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Rocuronium

产品号 DB00728 公司名称 DrugBank
CAS号 119302-91-9 公司网站 http://www.ualberta.ca/
分子式 C32H53N2O4+ 电 话 (780) 492-3111
分子量 529.77422 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 609

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产品别名

标题
Rocuronium
IUPAC标准名
1-[(1S,2S,4S,5S,7S,10R,11S,13S,14R,15S)-14-(acetyloxy)-5-hydroxy-2,15-dimethyl-4-(morpholin-4-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-13-yl]-1-(prop-2-en-1-yl)pyrrolidin-1-ium
IUPAC传统名
rocuronium
商标名
Rocuronium bromide
Zemuron

产品登记号

PubChem CID 441290
CAS号 119302-91-9
PubChem SID 46506855

产品性质

溶解度 Complete

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
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.
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.
Pharmacology Neuromuscular blocking agents are drugs that cause skeletal muscle relaxation primarily by causing a decreased response to the neurotransmitter acetylcholine (ACh) at the myoneural (neuromuscular) junction of skeletal muscle. At that site, ACh normally produces electrical depolarization of the postjunctional membrane of motor end-plate, which leads to conduction of muscle action potential and subsequently induces skeletal muscle contraction. Neuromuscular agents are classified as depolarizing or nondepolarizing. Rocuronium is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. Rocuronium, like vecuronium is longer acting in infants than in children. However, unlike vecuronium, rocuronium retains the characteristics of an intermediate-acting NMBD in infants.
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.
Affected Organisms
Humans and other mammals
Biotransformation Rocuronium is metabolized to a less active metabolite, 17-desacetyl-rocuronium, and is eliminated primarily by the liver.
Absorption Poorly absorbed from the GI tract.
Half Life 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.
Protein Binding Approximately 30% bound to human plasma proteins.
Elimination Studies of distribution, metabolism, and excretion in cats and dogs indicate that rocuronium is eliminated primarily by the liver.
Distribution * 0.3 L/kg [3 to <12 mos]
* 0.26 L/kg [1 to <3 yrs]
* 0.21 L/kg [3 to <8 yrs]
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]
References
Agoston S, Vandenbrom RH, Wierda JM: Clinical pharmacokinetics of neuromuscular blocking drugs. Clin Pharmacokinet. 1992 Feb;22(2):94-115. [Pubmed]
Khuenl-Brady KS, Sparr H: Clinical pharmacokinetics of rocuronium bromide. Clin Pharmacokinet. 1996 Sep;31(3):174-83. [Pubmed]
Alvarez-Gomez JA: [Rocuronium] Rev Esp Anestesiol Reanim. 1997 Oct;44(8):310-4. [Pubmed]
Wicks TC: The pharmacology of rocuronium bromide (ORG 9426). AANA J. 1994 Feb;62(1):33-8. [Pubmed]
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]
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]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Alvarez-Gomez JA: [Rocuronium] Rev Esp Anestesiol Reanim. 1997 Oct;44(8):310-4. Pubmed
  • Wicks TC: The pharmacology of rocuronium bromide (ORG 9426). AANA J. 1994 Feb;62(1):33-8. Pubmed
  • Agoston S, Vandenbrom RH, Wierda JM: Clinical pharmacokinetics of neuromuscular blocking drugs. Clin Pharmacokinet. 1992 Feb;22(2):94-115. Pubmed
  • Khuenl-Brady KS, Sparr H: Clinical pharmacokinetics of rocuronium bromide. Clin Pharmacokinet. 1996 Sep;31(3):174-83. Pubmed
  • 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
  • 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