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Calabadion

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https://www.readbyqxmd.com/read/27341276/a-novel-strategy-to-reverse-general-anesthesia-by-scavenging-with-the-acyclic-cucurbit-n-uril-type-molecular-container-calabadion-2
#1
Daniel Diaz-Gil, Friederike Haerter, Shane Falcinelli, Shweta Ganapati, Gaya K Hettiarachchi, Jeroen C P Simons, Ben Zhang, Stephanie D Grabitz, Ingrid Moreno Duarte, Joseph F Cotten, Katharina Eikermann-Haerter, Hao Deng, Nancy L Chamberlin, Lyle Isaacs, Volker Briken, Matthias Eikermann
BACKGROUND: Calabadion 2 is a new drug-encapsulating agent. In this study, the authors aim to assess its utility as an agent to reverse general anesthesia with etomidate and ketamine and facilitate recovery. METHODS: To evaluate the effect of calabadion 2 on anesthesia recovery, the authors studied the response of rats to calabadion 2 after continuous and bolus intravenous etomidate or ketamine and bolus intramuscular ketamine administration. The authors measured electroencephalographic predictors of depth of anesthesia (burst suppression ratio and total electroencephalographic power), functional mobility impairment, blood pressure, and toxicity...
August 2016: Anesthesiology
https://www.readbyqxmd.com/read/27187129/effectiveness-versus-efficacy-of-calabadion-and-sugammadex-for-nondepolarizing-neuromuscular-blocking-agent-reversal
#2
Grace Lim, Douglas P Landsittel
No abstract text is available yet for this article.
June 2016: Anesthesiology
https://www.readbyqxmd.com/read/26799963/reversing-neuromuscular-blockade-inhibitors-of-the-acetylcholinesterase-versus-the-encapsulating-agents-sugammadex-and-calabadion
#3
REVIEW
Friederike Haerter, Matthias Eikermann
INTRODUCTION: Acetylcholinesterase inhibitors (neostigmine, edrophonium) and encapsulating agents (sugammadex and calabadion) can be used to reverse residual neuromuscular blockade (NMB). AREAS COVERED: This review provides information about efficacy, effectiveness, and side effects of drugs (acetylcholinesterase inhibitors and encapsulating agents) used to reverse neuromuscular blocking agents (NMBAs). EXPERT OPINION: The therapeutic range of acetylcholinesterase-inhibitors is narrow and effectiveness studies demonstrate clinicians don't use these unspecific reversal agents effectively to increase postoperative respiratory safety...
2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/26648135/in-vitro-selectivity-of-an-acyclic-cucurbit-n-uril-molecular-container-towards-neuromuscular-blocking-agents-relative-to-commonly-used-drugs
#4
Shweta Ganapati, Peter Y Zavalij, Matthias Eikermann, Lyle Isaacs
An acyclic cucurbit[n]uril (CB[n]) based molecular container (2, a.k.a. Calabadion 2) binds to both amino-steroidal and benzylisoquinolinium type neuromuscular blocking agents (NMBAs) in vitro, and reverses the effect of these drugs in vivo displaying faster recovery times than placebo and the γ-cyclodextrin (CD) based and clinically used reversal agent Sugammadex. In this study we have assessed the potential for other drugs commonly used during and after surgery (e.g. antibiotics, antihistamines, and antiarrhythmics) to interfere with the ability of 2 to bind NMBAs rocuronium and cisatracurium in vitro...
January 28, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/26418697/comparative-effectiveness-of-calabadion-and-sugammadex-to-reverse-non-depolarizing-neuromuscular-blocking-agents
#5
COMPARATIVE STUDY
Friederike Haerter, Jeroen Cedric Peter Simons, Urs Foerster, Ingrid Moreno Duarte, Daniel Diaz-Gil, Shweta Ganapati, Katharina Eikermann-Haerter, Cenk Ayata, Ben Zhang, Manfred Blobner, Lyle Isaacs, Matthias Eikermann
BACKGROUND: The authors evaluated the comparative effectiveness of calabadion 2 to reverse non-depolarizing neuromuscular-blocking agents (NMBAs) by binding and inactivation. METHODS: The dose-response relationship of drugs to reverse vecuronium-, rocuronium-, and cisatracurium-induced neuromuscular block (NMB) was evaluated in vitro (competition binding assays and urine analysis), ex vivo (n = 34; phrenic nerve hemidiaphragm preparation), and in vivo (n = 108; quadriceps femoris muscle of the rat)...
