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  1. Article: New drug sugammadex: a selective relaxant binding agent.

    Welliver, Mark

    AANA journal

    2006  Volume 74, Issue 5, Page(s) 357–363

    Abstract: ... selective relaxant binding agents, which binds and inactivate aminosteroid nondepolarizing muscle relaxants ... while maintaining aqueous solubility. Encapsulation of molecules is the principal action of a new drug class ... The Netherlands), and it may hold promise for a new concept in muscle relaxant reversal. Encapsulation rather ...

    Abstract Cyclodextrins are molecules with a hollow, truncated cone shape that possess unique lipophilic and hydrophilic properties. These unique properties enable cyclodextrins to engulf and bind lipophilic molecules while maintaining aqueous solubility. Encapsulation of molecules is the principal action of a new drug class, selective relaxant binding agents, which binds and inactivate aminosteroid nondepolarizing muscle relaxants. Sugammadex is the name of a modified cyclodextrin currently in phase 3 studies by Organon International (Oss, The Netherlands), and it may hold promise for a new concept in muscle relaxant reversal. Encapsulation rather than competitive antagonism of neuromuscular blockade may be a future modality of anesthetic practice.
    MeSH term(s) Androstanols/antagonists & inhibitors ; Anesthesia/methods ; Anesthesia/trends ; Animals ; Binding, Competitive ; Cats ; Chemistry, Pharmaceutical ; Clinical Trials as Topic ; Drug Carriers ; Drug Evaluation ; Forecasting ; Guinea Pigs ; Haplorhini ; Humans ; Metabolic Clearance Rate ; Mice ; Neuromuscular Nondepolarizing Agents/antagonists & inhibitors ; Solubility ; gamma-Cyclodextrins/chemistry ; gamma-Cyclodextrins/pharmacology ; gamma-Cyclodextrins/therapeutic use
    Chemical Substances Androstanols ; Drug Carriers ; Neuromuscular Nondepolarizing Agents ; gamma-Cyclodextrins ; Sugammadex (361LPM2T56) ; rocuronium (WRE554RFEZ)
    Language English
    Publishing date 2006-10
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 603605-3
    ISSN 0094-6354
    ISSN 0094-6354
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 1286: Show issues Location:
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  2. Article ; Online: Neuromuscular transmission: new concepts and agents.

    de Boer, Hans D

    Journal of critical care

    2009  Volume 24, Issue 1, Page(s) 36–42

    Abstract: Sugammadex is the first selective relaxant binding agent which was originally designed to reverse ... the steroidal NMB drug rocuronium. The results of recent studies demonstrate that sugammadex is effective ... side-effects. Sugammadex-rocuronium complexes are highly hydrophilic and it has been demonstrated ...

    Abstract Sugammadex is the first selective relaxant binding agent which was originally designed to reverse the steroidal NMB drug rocuronium. The results of recent studies demonstrate that sugammadex is effective for reversal of rocuronium and vecuronium-induced neuromuscular block without apparent side-effects. This is in contrast to the currently available cholinesterase inhibitors used to reverse neuromuscular block and which are even ineffective against profound neuromuscular block and have a number of undesirable side-effects. Sugammadex-rocuronium complexes are highly hydrophilic and it has been demonstrated that sugammadex is excreted in a rapid and dose-dependent manner in urine, resulting in a complete elimination from the body. The ability of sugammadex to reverse rocuronium and vecuronium-induced neuromuscular block may have major implications for routine anesthetic practice. Once sugammadex becomes commercially available, anesthesiologists will be capable of maintaining the desired depth of neuromuscular block at any time, thereby assuring optimal surgical conditions. The mechanism by which sugammadex encapsulates rocuronium and vecuronium appears to be superior to currently used neuromuscular block reversal strategies in terms of speed, efficacy and side effects. In this article, clinical studies of sugammadex are discussed.
    MeSH term(s) Androstanols/antagonists & inhibitors ; Anesthesia Recovery Period ; Chemistry, Pharmaceutical ; Cholinesterase Inhibitors/adverse effects ; Cholinesterase Inhibitors/therapeutic use ; Dose-Response Relationship, Drug ; Drug Monitoring ; Humans ; Metabolic Clearance Rate ; Monitoring, Intraoperative ; Muscarinic Antagonists/therapeutic use ; Neuromuscular Blockade/adverse effects ; Neuromuscular Blockade/methods ; Neuromuscular Junction/drug effects ; Neuromuscular Nondepolarizing Agents/antagonists & inhibitors ; Patient Selection ; Safety ; Synaptic Transmission/drug effects ; Treatment Outcome ; Vecuronium Bromide/antagonists & inhibitors ; gamma-Cyclodextrins/metabolism ; gamma-Cyclodextrins/pharmacology ; gamma-Cyclodextrins/therapeutic use
    Chemical Substances Androstanols ; Cholinesterase Inhibitors ; Muscarinic Antagonists ; Neuromuscular Nondepolarizing Agents ; gamma-Cyclodextrins ; Sugammadex (361LPM2T56) ; Vecuronium Bromide (7E4PHP5N1D) ; rocuronium (WRE554RFEZ)
    Language English
    Publishing date 2009-03
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 632818-0
    ISSN 1557-8615 ; 0883-9441
    ISSN (online) 1557-8615
    ISSN 0883-9441
    DOI 10.1016/j.jcrc.2008.08.004
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2152: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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