Pharm Exam IV: Kaitlyn's NMBD Reversal Agents Flashcards

1
Q

What are the three NMBD Reversal Agents?

A

Edrophonium
Neostigmine
Sugammadex

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2
Q

What are the two Anti-Cholinergic Agents given in conjunction with NMBD reversal agents to prevent unwanted side effects?

A

Atropine Sulfate
Glycopyrrolate

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3
Q

What family does Vecuronium, Rocuronium and Pancuronium belong in?

A

Aminosteroids

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4
Q

What family does Cisatracurium, Mivacurium and Atracurium belong in?

A

Benzylisoquinolones

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5
Q

What are the three MOA/Classifications (aka’s) of NMBD reversal agents?

A

AcetylcholinEsterase (AchE) Inhibitors
Cholinergic Agents
Competetive Antagonists

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6
Q

What NMBD reversals do to reverse paralytics?

A

-They increase Ach at the NMJ and Preganglionic fibers.
-They do this by blocking AchE, competing for the muscarinic or nicotinic cholinergic receptors at the NMJ alpha subunits.

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7
Q

Do AChE inhibitors work with deep neuromuscular blockade?

A

No - there is a Ceiling effect - you have to wait till it wears off to reverse

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8
Q

Reversal of NMJ blockade is dependent on these 5 factors:

A

-Depth of block
-Drug choice (neo vs edro)
-Dose
-Rate of plasma clearance
-Anesthetic agent and depth

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9
Q

What is the max dosage of neostigmine?

A

40 - 70 mcg/kg

0.04 - 0.07 mg/kg

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10
Q

What is the onset and duration of neostigmine?

A

Onset: 5 - 10 min
Duration: 60 min

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11
Q

What is the dosage of edrophonium?

A

0.5-1 mg/kg

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12
Q

What is the onset and duration of Edrophonium (Enlon)?

A

Onset: 1-2 min
Duration: 5-15 min

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13
Q

What is the dose of Sugammadex?

A

2-16mg/kg

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14
Q

What is the onset and duration of Sugammadex?

A

Onset: 1-4 min
Duration: 1.5-3hrs

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15
Q

Differentiate a moderate block vs a deep block.

A

Moderate: 2/4 twitches on TOF
Deep: No twitches to TOF, but will have a 1-2 twitch w/ post tetanic stimulation

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16
Q

What is the Sugammadex dose for a moderate block?

A

2 mg/kg

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17
Q

What is the Sugammadex dose for a deep block?

A

4 mg/kg

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18
Q

What is the sugammadex dose for an extreme (overdose) block?

A

8 - 16 mg/kg
Recurarization (reparalyzation): not observed at appropriate doses.

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19
Q

What percentage of neostigmine is renally excreted?

A

50%

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20
Q

What percentage of both pyridostigmine and edrophonium are renally excreted?

A

75%

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21
Q

How are NMBD reversal agents cleared if the patient has no innate renal function?

A

30 - 50% cleared hepatically

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22
Q

What happens to renal excretion of NMBD reversal agents if someone has chronic renal failure?

A

Decrease in plasma clearance - prolongs drug action

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23
Q

What are the side effects of increase Nicotinic/Muscarinic Activity in the CV system?

A

Bradycardia, dysrhythmias, asystole, decreased SVR

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24
Q

What are the side effects of increase Nicotinic/Muscarinic Activity in the Pulmonary system?

