(Chemistry, History, and brief summary)
m
Line 1: Line 1:
{{Infobox drug reference
{{Infobox drug reference
| trade_names =  
| trade_names = Nimbex
| drug_class = Neuromuscular blocker
| drug_class = Neuromuscular blocker
| drug_class_color = neuromuscular_blocker
| drug_class_color = neuromuscular_blocker
| uses =  
| uses = Tracheal intubation, surgical relaxation, optimizing mechanical ventilation, patients with ARDS
| contraindications =  
| contraindications = Known hypersensitivity
| routes = IV
| routes = IV
| dosage =  
| dosage =  
Line 11: Line 11:
| clearance =  
| clearance =  
| halflife_elimination =  
| halflife_elimination =  
| adverse_effects =  
| adverse_effects = Anaphylactic reaction, histamine release, muscle weakness from prolong use, PTSD if adequate sedation is not used, respiration depression if incomplete reversal
| metabolism =  
| metabolism =  
| duration =  
| duration = 45 minutes
| time_onset =  
| time_onset =  
| dosage_calculation = cisatracurium
| dosage_calculation = cisatracurium
Line 20: Line 20:
}}
}}


Cisatracurium is a benzylisoquinolinium intermediate acting non-depolarizing neuromuscular blocking agents used commonly 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 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.  


==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. -->==
Line 41: Line 41:
* Known hypersensitivity
* Known hypersensitivity


===Precautions<!-- List precautions for use of the drug. If none, this section may be removed. -->===
===Precautions<!-- List precautions for use of the drug. If none, this section may be removed. --><ref name=":0">{{Citation|last=Strawbridge|first=Andrew D.|title=Cisatracurium|date=2022|url=http://www.ncbi.nlm.nih.gov/books/NBK539842/|work=StatPearls|place=Treasure Island (FL)|publisher=StatPearls Publishing|pmid=30969664|access-date=2023-01-05|last2=Khanna|first2=Niloufar R.|last3=Hauser|first3=Joshua M.}}</ref>===


* Patients with myasthenia gravis/myathenic syndrome  
* Patients with myasthenia gravis/myathenic syndrome  
Line 65: Line 65:


====Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. -->====
====Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. -->====
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.  
 
* 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<!-- Describe any potential adverse effects of the drug. -->====
====Adverse effects<!-- Describe any potential adverse effects of the drug. -->====
Line 79: Line 80:


===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>
* With prolonged infusion, elimination half life is 20 minutes <ref name=":1" />


==Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. -->==
==Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. -->==
1 R-cis 1'R-cis stereoisomer of the 10 stereoisomers that comprise atracurium
1 R-cis 1'R-cis stereoisomer of the 10 stereoisomers that comprise atracurium<ref name=":0" />


==History<!-- Describe the historical development of the drug. -->==
==History<!-- Describe the historical development of the drug. -->==
The development involved isolation and testing of individual stereoisomers from the mixture found in atracurium
The development involved isolation and testing of individual stereoisomers from the mixture found in atracurium<ref name=":1" />


==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]]

Revision as of 09:21, 5 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, muscle weakness from prolong use, PTSD if adequate sedation is not used, respiration depression if incomplete reversal

Pharmacokinetics
Duration of action

45 minutes

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

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.

Uses

  • Optimizing tracheal intubation condition among patients with renal or hepatic dysfunction
    • Abduction of vocal cords
    • Opening of mouth
    • Reduction in coughing and gagging
  • 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.

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
  • Patient 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

  • Eliminated via Hofmann elimination
  • 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

  • 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

  • Strawbridge AD, Khanna NR, Hauser JM. Cisatracurium. [Updated 2022 Jul 11]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK539842/[1]
  • Anita Gupta, Nina Singh-Radcliff. Pharmacology in Anesthesia Practice. Oxford University Press; 2013. Accessed January 5, 2023. https://search-ebscohost-com.laneproxy.stanford.edu/login.aspx?direct=true&db=nlebk&AN=603930&site=ehost-live[3]
  • Lien, Cynthia A.; Eikermann, Matthias (2013), "Neuromuscular Blockers and Reversal Drugs", Pharmacology and Physiology for Anesthesia, Elsevier, pp. 325–348, retrieved 2023-01-05[2]
  1. 1.0 1.1 1.2 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 2.3 Lien, Cynthia A.; Eikermann, Matthias (2013), "Neuromuscular Blockers and Reversal Drugs", Pharmacology and Physiology for Anesthesia, Elsevier, pp. 325–348, retrieved 2023-01-05
  3. Nina., Gupta, Anita. Singh-Radcliff, (2013). Pharmacology in anesthesia practice. Oxford University Press. ISBN 978-0-19-978267-3. OCLC 940638246.CS1 maint: extra punctuation (link)