Sugammadex: Clinical Pharmacokinetics and Pharmacodynamics
Purpose of Review
The purpose of this chapter is to provide an evidence based understanding of the pharmacokinetics and pharmacodynamics of sugammadex.
Sugammadex is a c-cyclodextrin that rapidly reverses the effect of aminosteroid nondepolarizing neuromuscular blocking agents (NMBAs) rocuronium and vecuronium by forming an inactive 1:1 complex. It is only available in an intravenous form with a bioavailabilty of 100%. It does not bind to plasma proteins and is eliminated unchanged by the kidneys. The type of NMBA used and the degree of the residual neuromuscular blockade at the time of administration determine the dose of sugammadex needed and the speed of reversal. Plasma levels of exogenous compounds with similar steroidal structure, such as some hormones, hormonal contraceptives, and pheromones may also be reduced following administration of sugammadex. While the package insert does not indicate dosage adjustments in elderly patients, or those with hepatic, cardiac, pulmonary comorbidities (not approved in pediatric patients less than 18 years or patients with a creatinine clearance less than 30 ml/min), sugammadex dosing possibly should be adjusted based upon the patient’s age and comorbidities, including liver or kidney failure and morbid obesity.
Sugammadex has been shown to be an effective agent in reversing the effects of NMBAs with an acceptable safety and efficacy profile.
KeywordsSugammadex Pharmacokinetics Pharmacodynamics Clinical therapeutics
The authors wish to thank Nathaniel Bailey, MD, and Chrisana Grande, PhD, of Merck, for providing editorial support and references for the Bleeding section and for sharing insight and information on Drug Interactions and Affinity. The section on Sugammadex and Bleeding was adapted and modified from an unpublished, limited distribution monograph provided by Merck.
Compliance with Ethical Standards
Conflict of Interest
Jennifer Nguyen-Lee declares that she has no conflict of interest.
Natalie Moreland declares that she has no conflict of interest.
Alireza Sadoughi declares that he has no conflict of interest.
Reza Borna declares that he has no conflict of interest.
Ali Salehi declares that he has no conflict of interest.
Jonathan S. Jahr has received compensation for service on a speaker’s bureau from Merck, the manufacturer of sugammadex.
Human and Animal Rights and Informed Consent
This article does not contain any studies with human or animal subjects performed by any of the authors.
Papers of particular interest, published recently, have been highlighted as: • Of importance •• Of major importance
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