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Flashcards in NSAIDS Deck (30):

What are NSAIDs?

Non Steroidal Anti Inflammatory Drugs


What do NSAIDs do?

Analgesic (anti-pain), antipyretic (anti-fever), anti-inflammatory (except acetaminophen)
With a ceiling effect


How do NSAIDs work?

Stop the formation of prostaglandins by blocking the COX 1,2,3 enzymes


What does cyclo-oxygenase-1 do?

Found in many cell types. Many critical functions like maintaining stomach lining
Not involved in fever


What does cyclo-oxygenase 2 do?

This form is induced in immune cells
Responsible for pain, inflammation and fever


What are the 3 phases of inflammation?

Acute transient phases (local vasodilation, increased capillary permeability)
Delayed subacute phase (infiltration of leukocytes and phagocytes)
Chronic proliferative phase (tissue degeneration and fibrosis)


What do prostaglandins do?

Released following cell damage, cause local inflammation, increased blood flow, severe pain, increase hypothalamic set point, stimulate local pain fibres


What are NSAIDs most useful for?

Uterine cramping, joint swelling
Would be more superior than opioids but take too long to work


What are the other effects of prostaglandins?

Platelet aggregation formation, modulate stomach acidity and mucous lining, uterine contraction


What are the 2 mechanisms of action of ASA?

Irreversibly acetylates COX enzymes (unlike the other NSAIDs) with the effect lasting as long as it takes to replace the enzymes
Not dependent on clearance


How can caffeine be used to help NSAIDs?

Will increase the effect of all non-opioid analgesics to give a co-analgesic effect.
60-120 mg (cup of coffee)


What happens in caffeine withdrawal?

Sudden onset of a headache


What can cause salicylate overdose?

Pepto bismol (bismuth salicylate) and methylsalicylate (oil of wintergreen-4 ml)


What are some symptoms of salicylate overdose?

Increase in metabolic rate due to interference with oxidative metabolism (hyperventilation, metabolic acidosis, severe hypoglycemia)


What are the immediate dangers of a salicylate overdose?

Hyperthermia, dehydration and hypoglycemia


What is the treatment of salicylate overdose?

Parenteral fluids and glucose (always, immediately), parenteral sodium bicarbonate, acetazolamide, activated charcoal (only within 2 hours), polyelectrolyte lavage (for modified release salicylate) or hemodialysis (severe)


What are the salycilates?

Methylsalicylate, bismuth salicylate, aspirin


Which NSAIDs are in the proprionic acid class?

Ibuprofen (less GI effects), Naproxen (twice daily dosing)


What is diclofenac?

A prescription only high potency NSAID with a higher GI bleed risk
Used for inflammatory pain (arthritis, post operative swelling, gout), sometimes endometriosis
Gel for muscular/joint pain


What is indomethacin used for?

Specifically for gout pain and swelling


Why are there GI side effects with NSAIDs?

Prostaglandins are made by the gastric mucosa and surpress acid production, increase gastric blood flow and increase secretion of mucin.
Non selective COX inhibitors inhibit COX-1, increasing acid production and decreasing mucous protection.


What is misoprostol? What is it used for?

A prostaglandin analog (similar structure and function) that is given with ASA to supply the stomach with the prostaglandin effect lost with non-selective COX inhibitors


What are some adverse effects from NSAIDs?

Reye's Syndrome (ASA in children with viral infections and genetic predisposition)


What are some drug interactions with NSAIDs?

Inhibits alcohol, warfarin and rofecoxib


In what patients should NSAID use be cautioned?

Hypertension, angina, (increase in circulating volume) bleeding disorders


What are some example of COX 2 selective inhibitors?

Vioxx and Bextra (pulled, heart attack risk)
Celebrex has black box warning


How are the analgesic effects of acteaminophen different from other NSAIDs?

Acts centrally, thus no ceiling effect


How does acetaminophen overdose occur?

A highly reactive metabolite of acetaminophen depletes GSH (antioxidant) in the liver causing damage to liver indirectly from loss of anti-oxidant and directly from highly reactive intermediate.


What are the signs and symptoms of acetaminophen overdose?

Severely elevated serum transaminase levels, hepatic encephalopathy and jaundice


What is the best way to treat a headache?

Highest dose of NSAID, cup of coffee and glass of cold water.