Rocuronium

Rocuronium
Names
Trade namesZemuron, Esmeron, others
Other namesRocuronium bromide, [3-hydroxy-10,13-dimethyl-2-morpholin-4-yl-16-(1-prop-2-enyl-2,3,4,5-tetrahydropyrrol-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate
IUPAC name
  • 1-((2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-17-acetoxy-3-hydroxy-10,13-dimethyl-2-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-16-yl)-1-allylpyrrolidinium bromide
Clinical data
Drug classNeuromuscular blocker
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • C
Routes of
use		Intravenous
Onset of action60 secs[1]
Duration of action25 to 90 mins[1][2]
Typical dose1.2 mg/kg[1]
External links
AHFS/Drugs.comMonograph
Legal
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetics
BioavailabilityNA
Protein binding~30%
MetabolismSome de-acetylation
Elimination half-life66–80 minutes
ExcretionUnchanged, in bile and urine
Chemical and physical data
FormulaC32H53BrN2O4
Molar mass609.690 g·mol−1
3D model (JSmol)
SMILES
  • CC(=O)O[C@H]1[C@H](C[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC[C@@H]4[C@@]3(C[C@@H]([C@H](C4)O)N5CCOCC5)C)C)[N+]6(CCCC6)CC=C.[Br-]
InChI
  • InChI=1S/C32H53N2O4.BrH/c1-5-14-34(15-6-7-16-34)28-20-26-24-9-8-23-19-29(36)27(33-12-17-37-18-13-33)21-32(23,4)25(24)10-11-31(26,3)30(28)38-22(2)35;/h5,23-30,36H,1,6-21H2,2-4H3;1H/q+1;/p-1/t23-,24+,25-,26-,27-,28-,29-,30-,31-,32-;/m0./s1 ☒N
  • Key:OYTJKRAYGYRUJK-FMCCZJBLSA-M ☒N

Rocuronium, sold under a number of brands, is a medication used to paralyze muscles for endotracheal intubation, including rapid sequence induction (RSI).[3][4] It may also be used to relax muscles during surgery and when people are on a ventilator.[3] It is given by injection into a vein.[3] A single dose begins working after about 45 to 120 seconds and lasts for 25 to 90 minutes.[1][2]

Common side effects include low blood pressure and high blood pressure.[3] Other serious side effects may include anaphylaxis and prolonged muscle weakness.[3][5] While not well studied in pregnancy, no harms have been found.[6] Breastfeeding shortly following use is likely okay.[7] Rocuronium is a neuromuscular blocker of the non-depolarizing type.[8]

Rocuronium was approved for medical use in the United States in 1994.[3] It is avaliable as a generic medication.[9][10] In the United States it costs about 40 USD for 500 mg as of 2020.[11] In the United Kingdom this amount costs the NHS about 25 pounds.[10] Rocuronium is stable at room temperature for about 12 weeks.[2]

Medical use

Rocuronium is used to paralyze muscles for endotracheal intubation, including rapid sequence induction (RSI).[3][4]

It should only be used with appropriate sedation.[5]

Dosage

The typical dose for rapid sequence intubation is 1.2 mg per kg.[1] Repeat doses of 0.6 mg per kg may be used.[1] An infusion of 10 to 12 micrograms per kg per min may also be used.[8]

In those who are very obese doses may be based on ideal body weight rather than actual body weight.[10] Evidence for this recommendation; however, is poor as of 2021.[12]

The dosage does not need to be changed in those with kidney problems.[3] Though lower doses may be required in those with liver problems with prolonged use.[10] Larger doses may be needed in people with large area burn and those with liver problems.[3]

Pharmacology

It is an aminosteroid non-depolarizing neuromuscular blocker.

Mechanism of action

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.[13]

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).[14]

The γ-cyclodextrin derivative sugammadex has been recently introduced as a novel agent to reverse the action of rocuronium.[15] 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,[16] but finally approved the medication for use during surgical procedures in the United States on December 15, 2015.[17] 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.[18]

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.

