m
(Many minor changes)
 
Line 11: Line 11:
| clearance =  
| clearance =  
| halflife_elimination =  
| halflife_elimination =  
| adverse_effects = Anaphylactic reaction, histamine release, muscle weakness from prolong use, PTSD if adequate sedation is not used, respiration depression if incomplete reversal
| adverse_effects = Anaphylactic reaction
Histamine release
| metabolism = Hofmann Elimination
| metabolism = Hofmann Elimination
| duration = 45 minutes
| duration = 45 minutes
| time_onset =  
| time_onset = 3 to 5 minutes
| dosage_calculation = cisatracurium
| dosage_calculation = cisatracurium
| mechanism = Nicotinic acetylcholine antagonism
| mechanism = Nicotinic acetylcholine antagonism
Line 20: Line 21:
}}
}}


Cisatracurium is a benzylisoquinolinium intermediate acting non-depolarizing neuromuscular blocking agents used for tracheal intubation and surgical relaxation in patients with renal or hepatic dysfunction. It is also used to provide paralysis in patients with acute respiratory distress syndrome in the intensive care unit.  
'''Cisatracurium''' is a benzylisoquinolinium intermediate acting nondepolarizing neuromuscular blocking agent used for tracheal intubation and surgical relaxation. Unlike agents such as [[rocuronium]] or [[vecuronium]], cisatracurium is metabolized via Hofmann elimination, making it a safer choice for patients with severe renal or hepatic dysfunction. However, due to its longer onset of action, it is rarely used outside this population, and is not considered appropriate for use in a [[rapid sequence induction]]. It is also used as an infusion to provide paralysis in intubated patients with acute respiratory distress syndrome in the intensive care unit.  


==Uses<!-- Describe uses of the drug. If appropriate, add subsections for each indication. -->==
==Uses<!-- Describe uses of the drug. If appropriate, add subsections for each indication. -->==


* Optimizing tracheal intubation condition among patients with renal or hepatic dysfunction  
* Muscle relaxation for intubation
** Abduction of vocal cords 
**Primarily used in patients with severe renal and/or hepatic dysfunction
** Opening of mouth 
**Not appropriate for RSI due to longer onset of action
** Reduction in coughing and gagging 
* Maintenance of surgical relaxation
* Provide surgical relaxation mainly in patients with renal or hepatic dysfunction.
* Optimizing mechanical ventilation conditions 
** Reduction in bucking/coughing
** Reduction in breath stacking


* Provide paralysis in patients with acute respiratory distress syndrome in the intensive care unit via continuous infusion early in the course of ARDS for patients with a PaO2/FiO2 less than 150. The proposed mechanism of the beneficial effect is possibly by lowering trans-pulmonary pressure reducing barotrauma.
* Paralysis in patients with acute respiratory distress syndrome in the intensive care unit via continuous infusion
**Used early in the course of ARDS for patients with a PaO2/FiO2 less than 150  
**The proposed mechanism of the beneficial effect is possibly by lowering transpulmonary pressure reducing barotrauma  


==Contraindications<!-- List contraindications and precautions for use of the drug. -->==
==Contraindications<!-- List contraindications and precautions for use of the drug. -->==
Line 50: Line 49:
* Muscular dystrophy (Duchenne type)
* Muscular dystrophy (Duchenne type)
* Myotonia including dystrophic, congenital,, and paramyotonia  
* Myotonia including dystrophic, congenital,, and paramyotonia  
* Patient may have resistance include:  
* Patients who may have resistance include:  
** Burn injury  
** Burn injury  
** Cerebral palsy  
** Cerebral palsy  
Line 61: Line 60:
===Pharmacodynamics<!-- Describe the effects of the drug on the body. If appropriate, add subsections by organ system -->===
===Pharmacodynamics<!-- Describe the effects of the drug on the body. If appropriate, add subsections by organ system -->===


* Eliminated via Hofmann elimination
* Roughly about 3 times the potency of atracurium
* Roughly about 3 times the potency of atracurium


Line 81: Line 79:
===Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. -->===
===Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. -->===


* Duration of action after 2 x ED<sub>95</sub> is 45 minutes <ref name=":1">{{Citation|last=Lien|first=Cynthia A.|title=Neuromuscular Blockers and Reversal Drugs|date=2013|url=http://dx.doi.org/10.1016/b978-1-4377-1679-5.00019-3|work=Pharmacology and Physiology for Anesthesia|pages=325–348|publisher=Elsevier|access-date=2023-01-05|last2=Eikermann|first2=Matthias}}</ref>
* Eliminated via Hofmann elimination
*Duration of action after 2 x ED<sub>95</sub> is 45 minutes <ref name=":1">{{Citation|last=Lien|first=Cynthia A.|title=Neuromuscular Blockers and Reversal Drugs|date=2013|url=http://dx.doi.org/10.1016/b978-1-4377-1679-5.00019-3|work=Pharmacology and Physiology for Anesthesia|pages=325–348|publisher=Elsevier|access-date=2023-01-05|last2=Eikermann|first2=Matthias}}</ref>
* With prolonged infusion, elimination half life is 20 minutes <ref name=":1" />
* With prolonged infusion, elimination half life is 20 minutes <ref name=":1" />


Line 91: Line 90:


