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NSAIDS

NSAIDs, or non-steroidal anti-inflammatory drugs, are classified into nonselective COX inhibitors, preferential COX-2 inhibitors, selective COX-2 inhibitors, and analgesic-antipyretics, each with distinct mechanisms and uses. They primarily work by inhibiting cyclooxygenase (COX) enzymes, leading to reduced pain, fever, and inflammation, but can have adverse effects such as gastrointestinal irritation and renal issues. Key examples include aspirin, ibuprofen, and celecoxib, with specific pharmacokinetics and therapeutic applications.

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3 views10 pages

NSAIDS

NSAIDs, or non-steroidal anti-inflammatory drugs, are classified into nonselective COX inhibitors, preferential COX-2 inhibitors, selective COX-2 inhibitors, and analgesic-antipyretics, each with distinct mechanisms and uses. They primarily work by inhibiting cyclooxygenase (COX) enzymes, leading to reduced pain, fever, and inflammation, but can have adverse effects such as gastrointestinal irritation and renal issues. Key examples include aspirin, ibuprofen, and celecoxib, with specific pharmacokinetics and therapeutic applications.

Uploaded by

sakshi21524
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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NSAIDS

1. Definition
 NSAIDs = Non-steroidal anti-inflammatory drugs
 Actions:
o Analgesic

o Antipyretic

o Anti-inflammatory

 Mechanism:
👉 Inhibit cyclooxygenase (COX) → ↓ Prostaglandin synthesis

🔹 2. Classification (VERY IMPORTANT – 5 MARKS ⭐)


A. Nonselective COX inhibitors
 Salicylates → Aspirin
 Propionic acid → Ibuprofen, Naproxen
 Fenamates → Mefenamic acid
 Enolic acid (Oxicams) → Piroxicam
 Acetic acid → Indomethacin, Diclofenac

B. Preferential COX-2 inhibitors


 Diclofenac
 Nimesulide
 Meloxicam

C. Selective COX-2 inhibitors


 Celecoxib
 Etoricoxib

D. Analgesic-antipyretic (poor anti-inflammatory)


 Paracetamol

🔹 3. Mechanism of Action ⭐
 Arachidonic acid → COX → Prostaglandins
 NSAIDs:
o Block COX enzyme

o ↓ PGs → ↓ pain, fever, inflammation

👉 Aspirin:
 Irreversible COX inhibition
Others:
 Reversible inhibition

🔹 4. Pharmacological Actions
1. Analgesic
 Mild–moderate pain
 ↓ PG-mediated pain sensitization
2. Antipyretic
 ↓ hypothalamic PGE2 → ↓ fever
3. Anti-inflammatory
 ↓ vasodilation + edema
4. Antiplatelet (ONLY Aspirin)
 ↓ TXA2 → ↓ platelet aggregation

🔹 5. Pharmacokinetics (WRITE ONLY THIS IN EXAM)


 Route: Oral (most), some IM/IV
 Protein binding: Highly protein bound
 Metabolism: Liver
 Excretion: Kidney
 Half-life:
o Short → Ibuprofen

o Long → Piroxicam

🔹 6. Adverse Effects ⭐
GIT
 Gastritis
 Peptic ulcer
Kidney
 Salt & water retention
 ↓ renal function
Blood
 Bleeding (Aspirin)
Others
 Hypersensitivity
 Bronchospasm (aspirin asthma)

🔹 7. Therapeutic Uses
 Pain (headache, muscle pain)
 Fever
 Inflammation (arthritis)
 Dysmenorrhea
 Migraine

🔹 8. Important Extra Points (HIGH-YIELD)


 COX-1 → Physiological (gastric protection)
 COX-2 → Inflammation
👉 So:
 Nonselective NSAIDs → more gastric side effects
 COX-2 selective → less gastric damage

A. NONSELECTIVE COX INHIBITORS

🔹 1. ASPIRIN
Class: Salicylate
Mechanism:
 Irreversibly inhibits COX-1 & COX-2
 ↓ Prostaglandins (pain, fever, inflammation)
 ↓ TXA2 → ↓ platelet aggregation
Pharmacokinetics:
 Route: Oral
 Protein binding: High (~90%)
 Metabolism: Liver (to salicylate)
 Excretion: Kidney
 Half-life:
o Low dose: 3–6 hrs

o High dose: up to 15 hrs

Uses:
 Analgesic
 Antipyretic
 Anti-inflammatory
 Antiplatelet (low dose)
Adverse effects:
 Gastritis, ulcer
 Bleeding
 Tinnitus (salicylism)
 Metabolic acidosis (high dose)
⭐ Special:
 ONLY NSAID with irreversible action
 Causes Reye’s syndrome (children)

