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Statements

Subject Item
n2:DB00728
rdf:type
n3:Drug
n3:description
Rocuronium (rapid onset-curonium) is a desacetoxy analogue of vecuronium with a more rapid onset of action. It is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Introduced in 1994, rocuronium has rapid onset, and intermediate duration of action. It is marketed under the trade name of Zemuron in the United States and Esmeron in most other countries. 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). The γ-cyclodextrin derivative sugammadex (trade name Bridion) has been recently introduced as a novel agent to reverse the action of rocuronium.
n3:dosage
n21:271B508A-363D-11E5-9242-09173F13E4C5 n21:271B508B-363D-11E5-9242-09173F13E4C5 n21:271B508C-363D-11E5-9242-09173F13E4C5 n21:271B508D-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Agoston S, Vandenbrom RH, Wierda JM: Clinical pharmacokinetics of neuromuscular blocking drugs. Clin Pharmacokinet. 1992 Feb;22(2):94-115. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/1551294 # Khuenl-Brady KS, Sparr H: Clinical pharmacokinetics of rocuronium bromide. Clin Pharmacokinet. 1996 Sep;31(3):174-83. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8877248 # Alvarez-Gomez JA: [Rocuronium] Rev Esp Anestesiol Reanim. 1997 Oct;44(8):310-4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9424684 # Wicks TC: The pharmacology of rocuronium bromide (ORG 9426). AANA J. 1994 Feb;62(1):33-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8122487 # Sparr HJ, Beaufort TM, Fuchs-Buder T: Newer neuromuscular blocking agents: how do they compare with established agents? Drugs. 2001;61(7):919-42. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11434449 # Hemmerling TM, Russo G, Bracco D: Neuromuscular blockade in cardiac surgery: an update for clinicians. Ann Card Anaesth. 2008 Jul-Dec;11(2):80-90. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18603747
n3:group
approved
n3:halfLife
The rapid distribution half-life is 1-2 minutes and the slower distribution half-life is 14-18 minutes. Renal impairment has no net effect on half-life, however, half-life is almost doubled in patients with impaired liver function.
n3:indication
For inpatients and outpatients as an adjunct to general anesthesia to facilitate both rapid sequence and routine tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
n3:manufacturer
n9:271B5082-363D-11E5-9242-09173F13E4C5 n9:271B5083-363D-11E5-9242-09173F13E4C5 n9:271B5080-363D-11E5-9242-09173F13E4C5 n9:271B5081-363D-11E5-9242-09173F13E4C5 n9:271B5086-363D-11E5-9242-09173F13E4C5 n9:271B5084-363D-11E5-9242-09173F13E4C5 n9:271B5085-363D-11E5-9242-09173F13E4C5
owl:sameAs
n12:DB00728 n22:DB00728
dcterms:title
Rocuronium
adms:identifier
n7:Rocuronium n17:46506855 n18:441290 n19:D00765 n20:0781-3220-75 n24:4003 n25:4003 n26:DB00728 n27:8884 n28:390053 n30:PA164754992
n3:mechanismOfAction
Rocuronium acts by competing for cholinergic receptors at the motor end-plate. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium. Rocuronium acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur. Evidence also suggests that nondepolarizing agents can affect ACh release. It has been hypothesized that nondepolarzing agents bind to postjunctional ("curare") receptors and may therefore interfere with the sodium and potassium flux, which is responsible for depolarization and repolarization of the membranes involved in muscle contraction.
n3:packager
n9:271B507E-363D-11E5-9242-09173F13E4C5 n9:271B507F-363D-11E5-9242-09173F13E4C5 n9:271B507C-363D-11E5-9242-09173F13E4C5 n9:271B507D-363D-11E5-9242-09173F13E4C5 n9:271B507A-363D-11E5-9242-09173F13E4C5 n9:271B507B-363D-11E5-9242-09173F13E4C5 n9:271B5079-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination
Studies of distribution, metabolism, and excretion in cats and dogs indicate that rocuronium is eliminated primarily by the liver.
n3:synonym
Rocuronium SID50112687
n3:toxicity
No cases of significant accidental or intentional overdose have been reported. Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.
n3:volumeOfDistribution
* 0.3 L/kg [3 to <12 mos] * 0.26 L/kg [1 to <3 yrs] * 0.21 L/kg [3 to <8 yrs]
n15:hasAHFSCode
n16:12-20-00
n3:proteinBinding
Approximately 30% bound to human plasma proteins.
n3:salt
n3:synthesisReference
Eliezer Adar, David Sondack, Oded Friedman, Iosef Manascu, Tamir Fizitzki, Boris Freger, Oded Arad, Alexander Weisman, Joseph Kaspi, "Processes for the preparation of rocuronium bromide and intermediates thereof." U.S. Patent US20050159398, issued July 21, 2005.
n4:hasConcept
n5:M0171457
foaf:page
n14:rocuronium.htm n29:rocuronium.html
n3:IUPAC-Name
n8:271B5092-363D-11E5-9242-09173F13E4C5
n3:InChI
n8:271B5098-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n8:271B5097-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n8:271B5094-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n8:271B5095-363D-11E5-9242-09173F13E4C5
n3:SMILES
n8:271B5096-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n8:271B50A8-363D-11E5-9242-09173F13E4C5 n8:271B5090-363D-11E5-9242-09173F13E4C5
n3:logP
n8:271B508E-363D-11E5-9242-09173F13E4C5 n8:271B5091-363D-11E5-9242-09173F13E4C5
n3:logS
n8:271B508F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n8:271B509E-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n8:271B509F-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n8:271B5099-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n8:271B509A-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n8:271B509C-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n8:271B509B-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n8:271B509D-363D-11E5-9242-09173F13E4C5
n3:absorption
Poorly absorbed from the GI tract.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
143558-00-3
n3:category
n3:clearance
* 0.25 L/kg/hr [Adults (Ages 27 to 58 years)] * 0.21 L/kg/hr [Geriatrics (>=65 yrs)] * 0.16 L/kg/hr [Normal ewnal and hepatice function] * 0.13 L/kg/hr [Renal transplant patients] * 0.13 L/kg/hr [Hepatic dysfunction patients] * 0.35 +/- 0.08 L/kg/hr [Pediatric Patients 3 to <12 mos] * 0.32 +/- 0.07 L/kg/hr [Pediatric Patients 1 to 3 yrs] * 0.44 +/- 0.16 L/kg/hr [Pediatric Patients 3 to 8 yrs]
n3:containedIn
n23:271B5088-363D-11E5-9242-09173F13E4C5 n23:271B5089-363D-11E5-9242-09173F13E4C5 n23:271B5087-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n8:271B50A4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n8:271B50A6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n8:271B50A7-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n8:271B50A3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n8:271B50A2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n8:271B50A5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n8:271B5093-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n8:271B50A0-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n8:271B50A1-363D-11E5-9242-09173F13E4C5