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Non-Opioids & Centrally/Peripherally Acting Analgesics Flashcards

1
Q

What mitigates the development of tolerance and opioid induced reward system?

A

Inhibiting microglial activation

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2
Q

Transition from acute to chronic pain involves:

A

Release of inflammatory mediators

Activation of microglia (1st/main form of active immune defense in CNS)

Changes in protein expression in the dorsal horn

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3
Q

Chronic release of microglia d/t chronic opioid use is responsible for:

A

Release of proinflammatory cytokines

Release of chemokines

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4
Q

Where do descending noradrenergic pathways originate?

A

Nuclei A5 and A7 in the pons and midbrain

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5
Q

What role do alpha 2 agonists play on neuraxial analgesia

A

Inhibitory role on sympathetic preganglionic neuron activity

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6
Q

where does clonidine inhibit nociceptive impulse of post-junctional alpha-2?

A

Dorsal horn of spinal cord

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7
Q

How does spinal clonidine effect LA

A

Causes a prolongation of sensory and motor block

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8
Q

Epidural dose of clonidine

A

75-150 mcg

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9
Q

Intrathecal dose of clonidine

A

15 - 40 mcg

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10
Q

Dose of clonidine for caudal block

A

1 mcg/kg

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11
Q

________ in concentration of 1-2mcg/ml may have beneficial effects in women with preeclampsia by stablizing BP

A

Clonidine

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12
Q

What is the black box warning for clonidine

A

Not recommended for obstetrical, postpartum, or perioperative pain management d/t risk of hemodynamic instability (especially hypotension & bradycardia) from epidural clonidine

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13
Q

How does clonidine affect hyperalgesia?

A

Prevents increased risk of pts w/ severe post op pain and central sensitization from developing persistent, long-term, chronic pain after surgery

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14
Q

Which has a higher affinity & more selectivity for alpha-2 receptors (Dexmedetomidine/Clonidine)?

A

Dexmedetomidine

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15
Q

_____ of intrathecal Dex is equipotent with _____ of clonidine

A

3 mcg; 30 mcg

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16
Q

Intrathecal Dex at ____ causes sig longer sensory & motor blockade than ______

A

5 mcg; Fentanyl 125 mcg

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17
Q

The addition of ______ Dex epidurally prolongs duration of analgesia & decreases requirement of rescue analgesics in patients having:

A

2mcg/kg
Lower limb orthopedic sx
Abdominal sx
C section (may lower HR and BP)

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18
Q

How does epidural Dex affect thoracic sx?

A

Decreases anesthetic requirements
Prevents awareness during anesthesia
Improves intro op O2 & post op analgesia

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19
Q

When giving Neostigmine, which neuraxial is nausea & vomiting less frequent?

A

Epidural

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20
Q

Doses of Neostigmine greater than ____ mcg have been associated with sedation

A

100

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21
Q

Which excitatory neurotransmitters are released from prolonged Ketamine stimulation of NMDA receptors?

A

Glutamate
Aspartate
Neurokinin

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22
Q

The primary analgesic effect mediated by Ketamine antagonizing NMDA receptors is located on secondary afferent neurons where?

A

Dorsal horn of the spinal cord

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23
Q

Why is there little clinical use of intrathecal ketamine?

A

Neurotoxicity

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24
Q

How does tramadol provide analgesia?

A

Combining mu-opioid and monoaminergic activity through the inhibition of neuronal uptake of serotonin & NorEpi

25
How does droperidol work on nausea
Acts as a dopaminergic antagonist directly at the brainstem chemoreceptor trigger zone (CTZ), the floor of the 4th ventricle
26
Baclofen is an agonist of which receptor?
GABA-B
27
How does baclofen work postsynaptically?
Activating the G protein linked GABA-B receptors in lamina II & III that result in increased K conductance & membrane hyperpolarization
28
How does baclofen work presynaptically?
Inhibits Ca conductance and the release of glutamate & substance P
29
Baclofen has ___ lipid solubility and ___ molecular weight that make it appropriate for spinal action when delivered by epidural
Low; low
30
Intrathecal dose of Baclofen through programmable intrathecal pump
25-200 mcg/day
31
Common S/E of baclofen:
Sedation, drowsiness, headache, nausea, weakness | Serious: rhabdomyolysis, multiple organ failure
32
What type of drug is Ketorolac?
COX inhibitor
33
NSAIDS can be classified according to numerous characteristics such as?
COX selectivity and chemical & pharmacologic properties
34
Are all NSAIDS completely COX-2 selective?
None are completely COX-2 sensitive
35
What is the only COX-2 inhibitor available for clinical use?
Celecoxib
36
What is the most COX-1 selective clinically used NSAID?
Ketorolac
37
What is the plasma half-life of NSAIDS?
0.25 to >70 hrs
38
NSAIDS are _____ protein bound
> 90%
39
COX-1 controls: (renal)
Hemodynamics and glomerular filtration rate
40
COX-2 controls: (renal)
Salt and water balance
41
NSAID hypersensitive rxns occur w/ what conditions?
Nasal polyps & asthma
42
What is the most efficacious way to used Tylenol for superior analgesia?
With an NSAID
43
The oldest medicinal compound in the world
Acetylsalicylic acid (aspirin)
44
MOA of aspirin
Irreversible inhibition of COX enzymes
45
Why does ASA have long lasting effects despite rapid metabolism?
COX enzymes are inhibited until new protein is produced
46
Salicylate levels for mild toxicity
300-600 mg/L
47
Salicylate levels for moderate toxicity
600-800 mg/L
48
Salicylate levels for severe toxicity
> 800 mg/L
49
Steroids with most powerful anti inflammatory characteristics
Glucocorticoids
50
The primary corticosteroid
Hydrocortisone
51
Adrenal cortical steroid hormones with greater effect on water & electrolyte balance
Mineralocorticoid
52
Cortisone
Anti inflammatory potency: 0.8 Dose: 25 mg Elim h/t: 0.5 hrs Duration: 8-36 hrs
53
Prednisolone
Anti inflammatory potency: 4 Dose: 5mg Elim h/t: 2-4 hrs Duration: 12-36 hrs
54
Prednisone
Anti inflammatory potency: 4 Dose: 5 mg Elim h/t: 2-4 hrs Duration: 12-36 hrs
55
Methylprednisolone
Anti inflammatory potency: 5 Dose: 4 mg Elim h/t: 2-4 hrs Duration: 12-36 hrs
56
Dexamethasone
Anti inflammatory potency: 25 Dose: 0.75 mg Elim h/t: 3.5-5 hrs Duration: 36-54 hrs
57
The overall effect of alpha-2 agonists is a _________ resulting in:
Sympatholysis; analgesia, hypotension, bradycardia, sedation
58
How does Neostigmine lead to bronchospasm?
By stimulating muscarinic receptors in bronchial smooth muscles

Pharm (15 decks)

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