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Anesthesia Drug Test Quick Facts > Acetylcholinesterase Inhibitors > Flashcards

Acetylcholinesterase Inhibitors Flashcards

1
Q

brand name of neostigmine

A

Bloxiverz

prostigmin

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2
Q

how is neostigmine supplied?

A

1mg/mL

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3
Q

classification of neostigmine

A

quaternary ammonium anticholinesterase

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4
Q

MOA of neostigmine

A

reversible inhibition of the enzyme acetylcholinesterase
Hydrolyzed by Achesterase and in the process the ach esterase gets carbamylated (forms a drug enzyme complex) and becomes inefficient at hydrolyzing acetylcholine until the drug enzyme bond dissociates.
This inhibition of the hydrolysis of acetylcholine results in greater availability of Ach at its sites of action, which include preganglionic sympathetic and parasympathetic nerve endings and the NMJ.
Primary effect at post synaptic

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5
Q

use of neostigmine

A

antagonie effects of NDNMB
tx of atony in urinary bladder
off-label for dx and tx of MG in children

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6
Q

dose of reversal of non depolarizing NMB of neostigmine

A

IV 0.03-0.07 mg/kg

*glycopyrolate 0.01mg/kg or atropine 0.02 mg/kg must be given prior to or in conjunction with neostigmine to prevent bradycardia

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7
Q

what determines initial and subsequent doses of neostigmine?

A

TOF

Drug used as paralytic

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8
Q

dose of neostigmine with Roc typically

A

0.03 mg/kg

shorter half life NMBA

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9
Q

dose of neostigmine with NMBA with longer halflives

A 
ved
panc
0.07 mg/kg
or first twitch response is relatively weak
rapid recovery is needed
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10
Q

how is neostigmine dosed with renal patients

A

reduction of dose

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11
Q

how does neostigmine affect elderly pt?

A

prolonged duration

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12
Q

how does neostigmine affect infants?

A

dose can be reduced

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13
Q

dose of neostigmine for post op renal retention

A

IM Sub Q

0.25 mg

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14
Q

onset of neostigmine

A

IV 7-11 minues

intermediate

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15
Q

peak of neostigmine

A

5-10 minues

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16
Q

duration of neostigmine

A

54 minues

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17
Q

half life of neostigmine

A

77 minutes

doubles’ in renal pt

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18
Q

metabolism of neostigmine

A

hepatic metabolist 50%
without renal function
metabolite active 1/10th activity of neostigmine

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19
Q

elimination of neostigmine

A

50% renal unchanged drug

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20
Q

adverse effects of neostigmine

A

CV: BRADYCARDIA, hypotension, decreased SVR, increase is CAD arrhythmias, ACS, or MG or BB pts

Syncope, tachycardia, sinus arrest & brady not stopped post transplant even with glycol

CNS: convulsions, dizzy, drowsy, dysphonia, HA, LOC

Derm, rash, thrombophlebitis, urticarial,

GI: diarrhea, dysphagia, flatulence, hyperperistalsis, Nausea, salivation, cramps vomit, PONV

GU: urgency

NM: arthralgieas fasciculation, crams, spasm, weak

Ocular, small pupils (miosis) can not accomidate near vision

Resp: bronch constrict dyspnea, secretions, laryngospasm, resp arrest, resp depression, resp muscle paralysis

Allergic, analphylaxis, diaphoresis

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21
Q

contraindications of neostigmine

A

cholinergic crisis

hx of rxn with bromides

*crisis= overdose of cholinergic- brady cardia- atropine must be ready all muscarinic symptoms listed – bradycardia and resp muscle paralysis may be fatal

marked and prolonged inhibition of plasma cholinesterase: leaks to prolonged effect of SUCC

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22
Q

how does volatile agent affect neostigmine?

