Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology 680 > Anticholinesterase and Anticholinergics > Flashcards

Anticholinesterase and Anticholinergics Flashcards

(61 cards)

Start Studying
1
Q

inhibition of AChE allows for __ ACh to be available

A

more

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

the enzyme that hydrolyzes ACh molecules at 300,000 molecules per minute

A

acetylcholinesterase (AChE)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

this MOA of anticholinesterases inhibits AChE by causing carbamylation of AChE or by attaching to the enzyme

A

enzyme inhibition

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

this MOA of anticholinesterases causes increased availability of ACh, which in the absence of a nmb can cause contractions

A

presynaptic effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

this MOA of anticholinesterases causes decreased sensitivity resulting in a blockade effect due to an increased amount of ACh at the NMJ

A

direct effect on NMJ

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

these two anticholinesterases “compete” with ACh to be hydrolyzed by the AChE. If these drugs “win” they cause the enzyme to be carbamylated and decrease its ability to hydrolyze ACh

A

neostigmine and pyridiostigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

this anticholinesterase attaches to AChE electrostatically to decrease its ability to hydrolyze ACh

A

edrophonium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

causes chemical change in the enzyme and reversibly inhibits its ability to hydrolyze ACh by being hydrolyzed by AChE

A

neostigmine, pyridostigmine and physostigmine

carbamylation of AChE - reversible inhibition

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

carbamylated AChE 1/2 life is..

A

15-30 mins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

forms a reversible electrostatic attachment to AChE to inhibit its ability to hydrolyze ACh so ACh can move around and do its business

A

electrostatic bound - truly reversible inhibition

endrophonium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

these from an irreversible complex that must be replaced with generation of NEW enzyme

A

organophosphate anticholinesterase agents

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

examples of organophosphase anticholinesterase agents

A

echothiophate - eye drops
insecticides (dog washer)
nerve gases - think war

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

neostigmine, pyridostigmine and endrophonium share these chemical properties

A

have a quaternary ammonium (found on NMB and ACh)

poor lipid solubility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

tertiary amine that is lipid soluble and can cross the BBB

A

physostigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Dose 0.06 mg/kg (max 0.07 (peds) and 5 mg)
Onset 7 to 11 mins
elimination 50% renal and 50% plasma esterases and hepatic met

A

neostigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

important doses to know RAN

A

Rubinol 0.015
Atropine 0.030
Neostigmine 0.060

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Dose 0.5 to 1 mg/kg
onset 30-60 seconds
elimination is 75% renal

A

endrophonium (enlon)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

dose 0.3 mg/kg
onset 10-20 mins
elimination 75% renal

A

pyridostigmine (mestinon)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

dose 0.5 - 2 mg
onset 5 mins
elimination hepatic and hydrolysis by cholinesterases

A

physostigmine (antilirium)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

used to treat CNS effects of anticholinergic agents, anesthetics, reduces shivering, emergence delirium

A

physostigmine (antilirium)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

what anticholinesterase is better to reverse atracurium

A

edrophonium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

what anticholinesterase is better to reverse vecuronium

A

neostigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

deep NMB is reversed better with …

A

neostigmine (think infusions of atracurium, vecuronium, pancuronium)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

once AChE is maximally inhibited, giving more of a anticholinesterase will NOT reverse a NMB

A

ceiling effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
what 5 things effect the reversal of NMB?
``` antibiotics hypothermia resp acidosis hypokalemia met acidosis ```
26
What are the two types of cholinergic receptors (ACh)
nicotinic and muscarinic
27
all receptors within a ANS ganglion and NMJ
nicotonic
28
Muscarinic receptor locations (M1. M2, M3)
M1 - the CNS, stomach M2 - heart, airway smooth muscles M3 - airway smooth muscles and salivary glands, contraction and secretion
29
what is the goal of an anticholinesterase
reversal of nmj blockade
30
cardiovascular effects of anticholinesterases
bradycardia, junctional rhythm, PVCs, vent rhythms, asystole | by the slowing of AV node conduction
31
GI GU effects of anticholinesterases
increased secretions increased motility Post op N/V (PONV)
32
pulmonary effects of anticholinesterases
bronchoconstriction | increased secretions
33
effects of anticholinesterases on opthalmic
miosis - pupil contriction constriction of ciliary muscles (far sighted) decreased intraocular pressure
34
muscular effects of anticholinesterases
contractions and fasciculations so use caution with pt exhibiting myotonia, muscular dystrophies, spinal cord transection and burns
35
what causes an anticholinesterase overdose?
too little ACh
36
weakness ranging in paralysis
nicotinic anticholinesterases OD
37
miosis, inability to focus vision close, salivation, bronchoconstriction, bradycardia, abd cramps, loss of bowel and bladder control
muscarinic anticholinesterase OD
38
confusion, ataxia, seizures, coma, resp depression
CNS anticholinesterases OD
39
How do you treat anticholinesterases OD?
atropine - anti muscarinic pralidoxime - antidote, but give within mins ventilatory support control of seizures
40
attaches to site where a cholinesterase inhibitor has attaches, then attaches to the inhibitor, removes the organophoshphate from cholinesterase which allows AChE to work again
MOA of pralidoxime
41
how to prevent muscarinic effects of anticholinesterases
pretreat with anticholinergic drug | atropine, gycopyrrolate, scopalamine
42
compete with ACh for all muscarinic receptors and bine reversibly with receptors
anticholinergic agents
43
Dose 0.03 mg/kg onset 1 min elimination by liver and renal
atropine
44
what anticholinergic should you use with endrophonium
atropine
45
atropine has a __ which means it is lipid soluble and could have cns effects
tertiary ammonium
46
what anticholinergic to give with neostigmine
glycopyrrolate (rubinol)
47
dose 0.015 onset 2-3 mins excreted renally
glycopyrrolate (robinol)
48
can robinol cross the bbb
no because it is a quarternary ammonium so has minimal or no cns effects
49
dose 0.4 mg im/iv onset IV 10 mins, IM 30-60 mins elimination hepatic
scopalamine
50
this med is given with emergent cases if you have hemodynamic instability, it can also cause amnesia sedation, treats ponv
scopalamine
51
antisialagogue effect sedation prophylactic for vagal response
clinical uses of anticholinergics
52
what two antichol cause glaucoma mydriatic effect and crosses the placental membrane
atropine and scopalamine
53
HR increases the most with which antichol
atropine
54
which has the best antisialagogue effect (dries up secretions)
scopalamine
55
what antichol enhances side effects of opioids and benzos
scopalamine
56
how does using an anticholinergic treat bradycardia. what two are used for this
blocks the effect of ACh on the SA node (shortens PR interval) atropine > robinol
57
what two meds are ideal in neonate/infant group because their HR is tied with CO?
atropine and neostigmine
58
some clinical uses of anticholinergics
bronchodilation antispasmotic (biliary, uretrl) mydriasis and cyclopleiga prophylaxis of PONV
59
CNS effects from scopolamine and atropine cause restlessness and hallucinations to somnolence and unconsciousness
central anticholinergic syndrome
60
treatment of central anticholinergic syndrome?
physostigmine 0.015-0.060 mg/kg
61
dry mouth, blurred vision, tachycardia, dilation of cutaneous vessels, increased temp, sensitivity to light
symptoms of central anticholinergic syndrome

Pharmacology 680 (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions