Difference between revisions of "Cisatracurium"
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{{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 = | ||
|halflife_redistribution=|protein_binding=|clearance=|halflife_elimination=|adverse_effects=|metabolism=|duration=|time_onset=|mechanism=Nicotinic acetylcholine antagonism|image_file=Cisatracurium.svg}} | | halflife_redistribution = | ||
| protein_binding = | |||
| clearance = | |||
| halflife_elimination = | |||
| adverse_effects = Anaphylactic reaction | |||
Histamine release | |||
| metabolism = Hofmann Elimination | |||
| duration = 45 minutes | |||
| time_onset = 3 to 5 minutes | |||
| dosage_calculation = cisatracurium | |||
| mechanism = Nicotinic acetylcholine antagonism | |||
| image_file = Cisatracurium.svg | |||
}} | |||
'''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. -->== | ||
* 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<!-- List contraindications and precautions for use of the drug. -->== | ==Contraindications<!-- List contraindications and precautions for use of the drug. -->== | ||
| Line 17: | Line 38: | ||
===Absolute contraindications<!-- List absolute contraindications for use of the drug. If none, this section may be removed. -->=== | ===Absolute contraindications<!-- List absolute contraindications 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. -->=== | * Known hypersensitivity | ||
===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 | |||
* 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== | ==Pharmacology== | ||
===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 -->=== | ||
* Roughly about 3 times the potency of atracurium | |||
====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. | |||
====Adverse effects<!-- Describe any potential adverse effects of the drug. -->==== | ====Adverse effects<!-- Describe any potential adverse effects of the drug. -->==== | ||
* 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<!-- Describe the pharmacokinetics of the drug. -->=== | ===Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. -->=== | ||
* 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" /> | |||
==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<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<ref name=":1" /> | |||
==References== | ==References== | ||
Latest revision as of 13:14, 8 January 2023
Cisatracurium
| Trade names |
Nimbex |
|---|---|
 | |
| 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 | |
| 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
- ↑ 1.0 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
- ↑ 2.0 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
Top contributors: Cornel Chiu and Chris Rishel