Fitzy: Osteoarthritis and Joint Inflammation Pharmacology Flashcards

1
Q

What analgesics are used for osteoarthritis?

A
  • acetaminophen (non narcotic)

- Tamadol and codeine are narcotics

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2
Q

What anti inflammatory agents are used for osteoarthritis?

A
  • NSADs
    • gastric anti-secretory agent
  • triamcinolone (corticosteroid
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3
Q

in the first step in pain relief in osteoarthritis, what do we use?

A
  • acetaminophen

- … WITHOUT inflammation

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4
Q

is acetaminophen an anti inflammatory agent?

A

NO!

-it’s an analgesic and anti pyretic agent, but not an anti inlammatory agent

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5
Q

fun fact, what was the important thing about acetylsalicylic acid (aspirin)?

A
  • it has irreversible inhibition of COX

- acetylates it

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6
Q

what actually is acetaminophen?

A

-acetyl-p-aminophenol

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7
Q

complications and risks from acetaminophen overdose?

A

-serious, potentially lethal liver toxicity

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8
Q

how will a person with liver toxicity present?

A
  • ER

- emesis, jaundice, and altered mental status

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9
Q

What does acetaminophen get converted to that hurts us?

A
  • NAPQI by CYP450, then that gets a glutathione group added onto it
  • depletes glutathione content
  • once we run out of GSH, then we can’t detoxify NAPQI and it reacts irreversibly with cell proteins
  • Catastrophic cell damage
  • CYP 450 does this
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10
Q

What histologic finding do we find from NAPQI toxicity?

A
  • centrolobular necrosis

- the central part is where there is a lot of CYP 450… makes senseWhat i

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11
Q

what is the antidote for acetaminophen overdose?

A
  • N-Acetylcysteine.. NAC
  • it replenishes the GSH pool
  • it also reacts directly with NAPQI to deactivate it… spares proteins and salvages cells
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12
Q

if acetaminophen doesn’t work for osteoarthritis, what do we go to next?

A

-NSAIDs!

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13
Q

What was the bolded drug on the NSAID list that is the only US NSAID in injectable formulation?

A

-Ketorolac

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14
Q

What should make us wear of treating this with an NSAId?

A
  • GI risk
  • CV risk
  • Htn, atherosclerosis, smoking
  • Hypersensitivity
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15
Q

How many NSAIDs should be used at once?

A

-one and only one

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16
Q

What is the exception to the one at a time rule?

A
  • use of cardioprotective dose of aspirin with other NSAIDs
  • Caution: low dose aspirin may increase the risk of upper GI bleeding in patients taking NSAIDs…. antithrombotic effects
17
Q

If someone is having adverse effects to an NSAID, what do we switch on them?

A

-the CLASS of NSAIDs that they are taking

18
Q

Is celecoxib safer for the GI tract?

A
  • yes!

- remember they are only annoying for the renal arteries because they selectively inhibit COX2

19
Q

What are potential complications attributed to Coxibs?

A
  • Cardiovascular safety
  • they spare COX1 so the platelets can still make TxA2
  • endothelium can make PGI2… and that was on the other end of the hemostasis scale from TxA2..
  • if we inhibit COX-2, TxA2»> PGI2
  • even so, Celecoxib is the safest thing on the market
20
Q

If the symptoms persist, worsen, and NSAIDs fail, what do we do?

A
  • Intra-articular anti-inflammatory steroids
  • Triamcinolone acetonide
  • Triamcinolone hexonide
  • limited systemic exposure; fewer side effects compared to systemic corticosteroids
21
Q

What is the difference betwee NSAIDs and Triamcinolone?

A
  • NSAIDs will inhibit COX-2 directly
  • Triamcinolone will repress the OCS2 mRNA protein induction.. less COX2, less PGs formed… it just goes a step further back
22
Q

What were the narcotic analgesics again?

A
  • Tramadol
  • Codeine
  • use alone or combined with a cetaminophen and it’s only short term
23
Q

What kind of receptor do the narcotics bind?

A
  • Mu receptors
  • they are Mu receptor agonists
  • Morhpine, Codeine, Tramadol
24
Q

What are the side effects of narcotics?

A
  • increase smooth muscle tonen and inhibit the coordinated peristalsis required for propulsion, which contributes to nausea and vomiting as well as constipation
  • constipation can be an intolerable side effect in some patients who need to take opioid (tramadol or codeine taken chronically)
25
Q

Tramadol, what is it?

A
  • Moderate Mu agonist
  • N-desmethyl is the active metabolite
  • analgesia-moderate pain
  • inhibits catecholamine reuptake
26
Q

What patients do we have to be cautious with when using tramadol?

A

-patients on tricyclic, or SRI anti-depressants

27
Q

What nasty side effect is associated with Tramadol?

A

-seizures