NSAIDs mechanism, mechanism of NSAIDs

 

NSAIDs mechanism, Mechanism of NSAIDs

 

What is NSAIDs?

‘NSAIDs’ is an abbreviation of Non Steroidal Anti Inflammatory Drugs. The drugs inhibit an action of COX 1 & COX2(COX=cyclo-oxygenase) that promote to produce prostaglandins. Prostaglandins cause hyperalgesia(pain). So, if we inhibit prostaglandins from producing, we can reduce pain of stimulated tissue.

Prostaglandins also are involved inflammation process. So, if we suppress production of prostaglandins, we can suppress inflammation, too. That’s why we call ‘anti-inflammatory drugs’.

 

Mechnism

Phospholipids from cell membrane are converted to arachidonic acid by phospholipase-A2. Arachidonic acid is converted to endoperoxides(PGG2, PGH2 = prostaglandins). And then endoperoxides is changed to three types materials. 1. Prostanglandins(PGE2, PGD2, causing pain) 2. Thromboxane-A2(platelet aggregation, vasoconstriction) 3. Prostacyclin(=PGI2, vasodilation, disaggregation)

 

Type of drugs

We have different kinds of NSAIDs.

1.     Salicylate acid: aspirin

2.     Acetic Acid Derivate: Diclofenac, Indomethacin

3.     COX 2 inhibitors: Celecoxib

4.     Enolic Acid Derivate: Proxicam

5.     Propionic Acid Derivate: Ibuprofen, Naproxen, Fenoprofen

 

 

Side effects

NSAIDs are very effective and used widely to relieve pain, especially arthritis in old age. But they have side effects of GI system.

COX1 protects mucous membrane of stomach so COX inhibitors can cause GI bleeding or peptic ulcer disease because the drugs inhibit the action of COX1. So if you have serious GI trouble or problems, you can choose selective COX2 inhibitors. Selective COX2 inhibitors such as celecoxib don’t affect the action of COX1. So they don’t cause side effects of GI system.