Nonopioids Analgesics (Exam 2) Flashcards
Nonopioid Analgesic Classes
NSAIDs
Acetylsalicylic acid (Aspirin)
Acetaminophen (Tylenol)
Cannabinoids
NSAIDs
MoA
inhibit an enzyme Cycloxygenase responsible for prostaglandin & thromboxane synthesis
Antipyretic, analgesic, and anti-inflammatory.
Acetylsalicylic acid (Aspirin)
MoA
similar to NSAIDS but irreversible inhibitor of COX
binds permanently & destroy (longer HLoE & long term issues)
Acetaminophen (Tylenol)
similar to NSAIDS
but not anti-inflammatory
? inhibit COX but not in periphery. Probably CNS.
(Periphery: H2O2 inhibits TYLENOL)
T/F
Aspirin is a reversible COX inhibitor.
False
NSAIDS = reversible
Acetylsalicylic acid (Aspirin) = irreversible
T/F
Aspirin’s effects last longer than ibuprofen.
True
Aspirin’s COX inhibitory effects are irreversible
Cannabinoids
receptors
specific receptors
(All Gi/0 type)
CB1: brain & SC
CB2: mainly immune
Cannabinoids
limitations
Research weak
CBD (cannabidiol) oil questionable. Some degree of pain relief.
Analgesia d/t sedation
Analgesic dose also causes too much sedation/fxnl limitation
Centrally Acting Nonopioid Analgesics
a2-Adrenergic Agonists:
Clonidine
Dexmedetomidine
Acetylcholinesterase Inhibitors (AChEI’s)
BZDs:
Midazolam
Anesthetics:
Ketamine
Conopeptides:
Ziconotide
GABA Agonists:
Baclofen
Others (weaker proof of benefit):
Ketorolac (NSAID)
Gabapentin
Magnesium Sulfate
Calcitonin
Adenosine
Octreotide
Tramadol
Droperidol
a2-Adrenergic Agonists
MoA
↓NE release in multiple pathways (CNS pain pathways)
stimulate pre-synaptic a2 receptors
↓
block vesicle fusion & NE release from pre-synaptic terminal.
a2-Adrenergic Agonists
Major effect on pain is on…
sympathetic preganglionic neuronal activity
Clonidine
partial a2 receptor agonist
Neuraxial use: cancer, non-cA, post-op pain.
use w/ LAs: potentiate effects
synergistically w/ opioids
Black-box warning for neuraxial administration in obstetrics due to maternal hemodynamic instability.
clonidine
T/F
Norepi can inhibits its own release
True
Norepi can bind to a2 receptor and prevents vesicle and NT release
(Precedex can do this bc its an a2 agonist)
Which is more potent?
Clonidine
Dexmedetomidine
Dexmedetomidine
Dexmedetomidine
a2 receptor agonist
Fewer systemic & HD SEs vs clonidine
a/w demyelination following epidural dosing
Acetylcholinesterase Inhibitors (AChEI’s)
Neostigmine
Blocks ACh metab in synapse
by blocking post-syn sites where ACh would normally bind to and be metabolized
↓
more free ACh in synapse
Intrathecal: released ACh continues to stimulate muscarinic receptors = minor pain relief
adjunct w/ intrathecal LAs & opioids
high SE profile may outweigh small benefit
AChase is located on the (pre/post) synaptic membrane
post
ACh is broken down into…
choline
acetic acid
(Dont confuse w/ Suxx metab)
adrenergic vs. cholinergic
cause of inhibition/limited action
adrenergic: uptake carrier (reuptake of Norepi)
cholinergic: enzyme breaks down substance @ post-syn membrane (AChase)
Form in which ACh is taken back up by neuron for reuse
choline
Neostigmine can provide pain relief. Why is its use for this purpose not common?
high SE profile may outweigh small benefit
T/F
BARBs can be used for pain relief.
False
enhance pain response
Ketamine
Analgesic (anesthetic & subanesthetic doses)
Neuraxial +/- LAs: effective post-op pain relief
synergism w/ opioids
