Sugammadex
Sugammadex is a medication prescribed in the reversal of neuromuscular blockade induced by rocuronium and vecuronium. It is the first selective relaxant binding agent (SRBA) in general anesthesia. Usage of the aminosteroid non-depolarizing neuromuscular-blocking agents such as vecuronium or rocuronium results in the neuromuscular blockade. Sugammadex is a unique and novel cyclodextrin. Termed a neuromuscular reversal drug, it is the first in a new class of selective relaxant binding agents, which reverse neuromuscular blockade. Sugammadex is effective in reversing moderate or deep cases of neuromuscular blockade. Doctors around the world are looking forward to sugammadex eliminating many of the shortcomings of the general anesthetic practice, specifically in the context of antagonism to rocuronium and other aminosteroid muscle relaxants.
Sugammadex is sold under the brand name Bridion.
Merck pharm now owns and sells Sugammdex. However, Organon pharmaceutical company at the Newhouse Research Site in Scotland discovered Sugammdex but Organon was bought by Schering-Plough in 2007. Schering-Plough later merged with Merck in 2009.
While Sugammadex got approval for use in the European Union in 2008, the US Food and Drug Administration initially rejected Schering-Plough’s New Drug Application for Sugammadex in 2008. However, it was eventually approved for sales in the United States in 2015.
Forms and Dose
Sugammadex is both available and administered as a single bolus injection.
For reversing the neurotransmission blockage by rocuronium and vecuronium, the standard adult dose is 4 mg per kilo of body weight. If spontaneous recovery of the twitch response has reached 1 to 2 post-tetanic counts and there are no twitch responses to train-of-four stimulation, the recommended adult dose is 2 mg per kilo of body weight is recommended if spontaneous recovery has reached the reappearance of the second twitch in response to TOF stimulation. For reversing Rocuronium effects only, the recommended adult dose is 16 mg per kilo if there is a clinical need to reverse neuromuscular blockade soon within 3 minutes of administration of a single dose of 1.2 mg per kilo.
The price of Sugammadex
In the USA, consumers have to pay around $1,103 for a supply of 20 milliliters for an intravenous solution (100 mg/mL). and in Australia, the cost of a 200mg vial of Sugammadex varies from A$45 to 195, depending on the brand.
How does Sugammadex work?
Sugammadex actions in the body deactivate rocuronium. It does this encapsulating the free molecule to form a stable complex. Sugammadex exerts its effect by forming very tight complexes at a 1:1 ratio with aminosteroid muscle relaxants creating intermolecular forces, thermodynamic bonds, and hydrophobic interactions. To make a tight sugammadex–rocuronium complex. This complex has a very high association rate and a very low dissociation rate. This results in a reduction in free rocuronium plasma concentration. So it creates a gradient between the tissue compartment and plasma so that the free rocuronium moves from tissue to plasma, with a reduction in nicotinic receptor occupancy at the Neuro-Muscular Junction.
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