A

delay reversal

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23
Q

what is best for reversing atracurium

A

edrophonium

not neostigmine

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24
Q

typical dose of neostigmine

A

1 mg
glycopyrolate - onset matches onset of neostigmine better than atropine- would see initial tackycardia with atropine/neo and brady cardia as atropine is faster off

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25
brand name of edrophonium
Tensilon | Enlon
26
how is edrophonium supplied
10mg/mL
27
classification of edrophonium
quaternary ammonium anticholinesterase
28
MOA of edrphonium
Forms a reversible electrostatic attachment to the acetylcholinesterase enzyme in order to inhibit its activity. Normally it rapidly hydrolyzes Ach into chiline and acetic acid. More Ach at sites of action! Reversal Pre-Synaptic affecting Ach release more. But parasympathetic and NMJ as well. fasciculate d/t pre-synaptic MOA if no NMNMB on board
29
what can high doses of edrophonium lead to?
excess of Ach at the NMJ and cause desensitization leading to neuromuscular blockade
30
dose of edrophonium for reversal of NBNMB
reversal of non depolarizing neuromuscular blocking agents IV 0.5 mg/kg MUST give with atropine 7mcg/kg upto 10-15 mcg/kg) 1 mg/kg if twitch is
31
onset of edrophonium
IV 30-60 seconds SHORT ONSET
32
duration of edrophonium
60 minutes
33
peak of edrophonium
5-10 minutes reach peak
34
half life of edrophonium
110 mins (doubles when anephric)
35
elimination of edrophonium
67% renal
36
metabolism of edrophonium
Without renal function, hepatic metabolism is 30% conjugation
37
adverse reactions with edrophonium
Mild b/c short act CV: BRADYCARDIA, hypotension, av block, nodal rhythm changes Syncope, tachycardia CNS: convulsions, dizzy, drowsy, dysphonia, HA, LOC Derm, rash, thrombophlebitis, urticarial, GI: diarrhea, dysphagia, flatulence, hyperperistalsis, Nausea, salivation, cramps vomit GU: urgency NM: arthralgieas fasciculation, crams, spasm, weak Ocular, small pupils (miosis) can not accomidate near vision Resp: bronch constrict dyspnea, secretions, laryngospasm, resp arrest, resp depression, resp muscle paralysis Allergic, analphylaxis, diaphoresis
38
contraindications with edrophonium
Hypersensitivity to this, sulfites, GI/GU obstruction, with MG risk of cholinergic crisis if they have also received NDNMB
39
predominate site of edrophonium's action?
pre-synaptic Ach release
40
predominate site of neostigmine's action?
post-synaptic
41
which anticholineric has the most similar onset to edrophonium?
atropine rapid onset for both preferred with edrophonim
42
can edrophonium be used to reverse a phase II block fro Sch?
yes | as long as the pt does not have atypical plasma cholinesterase
43
what are the desired effects of NMB reversal?
want nicotinic cholinergic effects = reverse weakness want to minimize muscarinic cholinergic effects (give anti-cholinergic)
44
brand name of physostigmine
physostigmine | no brand name
45
how is physostigmine supplied?
1 mg/mL
46
classification of physostigmine?
lipid soluble tertiary amine | carbamate
47
MOA of physostigmine
inhibits the enzyme of acetylcholinesterase and prolongs the central and peripheral effects of acetylcholine
48
property of physostigmine
tertiary amine lipid soluble crosses BBB easily increases concentration of Ach in the brain
49
uses of physostigmine
antagonism of central anticholinergic effects reversal of toxic life-threatening delirium from pure anticholinergic agents (atropine, diphenhydramine, dimenhydrinate, Atropa belladonna, jimson weed) *treats somnolent effects of opiods and may reverse the depression of the ventilator response to C02 but no analygesia of morphine *post of shivering
50
dose of physostigmine for reversal of toxic anticholinergic effect
15-60 mcg/kg initial, 0.5-2 mg repeat q 10-30 minutes until response NO faster than 1mg/min
51
peak of physostigmine
no peak
