NSAIDS Flashcards
aspirin chemical name
Acetyl-salicylic acid
NSAID target
Prostaglandin synthesis
Rate limiting step of prostaglandin synthesis
COX activity
COX-1 Functions
Fever
Pain
Protect mucosal lining of stomach
Increase platelet aggregation
Regulate kidney function
Prototype COX-1 inhibitor
Aspirin
COX-2 Functions
Pain
Protect mucosal lining of stomach
Decrease platelet aggregation in endothelial cells
Wound healing
Inflammation
Prototype COX-2 inhibitor
Celecoxib
Aspirin dose
325 mg
Aspirin is hydrolyzed to:
Salicylic acid
Salicylate NSAID metabolism
Low dose:
High dose:
Low dose: conjugated in liver; first order kinetics
High dose: excreted.by kidneys unmetabolized; zero order kinetics
Low dose aspirin uses:
Pain
Fever
Anticoagulation
High dose aspirin uses:
Inflammation
Aspirin mechanism of anti-coagulation
Salicylate Irreversibly/covalently binds to COX-1 to decrease platelet synthesis of thromboxanes
Aspirin side effects
Bleeding
GI irritation
Premature closure of ductus arteriosus
Aspirin contraindications
Clotting deficiencies
Children
Late pregnancy
Aspirin drug interactions
Warfarin, methotrexate, sulfonamides
Aspirin overdose treatment
Bowel irrigation
Activated charcoal
Volume repletion
Alkalinization of urine
Non-aspirin NSAIDs are derivatives of:
Proprionic acid
Ibuprofen brand names
Motrin
Advil
Celecoxib brand name
Celebrex
Naproxen brand name
Aleve
Ibuprofen dose:
200mg for pain and fever
400mg for anti-inflammatory
Non-aspirin NSAID adverse effects
GI irritation
Increased bleeding time (shorter term than aspirin; reversible)
Drug interactions (high albumin binding)
Renal toxicity
Indomethacin is a derivative of:
Acetic acid
Indomethacin is more/less potent than aspirin?
More potent (10-20x)
Indomethacin main use
Severe inflammation
Not used for pain or.fever due to severe side effects
Celecoxib mechanism of action
Selective COX-2 inhibitor
Celecoxib uses
Decrease inflammation and pain with less side effects than COX-1 inhibitors
Celecoxib adverse effects
Edema
GI upset
Increase risk of MI
Acetaminophen chemical name
Acetyl para-amino phenol (APAP)
Acetaminophen MOA
Unknown
Probably COX and prostaglandin inhibition
Acetaminophen dose
325mg
Acetaminophen uses
Pain
Fever
NOT inflammation
Maximum daily dose of acetaminophen
4g
Acetaminophen adverse effects
Hepatic damage
Skin rash
Mucosal lesions
Nephrotoxicity
Acetaminophen overdose symptoms
GI distress
Hepatotoxicity
Acetaminophen overdose treatment
Supportive care
Activated charcoal
N-acetyl-cysteine (Acetadote)
Which of the following drugs is specifically approved for and frequently
advertised for treating menstrual cramps and pain?
A. Indomethacin
B. Naproxen
C. Celecoxib
D. Aspirin
E. Acetaminophen
B. Naproxen
In a setting of overdose toxicity with aspirin, which of the following
pairs the most serious concern with its appropriate treatment?
A. hepatotoxicity, treated with sodium bicarbonate.
B. hepatotoxicity, treated with N-acetyl-cysteine.
C. long-lasting inhibition of coagulation, treated with N-acetyl-cysteine.
D. risk of GI ulceration, treated with prostaglandin analogs, such as
misoprostol.
E. respiratory and metabolic acidosis, treated with sodium bicarbonate
E. respiratory and metabolic acidosis, treated with sodium bicarbonate
A drug whose use is limited to specific types of severe inflammation
because of its significant toxicities in other settings is
A. naproxen sodium.
B. indomethacin.
C. celecoxib.
D. prednisolone.
E. acetaminophen.
B. indomethacin
Aspirin is the only drug specifically recommended for decreasing the
risk of myocardial infarction and stroke in middle-aged and aging
persons or those with a prior incident. This is because aspirin
A. is more COX-2 selective than any other NSAIDs.
B. is the only NSAID that inhibits platelets significantly because of its
selective uptake by platelets.
C. has significantly greater COX-2 inhibition than any of the other orally
effective NSAIDs.
D. causes irreversible covalent acetylation of COXs in platelets.
E. inhibits prostacyclin production to a greater extent than
thromboxane production
D. causes irreversible covalent acetylation of COXs in platelets.
GI distress and potential GI hemorrhage with prolonged use is a
greater concern with
A. aspirin than with other salicylates.
B. ibuprofen than with aspirin.
C. celecoxib than with naproxen.
D. aspirin than with celecoxib.
E. acetaminophen than with ibuprofen.
D. aspirin than with celecoxib
A 3-year -old child is brought to the emergency room after ingesting the
remaining aspirin tablets from a 50-tablets bottle about 3 hours earlier
The mother estimates that 30-35 tablets were in the bottle. The child is
unconscious and given sodium bicarbonate intravenously. Which of
the following best describes the goal of the sodium bicarbonate?
A. To alkalinize the plasma, to prevent respiratory acidosis
B. To alkalinize the urine, to remove salicylate from the plasma by ion
trapping.
C. To neutralize the salicylic acid in the blood stream
D. To prevent binding of the aspirin to plasma binding proteins that can
cause indirect side effects
E. To serve as a sulfhydryl group “sink” to react with the excess salicylic
acid
B. To alkalinize the urine, to remove salicylate from the plasma by ion trapping
