Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/08/19 05:46:25」(JST)

wiki en

Rocuronium bromide (brand names 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 endotracheal intubation and rapid sequence induction (RSI), although Suxamethonium chloride is usually selected for RSI given its fast onset of action compared with rocuronium.^[1]

Pharmacology

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.^[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) 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 during surgical procedures in the United States on December 15, 2015.^[6] 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.

Society and Culture

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.^{[citation needed]}

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.^[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. PMID 26512948. doi:10.1002/14651858.CD002788.pub3.
^ Hunter JM (April 1996). "Rocuronium: the newest aminosteroid neuromuscular blocking drug". British Journal of Anaesthesia. 76 (4): 481–3. PMID 8652315. doi:10.1093/bja/76.4.481.
^ 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. PMID 17312211. doi:10.1213/01.ane.0000244594.63318.fc.
^ McKee, Selina (September 24, 2013). "FDA turns down Merck & Co's sugammadex again". PharmaTimes.
^ "Press Announcements - FDA approves Bridion to reverse effects of neuromuscular blocking drugs used during surgery". www.fda.gov. Retrieved 2017-01-07.
^ Carron, Michele; Zarantonello, Francesco; Tellaroli, Paola; Ori, Carlo. "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.
^ "Ohio to resume executions using a three-drug combination in January". BBC News. 2016-10-03. Retrieved 2017-01-07.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 手術室外での小児への迅速導入気管挿管（RSI）：鎮静薬と筋弛緩薬 rapid sequence intubation rsi outside of the operating room in children medications for sedation and paralysis
2. 重症筋無力症患者に対する麻酔 anesthesia for the patient with myasthenia gravis
3. Neuromuscular blocking agents (NMBAs) for rapid sequence intubation in adults outside of the operating room
4. 重症患者における神経筋遮断剤の使用 use of neuromuscular blocking medications in critically ill patients
5. 全身麻酔：維持と覚醒 general anesthesia maintenance and emergence

English Journal

Sugammadex and rocuronium-induced anaphylaxis.

Baldo B.SourceSydney, Australia Email: babaldo@iinet.net.au.
Anaesthesia.Anaesthesia.2012 Oct;67(10):1174-5. doi: 10.1111/j.1365-2044.2012.07289.x.
PMID 22950397

Effects of sugammadex and rocuronium mast cell number and degranulation in rat liver.

Tomak Y, Yılmaz A, Bostan H, Tümkaya L, Altuner D, Kalkan Y, Erdivanlı B.SourceAssistant Professors, Department of Anaesthesiology and Reanimation Department of Biochemistry Department of Histology and Embryology Department of Pharmacology, Rize University, Medical Faculty, Rize, Turkey Medical Doctor, Department of Anaesthesiology and Reanimation, Rize Education and Research Hospital, Rize, Turkey.
Anaesthesia.Anaesthesia.2012 Oct;67(10):1101-4. doi: 10.1111/j.1365-2044.2012.07264.x. Epub 2012 Jul 24.
We investigated the effect of rocuronium- and sugammadex-induced mast cell increase and degranulation in rat portal triads. Forty-two rats, in six groups, received either rocuronium 1 mg.kg(-1) ; sugammadex 15 mg.kg(-1) ; sugammadex 100 mg.kg(-1) ; rocuronium 1 mg.kg(-1) and 5 min later,
PMID 22827538

