7 NMJ Flashcards
Which muscle type does NMJ drugs work on?
skeletal
Why was NMJ drugs introduced in addition to diethyl ether?
diethyl ether was GOOD at inducing unconsciousness and analgesia but NOT very potent at muscle relaxation
What was the first NMJ drug?
curare
Neuromuscular blockers are specific to which type of receptor?
nicotinic ACh
What are two classes of muscle relaxants?
depolarizing (sucs), non-depolarizing
Succinylcholine
agonist for ACh
depolarizing, stimulates muscle (fasciculation)
very rapid, emergency use
metabolized by plasma cholinesterase
many side-effects
Succinylcholine side effects
Bradycardia (esp. children).
• Muscle pains.
• Hyperkalaemia (burns, muscular disease, spinal injury)
• Allergy.
• ↑ intracranial & intraocular pressure.
• (Malignant hyperthermia.)
• (Prolonged in cholinesterase deficiency.)
Are non-depolarizing NMJ drugs competitive or non-competitive inhibition?
competitive at the post-synaptic receptors
two classes of non-depolarizing NMJ are?
Benzylisoquinolines
Aminosteroids
Atracurium
Non organ-dependent elimination: - Ester hydrolysis (enzymic). - Hofmann degradation (non-enzymic). • Causes histamine release. • 10 stereo-isomers.
What’s the advantage of Cisatracurium compared to Atracurium
1 of the isomers
Less histamine release.
• CVS stable
Aminosteroids examples
Rocuronium
Vecuronium
Pancuronium
aminosteroid advantages and composition
completely synthetic, two active sites joined by steroid group
No histamine release
CVS stable
how do you monitor NMJ blockage?
Peripheral nerve stimulator
If NMJ drug is overdosed, how would you reverse the effects?
Anti-Cholinesterase Drugs
• Inhibit Acetylcholinesterase.
• Increase ACh concentration.
• Displace drug from receptor.