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
Q

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

A

Hyper-peristalsis, enhanced gastric fluid secretion, PONV

26
Q

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

A

Miosis - constriction of the pupil

27
Q

How do you prevent side effects from NMBD reversal agents?

A

Give Anti-cholinergic/ Anti-muscarinic agents

28
Q

If you’re concerned about someone’s cardiac status due to existing disease, which Anticholinergic drug would you use?

A

Glycopyrrolate

29
Q

How long does glycopyrrolate need to be administered over?

A

2 - 5 min

30
Q

What AChE inhibitor is glycopyrrolate used with?

A

Neostigmine
Pyridostigmine

31
Q

What NMBD(s) is atropine used with?

A

Edrophonium

32
Q

What is the dose of Atropine?

A

7 - 10 mcg/kg

33
Q

What common side effects are seen right after atropine administration?

A

Mydriasis - dilation of the pupil
Initial Tachycardia

34
Q

What is the dose of glycopyrrolate?

What is the max dose?

A

7 - 15 mcg/kg

1mg max dose

35
Q

What causes persistent NM blockade?

A

When AchE is maximally inhibited
No further anticholinesterase is effective

36
Q

How to treat Persistent NM blockade?

A

Sedation and postop ventilation

37
Q

When do you test twitches?

A

Check you baseline twitches before you give paralytic.

38
Q

What Factors Influence NMBD Reversal?

A

-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
Q

What reversal drug is specific to mivacurium?

A

Purified human plasma cholinesterase - don’t really use anymore for risk of infections

40
Q

What reversal drug is specific to Gantacurium?

A

Cystiene - expensive

41
Q

What reversal drug is very specific to rocuronium?

A

Sugammadex

42
Q

What other drugs can Suggamadex can reverse? In which class?

A

Aminosteroid - vecuronium - metabolized by renal and hepatic system

43
Q

What type of drug is sugammadex?

A

Selective relaxant-binding agent
-γ-cyclodextrin
-dextrose units from starch - diabetic issues?
-Highly water soluble - contraindicated in renal failure or decreased renal function

44
Q

What is the MOA of Sugammadex?

A

-intermolecular (van der Walls) forces

-thermodynamic (hydrogen) bonds

-hydrophobic interactions* very tight reversal by encapsulation and excreted in urine

45
Q

What’s another name for Sugammadex?

A

Bridion

46
Q

What drugs does sugammadex work with?

A

Roc > Vec > Pancuronium

47
Q

How is sugammedex eliminated?

A

Urine
70% gone in 6 hours

90% gone in 24 hours

48
Q

When is Sugammadex ABSOLUTELY Contraindicated?

A

Renal impairment with dialysis

49
Q

What is the E ½ time of sugammadex?

A

2 hours
- if it binds intravascularly, it renders rocuronium non-functional

50
Q

What are the side effects of Sugammadex?

A

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
Q

If 1.2 mg/kg of rocuronium needs to be re-administered after reversal with sugammedex. What is the minimum waiting time?

A

5 min

52
Q

If 0.6 mg/kg of rocuronium needs to be re-administered after reversal with sugammedex. What is the minimum waiting time?

A

4 hours

53
Q

If 0.1 mg/kg of vecuronium needs to be re-administered after reversal with sugammedex. What is the minimum waiting time?

A

4 hours

54
Q

What else could you do if you can’t wait to paralyze the patient?

A

Give a different type of NMBD like a benzylisoquinolone - Atracurium, Cisatracurium at normal doses

55
Q

What drugs/conditions are relative contraindications to sugammadex?

A

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
Q

What is recurarization?

A

Resumption of NMJ blockade after period of reversal

57
Q

What s/s would indicated recurarization?

Say you just brought the patient to PACU.

A

-↓ 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
Q

What drug and dose would be a good choice for a recurarizing patient in the PACU?
Why might this be a good choice?

A

-Neostigmine 0.05 mg/kg IV
-Longer duration of action

He also loves physotigmine

59
Q

How do team/group acknowledge mistakes?

A

Team/group factors.