NSAIDs Flashcards
Name 3 chemical mediators of inflammation.
1) kinins
2) histamine
3) neuropeptides
Give an example of a kinin.
bradykinin
Give an example of a neuropeptide.
substance P
Tissue destruction leads to release of _____ and synthesis of _____.
chemical mediators; eicosanoid mediators
Where do eicosanoid mediators derive from?
arachadonic acid
What is the target of an NSAID?
COX-1 and COX-2
By inhibiting COX1 and 2, production of ____ and ____ will decrease.
inflammatory prostaglandins; thromboxanes
COX is the major synthetic enzyme for ___ and ____.
prostaglandins (PGs); thromboxane A2 (TXA2)
What are the 4 therapeutic uses of an NSAID?
1) analgesia
2) antipyretic
3) anti-inflammatory
4) antithrombogenesis
How is analgesia achieved by an NSAID?
inhibition of inducible COX-2 at sites of tissue injury
How is an antipyretic affect achieved by an NSAID?
inhibition of inducible COX-2 in the hypothalamus
How is an anti-inflammatory affect achieved by an NSAID?
inhibition of inducible COX-2 at sites of inflammation
How is an antithrobogenesis affect achieved by an NSAID?
inhibition of constituitive COX-1 in platelets
Name 5 common side affects of NSAIDs.
1) GI ulcers, bleeding, nausea
2) increased bleeding problems
3) renal failure and nephritis
4) interference with uterine contractions
5) increased thrombotic events
Aspirin group
irreversible inhibition of COX-1 AND COX-2
traditional NSAIDs group
reversible inhibition of COX-1 and COX-2
acetaminophen group
inhibits COX-2 in CNS ONLY
cox-2 selective inhibitors group
selective reversible inhibition of COX-2 ONLY
Name the 5 chemical classes of traditional NSAIDs.
1) salicylates
2) pyrazolone derivatives
3) acetic/carboxylic acids
4) oxicam derivatives
5) propionic acid derivatives
What are salicylates used for?
analgesic, antipyretic, anti-inflammatory
What are pyrazolone derivatives used for?
analgesic, antipyretic, anti-inflammatory
What are acetic/carboxylic acids used for?
analgesic, antipyretic, anti-inflammatory
What are oxicam derivatives used for?
analgesic, antipyretic, anti-inflammatory
What are propionic acid used for?
analgesic, antipyretic, anti-inflammatory
What is aspirin used for?
analgesic, antipyretic, anti-inflammatory, antithrombotic
Name 2 Pyrazolone derivatives.
1) phenylbutazone
2) oxyphenbutazone
Name 4 acetic/carboxylic acids.
1) Indomethacin
2) Sulindac
3) Ketorolac
4) Nabumetone
Name 2 oxicam derivatives.
1) piroxicam
2) meloxicam
Name 5 proprionic acid derivatives.
1) ibuprofen
2) naproxen
3) ketoprofen
4) flurbiprofen
5) oxaprozin
Name one positive and one negative to pyrazolone derivative use.
positive: more potent and longer lasting
negative: serious toxicities with chronic use or misuse
Name one positive and one negative to pyrazolone acetic/carboxylic acid use.
positive: fewer toxic rxns than pyrazolones
negative: more total adverse rxns; limited to arthritis
Name one positive and one negative to oxicam derivative use.
positive: Potent, extremely long half-lives (15-50 hrs)
negative: Potent, extremely long half-lives (15-50 hrs)
Name one positive and one negative to proprionic acid derivative use.
positive: better tolerated than other NSAIDs
negative: general NSAID risks
What is acetaminophen used for?
Analgesic; antipyretic
What is a positive to acetaminiophen use?
less GI side effects
What is celecoxib (Celebrex) used for?
Analgesic, antipyretic, anti-inflammatory
What is a positive to celecoxib (Celebrex) use?
less GI side effects
Treatment of ____ pain usually requires opiod analgesics.
visceral
Treatment of visceral pain usually requires _____.
opiod analgesics
What is visceral pain caused by?
direct stimulation of sensory nerves (Aδ)
What is the dose for anti-inflammatory NSAID affects?
> 4g/day
What is the mechanism of action for the anti-platelet affect seen with NSAIDs?
inhibition of platelet aggregation
Why is platelet clumping prevented for the life of the platelet?
platelets cannot synthesize new COX-1
Where is the largest concentration of acetylsalicylic acid?
in the portal vein
_____ is rapidly hydrolyzed to salicylate by esterases in blood.
Acetylsalicylic acid
Acetylsalicylic acid is rapidly hydrolyzed to _____ by _____ in blood.
salicylate; esterases