Pharmacology of NSAIDs Flashcards
What are the properties of NSAIDS
Analgesisa, antipyresis, anti-inflammatory
What type of prostaglandins are produced by COX-1
support platelets and protect the stomach
Which COX enzymes are active under healthy conditions, expressed in inflammatory cells
COX-1 (constitutive), COX-2 (inducible)
Which COX-2 selective enzyme inhibitor reduces hormones causing inflammation and pain in the body, the biggest drawback
Celecoxib, increase cardiovascular thrombotic events
T/F: Ibuprofen is COX-1 selective
False: Ibuprofen is nonselective for COX-1 and COX-2
What is the product of the COX-1 isoform and what are the functions
Thromboxane (TXA2): vasoconstriction and platelet aggregation (thrombosis)
What is the product of the COX-2 isoform and what are the functions
Prostacyclin (PGI2): vasodilator and inhibits platelet aggegation
How do selective COX-2 inhibitors increase cardiac events
Homeostatic balance between TXA2 and PGI2 shifts to cause more thrombosis
T/F: NSAID anti-inflammatory effects require higher doses compared with analgesic doses
True
What are characteristics that NSAIDs have that opiates don’t
Ceiling effect, anti-inflammation, antiplatelet effect
In peripheral pain what are the steps prostaglandins make to increase pain
Arachidonic acid is released during tissue damage, arachidonic acid is then metabolized to prostaglandin, prostaglandin blocks the potassium efflux released from nociceptors following damage resulting in additional depolarization making the nociceptor more sensitive
How do NSAIDS cause analgesia
Reduces sensitization of nociceptive nerve ending to mediators like bradykinin and histamine
Which prostaglandin increases body temperature, how
PGE2, Receptors on neurons in hypothalamus recognize PGE2 and the body temperature resets to a few degrees higher than normal
What are the effects NSIADs have on fever
Innhibit PGE2 synthesis at thermoregulatory centers in the hypothalamus leading to body temperature resetting to normal, sweating, vasodilation
T/F: NSAIDs taken when a patient has normal body temperature casues them to be colder
False: NSAIDs has little effect on “normal” body temperature
Which prostaglandins csensitize skin pain receptors
PGE2 and PGI2
How do prostaglandins cause inflammation
Direct vasodilation and potentiation of other vasodilatiors (bradykinin and histamine) increasing blood flow, potentiation of effects of bradykinin and histamine on vascular permeability lead to edema and swelling
Which NSAID is most effective as antifinflammaotry and is used to close the ductus arteriosus
Indomethacin
What are the propionic acids
Ibuprofen, ketoprofen, and naproxen
What are the acetic acid derivatives
Indomethcin, Etodolac, ketorolac, sulindac, diclofenac
What are the fenmates
Mefenamic acid and meclofenamic acid
What are the oxicams
Meloxicam and piroxicam
What is the non acidic compound NSAID
Nabumetone
Which NSAIDs are most COX-2 selective
Etodolac and Meloxicam
What are the topical NSIADS
Diclofenac and ketoprofen
T/F: Mefenamic is needs no dose reduction required for renal impairment
True
What are the formulations for ketorolac, when is it used, cautious tip
oral, IV and IM/ postoperations for analgesia/ causes ulcers more frequently so use no more than 5 days
Which NSAID is once daily dosing
Piroxicam
T/F: Selective COX-2 inhibitors are useful in patient unable to tolerate conventional NSAIDs
True
What is the active metabolite of acetaminophen (paracetamol)
Phenacetin
What are the proposed ways APAP works
inhibits COX-3, work in the CNS
What are properties APAP has, normal dose
Analgesic and antipyretic/ 2-4 grams per day (no more than 4)
Why does acetaminopehn cause toxicity
NAPQI binds with hepatocytes leading to liver injury
What is the most common cause of death ffollowing an aspirin oversoe
Cadiopulmonary arrest usually due to pulmonary edema (respiratory and renal depression)
Which NSAID is associated with ringing in the ear, which is the safest non-selective NSAID for people iwth CAD
Aspirin, Naproxen
