Rocuronium bromide is a
competitive antagonist for the
nicotinic acetylcholine receptors at the neuromuscular junction. Of the
neuromuscular-blocking drugs it is considered to be a non-depolarizing neuromuscular junction blocker, because it acts by dampening the receptor action causing muscle relaxation, instead of continual depolarisation which is the mechanism of action of the depolarizing neuromuscular junction blockers, like
succinylcholine.
It was designed to be a weaker antagonist at the neuromuscular junction than
pancuronium; hence its monoquaternary structure and its having an
allyl group and a pyrrolidine group attached to the D ring quaternary nitrogen atom. Rocuronium has a rapid onset and intermediate duration of action.[2]
There is considered to be a risk of allergic reaction to the drug in some patients (particularly those with
asthma), but a similar incidence of allergic reactions has been observed by using other members of the same drug class (non-depolarizing neuromuscular blocking drugs).[3]
The γ-
cyclodextrin derivative
sugammadex (trade name Bridion) is an agent to reverse the action of rocuronium by binding to it with high affinity.[4] Sugammadex has been in use since 2009 in many European countries; however, it was turned down for approval twice by the US FDA due to concerns over allergic reactions and bleeding,[5] but finally approved the medication for use during surgical procedures in the United States on December 15, 2015.[6] The acetylcholinesterase inhibitor
neostigmine can also be used as a reversal agent of rocuronium but is not as effective as sugammadex. Neostigmine is often still used due to its low cost compared with sugammadex.[7]
History
It was introduced in 1994, and is marketed under the trade name of Zemuron in the
United States and Esmeron in most other countries.
On October 3, 2016, the U.S. state of
Ohio announced that it would resume executions on January 12, 2017, using a combination of
midazolam, rocuronium bromide, and
potassium chloride. Prior to this, the last execution in Ohio was in January 2014.[9]
^Carron M, Zarantonello F, Tellaroli P, Ori C (December 2016). "Efficacy and safety of sugammadex compared to neostigmine for reversal of neuromuscular blockade: a meta-analysis of randomized controlled trials". Journal of Clinical Anesthesia. 35: 1–12.
doi:
10.1016/j.jclinane.2016.06.018.
PMID27871504.