Flashcards in Drugs for Inflammation Deck (22):
1
What is the general action of glucocorticoids?
inhibit AA release and metabolism
2
What is the action of NSAIDs?
COX inhibition
3
What is the effect of antagonising CysLT1 receptors?
block LTC4 and LTD4 actions. Prevent bronchospasm and nasal congestion
4
T/F The action of the inducible Cox-2 is not as strong as the constitutive Cox-1
False, Cox-2 can be 100x more potent
5
What is one reason why tumor cells often cause acute and chronic inflammation
tumors induce Cox-2
6
Which prostaglandin is most related to inflammation
PGE2
7
What prevents us from using prostaglandin as drugs?
too unstable and expensive
8
T/F Aspirin is indicated for patients with gout
False, although anti-inflammatory, aspirin can compete with the clearance of urea at the kidneys
9
Why is NSAID useful for gout?
It blocks the action of PGE2, hence reducing inflammation
10
How does NSAID cause analgesia?
by removing sensitisation from AA products
11
Why is paracetamol preferred as an antipyretic?
aspirin tends to cause gastric bleeding more so than paracetamol
12
How does NSAID cause gastric ulcer?
by inhibiting PGE2, it also inhibits the ability to repair gastric mucosa. Without the protective effect of PGE2, there may be acid reaching the gastric lumen
13
T/F NSAID is an anti-coagulative
True
14
T/F low dose aspirin can prevent CV disease
True, because it affects only platelets in the portal circulation, reducing TXA2 but not affecting vascular PGI2
15
T/F NSAIDs can sometimes cause bronchoconstriction
True, some individuals are hypersensitive, and can overproduce leukotrienes
16
How is aspirin different to other NSAIDs?
it's irreversible
17
Which drug is Reye's syndrome associated with?
aspirin
18
How is paracetamol different to NSAIDs?
it's analgesic, antipyretic, but not anti-inflammatory
19
What is the theory of COX-2 selectivity?
its hydrophobic pocket for AA is larger than that of COX-1, so it can reduce GIT side effect while retaining efficacy
20
Why has some COX-2 agents been withdrawn?
they increase CV risk in the long run, because COX-2 is the main contributor of coronary artery integrity
21
What are the three mechanisms of action of glucocorticoids?
direct transactivation
direct transrepression
tethered transrepression
22