NMB Reversal Agents & Anticholinergics Flashcards
What three ways do AchE inhibitors bind to and inhibit AchE?
Electrostatic attachment
Carbamyl esters
Phosphorylation
What does edrophonium inhibit Ach?
Electrostatic attachment
How does neostigmine, pyridostigmine and physostigmine inhibit Ach?
Formation of carbamyl esters
What do organophosphates and echothiopate inhibit Ach?
Phosphorylation
(This is non-competitive)
What are the pharmacokinetics and pharmacodynamics or edrophonium?
Dose: 0.5-1.0 mg/kg
Onset: 1-2 minutes
Duration: 30 mins
Metabolism: renal ~ 75%; liver 25%
Best pairing: Atropine!
What are the pharmacokinetics and pharmacodynamics of neostigmine?
Dose: 0.02-0.07 mg/kg
Onset: 5-15 mins
Duration: 45-90 mins
Metabolism: renal 50%; liver 50%
Best pairing: Glyco
What are the pharmacokinetics and pharmacodynamics of pyridostigmine?
Dose: 0.1-0.3 mg/kg
Onset: 10-20 mins
Duration: 60-120
Metabolism: renal (75%); Liver (25%)
Best pairing: Glyco
Which AchE inhibitors pass through the blood-brain barrier? Which do not?
Does pass: physostigmine
Does not pass: edeophonium, neostigmine, pyridostigmine
What are the side effects of AchE inhibitors? Think mnemonic dumbbells
D: diarrhea
U: urination
M: miosis
B: Bradycardia
B: bronchoconstriction
E: Emesis
L: lacrimination
L: laxation (pooping)
S: salivation
Which anticholinergic is most likely to cause xerostomia (dry mouth)
Glycopyrrolate
What are atropine’s main effects?
HR > Smooth muscle relaxation (bronchodilation) > Mydriasis
What are scopolamine’s main effects?
Sedation = antisialagogue = mydrasis = motion induced nausea
What are gylcos main effects?
Antisialagogue = HR = smooth muscle dilation
(Not as much as atropine though)
Which muscarinic antagonists are tertiary amines?
Atropine
Scopolamine
They pass the BBB
Does muscarinic antagonists affect HR in transplant patients?
No. The nerve endings are denervated
