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Discovery of an Ultralong-acting Nondepolarizing Neuromuscular Blocker That Displays Short Onset Time and On-Demand Rapid Reversal by a Biocompatible Antagonist.
J Med Chem
January 2025
Department of Chemistry, Fudan University, 2205 Songhu Road, Shanghai 200438, China.
The combination of ultralong-acting neuromuscular block and subsequent on-demand rapid reversal may provide prolonged surgeries with improved conditions by omitting continuous or repetitive blocker administration, enabling a more stable and predictable hemodynamic profile and eliminating residual block. For this target, we prepared 19 imidazolium-incorporated tetracationic macrocycles. In vivo studies with rats revealed that one macrocycle (IMC-14) displays extremely high blocking activity.
View Article and Find Full Text PDF[Comparative analysis of the efficacy of domestic and imported sugammadex for reversal of rocuronium-induced deep neuromuscular block in adult patients].
Zhonghua Yi Xue Za Zhi
January 2025
Department of Biomedical Statistics, Peking University First Hospital, Beijing100034, China.
To evaluate the efficacy of domestic and imported sugammadex for reversal of rocuronium-induced deep neuromuscular block (NMB) in adult patients. The clinical data of adult patients who scheduled for elective surgery with general anesthesia that required muscle relaxants in Peking University First Hospital from June 2023 to June 2024 were prospectively included. The patients were devided into domestic group and imported group according to random number table method.
View Article and Find Full Text PDFSkeletal Muscle Relaxants and Their Impact on Intracranial Pressure in Neurosurgery.
Med Sci Monit
January 2025
Department of Rheumatology, University Clinical Hospital No. 1 Szczecin, Szczecin, Poland.
Skeletal muscle relaxants have their place in everyday use in numerous anesthesiological procedures, such as preparing a patient for surgery, supporting mechanical ventilation, and performing effective intubation. These drugs can be divided, based on their mechanism of action, into depolarizing skeletal relaxants, such as succinylcholine, and non-depolarizing skeletal muscle relaxants. Non-depolarizing agents are further categorized, based on their structure, into steroidal (eg, rocuronium) and benzylisoquinoline (eg, atracurium) compounds.
View Article and Find Full Text PDFTrichostatin A reverses rocuronium resistance in burn-injured rats.
Burns
December 2024
Department of Anesthesiology, Shanghai General Hospital, Shanghai Jiaotong University, School of Medicine, Shanghai, China. Electronic address:
Aims: This study aimed to investigate whether the histone deacetylase HDAC4 inhibitor, trichostatin A (TSA), could reverse resistance to non-depolarizing muscle relaxants (NDMRs) caused by burn injuries.
Materials And Methods: A rat burn injury model was established, in which TSA was administered to inhibit HDAC4 expression. The potency of rocuronium was assessed through tension tests, and the levels of HDAC4 and myogenin proteins were determined using Western blot.
Factors Associated With Decision to Use and Dosing of Sugammadex in Children: A Retrospective Cross-Sectional Observational Study.
Anesth Analg
January 2025
From the Department of Anesthesiology, University of Michigan, Ann Arbor, Michigan.
Background: Sugammadex was initially approved for reversal of neuromuscular blockade in adults in the United States in 2015. Limited data suggest sugammadex is widely used in pediatric anesthesia practice however the factors influencing use are not known. We explore patient, surgical, and institutional factors associated with the decision to use sugammadex versus neostigmine or no reversal, and the decision to use 2 mg/kg vs 4 mg/kg dosing.
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