A

Bronchoconstriction, increased airway resistance, increased salivation

25
What are the side effects of increase Nicotinic/Muscarinic Activity in the GI system?
Hyper-peristalsis, enhanced gastric fluid secretion, PONV
26
What are the side effects of increase Nicotinic/Muscarinic Activity in the Eyes?
Miosis - constriction of the pupil
27
How do you prevent side effects from NMBD reversal agents?
Give Anti-cholinergic/ Anti-muscarinic agents
28
If you’re concerned about someone’s cardiac status due to existing disease, which Anticholinergic drug would you use?
Glycopyrrolate
29
How long does glycopyrrolate need to be administered over?
2 - 5 min
30
What AChE inhibitor is glycopyrrolate used with?
Neostigmine Pyridostigmine
31
What NMBD(s) is atropine used with?
Edrophonium
32
What is the dose of Atropine?
7 - 10 mcg/kg
33
What common side effects are seen right after atropine administration?
Mydriasis - dilation of the pupil Initial Tachycardia
34
What is the dose of glycopyrrolate? What is the max dose?
7 - 15 mcg/kg 1mg max dose
35
What causes persistent NM blockade?
When AchE is maximally inhibited No further anticholinesterase is effective
36
How to treat Persistent NM blockade?
Sedation and postop ventilation
37
When do you test twitches?
Check you baseline twitches before you give paralytic.
38
What Factors Influence NMBD Reversal?
-Intensity of block -Which NMBD did you use? -Continued volatile anesthetic -Which reversal drug are you using -Patient conditions -Metabolic acidosis -Respiratory acidosis -Hypothermia
39
What reversal drug is specific to mivacurium?
Purified human plasma cholinesterase - don't really use anymore for risk of infections
40
What reversal drug is specific to Gantacurium?
Cystiene - expensive
41
What reversal drug is very specific to rocuronium?
Sugammadex
42
What other drugs can Suggamadex can reverse? In which class?
Aminosteroid - vecuronium - metabolized by renal and hepatic system
43
What type of drug is sugammadex?
Selective relaxant-binding agent -γ-cyclodextrin -dextrose units from starch - diabetic issues? -Highly water soluble - contraindicated in renal failure or decreased renal function
44
What is the MOA of Sugammadex?
-intermolecular (van der Walls) forces -thermodynamic (hydrogen) bonds -hydrophobic interactions* very tight reversal by encapsulation and excreted in urine
45
What's another name for Sugammadex?
Bridion
46
What drugs does sugammadex work with?
Roc > Vec > Pancuronium
47
How is sugammedex eliminated?
Urine 70% gone in 6 hours 90% gone in 24 hours
48
When is Sugammadex ABSOLUTELY Contraindicated?
Renal impairment with dialysis
49
What is the E ½ time of sugammadex?
2 hours - if it binds intravascularly, it renders rocuronium non-functional
50
What are the side effects of Sugammadex?
Works on the chemoreceptors trigger zone - aka vomiting center: Dose related: -N/V -Pruritis - Urticaria -marked bradycardia - get glyco and atropine -Anaphylaxis -some people it doesn't work
51
If 1.2 mg/kg of rocuronium needs to be re-administered after reversal with sugammedex. What is the minimum waiting time?
5 min
52
If 0.6 mg/kg of rocuronium needs to be re-administered after reversal with sugammedex. What is the minimum waiting time?
4 hours
53
If 0.1 mg/kg of vecuronium needs to be re-administered after reversal with sugammedex. What is the minimum waiting time?
4 hours
54
What else could you do if you can't wait to paralyze the patient?
Give a different type of NMBD like a benzylisoquinolone - Atracurium, Cisatracurium at normal doses
55
What drugs/conditions are relative contraindications to sugammadex?
Oral Contraceptives -Binds with Progesterone (7 days) Toremifene (non-steroidal anti-estrogen) - cancer medication -Displaces NMBD from Sugammadex Coagulopathy/Bleeding -Heparin/LMWH; Elevated PTT, PT, INR Recurarization -Lower than recommended doses.
56
What is recurarization?
Resumption of NMJ blockade after period of reversal
57
What s/s would indicated recurarization? Say you just brought the patient to PACU.
-↓ SpO₂ -↓ respiratory effort -Floppy/uncoordinated - can't lift head or grasp hand. -Pharyngeal collapse and respiratory obstruction -Sometimes can verbalize a suffocating feeling to unresponsive
58
What drug and dose would be a good choice for a recurarizing patient in the PACU? Why might this be a good choice?
-Neostigmine 0.05 mg/kg IV -Longer duration of action He also loves physotigmine
59
How do team/group acknowledge mistakes?
Team/group factors.