NMBD Reversal Agents (Ex IV) Flashcards
How long, generally, until NMJ blockade is fully reversed with neostigmine?
20-30 min
Do AChE inhibitors work with deep neuromuscular blockade?
No
Reversal of NMJ blockade is dependent on these 5 factors:
- Depth of block
- AChE-i choice
- Dose administered
- Rate of plasma clearance of NMBD
- Anesthetic agent and depth
Which paralytic has to be reconstituted with 10mL of H₂O ?
Vecuronium
What is the dosage of neostigmine and its max?
40 - 70 mcg/kg
max: 5mg
What is the onset and duration of neostigmine?
Onset: 5 - 10 min
Duration: 60 min
What is the dosage of edrophonium?
0.5 - 1 mg/kg
What is the onset and duration of edrophonium?
Onset: 1-2 min
Duration: 5-15 min
What percentage of neostigmine is renally excreted?
50%
What percentage of both pyridostigmine and edrophonium are renally excreted?
75%
How are NMB reversal agents cleared if the patient has no innate renal function?
30 - 50% cleared hepatically
What is the major side effect of NMBD reversal agents?
↑PSNS activity (from increased nACh and mACh activity)
SLUDGE-M symptoms
What drugs would be coupled with NMBD reversal agents to prevent adverse side effects from these drugs?
Anti-cholinergic / Anti-muscarinics
- Atropine
- Glycopyrrolate
If you’re concerned about someone’s cardiac status due to existing disease, which Anticholinergic drug would you use?
Glycopyrrolate
What NMB reversal drug is glycopyrrolate used with?
- Neostigmine
What NMB reversal is atropine used with?
Edrophonium
What is the dose of Atropine?
7 - 10 mcg/kg
What common side effects are seen after atropine administration?
- Mydriasis (pupil dilation)
- initial Tachycardia
How long does glycopyrrolate need to be administered over?
2 - 5 min
What is the dose and max for glycopyrrolate?
7 - 15 mcg/kg
1mg maximum
What reversal drug is specific to mivacurium?
Purified human plasma cholinesterase
What reversal drug is specific to gantacurium?
Cystiene
What reversal drug is very specific to rocuronium? What other NMBDs is this drug effective in reversing?
Sugammadex (Bridion)
Aminosteroids
What type of drug is sugammadex?
Selective relaxant-binding agent
What should be known about sugammadex’s organic structure and physical properties? (3)
- γ-cyclodextrin
- Dextrose units from starch
- Highly H₂O-soluble (large renal excretion)
What is the MOA of Sugammadex?
Encapsulates aminosteroids (mostly rocuronium) via:
- Van der Waals forces
- H-bonds
- Hydrophobic interactions
What drugs does sugammadex work with?
Aminosteroids
Roc > Vec > Pancuronium
What is the E ½ time of sugammadex?
2 hours
How is sugammadex eliminated? What is an important consideration regarding excretions?
Urine:
- 70% gone in 6 hours
- 90% gone in 24 hours
Renal impairment: Contraindicated with dialysis pts
Differentiate a moderate block vs a deep block.
- Moderate: 2/4 twitches on TOF
- Deep: No twitches to TOF (minimal posttetanic response)
What is the Sugammadex dose for a moderate block?
2 mg/kg
What is the Sugammadex dose for a deep block?
4 mg/kg
What is the sugammadex dose for an extreme block?
8 - 16 mg/kg
What are the side effects of Sugammadex? (4)
- marked Bradycardia
- dose-related N/V
- dose-related Pruritis
- dose-related Urticaria
What drugs/conditions are relative contraindications to sugammadex?
- Contraceptives
- Toremifene (displaces NMB from sugammadex)
- Coagulopathy/bleeding
- ESRD (excreted renally)
What is recurarization?
Resumption of NMJ blockade after period of reversal
What s/s would indicate recurarization? (5)
Say you just brought the patient to PACU.
- ↓ SpO₂
- ↓ respiratory effort
- Floppy/uncoordinated
- Unresponsive
- suffocating feeling
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 (40-70mcg/kg)
- Longer duration of action (60min)
What is the only used long-acting NMBD? intermediate-acting NMBDs? short-acting NMBD?
Long
Pancuronium (AS)
Intermediate
Rocuronium (AS)
Vecuronium (AS)
Atracurium (BNZ)
Cisatracurium (BNZ)
Short
Mivacurium (BNZ)
