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