Search

Background: Ventricular tachycardia storm is a syndrome defined by the presence of at least three episodes of ventricular tachycardia over a 24-h period, requiring termination by intervention. Standard therapy consists initially of using intravenous betablockers (if left ventricular ejection fraction is preserved) and Amiodarone, in addition to intravenous Lidocaine (in case of ischemic etiology) and light sedation. In the present case, a ventricular tachycardia storm episode is terminated by Esmolol, a particular intravenous betablocker, despite acute decompensated heart failure. Case presentation: We report the case of an 89-year-old patient presenting for a ventricular tachycardia storm and acute heart failure with reduced left ventricle ejection fraction of coronary ischemic origin that persisted despite coronary revascularization, oral betablocker, intravenous Amiodarone and Lidocaine, light sedation, and multiple electrical cardioversion. Emergency catheter ablation was not feasible due to meteorological conditions. We decided to use an intravenous betablocker despite the presence of acute heart failure. We favored use of intravenous Esmolol over other intravenous betablockers due to its short half-life and thus his rapid elimination, a unique characteristic for Esmolol. Intravenous Esmolol has successfully terminated the ventricular tachycardia without causing cardiogenic shock. Conclusions: Intravenous Esmolol can be used safely in patients with acute decompensated heart failure to terminate an electrical storm after failure of other measures. Close monitoring of the patient remains essential. [ABSTRACT FROM AUTHOR]

Background: Disorders of the gut microbiome could be responsible for the progression of multiple organ dysfunction syndrome. In this study, we examined the effect of esmolol on the gut microbiome in a rat model of sepsis induced by cecal ligation and puncture (CLP). Methods: The animals (n = 32) were randomly divided into 3 groups: Sham group (sham operation + normal saline treatment, n = 8), CLP group (cecal ligation and puncture + normal saline treatment, n = 12), and CLP + ESM group (cecal ligation and puncture + esmolol treatment, n = 12). After 24 h, feces in the colon were collected for 16S rRNA gene sequencing and nitric oxide analysis. In addition, colon was removed for immunohistochemical staining of inducible nitric oxide synthase (iNOS). Results: Four rats in the CLP group and two rats in the CLP + ESM group died. The abundance of Lactobacillus in the CLP + ESM group was higher than CLP group (P = 0.048). In the linear discriminant analysis effect size analysis, Norank f Muribaculaceae, Escherichia–Shigella and Lactobacillus were the predominant bacteria in the Sham group, CLP group and CLP + ESM group, respectively. The iNOS expression in colonocytes stained by brown in the CLP group were much more than Sham group (P = 0.001). Compared to CLP group, the iNOS expression in colonocytes reduced after esmolol treatment (P = 0.013). The concentration of nitric oxide in colon feces was different in Sham group, CLP group and CLP + ESM group (1.31 ± 0.15μmmol/l vs. 1.98 ± 0.27μmmol/l vs. 1.51 ± 0.14μmmol/l, P = 0.001). In addition, the concentration of nitric oxide in CLP group was higher than Sham group (P = 0.001) or CLP + ESM group (P = 0.001). Conclusions: Esmolol increased the fecal abundance of Lactobacillus in a rat model of sepsis. Moreover, esmolol reduced the iNOS expression of colonocytes and the nitric oxide concentration of colon feces. [ABSTRACT FROM AUTHOR]

Objective: D-Transposition of the great arteries (d-TGA) is the most common congenital heart disease requiring surgical correction within the neonatal period. Sinus tachycardia often persists postoperatively, potentially affecting cardiac function. This study aimed to investigate the efficacy and safety of the short-acting beta-1-selective beta-blocker esmolol in controlling heart rate in neonatal cardiac surgery with cardiopulmonary bypass (CPB).A retrospective cohort study was conducted on neonates undergoing surgery for d-TGA. The study cohort included 112 patients, divided into an esmolol intervention group (n = 57) and a control group (n = 55). Baseline characteristics, hemodynamic parameters and outcome measures were assessed.In the esmolol group, median heart rate at ICU admission was significantly higher compared to the control group (155 vs. 147 bpm, p = 0.018). After a median time of 11 h, heart rate was lower among the esmolol patients (135 vs. 144 bpm, p < 0.001). There were no differences in other hemodynamic parameters between the two groups. Patients treated with esmolol required longer catecholamine support while no difference regarding survival, duration of invasive ventilation and ICU stay were noticed.No relevant hemodynamic difference was seen between neonates treated with perioperative esmolol and the control group and outcome did not differ. This indicates non-inferiority of perioperative betablocker therapy in young age. Prospective and placebo-controlled assessment of perioperative esmolol therapy in neonates is needed.Methods: D-Transposition of the great arteries (d-TGA) is the most common congenital heart disease requiring surgical correction within the neonatal period. Sinus tachycardia often persists postoperatively, potentially affecting cardiac function. This study aimed to investigate the efficacy and safety of the short-acting beta-1-selective beta-blocker esmolol in controlling heart rate in neonatal cardiac surgery with cardiopulmonary bypass (CPB).A retrospective cohort study was conducted on neonates undergoing surgery for d-TGA. The study cohort included 112 patients, divided into an esmolol intervention group (n = 57) and a control group (n = 55). Baseline characteristics, hemodynamic parameters and outcome measures were assessed.In the esmolol group, median heart rate at ICU admission was significantly higher compared to the control group (155 vs. 147 bpm, p = 0.018). After a median time of 11 h, heart rate was lower among the esmolol patients (135 vs. 144 bpm, p < 0.001). There were no differences in other hemodynamic parameters between the two groups. Patients treated with esmolol required longer catecholamine support while no difference regarding survival, duration of invasive ventilation and ICU stay were noticed.No relevant hemodynamic difference was seen between neonates treated with perioperative esmolol and the control group and outcome did not differ. This indicates non-inferiority of perioperative betablocker therapy in young age. Prospective and placebo-controlled assessment of perioperative esmolol therapy in neonates is needed.Results: D-Transposition of the great arteries (d-TGA) is the most common congenital heart disease requiring surgical correction within the neonatal period. Sinus tachycardia often persists postoperatively, potentially affecting cardiac function. This study aimed to investigate the efficacy and safety of the short-acting beta-1-selective beta-blocker esmolol in controlling heart rate in neonatal cardiac surgery with cardiopulmonary bypass (CPB).A retrospective cohort study was conducted on neonates undergoing surgery for d-TGA. The study cohort included 112 patients, divided into an esmolol intervention group (n = 57) and a control group (n = 55). Baseline characteristics, hemodynamic parameters and outcome measures were assessed.In the esmolol group, median heart rate at ICU admission was significantly higher compared to the control group (155 vs. 147 bpm, p = 0.018). After a median time of 11 h, heart rate was lower among the esmolol patients (135 vs. 144 bpm, p < 0.001). There were no differences in other hemodynamic parameters between the two groups. Patients treated with esmolol required longer catecholamine support while no difference regarding survival, duration of invasive ventilation and ICU stay were noticed.No relevant hemodynamic difference was seen between neonates treated with perioperative esmolol and the control group and outcome did not differ. This indicates non-inferiority of perioperative betablocker therapy in young age. Prospective and placebo-controlled assessment of perioperative esmolol therapy in neonates is needed.Conclusion: D-Transposition of the great arteries (d-TGA) is the most common congenital heart disease requiring surgical correction within the neonatal period. Sinus tachycardia often persists postoperatively, potentially affecting cardiac function. This study aimed to investigate the efficacy and safety of the short-acting beta-1-selective beta-blocker esmolol in controlling heart rate in neonatal cardiac surgery with cardiopulmonary bypass (CPB).A retrospective cohort study was conducted on neonates undergoing surgery for d-TGA. The study cohort included 112 patients, divided into an esmolol intervention group (n = 57) and a control group (n = 55). Baseline characteristics, hemodynamic parameters and outcome measures were assessed.In the esmolol group, median heart rate at ICU admission was significantly higher compared to the control group (155 vs. 147 bpm, p = 0.018). After a median time of 11 h, heart rate was lower among the esmolol patients (135 vs. 144 bpm, p < 0.001). There were no differences in other hemodynamic parameters between the two groups. Patients treated with esmolol required longer catecholamine support while no difference regarding survival, duration of invasive ventilation and ICU stay were noticed.No relevant hemodynamic difference was seen between neonates treated with perioperative esmolol and the control group and outcome did not differ. This indicates non-inferiority of perioperative betablocker therapy in young age. Prospective and placebo-controlled assessment of perioperative esmolol therapy in neonates is needed. [ABSTRACT FROM AUTHOR]