Executions

On July 27, 2012, the U.S. state of Virginia replaced pancuronium bromide, one of the three drugs used in execution by lethal injection, with rocuronium bromide.[19]

On 3 October 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.[20]

On August 24, 2017, the U.S. state of Florida executed Mark James Asay using a combination of etomidate, rocuronium bromide, and potassium acetate.[21]

References

  1. 1 2 3 4 5 6 "Rapid sequence intubation - WikEM". wikem.org. Archived from the original on 3 August 2020. Retrieved 19 August 2020.
  2. 1 2 3 "Succinylcholine vs. Rocuronium: Battle of the RSI Paralytics". JEMS. 14 May 2019. Archived from the original on 24 September 2020. Retrieved 28 September 2020.
  3. 1 2 3 4 5 6 7 8 9 "Rocuronium Bromide Monograph for Professionals". Drugs.com. Archived from the original on 26 June 2019. Retrieved 19 August 2020.
  4. 1 2 Tran, DT; Newton, EK; Mount, VA; Lee, JS; Wells, GA; Perry, JJ (29 October 2015). "Rocuronium versus succinylcholine for rapid sequence induction intubation". The Cochrane Database of Systematic Reviews. 10 (10): CD002788. doi:10.1002/14651858.CD002788.pub3. PMC 7104695. PMID 26512948.
  5. 1 2 Jain, Ankit; Wermuth, Harrison R.; Maani, Christopher V. (2020). "Rocuronium". StatPearls. StatPearls Publishing. Archived from the original on 29 August 2021. Retrieved 19 August 2020.
  6. ↑ "Rocuronium (Zemuron) Use During Pregnancy". Drugs.com. Archived from the original on 3 December 2020. Retrieved 19 August 2020.
  7. ↑ "Rocuronium". Drugs and Lactation Database (LactMed). National Library of Medicine (US). 2006. Archived from the original on 30 November 2020. Retrieved 19 August 2020.
  8. 1 2 "Rocuronium - WikEM". wikem.org. Archived from the original on 4 October 2017. Retrieved 19 August 2020.
  9. ↑ "Rocuronium (Zemuron) | Davis's Drug Guide". nursing.unboundmedicine.com. Archived from the original on 13 August 2020. Retrieved 19 August 2020.
  10. 1 2 3 4 BNF 79. London: Pharmaceutical Press. March 2020. p. 1379. ISBN 978-0857113658.
  11. ↑ "Rocuronium Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 10 November 2019. Retrieved 19 August 2020.
  12. ↑ Erstad, Brian L; Barletta, Jeffrey F (March 2021). "Dosing of neuromuscular blocking agents in patients with obesity: A narrative review". Anaesthesia and Intensive Care. 49 (2): 98–104. doi:10.1177/0310057X20968573. ISSN 0310-057X.
  13. ↑ Hunter JM (April 1996). "Rocuronium: the newest aminosteroid neuromuscular blocking drug". British Journal of Anaesthesia. 76 (4): 481–3. doi:10.1093/bja/76.4.481. PMID 8652315. Archived from the original on 2013-01-13. Retrieved 2020-07-19.
  14. ↑ Burburan SM, Xisto DG, Rocco PR (June 2007). "Anaesthetic management in asthma". Minerva Anestesiologica. 73 (6): 357–65. PMID 17115010.
  15. ↑ Naguib M (March 2007). "Sugammadex: another milestone in clinical neuromuscular pharmacology". Anesthesia and Analgesia. 104 (3): 575–81. doi:10.1213/01.ane.0000244594.63318.fc. PMID 17312211. Archived from the original on 2021-08-29. Retrieved 2020-07-19.
  16. ↑ McKee, Selina (September 24, 2013). "FDA turns down Merck & Co's sugammadex again". PharmaTimes. Archived from the original on February 22, 2014.
  17. ↑ "Press Announcements - FDA approves Bridion to reverse effects of neuromuscular blocking drugs used during surgery". www.fda.gov. Archived from the original on 2015-12-15. Retrieved 2017-01-07.
  18. ↑ Carron, Michele; Zarantonello, Francesco; Tellaroli, Paola; Ori, Carlo (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. PMID 27871504.
  19. ↑ "Virginia Department of Corrections Operating Procedure: Execution Manual" (PDF). 2017-02-07. Archived (PDF) from the original on 2017-10-26. Retrieved 2017-10-25.
  20. ↑ "Ohio to resume executions using a three-drug combination in January". BBC News. 2016-10-03. Archived from the original on 2016-10-05. Retrieved 2017-01-07.
  21. ↑ Jason Dearon. "Florida executes convicted killer Mark Asay using new drug". Sun Sentinel. Archived from the original on 2017-08-25. Retrieved 2020-07-19.
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