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Daddy Pharm > Nonopioids Analgesics (Exam 2) > Flashcards

Nonopioids Analgesics (Exam 2) Flashcards

1
Q

Nonopioid Analgesic Classes

A

NSAIDs
Acetylsalicylic acid (Aspirin)
Acetaminophen (Tylenol)
Cannabinoids

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2
Q

NSAIDs
MoA

A

inhibit an enzyme Cycloxygenase responsible for prostaglandin & thromboxane synthesis

Antipyretic, analgesic, and anti-inflammatory.

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3
Q

Acetylsalicylic acid (Aspirin)
MoA

A

similar to NSAIDS but irreversible inhibitor of COX

binds permanently & destroy (longer HLoE & long term issues)

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4
Q

Acetaminophen (Tylenol)

A

similar to NSAIDS
but not anti-inflammatory

? inhibit COX but not in periphery. Probably CNS.
(Periphery: H2O2 inhibits TYLENOL)

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5
Q

T/F
Aspirin is a reversible COX inhibitor.

A

False
NSAIDS = reversible
Acetylsalicylic acid (Aspirin) = irreversible

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6
Q

T/F
Aspirin’s effects last longer than ibuprofen.

A

True
Aspirin’s COX inhibitory effects are irreversible

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7
Q

Cannabinoids
receptors

A

specific receptors
(All Gi/0 type)

CB1: brain & SC
CB2: mainly immune

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8
Q

Cannabinoids
limitations

A

Research weak
CBD (cannabidiol) oil questionable. Some degree of pain relief.

Analgesia d/t sedation
Analgesic dose also causes too much sedation/fxnl limitation

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9
Q

Centrally Acting Nonopioid Analgesics

A

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

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10
Q

a2-Adrenergic Agonists
MoA

A

↓NE release in multiple pathways (CNS pain pathways)

stimulate pre-synaptic a2 receptors
↓
block vesicle fusion & NE release from pre-synaptic terminal.

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11
Q

a2-Adrenergic Agonists
Major effect on pain is on…

A

sympathetic preganglionic neuronal activity

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12
Q

Clonidine

A

partial a2 receptor agonist

Neuraxial use: cancer, non-cA, post-op pain.

use w/ LAs: potentiate effects

synergistically w/ opioids

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13
Q

Black-box warning for neuraxial administration in obstetrics due to maternal hemodynamic instability.

A

clonidine

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14
Q

T/F
Norepi can inhibits its own release

A

True
Norepi can bind to a2 receptor and prevents vesicle and NT release

(Precedex can do this bc its an a2 agonist)

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15
Q

Which is more potent?
Clonidine
Dexmedetomidine

A

Dexmedetomidine

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16
Q

Dexmedetomidine

A

a2 receptor agonist

Fewer systemic & HD SEs vs clonidine

a/w demyelination following epidural dosing

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17
Q

Acetylcholinesterase Inhibitors (AChEI’s)
Neostigmine

A

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

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18
Q

AChase is located on the (pre/post) synaptic membrane

A

post

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19
Q

ACh is broken down into…

A

choline
acetic acid

(Dont confuse w/ Suxx metab)

20
Q

adrenergic vs. cholinergic
cause of inhibition/limited action

A

adrenergic: uptake carrier (reuptake of Norepi)

cholinergic: enzyme breaks down substance @ post-syn membrane (AChase)

21
Q

Form in which ACh is taken back up by neuron for reuse

A

choline

22
Q

Neostigmine can provide pain relief. Why is its use for this purpose not common?

A

high SE profile may outweigh small benefit

23
Q

T/F
BARBs can be used for pain relief.

A

False
enhance pain response

24
Q

Ketamine

A

Analgesic (anesthetic & subanesthetic doses)

Neuraxial +/- LAs: effective post-op pain relief

synergism w/ opioids

25
Q

Ketamine
noncompetitively inhibits NMDA of…

A

secondary afferent neurons in SC dorsal horn

26
Q

Ketamine
SEs

A

sedation
headache
possible psychotic rxn
transient burning back pain during admin

27
Q

Ketamine
benefits

A

lack of CV SE’s & respiratory depression

28
Q

Midazolam
MoA
Receptors & their location

A

GABAA: ↑ inhibition & block pain transmission

act in dorsal horn (high [ ] GABAAr; Lamina II)

opioid receptor activity: stimulates release of endogenous opioids

29
Q

Can we give Versed neuroaxially?

A

No proven neurotoxic effects

30
Q

location of high [ ] of GABA(A) receptors

A

dorsal horn; laminae II

31
Q

(Conopeptides)
Ziconotide (Prialt)
structure

A

25 AA polypeptide derived from conotoxin (from marine snail)

32
Q

Ziconotide (Prialt)

A

(Conopeptides)

selective antagonist of neuronal (N-type) voltage-gated Ca channels in presynaptic nerve terminals in the dorsal horn.

block nerve transmission by blocking NE release

sympatholytic

IV: ↓ MAP & SBP
intrathecal: minimal effect

33
Q

Only currently FDA approved nonopioid for IT use to treat neuropathic pain.

A

Ziconotide (Prialt)

34
Q

Ziconotide (Prialt)
SEs
limitations

A

> 90%
dizziness, confusion, ataxia, memory impairment, suicide ideations

High costs and SE’s limit use.
last resort

35
Q

GABA(B)

A

G protein complex system

36
Q

Sympatholytic

A

blocks SNS & norepi

37
Q

Baclofen (Lioresal)

A

GABA(B) agonist
via G-protein system
↓
activate K channels & hyperpolarize internal membrane

inhibitory effects like GABAA but diff moA

Acts in lamina II & III (DH) presynaptically to inhibit depolarization & decrease Ca entry
↓
decreases afferent pain transmission

38
Q

T/F
Baclofen (Lioresal) is a GABA(A) agonist.

A

False
GABA(B)

B for Baclofen

39
Q

GABA(B) conducts which ion?

A

K

40
Q

Baclofen
uses

A

Intrathecal: chronic pain syndrome from MS & complex regional pain syndrome

back pain (with root compression)

spasticity (ie: cerebral palsy)

Use with Bupivocaine: ↓ postop opioid use

41
Q

Baclofen
SEs

A

sedation
drowsiness
nausea
headache
weakness

Rare but serious:
rhabdomyolysis
multiple organ failure

42
Q

A/w rhabdomyolysis & multiple organ failure

A

Baclofen

43
Q

Gabapentin

A

precursor of GABA; weak pain relief

44
Q

Adenosine is considered “other”

A

has its own receptor type

45
Q

Magnesium Sulfate & Calcitonin
for pain relief

A

Controls Ca and thus ability to stimulate neurons

46
Q

Droperidol use

A

neuroleptic anesthesia

Daddy Pharm (13 decks)

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