Reversal Agents - Quiz 8 Flashcards
What happens to the Heart with SNS Stimulation?
↑HR
↑Conduction Velocity
↑Automaticity
↑Contractility
What happens to the Heart with PNS Stimulation?
↓HR
↓Conduction Velocity
↓Contractility (Slight)
What happens to Bronchial Smooth Muscles with SNS Stimulation and PNS Stimulation?
SNS: Relaxation
PNS: Contraction
What happens to Sphincters w/ SNS & PNS Stimulation?
SNS: Contraction
PNS: Relaxation
What happens to the Uterus & Ureters w/ SNS & PNS Stimulation?
SNS: Contraction
PNS: Relaxation
How does SNS Stimulation affect the Liver?
Glycogenolysis & Gluconeogenesis
How does PNS Stimulation affect the Liver?
Glycogen Synthesis
What happens to the Pancreas w/ SNS & PNS Stimulation?
SNS: ↓B-Cell Secretion
PNS: ↑B-Cell Secretion
How are the Salivary & Sweat Glands affected by SNS & PNS Stimulation?
↑Secretions
(More Salivary Secretions w/ PNS)
How are all Arterioles affected by SNS & PNS Stimulation?
SNS: Constriction
PNS: Relaxation
(Beta SNS Stimulation of Coronary Arterioles = Relaxation)
Which Anticholinesterase Drug is classified as a Tertiary Amine?
Physostigmine
Which Anticholinesterase Drugs are classified as Quaternary Ammoniums?
Edrophonium
Neostigmine
Pyridostigmine
How does SNS & PNS Stimulation affect the Eyes?
SNS: Mydriasis
PNS: Miosis
How does Neostigmine, Pyridostigmine, & Physostigmine increase ACh Availability?
They get hydrolyzed by acetylcholinesterase, which then carbamylates and blocks the enzyme’s ability to hydrolyze ACh
Which Reversal Agent forms magnetic/electrostatic bond that reversibly causes Acetylcholinesterase Inhibition?
Edrophonium
What happens if you give Reversal Agents without there being any NMBs?
Overflow of ACh = fasciculations/muscle twitches
Can look like a Phase I NMB Block
What is the Onset of Action for Edrophonium?
1-2 minutes
How does Neostigmine compare to Edrophonium?
More Profound & Potent than Edrophonium
Slower Onset: 7-11 Min
What is the Duration of Action for all of the Reversal Agents?
1-2 Hrs
What determines the Potency of Reversal Agents?
- The NMB being reversed
- Speed of Spont. Recovery
- Depth of Block when Reversal given
- End Point
Once anticholinergic enzymes are completely blocked by the reversal agent, how does re-dosing effect patient’s recovery?
No benefits = keep patient sedated & intubated until spont recovery
What factors can slow down NMB Reversal?
Hypothermia
ABX
Acidosis
Hypokalemia
What are the Muscuranic Side effects of having Increased ACh from Reversal Agents?
Bradycardia
Salivation
Bronchoconstriction
Miosis
Hyperperistalsis
PONV
Which Reversal Agents have Marked & Prolonged Inhibition of Plasma Cholinesterase?
Neostigmine & Pyridostigmine
What can be mixed w/ Reversal Agents to minimize Muscuranic Side effects?
Anticholinergic Drugs w/ faster onset than Anticholinesterase
Which class of Anticholinesterase Drugs can cross the Blood Brain Barrier?
Tertiary Amines - Physostigmine
What can Physostigmine be used for as a Reversal other than for NMBs?
Central Anticholinergic Syndrome
Restlessness/Confusion
Opioids
Benzos
Ketamine
Antidepressants
What are some uses for Antiacetylcholinesterases outside of the OR?
Myasthenia Gravis
Glaucoma
Post-Op Pain/Shivering
Alzheimer’s - Aricept, Razadyne, Exelon
Chronic Fatigue
What are treatments for Reversal Agent Overdose?
Atropine
Pralidoxime - Acetylcholinesterase Reactivator
Supportive Measures
What are the naturally occuring anticholingergic that are tertiary amines?
Atropine & Scopolamine
What is the quarternary ammonium anticholinergic?
Glycopyrrolate
What is the Mechanism of Action for Anticholinergics?
Competitively Binds @ Muscuranic Receptor and Blocks ACh from binding there
Where are the M1 Muscarinic Receptors?
CNS & Stomach
Where are the M2 Muscarinic Receptors?
Lungs & Heart
Where are the M3 Muscarinic Receptors?
CNS
Airway
Smooth Muscle
Glandular Tissue
Where are the M4 Muscarinic Receptors?
CNS & Heart
Where are the M5 Muscarinic Receptors?
CNS
What are the effects at the Odd # Muscarinic Receptors (M1, M3, M5)?
Stimulatory
↑Calcium
↑MAP
What are the effects at the Even # Muscarinic Receptors (M2, M4)?
Inhibitory
↓MAP
↓Calcium
↓Adenylyl Cyclase
B/t Atropine & Glycopyrrolate, which has a faster onset and longer duration?
Atropine is Faster - 1 Min
Glycopyrrolate - 2-3 Min
Both Lasts 30-60 min
What are some Pre-Op uses for Anticholinergics?
Sedation
Saliva Reduction
Prevent Vagal Reflexes
Bronchodilation
Prevent Nausea
Which Anticholinergic would be most potent for Sedation?
Scopolamine
100x more potent than Atropine
Amnesic
Why is Neostigmine + Glycopyrrolate preferred over Neostigmime + Atropine?
CNS effects of Atropine along w/ Neostigmine cause delayed arousal for first 30 min after cessation of anesthesia
What are the effects of using Anticholinergics on the Elderly?
Restlessness
Delayed Awakening
Increased IOP
How does Scopolamine & Glycopyrrolate compare to Atropine when used to reduce Salivary Effects?
Scopolamine 3X more potent
Glycopyrrolate 2x more potent & longer duration
Which drug is commonly used to prevent Vagal Reflexes and to treat IntraOp Bradycardia?
Atropine
Which drug is commonly used to Prevent Motion Sickness?
Transdermal Scopolamine
One Pupil might be bigger
What are symptoms of Anticholinergic Overdose?
Restlessness to Unconsciousness
Dried Out
Blurred Vision
Tachycardia
Increased Temp
Orthostatic Hypotension
Can Be Fatal
What should be used to treat Anticholinergic Overdose?
Physostigmine 15-60 mcg/kg
What were the results of the RECITE study?
Rocuronium + Neostigmine = more than half had residual block
What chemical structure does Suggamadex have?
Used for Vecuronium & Rocuronium
Hydrophobic Center & Hydrophillic Exterior
Able to Reduce Deep Blocks
What are the Adverse Effects of Suggamadex?
Bradycardia
Bleeding
N/V
Hypotension
Headache
Not Recommended for Renal Patients
How is Suggamdex Eliminated?
Kidneys
t1/2 = 2hrs
How does Suggamadex compare to Neostigmine for Rocuronium & Vecuronium Reversal?
Suggamadex is 6x faster & 17x faster for a deep block
Safer
Less Residual Block
How does Suggamadex compare to Neostigmine + Glycopyrrolate for reversal after abdominal surgery?
Neostigmine + Glygopyrrolate: 43% residual Block
Suggamadex: 0% residual block
If someone on Birth Control receives Sugammadex, how long should they use a backup method for Birth Control?
For 7 Days after receiving Sugammadex