The article presents case studies of 10-year-old boy with generalized tonic–clonic seizures; 27-year-old adult patient with tic complaints; and a 33-year-old female who presented to the emergency department with the complaint of neck pain. Topics include treatment method, in metastatic or unresectable cases with histopathologically highrisk criteria such as nuclear pleomorphism; and Pathological brain stem and cerebellar signal changes or pathological contrast enhancement were undetectable.

Background: Novel topical esmolol is shown to significantly improve wound healing than standard of care. Certain patient-related factors especially anemia and poor glycemic control may impede wound healing.To study whether novel topical esmolol may circumvent patient-related factors to improve wound healing in diabetic foot ulcer (DFU).The present study is a double-blind, vehicle (placebo)-controlled, randomized clinical trial in subjects with non-infected DFU of University of Texas grade 1A and 1C. Participants were randomized to receive either topical esmolol gel (Galnobax) with standard of care (SoC), SoC only, and vehicle (Placebo) with SoC in 3:3:1 proportion. The hematologic and biochemistry parameters were evaluated at the screening visit and at every 4 weeks after randomization during treatment phase and at the end of the study (EOS). Outcome was the proportion of complete ulcer closure with reference to baseline hemoglobin, albumin, and HbA1c during the 12-week treatment phase.A total of 176 subjects were included. Ninety-four out of 140 participants (67.1%) had anemia at baseline. Among anemic participants, 57.4% ulcers closed in the Galnobax group whereas 42.6% closed in the SoC only group during the 12-week treatment phase (p = 0.148, OR = 1.823, 95% CI = 0.80–4.13). One-third participants reported albumin < 4.0 g/dL. Among participants having albumin < 4.0 g/dL (one-third of participants), the proportion of ulcer closure was 60.9% in the Galnobax group compared to 42.1% in the SoC only group (p = 0.225, OR = 2.139, 95% CI = 0.62–7.37). The proportion of ulcer closure in Galnobax with the SoC group was higher (72.5%) compared to the SoC only group (43.5%) (p = 0.0067, OR = 3.427, 95% CI = 1.38–8.48) in participants with poor glycemic control (HbA1c > 8%).Novel topical esmolol with SoC treatment exhibited significant DFU healing independent of patient-related factors including anemia, hypoalbuminemia, and poor glycemic control.Objective: Novel topical esmolol is shown to significantly improve wound healing than standard of care. Certain patient-related factors especially anemia and poor glycemic control may impede wound healing.To study whether novel topical esmolol may circumvent patient-related factors to improve wound healing in diabetic foot ulcer (DFU).The present study is a double-blind, vehicle (placebo)-controlled, randomized clinical trial in subjects with non-infected DFU of University of Texas grade 1A and 1C. Participants were randomized to receive either topical esmolol gel (Galnobax) with standard of care (SoC), SoC only, and vehicle (Placebo) with SoC in 3:3:1 proportion. The hematologic and biochemistry parameters were evaluated at the screening visit and at every 4 weeks after randomization during treatment phase and at the end of the study (EOS). Outcome was the proportion of complete ulcer closure with reference to baseline hemoglobin, albumin, and HbA1c during the 12-week treatment phase.A total of 176 subjects were included. Ninety-four out of 140 participants (67.1%) had anemia at baseline. Among anemic participants, 57.4% ulcers closed in the Galnobax group whereas 42.6% closed in the SoC only group during the 12-week treatment phase (p = 0.148, OR = 1.823, 95% CI = 0.80–4.13). One-third participants reported albumin < 4.0 g/dL. Among participants having albumin < 4.0 g/dL (one-third of participants), the proportion of ulcer closure was 60.9% in the Galnobax group compared to 42.1% in the SoC only group (p = 0.225, OR = 2.139, 95% CI = 0.62–7.37). The proportion of ulcer closure in Galnobax with the SoC group was higher (72.5%) compared to the SoC only group (43.5%) (p = 0.0067, OR = 3.427, 95% CI = 1.38–8.48) in participants with poor glycemic control (HbA1c > 8%).Novel topical esmolol with SoC treatment exhibited significant DFU healing independent of patient-related factors including anemia, hypoalbuminemia, and poor glycemic control.Methods: Novel topical esmolol is shown to significantly improve wound healing than standard of care. Certain patient-related factors especially anemia and poor glycemic control may impede wound healing.To study whether novel topical esmolol may circumvent patient-related factors to improve wound healing in diabetic foot ulcer (DFU).The present study is a double-blind, vehicle (placebo)-controlled, randomized clinical trial in subjects with non-infected DFU of University of Texas grade 1A and 1C. Participants were randomized to receive either topical esmolol gel (Galnobax) with standard of care (SoC), SoC only, and vehicle (Placebo) with SoC in 3:3:1 proportion. The hematologic and biochemistry parameters were evaluated at the screening visit and at every 4 weeks after randomization during treatment phase and at the end of the study (EOS). Outcome was the proportion of complete ulcer closure with reference to baseline hemoglobin, albumin, and HbA1c during the 12-week treatment phase.A total of 176 subjects were included. Ninety-four out of 140 participants (67.1%) had anemia at baseline. Among anemic participants, 57.4% ulcers closed in the Galnobax group whereas 42.6% closed in the SoC only group during the 12-week treatment phase (p = 0.148, OR = 1.823, 95% CI = 0.80–4.13). One-third participants reported albumin < 4.0 g/dL. Among participants having albumin < 4.0 g/dL (one-third of participants), the proportion of ulcer closure was 60.9% in the Galnobax group compared to 42.1% in the SoC only group (p = 0.225, OR = 2.139, 95% CI = 0.62–7.37). The proportion of ulcer closure in Galnobax with the SoC group was higher (72.5%) compared to the SoC only group (43.5%) (p = 0.0067, OR = 3.427, 95% CI = 1.38–8.48) in participants with poor glycemic control (HbA1c > 8%).Novel topical esmolol with SoC treatment exhibited significant DFU healing independent of patient-related factors including anemia, hypoalbuminemia, and poor glycemic control.Results: Novel topical esmolol is shown to significantly improve wound healing than standard of care. Certain patient-related factors especially anemia and poor glycemic control may impede wound healing.To study whether novel topical esmolol may circumvent patient-related factors to improve wound healing in diabetic foot ulcer (DFU).The present study is a double-blind, vehicle (placebo)-controlled, randomized clinical trial in subjects with non-infected DFU of University of Texas grade 1A and 1C. Participants were randomized to receive either topical esmolol gel (Galnobax) with standard of care (SoC), SoC only, and vehicle (Placebo) with SoC in 3:3:1 proportion. The hematologic and biochemistry parameters were evaluated at the screening visit and at every 4 weeks after randomization during treatment phase and at the end of the study (EOS). Outcome was the proportion of complete ulcer closure with reference to baseline hemoglobin, albumin, and HbA1c during the 12-week treatment phase.A total of 176 subjects were included. Ninety-four out of 140 participants (67.1%) had anemia at baseline. Among anemic participants, 57.4% ulcers closed in the Galnobax group whereas 42.6% closed in the SoC only group during the 12-week treatment phase (p = 0.148, OR = 1.823, 95% CI = 0.80–4.13). One-third participants reported albumin < 4.0 g/dL. Among participants having albumin < 4.0 g/dL (one-third of participants), the proportion of ulcer closure was 60.9% in the Galnobax group compared to 42.1% in the SoC only group (p = 0.225, OR = 2.139, 95% CI = 0.62–7.37). The proportion of ulcer closure in Galnobax with the SoC group was higher (72.5%) compared to the SoC only group (43.5%) (p = 0.0067, OR = 3.427, 95% CI = 1.38–8.48) in participants with poor glycemic control (HbA1c > 8%).Novel topical esmolol with SoC treatment exhibited significant DFU healing independent of patient-related factors including anemia, hypoalbuminemia, and poor glycemic control.Conclusions: Novel topical esmolol is shown to significantly improve wound healing than standard of care. Certain patient-related factors especially anemia and poor glycemic control may impede wound healing.To study whether novel topical esmolol may circumvent patient-related factors to improve wound healing in diabetic foot ulcer (DFU).The present study is a double-blind, vehicle (placebo)-controlled, randomized clinical trial in subjects with non-infected DFU of University of Texas grade 1A and 1C. Participants were randomized to receive either topical esmolol gel (Galnobax) with standard of care (SoC), SoC only, and vehicle (Placebo) with SoC in 3:3:1 proportion. The hematologic and biochemistry parameters were evaluated at the screening visit and at every 4 weeks after randomization during treatment phase and at the end of the study (EOS). Outcome was the proportion of complete ulcer closure with reference to baseline hemoglobin, albumin, and HbA1c during the 12-week treatment phase.A total of 176 subjects were included. Ninety-four out of 140 participants (67.1%) had anemia at baseline. Among anemic participants, 57.4% ulcers closed in the Galnobax group whereas 42.6% closed in the SoC only group during the 12-week treatment phase (p = 0.148, OR = 1.823, 95% CI = 0.80–4.13). One-third participants reported albumin < 4.0 g/dL. Among participants having albumin < 4.0 g/dL (one-third of participants), the proportion of ulcer closure was 60.9% in the Galnobax group compared to 42.1% in the SoC only group (p = 0.225, OR = 2.139, 95% CI = 0.62–7.37). The proportion of ulcer closure in Galnobax with the SoC group was higher (72.5%) compared to the SoC only group (43.5%) (p = 0.0067, OR = 3.427, 95% CI = 1.38–8.48) in participants with poor glycemic control (HbA1c > 8%).Novel topical esmolol with SoC treatment exhibited significant DFU healing independent of patient-related factors including anemia, hypoalbuminemia, and poor glycemic control. [ABSTRACT FROM AUTHOR]

