Pharm approach to pain Flashcards

1
Q

what are analgesics?

A

drugs that relieve pain without causing loss of consciousness

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2
Q

what is secondary hyperalgesia?

A

pain caused by glutamate stimulation of spinal NMDA receptors

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3
Q

what are the characteristics of COX1?

A

expressed in all tissue
responds to physiological stimuli
responds to pathological stimuli (inflammation)

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4
Q

what is the COX1 pain pathway?

A
  1. inflammation stimulates AA release
  2. COX1 converts AA to PGE2
  3. PGE2 causes symptoms
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5
Q

what are the characteristics of COX2?

A

expressed in some tissue
physiological role in kidney and complements COX1
response to pathological stimuli (inflammation)

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6
Q

what is the COX2 pain pathway?

A
  1. inflammation induces COX2 expression
  2. COX2 also converts AA into PGE2
  3. COX2 derived PGE2 amplifies symptoms
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7
Q

what are the NSAIDs?

A
ASA
ibuprofen
celecoxib
diclofenac
inomethacin
ketorolac (Toradol)
naproxin (Aleve)
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8
Q

what is the MOA of most NSAIDs?

A

inhibits COX1 and COX2

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9
Q

which NSAID only inhibits COX2?

A

celecoxib

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10
Q

what are the adverse reactions of ASA?

A

GI bleeding
hemostatic defects
toxicity leading to respiratory failure

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11
Q

what is the toxic dose of ASA?

A

400-500 mcg/mL

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12
Q

what is the dose of ASA for antiplatelet or analgesia use?

A

100 mcg/mL

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13
Q

what is the dose of ASA for anti-inflammatory use?

A

150-300 mcg/mL

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14
Q

what is the dose of ASA for the treatment of rheumatic fever?

A

250-400 mcg/mL

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15
Q

what is the progression of ASA toxicity?

A
  1. salicylates uncouple ox phos in CNS
  2. resp center sees decreased ATP as hypoxemia
  3. hyperventilation causes respiratory alkalosis
  4. organic acids accumulate from Krebs cycle dysfunction
  5. metabolic acidosis becomes life-threatening
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16
Q

what are the adverse reactions of ibuprofen?

A

fetal renal dysfunction in pregnancy
increase risk of MI and stroke
increase risk of GI bleed

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17
Q

what are the adverse reactions of celecoxib?

A

fetal renal dysfunction in pregnancy
increase risk of MI and stroke
increase risk of GI bleed

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18
Q

what are the 4 major actions of ASA?

A

anti-inflammatory
mild to moderate pain relief
fever reduction
prevention of MI or stroke (anti-platelet)

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19
Q

what are the differences between ASA and other NSAIDs?

A

other NSAIDs:
reversible
increase the risk of MI and stroke

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20
Q

how is celecoxib different from ASA and other NSAIDs?

A

less likely to cause gastric ulceration
no risk of bleeding
increases MI and stroke risk

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21
Q

what are the contraindications of using NSAIDs?

A
CKD
gastric/duodenal ulcer
heart failure
uncontrolled HTN
allergy
anticoagulant use
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22
Q

what are the possible MOAs of acetaminophen?

A

TRPV1 activator
central PG synthase inhibitor
cannabinoid receptor activator

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23
Q

what is the major adverse reaction of acetaminophen?

A

hepatotoxicity due to overdose

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24
Q

what are the effects of acetaminophen?

A

suppresses pain and fever

NOT anti-inflammatory

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25
Q

how do you treat acetaminophen toxicity?

A

acetylcysteine

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26
Q

who should not take acetaminophen?

A

people with liver disease

people who take warfarin (increased risk of bleeding)

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27
Q

what is the MOA of opioids?

A

act on central and peripheral µ, ∂ and k receptors

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28
Q

what is the blackbox warning of morphine?

A

respiratory depression with/without combining with other drugs

29
Q

what are the adverse reactions of opioids?

A

constipation
CNS depression
hypotension

30
Q

when are patients at risk for physical opioid dependence?

A

when used at high doses for > 20 days

31
Q

what are indications for opioid use?

A
post-op pain
obstetric analgesia
MI
head injury
chronic non-cancer pain
32
Q

what are the first-line agents for neuropathic pain?

A

calcium channel alpha 2 delta ligands
SNRIs
TCA

33
Q

what is the MOA of amitriptyline?

A

TCA

inhibition of NE and 5-HT reuptake

34
Q

what are the adverse reactions of amitriptyline?

A
dry mouth
constipation
tachycardia
nausea
vomiting
sedation
mental clouding
35
Q

what is the MOA of duloxetine?

