Kinetics of esmolol, an ultra-short-acting beta blocker, and of its major metabolite

Sum, Check Y.; Yacobi, Avraham; Kartzinel, Ronald; Stampfli, Herman F.; Davis, Charles S.; Lai, Chii‐Ming

doi:10.1038/clpt.1983.193

Cited by 199 publications

(91 citation statements)

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“…The high clearance value for flestolol (154-260 ml mifn1 kg-) obtained in this study, relative to the estimates of liver blood flow in man, indicates that hepatic clearance contributes very little to thp systemic clearance of flestolol. Similar high ciearance value was reported for another short-acting ,B-adrenoceptor blocker (Sum et al, 1983).…”

Section: Discussionsupporting

confidence: 67%

Pharmacokinetics of flestolol in man: preliminary data.

Achari¹,

Hulse²,

Drissel³

et al. 1985

Brit J Clinical Pharma

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The steady state pharmacokinetics of flestolol, a short acting 3-adrenoceptor blocking agent, were studied in six healthy subjects following intravenous infusion of six different doses; 18, 24, 35, 50, 75 and 100 ,ug kg-1 min-', for 60 min. Steady state blood levels increased linearly with dose for all six subjects. The overall mean half-life was 6.5 min. The total body clearance averaged 208 ml min'l kg-' indicating significant extrahepatic metabolism of the drug. There were no significant changes in the half-lives or the total body clearances after the six doses, suggesting that the kinetics of flestolol are linear over the dose range studied.

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Section: Discussionsupporting

confidence: 67%

Pharmacokinetics of flestolol in man: preliminary data.

Achari¹,

Hulse²,

Drissel³

et al. 1985

Brit J Clinical Pharma

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“…15) Amiodarone is available not only for rhythm control but also rate control, 16) whereas the half-life period is very long and it is difficult to adjust its dose within an appropriate range. Another intravenous β blocker, esmolol, also has high β1 selectivity and a short half-life period, 17,18) and its strong negative inotropic effect sometimes results in severe hypotension. 19) Because patients with severe hypotension (systolic blood pressure < 90 mmHg) were excluded in the J-land study, 5) there is little evidence about its use in patients like the present case.…”

Section: Discussionmentioning

confidence: 99%

An Experience of Landiolol Use for an Advanced Heart Failure Patient With Severe Hypotension

et al. 2015

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SummaryTachyarrhythmias such as atrial fibrillation (AF) or atrial flutter (AFL) sometimes invoke life-threatening collapse of hemodynamics in patients with severe heart failure. Recently, landiolol, an ultra-short acting β1-selective antagonist, has been reported to be safe and useful for the treatment of supraventricular tachyarrhythmias with reduced left ventricular function. Here we report a case of advanced heart failure with severe hypotension who was treated successfully by landiolol for rapid AF. The patient was a 20-year old male with dilated cardiomyopathy. He presented with low output syndrome in spite of optimal medical therapy and was referred to our department to consider ventricular assist device implantation and heart transplantation. Soon after admission, he developed rapid atrial fibrillation at 180 beats per minute (bpm) followed by severe hypotension and liver enzyme elevation. Low dose landiolol at 2 μg/kg/minute was started because digoxin was not effective. After landiolol administration, his heart rate decreased to 110 bpm, and finally returned to sinus rhythm without hemodynamic deterioration. Intra-aortic balloon pumping was inserted soon after sinus recovery and he was discharged successfully with an implantable left ventricular assist device. (Int Heart J 2015; 56: 564-567) Key words: Atrial fibrillation, Stage D heart failure, Negative chronotropic effect, Ventricular assist device I t is well known that β blocker treatment is crucial for the improvement of prognosis among patients with systolic heart failure. 1-3) However, the usage of β blockers during the acute phase of decompensated heart failure is still a matter of debate. Propranolol, a classic intravenous form of β blocker, has been used widely for perioperative arrhythmias. However, there are concerns about bronchospasm due to the non-selectivity of β adrenergic receptors. Their long half-life period may also result in the prolongation of adverse events if they occur.Landiolol was developed in Japan and introduced as an ultra-short acting intravenous β blocker. It has very high selectivity for β1 receptors and is rapidly degraded by carboxylesterase and cholinesterase in the liver and blood, respectively. Recently, many papers have reported on the benefits of landiolol for the control of perioperative tachyarrhythmias. 4) However, the indication of landiolol has been limited in patients with preserved ejection fraction, and only digoxin is indicated to control heart rate in patients with severe left ventricular (LV) dysfunction.The J-Land study (Japanese landiolol versus digoxin study) demonstrated that landiolol achieved faster control of heart rate among AF/AFL patients with LV dysfunction compared with digoxin. 5,6) The safety profiles were comparable between the two drugs. In the J-Land study, however, patients with severe LV dysfunction (ejection fraction: EF < 25%) or severe hypotension (systolic blood pressure < 90 mmHg) were excluded and there has been limited experience of landiolol among such patients. We here r...

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“…[19] Esmolol may block beta adrenoreceptors within the brainstem and decrease the neuronal inflow into central nervous system. [24] The dose of esmolol was chosen arbitrarily, depending on a pilot study which shows that such a low dose used in our study may be effective to attenuate propofol injection related pain. There is a dose dependent risk of hypotension and bradycardia, when esmolol is combined with anesthetics such as propofol and fentanyl.…”

Section: Discussionmentioning

confidence: 99%

Pretreatment with a very low dose of intravenous esmolol reduces propofol injection pain.

E¹,

Titiz²,

Akpek³

et al. 2013

Agri

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SummaryObjectives: Propofol causes considerable pain upon injection, although different methods and propofol formulations have been used to decrease this pain. We aimed to investigate the effect of i.v. esmolol pretreatment on propofol injection pain.Methods: Ninety ASA I-II patients undergoing elective surgery under general anesthesia were randomly assigned into three groups of thirty each. A 20 G cannula was inserted into the dorsum of the nondependent hand. After venous occlusion for one minute, groups E, L and S were pretreated with 5 mg/ml (total 2 ml) esmolol, 40 mg lidocaine and 2 ml saline i.v. respectively. After release of venous occlusion, one fourth of the total propofol dose was administered at a rate of 0.5 ml/sec. During the injection of both pretreatment solution and propofol, patient pain was assessed by using 4 point scale. Heart rate and noninvasive arterial blood pressure values were recorded before induction, just after entubation and five minutes after entubation. Results:Demographic values were similar among groups. Incidence of pain on injection of propofol in the control, esmolol and lidocaine groups was 90%, 33.3%, 50% respectively (p<0.05). Heart rate, systolic arterial pressure, and diastolic arterial pressure values were not different between the groups.Conclusion: Pretreatment with low dose esmolol i.v. seems to be effective in attenuating pain during propofol injection.

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Kinetics of esmolol, an ultra-short-acting beta blocker, and of its major metabolite

Cited by 199 publications

References 0 publications

Pharmacokinetics of flestolol in man: preliminary data.

Pharmacokinetics of flestolol in man: preliminary data.

An Experience of Landiolol Use for an Advanced Heart Failure Patient With Severe Hypotension

Pretreatment with a very low dose of intravenous esmolol reduces propofol injection pain.

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