Primary vasopressor efficacy of epinephrine during cardiopulmonary resuscitation (CPR) is due to its α-adrenergic effects. However, epinephrine plays β1-adrenergic actions, which increasing myocardial oxygen consumption may lead to refractory ventricular fibrillation (VF) and poor outcome. Effects of a single dose of esmolol in addition to epinephrine during CPR were investigated in a porcine model of VF with an underlying acute myocardial infarction. VF was ischemically induced in 16 pigs and left untreated for 12 min. During CPR, animals were randomized to receive epinephrine (30 µg/kg) with either esmolol (0.5 mg/kg) or saline (control). Pigs were then observed up to 96 h. Coronary perfusion pressure increased during CPR in the esmolol group compared to control (47 ± 21 vs. 24 ± 10 mmHg at min 5, p < 0.05). In both groups, 7 animals were successfully resuscitated and 4 survived up to 96 h. No significant differences were observed between groups in the total number of defibrillations delivered prior to final resuscitation. Brain histology demonstrated reductions in cortical neuronal degeneration/necrosis (score 0.3 ± 0.5 vs. 1.3 ± 0.5, p < 0.05) and hippocampal microglial activation (6 ± 3 vs. 22 ± 4%, p < 0.01) in the esmolol group compared to control. Lower circulating levels of neuron specific enolase were measured in esmolol animals compared to controls (2[1–3] vs. 21[16–52] ng/mL, p < 0.01). In this preclinical model, β1-blockade during CPR did not facilitate VF termination but provided neuroprotection. [ABSTRACT FROM AUTHOR]

β-blockers having specific affinities to β-adrenergic receptors are routinely used to treat cardiovascular problems. Additionally, it has been demonstrated that these drugs can be effective in treating apoptosis-related diseases. The current study was conducted to investigate the cytotoxic and apoptotic effects of β-1 selective esmolol, β-2 selective ICI-118,551, and non-selective nadolol blockers on the cancerous and healthy lung cells. MTT test was used to evaluate cytotoxicity. Apoptotic actions were examined by using Annexin V-FITC/PI assay, JC-1 staining, ROS test, and the determination of the caspase-4 and -9, Bcl-2, Bax, Bax/Bcl-2, and JNK levels. Although the MRC-5 showed greater resistance than A549 cells, the β-blockers at 150–250 µM exhibited different levels of cytotoxic effect on both lung cell lines. Esmolol was found to be the most ineffective blocker and the increases in Bcl-2 protein levels were appeared to be effective in resistance to this drug. The increases in reactive oxygen species (ROS) together with the increase in caspase-4 and Bax protein levels have been shown to play a role in ICI-118,551 induced lung cell death. Nadolol was the most effective blocker increasing the total apoptotic cell population in both lung cells, which was based on both mitochondrial and endoplasmic reticulum stress. When the selectivities of the β-blockers are considered, it seems that β-2 specific antagonism predominantly mediated the death of lung cells, and the overwhelming factors causing apoptosis mainly varied depending on the selectivity of the blockers. [ABSTRACT FROM AUTHOR]

