Generic Name

Advil

Mechanism

• Ibuprofen competitively inhibits the cyclo‑oxygenase (COX) enzymes, primarily COX‑1 and COX‑2, which convert arachidonic acid to prostaglandins.
• By reducing prostaglandin production, it diminishes pain signaling, inhibits fever by acting on the hypothalamic thermoregulatory center, and reduces local inflammation and edema.
• The non‑selective inhibition explains both its therapeutic benefits and its gastrointestinal (GI) side‑effects.

Pharmacokinetics

• Absorption: Rapid oral absorption; peak plasma concentration occurs within 1–2 h.
• Bioavailability: ~80 % with food, reduced slightly with high‑fat meals.
• Distribution: Widely distributed; protein binding ~87 % (primarily to albumin).
• Metabolism: Primarily hepatic via CYP2C9 to inactive metabolites; minimal renal excretion of unchanged drug.
• Elimination: Half‑life ~2 – 3 h; clear by the kidneys.
• Drug interactions: Inhibits CYP2C9, can increase levels of warfarin, methotrexate, and other NSAIDs.

Indications

• Analgesia: Mild‑to‑moderate pain (headache, dental pain, musculoskeletal pain).
• Anti‑inflammation: Rheumatoid arthritis, osteoarthritis, gouty arthritis.
• Antipyresis: Febrile illnesses including viral infections.
• Pre‑operative analgesia to reduce opioid requirement.

Contraindications

• Absolute Contraindications: Known hypersensitivity to ibuprofen or other NSAIDs; active peptic ulcer disease or GI bleeding; severe hepatic impairment.
• Relative Contraindications:
• *Pregnancy* – use only in the third trimester for pain control; avoid in first and second trimesters.
• *Cardiovascular disease* – increased risk of hypertension and water‑retention.
• *Renal impairment* – dosage adjustment may be needed.
• Warnings:
• Long‑term use (>10 days) raises GI, renal, and cardiovascular risks.
• Concurrent use with anticoagulants amplifies bleeding risk.

Dosing

• Route: Oral (tablet, capsule, suspension); intravenous is used in hospital settings for severe pain.

Adverse Effects

• Common (≥ 1 %):
• Gastrointestinal upset (nausea, dyspepsia)
• Headache, dizziness
• Rash, pruritus
• Mild elevation of liver enzymes
• Serious (≤ 0.1 %):
• Upper GI bleeding, perforation
• Renal failure/chronic kidney disease exacerbation
• Hypersensitivity reactions (angioedema, anaphylaxis)
• Cardiovascular events (hypertension, edema, MI risk escalation)

Monitoring

• Baseline labs: CBC, renal function tests (serum creatinine, BUN), liver enzymes.
• Periodic assessment:
• Check renal function monthly if used > 2 weeks.
• Monitor blood pressure and edema.
• Assess for GI symptoms or bleeding.

Clinical Pearls

1. IBU → U & B:
• For patients at high GI risk, co‑prescribe *proton‑pump inhibitors* or *misoprostol*.

2. Short‑term only:
• Keep therapy ≤ 10 days for acute pain to minimize GI bleeding risk; for chronic arthritis, prescribe the lowest effective dose.

3. Weilard Effect:
• Use with caution in patients on anticoagulants; consider use of *paracetamol* (acetaminophen) as first‑line alternative if risk high.

4. Pediatric dosing:
• Weight‑based dosing is crucial; avoid exceeding 10 mg/kg/day in children 6–12 y.

5. Pregnancy cautious:
• Use only in third trimester for maternal comfort; avoid otherwise.

This Advil drug card provides essential pharmacology facts—mechanism, PK, indications, contraindications, dosing, side‑effects, and practice pearls—tailored for medical students, clinicians, and pharmacists seeking quick reference.