NMB Reversal Agents Flashcards

1
Q

What are the two classes of reversal agents?

A
  • acetylcholinesterase inhibitors/anticholinergics
  • selective relaxant binding agent
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2
Q

What reversal agents are considered acetylcholinesterase inhibitors/anticholinergics?

A
  • neostigmine
  • edrophonium
  • pyridostigmine
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3
Q

Which acetylcholinesterase inhibitor is NOT actually used for reversal? What is it used for?

A
  • physostigmine
  • used to treat anticholinergic crisis
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4
Q

What class of reversals does sugammadex fall under?

A

selective relaxant binding agent

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5
Q

How do anticholinesterases work?

A

block/inhibit the breakdown of acetylcholine by blocking acetylcholinesterase (which normally breaks down ACh). this increases number of available ACh at the synaptic cleft, giving it a better chance of binding to receptors than NMBAs

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6
Q

What is acetylcholinesterase (AChE)?

A

enzyme responsible for hydrolysis/breakdown of acetylcholine

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7
Q

Blocking ___________ is a mechanism used to reverse NMBAs

A

acetylcholinesterase (AChE)

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8
Q

Myasthenia gravis can be diagnosed and treated by?

A

administrating acetylcholinesterase inhibitor; prevents breakdown of acetylcholine and increases # of ACh to produce muscle response

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9
Q

What is myasthenia graves? What agent can be used for diagnosis and treatment?

A
  • autoimmune disease where the immune system attacks the NMJ
  • acetylcholinesterase inhibitor
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10
Q

What are some side effects of anticholinesterase agents? (neostigmine, edrophonium, physostigmine)

A
  • unwanted muscarinic stimulation (SLUDGE)
  • cholinergic crisis
  • bronchospasm
  • increased secretions
  • bradycardia (slowing conduction velocity at AV node)
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11
Q

What are some side effects of cholinergic crisis?

A
  • SLUDGE
  • bronchospasm
  • bradycardia
  • hypotension
  • muscle cramping
  • weakness
  • restless, anxiety, confused, seizures, coma
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12
Q

Cholinergic crisis means too much or too little acetylcholine?

A

too much ACh

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13
Q

When are cholinesterase inhibitors used?

A
  • reversal of NMBAs
  • myasthenia gravis dx or tx
  • anticholinergic syndrome tx (atropine overdose)
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14
Q

What are S/S of mild, moderate, and severe anticholinergic syndrome?

A
  • Mild: tachycardia, flushed face, mydriasis (dilation), blurry vision, dry mouth, dry skin, fever
  • Moderate: agitated/delirium, urinary retention, HTN, hyperthermia
  • Severe: CNS depression, coma, seizures, dysrhythmias, hypotension, rhabdomyolysis
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15
Q

Anticholinergic syndrome is too much or too little acetylcholine?

A

too little ACh

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16
Q

What are some basic signs and symptoms of anticholinergic crisis?

A
  • mad as a hatter (delusional)
  • dry as a bone (skin, mucous membranes)
  • red as a beet (flushing)
  • hot as a hare (fever/hyperthermia)
  • blind as a bat (mydriasis/dilation)
    picture Alice with anticholinergic crisis)
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17
Q

Overdose of what agents can lead to anticholinergic crisis?

A
  • atropine
  • scopalamine
  • antihistamines
  • tricyclic antidepressants
  • antispasmodics
  • jimson weed
  • meclizine
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18
Q

What can be used to treat anticholinergic crisis?

A

physostigmine
- increases amount of ACh

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19
Q

Physostigmine is a _______ (tertiary/quaternary) amine and ________ (can/cannot) cross the BBB

A
  • tertiary amine
  • CAN cross the BBB
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20
Q

Neostigmine is a quaternary or tertiary ammonium? Can it penetrate the BBB?

A
  • quaternary ammonium
  • CANNOT penetrate the BBB
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21
Q

How does neostigmine work?

A

inhibits hydrolysis of ACh by AChE by blocking AChE at all cholinergic synapses
- causes PNS effects

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22
Q

Neostigmine is usually given with ______________ to decrease muscarinic side effects

A

glycopyrrolate (anticholinergic)

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23
Q

Neostigmine Dosing

A

0.04-0.07 mg/kg
Ceiling dose: 70 mcg/kg

24
Q

Neostigmine onset and duration

A

Onset: 3-5 min
Duration: 30-60 min

25
Q

Which NMB reversal agent has a ceiling effect? What is this ceiling effect?

A
  • neostigmine
  • 70 mcg/kg
  • will worsen muscle weakness
26
Q

What is the ceiling effect dose of neostigmine?

