Reversal Agents - Quiz 8 Flashcards by Donny Le

What happens to the Heart with SNS Stimulation?

↑HR

↑Conduction Velocity

↑Automaticity

↑Contractility

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What happens to the Heart with PNS Stimulation?

↓HR

↓Conduction Velocity

↓Contractility (Slight)

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What happens to Bronchial Smooth Muscles with SNS Stimulation and PNS Stimulation?

SNS: Relaxation

PNS: Contraction

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What happens to Sphincters w/ SNS & PNS Stimulation?

SNS: Contraction

PNS: Relaxation

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What happens to the Uterus & Ureters w/ SNS & PNS Stimulation?

SNS: Contraction

PNS: Relaxation

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How does SNS Stimulation affect the Liver?

Glycogenolysis & Gluconeogenesis

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How does PNS Stimulation affect the Liver?

Glycogen Synthesis

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What happens to the Pancreas w/ SNS & PNS Stimulation?

SNS: ↓B-Cell Secretion

PNS: ↑B-Cell Secretion

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How are the Salivary & Sweat Glands affected by SNS & PNS Stimulation?

↑Secretions

(More Salivary Secretions w/ PNS)

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How are all Arterioles affected by SNS & PNS Stimulation?

SNS: Constriction

PNS: Relaxation

(Beta SNS Stimulation of Coronary Arterioles = Relaxation)

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Which Anticholinesterase Drug is classified as a Tertiary Amine?

Physostigmine

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Which Anticholinesterase Drugs are classified as Quaternary Ammoniums?

Edrophonium

Neostigmine

Pyridostigmine

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How does SNS & PNS Stimulation affect the Eyes?

SNS: Mydriasis

PNS: Miosis

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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

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Which Reversal Agent forms magnetic/electrostatic bond that reversibly causes Acetylcholinesterase Inhibition?

Edrophonium

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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

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What is the Onset of Action for Edrophonium?

1-2 minutes

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How does Neostigmine compare to Edrophonium?

More Profound & Potent than Edrophonium

Slower Onset: 7-11 Min

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What is the Duration of Action for all of the Reversal Agents?

1-2 Hrs

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What determines the Potency of Reversal Agents?

The NMB being reversed
Speed of Spont. Recovery
Depth of Block when Reversal given
End Point

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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

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What factors can slow down NMB Reversal?

Hypothermia

ABX

Acidosis

Hypokalemia

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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