NSAIDs Flashcards
what are 4 uses of NSAIDs?
- Mild to moderate pain relief
- Anti-inflammatory
- Analgesic
- Anti-pyretic
What is the largest group of drugs having adverse effects?
NSAIDs
The use of lower doses of multiple drug classes provides higher safety and less negative side effects is known as what?
Multi-modal analgesia
NSAIDs have sparing effects on what other category of drug?
Opioids
What is the rate-limiting step of the arachidonic acid cascade?
Release of AA from membrane phospholipid catalyzed by enzyme phospholipase A2.
Cyclooxygenase (COX) oxidizes arachidonic acid (AA) to what?
Prostaglandins (PGs)
Lipoxygenase (LOX) oxidizes AA to what?
Leukotrienes
Are prostaglandins continually synthesized?
Yes
Are prostaglandins stored?
No
Where do prostaglandins act?
Locally at site of production.
T/F: Prostaglandins have only a few physiological functions.
False - Prostaglandins have many physiological functions.
What can inhibition of prostaglandins result in?
Serious side effects.
What are 2 functions of COX 1?
- Mucosal defense
- Platelet function (TxA2)
What effect does COX 2 have on mucosa?
Prevents erosions & promotes healing.
Which COX acts as an anti-inflammatory?
How?
- COX 2
- Inhibits leukocyte adherence
Which COX offers renal protection?
COX 2
Which COX is involved with fever initiation?
COX 3
What are 4 functions COX inhibition affects?
- Primary plug formation of platelets
- Renal & gastric mucosa vascular tone
- Smooth muscle contraction
- Temperature regulation
T/F: Different drugs inhibit COX 1, 2 & 3 variably.
True
Which COX is involved with vicero-nociception and thermal stimulation?
COX 1
T/F: COX 1 is involved in constitutive functions with COX 2.
True
Which COX is inducible?
COX 2
Which COX is up-regulated during inflammatory states?
COX 2
There is over a 20 times greater presence of which COX at injured sites?
COX 2
Which COX has a key role in nociception?
COX 2
What are 2 functions of COX 3?
- Pyrexia
- Analgesia
Does COX 3 have better or poorer anti-inflammatory properties than COX 1 & 2?
Poorer
COX 3 is derived from what?
COX 1 gene
What are 5 drugs that inhibit both COX 1 & 2?
- Aspirin
- Phenylbutazone
- Ketoprofen
- Ketorolac
- Flunixin meglumine
What are 5 drugs that are COX 2 preferential and have weak COX 1 inhibition?
- Meloxicam
- Carprofen
- Etodolac
- Vedaprofen
- Tolfenamic acid
What are 3 drugs that are COX 2 selective?
- Deracoxib
- Firocoxib
- Robenacoxib
What are 2 drugs that are COX 3 preferential and have weak COX 1 & 2 inhibition?
- Acetaminophen
- Diclofenac
What is an example of a COX & LOX inhibitor?
Tepoxalin
What do prostaglandins mediate?
- Pain
- Inflammation
Prostaglandins have what type of central effects?
Central anti-nociceptive effects
Are NSAIDs highly protein bound?
How might this affect other drugs?
- Yes
- May displace other drugs and increase their plasma concentration.
What are 2 concerns with giving NSAIDs?
- Patient with underlying organ dysfunction.
- Patient receiving other highly protein-bound drugs with narrow therapeutic index.
Do NSAIDs have a wide or narrow safety margin?
Narrow
Can the upper dose limit be exceeded with NSAIDs?
No
What dose of NSAIDs should be used?
Lowest effective dose
How much time should be waited in between drugs?
Minimum of 7 days