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NSAID

Non-steroidal anti-inflammatory drugs (NSAIDs) can be classified based on their selectivity for inhibiting cyclooxygenase (COX) enzymes. Non-selective NSAIDs inhibit both COX-1 and COX-2, preferential NSAIDs mainly inhibit COX-2, and selective NSAIDs specifically target COX-2. COX-1 is constitutively expressed and acts as a housekeeping enzyme, while COX-2 expression is induced during tissue injury and inflammation. By selectively inhibiting COX-2, NSAIDs can provide anti-inflammatory and analgesic effects without the gastrointestinal side effects of non-selective inhibition of COX-1. NSAIDs work by blocking the COX enzyme pathway

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566 views

NSAID

Non-steroidal anti-inflammatory drugs (NSAIDs) can be classified based on their selectivity for inhibiting cyclooxygenase (COX) enzymes. Non-selective NSAIDs inhibit both COX-1 and COX-2, preferential NSAIDs mainly inhibit COX-2, and selective NSAIDs specifically target COX-2. COX-1 is constitutively expressed and acts as a housekeeping enzyme, while COX-2 expression is induced during tissue injury and inflammation. By selectively inhibiting COX-2, NSAIDs can provide anti-inflammatory and analgesic effects without the gastrointestinal side effects of non-selective inhibition of COX-1. NSAIDs work by blocking the COX enzyme pathway

Uploaded by

Shubhangi
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Classification and Mechanism of Action

NSAID
Non steroidal anti-inflammatory Drugs

*Classification- KD
Tripathi

Non-Selective Preferential Selective Analgesic-Antipyretic


with poor
COX Inhibitor COX2 Inhibitor COX2 Inhibitor Anti-inflammatory
Nimesulide, Diclofenac, Celecoxib, Etoricoxib, Parecoxib Action
Aceclofenac, Meloxicam, Etodolac

Category Example
Salicylates Aspirin Example
Propionic acid derivative Ibuproprofen, Naproxen, Ketoprofen, Flurbiprofen Paracetamol (Acetaminophen)
Fenamate Mephenmic acid www.facebook.com/pharmavideo/ Metamizol, Propiphenazone
Enolic acid derivative Piroxicam, Tenoxicam Nefopam
Acetic acid derivative Ketorolac, Indomethacin, Nabumetone
*Constitutive = Constant Production
Pyrazolone derivative Phenylbutazone, Oxyphenbutazone

Key Point (Solution) - As name Indicate NSAIDs are those agents which are used to get relief from pain, inflammation and fever.
And as per the COX pathway we understand that COX-1 and COX-2 ultimately form prostaglandin which initiates perception of
pain and inflammation. So anyhow if we block or inhibit the synthesis of PG we may reduce pain and inflammation. Although
COX-1 is constitutive in nature thus it always get secreted without induction of injury and called as a house keeper so it’s better to
inhibit COX-2 rather than COX-1.
* Tissue Injury
(Applicable for COX-2)

Breakdown of Membrane Phospholipids

Arachidonic acid

Mechanism of Action
Cyclooxygenase Pathway
*Rough Idea- Lippincott

COX-2 gene transcription


COX-1 perform housekeeping function

COX-1 gene transcription Induced by-


Oxidative Stress, Injury, Ischemia, Seizures
Like neutralizing gastric acids

Glucocorticoids Inhibit
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mRNA
mRNA
Inhibit

Selective
Non-Selective COX-2Inhibitor
Inhibit COX Inhibitor Celecoxib, Etoricoxib, Parecoxib

Non-Selective
Inhibit Inhibit
COX Inhibitor

COX- 1 Side Effect- Gastric Ulcer COX- 2

PROSTAGLANDIN
S
*Diagrams and explainations are made by solution-pharmacy
E Mail- [email protected] & Reach solution at- www.facebook.com/pharmavideo/

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