Rocuronium bromide
 | |
| Clinical data | |
|---|---|
| AHFS/Drugs.com | Monograph |
| Routes of administration | Intravenous |
| ATC code | M03AC09 (WHO) |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | NA |
| Protein binding | ~30% |
| Metabolism | some de-acetylation |
| Biological half-life | 66–80 minutes |
| Excretion | Unchanged, in bile and urine |
| Identifiers | |
| |
| Synonyms | [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 |
| CAS Number |
119302-91-9  |
| PubChem (CID) | 441290 |
| IUPHAR/BPS | 4003 |
| DrugBank |
DB00728  |
| UNII |
I65MW4OFHZ |
| ChEMBL |
CHEMBL1201244 |
| Chemical and physical data | |
| Formula | C32H53N2O4+ |
| Molar mass | 529.774 g/mol |
| (what is this?) (verify) | |
Rocuronium (Zemuron, Esmeron) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia to facilitate endotracheal intubation by providing skeletal muscle relaxation, most commonly required for surgery or mechanical ventilation. It is used for both standard and rapid sequence induction (RSI), although Suxamethonium chloride is usually selected for RSI given its faster onset of action compared to rocuronium.[1]
Development
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] It was introduced in 1994, and 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).[3]
The γ-cyclodextrin derivative sugammadex (trade name Bridion) has been recently introduced as a novel agent to reverse the action of rocuronium.[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 in the United States on December 15, 2015.[6]
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.
On 3rd October, 2016, the U.S. state of Ohio announced that it would resume executions on January 12, 2017, using a cocktail of midazolam, rocuronium bromide, and potassium chloride. Prior to this, the last execution in Ohio was in January 2014.[7]
It is colloquially referred to as "roc."[8]
References
- ↑ 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: CD002788. doi:10.1002/14651858.CD002788.pub3. PMID 26512948.
- ↑ 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.
- ↑ Burburan SM, Xisto DG, Rocco PR (June 2007). "Anaesthetic management in asthma". Minerva Anestesiologica. 73 (6): 357–65. PMID 17115010.
- ↑ 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.
- ↑ McKee, Selina (September 24, 2013). "FDA turns down Merck & Co's sugammadex again". PharmaTimes.
- ↑ http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm477512.htm
- ↑ http://www.bbc.co.uk/news/world-us-canada-37545854
- ↑ Hemon, Aleksandar (June 13, 2011). "The Aquarium". The New Yorker.