Neuromuscular block
The primary target of Sugammadex sodium is the neuromuscular blocking agents rocuronium and vecuronium. It acts as a selective relaxant binding agent, forming a 1:1 complex with these drugs. The complex is then excreted renally. By binding to and encapsulating the neuromuscular blocking agents, sugammadex rapidly reverses their effects, restoring neuromuscular function.

Sugammadex at concentrations of 50 and 100 μg/mL significantly enhanced the cell viability in C6 cells after the cytotoxicity induced by glutamate (p < 0.001). Moreover, sugammadex considerably decreased the levels of nNOS NO and TOS and the number of apoptotic cells and increased the level of TAS (p < 0.001). Sugammadex has protective and antioxidant properties on cytotoxicity and could be an effective supplement for neurodegenerative diseases such as Alzheimer and Parkinson if further research in vivo supports this claim[5].
In vitro, sugammadex sodium has been shown to bind to rocuronium and vecuronium with high affinity. It forms a stable complex with these drugs, preventing them from interacting with the nicotinic receptor. The compound's binding affinity and selectivity have been confirmed in various in vitro studies.

Rats given sugammadex (100 mg/kg, intravenous injection, once) at the start of reperfusion an hour after ischemia show protective effects against kidney damage [2
In vivo, sugammadex sodium is used for the reversal of neuromuscular blockade induced by rocuronium and vecuronium during surgery. It is administered intravenously and rapidly reverses the effects of these muscle relaxants. The compound is effective in both children and adults. It is approved for use in many countries.

In vitro enzyme or receptor binding assays for sugammadex sodium involve studying its binding to rocuronium and vecuronium. The binding affinity can be measured using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The inhibition of the interaction between the neuromuscular blocking agents and the nicotinic receptor can be assessed using competitive binding assays.

This experiment was intended to evaluate the effect of sugammadex on the cytotoxicity induced by glutamate, involving the nitric oxide and oxidative stress pathways. C6 glioma cells were used in the study. Glutamate was given to cells in the glutamate group for 24 h. Sugammadex at different concentrations was given to cells in the sugammadex group for 24 h. Cells in the sugammadex + glutamate group were pre-treated with sugammadex at various concentrations for 1 h and then exposed to glutamate for 24 h. XTT assay was used to assess cell viability. Levels of nitric oxide (NO), neuronal nitric oxide synthase (nNOS), total antioxidant (TAS), and total oxidant (TOS) in the cells were calculated using commercial kits. Apoptosis was detected by TUNEL assay[5].
In vitro cell-based assays for sugammadex sodium are not typically performed, as it does not have direct biological activity on cells. Its effects are mediated through the binding of neuromuscular blocking agents. The compound's activity is assessed in functional assays measuring muscle contraction.

Methods: Four female rhesus monkeys each underwent three experiments. In each experiment, first, a 100-microg/kg dose of rocuronium was injected and spontaneous recovery was monitored. After full recovery, a 500-microg/kg dose of rocuronium was injected. Up to this point, all three experiments in a single monkey were identical. One minute after this rocuronium injection, either one of the two tested dosages of sugammadex (1.0 or 2.5 mg/kg) was injected or saline was injected.[1]
Results: Injection of 100 microg/kg rocuronium resulted in a mean neuromuscular blockade of 93.0% (SD = 4%), and profound blockade was achieved by injection of 500 microg/kg. In all experiments, a 100% neuromuscular blockade was achieved at this dose. After injection of the high rocuronium dose, the 90% recovery of the train-of-four ratio took 28 min (SD = 7 min) after saline, 26 min (SD = 9.5 min) after 1 mg/kg sugammadex, and 8 min (SD = 3.6 min) after 2.5 mg/kg sugammadex. Signs of residual blockade or recurarization were not observed. Injection of sugammadex had no significant effects on blood pressure or heart rate.[1]
Conclusions: Chemical encapsulation of rocuronium by sugammadex is a new therapeutic mechanism allowing effective and rapid reversal of profound neuromuscular blockade induced by rocuronium in anesthetized rhesus monkeys.[1]
In vivo animal experiments for sugammadex sodium are conducted using animal models to study its efficacy in reversing neuromuscular blockade. The compound is administered intravenously, and muscle function is assessed using electromyography or by measuring the train-of-four (TOF) ratio. The reversal of neuromuscular blockade is evaluated.

Pharmacokinetic (PK) properties of sugammadex sodium indicate that it is administered intravenously. The compound has a molecular weight of 2178.01 and a molecular formula of C72H104Na8O48S8. It is a modified γ-cyclodextrin. The compound is rapidly distributed and is excreted unchanged in the urine. Its half-life is approximately 2-3 hours.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Currently, there is no information on the clinical use of sugammadex sodium during lactation. Because sugammadex sodium is a large, highly polar drug with a molecular weight of 2002 Da, its concentration in breast milk is likely to be very low, and oral absorption by the infant is unlikely. Use of sugammadex sodium during lactation is acceptable.
◉ Effects on Breastfed Infants
As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
As of the revision date, no relevant published information was found.
Toxicology (toxicology) data for sugammadex sodium indicate that it is generally well-tolerated. Common side effects may include headache, nausea, and vomiting. The compound may also cause a decrease in heart rate and blood pressure. Rare but serious side effects include anaphylaxis and bronchospasm.

