Neuromuscular block

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].

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

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].

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]

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the clinical use of sugammadex during breastfeeding. Because sugammadex is a large, highly polar molecule with a molecular weight of 2002 Da., the amount in milk is likely to be very low and oral absorption by the infant is unlikely. Sugammadex is acceptable to use during breastfeeding.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[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.

Sugammadex sodium is an organic sodium salt that is the octasodium salt of sugammadex. Used for reversal of neuromuscular blockade induced by rocuronium and vecuronium in adults undergoing surgery. It has a role as a neuromuscular agent. It contains a sugammadex(8-).
Sugammadex Sodium is the sodium salt form of sugammadex, a biologically inert, selective relaxant binding agent (SRBA) composed of a modified, anionic gamma cyclodextrin derivative containing a hydrophilic exterior and a hydrophobic core, with neuromuscular blocking drug (NMBD) reversal activity. Upon administration, the negatively charged carboxyl-thio-ether groups of sugammadex selectively and reversibly bind to the positively charged quaternary nitrogen of a steroidal NMBD, such as rocuronium and vecuronium, which was administered at an earlier time for anesthetic purposes. The encapsulation of the NMBD by sugammadex blocks its ability to bind to nicotinic receptors in the neuromuscular junction and thereby reverses the NMBD-induced neuromuscular blockade.
A gamma-cyclodextrin that functions as a reversal agent for the neuromuscular blocker ROCURONIUM BROMIDE.
See also: Sugammadex (has active moiety).

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Drug Indication
Reversal of neuromuscular blockade induced by rocuronium or vecuronium in adults. For the paediatric population: sugammadex is only recommended for routine reversal of rocuronium induced blockade in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade induced by rocuronium or vecuronium. For the peadiatric population: sugammadex is only recommended for routine reversal of rocuronium-induced blockade in children and adolescents.
Reversal of neuromuscular blockade induced by rocuronium or vecuronium in adults.
Reversal of neuromuscular blockade induced by rocuronium or vecuronium. For the paediatric population: sugammadex is only recommended for routine reversal of rocuronium induced blockade in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade induced by   rocuronium or vecuronium in adults. For the paediatric population: sugammadex is only recommended for routine reversal of rocuronium induced blockade in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade induced by rocuronium or vecuronium in adults. For the paediatric population: sugammadex is only recommended for routine reversal of rocuronium induced blockade in children and adolescents aged 2 to 17 years.

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.)