The doughnut and the hole: a new pharmacological concept for anaesthetists

Hunter, Jennifer M.; Flockton, E.

doi:10.1093/bja/ael158

Cited by 58 publications

(30 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It does not have any effect on ACh concentration or on its metabolism nor on nicotinic or muscarinic receptors. It has a donut-like structure, and its power to encapsulate rocuronium into its cavity is very strong (Figure 1) (47,69,95,98). This strength was clinically illustrated by Cammu et al who administered simultaneously but in opposite arms rocuronium 1.2 mgAEkg )1 and sugammadex either 16, 20 or 32 mgAEkg )1 and found that all volunteers maintained a TOF ratio at ‡0.90 at all times during the study period (99).…”

Section: Clinical Effects Of Sugammadexmentioning

confidence: 97%

“…Anticholinesterases inhibit acetylcholinesterase throughout the body, not only at nicotinic receptors of the neuromuscular junction. The effects of neostigmine mediated via muscarinic receptors include bradycardia, hypotension, salivation, increased gastrointestinal motility, and bronchospasm (95). To counteract these severe untoward effects, an antimuscarinic drug, like atropine or glycopyrrolate, has to be coadministered with anticholinesterases.…”

Section: Clinical Effects Of Anticholinesterasesmentioning

confidence: 99%

See 1 more Smart Citation

Neuromuscular block and current treatment strategies for its reversal in children

Meretoja

2010

Pediatric Anesthesia

View full text Add to dashboard Cite

Even though neuromuscular blocking agents are an essential part of balanced anesthesia and the risks of residual paralysis are well documented, many anesthetists seldomly monitor neuromuscular block. Classical reversal agent neostigmine is unable to antagonise a deep neuromuscular block and is rather slow to antagonise even a moderate block. These caveats may have introduced a practice to use muscle relaxants mainly for an endotracheal intubation. This review presents current views on the effects of muscle relaxants and their reversal agents in pediatric patients. This may help clinicians to reconsider the value of muscle relaxants during anesthesia in children.

show abstract

Section: Clinical Effects Of Sugammadexmentioning

confidence: 97%

Section: Clinical Effects Of Anticholinesterasesmentioning

confidence: 99%

Neuromuscular block and current treatment strategies for its reversal in children

Meretoja

2010

Pediatric Anesthesia

View full text Add to dashboard Cite

show abstract

“…The structure of this modified ␥-cyclodextrin is such that all four hydrophobic rings of the steroidal neuromuscular blocking agent fit within the concentric doughnut shape of sugammadex, forming a tight 1:1 complex between sugammadex and the aminosteroid-based relaxant. 38,39 To facilitate binding, this cyclodextrin was further modified with a series of acidic functional groups to form an electrostatic interaction with the positive nitrogen of the blocker (Figure 2). 37,40 Due to the structural specificity, sugammadex does not diminish the effects of nondepolarizing agents of the benzylisoquinolinium class.…”

Section: Pharmacologymentioning

confidence: 99%

Sugammadex: A Novel Agent for the Reversal of Neuromuscular Blockade

2007

View full text Add to dashboard Cite

To achieve spontaneous ventilation after completion of surgery, the nondepolarizing effects on skeletal muscle relaxation are often reversed by administration of an acetylcholinesterase inhibitor. However, these agents increase acetylcholine at both the neuromuscular junction and the muscarinic receptors. Therefore, coadministration of an anticholinergic agent is required to prevent parasympathetic adverse effects. In addition, a relative pharmacologic ceiling effect is seen with inhibition of acetylcholinesterase, necessitating some recovery of neuromuscular function before an acetylcholinesterase inhibitor is administered. Sugammadex is a new modified gamma-cyclodextrin compound under clinical investigation in the United States. It does not interact with cholinergic mechanisms to elicit reversal. Instead, it is a selective relaxant binding agent and acts by forming a 1:1 complex with steroidal nondepolarizing neuromuscular blockers in the plasma, lowering the effective concentration available at the receptor. Due to its selectivity, sugammadex does not inhibit the effects of nondepolarizing agents of the benzylisoquinolinium class. In contrast to acetylcholinesterase inhibition, sugammadex is effective even when administered during profound blockade, and it does not require coadministration of an anticholinergic agent. It provides a novel mechanism of action for reversal of the neuromuscular block induced by nondepolarizing aminosteroidal agents.

show abstract

“…cisatracurium, vecuronium, and rocuronium) neuromuscular blocking drugs should be used [100]. A novel cyclodextrin compound, namely sugammadex [101], can facilitate more rapid reversal of steroid-based, nondepolarizing neuromuscular blockers than a combination of either edrophonium-atropine or neostigmine-glycopyrrolate, without anticholinergic side effects [102 ]. Use of this reversal agent may also lead to earlier tracheal extubation after surgery and reduce postoperative respiratory complications caused by residual muscle paralysis.…”

Section: General Anesthesiamentioning

confidence: 99%

Fast-track anesthetic techniques for ambulatory surgery

White

Eng

2007

Current Opinion in Anaesthesiology

View full text Add to dashboard Cite

The pivotal role played by the anesthesiologist as the key perioperative physician in facilitating the recovery process has assumed increased importance in the current outpatient fast-track recovery environment. The choice of premedication, anesthetic, analgesic and antiemetic drugs, as well as cardiovascular, hormonal and fluid therapies, can all influence the ability to fast-track outpatients after ambulatory surgery.

show abstract

The doughnut and the hole: a new pharmacological concept for anaesthetists

Cited by 58 publications

References 14 publications

Neuromuscular block and current treatment strategies for its reversal in children

Neuromuscular block and current treatment strategies for its reversal in children

Sugammadex: A Novel Agent for the Reversal of Neuromuscular Blockade

Fast-track anesthetic techniques for ambulatory surgery

Contact Info

Product

Resources

About