Background: Vasopressors are administered to critically ill patients with vasodilatory shock not responsive to volume resuscitation, and less often in cardiogenic shock, and hypovolemic shock.Objectives: The objectives are to review safety and efficacy of vasopressors, pathophysiology, agents that decrease vasopressor dose, predictive biomarkers, β1-blockers, and directions for research.Methods: The quality of evidence was evaluated using Grading of Recommendations Assessment, Development, and Evaluation (GRADE).Results: Vasopressors bind adrenergic: α1, α2, β1, β2; vasopressin: AVPR1a, AVPR1B, AVPR2; angiotensin II: AG1, AG2; and dopamine: DA1, DA2 receptors inducing vasoconstriction. Vasopressor choice and dose vary because of patients and physician practice. Adverse effects include excessive vasoconstriction, organ ischemia, hyperglycemia, hyperlactatemia, tachycardia, and tachyarrhythmias. No randomized controlled trials of vasopressors showed a significant difference in 28-day mortality rate. Norepinephrine is the first-choice vasopressor in vasodilatory shock after adequate volume resuscitation. Some strategies that decrease norepinephrine dose (vasopressin, angiotensin II) have not decreased 28-day mortality while corticosteroids have decreased 28-day mortality significantly in some (two large trials) but not all trials. In norepinephrine-refractory patients, vasopressin or epinephrine may be added. A new vasopressor, angiotensin II, may be useful in profoundly hypotensive patients. Dobutamine may be added because vasopressors may decrease ventricular contractility. Dopamine is recommended only in bradycardic patients. There are potent vasopressors with limited evidence (e.g. methylene blue, metaraminol) and novel vasopressors in development (selepressin).Conclusions: Norepinephrine is first choice followed by vasopressin or epinephrine. Angiotensin II and dopamine have limited indications. In future, predictive biomarkers may guide vasopressor selection and novel vasopressors may emerge. [ABSTRACT FROM AUTHOR]

Supraventricular tachycardia (SVT) is the most common arrhythmia in infants. Older children and adults with SVT are commonly managed with catheter ablation of the SVT substrate; however, such treatment is the last resort in infants because the risks of the procedure outweigh its benefits and most SVTs in infants resolve spontaneously in the first year of life. SVT in infants is generally managed with electrical cardioversion, vagal manoeuvres and antiarrhythmic drugs (e.g. adenosine, esmolol and procainamide as acute therapy, and digoxin and class Ic, II or III antiarrhythmics, most commonly propranolol, as chronic therapy). [ABSTRACT FROM AUTHOR]

The neuroimmunoregulation of inflammation has been well characterized. Entamoeba histolytica provokes an inflammatory response in the host in which macrophages and neutrophils are the first line of defense. The aim of this study was to analyze the effect of the 220 kDa lectin of Entamoeba histolytica on stimulation of human macrophages and neutrophils, especially the secretion of cytokines and the relation of these to neurotransmitters. Human cells were interacted with L220, epinephrine, nicotine, esmolol and vecuronium bromide. The concentrations of IL-1β, IFN-γ, TNF-α and IL-10 were determined by ELISA at, 4 h of interaction. L220 has a cytokine stimulating function of macrophages and neutrophils for secretion of IL-1β, and IL-10 only by macrophages, which was modulated by the effect of vecuronium on cholinergic receptors in this immune cells. [ABSTRACT FROM AUTHOR]

Purpose: The aim of this prospective study was to compare in non-Asian subjects the pharmacokinetics (PK), pharmacodynamics (PD), safety, and tolerability of two short-acting cardioselective β1-adrenergic antagonists, landiolol and esmolol, after administration of three different bolus dosages. Materials and methods: We conducted a single-center, prospective, double-blinded, randomized study in three cross-over periods with 12 healthy subjects (7 women and 5 men, mean age of 24.5 ± 6.9 years) each receiving three doses of landiolol (0.1, 0.2, and 0.3 mg/kg BW) either in a newly developed concentrate i.v. formulation (Rapibloc® 20 mg/2 mL concentrate) or a lyophilized formulation, or three doses of esmolol (0.5, 1, and 1.5 mg/kg BW) in an i.v. formulation (Brevibloc® 100 mg/10 mL). PK and PD parameters, safety, and tolerability were assessed. Findings: Results of the two landiolol formulations were reported previously and were similar. For the landiolol concentrate formulation and esmolol, maximum blood concentrations were rapidly reached (mean t ranged between 1.8 and 3.0 min for landiolol and 1.8 to 2.4 min for esmolol). The parent drugs disappeared very fast from the blood stream, with a t of 3.2 ± 1.2 (SD) minutes and 3.7 ± 2.1 (SD) minutes for the low doses of landiolol and esmolol, respectively. Despite comparable injection rates (0.1 or 0.5 mg/kg/15 s for landiolol and esmolol, respectively), the onset of significant heart rate reduction occurred earlier in response to landiolol (1 min) than in response to esmolol (2 min). In addition, significantly lower heart rate values were obtained at every dose level of landiolol, in comparison to esmolol ( p < 0.05). Both compounds reduced the systolic blood pressure to a comparable degree. Especially at the highest dose, the duration of blood pressure reduction was longer under esmolol compared to landiolol. Seven mild to moderate adverse events occurred after administration of landiolol, and five occurred after administration of esmolol. No serious adverse events were reported in this study. Implications: Heart rate reduction induced by a new liquid formulation of landiolol occurred faster, was more pronounced, and lasted longer than the effects of corresponding standard esmolol doses. Both agents reduced systolic blood pressure to a comparable degree, but the blood pressure decrease lasted longer after esmolol infusion. The local tolerance and safety profiles of the two formulations were similar. In summary, compared to esmolol, landiolol shows a more prominent and pronounced bradycardic effect in relation to its blood pressure-lowering effect, an action profile that might be of specific advantage in the perioperative setting. Trial registration: NCT01652898 and 2012-002127-14. [ABSTRACT FROM AUTHOR]

Purpose: Ventricular-arterial (V-A) decoupling decreases myocardial efficiency and is exacerbated by tachycardia that increases static arterial elastance (Ea). We thus investigated the effects of heart rate (HR) reduction on Ea in septic shock patients using the beta-blocker esmolol. We hypothesized that esmolol improves Ea by positively affecting the tone of arterial vessels and their responsiveness to HR-related changes in stroke volume (SV).Methods: After at least 24 h of hemodynamic optimization, 45 septic shock patients, with an HR ≥95 bpm and requiring norepinephrine to maintain mean arterial pressure (MAP) ≥65 mmHg, received a titrated esmolol infusion to maintain HR between 80 and 94 bpm. Ea was calculated as MAP/SV. All measurements, including data from right heart catheterization, echocardiography, arterial waveform analysis, and norepinephrine requirements, were obtained at baseline and at 4 h after commencing esmolol.Results: Esmolol reduced HR in all patients and this was associated with a decrease in Ea (2.19 ± 0.77 vs. 1.72 ± 0.52 mmHg l(-1)), arterial dP/dt max (1.08 ± 0.32 vs. 0.89 ± 0.29 mmHg ms(-1)), and a parallel increase in SV (48 ± 14 vs. 59 ± 18 ml), all p < 0.05. Cardiac output and ejection fraction remained unchanged, whereas norepinephrine requirements were reduced (0.7 ± 0.7 to 0.58 ± 0.5 µg kg(-1) min(-1), p < 0.05).Conclusions: HR reduction with esmolol effectively improved Ea while allowing adequate systemic perfusion in patients with severe septic shock who remained tachycardic despite standard volume resuscitation. As Ea is a major determinant of V-A coupling, its reduction may contribute to improving cardiovascular efficiency in septic shock. [ABSTRACT FROM AUTHOR]

