NMB reversal agents

Question 1

what type of bond is formed when edrophonium binds to the anionic site in acetylcholinesterase

Answer 1

electrostatic

Question 2

how does edrophonium, neostigmine, and pyridostigmine work

Answer 2

reversibly inhibits AchE which inadvertently increases Ach at the NMJ.

Question 3

which drugs inhibit pseudocholinesterase

Answer 3

neostigmine and pyridostigmine (not edrophonium, which inhibits AchE)

Question 4

2 ways that AchE inhibitor increases concentration of Ach at nicotinic receptor

Answer 4

1. enzyme inhibition
2. presynaptic effects

Question 5

AchE inhibiting drugs bind to and inhibit AchE by interacting with these sites in 1 of 3 ways

Answer 5

1. electrostatic attachment
2. formation of carbamyl esters
3. phosphorylation

Question 6

how Ach is inhibited: electrostatic attachment
type of inhibition:
examples:

Answer 6

type of inhibition: competitive
examples: edrophonium

Question 7

how Ach is inhibited: formation of carbamyl esters
type of inhibition:
examples:

Answer 7

type of inhibition: competitive
examples: neostigmine, pyridostigmine, physostigmine

Question 8

how Ach is inhibited: phosphorylation
type of inhibition:
examples:

Answer 8

type of inhibition: non competitive
examples: organophosphates, echothiopate

Question 8

how Ach is inhibited: phosphorylation
type of inhibition:
examples:

Answer 8

type of inhibition: non competitive
examples: organophosphates, echothiopate

Question 9

primary MOA of edrophonium is most likely

Answer 9

presynaptic (more Ach avail stimulates release of more Ach)

Question 10

edrophonium
dose
onset
DOA
metabolism and elimination
best pairing

Answer 10

dose: .5-1mg/kg
onset: 1-2m
DOA: 30-60m
metabolism and elimination: renal 75%, liver 25%
best pairing: atropine

Question 11

neostigmine
dose
onset
DOA
metabolism and elimination
best pairing

Answer 11

dose: .02-.07mg/kg
onset: 5-15m
DOA: 45-90m
metabolism and elimination: renal 50% liver 50%
best pairing: glyco

Question 12

pyridostigmine
dose
onset
DOA
metabolism and elimination
best pairing

Answer 12

dose: .1-.3
onset: 10-20m
DOA: 60-120m
metabolism and elimination: renal 75% liver 25%
best pairing: glyco

Question 13

renal failure and AchE

Answer 13

prolongs DOA of AchE and NMB but no need to re dose anything

Question 14

quarternary amine AchE’s

Answer 14

edrophonium, neostigmine, pyridostigmine

Question 15

which AchE can you use for postop shivering

Answer 15

physostigmine 40mcg/kg

Question 16

by increasing Ach availability, AchE’s produce these PSNS SE’s

Answer 16

DUMBBELLS
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation (increased tear production)
Laxation (elimination of fecal waste)
Salivation

Question 17

compared to atropine, glyco is more likely to produce

Answer 17

xerostomia (dry mouth)

Question 18

review scopolamine, atropine, and glyco in terms of how much each (in comparison to each other)
increases HR
smooth muscle relaxation
sedation
antisialagogue
mydriasis and cycloplegia
prevent motion induced nausea
decreases gastric H+ secretion

Answer 18

Question 19

why does glyco not possess CNS activity

Answer 19

it is a quarternary amine

Question 20

best to least antagonized drug with sugammadex

Answer 20

roc>vec>panc

Question 21

how is sugammadex excreted

Answer 21

unchanged via kidneys

Question 22

finish this chart
(dose per twitch response)

Answer 22

Question 23

use patients ______ body weight to dose sugammadex

Answer 23

actual

Question 24

what if the patient needs to be re dosed after 16mg/kg sugammadex within 24h?

Answer 24

use non amino steroid NMB (atracurium, cis, mivacurium) or succ

Question 25

what if the patient needs to be re dosed after <4mg/kg sugammadex has been given?

Answer 25

sugammadex in last 5m-4h–>1.2mg/kg roc
>4 hours ago: .6mg/kg roc or .1mg/kg vec

Question 26

how long does sugammadex reduce effectiveness of contraceptives

Answer 26

7 days

Question 27

4 drugs that decrease shivering in the PACU

Answer 27

physostigmine
meperidine
clonidine
dexmedetomidine

Question 28

does glyco cause sedation or mydriasis or prevent nausea

Answer 28

no