apex cholinergics

Question 1

AchE Inhibitors: MOA

Answer 1

acetylcholinesterase hydrolyzes Ach into choline and acetate. This enzyme is found at the nicotinic receptors at the NMJ. even though concentration of Ach is increased, the neuromuscular blocker still needs to be eliminated from the body.

Question 2

Tell me about pseudocholinesterase

Answer 2

it is located in the PLASMA! it metabolizes succinylcholine. it is inhibited by neostigmine and pyridostigmine but not EDROPHONIUM. there if succs is given after neostigmine or pyridostigmine succs will be prolonged.

Question 3

achE Inhibitors at the presynaptic receptor 2 functions

Answer 3

1. stimulate the presynaptic receptor and cause it to release additional Ach.
2. increase the concentration of Ach in the region.

Question 4

Renal Failure and AchE Inhibitors & NMBs

Answer 4

renal failure prolongs the duration of both Ache Inhibitors and nmb’s both drugs remain in the body for a longer period of time. there is no need to adjust the dose of AchE inhibitors or re dose it.

Question 5

Tell me about giving additional doses of Ache inhibitors?

Answer 5

it has a ceiling effect above which additional drug does not produce better recovery.

Question 6

what happens with AchE Inhibitors and depth of block

Answer 6

the onset of actions inversely related to the depth of the block. it will take longer to reach peak effect with a 90% twitch suppression when compared to a 50% twitch suppression

Question 7

what happens when you mix AchE inhibitors?

Answer 7

it has an additive effect

Question 8

antagonism of Neostigmine is faster in what population

Answer 8

faster in infants and children compared to adults.

Question 9

neostigmine Side effect

Answer 9

associated with N&V

Question 10

name 3 drugs (AchE Inhibitors) that do NOT pass through the blood brain barrier

Answer 10

edrophonium, neostigmine, pyridostigmine

Question 11

name 1 drug (AchE) that does pass through the blood brain barrier

Answer 11

Physostigmine

Question 12

name a drug that reduces the incidence of post operative shivering

Answer 12

physostigmine! matches the efficacy of meperidine and clonidine

Question 13

intrathecal Neostigmine

Answer 13

produces analgesia, side effects include nausea vomiting pruritus and prolongation of sensory and motor block

Question 14

increase the concentration of acetylcholine at the muscarinic receptors what are the side effects?
is it parasympathetic or sympathetic?
how do we increase the amount of ACH at these receptors

Answer 14

we use the ACHE inhibitors 
they cause predictable set of parasympathetic side effects
diarrhea
urination
miosis
bronchostriction
bradycardia
excitation of the skeletal muscles/ emesis
lacrimination
laxation
salviation

Question 15

muscarinic antagonists

tell me the order of heart rate increase greatest to least

Answer 15

atropine-glycopyrrolate-scopolamine

Question 16

smooth muscle relaxation greatest to least

Answer 16

atropine=glycopyrrolate-scolopamine

Question 17

sedation greatest to least

Answer 17

scopolamine!! some atropine none for glycopyrolate

Question 18

antisialagogue greatest to least

Answer 18

scopolamine - glycopyrrolate- atropine

Question 19

mydriasis/cycloplegia greatest to least

Answer 19

scopolamine- some atropine non glycopyrolate.

Question 20

prevent motion induced nausea greater to least

Answer 20

scopolamine some atropine, none glycopyrrolate

Question 21

decrease gastric H+ secretion

Answer 21

scopolamine=atropine=glycopyrrolate

Question 22

affect fetal heart rate

Answer 22

NONE

Question 23

Name 2 drugs that are naturally occurring?

what membranes do they cross?

Answer 23

atropine and scopolamine are naturally occurring and are lipophilic, they easily cross BBB, GI Tract and placenta

Question 24

what drug is not naturally occurring?

Answer 24

Glycopyrrolate is is ionized and cannot cross the placenta

Question 25

do muscarinic antagonist affect the heart rate of heart transplant patient?

Answer 25

NO, even so these patients will still experience other cholinergic effects form AchE inhibitors so they should receive a muscarinic antagonist with an AchE inhibitor.

Question 26

sugammadex which drugs does it work with

Answer 26

Roc, Vec, pan

Question 27

dose of sugammadex? 2/4 twitches or better?

Answer 27

2mg/kg

Question 28

TOF 0/4

Answer 28

4mg/kg

Question 29

1.2mg/kg of rocuronium and reversing 3 minutes after roc sugammadex dose?

Answer 29

16mg/kg

Question 30

how is sugammadex secreted

Answer 30

unchanged by the kidneys

Question 31

what do you do if sugammadex was given within 24 hours and patents needs to be reparalyzed?

Answer 31

succs, atracurium, cisatrcurium or mivacurium.

if the sugammadex dose was equal or less than 4mg/kg you can redoes roc or vec

Question 32

tell me about sugammadex and oral contraceptive

Answer 32

it binds to it. tell your patient to use other forms for 1 week of protection.