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What chemical is a key inflammatory mediator in tissue damage? What does it do?
bradykinin
stimulates arachidonic acid production
How is arachidonic acid converted to prostaglandins?
by cyclooxygenase (COX-1 and COX-2)
Differentiate COX-1 & COX-2
COX-1: maintain homeostatic functions
COX-2: mediate inflammation
What inhibits both COX-1 & COX-2?
is it patient pt dependent?
NSAIDs
*NSAID selection is pt dependent*
What are contraindications for NSAIDs? (5)
• Nursing and pregnancy
• Serious bleeding
• Allergy, Asthma, Angioedema
• Impaired renal function
• Drug (anticoagulant)
How does COX-1 & COX-2 affect thrombosis?
COX-1: anti-thrombotic side effects
COX-2: pro-thrombotic side effects
______ is an irreversible inhibitor of COX-1 & COX-2 and why
aspirin
enables anti-platelet activity (anti COX-1) prophylaxis
What are reversible inhibitors of COX-1 & COX-2
ibuprofen and other propionic acid derivative NSAIDs
NSAIDs such as ibuprofen interfere with what effect of aspirin therapy?
cardioprotective anti-platelet effect
(if aspirn and iborfen is in the body at the same time, aspirn needs to get to the cox-1 receptior, but if ibrofen get to it first aspin usaage will be reduced and less binding time beucse ibropfron is hort time while apsin is lobner)
The anti-inflammatory effects of selective COX-2 inhibitors are offset by what risk?
higher thrombotic risk
(just beucase cox -2 inhibior decreases plateltes clupinb, you can still get cloting cox-1 form thomboxane and have a clot in the artery and therfoe a stoke or mi)
What is the only FDA approved selective COX-2 inhibitor? why?
celecoxib
no platelet inhibition > good for warfarin patients
(it has little effect on platlets not clotting, so paltelts can still clot normally whoch is good beucase warfain already has increased bleeding)
acetaminophen charcstrisctics
when is it good
CNS
- good for analgesia
*Acetaminophen is a good alternative for pts with NSAID contraindications*
NSAIDs charcstrisctics
- PNS
- better anti-inflammatory
What is the drug of choice when treating fevers in children?
acetaminophen
What happens with acetaminophen overdose? how does this happen?
liver cell death
excess production of the toxic metabolite (NAPQ1) that depleted protective liver glutathione
NSAIDSs such as Idomethacin are a first line treatment for what? What if the patient has a contraindication to NSAID use?
acute gout
colchicine is used instead
Studies suggest that dental pain is most amenable to treatment by what drugs?
NSAID analgesics or acetaminophen
The NSAID plateau effect describes how maximum alleviation of acute pain occurs between what doses? What happens past this range?
650-1000mg
NSAID toxicity becomes apparent
What can be used to push past the NSAID plateau effects, minimizing the use of opioids and why
acetaminophen combined with an NSAI; enables additive analgesia
(rember the plateau effect is whn u keep taking nsaids and it gets to the point that ur are not longer getting therapeutic effects or less of it)
What combination of drugs is useful for patients with emotional pain components?
and what else can it do
NSAID/opiod
can also provide additive analgesia beyond the NSAID plateau effect for serve pain
What are side effects of using NSAID/opioid in combination to push past the plateau effect?
nausea, constipation and depression
Depending on patient-specific contraindications, what may be better than NSAID/opioid combos for severe pain situations such as bony impaction surgery?
ketorolac