Flashcards in L11-12 Anti-inflammatories Deck (89)
Loading flashcards...
1
What does NSAID stand for
Non-steroidal anti-inflamatory drug
2
When was the natural precurrsor to aspirin disocered
5th century
3
What does coxib stand for
COX2 - Inhibitors
4
What was significant in 18228
Leroux isolated the active ingredient for aspirin from the willow tree
5
What is the active ingredient in aspirin
Salicyclic acid
6
What was done in 1897 to produce the first synthetic drug, who was this done by
Hoffman
Ester group was added to form acetyl-salcylic acid
7
What was acetyl-salicyclic acid used to treat, why was this better than other treatments
Arthritus
Tolerated better by the GI system
8
What is different between all of the various NSAIDS
Phramacokinetics, derivation and side effects
9
What are NSAIDs generally prescribed for
Rheumatic musculoskeletal problems
10
What group of people are especially at risk when taking NSAIDs
Elderly
11
Two NSAID examples
Paracetamol
12
What are coxibs
Group of drugs which act to inhibit COX-2
13
What does phospholipase A catalyse
The conversion of phospholipid to aracidonate
14
What catalyses the conversion of phospholipid to aracidonate
Phospholipase A
15
What group of enzymes catlayse the conversion of aracidonate to thromboxane and prostaglandins
Cyclo-oxygenases
16
What does the COX enzyme (cyclo-oxygenase) catalyse
The conversion of aracidonate to thromboxane and prostaglandins
17
What is the action of NSAIDs on cyclo-oxygenases
What effect does this have on prostaglandins and thromboxane
Inhibits
Decreases the levels of prostaglandins and thromboxanes
18
Effects of PGI2
Vasodilator
Hyperalgesic
Stops platelet aggregation
19
Effects of PGD2
Vasodilator
Inhibits the aggregation of platelets
20
Effects of PGE2
Vasodilator
Hyperalgesic
21
Effect of thromboxane A2
Thrombotic : it stimulates activation of new platelets as well as increases platelet aggregation
Vasoconstrictor
22
What effect would thromboxane A2 have on clot formation
Would cause the formation of blood clots
23
What is the effect on PGs and thromboxane of NSAIDS
Decrease both
24
Describe the anti-inflammatory effects of NSAIDs
Decrease vasodilation --> reduce oedema
Ineffective against mediators that contribute to tissue damage associated with chronic inflammatory conditions
25
Describe the analgesic effects of NSAIDs
Decrease the prostaglandin production in damaged/inflamed tissue
PG is responsible for the sensitisation of nociceptors to inflammatory mediators (e.g. bradykinin)
26
What does analgesic mean
Reduction of pain
27
Describe the anti-pyretic effects of NSAIDs
Thermostat in the hypothalamus is activated by IL-1
COX2 induction causes production of PGE-2 signals to IL-1
Inhibition of COX2 here leads to less signalling of PGE2 to IL-1 which leads to a reduction of activation of the hypothalamus
28
Why are NSAIDS used after surgery
As can reduce the need for opiate drugs when given in the right combination
29
Why are NSAIDs effective at treating headaches
May be due to the ability to deecrease vasodilation
Vasodilation of the cerebral vasculature is what is thought to be behind headaches
30
