Sugammadex Sodium

Sugammadex sodium is a synthetic γ-cyclodextrin derivative, and acts as a new reversal agent for neuromuscular block.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

Injection of sugammadex has no significant effects on blood pressure or heart rate. After injection of the high rocuronium dose, the 90% recovery of the train-of-four ratio takes 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[1]. Sugammadex causes a rapid and complete reversal of rocuronium-induced neuromuscular block. The recovery time to train of four ratio=0.9 after spontaneous recovery is 14.4 min (SD=3.4 min; n=14). This is reduced significantly to 3.7 min (SD=3.3 min; n=4) with sugammadex 0.5 mg/kg and to 1.9 min (SD=1.0 min; n=4) with sugammadex 1.0 mg/kg[2]. The estimated half-life of sugammadex in Rhesus monkey is 30 (SEM=4.9) min[3].

Female rhesus monkeys with a body weight of 5.2-7.1 kg are sedated with 10 mg/kg ketamine intramuscularly. Two intravenous lines are placed: one for anesthetic administration, including rocuronium, the other for test drug administration. This is followed by intravenous injection of 25 mg/kg pentobarbitone sodium and a subsequent continuous infusion of 5-10 mg/kg/h. The monkeys are intubated endotracheally, and the lungs are ventilated with a mixture of oxygen and nitrous oxide (volume ratio of 2:3). Four animals are each studied on three different occasions. The occasions differed by the administration of either saline or a low (1.0 mg/kg) or high (2.5 mg/kg) dose of sugammadex. Between the experiments, the monkeys recover for at least 6 weeks. Heart rate and oxygen saturation are determined at the ear with a pulse oximeter. Blood pressure is determined with a cuff placed around the tail. Body temperature is measured by a rectal probe and kept at 37°C-38°C.

[1]. de Boer HD, et al. Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized rhesus monkeys. Anesthesiology. 2006 Apr;104(4):718-23.

[2]. 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.

[3]. 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 3.

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