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Ibuprofen Data - Uses, Dosage, Drug class, Brand name, Warnings, etc



Pharmacology Ibuprofen is an NSAID with analgesic and antipyretic properties. It is a nonselective inhibitor of cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) and reversibly alters platelet function and prolongs bleeding time.
Administration and Adult Dosage - PO for mild to moderate pain: 400 mg every 4–6 hr as needed
- PO for primary dysmenorrhea: 400 mg every 4 hr as needed
- PO for rheumatoid arthritis and osteoarthritis: 400–800 mg 3–4 times daily, to a maximum of 3.2 g/day
Special Populations - Pediatric Dosage - PO for fever (6 months–12 yr):
    • 5 mg/kg for fever <102.5°F or 10 mg/kg for fever >102.5°F every 6–8 hr, to a maximum of 40 mg/kg/day
- PO for pain (6 months–12 yr): 10 mg/kg every 6–8 hr as needed, to a maximum of 40 mg/kg/day
- PO for juvenile arthritis: 30–40 mg/kg/day in 3–4 divided doses; 20 mg/kg/day for milder disease
Special Populations - Geriatric Dosage Use minimal effective dosages; elderly are more susceptible to GI bleeding and acute renal insufficiency.
Dosage Forms - Capsule: 200, 400 mg
- Chewable Tablet: 50, 100 mg
- Tablet: 100, 200, 400, 600, 800 mg
- Drops: 40 mg/mL
- Suspension: 20, 40 mg/mL
Patient Instructions - Take with food, milk, or antacid to minimize stomach upset
- Report symptoms of gastrointestinal ulceration or bleeding, skin rash, weight gain, or edema
- Dizziness may occur; use caution until the extent of this effect is known
Missed Doses - If taken on a regular schedule, take a missed dose as soon as remembered
- If near the time for the next dose, take that dose only; do not double the dose or take extra
Pharmacokinetics - Serum Levels - Antipyretic effect: 10 mg/L (48 µmol/L)
- Toxicity (acute overdose): >200 mg/L (971 µmol/L) 1 hr post-ingestion may be associated with severe toxicity (apnea, metabolic acidosis, coma)
Pharmacokinetics - Fate - Absorption: Rapidly absorbed from the GI tract; bioavailability >80%
- Peak Serum Levels (children):
    • 5 mg/kg: 17–42 mg/L (82–204 µmol/L) in 1.1 ± 0.3 hr
    • 10 mg/kg: 25–53 mg/L (121–257 µmol/L) in 1.1 ± 0.3 hr
- Protein Binding: >99%
- Metabolism: To at least 2 inactive metabolites
- Distribution: Vd = 0.15 ± 0.02 L/kg, increased in cystic fibrosis
- Clearance: Cl = 0.045 ± 0.012 L/hr/kg, increased in cystic fibrosis
- Excretion: <1% unchanged in urine
Pharmacokinetics - t¹⁄₂ - Elimination half-life: 2 ± 0.5 hr
Adverse Reactions & Side Effects Occasional:
- Gastric distress, blood loss, diarrhea, vomiting, dizziness, skin rash
- GI ulceration (higher risk in elderly and with higher dosages)
- Fluid retention
Other:
- Renal dysfunction, particularly in pre-existing renal disease, CHF, or cirrhosis
Rare:
- Slight rise in bleeding time, elevated liver enzymes, lymphopenia, agranulocytosis, aplastic anemia, aseptic meningitis
Contraindications - Syndrome of nasal polyps
- Angioedema
- Bronchospastic reactivity to aspirin or other NSAIDs
Precautions & Warnings - Avoid during pregnancy
- Use with caution in patients with pre-existing renal disease, CHF, cirrhosis, history of ulcer disease or bleeding, or risk factors for peptic ulcer disease (e.g., advanced age)
Drug Interactions - May inhibit antihypertensive response to ACE inhibitors, beta-blockers, diuretics, and hydralazine
- May inhibit natriuretic effect of diuretics
- Possible GI bleeding and antiplatelet effect increase bleeding risk during anticoagulant therapy
- May decrease renal lithium clearance
- Some NSAIDs (e.g., indomethacin, ketoprofen) reduce methotrexate clearance
- NSAIDs may reduce renal function
Parameters to Monitor - Monitor for blood loss, weight gain, and renal function during long-term use
Class and Drug Brand Name - Class: Analgesic and Anti-Inflammatory Drugs
- Brand Names: Advil, Motrin, Nuprin, Various
Notes - Misoprostol is effective in preventing NSAID-associated GI ulceration
- H2-receptor antagonists prevent duodenal but not gastric ulcerations and may mask symptoms of NSAID-induced GI ulceration
- Proton-pump inhibitors (e.g., omeprazole) are effective in treating NSAID-related dyspepsia and preventing NSAID-induced ulcers
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