Rocuronium bromide

Chemical properties

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The Uses of Rocuronium bromide

A non-depolarizing neuromuscular blocker used in anesthesia to help insert breathing tubes.

The Uses of Rocuronium bromide

Aminosteroid, competitive neuromuscular blocker

Description

Rocuronium bromide is a short-acting nondepolarizing steroidal neuromuscular blocker introduced in the U.S.A as Zemuron and in the United Kingdom as Esmeron. k is indicated for use as an adjunct to general anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Rocuroniurn bromide has a significantly more rapid onset than other intermediate acting neuromuscular blockers, comparable to succinylcholine but with a very stable cardiovascular profile and has an improved side effect profile. It has been reported that good to excellent intubation conditions were achieved only one minute after a bolus dose of 600μg/kg of rocuronium bromide. It has a short duration of action, therefore, is useful for rapid sequence intubation without unacceptable delays in the spontaneous recovery of neuromuscular function.

Originator

Organon (Netherlands)

What are the applications of Application

Rocuronium bromide is a non-depolarizing neuromuscular blocker used in anesthesia to help insert breathing tubes

Definition

ChEBI: Rocuronium bromide is the organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents. It has a role as a neuromuscular agent and a muscle relaxant. It is an organic bromide salt and a quaternary ammonium salt. It contains a rocuronium. It derives from a hydride of a 5alpha-androstane.

brand name

Zemuron (Organon).

Biological Functions

Rocuronium bromide (Zemuron) is a recently approved amino steroid neuromuscular blocking agent. It has a rapid onset of action (1 minute), but its duration of action is intermediate (55 minutes), about that of vecuronium. On rare occasions, it may release histamine and cause cardiac irregularities. Rapacuronium bromide (Raplon) is the most recent neuromuscular blocking agent approved by the United States Food and Drug Administration (FDA). It is an analogue of vecuronium and is thus categorized as an amino steroid. It has a rapid onset of action (1.5 minutes) and a short to intermediate duration of action (20 minutes).This makes it a suitable alternative to mivacurium or succinylcholine for short procedures. It is eliminated mainly by the liver.Adverse effects are dose dependent; they include tachycardia, hypotension, and bronchospasm. These effects may be related to the ability of the drug to release a small amount of histamine.

Clinical Use

Muscle relaxant in general anaesthesia, medium duration

Side Effects

Common side effects of Rocuronium bromide include anaphylactic reactions, residual neuromuscular weakness, critical illness myopathy and polyneuropathy. Systemic anaphylactic reactions should be suspected in any patient who develops sudden cardiovascular collapse with cutaneous signs of anaphylactic reaction after Rocuronium bromide administration. Adverse effects of residual neuromuscular blockade have been shown to increase postoperative morbidity and mortality. The inability to fully reverse the effects of neuromuscular blockade may result in an increased risk of postoperative respiratory dysfunction, including hypoxia, need for mechanical ventilation, and increased length of hospital stay. Prolonged infusion of neuromuscular blockade may prolong skeletal muscle weakness due to myopathy caused by critical illness, in patients on steroids or with multiple organ failure. Rocuronium bromide has been shown to be very stable and has no effect on heart rate or blood pressure.

Safety

Limited information on the use of rocuronium during breastfeeding indicates that no adverse infant effects occur. Because it is short acting, highly polar and poorly absorbed orally, it is not likely to reach the breastmilk in high concentration or to reach the bloodstream of the infant. When a combination of anesthetic agents is used for a procedure, follow the recommendations for the most problematic medication used during the procedure. General anesthesia for cesarean section using rocuronium as a component may delay the onset of lactation.

Drug interactions

Potentially hazardous interactions with other drugs
Anaesthetics: enhanced muscle relaxant effect.
Anti-arrhythmics: procainamide enhances muscle relaxant effect.
Antibacterials: effect enhanced by aminoglycosides, clindamycin, polymyxins and piperacillin.
Antiepileptics: muscle relaxant effects antagonised by carbamazepine; effects reduced by long-term use of fosphenytoin and phenytoin but might be increased by acute use.
Botulinum toxin: neuromuscular block enhanced (risk of toxicity).

Metabolism

Rocuronium is metabolised by the liver to a less active metabolite, 17-desacetylrocuronium which is reported to have weak neuromuscular blocking effect.
Up to 40% of a dose may be excreted in the urine within 24 hours; rocuronium is also excreted in the bile. After injection of a radiolabelled dose of rocuronium bromide, excretion of the radiolabel is on average 47% in urine and 43% in faeces after 9 days. Approximately 50% is recovered as the parent compound. No metabolites are detected in plasma.