*NMBD Reversal Agents (Exam IV) Flashcards
What are the 3 classifications of NMBD Reversal Agents?
- AcetylcholineEsterase (AchE) Inhibitors
- Cholinergic Agents
- COMPETITIVE ANTAGONISTS
S9
What is the MOA if AChE
- Rapid hydrolysis (catalyze) of Ach
Inhibition of Esterase enzyme = more Acetylcholine available → Ach binds to alpha subunits
S9
Where is AChE available at?
- Preganglionic (SNS & PNS)
- NMJ: neuromuscular junction
S9
Do AChE inhibitors work with deep neuromuscular blockade?
No
S10
What do we do when patient has deep NM blocked according to Dr. Castillo?
WAIT
until we get a TOF and Tetany
What is the max dosage of neostigmine?
40 - 70 mcg/kg
0.04 - 0.07 mg/kg
S10
What is the max dosage of edrophonium?
1 mg/kg
S10
Reversal of NMJ blockade is dependent on these 5 factors:
- Depth of block
- AChE Inhibitor choice (neo vs edro)
- Dose
- Rate of plasma clearance
- Anesthetic agent choice and depth
S11
What is the ED50 and ED90 of Pancuronium?
ED50 = 0.036
ED90 = 0.067
What is the ED50 and ED90 of Rocuronium?
ED50 = 0.147
ED90 = 0.305
What is the ED50 and ED90 of Vecuronium?
ED50 = 0.027
ED90 = 0.043
What is the ED50 and ED90 of Atracurium?
ED50 = 0.12
ED90 = 0.21
What is the ED50 and ED90 of Cisatracurium?
ED50 = 0.026
ED90 = 0.040
What is the ED50 and ED90 of Mivacurium?
ED50 = 0.039
ED90 = 0.067
What is the onset and duration of neostigmine?
Onset: 5 - 10 mins
Duration: 60 mins
S14
What is the dosage of edrophonium?
0.5 to 1 mg/kg
S14
What is the onset and duration of edrophonium?
Onset: 1-2 mins
Duration: 5-15 mins
S14
What percentage of neostigmine is renally excreted?
50%
S16
What percentage of both pyridostigmine and edrophonium are renally excreted?
75%
S16
How does Chronic Renal Failure affect NMBD reversal agents?
decreases plasma clearance
→ prolonged action
S16
How are NMB reversal agents cleared if the patient has no innate renal function?
30 - 50% cleared hepatically
S16
What is the major side effect of NMBD reversal agents?
Increased Nicotinic/Muscarinic Activity
S17
What CV side effects of NMBD Reversal Agents?
- Bradycardia
- dysrhythmias
- asystole
- ↓SVR
S17
What pulmonary side effects of NMBD Reversal Agents?
- Bronchoconstriction
- increased airway resistance
- increased salivation
S17
What GI side effects of NMBD Reversal Agents?
- Hyperperistalsis
- enhanced gastric fluid secretion
- PONV
S17
What opthalmic side effects of NMBD Reversal Agents?
Miosis
S17
What drugs would be coupled with NMBD reversal agents to prevent adverse side effects from these drugs?
Anti-cholinergic / Anti-muscarinics
- Atropine
- Glycopyrrolate
S18
If you’re concerned about someone’s cardiac status due to existing disease, which Anticholinergic drug would you use?
Glycopyrrolate
S18
What NMBD Reversal(s) is glycopyrrolate used with?
- Neostigmine
- Pyridostigmine
S18
What NMBD Reversal(s) is atropine used with?
Edrophonium
S18
What is the dose of Atropine?
7 - 10 mcg/kg
S18
What common side effects are seen right after atropine administration?
- Mydriasis
- Tachycardia
S18
What is the maximum dose of glycopyrrolate?
1mg max dose
S18
How long does glycopyrrolate need to be administered over?
2 - 5 min
administer SLOWLY
S18
What is the mechanism when there is persistent NM blockade?
- Acetylcholinesterase is maximally inhibited
- No further anticholinesterase is effective
S20
What is the intervention for persistent NM blockade?
Sedation and postop ventilation
S20
What do you need to do before giving paralytics during Induction according to Dr. Castillo?
CHECK YOUR BASELINE TOF!!
(make sure to test the TOF and it has adequate batteries also)
What factors influencing NMBD Reversal?
- Intensity of block
- Which NMBD did you use (renal vs liver)?
- Continued volatile anesthetic?
- Which reversal drug are you using?
- Patient conditions
-Metabolic acidosis
-Respiratory acidosis
-Hypothermia
S21
What to do when titrating down Glycopyrrolate according to Dr. Castillo?
Be careful with titrating down and DO NOT go below 50%
NMBD Reversal Agents
What reversal drug is specific to mivacurium?
Purified human plasma cholinesterase
S22
What reversal drug is specific to Gantacurium?
Cystiene
S22
What reversal drug is very specific to rocuronium?
Sugammadex
S22
What type of drug is sugammadex?
Selective relaxant-binding agent
S22
What should be known about sugammadex’s organic structure and physical properties?
- γ-cyclodextrin
- Dextrose units from starch
- Very H₂O-soluble
S24
What is the MOA of Sugammadex?
Encapsulates rocuronium via:
- Intermolecular (Van der Waals forces)
- Thermodynamic (H-bonds)
- Hydrophobic interactions
S25
What drugs does sugammadex work with?
Roc > Vec > Pancuronium
S25
Where does Sugammadex binds to?
The “free drug” in plasma
S25
What is the E ½ time of sugammadex?
2 hours
S26
How is sugammedex eliminated?
Urine:
- 70% gone in 6 hours
- 90% gone in 24 hours
Renal impairment: cleared with dialysis
S26
What is the Sugammadex dose for a moderate block?
2 mg/kg
S27
What is the Sugammadex dose for a deep block?
4 mg/kg
S27
Differentiate a moderate block vs a deep block.
- Moderate: 2/4 twitches on TOF
- Deep: No twitches to TOF
S27
What is the sugammadex dose for an extreme (overdose) block?
8 - 16 mg/kg
S28
What are the side effects of Sugammadex?
- dose-related Pruritis
- dose-related Urticaria
- dose-related N/V
- Anaphylaxis
- Bradycardia
S31
What is the NMBD and dose to administer after waiting 5 minutes after Reversal?
1.2 mg/kg ROCuronium
S32
What is the NMBD and dose to administer after waiting 4 hours after Reversal?
0.6 mg/kg ROCuronium
or
0.1 mg/kg VECuronium
S32
What drugs/conditions are relative contraindications to sugammadex?
- Contraceptives
- Toremifene (displaces NMBD from sugammadex)
- Coagulopathy
- ESRD (excreted renally)
- Recurarization (lower than recommended dose)
S33
What is
Recurarization?
aka REPARALYZED the patient
Resumption of NMJ blockade after period of reversal
S36
What s/s would indicate recurarization?
Say you just brought the patient to PACU.
- ↓ SpO₂
- Unresponsive
- Floppy/uncoordinated
- ineffective abdominal and intercostal activity
S36
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
S38
What specific s/s of Recurarization?
- sometimes can verbalize: suffocating feeling
- unable to sustain head lift or hand grasp
- worst case: pharyngeal collapse and respiratory obstruction
S40
What are treatments goals of Recurarization?
Treat urgently and aggressively
* Re-sedate the patient
* Give additional reversal agents in divided doses (Neostigmine 0.05 mg/kg IV = longer duration of action).
S40