We have performed a systematic literature review and a meta-analysis investigating the effect of beta-adrenergic antagonist on perioperative pain in randomized clinical trials (RCTs). The search included the CENTRAL, CINAHL, EMBASE, and MEDLINE databases (from inception to 10 February 2015). From the retrieved full texts, we hand-searched the references and PubMed related citations. A total of 11 RCTs consisting data of 701 adult patients were eligible for this systematic review. Esmolol was evaluated in ten trials and propranolol in one. Esmolol decreased the need for rescue analgesics by 32-50 %; p < 0.05 ( n = 7) and the proportion of patients needing rescue analgesia from 100 to 65 %; p < 0.005 ( n = 1), and propranolol decreased the need for rescue analgesics by 72 %; p < 0.001 ( n = 1). The time to the first rescue analgesics was longer ( p < 0.05) and pain ratings were lower ( p < 0.05) in patients with beta-adrenergic antagonists. However, in two opioid-controlled studies, one in knee arthroscopy and another in tubal ligation patients, the proportion of patients needing rescue analgesia was two-times higher in esmolol-treated patients: 52-57 vs. 23-34 %, p < 0.05. Adverse effects were rarely reported, and as reported were mostly cardiovascular alterations. In conclusion, intra-operative beta-adrenergic antagonists' administration may decrease postoperative pain and analgesic consumption when given as an adjuvant to general anesthesia. [ABSTRACT FROM AUTHOR]

β blockers reduce cerebral oxygenation after acute hemodilution and may contribute to the incidence of stroke when used perioperatively. The goal of the study was to investigate whether cerebral tissue oxygenation using near infrared spectroscopy can detect the β blocker-induced decrease in cerebral oxygenation depending on the severity of hemodilution and/or the dose of β blockers. Animals were anesthetized with 2% isoflurane and randomly assigned to a landiolol or esmolol group. After baseline measurement, landiolol or esmolol was administered at 40 µg/kg/min for 20 min, increased to 200 µg/kg/min for 20 min, and then stopped. Hemodynamic and arterial variables and the tissue oxygenation index (TOI) were recorded at each β blocker dose. Two stages of hemodilution were sequentially induced by repeated hemorrhage of 600 ml (33% of estimated blood volume) and infusion of the same volume of hydroxyethylstarch. During each stage, landiolol or esmolol was similarly administered and measurements were made. Landiolol and esmolol both dose-dependently decreased heart rate, mean arterial pressure and cardiac output, depending on the severity of hemodilution. Landiolol at 40 µg/kg/min was almost equivalent in potency to 200 µg/kg/min esmolol for decreasing HR before hemodilution. Based on the TOI, short-acting β blockers reduced cerebral oxygenation in a dose-dependent manner during hemodilution, and oxygenation returned to the baseline level after drug infusion was stopped. TOI may be useful for identification of a decrease in cerebral oxygenation for patients receiving β blockade during surgery associated with major bleeding. [ABSTRACT FROM AUTHOR]

Background Esmolol is the fi rst intravenous, short-acting, titratable β-blocker for use in critical care and surgical settings. It infl uences core components of an anesthetic regimen, such as analgesia, hypnosis, and memory function. Aims To investigate whether perioperative esmolol infusion as an adjuvant to total intravenous anesthesia could affect the total anesthetic and analgesic requirements in adult patients undergoing arthroscopic shoulder surgery. Settings and design A randomized, double-blinded, prospective study. Materials and methods Eighty adult ASA I and II pat ients scheduled for elective arthroscopic rotator cuff repair were randomized into the esmolol group (n = 40) and the control group (n = 40). In the esmolol group, 1 mg/kg esmolol was given as a bolus over 30 s, followed by 15 μg/kg/min as an intravenous infusion, and in the control group, the same volume of normal saline was given during the same time period. The heart rate, the mean arterial blood pressure, the depth of anesthesia, the duration of anesthesia, the recovery time, total anesthetic requirements, the postoperative pain score (VAS), and the to tal postoperative analgesic requirements were monitored and calculated during the perioperative period. Results There was no signifi cant difference between both groups regarding the demographic data using the unpaired t-test. There was a signifi cant difference between both groups (P < 0.05) regarding different parameters, except the duration of anesthesia, using the unpaired t-test. Preoperative mean values of heart rate (beats/min) and the mean arterial blood pressure (mmHg) were comparable between the two groups (P > 0.05). However, after induction of anesthesia and thereafter, there was a signifi cant reduction in heart rate and mean arterial bl ood pressure mean values in the esmolol group when compared with the control group (P < 0.05). A signifi cant change in bispectral index was noticed within each group in comparison with the baseline using the paired t-test. However, there was no signifi cant difference between both groups. Postoperative pain assessments by VAS (0-100 mm) showed signifi cantly lower pain scores in the esmolol group compared with the control group by the paired t-test (P < 0.05). There was a highly signifi cant reduction (P < 0.001) in the total cumulative doses of morphine consumption by PCA during the fi rst 24 h in the esmolol group compared with the control group. Conclusion Perioperative esmolol infusion reduces the total anesthetic and analgesic requirements and postoperative pain. Hence, esmolol can be considered as safe and suitable adjuvant to total intravenous anesthesia. [ABSTRACT FROM AUTHOR]

Context Ambulatory surgery has a target of rapid recovery and discharge. Esmolol has sparing effects on inhalational anesthetics and opioids. Aim The aim of the study was to demonstrate effects of esmolol infusion on recovery profi le and discharge from postanesthesia care unit (PACU). Settings and design This study was a randomized, double-blind, and controlled study. Patients and methods Sixty female patients scheduled for elective gynecologic laparoscopic surgery under general anesthesia were divided into two groups. Patients were given either esmolol loading and maintenance doses (the esmolol group) or equivalent volume of normal saline (the control group). Esmolol was given as a loading dose of 1 mg/kg just before induction of anesthesia followed by an infusion of 30 μg/kg/min. Depth of anesthesia was controlled by bispectral index monitoring and variable dose propofol infusion, whereas fentanyl and sevofl urane doses were fi xed throughout the procedure. Times denoting recovery from anesthesia were recorded. Patients who reached White-Song score of 12 plus pain numerical rating scale below 4 were discharged from PACU. Time needed for PACU discharge was recorded. Results Compared with the control group, the esmolol group had following statistically signifi cant results: lower blood pressure and heart rate, less fl uctuant bispectral index values, lower amount of propofol infusion used, shorter times for immediate postoperative eye opening, extubation, tongue protrusion, and ability of the patient to mention her name, lower pain scores, fewer patients needed analgesics and earlier discharge from PACU. Conclusion Intraoperative esmolol infusion is associated with hemodynamic stability and antinociceptive properties. Recovery profi le was excellent and helped early discharge from PACU. [ABSTRACT FROM AUTHOR]