Japanese Journal

症例報告ロクロニウムによるアナフィラキシーの1例

磯久太郎,益田浩司,影山京子 [他]
臨床皮膚科 65(12), 937-940, 2011-11
NAID 40019039079

スガマデクス投与30分後に再手術のためロクロニウムを再投与した2歳児の症例

西雅利,藤井怜,新田俊一
麻酔 60(10), 1189-1191, 2011-10
NAID 40019005177

Related Pictures

★リンクテーブル★

リンク元	「麻酔」「ロクロニウム」
拡張検索	「rocuronium bromide」

「麻酔」

Rocuronium bromide
Clinical data
AHFS/Drugs.com	Monograph
Routes of; administration	Intravenous
ATC code	M03AC09 (WHO);
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	NA
Protein binding	~30%
Metabolism	some de-acetylation
Biological half-life	66–80 minutes
Excretion	Unchanged, in bile and urine
Identifiers
	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;
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	441351;
IUPHAR/BPS	4003;
DrugBank	DB00728 ;
ChemSpider	390104 ;
UNII	I65MW4OFHZ;
ChEMBL	CHEMBL1201244 ;
Chemical and physical data
Formula	C32H53BrN2O4
Molar mass	609.678 g/mol
3D model (JSmol)	Interactive image;
	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 ; Key:OYTJKRAYGYRUJK-FMCCZJBLSA-M ;
(what is this?) (verify)

　　[★]

英: anesthesia
関: 麻酔機、術前準備

全身麻酔

1. Semi-rapid induction （成人の場合の基本）

(a) モニター装着，静脈確保．
(b) propofol（ 2 mg/kg ）remifentanil（ 0.5 μg/kg/min ）で入眠．
(c) rocuronium（ 0.6 mg/kg ）で筋弛緩．
(d) 100%酸素でBag & Mask
(e) 麻酔が深くなったら気管挿管．

目的別の麻酔方法

心臓手術：on-pump CAB, off-pump CAB
肺手術：一側肺換気
産科麻酔：筋弛緩薬以外は胎盤を通過すると考えて良いと思われる。硬膜外麻酔でオピオイドを投与するのは分娩後。

帝王切開術：脊髄くも膜下麻酔

参考

1. 研修医用のマニュアル - 神戸大学大学院医学系研究科外科系講座麻酔科学分野

http://www.med.kobe-u.ac.jp/anes/manual.html

2. 麻酔科レジデントマニュアル麻酔応用編筑波大学附属病院麻酔科 2011 年ver.1.4

http://www.md.tsukuba.ac.jp/clinical-med/anesthesiology/tsukuba_new_anesthesiology/pdf/manual3advanced110325.pdf

「ロクロニウム」

　　[★]

英: rocuronium
化: 臭化ロクロニウム、rocuronium bromide Rb
商: エスラックス、Zemuron
関: 筋弛緩薬、非脱分極性筋弛緩薬

筋弛緩薬;四級アンモニウム;神経筋遮断薬;競合性
拮抗薬：スガマデクス

「rocuronium bromide」

　　[★] ロクロニウム rocuronium。臭化ロクロニウム

[1] 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. PMID 26512948. doi:10.1002/14651858.CD002788.pub3.

[pmid8652315-2] Hunter JM (April 1996). "Rocuronium: the newest aminosteroid neuromuscular blocking drug". British Journal of Anaesthesia. 76 (4): 481–3. PMID 8652315. doi:10.1093/bja/76.4.481.

[pmid17115010-3] Burburan SM, Xisto DG, Rocco PR (June 2007). "Anaesthetic management in asthma". Minerva Anestesiologica. 73 (6): 357–65. PMID 17115010.

[pmid17312211-4] Naguib M (March 2007). "Sugammadex: another milestone in clinical neuromuscular pharmacology". Anesthesia and Analgesia. 104 (3): 575–81. PMID 17312211. doi:10.1213/01.ane.0000244594.63318.fc.

[5] McKee, Selina (September 24, 2013). "FDA turns down Merck & Co's sugammadex again". PharmaTimes.

[6] "Press Announcements - FDA approves Bridion to reverse effects of neuromuscular blocking drugs used during surgery". www.fda.gov. Retrieved 2017-01-07.

[7] Carron, Michele; Zarantonello, Francesco; Tellaroli, Paola; Ori, Carlo. "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.

[8] "Ohio to resume executions using a three-drug combination in January". BBC News. 2016-10-03. Retrieved 2017-01-07.

匿名

検索

案内

案内

rocuronium