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Ibuprofen
Ibuprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID) primarily prescribed for the treatment of pain, inflammation, and fever. It is available over-the-counter (OTC) and by prescription, making it one of the most commonly used medications worldwide. Ibuprofen is known for its efficacy in managing mild to moderate pain and inflammation, but its use requires careful monitoring due to the risk of side effects, particularly gastrointestinal and cardiovascular complications. This article provides a detailed overview of ibuprofen, including its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names, referencing authoritative sources such as the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology
Ibuprofen exerts its therapeutic effects through its action on the cyclooxygenase (COX) enzymes. Its key mechanisms include:
- Inhibition of Cyclooxygenase (COX) Enzymes:
- Ibuprofen inhibits both COX-1 and COX-2 enzymes, which are involved in the synthesis of prostaglandins and thromboxanes.
- COX-1 is responsible for the production of prostaglandins that protect the gastric mucosa and regulate platelet function.
- COX-2 is induced during inflammation and is responsible for the production of prostaglandins that mediate pain, inflammation, and fever.
- Reduction of Prostaglandin Synthesis:
- By inhibiting COX enzymes, ibuprofen reduces the production of prostaglandins, leading to decreased inflammation, pain, and fever.
- Antipyretic Effects:
- Ibuprofen reduces fever by inhibiting prostaglandin synthesis in the hypothalamus, which regulates body temperature.
Ibuprofen is approved for a variety of clinical conditions, including:
- Pain Relief:
- Management of mild to moderate pain, such as headaches, dental pain, menstrual cramps, and musculoskeletal pain.
- Inflammation:
- Treatment of inflammatory conditions, such as rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.
- Fever:
- Reduction of fever in adults and children.
- Off-Label Uses:
- Management of patent ductus arteriosus (PDA) in premature infants.
- Adjunctive therapy for migraine headaches.
The dosage of ibuprofen varies depending on the indication, patient age, and formulation. The following dosing guidelines are based on the British National Formulary (BNF) and clinical pharmacology references:
- Adults:
- Pain and Inflammation: 400–600 mg three to four times daily, not exceeding 2400 mg daily.
- Fever: 200–400 mg every 4–6 hours as needed, not exceeding 1200 mg daily.
- Children:
- Pain and Fever: 5–10 mg/kg every 6–8 hours, not exceeding 40 mg/kg daily.
- Juvenile Idiopathic Arthritis: 30–40 mg/kg daily in divided doses, not exceeding 2400 mg daily.
Important Considerations:
- Ibuprofen is available in oral tablets, capsules, suspensions, and topical formulations.
- Dose adjustments may be necessary for patients with hepatic or renal impairment.
- Ibuprofen should be taken with food or milk to minimize gastrointestinal side effects.
Ibuprofen is generally well-tolerated, but it is associated with a range of side effects, some of which can be serious. Common side effects include:
- Gastrointestinal:
- Nausea, vomiting, dyspepsia, and abdominal pain.
- Gastric ulcers and gastrointestinal bleeding (rare but serious).
- Cardiovascular:
- Increased risk of myocardial infarction and stroke, particularly with long-term use or high doses.
- Renal:
- Acute kidney injury and interstitial nephritis (rare).
- Other:
- Headache, dizziness, and rash.
Serious Side Effects:
- Gastrointestinal Bleeding: Particularly in elderly patients or those with a history of peptic ulcer disease.
- Hypersensitivity Reactions: Stevens-Johnson syndrome (SJS) and anaphylaxis (rare).
- Hepatotoxicity: Elevated liver enzymes and, rarely, severe liver damage.
Ibuprofen requires careful monitoring and adherence to specific precautions to ensure patient safety:
- Gastrointestinal Risk:
- Use with caution in patients with a history of peptic ulcer disease or gastrointestinal bleeding. Consider concomitant use of a proton pump inhibitor (PPI) for gastroprotection.
- Cardiovascular Risk:
- Use with caution in patients with a history of cardiovascular disease. Regular monitoring of cardiovascular health is recommended.
- Renal Impairment:
- Use with caution in patients with impaired kidney function. Avoid use in severe renal impairment (CrCl <30 mL/min).
- Pregnancy and Lactation:
- Ibuprofen should be avoided during the third trimester of pregnancy due to the risk of premature closure of the ductus arteriosus. It is excreted in breast milk, so breastfeeding is generally not recommended.
- Elderly Patients:
- Lower doses may be required due to increased sensitivity to side effects, particularly gastrointestinal and renal.
Ibuprofen has a significant potential for drug interactions due to its effects on prostaglandin synthesis and metabolism. Key interactions include:
- Anticoagulants:
- Ibuprofen may enhance the anticoagulant effects of warfarin, increasing the risk of bleeding.
- Other NSAIDs:
- Concurrent use with other NSAIDs increases the risk of gastrointestinal side effects.
- Antihypertensives:
- Ibuprofen may reduce the efficacy of antihypertensive medications, such as ACE inhibitors and beta-blockers.
- Diuretics:
- Ibuprofen may reduce the diuretic and antihypertensive effects of diuretics.
- Lithium:
- Ibuprofen may increase lithium levels, increasing the risk of toxicity.
Ibuprofen is the generic name for this medication. It is marketed under various brand names, depending on the country and manufacturer. Some examples include:
- Advil (a well-known brand in the United States and other regions).
- Nurofen (a well-known brand in the United Kingdom and other regions).
- Ibuprofen Accord.
- Ibuprofen Mylan.