Objectives This study was designed as a randomized comparison of postoperative pain after inguinal herniotomy in patients treated with intravenous esmolol and others treated with ropivacaine abdominal wound infiltration. Patients and methods Sixty American Society of Anesthesiologists physical status I-II patients undergoing herniotomy and anesthetized with isoflurane were randomized into one of two groups. Group R received 20 ml of ropivacaine 0.75% in 20 ml of saline 0.9% preincisional wound infiltration and group E patients received a bolus of esmolol 0.5 mg/kg intravenous at induction followed by an infusion of 5-15 mg/kg/min. After surgery, a bolus of pethidine was given according to visual analogue scale for pain intensity. Results Patients in group E had lower pain scores than patients in group R. Median consumption of pethidine was higher in group R than in group E. Conclusion Intravenous esmolol reduces pethidine consumption and provides more analgesia compared with preincisional ropivacaine infiltration in patients undergoing herniotomy [ABSTRACT FROM AUTHOR]

Purpose: The main aims of rapid sequence induction (RSI) are prompt and adequate muscle relaxation for tracheal intubation and hemodynamic stability during and after intubation. The purpose of the present study was to investigate the effects of nicardipine and esmolol on the action of rocuronium and intubation conditions during RSI. Methods: Adult patients ( n = 82) were randomly allocated to one of three groups. One minute prior to the induction of sevoflurane-based general anesthesia, patients received 20 μg/kg of nicardipine (N group; n = 27) or 0.5 mg/kg of esmolol (E group; n = 27), or 5 ml of saline (C group; n = 28). Patients were assessed according to intubation conditions, the onset time of rocuronium, mean arterial pressure (MAP), and heart rate (HR) during RSI. Results: The intubation conditions and score were significantly better in the C and N groups than in the E group ( P < 0.001). The onset time of rocuronium was shortened in the N group and prolonged in the E group when compared to the C group ( P < 0.001). A significant attenuation in the increase of MAP immediately after intubation was observed in the N group as compared with the C and E groups ( P < 0.008). HR was significantly lower in the E group than in the N and C groups ( P < 0.01). Conclusion: Pretreatment with nicardipine for RSI improved intubation conditions and shortened the onset time of rocuronium and attenuated changes in MAP after intubation. Esmolol may disturb intubation conditions and the onset of action of rocuronium, despite being effective in alleviating responses of HR after RSI. [ABSTRACT FROM AUTHOR]

We hypothesized that locally administrated β-adrenoreceptor agonist can modulate the inflammatory nociceptive parameters in carrageenan (CG)-induced peripheral inflammatory pain. This study was therefore aimed to assess the preventive and therapeutic effects of a β-agonist, dobutamine, by investigating its pretreatment and posttreatment actions on the inflammation-induced hypersensitivities (thermal hyperalgesia, mechanical allodynia) to cutaneous stimulation, edema, and several biochemical oxidant and anti-oxidant parameters in a rat model of CG-induced hind paw inflammation. Effects of dobutamine were compared with those of esmolol, a β-adrenoreceptor antagonist. CG injection to healthy rats lowered the thermal latencies (from 10.1 ± 0.2 to 4.9 ± 0.1 s) and mechanical thresholds (from 32.9 ± 0.5 to 18.9 ± 1.3 g) and caused the hyperalgesia and allodynia. In CG-induced inflamed paws, while intraplantar esmolol treatment (1 mg) produced significant decreases in latencies (4.1 ± 0.1 s) and thresholds (15.2 ± 2.4 g), dobutamine (1 mg) increased the latencies (11.3 ± 0.5 s) and thresholds (26.3 ± 2.8 g). In contrast to esmolol, dobutamine increased the superoxide dismutase level and decreased the myeloperoxidase, malondialdehyde, and nitric oxide levels in CG-induced inflamed paws. The present results can reveal that β-adrenoreceptors may play a role in inflammatory nociceptive processes, and locally treated β-adrenoreceptor agonists such as dobutamine can be a preferable, appropriate choice for the management of inflammatory nociception due to their preventive and therapeutic effects on CG-induced peripheral inflammatory nociception. [ABSTRACT FROM AUTHOR]

Purpose: Ischemia/reperfusion injury remains an untreated clinical problem in patients with acute myocardial infarction (AMI) despite significant advances in emergent revascularization through percutaneous coronary intervention (PCI). Pharmacological intervention for infarct size reduction is unavailable. We have identified that the medications milrinone and esmolol, when administered together at the beginning of the reperfusion, significantly decrease infarct size via reducing reperfusion injury in an experimental model. The present study tested the safety of combination therapy of milrinone and esmolol (M + E) in patients with AMI. Methods: Sixteen subjects with AMI requiring PCI were consecutively recruited. M + E was intravenously infused simultaneously for 10 min started at 5 min before anticipated angioplasty balloon inflation. Another 16 consecutively recruited AMI patients requiring PCI served as a placebo arm treated per routine clinical protocol. Blood pressure (BP) and heart rate (HR) were monitored continuously during PCI. Results: M + E combination therapy resulted in a trend of non-significant reduction in BP compared with a control group. There was a modest but significant increase in HR at the later phase of M + E infusion compared with a control group. No significant cardiac arrhythmia was induced during M + E infusion. Conclusions: The combination therapy with M + E produces a minimal change in hemodynamics and appears safe as an adjunctive therapy to PCI in AMI patients. Further studies are warranted. [ABSTRACT FROM AUTHOR]

Intraoperative bleeding causing poor visibility of surgical field is of major concern during functional endoscopic sinus surgery (FESS) and impaired visibility may result in many complications. The study aimed to compare surgical conditions for FESS during controlled hypotension provided by esmolol or nitroglycerine (NTG) under general anaesthesia. 52 adult patients of both sexes requiring FESS under general anaesthesia were randomly divided to receive either esmolol (group ESM, n = 26) or NTG (group NTG, n = 26) to provide controlled hypotension. Surgical condition was assessed by surgeon using average category scale (ACS) of 0-5, a value of 2-3 being ideal. In both groups mean arterial blood pressure (MABP) was gradually reduced till ACS for assessment of surgical condition (ACS) of 2-3 or lowest targeted MABP (60 mm of Hg) was achieved. Both the drugs produced desired hypotension and improved surgical condition by reducing operative field bleeding but ideal operative conditions were achieved at mild hypotension (MABP 75-70) in ESM group while same conditions were achieved at MABP of 69-65 mm of Hg in NTG group. Mean heart rate was significantly higher in NTG group as compared to ESM group. Blood loss was significantly less in ESM group. Both NTG and esmolol can be used safely to provide controlled hypotension during FESS. Both the drugs improved visibility of surgical field by reducing capillary bleeding. But esmolol offered better operative conditions with only minimal reduction in MABP. No reflex tachycardia and less intraoperative haemorrhage were additional advantages of esmolol. [ABSTRACT FROM AUTHOR]

