NSAIDs Flashcards
What are the objectives of using NSAIDs?
Used to minimize the unpleasant aspects of inflammation without altering the mental status
What are the functions f COX1?
Numerous functions in homeostasis including gastroprotectant (mucous protection), platelet aggregation, and regulation of renal blood flow
T/F COX1 activity is required for homeostasis
TRUE
T/F If given the choice, you would prefer to inhibit COX1
FALSE; want to try and avoid this
T/F COX2 has a major function in homeostasis with a high basal activity
FALSE; COX2 has a minor role in homeostasis and a low basal activity
What does COX2 play a role in?
Kidney and renin system
Pregnancy: implantation
COX2 is constitutively and inducibly produced. Which ones occurs more?
Inducibly
Inducible COX2 leads to:
Pain
Inflammation
Fever
COX3 is a major regulator of:
pyresis
What is the mechanism of action for NSAIDs?
Physically interact with and thus inhibit the action of COX
What are the 4 indications and therapeutic uses for NSAIDs?
Alleviation of mild to moderate pain
Anti-pyrexia
Anti-inflammatory
Anti-coagulation
What types of pain does NSAIDs alleviate?
Chronic pain Increase the threshold for activating nociceptors Neuropathic pain partially Hyperalgesia Allodynia: partially Visceral pain is alleviated by 1 NSAID
What is the one type of pain no NSAID alleviates?
Acute and/or severe pain
What COX does an NSAID target to alleviate fever?
COX3; restores the status quo of thermoregulation
How do NSAIDs work as anti-inflammatories?
Block PGE2 mediated vasodialtion, including cause by LPS
Block PGE2 mediated synthesis of numerous pro-inflammatory mediators
How do NSAIDs work as anti-coagulants?
Block the synthesis of thromboxanes
LOX activity is inducible as part of what?
Severe inflammation
T/F Inhibition of LOX has no effect upon pain
TRUE
What are some of the adverse side effects seen with NSAID use?
GI ulceration: Key to producing gastric mucous
Hepatotoxic: mechanism unclear
Nephrotoxic: PGs modulate renal effects upon fluid elimination and renin secretion
CV issues: GI2 is key to prevent platelet aggregation and maintain shape of vascular endothelium
What would you use with NSAIDs to prtoect the GI mucosa?
Misoprostol; a PGE1 analog
LOX inhibition is also gastroprotective
Name 4 adverse drug reations/interactions involving NSAIDs
W/ corticosteroids: indifferent to each others activity and both harm the GI
W/ anticoagulants: potentiate each other. Patient becomes super anti-coagulant
W/ antihypertensives: antagonize each other
W/ aminoglycoside: both drugs are nephrotoxic
Why can’t you just go around hammering COX2 all willy nilly like?
It plays very specific homeostatic functions like kidney hemodynamics and CV integrity
Why doesn’t NSAIDs work against Rheumatoid arthritis?
Activated platelets release microparticles that erode the joint surfaces and that release is COX-independent
In surgery, which COX is king?
COX1»_space;> COX2
In inflammation/infection what is the COX of the walk?
COX 2»_space;> COX 1
Name 3 functions of COX1 in homeostasis:
- Gastroprotectant
- Platelet aggregation
- Regulation of renal blood flow
How do NSAIDs alter nociception?
Increases the threshold for activating nociceptors; requires a more powerful stimulus
How do COX1 and COX2 differ with regards to basal activity?
COX1 = high basal activity COX2 = low basal activity
What is a potentially better NSAID target, COX1 or COX2?
COX2
