Exam 4; Aspirin and NSAIDs Flashcards
What are the four major effects NSAIDs
analgesic
anti-pyretic
anti-inflammatory
anti-platelet (decrease in clotting
What is the clinical use for aspirin and NSAIDs at low doses
aches and pains
inhibition of clotting
What is the clinical use for aspirin and NSAIDs at high doses
pain/arthritis
What is the chemistry behind aspirin
salicylic acid + acetyl group → acetylsalicylic acid
What is the pharmacokinetics behind acetylsalicylic acid
its a weak acid that is more readily absorbed in a weak acid like the stomach)
acetylsalicylic acid is dissociated in the plasma to what, which can have what effects
into salicylic acid which strongly binds to plasma proteins which then can displace other proteins and drugs
What is the mechanism behind aspirin
it inhibits prostaglandin metabolism by inhibiting the enzyme cyclooxygenase
What are the two different types of cyclooxygenase that aspirin effects
COX1; all cells have this and it regulates prostaglandin synthesis
COX2; inflammatory cells have it which is responsible for the inflammation process
How does aspirin affect temperature
it lowers the temperature of a fever, but only in those with fever
may act in the CNS to counteract pyrogens
How does aspirin affect peripheral vasculature
may cause mild peripheral vasodilation
The use of aspirin to treat this is potentially very dangerous
viral infection in children; could cause Reye’s syndrome
What is the mechanism behind the analgesic effect of aspirin
decrease PG production (which are neuromodullary and may regulate pain)
has both central and peripheral effects
What is the mechanism being the anti-inflammatory effect of aspirin
PGs serve as vital signs for inflammation, so decreasing them decreases the signs and may also decrease immune cell migration and activity
What is the mechanism behind the anti-clotting effects of aspirin
ASA causes irreversible inhibition of platelet COX preventing the synthesis of thromboxane
What is the lethal dose of aspirin in children
4gram or 12 regular aspirin
What is the lethal dose of aspirin in adults
20 grams or 50-60 regular aspirin
What results in death from an overdose of aspirin
severe pulmonary edema
Which side effects are the most common when taking aspirin
GI effects; salicylic acid is a direct irritant
What is the mechanism behind GI upset involving aspirin
decreased mucosal production in GI
decreased bicarbonate in the GI; no longer a counter mechanism of stomach acid
What are two CNS effects of aspirin
tinnitus
increase respiration rate
In which patients is aspirin contraindicated
in patients with clotting deficiencies
Aspirin has a direct effect on which part of the eye
the iris, it reduces mitosis that occurs during and after eye surgery
How does aspirin affect the kidney
decreased kidney perfusion
True or False
Aspirin does not cause hypersensitivity reactions
False, it does
Aspirin causes this in pregnant women
inhibits labor, prolonging gestation
Aspirin can cause this, especially with patients with nasal polyps
bronchospasms
Which drug is not a NSAID because it has no anti-inflammatory or anti-platelet effects
acetaminophen
An OD of acetaminophen (20-30) tablets can cause what
irreversible liver damage
What is the mechanism behind acetaminophoen affecting the liver
most common cause of acute liver failure
reduces glutathione in the liver
will confound with an already damaged liver (like in alcoholics)
Which drug family are the NSAIDs
propionic acid derivatives; ibuprofen and the other "pro's" naproxyn fenoprofen ketoprofen flurbiprofen oxaprozin suprofen
What are the three NSAIDs that are acetic acid derivatives
Indomethacin
tolmetin
sulindac
What is the mechanism behind Indomethacin
very potent COX inhibitor
What are the side effects of indomethacin
thrombocytopenia
corneal opacities
plastic edema
What are side other NSAIDs
pyroxicam disclofenac bromfenac nepafenac etodolac nabumeone
This is a selective COX2 inhibitor
celecoxib
What is celecoxib used to help prevent
helps prevent the GI upset that aspirin usually cause
2 similar drugs to celecoxib have been pulled from the market, why?
may cause in increase in MI and stroke
All NSAIDs at high enough doses may have what
similar effects