Hypertension is an extremely pervasive condition that affects a large percentage of the world population. Although guidelines exist for the treatment of the patient with elevated blood pressure, there remains a paucity of literature and accepted guidelines for the perioperative evaluation and care of the patient with hypertension who undergoes either cardiac or noncardiac surgery. Of particular importance is defining the patients most vulnerable to complications and the indications for immediate and rapid antihypertensive treatment and/or cancellation of surgery to reduce these risks in each of the three perioperative settings: preoperative, intraoperative, and postoperative. This review also examines the parenteral antihypertensive medications most commonly administered in the perioperative setting. [ABSTRACT FROM AUTHOR]

Copyright of Wiener Klinische Wochenschrift is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Purpose: The aim of this experimental study is to investigate cardiovascular tolerance of blockade of beta-adrenergic receptors in an endotoxin model. Design: Prospective, randomized, controlled study. Setting: Animal laboratory in a university medical center. Methods: Ten anesthetized, mechanically ventilated pigs were challenged with intravenous lipopolysaccharide (LPS) to achieve a status of profound hypodynamic shock. Systemic and pulmonary hemodynamics and cardiac output were continuously monitored throughout the 5-h study period, and blood samples were taken at baseline ( T − 30 min), 1 h from the beginning of LPS infusion ( T + 60 min), and every 2 h ( T + 180 min and T + 300 min). Animals were randomly assigned to continuous intravenous esmolol infusion titrated to decrease heart rate by 20% or isotonic saline. Results: Esmolol decreased heart rate by 20%, while in the saline group, heart rate increased by 7% and 22% at T + 180 min and T + 300 min, respectively ( p < 0.001). In esmolol-treated animals, cardiac index decreased by 9% at T + 180 min and by 2% at T + 300 min, and in controls by 14% at T + 180 min and by 27% at T + 300 min ( p = 0.870). In esmolol-treated animals, median (interquartile range, IQR) stroke index was 31 (6) and 47 (11) ml/min/m at T + 180 min and T + 300 min, respectively, and decreased steadily from 45 (20) to 18 (13) ml/min/m in controls ( p = 0.030). There were no significant differences between groups for any other hemodynamics variables, except for systemic vascular resistance (SVR) ( p = 0.017). Conclusions: In large animals with endotoxemic shock, continuous infusion of esmolol, a selective beta-1 adrenergic blocker, titrated to decrease heart rate by 20%, was well tolerated and may offset LPS-induced cardiac dysfunction by a preload positive effect. [ABSTRACT FROM AUTHOR]

Introduction: The present study determined whether late-ischemia/early reperfusion therapy with the β-adrenergic receptor (AR) blocker esmolol and phosphodiesterase III inhibitor milrinone reduced left ventricular (LV) myocardial infarct size (IS). Methods and Results: In an ischemia/reperfusion rat model (30-min ischemia/4-hr reperfusion), esmolol, milrinone or esmolol + milrinone were intravenous (IV) infused over 10 min (from the last 5min of ischemia to the first 5min of reperfusion). LV-IS were 48.9 ± 8.9%, 41.5 ± 5.4%, 25.8 ± 7.7% and 16.8 ± 7.3% for saline, esmolol, milrinone, and esmolol + milrinone, respectively ( n = 12/group). Esmolol + milrinone further reduced LV-IS compared with esmolol or milrinone alone ( p < 0.05). LV-IS-reduction induced by esmolol + milrinone was eliminated in the presence of protein kinase A-(PKA)-inhibitor (Rp-cAMPS) or Akt-inhibitor (AKT 1/2 kinase inhibitor). In mixed rat ventricular cardiomyocyte cultures, intra-ischemic application of esmolol, milrinone or esmolol + milrinone reduced myocyte death rates by 5.5%, 13.3%, and 16.8%, respectively, compared with saline ( p < 0.01). This cell protective effect by esmolol + milrinone was abrogated in the presence of PKA-inhibitor or Akt-inhibitor. Esmolol, milrinone or esmolol + milrinone increased myocardial PKA activity by 22%, 28% and 59%, respectively, compared with saline ( n = 6, p < 0.01). No non-specific adverse effect of Rp-cAMPS on myocytes was identified in a purified myocyte preparation during hypoxia/re-oxygenation. Antiapoptotic pathways were assessed by measuring myocardial phosphorylated Akt (pAkt) levels combined with terminal dUTP nick-end labelling staining analysis. Ten minutes following infusion of esmolol, milrinone or esmolol + milrinone, there were 1.7-, 2.7-, and 6-fold increase in tissue pAkt levels, respectively. This esmolol + milrinone induced pAkt activation was abolished in the presence of PKA inhibitor. Esmolol, milrinone and esmolol + milrinone reduced myocyte apoptosis rates by 22%, 37% and 60%, respectively, compared with saline ( p < 0.01). Conclusions: Late-ischemia/early reperfusion therapy with esmolol + milrinone additively reduces LV-IS associated with robust activation of myocardial PKA and subsequent Akt-antiapoptotic pathway. [ABSTRACT FROM AUTHOR]

Background: The adult practice for ECG-gated single-source 64-slice coronary CTA (CCTA) includes administering beta-blockers to reduce heart rate. There are limited data on this process in children. Objective: To evaluate the safety and efficacy of a drug regimen to decrease heart rate before performing CCTA in children. Materials & methods: IV remifentanil and esmolol infusion were chosen to decrease heart rate in 41 children (mean age 6.5 years) while they were under general anesthesia (GA) for CCTA. Drug doses, changes in heart rate and procedural complications were recorded. CCTA image quality was graded on a scale of 1 to 5. The relationships between image quality and heart rate and image quality and age were evaluated. Patient effective radiation doses were calculated. Results: Heart rates were lowered utilizing esmolol (4 children), remifentanil (2 children) or both (35 children); 26 children received nitroglycerin for coronary vasodilation. The mean decrease in heart rate was 26%. There were no major complications. The average image-quality score was 4.4. Higher heart rates were associated with worse image quality ( r = 0.67, P < 0.0001). Older age was associated with better image quality ( r = 0.66, P < 0.0001). Effective radiation doses were 0.7 to 7.0 mSv. Conclusion: Heart rate reduction for pediatric CCTA can be safely and effectively achieved while yielding high-quality images. [ABSTRACT FROM AUTHOR]

The article discusses a study conducted by scientists A. Morelli and coworkers on septic shock which represents maximum physical stresses to the organism and physiological response to sepsis includes increased release of cachotelamines and cardiac beta 1-adrenergic receptors. Topics discussed include hemodynamic stabilization, benefit of the combination of esmolol and milrinone in sepsis, and use of beta-blockers.

The authors present a study on cardiac assessment in the critically ill septic patient by referring to the lack of precise evaluation by practicing clinicians and discuss the cardiovascular (CV) performance or efficiency as a tool in this regards. Also discussed is the role of beta blockers such as esmolol in the improvement of cardiovascular efficiency.

