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NSAIDs

The document discusses Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) that inhibit cyclooxygenase enzymes to provide anti-inflammatory, analgesic, and antipyretic effects. It categorizes NSAIDs into nonselective COX inhibitors, preferential COX-2 inhibitors, and selective COX-2 inhibitors, listing various drugs under each category. Important points about specific drugs, such as Celecoxib and Nimesulide, are also highlighted.

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4 views4 pages

NSAIDs

The document discusses Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) that inhibit cyclooxygenase enzymes to provide anti-inflammatory, analgesic, and antipyretic effects. It categorizes NSAIDs into nonselective COX inhibitors, preferential COX-2 inhibitors, and selective COX-2 inhibitors, listing various drugs under each category. Important points about specific drugs, such as Celecoxib and Nimesulide, are also highlighted.

Uploaded by

aagaman2k23
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

.

1 Medicinal Chemistry
.

Non-Steroidal Anti-Inflammatory
Drugs (NSAIDs)

Introduction
Drugs that inhibit cyclooxygenase (COX-1 and COX-2) enzymes, thereby blocking prostaglandin synthesis to
produce anti-inflammatory, analgesic, and antipyretic effects.
CLASSIFICATION:
Category Subclass Drugs
Nonselective COX inhibitors Salicylates Aspirin
Ibuprofen, Naproxen, Ketoprofen,
Propionic acid derivatives
Flurbiprofen
Fenamate Mefenamic acid
Enolic acid derivatives Piroxicam, Tenoxicam
Acetic acid derivatives Ketorolac, Indomethacin, Nabumetone
Phenylbutazone, Oxyphenbutazone,
Pyrazolone derivatives
Propyphenazone
Nimesulide, Diclofenac, Aceclofenac,
Preferential COX-2 inhibitors
Meloxicam, Etodolac
Selective COX-2 inhibitors Celecoxib, Etoricoxib, Parecoxib
Analgesic-antipyretics with poor Para-aminophenol
Paracetamol (Acetaminophen)
anti-inflammatory action derivative
Benzoxazocine derivative Nefopam

SALYCYLATES:

Carboxylic acid (-COOH): Causes


GIT irritation & ulceration

Phenolic –OH shifted to meta or


para position: Abolishes activity

• Halogen substitution on aromatic ring: ↑ Potency but ↑ Toxicity


• Aromatic substitution at 5th position: ↑ Anti-inflammatory activity (e.g., Diflunisal)

2 Medicinal Chemistry
.

IMPORTANT DRUGS:

3 Medicinal Chemistry
.

Important points to be noted:


❖ Celecoxib → Pyrazole ring, sulfonamide group
❖ Rafecoxib → Furan ring
❖ Parecoxib → Prodrug of Valdecoxib
❖ Nimesulide, Nabumetone → Preferential COX-2 inhibitor

4 Medicinal Chemistry

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