Neuromuscular Agents Flashcards
Types of nicotinic receptors
Nn: CNS excitation
Ng: autonomic ganglia –> ganglionic transmission
Nm: skeletal muscle contraction
What are the nondepolarizing NM blockers?
Isoquinolones: -atracurium -cisatracurium -doxacurium Steroid-like -Pancuronium -Rocuronium -Vecuronium
What are the depolarizing NM blockers?
succinylcholine
What isoquinolone is no longer used?
Tubocurarine
Describe the onset, elimination, and clearance of isoquinolones
Onset: faster in younger patients
Elimination: spontaneous hydrolysis (atracurium and cisatracurium; temperature & pH dependent process
Clearance: 5-6 mL/kg/min
List the isoquinolones in order of potency and duration of action (highest to lowest)
Doxacurium
Cisatracurium
Atracurium
What are the indications of isoquinolones?
- skeletal muscle relaxation or mechanical ventilation during surgery
- endotracheal intubation
What is the reversal agent for isoquinolones?
Neostigmine with atropine
-increases ACh which stimulates nerve and mAChR
What are the adverse reaction of isoquinolones?
- dose dependent histamine release
- cutaneous flushing, hypotension
- CV effects (tachycardia)
- seizures wit atracurium
- Laudanosine (metabolite from cisatracurium)
Describe the elimination and clearance of steroid-like blockers
elimination: kidneys (pancuronium) and liver (rocuronium & vecuronium)
clearance: 1.7-5.3 mL/kg/min
What are the indications for steroid-like blockers?
- skeletal muscle relaxation or mechanical ventilation during surgery
- endotracheal intubation
- euthanasia (pancuronium/rocuronium)
What are the adverse effects of using steroid-like blockers?
- sinus tachycardia (pancuronium > rocuronium)
- hypotension
- at high doses – relaxed diaphragm mediated asphyxiation
What is the reversal agent for rocuronium and vecuronium?
neostigmine
- increase ACh –> stimulate nerve and nAChR
- 17 min reversal time
Describe Sugammadex
- used to reverse rocuronium (then vecuronium and pancuronium)
- rapid, so 1st selective relaxant binding agent (SRBA)
- doesn’t inhibit AChE
- inactivates rocuronium by wrapping around it
- expensive
What is the mode of action for succinylcholine?
repeated activation of nAChRs –> increased depolarization = paralysis