NMBA Reversal Agents Flashcards
other name for neostigmine
Prostigmin
dose for prostigmin
0.04-0.08 mg/kg
*5 mg max (comes in 5 mg vial)
MOA of neostigmine
inhibit hydrolysis of ACh by AChE
T or F: the more neostigmine you give, the more it reverses
F - has a ceiling effect!
T or F: Prostignmin easily crosses BBB
F - it is a quarternary ammonium thus does not cross well (its charged)
what medication (and what dose) is usually given with neostigmine. Why is this given?
glycopyrollate
0.2 mg per mg of neostigmine
decrease muscarinic effects of neostigmine
is neostigmine a reversal for depolarizing or non-depolarizing NMBD
non-depolarizing
Neostigmine:
onset-
duration-
metabolism-
excretion-
onset- 15 min (depend on twitches)
duration- 1-2 hours
metabolism- hepatic
excretion: urinary
other name for edrophonium
enlon
dose of enlon
0.5-1 mg/kg
what is typically given with edrophonium
Atropine
0.014 mg/mg of enlon
dose for enlon plus
0.05 - 0.1 mg/kg slowly over 1 minute
MOA of endrophonium
inhibit hydrolysis of ACh by AChE
IF you have a profound block, is neostigmine or endrophonium the better reversal agent?
neostigmine d/t longer DOA
T or F: Enlon easily crosses BBB
F - quarternary amine
Edrophonium
onset -
DOA
onset -1-2 min
DOA - very short
other name for pyridostigmine
regonol
indications for Regonol
- reversal
- myasthenia gravis
- pretreatment for soman nerve gas exposure
typically used in gulf-war as a oral dose prophylactically and if exposed, would take again
pyridostigmine
Regonol
onset-
DOA-
O- 2-5 min
DOA- 2-3 horus
T or F: Regonol does not easily cross BBB
T - its a quatenary amine
other name for physostigmine
antilirium
the only anticholinesterase that crosses BBB
physostigmine
dose of physostigmine
IV - 1-2 mg
*may repeat Q1-2 hour
indications for antilirium
- treatment for central anticholinergic syndrome
- treat anticholinergic toxicity
- not generally used as a reversal agent
MOA of physostigmine
inhibits cholinesterase
CNS effects of physostigmine
- agitation
- restless
- disoriented
- shivers
Physostigmine
onset-
DOA-
o- 5 min
DOA- 1-2 hours
*metabolism is rapid and may require repeat dosing
other name for sugammadex
bridion
dosage of bridion
routine:
2 mg/kg TOF2
4 mg/kg no TOF but 1-2 PTC
emergent reversal of RSI:
16 mg/kg
indications for suggamadex
reversal of zemuron and vecuronium
MOA of suggamadex
selective relaxant binding agent that encapsulates roc, vec, or pancuronium preventing their effects/actions
side effects of Suggamadex
At high dose =
Bradycardia
Hypotxn,
Cardiac arrest,
Headache,
N/V,
Anaphylaxis and
Hypersensitivity
May hinder effects of birth control and some antibiotics up to 7 days (Hormonal contraceptives and Toremifene)
contraindications (use caution in) of suggamadex
renal impairment
wait 24 hours before re-adminstering Roc/Vec/Panc
what meds are bridion incompatible with
- verapamil
- zofran
- ranitidine
onset of action for Bridion
~ 3 min
Suggamadex is modified ______________
y- cyclodextrin
How does Sugammadex alter coagulation?
Increases risk of coagulopathy and bleeding –> increases aPTT and PT, especially in those patients who were being treated with heparin or LMW heparin for thromboprophylaxis
Which drug increases a patient’s risk for coagulopathy and bleeding by increasing aPTT, and PT (especially in patients being treated with heparin or LMW heparin for thromboprophylaxis)?
sugammadex
Which drug interacts with hormonal contraceptives?
sugammadex
Sugammadex metabolism:
NOT metabolized; excreted UNCHANGED by kidneys, so take caution in patients with renal failure
N/V, hypotension, and headache are common adverse reactions to which NMB reversal agent?
Sugammadex
How can we prevent Sugammadex-induced bradycardia?
Give 100 mg over 1 min, then give the next 100 mg, etc.