A

70 mcg/kg

27
Q

When is neostigmine used?

A
  • deep blocks
  • moderate blocks (slow acting)
  • when spontaneous recovery is evident in the TOF!!!
28
Q

T/F: There are no recommendations on when to give neostigmine

A

false
- shouldn’t be given until spontaneous recovery is evident on the TOF

29
Q

What happens if we give surpass the ceiling effect dose of neostigmine?

A

may worsen the block and increase weakness; potentially increases the incidence of residual block

30
Q

How much neostigmine to how much glycopyrrolate?

A

1 mg neostigmine to 0.2 mg glycopyrrolate

31
Q

Is edrophonium a quaternary or tertiary amine? Does it cross the BBB?

A
  • quaternary amine
  • CANNOT cross the BBB
32
Q

How does edrophonium work?

A

inhibits the destruction of ACh by AChE by blocking AChE, thus increasing amounts of ACh

33
Q

What agent is edrophonium typically administered with? Why?

A
  • atropine
  • PROFOUND decrease in HR (down to the 30s) VERY quickly
34
Q

What is the mix of edrophonium and atropine called?

A

Enlon-Plus

35
Q

Edrophonium Dosing

A

0.5 - 1 mg/kg

36
Q

How much atropine is mixed per 1 mg of edrophonium?

A

0.014 mg of atropine per 1 mg of edrophonium

37
Q

Enlon-plus Dosing

A

0.05 - 0.1 mg/kg SLOWLY over 1 min

38
Q

Is Enlon-Plus sufficient enough to decrease risk of bradycardia?

A

No - typically still need to add more atropine

39
Q

Cholinergic syndrome is characterized as an overstimulation of _______ and ________ receptors

A
  • nicotinic
  • muscarinic
40
Q

What causes cholinergic syndrome?

A
  • too much anticholinesterase
  • organophosphate poisoning (found in pesticides/fertilizers)
  • nerve gas agents
41
Q

How is cholinergic crisis treated?

A
  • atropine (immediate tx)
  • benzos (versed/valium)
  • pralidoxime/obidoxime (affects acetylcholinesterase)
42
Q

What are two types of oximes used to treat cholinergic syndrome?

A
  • pralidoxime (2-PAM)
  • obidoxime (prevents aging and regenerates AChE)
43
Q

When should oximes be given?

A
  • to treat cholinergic crisis
  • prior to aging of the phosphate bond to the AChE molecule (rate of aging is unique to the organophosphate compound [sarin/VX in min; pesticides/fertilizers in min to days])
44
Q

Is physostigmine a quaternary or tertiary amine? Can it cross the BBB?

A
  • tertiary amine
  • it CAN cross the BBB; the only anticholinesterase that can cross BBB
45
Q

What is physostigmine used for?

A
  • NOT as a NMB reversal agent
  • to treat anticholinergic toxicity
46
Q

What s/s might we see that warrants physostigmine administration?

A
  • s/s of anticholinergic toxicity
  • flushing, dry skin/mucous membranes, mydriasis (dilation), loss of accommodation, AMS, fever, urinary retention, restless, shivers, agitation, disoriented
47
Q

Physostigmine Dosing

A

1-2 mg

48
Q

Overdose of what drugs can lead to anticholinergic toxicity?

A
  • atropine
  • scopolamine
  • tricyclic antidepressants
  • antihistamines
  • antipsychotics
49
Q

When is sugammadex used?

A

reversal of rocuronium or vecuronium (roc > vec)

50
Q

What is the generic name for Sugammadex?

A

bridion

51
Q

How does sugammadex/bridion work?

A
  • it is a selectrive relaxant binding agent
  • ENCAPSULATES roc or vec, prevents its action, and allows it to be excreted in urine
52
Q

Sugammadex Dosing

A
  • 2 mg/kg: TOF of 2
  • 4 mg/kg: no TOF twitches, or 1-2 post tetanic counts
  • 16 mg/kg: ONLY ROC; to reverse RSI dose of roc (we will see side effects at this dose)
53
Q

What are the side effects of sugammadex?

A
  • anaphylaxis
  • hypersensitivity
  • bradycardia
  • coagulopathy probs/bleeding (increased PTT, PT, and INR)
  • N/V
  • hypotension
  • headache
54
Q

What drugs does sugammadex interact with?

A
  • toremifene (breast cancer drug)
  • HORMONAL CONTRACEPTIVES (must educate patient they shouldn’t have sex for 7days)
55
Q

What is a huge warning that comes with sugammadex that anesthesia providers NEED to educate their patients about?

A

sugammadex will cause birth control to not work for 7 days. provider liable if patient gets pregnant