NMBA Reversal Agents

Question 1

Neostigmine (Bioxiverz)

MOA

Answer 1

nAChR
Competitive Antagonist

Inhibits destruction of ACh antagonizing acetylcholinesterase at NMJ

Co-administered with Glycopyrrolate

Question 2

Neostigmine (Bioxiverz)

Dosing

Answer 2

IV: 40-70 µg/kg (0.04-0.07 mg/kg)
50 µg/kg is typical (0.05 mg/kg)

Max: 60-80 µg/kg

Question 3

Neostigmine (Bioxiverz)

Onset
Duration

Answer 3

Onset
5-10 min

Duration
60 min

Question 4

Neostigmine (Bioxiverz)

Metabolism
&
Elimination

Answer 4

Metabolism/Elimination
Hepatic: 30-50%
Renal: 50%

Question 5

Neostigmine (Bioxiverz)

Side Effects
&
Considerations

Answer 5

CNS
Miosis

Cardiovascular
↓HR, dysrhythmias, asystole, ↓SVR

Respiratory
Bronchoconstriction,
↑ airway resistance, ↑ salivation

GI
Hyperperistalsis,
↑ gastric fluid secretion, PONV

Question 6

Glycopyrrolate (Robinol)

MOA

Answer 6

Receptor
mAChR

Competitive inhibitor of Ach at postganglionic sites

Co-administered with Neostigmine

Question 7

Glycopyrrolate (Robinol)

Dosing

Answer 7

IV: 7-15 µg/kg over 2 min

Commonly 200 µg (200mcg/ml) of glycopyrrolate per 1 mg (1mg/ml) of neostigmine = 1 ml of glycopyrrolate per 1 ml neostigmine

Max: 1 mg

Question 8

Glycopyrrolate (Robinol)

Onset
Duration

Answer 8

Onset
1 min

Duration
60 min

Question 9

Glycopyrrolate (Robinol)

Metabolism
&
Elimination

Answer 9

Metabolism/Elimination
Hepatic: Hydrolysis

Question 10

Glycopyrrolate (Robinol)

Side Effects
&
Consideration

Answer 10

CNS
Mydriasis

Cardiovascular
↑HR, dysrhythmias, asystole, ↑ SVR

Respiratory
Bronchodilation, ↓ airway resistance,
↓ salivation

GI
Dry mouth, ↓proximal gastric emptying
↓antral contractility & notably slows gastric emptying, & constipation

GU
Urinary retention

Does NOT cross the blood-brain barrier

I.g., Glycopyrrolate 0.2 mg/ml of Neostigmine

Question 11

Sugammadex (Bridion)

MOA

Answer 11

Intermolecular forces; Van Der Walls

Forms complex w/ rocuronium & vecuronium reducing amount available to nACH receptors at NMJ

Question 12

Sugammadex (Bridion)

Dosing

Answer 12

Moderate Block (TOF 2/4)
IV: 2 mg/kg

Deep Block (TOF 0/4)
IV: 4 mg/kg

Extreme Block (TOF 0/4)
IV: 8-16 mg/kg

Question 13

Sugammadex (Bridion)

Onset
Duration

Answer 13

Onset
1-4 min

Duration
1.5-3 hrs

Question 14

Sugammadex (Bridion)

Metabolism
&
Elimination

Answer 14

Elimination
Renal: 70% in 6 hr &
90% in 24 hr

Highly Water Soluble

Question 15

Sugammadex (Bridion)

Side Effects
&
Considerations

Answer 15

N/V, dry mouth, ↓HR, dizziness, pruritus, urticaria, anaphylaxis & ↓Renal excretion;

C/I ESRD & HD

Potential for no therapeutic effect

Binds to the free drug in PLASMA

Drug interactions:
Birth control inactivation; alternate BC for 7 days

Toremifene displaces NMBA from sugammadex