Sugammadex dose (with TOF of 2):
conc:
time until recovery:
2 mg/kg
(100 mg/cc)
2 mins until recovery
Sugammadex dose (with 1-2 PTC and no TOF twitches):
conc:
time until recovery:
4 mg/kg
(100 mg/cc)
3 mins until recovery
Sugammadex dose (just after administering RSI dose of Rocuronium):
conc:
time until recovery:
16 mg/kg
(100 mg/cc)
1.5 mins until recovery
Physostigmine dose to treat anticholinergic toxicity:
give 1-2 mg every 1-2 hrs, as needed
What drugs may cause anticholinergic toxicity?
- atropine
- scopolamine
- antihistamines
- antipsychotics
- cyclic antidepressants
Anticholinergic toxicity s/s:
flushing, dry skin and mucous membranes, mydriasis with loss of accommodation, altered mental status, fever and urinary retention
CNS: restlessness, shivers, agitation, disoriented
Cholinergic Syndrome crisis treatment:
Atropine, benzos (versed/valium), oximes (pralidoxime, obidoxime) –> oximes free AChAse from the anticholinesterase that is bound to it
Enlon-plus dose:
0.05-0.1 mg/kg IV
SLOWLY OVER 1 MIN
Edrophonium dose:
conc:
onset:
duration:
0.5-1 mg/kg IV
(10 mg/cc)
For every 1 mg of edrophonium, mix with 0.014 mg atropine (to prevent bradycardia)
onset: 1-2 mins
duration: short
Edrophonium is used for (light/moderate/deep) block reversal.
moderate
Edrophonium is a (tertiary amine/quaternary ammonium) and, therefore, (does/does not) cross the BBB.
quaternary ammonium; DOES NOT
___ is a mixture of Edrophonium and atropine together in the same vial.
Enlon-Plus
Edrophonium is administered with ___ in order to prevent ___ caused by the rapid ___ of Edrophonium.
Atropine
bradycardia
onset
Neostigmine dose:
conc:
onset:
duration:
0.05 mg/kg IV (max 5 mg)
(1 mg/cc)
for every 1 mg of Neostigmine, administer 0.2 mg Glycopyrrolate (0.2 mg/cc) to decrease muscarinic side effects (and GIVE GLYCO FIRST in case something happens between; we can handle tachycardia better than bradycardia)
onset: starting at 15 mins (twitch dependent)
duration: 1-2 hrs
Neostigmine is used for (light/moderate/deep) block reversal. How do we know when to use?
deep (use when 4 tactile TOF counts are present at adductor pollicis)
(more effective with moderate blocks)
What is our max dose of Neostigmine?
5 mg –> d/t ceiling effect
Neostigmine is a (tertiary amine/quaternary ammonium) compound and, therefore (does/does not) cross the BBB.
quaternary ammonium
does not
Neostigmine is used with ___ to decrease the ___ side effects of Neostigmine.
glycopyrrolate (anticholinergic)
muscarinic
Neostigmine blocks AChAse at ____________, causing (parasympathetic/sympathetic) effects.
ALL cholinergic synapses
parasympathetic
Physostigmine –> drug class:
acetylcholinesterase inhibitor (crosses BBB)
Edrophonium –> drug class:
acetylcholinesterase inhibitor
Neostigmine –> drug class:
acetylcholinesterase inhibitor
Sugammadex drug class:
selective relaxant binding agent
Which drugs are our acetylcholinesterase inhibitors?
Neostigmine
Edrophonium
Physostigmine (crosses BBB)
What side effects are caused by the administration of acetylcholinesterase inhibitors?
Think –> TOO MUCH ACh!!
SLUDGE (PNS activation)
Increased bronchial secretions/bronchospasm
Bradycardia caused by slowing conduction velocity of the cardiac impulse through the AV node
CNS excitement (physostigmine only)
Acetylcholinesterase inhibitors are used for what 3 purposes?
reversal of NMBs
myasthenia gravis (diagnosis and treatment)
treatment of central anticholinergic syndrome
___ is the enzyme responsible for the rapid hydrolysis of released acetylcholine.
Acetylcholinesterase
What are the two ways to reverse a patient from NMBs?
spontaneously
reversal drug
What 5 factors affect the reversal of NMBs?
- intensity of the block
- dose and choice of NMB
- drug interactions
- choice of reversal agent
- disease process (liver failure)
