Flashcards in antiflamm, antipyretic,analgesics Deck (74)
what is the physiologic process of inflammation?
Cyclooxygenase allows prostaglandin formation which modulates inflammation
what is the physiologic process of pain?
Prostaglandin E2 (PGE2) is thought to sensitize nerve endings to the action of bradykinin, histamine and other mediators release by the inflammatory process
what is the physiologic process of fever?
Anterior hypothalamic thermoregulatory center becomes elevated
Infection triggers WBC leading to cytokine production and subsequent PGE2 production
what are 3 of the most common "non-selective" (by FDA standards) cox inhibitors?
Ibuprofen (Motrin, Advil)*
Naproxen (Naprosyn, Aleve)*
what are the 2 nonacetylated salicylates?
Magnesium salicylate ( Doans Pills)
Salicylsalicylic Acid (Salsalate)
what are the 2 Cox-2 selective inhibitors?
where are the 3 major ADRs of NSAIDs?
what are 3 less common but dangerous ADRs of NSAIDs?
2 ADRs of Cox1 inhibition? which drugs do this?
GI mucosa... peptic ulcer and GI bleeding
NSAIDS + ASA
3 ADRs of Cox 1+2 inhibition? which drugs do this?
1. Na+ and H2O retention
3. hemodynamic acute kidney injury
what are 2 ADRs for when there is more Cox-2 inhibition than Cox-1 . which drugs do this?
MI and stroke
(ASA does the opposite, irreversibly inhibits Cox 1)
how does the inhibition of Cox1 cause peptic ulcers and GI bleeding?
inhibits PGE2 (prostoglandin) which usually serves for gastric protection (increased mucus secretion, increase HCO3, increase mucus flow)
how does the inhibition of Cox1 and Cox2 cause kidney issues?
inhibits PGE2 (prostoglandin) and PGI2 (prostacyclin) which together ...
-vasodilate afferent arteriole (increase GFR)
-increase Na+ and H2O secretion
how does the inhibition of Cox2 >Cox1 cause cardiovascular issues?
inhibits PGI2 (prostacyclin) and TXA2 (thromboxane) which together...
-vascular: Cox 2 and PGI2: vasodilates and inhibits platelet aggregation
-platelets: Cox1 and TXA2: vasoconstriction and platelet aggregation
when Cox2 inhibition is increased, you get more vasoconstriction, Plts aggregating... leads to stroke and MI ...
what irreversibly inhibits platelet Cox 1? what does this mean?
low dose ASA
-it inhibits vasoconstriction and plt aggregation
to avoid dyspepsia and diarrhea with NSAIDS, what do they recommend?
take them with food or milk
can taking with food/milk help NSAID-caused GI bleeding and ulcer ?
can you hae a GI bleed/ulcer without symptoms?
YES (poor coorelation between ulcers/bleed and symptoms)
how can you prevent ulcers with NSAIDs?
take NSAID with PPI or misoprostol.
what is ketolorac (toradol) used for?
analgesia (cox 1) : moderate to severe pain. good for when you want to avoid narcotics (i.e. drug addict or fear of respiratory depression or poor metabolizer )
which Cox pathway is targets for analgesia, which for inflammation?
Cox 1- analgesia
cox 2- inflammation
what are the dosing limits for ketolorac (toradol)?
why are there these limits?
IM loading dose then...
-max per day: 40mg
-max days in a row: 5 days
-max day-period: 20days
* risk of ulcers-GI bleed increases!!!!
which cox pathway is "cardioprotective"? what does this have to do with ASA?
cox 2- vasodilates and prevents plt aggregation
- ASA is considered "cardioprotective", it turns off Cox 1 and allows for Cox 2
NSAIDs elevate BP on average __ - ___ mmHg above pt's baseline
what is the boxed warning on all NSAIDs?
why is this?
May increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), and stroke, which can be fatal.
(they upset the balance between Cox 1 and Cox 2)
NSAID-associated heart failure is thought to be due to increased _____ _______ _______ and reduced _____ _______ caused by prostaglandin inhibition
increased peripheral vascular resistance
reduced renal perfusion
Cox 2 inhibition by NSAIDs poses more of a risk for patients with CVD or CVD risk:
1. increased risk of death or repeat attack within ___ years.
2. ___% of pts who used an NSAID post-MI died within the 1st year compared to those that didnt.
20% died within the 1st year
what are the 4 agents with high cox2 selectivity? (maybe weeds)
high cox 2 selectives have greater ____ risk but lesser ___ risk
greater CV risk
less GI risk