Severe, symptomatic hypertension occurs uncommonly in children, usually only in those with underlying congenital or acquired renal disease. If such hypertension has been long-standing, then rapid blood pressure reduction may be risky due to altered cerebral hemodynamics. While many drugs are available for the treatment of severe hypertension in adults, few have been studied in children. Despite the lack of scientific studies, some agents, particularly continuous intravenous infusions of nicardipine and labetalol, are preferred in many centers. These agents generally provide the ability to control the magnitude and rapidity of blood pressure reduction and should—in conjunction with careful patient monitoring—allow the safe reduction of blood pressure and the avoidance of complications. This review provides a summary of the underlying causes and pathophysiology of acute severe hypertension in childhood as well as a detailed discussion of drug treatment and the optimal clinical approach to managing children and adolescents with acute severe hypertension. [ABSTRACT FROM AUTHOR]

A new method is presented for the determination of five selected β-receptor antagonists by HPLC, which emphasizes sample preparation via retention on a new type of silica gel sorbent used for solid-phase extraction (SPE). Sorbents of this type were obtained by the chemical modification of silica gels of various porosities by cholesterol ligands. The cholesterol-based packing material was investigated by spectroscopic methods and elemental analysis. The recoveries obtained with the extraction procedure were optimum over a relatively broad sample pH range (3.08–7.50). Analytical factors such as the sample loading, the washing step and elution conditions, the concentration of β-receptor antagonists to be extracted, and the type of sorbent were found to play significant roles in the sample preparation procedure and would therefore need to be controlled to achieve optimum recoveries of the analytes. Under optimum conditions, the recoveries of nadolol, acebutolol, esmolol, oxprenolol and propranolol from spiked buffers, blood and urine were reproducible and dependent on the polarity or hydrophilicity of the compounds. The above analytes were determined by reverse-phase high-performance liquid chromatography (HPLC) with UV and ESI-ion trap mass spectrometry (MS) detection. The described method was found to be suitable for the routine measurement of compounds that are both polar and basic, and can be applied for the analysis of biological samples such as urine and blood in clinical, toxicological or forensic laboratories. The recovery measurements were performed on spiked human urine and serum, and on real samples of mouse blood serum. [ABSTRACT FROM AUTHOR]

We 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. Tachycardia 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 rates of left ventricular force development (LVdP/dtmax), and myocardial oxygen consumption (MVO2) were measured and compared. Both landiolol and esmolol produced dosedependent decreases in HR, LVDP, LVdP/dtmax, and MVO2. The HR lowering effects of the two agents were comparable. At concentrations of 3 · 10−5 and 1 · 10−4 M, esmolol produced more profound depression of LVDP (47 ± 26 and 12 ± 11 mmHg, respectively; mean ± SD) and reduction of LVdP/dtmax (650 ± 287 and 120 ± 103 mmHg·s−1) than landiolol (68 ± 20 and 64 ± 20 mmHg, and 897 ± 236 and 852 ± 240 mmHg·s−1, respectively). At the same concentrations, esmolol caused more profound reduction in MVO2 (40 ± 11 and 35 ± 10 μl·min−1 · g−1) than landiolol (50 ± 8 and 48 ± 8 μl·min−1 · g−1), respectively. Our results indicate that in the isolated rabbit heart, landiolol and esmolol had equipotent negative chronotropic effects, however, landiolol had a less potent negative inotropic effect than esmolol. [ABSTRACT FROM AUTHOR]

Esmolol is often used in the acute management of children with arrhythmias and/or hypertension; however, pharmacokinetic studies of the drug in children have been limited. The objective of this study was to determine the pharmacokinetics of esmolol in children with a history of supraventricular arrhythmias (SVT) who were scheduled for diagnostic electrophysiology study or a catheter ablation procedure. Subjects were stratified into two age groups: 2-11 and 12-16 years. After an episode of stimulated or spontaneous SVT, esmolol was administered intravenously as a 1,000 μg/kg bolus followed by continuous infusion at 300 μg/kg/mm. Blood samples were col- lected before, at 5, 10 and 15 mm after the loading dose, and 3, 6, 9, 12, 15 and 20 mm after the end of the infusion. Plasma concentration of esmolol was quantitated by a specific LC/MS assay. Pharmacokinetic data were avail- able for 25 subjects. Arterial esmolol concentrations were approximately five times greater than venous concentra- tions. Esmolol had an extremely short distribution half-life (0.6 mm), a rapid terminal elimination half-life (6.9 mm), and a rapid clearance (119 ± 51 mL/min/kg) which was not related to subject age or weight. Seventeen of the subjects (63%) converted to normal sinus rhythm in an average of 2 mm (range 0-5 mm). The pharmacokinetics of esmolol and its efficacy in terminating SVT in children is similar to that observed in adults. [ABSTRACT FROM AUTHOR]

Abstract The objective of this study was to evaluate the effectiveness and safety of esmolol-induced negative mo- and chronotropism during stent/balloon angioplasty for aortic coarctation. Balloon angioplasty and stent placement have become widely accepted therapies for native and recurrent coarctation of the aorta (CoA). Trauma to the vessel wall and stent migration related to forward dis- placement of the balloon and/or stent by cardiac output, are the most common complications. Controlling stroke vol- ume and heart rate may assist in balloon stability and accurate deployment of stents. All methods currently used to achieve this have significant limitations. We describe our experience using esmolol to control stroke volume and heart rate during balloonlstent angioplasty of CoA. We performed a retrospective review of all patients who had intravenous esmolol during percutaneous treatment of CoA. Six interventions were performed in six patients: coarctation stent angioplasty in five patients (two native coarctation) and balloon angioplasty alone in one patient. The median systolic blood pressure achieved during the procedure was 65 mmHg (range, 57-75) representing a median reduction of 40 mmHg (range, 20-80; p = 0.008) from baseline. The median heart achieved was 50 beats! mm (range, 20-80), representing a median reduction of 20 beats/mm (range, 15-90, p = 0.048) from baseline. Optimal stent position was obtained in all patients. Intra- venous esmolol controls periprocedural hemodynamics effectively and safely during percutaneous therapy for aortic coarctation, thereby aiding accurate stent placement. Further evaluation of its use during other percutaneous left heart interventions is required. [ABSTRACT FROM AUTHOR]

Electroconvulsive therapy (ECT) is used in the treatment of severe psychiatric disorders. It involves the induction of a seizure for therapeutic purposes by the administration of a variable-frequency electrical stimulus via electrodes applied to the scalp. The original application of ECT in non-anaesthetised patients resulted in many traumatic effects and was replaced, in the early 1960s, with a modified ECT regimen that used anaesthesia with neuromuscular blockade. This remains the worldwide standard today. The development of modern ECT devices, with improved impulse modes, has also reduced the incidence of post-interventional cognitive adverse effects. The variety of centrally-acting co-medications administered and the cardiovascular effects occurring during the procedure make patients receiving ECT a challenge for the anaesthetist. The efficacy of ECT depends on the production of adequate seizures; however, the anaesthetic agents commonly used during ECT suppress the generation of convulsions. Therefore, the efficacy of ECT requires knowledge of anaesthetic precepts, understanding of the interaction between anaesthetic drugs and seizure activity, and awareness of the physiological effects of ECT as well as the treatment of those effects. Successful and safe ECT depends on the correct choice of anaesthetic drugs for the individual patient, which have to be chosen with respect to the individual concomitant medication and pre-existing diseases. This review provides information for the optimal selection, set-up and practice of anaesthetic drug treatment in ECT. [ABSTRACT FROM AUTHOR]