Landiolol has a less potent negative inotropic effect than esmolol in isolated rabbit hearts

  title={Landiolol has a less potent negative inotropic effect than esmolol in isolated rabbit hearts},
  author={Kazutoshi Ikeshita and Kiyonobu Nishikawa and Sumiko Toriyama and Tomoyuki Yamashita and Yoshiyuki Tani and Tokuhiro Yamada and Akira Asada},
  journal={Journal of Anesthesia},
PurposeWe compared the negative chronotropic and inotropic effects of landiolol and esmolol, two clinically available short-acting β1-blockers with high β1-selectivity, using whole isolated rabbit heart preparations.MethodsTachycardia was induced by continuous perfusion of 10−7 M isoproterenol, and we used concentrations of landiolol or esmolol in ascending steps (1 · 10−6, 3 · 10−6, 1 · 10−5, 3 · 10−5, and 1 · 10−4 M). Heart rate (HR), left ventricular developed pressure (LVDP), the maximal… 

Direct effects of esmolol and landiolol on cardiac function, coronary vasoactivity, and ventricular electrophysiology in guinea-pig hearts.

Esmolol directly inhibits cardiac performance significantly more so than landiolol, an effect revealed to be at least in part mediated by esmolol-induced APD shortening.

Intravenous Amiodarone and Sotalol Impair Contractility and Cardiac Output, but Procainamide Does Not: A Langendorff Study

In isolated hearts, amiodarone and sotalol depressed myocardial contractility, cardiac output, and diastolic function, however, procainamide did not negatively affect myocardials performance and represents a favorable agent in settings of therapeutic equivalence.

Blood Pressure Recovery After Dobutamine Antagonism: Partial With Landiolol, None With Esmolol

Landiolol reduced the dobutamine‐induced heart rate and blood pressure increases better than esmolol, which may explain why landiolol that is devoid of effects on renin and sodium, calcium, and potassium channels behaves different from es Molol with respect to blood pressure recovery.

Landiolol, an Ultra-Short-Acting β1-Blocker, More Effectively Terminates Atrial Fibrillation Than Diltiazem After Open Heart Surgery

Landiolol is more effective and safer than diltiazem for patients with postoperative AF after open heart surgery, and conversion to normal sinus rhythm (NSR) within 8h after onset of AF.

Safety and efficacy of an ultrashort-acting β1-blocker on left ventricular dysfunction.

The occurrence of atrial fibrillation during the intensive care unit stay (during landiolol hydrochloride administration) was significantly lower in the administration group, and the difference remained significant after multiple logistic regression analysis.

Effect of landiolol in patients with tachyarrhythmias and acute decompensated heart failure (ADHF): a case series

A continuous infusion of a low dose of landiolol to manage tachycardia and ventricular or supraventricular tachyarrhythmias in haemodynamically unstable patients may be considered.

Landiolol, an ultra-short-acting β1-blocker, is useful for managing supraventricular tachyarrhythmias in sepsis.

Landiolol safely reduced heart rate and, in part, converted to sinus rhythm in septic patients with supraventricular tachyarrhythmias, and was observed more frequently in the landiolol group than in the control group.

Low-dose β-blocker in combination with milrinone safely improves cardiac function and eliminates pulsus alternans in patients with acute decompensated heart failure.

A low-dose β-blocker in combination with milrinone improved cardiac function in ADHF patients with tachycardia; therefore, it may be considered as an adjunct therapy for use when standard therapy with Milrinone is not effective at slowing HR.

Effects of landiolol hydrochloride on intractable tachyarrhythmia after pediatric cardiac surgery.

Addition of a β1-Blocker to Milrinone Treatment Improves Cardiac Function in Patients with Acute Heart Failure and Rapid Atrial Fibrillation

The addition of landiolol at doses of <3.0 µg/kg/min to milrinone improved cardiac function in decompensated chronic heart failure with rapid atrial fibrillation by selectively reducing HR.



In rabbits, landiolol, a new ultra-short-acting β-blocker, exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol

These results suggest that, in rabbits, landiolol has slightly more potent negative chronotropic action than esmolol with significantly less effects on blood pressure.

The negative inotropic effect of esmolol on isolated cardiac muscle

Apart from being a beta adrenergic blocker esmolol also exerts a direct negative inotropic effect on cardiac muscle due to its inhibition of the calcium current during the action potential.

Esmolol and Left Ventricular Function in the Awake Dog

In the awake dog, moderate to large doses of esmolol impair LV function; the lack of any negative chronotropic effect by es Molol suggests that the negative inotropic effect of es molol in this canine preparation is not by β1 blockade.

Electrophysiologic, cardiohemodynamic and beta-blocking actions of a new ultra-short-acting beta-blocker, ONO-1101, assessed by the in vivo canine model in comparison with esmolol.

The results suggest that the suppressive effects of ONO-1101 on cardiovascular performance are significantly less potent than those of esmolol at equipotent beta-blocking doses.

Esmolol inhibits Na+ current in rat ventricular myocytes.

The results suggest that esmolol inhibits I(Na) through sodium channel in rat ventricular myocytes by mechanisms involving preferential interaction with the inactivated state and acceleration of the development of inactivation directly from resting state.

Pharmacology and Pharmacokinetics of Esmolol

Experiments in the constant‐flow‐perfused isolated canine hindlimb indicate that therapeutic (beta blocking) doses of esmolol lack direct vascular effects and alpha‐adrenergic blocking activity and that therapeutic doses do not interfere with vascoconstrictor effects of peripheral sympathetic nerve stimulation.

Use of an ultra short-acting beta-blocker in patients with acute myocardial ischemia.

Esmolol is a new ultra short-acting (half-life [t1/2] beta 9 min) beta 1-adrenergic-receptor antagonist reported to have no intrinsic sympathomimetic activity and there was no significant change in the pulmonary capillary wedge pressure, respiratory rate, or PR interval during the maintenance phase.

Time course of a new ultrashort-acting beta-adrenoceptor-blocking drug, ONO-1101: comparison with those of esmolol and propranolol by using the canine isolated, blood-perfused heart preparations.

It is clearly demonstrated that ONO-1101 is an ultrashort-acting beta-blocker, but the recovery time is dose dependent, and that the beta-blocking action of ONo- 1101 is almost similar to or slightly more potent than esmolol or propranolol.

Effects of ONO-1101, a novel beta-antagonist, on action potential and membrane currents in cardiac muscle.

The results suggest that ONO-1101 is a potent beta-antagonist whose effects were removed quickly by washout and suggest that this agent may be effective in clinical use.

Myocardial protection: the efficacy of an ultra-short-acting beta-blocker, esmolol, as a cardioplegic agent.

Intermittent Esmolol arrest with global ischemia provided equivalent myocardial protection to intermittent crossclamping with fibrillation, continuous esmolol perfusion, and multidose St Thomas' Hospital solution.