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Pharmacology 680 > Anticholinesterase and Anticholinergics > Flashcards

Anticholinesterase and Anticholinergics Flashcards

1
Q

inhibition of AChE allows for __ ACh to be available

A

more

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2
Q

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

A

acetylcholinesterase (AChE)

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3
Q

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

A

enzyme inhibition

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4
Q

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

A

presynaptic effect

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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

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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

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7
Q

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

A

edrophonium

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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

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9
Q

carbamylated AChE 1/2 life is..

A

15-30 mins

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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

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11
Q

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

A

organophosphate anticholinesterase agents

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12
Q

examples of organophosphase anticholinesterase agents

A

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

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13
Q

neostigmine, pyridostigmine and endrophonium share these chemical properties

A

have a quaternary ammonium (found on NMB and ACh)

poor lipid solubility

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14
Q

tertiary amine that is lipid soluble and can cross the BBB

A

physostigmine

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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

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16
Q

important doses to know RAN

A

Rubinol 0.015
Atropine 0.030
Neostigmine 0.060

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17
Q

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

A

endrophonium (enlon)

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18
Q

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

A

pyridostigmine (mestinon)

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19
Q

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

A

physostigmine (antilirium)

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20
Q

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

A

physostigmine (antilirium)

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21
Q

what anticholinesterase is better to reverse atracurium

A

edrophonium

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22
Q

what anticholinesterase is better to reverse vecuronium

A

neostigmine

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23
Q

deep NMB is reversed better with …

A

neostigmine (think infusions of atracurium, vecuronium, pancuronium)

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24
Q

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

A

ceiling effect

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25
Q

what 5 things effect the reversal of NMB?

A 
antibiotics
hypothermia
resp acidosis
hypokalemia
met acidosis
26
Q

What are the two types of cholinergic receptors (ACh)

A

nicotinic and muscarinic

27
Q

all receptors within a ANS ganglion and NMJ

A

nicotonic

28
Q

Muscarinic receptor locations (M1. M2, M3)

A

M1 - the CNS, stomach
M2 - heart, airway smooth muscles
M3 - airway smooth muscles and salivary glands, contraction and secretion

29
Q

what is the goal of an anticholinesterase

A

reversal of nmj blockade

30
Q

cardiovascular effects of anticholinesterases

A

bradycardia, junctional rhythm, PVCs, vent rhythms, asystole

by the slowing of AV node conduction

31
Q

GI GU effects of anticholinesterases

A

increased secretions
increased motility
Post op N/V (PONV)

32
Q

pulmonary effects of anticholinesterases

A

bronchoconstriction

increased secretions

33
Q

effects of anticholinesterases on opthalmic

A

miosis - pupil contriction
constriction of ciliary muscles (far sighted)
decreased intraocular pressure

34
Q

muscular effects of anticholinesterases

A

contractions and fasciculations so use caution with pt exhibiting myotonia, muscular dystrophies, spinal cord transection and burns

35
Q

what causes an anticholinesterase overdose?

A

too little ACh

36
Q

weakness ranging in paralysis

A

nicotinic anticholinesterases OD

37
Q

miosis, inability to focus vision close, salivation, bronchoconstriction, bradycardia, abd cramps, loss of bowel and bladder control

A

muscarinic anticholinesterase OD

38
Q

confusion, ataxia, seizures, coma, resp depression

A

CNS anticholinesterases OD

39
Q

How do you treat anticholinesterases OD?

A

atropine - anti muscarinic
pralidoxime - antidote, but give within mins
ventilatory support
control of seizures

40
Q

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

A

MOA of pralidoxime

41
Q

how to prevent muscarinic effects of anticholinesterases

A

pretreat with anticholinergic drug

atropine, gycopyrrolate, scopalamine

42
Q

compete with ACh for all muscarinic receptors and bine reversibly with receptors

A

anticholinergic agents

43
Q

Dose 0.03 mg/kg
onset 1 min
elimination by liver and renal

A

atropine

44
Q

what anticholinergic should you use with endrophonium

A

atropine

45
Q

atropine has a __ which means it is lipid soluble and could have cns effects

A

tertiary ammonium

46
Q

what anticholinergic to give with neostigmine

A

glycopyrrolate (rubinol)

47
Q

dose 0.015
onset 2-3 mins
excreted renally

A

glycopyrrolate (robinol)

48
Q

can robinol cross the bbb

A

no because it is a quarternary ammonium so has minimal or no cns effects

49
Q

dose 0.4 mg im/iv
onset IV 10 mins, IM 30-60 mins
elimination hepatic

A

scopalamine

50
Q

this med is given with emergent cases if you have hemodynamic instability, it can also cause amnesia
sedation, treats ponv

A

scopalamine

51
Q

antisialagogue effect
sedation
prophylactic for vagal response

A

clinical uses of anticholinergics

52
Q

what two antichol cause glaucoma mydriatic effect and crosses the placental membrane

A

atropine and scopalamine

53
Q

HR increases the most with which antichol

A

atropine

54
Q

which has the best antisialagogue effect (dries up secretions)

A

scopalamine

55
Q

what antichol enhances side effects of opioids and benzos

A

scopalamine

56
Q

how does using an anticholinergic treat bradycardia. what two are used for this

A

blocks the effect of ACh on the SA node (shortens PR interval)
atropine > robinol

57
Q

what two meds are ideal in neonate/infant group because their HR is tied with CO?

A

atropine and neostigmine

58
Q

some clinical uses of anticholinergics

A

bronchodilation
antispasmotic (biliary, uretrl)
mydriasis and cyclopleiga
prophylaxis of PONV

59
Q

CNS effects from scopolamine and atropine cause restlessness and hallucinations to somnolence and unconsciousness

A

central anticholinergic syndrome

60
Q

treatment of central anticholinergic syndrome?

A

physostigmine 0.015-0.060 mg/kg

61
Q

dry mouth, blurred vision, tachycardia, dilation of cutaneous vessels, increased temp, sensitivity to light

A

symptoms of central anticholinergic syndrome

Pharmacology 680 (19 decks)

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