52
onset of physostigmine
several minutes *
53
duration of physostigmine
45-60 minutes | *shorter than the anticholinergics and MAY require redosing
54
adverse reactions with physostigmine
CV: Asystole, bradycardia, palpitation CNS: hallucinations, nervousness, restlessness, seizure GI: defication, diarrhea, nausea, salivation, stomach pain, vomiting GU: frequency NMS: twitching Ocular: lacrimation, miosis Respiratory: bronchospasm, dyspnea, pulmonary edema, respiratory distress, respiratory paralysis Msc. Diaphoresis, hypersensitivity * augments secretions of glands innervated by postganglionic cholinergic fibers: bronchial, lacrimal, sweat, salivary, gastric, intestinal, acini pancreatic
55
metabolism of physostigmine
hydrolysis of cholinesterases
56
elimination of physostigmine
?
57
contraindications of physostigmine
Bromide tox possible NO w/asthma, gangrene, DM, CV disease, obstruction of intestine or GU tract, vagotonic state, pt on choline esters, DNMBA (succs) *contains sodium bisulfite- allergic rxn
58
how does volatile anesthetic administration influence the effects of neostigmine and pyridostigmine
delays reversal
59
what conditions can inhibit reversal?
hypothermia hypokalemia acidosis some antibiotics
60
properties of pyridostigmine and neostigmine
quaternary ammonium group = POORLY lipid soluble | does not cross GI or BBB
61
brand name of pyridostigmine
mestinon | regonol
62
how is pyridostigmine supplied
5mg/mL
63
classification of pyridostigmine
quaternary ammonium anticholinesterase
64
MOA of Pyridostigmine
Reversible inhibition of the enzyme Acetylcholinesterase. Hydrolyzed by Ach-esterase and in the process the ach esterase gets carbamylated (forms a drug enzyme complex) and becomes inefficient at hydrolyzing acetylcholine until the drug enzyme bond dissociates. This inhibition of the hydrolysis of acetylcholine results in greater availability of Ach at its sites of action, which include preganglionic sympathetic and parasympathetic nerve endings and the NMJ. Primary effect at post synaptic
65
where is the primary effect of pyridostigmine?
Primary effect at post synaptic
66
dose of pyridostigmine
Reversal of NDNMB IV 0.1-0.25 mg/kg Glyco 10 mcg/kg or Atropine 20 mcg/kg IV must be given before Reduce with renal and elderly (d/t delayed plasma clearance) Push, IM, infusion also
67
MG oral dose of pyridostigmine
60-1500 usually 600 mg/day 5-6 dose divided over
68
onset of pyridostigmine
as long as 16 minutes onset is VERY slow expect tachycardia bc the onset of the atropine and glycol will occur before the effect of the drug
69
duration of pyridostigmine
IV 2-3 hours | oral upto 6-8 hours
70
what is oral pyridostigmine used to treat?
Myasthenia Gravis
71
peak of pyridostigmine
plasma concentrations peak in 5-10 minutes
72
half life of pyridostigmine
1-2 hours | unto 6 hours in renal failure
73
metabolism of pyridostigmine
in absence of renal function | hepatic metabolism is 25%
74
elimination of pyridostigmine
75% renal elimination as unchanged drug
75
Adverse effects of pyridostigmine
CV: BRADYCARDIA, hypotension, decreased SVR, increase is CAD arrhythmias, ACS, or MG or BB pts Syncope, tachycardia, sinus arrest & brady not stopped post transplant even with glycol CNS: convulsions, dizzy, drowsy, dysphonia, HA, LOC Derm, rash, thrombophlebitis, urticarial, GI: diarrhea, dysphagia, flatulence, hyperperistalsis, Nausea, salivation, cramps vomit, PONV GU: urgency NM: arthralgieas fasciculation, crams, spasm, weak Ocular, small pupils (miosis) can not accomidate near vision Resp: bronch constrict dyspnea, secretions, laryngospasm, resp arrest, resp depression, resp muscle paralysis Allergic, analphylaxis, diaphoresis
76
contraindications with pyridostigmine
Bromides rxn history (pills) GI/GU obstruction with MG risk of cholinergic crisis if they have also received NDNMB

Anesthesia Drug Test Quick Facts (19 decks)

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