December 2015: Anesthesiology
https://www.readbyqxmd.com/read/26087274/novel-neuromuscular-blocking-drugs-and-antagonists
#6
REVIEW
Paul M Heerdt, Hiroshi Sunaga, John J Savarese
PURPOSE OF REVIEW: This review summarizes recent progress in the development of new muscle relaxants that are inactivated by cysteine, and considers the evolving paradigm of selective relaxant binding or degrading agents that can reverse neuromuscular blockade at any time. RECENT FINDINGS: The benzylisoquinoline compound gantacurium is a nondepolarizing muscle relaxant with an ultrashort duration largely determined by the rapid rate at which endogenous L-cysteine binds to, and permanently inactivates, the molecule...
August 2015: Current Opinion in Anaesthesiology
https://www.readbyqxmd.com/read/25530723/residual-paralysis-does-it-influence-outcome-after-ambulatory-surgery
#7
Hassan Farhan, Ingrid Moreno-Duarte, Duncan McLean, Matthias Eikermann
Neuromuscular blocking agents are used to facilitate tracheal intubation in patients undergoing ambulatory surgery. The use of high-dose neuromuscular blocking agents to achieve muscle paralysis throughout the case carries an increased risk of residual post-operative neuromuscular blockade, which is associated with increased respiratory morbidity. Visually monitoring the train-of-four (TOF) fade is not sensitive enough to detect a TOF fade between 0.4 and 0.9. A ratio <0.9 indicates inadequate recovery. Quantitative neuromuscular transmission monitoring (e...
December 2014: Current Anesthesiology Reports
https://www.readbyqxmd.com/read/24215347/cucurbit-n-uril-type-hosts-for-the-reversal-of-steroidal-neuromuscular-blocking-agents
#8
REVIEW
Donal H Macartney
The ideal neuromuscular blocking agent (NMBA) is regarded as being a non-depolarizing equivalent of succinylcholine, having a rapid onset and short duration of action, with minimal side effects. In the absence of a single drug, the administration of an aminosteroid NMBA, such as rocuronium, followed by reversal using an acetylcholinesterase inhibitor, such as neostigmine, is commonly employed. A different and safer approach to rapidly reversing the action of the NMBA, by encapsulating it with a macrocyclic or acyclic host molecule, such as the cyclodextrin sugammadex or more recently, cucurbituril-type hosts such as cyclic cucurbit[7]uril and the acyclic glycoluril tetramer calabadion 1, is described...
November 2013: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/23549405/calabadion-a-new-agent-to-reverse-the-effects-of-benzylisoquinoline-and-steroidal-neuromuscular-blocking-agents
#9
Ulrike Hoffmann, Martina Grosse-Sundrup, Katharina Eikermann-Haerter, Sebastina Zaremba, Cenk Ayata, Ben Zhang, Da Ma, Lyle Isaacs, Matthias Eikermann
INTRODUCTION: To evaluate whether calabadion 1, an acyclic member of the Cucurbit[n]uril family of molecular containers, reverses benzylisoquinoline and steroidal neuromuscular-blocking agent effects. METHODS: A total of 60 rats were anesthetized, tracheotomized, and instrumented with IV and arterial catheters. Rocuronium (3.5 mg/kg) or cisatracurium (0.6 mg/kg) was administered and neuromuscular transmission quantified by acceleromyography. Calabadion 1 at 30, 60, and 90 mg/kg (for rocuronium) or 90, 120, and 150 mg/kg (for cisatracurium), or neostigmine/glycopyrrolate at 0...
August 2013: Anesthesiology
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