1. Clinical Overview
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) belonging to the propionic acid derivative class. It is a widely used, non-selective inhibitor of cyclooxygenase (COX) enzymes, providing analgesic, anti-inflammatory, and antipyretic effects. In the Indian market, it is one of the most commonly used over-the-counter and prescription medications for mild to moderate pain and fever.
| Onset | Duration | Bioavailability |
|---|---|---|
| Oral: 30-60 minutes for analgesic effect; 1-2 hours for peak anti-inflammatory effect. | Approximately 4-6 hours. | >80% |
2. Mechanism of Action
Ibuprofen exerts its therapeutic effects by non-selectively inhibiting the enzyme cyclooxygenase (COX), specifically the COX-1 and COX-2 isoforms. This inhibition blocks the conversion of arachidonic acid to prostaglandin G2 (PGG2) and subsequently to prostaglandin H2 (PGH2), the precursor for various prostanoids including prostaglandins (PGs), prostacyclin, and thromboxanes.
3. Indications & Uses
- Mild to moderate pain (e.g., headache, dental pain, dysmenorrhea)
- Fever (pyrexia)
- Inflammatory conditions (e.g., rheumatoid arthritis, osteoarthritis, ankylosing spondylitis)
4. Dosage & Administration
Adult Dosage: Analgesia/Antipyresis: 200-400 mg every 4-6 hours as needed. Do not exceed 1200 mg per day for OTC use. For inflammatory conditions (under medical supervision): 1200-2400 mg daily in 3-4 divided doses (max 3200 mg/day).
Administration: Take with food, milk, or a full glass of water to minimize gastric irritation. Do not crush or chew sustained-release formulations. Swallow tablet/capsule whole. For rapid onset, take on an empty stomach, but this increases GI upset risk.
5. Side Effects
Common side effects may include:
- Dyspepsia (indigestion, heartburn)
- Nausea
- Epigastric pain
- Headache
- Dizziness
- Rash
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Aspirin (low-dose) | Ibuprofen may antagonize the antiplatelet effect of aspirin. Reduced cardioprotection. | Major |
| Other NSAIDs (e.g., Diclofenac, Naproxen) | Increased risk of GI toxicity and renal impairment. No therapeutic advantage. | Major |
| Anticoagulants (Warfarin, NOACs) | Increased risk of bleeding due to antiplatelet effect and potential GI ulceration. | Major |
| Corticosteroids (e.g., Prednisolone) | Synergistic increase in risk of GI ulceration and bleeding. | Major |
| ACE Inhibitors (e.g., Ramipril) / ARBs (e.g., Telmisartan) | Reduced antihypertensive efficacy; increased risk of renal impairment. | Moderate |
| Diuretics (e.g., Furosemide, Hydrochlorothiazide) | Reduced diuretic and antihypertensive efficacy; risk of renal failure. | Moderate |
| Lithium | Decreased renal clearance of lithium, leading to increased serum levels and toxicity. | Major |
| Methotrexate (high-dose) | May decrease renal clearance of methotrexate, increasing toxicity risk. | Major |
| SSRIs (e.g., Sertraline, Escitalopram) | Increased risk of upper GI bleeding. | Moderate |
| Cyclosporine, Tacrolimus | Increased risk of nephrotoxicity. | Major |
7. Patient Counselling
- DO take with food or milk to reduce stomach upset.
- DO use the lowest effective dose for the shortest possible time.
- DO inform your doctor about all other medicines you are taking, including OTC drugs and supplements.
- DO stay well-hydrated, especially during prolonged use.
- DON'T take with alcohol.
- DON'T take other NSAIDs (like aspirin, diclofenac) concurrently unless directed by a doctor.
- DON'T crush or chew sustained-release tablets.
- DON'T use for more than 3 days for fever or 10 days for pain without consulting a doctor.
8. Toxicology & Storage
Overdose: Nausea, vomiting, epigastric pain, lethargy, drowsiness, headache, tinnitus, nystagmus, blurred vision. Severe overdose (>400 mg/kg in adults) can lead to metabolic acidosis, coma, seizures, acute renal failure, apnea, and cardiovascular collapse.
Storage: Store below 30°C (86°F) in a cool, dry place, protected from light and moisture. Keep out of reach of children. Do not use after the expiry date printed on the pack.