NSAIDs
NSAIDs
Introduction
Illustrated mechanism of action
Examples of Medication Brand Names (with Images)
Indication
Side Effects
Precautions & Contraindications
Monographs
Reference
NSAIDS
Introduction
NSAIDs, or Non-Steroidal Anti-Inflammatory Drugs, are a widely used group of medications that help relieve pain, reduce inflammation, and lower fever. They are commonly prescribed as well as available over-the-counter for conditions such as headaches, menstrual cramps, muscle pain, arthritis, and fever. Unlike corticosteroids, NSAIDs do not contain steroid components, making them preferable for many patients in need of anti-inflammatory treatment. Their primary mechanism of action involves the inhibition of cyclooxygenase enzymes (COX-1 and COX-2), which play a crucial role in the production of prostaglandins—substances responsible for causing inflammation, pain, and fever in the body. By reducing prostaglandin levels, NSAIDs help manage a variety of painful and inflammatory conditions. However, long-term or inappropriate use of NSAIDs can lead to side effects such as gastrointestinal irritation, ulcers, kidney problems, increased bleeding tendency, and cardiovascular risks. Despite these potential drawbacks, NSAIDs remain an essential and effective option in the management of pain and inflammation when used appropriately under medical guidance.
Illustrated mechanism of action
NSAIDs exert their therapeutic effects primarily by inhibiting cyclooxygenase (COX) enzymes, which play a central role in the biosynthesis of prostaglandins from arachidonic acid.
1. Arachidonic Acid Pathway:
• When cells are damaged due to injury or infection, phospholipase A2 is activated and releases arachidonic acid from membrane phospholipids.
• Arachidonic acid serves as the substrate for COX enzymes to produce prostaglandins, prostacyclins, and thromboxanes.
2. COX Enzymes:
• There are two main isoforms of the COX enzyme:
• COX-1: Constitutively expressed in most tissues; involved in maintaining gastric mucosal integrity, renal blood flow, and platelet aggregation.
• COX-2: Inducible and primarily expressed at sites of inflammation; responsible for the synthesis of pro-inflammatory prostaglandins.
3. NSAID Action:
• NSAIDs non-selectively inhibit COX-1 and COX-2 (e.g., ibuprofen, naproxen), or selectively inhibit COX-2 (e.g., celecoxib).
• This inhibition results in:
• Reduced prostaglandin synthesis, leading to:
• Decreased inflammation
• Reduced pain sensitivity (analgesic effect)
• Lowered fever (antipyretic effect)
4. Clinical Benefits and Risks:
• Therapeutic Effects: Anti-inflammatory, analgesic, and antipyretic.
• Adverse Effects (mostly due to COX-1 inhibition):
• Gastric ulcers and GI bleeding
• Impaired renal function
• Increased risk of cardiovascular events (especially with selective COX-2 inhibitors)
Examples of Medication Brand Name
Dispercam
Brufen
Diclac-N
Cataflam
Coxritor
Ambezin
Aneselacox
Melocam
Etodolac
Myoprox
Ketolac
Celebrex
Indocid
Sulindac oshar
Indication
Indications for NSAIDs (Non-Steroidal Anti-Inflammatory Drugs):
1. Pain Relief (Analgesia):
• Mild to moderate pain relief (headaches, toothaches, etc.)
• Post-surgical pain
• Musculoskeletal pain (e.g., back pain, strains, sprains)
• Pain due to injury or trauma
2. Inflammatory Conditions:
• Osteoarthritis (degenerative joint disease)
• Rheumatoid arthritis (autoimmune disorder affecting joints)
• Gout (pain and inflammation caused by high uric acid levels)
• Ankylosing spondylitis (inflammatory arthritis affecting the spine)
3. Fever Reduction (Antipyretic):
• Common cold, flu, or other febrile illnesses
• Post-vaccination fever in children or adults
4. Menstrual Pain (Dysmenorrhea):
• Relief of primary dysmenorrhea (painful menstruation)
5. Muscle and Joint Inflammation:
• Conditions like bursitis (inflammation of the bursa) or tendinitis (inflammation of tendons)
6. Post-traumatic and Post-surgical Inflammation:
• Inflammation and swelling after surgery, trauma, or injury
7. Acute Migraines:
• Relief from acute migraine attacks (especially with medications like ibuprofen or naproxen)
8. Dental Pain:
• Pain management following dental procedures or toothaches
9. Postpartum Pain Relief:
• Relief from pain after childbirth.
Side Effect
1. Gastrointestinal (GI) Side Effects:
• Nausea, vomiting
• Dyspepsia (indigestion)
• Gastric or duodenal ulcers
• GI bleeding or perforation (can be life-threatening)
2. Renal (Kidney) Effects:
• Reduced renal perfusion and glomerular filtration rate (GFR)
• Acute kidney injury (especially in dehydrated or elderly patients)
• Electrolyte imbalances (e.g., hyperkalemia, sodium retention)
3. Cardiovascular Risks:
• Hypertension
• Increased risk of myocardial infarction (heart attack)
• Increased risk of stroke
• Fluid retention and edema
4. Hematologic Effects:
• Inhibition of platelet aggregation (especially with non-selective NSAIDs like aspirin)
• Increased bleeding tendency
5. Hypersensitivity Reactions:
• Rashes, urticaria (hives)
• Anaphylaxis (rare)
• NSAID-exacerbated respiratory disease (asthma flare-ups)
6. Hepatic (Liver) Effects:
• Elevated liver enzymes
• Rare cases of hepatitis or liver failure
7. Central Nervous System (Less Common):
• Headache
• Dizziness
• Tinnitus (especially with high-dose aspirin)
Precautions & Contraindications
Precautions for NSAIDs:
1. Use cautiously in patients with gastrointestinal issues.
2. Monitor kidney function in patients with renal impairment.
3. Caution in patients with cardiovascular conditions.
4. Use with caution in patients with liver disease.
5. Asthmatic patients may experience worsened symptoms.
6. Monitor blood pressure in patients with hypertension.
7. Avoid in the third trimester of pregnancy.
8. Use cautiously in elderly patients.
Contraindications for NSAIDs:
1. Contraindicated in active peptic ulcers.
2. Contraindicated in severe renal impairment.
3. Contraindicated in active bleeding.
4. Contraindicated in patients with NSAID hypersensitivity.
5. Contraindicated in severe heart failure.
6. Contraindicated in the third trimester of pregnancy.
7. Contraindicated in active liver disease.
Monographs
https://www.nhs.uk/conditions/nsaids/
https://www.healthline.com/health/side-effects-from-nsaids
https://www.nhs.uk/medicines/ibuprofen-for-adults/who-can-and-cannot-take-ibuprofen/
https://www.ncbi.nlm.nih.gov/books/NBK548614/?utm_source=chatgpt.com
https://pmc.ncbi.nlm.nih.gov/articles/PMC7347500/?utm_source=chatgpt.com
https://search.app/TNmcSoyNwhLvC9LZ8
https://search.app/vdcS6HSc21gqKz5AA
https://search.app/RB7b8LTSmFPnnta17
https://search.app/KgibepcyLP7FReMG9