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Pharm > Non-Opioids & Centrally/Peripherally Acting Analgesics > Flashcards

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
Q

How does droperidol work on nausea

A

Acts as a dopaminergic antagonist directly at the brainstem chemoreceptor trigger zone (CTZ), the floor of the 4th ventricle

26
Q

Baclofen is an agonist of which receptor?

A

GABA-B

27
Q

How does baclofen work postsynaptically?

A

Activating the G protein linked GABA-B receptors in lamina II & III that result in increased K conductance & membrane hyperpolarization

28
Q

How does baclofen work presynaptically?

A

Inhibits Ca conductance and the release of glutamate & substance P

29
Q

Baclofen has ___ lipid solubility and ___ molecular weight that make it appropriate for spinal action when delivered by epidural

A

Low; low

30
Q

Intrathecal dose of Baclofen through programmable intrathecal pump

A

25-200 mcg/day

31
Q

Common S/E of baclofen:

A

Sedation, drowsiness, headache, nausea, weakness

Serious: rhabdomyolysis, multiple organ failure

32
Q

What type of drug is Ketorolac?

A

COX inhibitor

33
Q

NSAIDS can be classified according to numerous characteristics such as?

A

COX selectivity and chemical & pharmacologic properties

34
Q

Are all NSAIDS completely COX-2 selective?

A

None are completely COX-2 sensitive

35
Q

What is the only COX-2 inhibitor available for clinical use?

A

Celecoxib

36
Q

What is the most COX-1 selective clinically used NSAID?

A

Ketorolac

37
Q

What is the plasma half-life of NSAIDS?

A

0.25 to >70 hrs

38
Q

NSAIDS are _____ protein bound

A

> 90%

39
Q

COX-1 controls: (renal)

A

Hemodynamics and glomerular filtration rate

40
Q

COX-2 controls: (renal)

A

Salt and water balance

41
Q

NSAID hypersensitive rxns occur w/ what conditions?

A

Nasal polyps & asthma

42
Q

What is the most efficacious way to used Tylenol for superior analgesia?

A

With an NSAID

43
Q

The oldest medicinal compound in the world

A

Acetylsalicylic acid (aspirin)

44
Q

MOA of aspirin

A

Irreversible inhibition of COX enzymes

45
Q

Why does ASA have long lasting effects despite rapid metabolism?

A

COX enzymes are inhibited until new protein is produced

46
Q

Salicylate levels for mild toxicity

A

300-600 mg/L

47
Q

Salicylate levels for moderate toxicity

A

600-800 mg/L

48
Q

Salicylate levels for severe toxicity

A

> 800 mg/L

49
Q

Steroids with most powerful anti inflammatory characteristics

A

Glucocorticoids

50
Q

The primary corticosteroid

A

Hydrocortisone

51
Q

Adrenal cortical steroid hormones with greater effect on water & electrolyte balance

A

Mineralocorticoid

52
Q

Cortisone

A

Anti inflammatory potency: 0.8
Dose: 25 mg
Elim h/t: 0.5 hrs
Duration: 8-36 hrs

53
Q

Prednisolone

A

Anti inflammatory potency: 4
Dose: 5mg
Elim h/t: 2-4 hrs
Duration: 12-36 hrs

54
Q

Prednisone

A

Anti inflammatory potency: 4
Dose: 5 mg
Elim h/t: 2-4 hrs
Duration: 12-36 hrs

55
Q

Methylprednisolone

A

Anti inflammatory potency: 5
Dose: 4 mg
Elim h/t: 2-4 hrs
Duration: 12-36 hrs

56
Q

Dexamethasone

A

Anti inflammatory potency: 25
Dose: 0.75 mg
Elim h/t: 3.5-5 hrs
Duration: 36-54 hrs

57
Q

The overall effect of alpha-2 agonists is a _________ resulting in:

A

Sympatholysis; analgesia, hypotension, bradycardia, sedation

58
Q

How does Neostigmine lead to bronchospasm?

A

By stimulating muscarinic receptors in bronchial smooth muscles

Pharm (15 decks)

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