Sugammadex sodium

• CAT Number: I003249
• CAS Number: 343306-79-6
• Molecular Formula: C72H104Na8O48S8
• Molecular Weight: 2178.01
• Purity: ≥95%
• Solubility: H2O: ≥ 34 mg/mL
• Storage: Store at -20°C
• Related CAS: 343306-71-8(free acid)

Sugammadex sodium(CAT: I003249) is a synthetic derivative of γ-cyclodextrin and serves as a novel reversal agent for neuromuscular blockade. It is used to rapidly reverse the effects of neuromuscular blocking agents, such as rocuronium or vecuronium, which are commonly administered during surgical procedures to induce muscle relaxation. Sugammadex sodium works by encapsulating the neuromuscular blocking agent molecule, forming a stable complex that prevents it from binding to its target receptors, thereby facilitating its elimination from the body. This mechanism allows for a quicker recovery of muscle function and reversal of paralysis, enhancing patient safety and reducing the risk of postoperative complications.

Reference

1. Curr Opin Anaesthesiol. 2007 Aug;20(4):307-10.

Sugammadex: a novel neuromuscular blocker binding agent.

Fields AM(1), Vadivelu N.

Author information:
(1)Department of Anesthesiology, Yale University School of Medicine, New Haven,
CT 06520-8051, USA.

PURPOSE OF REVIEW: Sugammadex is a novel drug that binds selected neuromuscular
blocking drugs and prevents them from acting at the neuromuscular junction. Due
to its rapid onset and relative lack of side effects, this drug promises to
change the method of anesthesia delivery. This review summarizes the literature
on the drug and addresses some of the potential changes that it may bring.
RECENT FINDINGS: Currently in phase III clinical trials, sugammadex has been
shown to be safe and efficacious in small animal and human study groups and is
now undergoing wider clinical testing to secure FDA approval for general use.
SUMMARY: Sugammadex binds neuromuscular blocking drugs and encapsulates them,
making cholinesterase inhibitors unnecessary. Its rapid reversal of blockade
makes it possible to keep patients profoundly muscle relaxed until drapes come
down and it can enable a rapid return to spontaneous ventilation in a /’cannot
intubate, cannot ventilate/’ situation. Costs and date of availability have yet to
be determined.

2. Anesth Analg. 2007 Mar;104(3):575-81.

Sugammadex: another milestone in clinical neuromuscular pharmacology.

Naguib M(1).

Author information:
(1)Department of Anesthesiology and Pain Medicine, Unit 409, Anderson Cancer
Center, The University of Texas M. D., Houston, Texas 77030, USA.


Comment in
Anesth Analg. 2007 Nov;105(5):1506; author reply 1506-7.

Sugammadex is a revolutionary investigational reversal drug currently undergoing
Phase III testing whose introduction into clinical practice may change the face
of clinical neuromuscular pharmacology. A modified gamma-cyclodextrin, sugammadex
exerts its effect by forming very tight water-soluble complexes at a 1:1 ratio
with steroidal neuromuscular blocking drugs (rocuronium > vecuronium >>
pancuronium). During rocuronium-induced neuromuscular blockade, the IV
administration of sugammadex creates a concentration gradient favoring the
movement of rocuronium molecules from the neuromuscular junction back into the
plasma, which results in a fast recovery of neuromuscular function. Sugammadex is
biologically inactive, does not bind to plasma proteins, and appears to be safe
and well tolerated. Additionally, it has no effect on acetylcholinesterase or any
receptor system in the body. The compound/’s efficacy as an antagonist does not
appear to rely on renal excretion of the cyclodextrin-relaxant complex. Human and
animal studies have demonstrated that sugammadex can reverse very deep
neuromuscular blockade induced by rocuronium without muscle weakness. Its future
clinical use should decrease the incidence of postoperative muscle weakness, and
thus contribute to increased patient safety. Sugammadex will also facilitate the
use of rocuronium for rapid sequence induction of anesthesia by providing a
faster onset-offset profile than that seen with 1.0 mg/kg succinylcholine.
Furthermore, no additional anticholinesterase or anticholinergic drugs would be
needed for antagonism of residual neuromuscular blockade, which would mean the
end of the cardiovascular and other side effects of these compounds. The clinical
use of sugammadex promises to eliminate many of the shortcomings in our current
practice with regard to the antagonism of rocuronium and possibly other steroidal
neuromuscular blockers.

3. AANA J. 2006 Oct;74(5):357-63.

New drug sugammadex: a selective relaxant binding agent.

Welliver M(1).

Author information:
(1)University of Florida & Shands Health Science Center, Jacksonville, USA.


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.