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Mark Welliver - One of the best experts on this subject based on the ideXlab platform.

  • discovery development and clinical application of sugammadex sodium a selective relaxant Binding Agent
    Drug Design Development and Therapy, 2008
    Co-Authors: Mark Welliver, John P Mcdonough, Nicholas M Kalynych, Robert Redfern
    Abstract:

    Neuromuscular blockade, induced by neuromuscular blocking Agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking Agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking Agents. Sugammadex sodium is the first in a new class of drug called selective relaxant Binding Agents. Currently, in clinical trials, sugammadex, a modified gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking Agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential perioperative benefits.

  • New drug sugammadex: A selective relaxant Binding Agent
    AANA Journal, 2006
    Co-Authors: Mark Welliver
    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.

Robert Redfern - One of the best experts on this subject based on the ideXlab platform.

  • discovery development and clinical application of sugammadex sodium a selective relaxant Binding Agent
    Drug Design Development and Therapy, 2008
    Co-Authors: Mark Welliver, John P Mcdonough, Nicholas M Kalynych, Robert Redfern
    Abstract:

    Neuromuscular blockade, induced by neuromuscular blocking Agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking Agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking Agents. Sugammadex sodium is the first in a new class of drug called selective relaxant Binding Agents. Currently, in clinical trials, sugammadex, a modified gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking Agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential perioperative benefits.

F K Puhringer - One of the best experts on this subject based on the ideXlab platform.

  • sugammadex a selective relaxant Binding Agent providing rapid reversal
    Current Opinion in Anesthesiology, 2010
    Co-Authors: Christopher Rex, Urs Adrian Bergner, F K Puhringer
    Abstract:

    Purpose of review Sugammadex is a new reversal Agent with a unique mechanism of action in anaesthesia. Because of its rapid onset of action and its efficacy in determining neuromuscular blockade at any time, it opens up new perspectives in anaesthesia. Recent findings During the last few years, a lot of phase II and III studies have been published, investigating various groups of patients and clinical situations. Sugammadex has been shown to be a well tolerated drug, which appears to meet every challenge it is presented with in daily clinical practice. Summary Sugammadex binds amino-steroidal muscle relaxants by encapsulation. It enables rapid reversal of neuromuscular blockade at any time point and at any depth of block. Its effects are predictable and very reliable, in contrast to cholinesterase inhibitors. This opens up new perspectives in anaesthesia. Even an emergency reversal of high-dose rocuronium-induced neuromuscular blockade is possible with sugammadex and times to full recovery (TOF 0.9) are faster than after spontaneous recovery from suxamethonium.

Martine E Prins - One of the best experts on this subject based on the ideXlab platform.

Christopher Rex - One of the best experts on this subject based on the ideXlab platform.

  • sugammadex a selective relaxant Binding Agent providing rapid reversal
    Current Opinion in Anesthesiology, 2010
    Co-Authors: Christopher Rex, Urs Adrian Bergner, F K Puhringer
    Abstract:

    Purpose of review Sugammadex is a new reversal Agent with a unique mechanism of action in anaesthesia. Because of its rapid onset of action and its efficacy in determining neuromuscular blockade at any time, it opens up new perspectives in anaesthesia. Recent findings During the last few years, a lot of phase II and III studies have been published, investigating various groups of patients and clinical situations. Sugammadex has been shown to be a well tolerated drug, which appears to meet every challenge it is presented with in daily clinical practice. Summary Sugammadex binds amino-steroidal muscle relaxants by encapsulation. It enables rapid reversal of neuromuscular blockade at any time point and at any depth of block. Its effects are predictable and very reliable, in contrast to cholinesterase inhibitors. This opens up new perspectives in anaesthesia. Even an emergency reversal of high-dose rocuronium-induced neuromuscular blockade is possible with sugammadex and times to full recovery (TOF 0.9) are faster than after spontaneous recovery from suxamethonium.