (1) | Conform |
Solubility | This product is easily soluble in water and methanol, easily soluble in N,N-Dimethylformamide, soluble in ethanol, slightly soluble in acetonitrile | Conform |
Melting point | 123.0~127.0℃ | 124.8-125.4℃ |
Specific rotation | -9.0°~-11.0° | -9.75° |
Acidity | 3.5~5.5 | 4.7 |
Related Substances | Impurity LND-iA: NMT0.15% | 0.02% |
Impurity LND-iB: NMT0.1% | N.D. | |
Impurity LND-i0: NMT0.1% | 0.02% | |
Impurity S-DMHP: NMT0.1% | N.D. | |
Impurity LND-iD: NMT0.1% | N.D. | |
Impurity LND-iE: NMT0.1% | N.D. | |
Other single impurities:NMT0.1% | 0.05% | |
Total impurities:NMT1.0% | 0.22% | |
Water | NMT 1.0% | 0.66% |
Residue on ignition | NMT 0.1% | 0.06% |
Residual solvent | Acetonitrile:NMT0.041% | N.D. |
Ethyl acetate:NMT0.5% | N.D. | |
Isopropyl alcohol:NMT0.5% | N.D. | |
Acetone:NMT0.5% | 0.006% | |
Dichloromethane:NMT0.06% | N.D. | |
Bacterial endotoxin microbiological limits | NMT1.0EU/mg | Conforms |
Assay | 98.0%-102.0% | 99.99% |
Conclusion | The product conforms to the above specifications. | |
Landiolol hydrochloride is an ultra-short-acting, cardioselective beta-1 adrenergic receptor blocker (beta-blocker) used primarily in acute clinical settings. It is the hydrochloride salt of landiolol, with the chemical formula C₂₃H₃₅ClN₂O₇S·HCl.
Key Features:
High β₁-selectivity: ~250 times more selective for β₁-receptors (in the heart) than β₂-receptors (in lungs and blood vessels), reducing risks like bronchospasm.
Very short half-life: Approximately 3–4 minutes, allowing rapid onset and quick reversibility—ideal for critically ill or unstable patients.
Main Medical Uses:
Rapid Control of Tachycardia:
Used intravenously to manage excessive heart rate in conditions like:
Atrial fibrillation or flutter with rapid ventricular response
Postoperative tachycardia
Myocardial ischemia or heart failure with elevated heart rate
Perioperative Care:
Administered during or after cardiac and non-cardiac surgeries to stabilize heart rate without significantly lowering blood pressure.
Critical Care Settings:
Preferred in intensive care units (ICUs) due to its titratability and safety in patients with borderline hemodynamics.
Approved in Japan (2002) and the U.S. (2023, under brand name ZENEPAR™), landiolol hydrochloride offers a safer, more controllable alternative to traditional beta-blockers like esmolol—especially in patients at risk of hypotension or bronchospasm.
Clinically used for tachycardia arrhythmias during surgery.
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