NSAIDS Flashcards
Cox 1 = is _______ and expresses _____ primarily
Cox 2 = is ________ and expresses _____
Cox 1 = constitutively and noninflammatory cells
Cox 2 = inducible and inflammatory cells
Leukotriene play a key role in _____
allergies, allergic rhinitis, & asthma
Cox-1 is located ____ role is _____
Platelets Vasoconstriction + increase platelet aggregation = thrombosis
Cox-2 is located ____ and role is
Endothelial cells
vasodilation + decrease platelet aggregation
Thromboxane and Prostaglandins
Cox-1
Prostaglandins and Prostacyclin
Cox-2
Non-selective NSAIDs effects
reduce inflammation
reduce pain
reduce fever
Aspirin at low dose =
anti-platelet effects
Non-selective NSAIDs adverse effects
- increased gastric acid –> peptic ulcers + GI bleeds
- decreases renal blood flow –> increased RAAS, blood Ka+ levels & TPR
- Increased bleeding (anti-platelet)
- Increased cardiovascular events (MI & Stroke because of decreased prostacyclin) - except aspirin
- increased asthma
Contraindication for non-selective NSAIDs
Pregnancy = conception (hard for implantation)+ 3rd trimester (increased bleeding)
Aspirin MOA
irreversibly inhibits COX
Aspirin is _____ plasma protein bound and has first order kinetics at ___ does and zero order kinetics at __ does
highly
low
high
We must ____ urine to increase aspirin excretion
Alkalinize
Aspirin ADRs
anti-platelet = gastric ulceration because of ion trapping in gastric cells
increased bleeding risk
Hypersensitivity rxns
Asthma in people in aspirin hypersensitivity
Reye’s syndrome
Salicylism = respiratory alkalosis then metabolic acidosis + respiratory acidosis (increased lactic acid)
Non-selective NSAIDS =
Ibuprofen
Naproxen
Indomethacin (great inflammatory)
Ketorolac = greater analgesic effectiveness
____ helps keep ductus open
PGE1
Ibuprofen is dosed for
anti-inflammatory responses
Naproxen is useful for
acute gout + ankylosing spondylitis
Ketorolac is the only non-selective NSAID that is
potent analgesic = efficacy similar to morphine
ONLY available in parental formulation
Celecoxib
selective Cox-2 inhibitor that interacts with warfarin because of 2c9
also sulfa allergies
Acetaminophen MOA
Inhibits Cox-3 = analgesic & antipyretic effects
very weak Cox-1 & 2
Acetaminophen is preferred for patients that
current or previous peptic ulcers or GI bleeds
hemophilia
Acetaminophen FDA limit is
4000 mg/day
Acetaminophen is ____ plasma protein bound
poorly