==References==
==References==
* Strawbridge AD, Khanna NR, Hauser JM. Cisatracurium. [Updated 2022 Jul 11]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-. Available from: <nowiki>https://www.ncbi.nlm.nih.gov/books/NBK539842/</nowiki><ref name=":0" />
* Anita Gupta, Nina Singh-Radcliff. ''Pharmacology in Anesthesia Practice''. Oxford University Press; 2013. Accessed January 5, 2023. <nowiki>https://search-ebscohost-com.laneproxy.stanford.edu/login.aspx?direct=true&db=nlebk&AN=603930&site=ehost-live</nowiki><ref>{{Cite book|last=Nina.|first=Gupta, Anita. Singh-Radcliff,|url=http://worldcat.org/oclc/940638246|title=Pharmacology in anesthesia practice|date=2013|publisher=Oxford University Press|isbn=978-0-19-978267-3|oclc=940638246}}</ref>
* Lien, Cynthia A.; Eikermann, Matthias (2013), "Neuromuscular Blockers and Reversal Drugs", ''Pharmacology and Physiology for Anesthesia'', Elsevier, pp.&nbsp;325–348, retrieved 2023-01-05<ref name=":1" />


[[Category:Drug reference]]
[[Category:Drug reference]]
[[Category:Neuromuscular blockers]]
[[Category:Neuromuscular blockers]]
[[Category:Nondepolarizing neuromuscular blockers]]
[[Category:Nondepolarizing neuromuscular blockers]]

Latest revision as of 13:14, 8 January 2023

Cisatracurium
Trade names

Nimbex

Cisatracurium.svg
Clinical data
Drug class

Neuromuscular blocker

Uses

Tracheal intubation, surgical relaxation, optimizing mechanical ventilation, patients with ARDS

Contraindications

Known hypersensitivity

Routes of administration

IV

Dosage
Pharmacodynamics
Mechanism of action

Nicotinic acetylcholine antagonism

Adverse effects

Anaphylactic reaction Histamine release

Pharmacokinetics
Onset of action

3 to 5 minutes

Duration of action

45 minutes

Metabolism

Hofmann Elimination

Physical and chemical data
Article quality
Editor rating
Comprehensive
User likes
0

Cisatracurium is a benzylisoquinolinium intermediate acting nondepolarizing neuromuscular blocking agent used for tracheal intubation and surgical relaxation. Unlike agents such as rocuronium or vecuronium, cisatracurium is metabolized via Hofmann elimination, making it a safer choice for patients with severe renal or hepatic dysfunction. However, due to its longer onset of action, it is rarely used outside this population, and is not considered appropriate for use in a rapid sequence induction. It is also used as an infusion to provide paralysis in intubated patients with acute respiratory distress syndrome in the intensive care unit.

Uses

  • Muscle relaxation for intubation
    • Primarily used in patients with severe renal and/or hepatic dysfunction
    • Not appropriate for RSI due to longer onset of action
  • Maintenance of surgical relaxation
  • Paralysis in patients with acute respiratory distress syndrome in the intensive care unit via continuous infusion
    • Used early in the course of ARDS for patients with a PaO2/FiO2 less than 150
    • The proposed mechanism of the beneficial effect is possibly by lowering transpulmonary pressure reducing barotrauma

Contraindications

Absolute contraindications

  • Known hypersensitivity

Precautions[1]

  • Patients with myasthenia gravis/myathenic syndrome
  • Amyotrophic lateral sclerosis
  • Autoimmune disorders including polymyositis, dermatomyositis and systemic lupus erythematous
  • Familial periodic paralysis hyperkalemia
  • Guillain-Barré syndrome
  • Muscular dystrophy (Duchenne type)
  • Myotonia including dystrophic, congenital,, and paramyotonia
  • Patients who may have resistance include:
    • Burn injury
    • Cerebral palsy
    • Hemiplegia (on the affected side)
    • Muscular denervation
    • Severe chronic infection such as tetanus and botulism

Pharmacology

Pharmacodynamics

  • Roughly about 3 times the potency of atracurium

Mechanism of action

  • Competitive antagonism of acetylcholine at the post junctional receptors preventing depolarization of the muscle preventing any movement. Only one molecule of the neuromuscular blocker is needed to prevent activation of the receptor as it competes with acetylcholine at the two binding sites.

Adverse effects

  • Anaphylactic reaction
  • Histamine release leading to hypotension, bronchospasm, rash
  • Bradycardia
  • Muscle weakness or myopathy due to persistent failure of neuromuscular transmission and immobilization-induced atrophy of diaphragm
  • Posttraummatic stress syndrome from awareness during paralysis if sedation is not used adequately.
  • Impairment of ventilation-perfusion distribution and decreased right ventricular end-diastolic volume due to abolishment of spontaneous breathing.
  • Incomplete reversal of neuromuscular blocking agent leading to respiratory depression

Pharmacokinetics

  • Eliminated via Hofmann elimination
  • Duration of action after 2 x ED95 is 45 minutes [2]
  • With prolonged infusion, elimination half life is 20 minutes [2]

Chemistry and formulation

1 R-cis 1'R-cis stereoisomer of the 10 stereoisomers that comprise atracurium[1]

History

The development involved isolation and testing of individual stereoisomers from the mixture found in atracurium[2]

References

  1. 1.0 1.1 Strawbridge, Andrew D.; Khanna, Niloufar R.; Hauser, Joshua M. (2022), "Cisatracurium", StatPearls, Treasure Island (FL): StatPearls Publishing, PMID 30969664, retrieved 2023-01-05
  2. 2.0 2.1 2.2 Lien, Cynthia A.; Eikermann, Matthias (2013), "Neuromuscular Blockers and Reversal Drugs", Pharmacology and Physiology for Anesthesia, Elsevier, pp. 325–348, retrieved 2023-01-05