🔹 2. IBUPROFEN
Class: Propionic acid
Mechanism:
 Reversible COX inhibitor
Pharmacokinetics:
 Oral
 High protein binding
 Hepatic metabolism
 Half-life: ~2 hrs
Uses:
 Fever
 Mild–moderate pain
 Arthritis
Adverse effects:
 Mild gastric irritation
⭐ Special:
 Safest NSAID

🔹 3. NAPROXEN
Pharmacokinetics:
 Oral
 Half-life: ~12–15 hrs
Uses:
 Arthritis
 Musculoskeletal pain
⭐ Special:
 Long acting → BD dosing

🔹 4. KETOPROFEN
PK:
 Half-life: ~2–4 hrs
Uses:
 Pain, inflammation
⭐ Special:
 Strong anti-inflammatory

🔹 5. FLURBIPROFEN
Uses:
 Dental pain
 Inflammation

🔹 6. MEFENAMIC ACID
Class: Fenamate
PK:
 Half-life: ~2–4 hrs
Uses:
 Dysmenorrhea
Adverse:
 Diarrhea
⭐ Special:
 Best for menstrual pain

🔹 7. PIROXICAM
Class: Oxicam
PK:
 Half-life: ~45–50 hrs
Uses:
 Rheumatoid arthritis
Adverse:
 High gastric toxicity
⭐ Special:
 Once daily drug

🔹 8. TENOXICAM
PK:
 Half-life: ~60–70 hrs
⭐ Special:
 Very long acting

🔹 9. INDOMETHACIN
PK:
 Half-life: ~4–5 hrs
Uses:
 Rheumatoid arthritis
 Acute gout
 PDA closure
Adverse:
 Severe gastric irritation
 Headache, dizziness
⭐ Special:
 Most potent NSAID
 Used in Patent ductus arteriosus

🔹 10. DICLOFENAC
PK:
 Half-life: ~1–2 hrs
Uses:
 Arthritis
 Pain
⭐ Special:
 Very widely used
 Slight COX-2 preference

🔹 11. KETOROLAC
PK:
 Half-life: ~5–6 hrs
Uses:
 Severe acute pain (post-op)
⭐ Special:
 Strong analgesic (opioid alternative)

🔹 12. NABUMETONE
PK:
 Prodrug
 Half-life: ~24 hrs
⭐ Special:
 Less gastric toxicity

🔷 B. PREFERENTIAL COX-2 INHIBITORS

🔹 1. NIMESULIDE
PK:
 Half-life: ~2–5 hrs
Uses:
 Pain, fever
Adverse:
 Hepatotoxicity
⭐ Special:
 Restricted drug

🔹 2. ACECLOFENAC
PK:
 Half-life: ~4 hrs
⭐ Special:
 Better tolerated than diclofenac

🔹 3. MELOXICAM
PK:
 Half-life: ~20 hrs
Uses:
 Arthritis
⭐ Special:
 Less gastric damage

🔹 4. ETODOLAC
PK:
 Half-life: ~6–7 hrs
⭐ Special:
 Safer on stomach

🔹 5. DICLOFENAC
(Already covered)

🔷 C. SELECTIVE COX-2 INHIBITORS

🔹 1. CELECOXIB
PK:
 Half-life: ~11 hrs
Uses:
 Arthritis
⭐ Special:
 Less gastric ulcer

🔹 2. ETORICOXIB
PK:
 Half-life: ~22 hrs
⭐ Special:
 Highly COX-2 selective

🔹 3. PARECOXIB
PK:
 Injectable prodrug
⭐ Special:
 Used IV/IM

⚠️Class adverse effects:


 ↑ Risk of MI, stroke (thrombosis)

🔷 D. ANALGESIC-ANTIPYRETICS
🔹 1. PARACETAMOL
Mechanism:
 Central COX inhibition
PK:
 Oral
 Half-life: ~2–3 hrs
 Liver metabolism
Uses:
 Fever
 Mild pain
Adverse:
 Hepatotoxicity (overdose)
⭐ Special:
 No anti-inflammatory action
 Safest in pregnancy & children

🔹 2. METAMIZOLE (DIPYRONE)
Uses:
 Pain, fever
Adverse:
 Agranulocytosis
⭐ Special:
 Banned in many countries

🔹 3. NEFOPAM
Mechanism:
 Central analgesic (non-opioid)
Uses:
 Moderate pain
⭐ Special:
 No respiratory depression

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