[1]. de Boer HD, et al. Sugammadex, a new reversal agent for neuromuscular block induced by rocuronium in the anaesthetized Rhesus monkey. Br J Anaesth. 2006 Apr;96(4):473-9. Epub 2006 Feb 7.
[2]. Tercan M, Yılmaz İnal F, Seneldir H, Kocoglu H. Nephroprotective Efficacy of Sugammadex in Ischemia-Reperfusion Injury: An Experimental Study in a Rat Model. Cureus. 2021 Jun 17;13(6):e15726.
[3]. de Boer HD, et al. Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized rhesus monkeys. Anesthesiology. 2006 Apr;104(4):718-23.
[4]. de Boer HD, et al. Time course of action of sugammadex (Org 25969) on rocuronium-induced block in the Rhesus monkey, using a simple model of equilibration of complex formation. Br J Anaesth. 2006 Nov;97(5):681-6. Epub 2006 Oct.
[5]. Fundam Clin Pharmacol . 2023 Aug;37(4):786-793. doi: 10.1111/fcp.12890. Epub 2023 Mar 14.

Sugammadextrose sodium is an organic sodium salt, the octasodium salt of sugammadextrose. It is used to reverse neuromuscular blockade induced by rocuronium and vecuronium bromide in adult surgery. It is a neuromuscular blocking agent. It contains a sugammadextrose (8-) group. Sugammadextrose sodium is the sodium salt form of sugammadextrose, a bioinert selective muscle relaxant binder (SRBA) composed of a modified anionic γ-cyclodextrin derivative with a hydrophilic outer layer and a hydrophobic core, exhibiting neuromuscular blocking agent (NMBD) reversal activity. After administration, the negatively charged carboxysulfide group of sugammadextrose selectively and reversibly binds to the positively charged quaternary ammonium nitrogen atom of previously used steroidal NMBDs (such as rocuronium and vecuronium bromide) for anesthesia. The encapsulation of neuromuscular blocking agents (NMBDs) by sugammadextrose sodium blocks their binding to nicotine receptors at the neuromuscular junction, thereby reversing NMBD-induced neuromuscular blockade.
A gamma-cyclodextrin that can be used as a reversal agent for the neuromuscular blocking agent rocuronium bromide.
See also: Sugampazone sodium (containing the active ingredient).

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Drug Indications
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide in adults. For children: Sugampazone sodium is recommended only for routine reversal of neuromuscular blockade caused by rocuronium bromide in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide. For pediatric patients: Sugampazone sodium is recommended only for routine reversal of neuromuscular blockade caused by rocuronium bromide in children and adolescents.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide in adults.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide. For pediatric patients: Sugampazone sodium is recommended only for routine reversal of neuromuscular blockade caused by rocuronium bromide in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide in adults. For pediatric patients: Sugammadex sodium is recommended only for routine reversal of rocuronium-induced neuromuscular blockade in children and adolescents aged 2 to 17 years. It is also recommended for reversing rocuronium or vecuronium-induced neuromuscular blockade in adults. For pediatric patients: Sugammadex sodium is recommended only for routine reversal of rocuronium-induced neuromuscular blockade in children and adolescents aged 2 to 17 years.
Other information: Sugammadex sodium is marketed under the brand name Bridion. It is a selective relaxant binding agent used for the reversal of neuromuscular blockade induced by rocuronium and vecuronium. Its CAS number is 343306-79-6.

C72H104NA8O48S8

2177.9742

2176.26

C, 39.71; H, 4.81; Na, 8.44; O, 35.26; S, 11.78

343306-79-6

Sugammadex;343306-71-8

6918584

Typically exists as white to off-white solids at room temperature

1.275g/cm3 （计算值）

16

56

32

136

2790

40

S(C([H])([H])C([H])([H])C(=O)[O-])C([H])([H])[C@]1([H])[C@]2([H])[C@@]([H])([C@]([H])([C@]([H])(O1)O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O2)O[H])O[H].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

KMGKABOMYQLLDJ-LHCKBTHCSA-F

InChI=1S/C72H112O48S8.8Na/c73-33(74)1-9-121-17-25-57-41(89)49(97)65(105-25)114-58-26(18-122-10-2-34(75)76)107-67(51(99)43(58)91)116-60-28(20-124-12-4-36(79)80)109-69(53(101)45(60)93)118-62-30(22-126-14-6-38(83)84)111-71(55(103)47(62)95)120-64-32(24-128-16-8-40(87)88)112-72(56(104)48(64)96)119-63-31(23-127-15-7-39(85)86)110-70(54(102)46(63)94)117-61-29(21-125-13-5-37(81)82)108-68(52(100)44(61)92)115-59-27(19-123-11-3-35(77)78)106-66(113-57)50(98)42(59)90;;;;;;;;/h25-32,41-72,89-104H,1-24H2,(H,73,74)(H,75,76)(H,77,78)(H,79,80)(H,81,82)(H,83,84)(H,85,86)(H,87,88);;;;;;;;/q;8*+1/p-8/t25?,26?,27?,28?,29?,30?,31?,32?,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57+,58+,59+,60+,61+,62+,63+,64+,65+,66+,67+,68+,69+,70+,71+,72?;;;;;;;;/m0......../s1

6A,6B,6C,6D,6E,6F,6G,6H-octakis-S-(2-Carboxyethyl)-6A,6B,6C,6D,6E,6F,6G,6H-octathio-γ-cyclodextrin sodium salt

trade name: Bridion. Sugammadex sodium; Org25969; Org-25969; Org 25969; 361LPM2T56; Sugammadex; trade name: Bridion. Sugammadex sodium

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~45.91 mM)

Solubility in Formulation 1: 100 mg/mL (45.91 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)