Motrin

Motrin

Generic Name

Motrin

Mechanism

  • Selective, reversible inhibition of cyclo‑oxygenase (COX) – primarily COX‑1 and COX‑2 enzymes, reducing prostaglandin synthesis.
  • Decreases prostaglandin‑dependent vasodilation, vascular permeability, and nociceptor sensitization, thereby alleviating pain, lowering fever, and dampening swelling.
  • Inhibits platelet aggregation by blocking thromboxane A₂ formation, leading to modest antiplatelet effects.

Pharmacokinetics

  • Absorption: Rapid oral uptake; peak plasma concentrations 1–2 h after dosing.
  • Bioavailability: 50–70 % (food reduces peak level by ~20 %).
  • Distribution: Highly protein‑bound (~98 %).
  • Metabolism: Hepatic via CYP2C9 and CYP3A4 to inactive metabolites.
  • Elimination: 90 % renal (≈80 % as glucuronide conjugates); half‑life ≈2 h (shorter in young adults, longer in elderly).
  • Drug interactions: CYP3A4 inducers (e.g., rifampin) decrease plasma ibuprofen; CYP2C9 inhibitors (e.g., fluconazole) increase exposure.

Indications

  • Mild to moderate musculoskeletal pain (e.g., osteoarthritis, acute injury).
  • Meningitis‑related headache (followed by antibiotic therapy).
  • Dental pain post‑extraction.
  • Premenstrual syndrome symptomatic relief.
  • Management of febrile illnesses in children > 6 months.
  • CEST for short‑term rheumatologic and inflammatory disorders.

Contraindications

  • Known hypersensitivity to ibuprofen or other NSAIDs.
  • Active peptic ulcer or GI bleeding.
  • Severe hepatic or renal impairment (use with caution).
  • Pregnancy: third trimester contraindicated; first trimester discouraged.
  • Cardiovascular disease: increased risk of ischemic events with long‑term use.
  • Use caution in asthma patients (possible bronchospasm).
  • Children under 6 months: contraindicated.

Dosing

  • Adults: 200‑400 mg PO q6‑8 h PRN. Do not exceed 1200 mg/24 h (or 2400 mg/24 h with physician supervision).
  • Elderly: Initiate at lower doses (200 mg PO q8 h) due to reduced clearance.
  • Children (≥6 mo): 5‑10 mg/kg PO every 6‑8 h; maximum 40 mg/kg/24 h.
  • Extended‑release formulations (e.g., Motrin® XR) offer 24‑h dosing for chronic pain.
  • Take with food or a full glass of water to minimize GI irritation.

Adverse Effects

Common (≥5 %)
• Gastro‑intestinal upset (nausea, dyspepsia, belching)
• Headache, dizziness
• Mild rash or pruritus

Serious (≤1 %)
• Upper GI bleeding, ulcer perforation
• Renal impairment (acute tubular necrosis, oliguria)
• Hepatic dysfunction (ALT/AST ↑)
• Hypersensitivity reactions (angioedema, anaphylaxis)
• Cardiac events (hypertension, myocardial infarction, congestive heart failure)

Monitoring

  • Baseline: CBC, CMP, urinalysis, BP, eGFR.
  • Periodic: eGFR every 3–6 months in >65 yr or CKD pts; monitor hemoglobin/hematocrit for bleeding.
  • Liver enzymes if symptoms of hepatotoxicity (jaundice, malaise).
  • Blood pressure monthly if on long‑term therapy.

Clinical Pearls

  • “Trojan‐horse” for locale pain: ibuprofen’s ability to cross the blood‑brain barrier makes it effective for headaches and osteoarthritic joint pain.
  • Avoid rotavirus‑infected children if pubertal; risk of intussusception is >100× higher.
  • COX‑7 ocular (rare) side‑effects: solitary cases of well‑tolerated eye irritation; not dose‑related.
  • Combine with antacids (e.g., ranitidine) only if concomitant aspirin therapy is required; otherwise use PPI for high‑risk patients.
  • Drug‑drug caution: Concomitant use of Angiotensin‑Converting Enzyme inhibitors on a low dose of ibuprofen can worsen renal function; reduce ACE inhibitor dose or monitor SID.
  • Therapeutic drug monitoring: For patients with CYP2C9 polymorphisms (e.g., *3 allele) consider lower dosing due to slower metabolism.
  • Follow‑up: At 2‑4 weeks after initiating therapy to assess pain relief and check for GI symptoms.

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• *Prepared by the Pharmacology Reference Team. All data are up to date as of 2026 and based on peer‑reviewed literature.*

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Medical Disclaimer: Medical definitions are provided for educational purposes and should not replace professional medical advice, diagnosis, or treatment.

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