A

SNRI
inhibitor of neuronal 5-HT and NE reuptake
weak inhibitor of DA reuptake

36
Q

what are the adverse reactions of SNRIs?

A
nausea
dizziness
diaphoresis
sexual dysfunction
insomnia/agitation
hypertension
37
Q

what is the MOA of calcium channel alpha2-delta ligands?

A

modulates calcium influx at nerve terminals

GABA analog but does NOT bind to GABA receptors

38
Q

what are the indications for using pregabalin?

A

diabetic neuropathy
postherpetic neuralgia
partial seizures
fibromyalgia

39
Q

what are the calcium channel alpha2-delta ligands?

A

pregabalin

gabapentin

40
Q

what are the indications for using gabapentin?

A
broad-spectrum anti-seizure activity
post-herpetic neuralgia
diabetic neuropathy
migraine prophylaxis
fibromyalgia
restless leg syndrome
41
Q

what is the MOA of tramadol?

A

partial agonist of µ-opioid receptors in CNS

inhibits reuptake of 5-HT and NE

42
Q

what are the adverse reactions of tramadol?

A
sedation
dizziness
headache
dry mouth
constipation
43
Q

what are the indications for using tramadol?

A

moderate pain

  • stronger than ASA or acetaminophen
  • weaker than morphine
44
Q

what are the serious side effects of tramadol?

A

seizures in epileptics
hypertensive crisis if combine with MAO
serotonin syndrome if combined with SSRI, TCA, MAO

45
Q

what is the MOA of tapentadol?

A

moderate to strong µ-opioid receptor agonist

blocks reuptake of NE

46
Q

what is an indication for giving tapentadol?

A

patients who are not effectively treated with other non-opioids and opioids

47
Q

what is the MOA of ketamine?

A

noncompetitive NMDA receptor antagonist

48
Q

what are the indications for using ketamine?

A
agitation
sub-anesthetic doses for analgesia
depressive episode
procedural sedation
refractory status epilepticus
49
Q

what are adverse reactions of ketamine?

A

psych reactions:
agitation
confusion
hallucinations

50
Q

what is the MOA of dexmedetomidine?

A

alpha2-adrenergic agonist for analgesia and sedation

51
Q

what are the indications for using dexmedetomidine?

A

short-term sedation in intubated patients
sedation prior to procedures
administered IV for pain

52
Q

what are the adverse reactions of dexmedetomidine?

A
hypotension
bradycardia
nausea
dry mouth
transient HTN
agitation
constipation
respiratory depression
53
Q

what is the MOA of clonidine?

A

alpha2-adrenergic agonist used for HTN and relief of severe pain
blocks transmission of pain signals

54
Q

what are the indications for using clonidine?

A

severe cancer pain in patients not treated effectively with opioid alone

55
Q

what are the adverse reactions of clonidine?

A

hypotension
confusion
dry mouth

56
Q

what is the MOA of ziconotide?

A

selective N-type voltage-sensitive calcium channel antagonist on nociceptive afferent neurons

prevents transmission of pain signals

57
Q

what are the indications for using ziconotide?

A

chronic severe pain in those whom intrathecal administration is warranted and when refractory to other treatments

58
Q

what are the adverse reactions of ziconotide?

A

cognitive impairment and psych symptoms

59
Q

what drugs are contraindicated in pregnancy?

A

dexmedetomidine
clonidine
ziconotide

60
Q

what are the topical anti-pain agents?

A
capsaicin
camphor
menthol
topical NSAIDs
topical Na channel blockers
61
Q

what drugs can treat migraines?

A

sumatriptan
lasmiditan
ubrogepant
dihydroergotamine

62
Q

what is the MOA of sumatriptan?

A

selective 5HT1B and 5-HT1D agonist

activates receptors on the intracranial blood vessels and sensory nerves of the trigeminal system

63
Q

what are the adverse reactions to sumatriptan?

A
Torsades
MI
stroke
CNS depression
blindness or partial vision loss
serotonin syndrome
peripheral ischemia
64
Q

what is the MOA of lasmiditan?

A

high-affinity highly selective 5-HT1F receptor agonist

65
Q

what are the adverse reactions to lasmiditan?

A

CNS depression
serotonin syndrome
can potential toxic effects of other drugs

66
Q

what is the MOA of ubrogepant?

A

calcitonin gene-related peptide receptor antagonist

67
Q

what are the adverse reactions to ubrogepant?

A

nausea
somnolence
dry mouth

68
Q

what is the MOA of dihydroergotamine?

A

ergot alkaloid

binds to serotonin, adrenergic and dopamine receptors

69
Q

what are the adverse reactions to dihydroergotamine?

A

do not use with potent CYP3A4 inhibitors –> vasospasm

cardiac fibrosis