Ibuprofen for adults

Generic Name: Ibuprofen
Drug Class: Nonsteroidal Anti-inflammatory Drug (NSAID)
Therapeutic Class: Analgesic, Antipyretic, Anti-inflammatory
ATC Code: M01AE01
Regulatory Classification: Over-the-counter (OTC) for low-dose; prescription-only for higher doses or extended use
Common Brand Names: Advil, Motrin, Nurofen, Brufen, Midol, Calprofen (formulations may vary by region)

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Mechanism of Action

Ibuprofen is a non-selective inhibitor of cyclooxygenase enzymes (COX-1 and COX-2). By blocking COX activity, it reduces the formation of prostaglandins, which are responsible for pain, fever, and inflammation. COX-2 inhibition accounts for the therapeutic anti-inflammatory effects, whereas COX-1 inhibition is associated with adverse gastrointestinal (GI) and renal effects.

Therapeutic effects:

• Analgesic: Effective for mild to moderate pain

• Anti-inflammatory: Reduces inflammation in musculoskeletal and autoimmune conditions

• Antipyretic: Lowers elevated body temperature through hypothalamic regulation

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Approved Indications in Adults

1. Pain Management:

   • Headache (including tension-type and migraine)

   • Dental pain

   • Musculoskeletal pain (sprains, strains)

   • Menstrual pain (primary dysmenorrhea)

   • Postoperative pain

   • Back pain and neuralgia

2. Inflammatory Conditions:

   • Rheumatoid arthritis

   • Osteoarthritis

   • Ankylosing spondylitis

   • Gout (acute attacks)

   • Bursitis and tendonitis

3. Fever Reduction:

   • Management of fever in acute infections (e.g., cold, flu)

4. Other Uses (off-label or combination):

   • Patent ductus arteriosus in neonates (specialized setting)

   • As part of combination products (e.g., ibuprofen + lysine for migraine, ibuprofen + pseudoephedrine for cold symptoms)

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Pharmacokinetics

• Absorption: Rapid and complete from gastrointestinal tract

• Bioavailability: ~80–100%

• Peak Plasma Concentration: 1–2 hours post-dose

• Protein Binding: >98% to plasma albumin

• Metabolism: Hepatic via CYP2C9

• Half-life: 1.8–2.5 hours

• Elimination: Renal (as metabolites) and fecal (minor)

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Dosage and Administration

Over-the-Counter Use:

• 200–400 mg orally every 4–6 hours as needed

• Maximum OTC daily dose: 1200 mg/day

Prescription Use:

• 400–800 mg three or four times daily

• Maximum prescription dose: 3200 mg/day

Common Adult Regimens:

• Pain/Fever: 400 mg every 6 hours

• Osteoarthritis/Rheumatoid Arthritis: 600–800 mg three times daily (under medical supervision)

• Dysmenorrhea: Initial 400 mg, then 200–400 mg every 6 hours as needed

• Migraine (acute): 400–800 mg single dose

Administration Notes:

• Take with food or milk to reduce GI irritation

• Use lowest effective dose for the shortest duration

• Do not crush or chew extended-release formulations

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Contraindications

• Known hypersensitivity to ibuprofen or other NSAIDs

• History of NSAID-induced asthma, urticaria, or allergic reactions

• Active or history of gastrointestinal bleeding or peptic ulceration

• Severe hepatic impairment

• Severe renal impairment (GFR <30 mL/min)

• Severe heart failure (NYHA class IV)

• Third trimester of pregnancy

• Cerebrovascular bleeding or other active bleeding disorders

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Warnings and Precautions

Cardiovascular Risk:

• May increase risk of myocardial infarction (MI) and stroke, particularly with high doses or long-term use

• Avoid in patients with established cardiovascular disease unless absolutely necessary

Gastrointestinal Risk:

• Increases risk of bleeding, ulceration, and perforation, especially in elderly or those with prior ulcer history

• Consider gastroprotection (e.g., PPI) if used long-term or with aspirin

Renal Impairment:

• NSAIDs reduce renal perfusion via prostaglandin inhibition

• Monitor renal function in patients with CKD, heart failure, or dehydration

Hepatic Effects:

• Elevated liver enzymes reported; rare cases of severe liver injury

• Monitor ALT/AST in long-term users

Skin Reactions:

• Risk of serious, potentially fatal conditions such as Stevens-Johnson Syndrome (SJS), Toxic Epidermal Necrolysis (TEN)

Asthma:

• NSAIDs may trigger bronchospasm in aspirin-sensitive asthmatics

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Adverse Effects

Common (1–10%):

• Nausea

• Dyspepsia

• Diarrhea or constipation

• Headache

• Dizziness

• GI discomfort

Less Common to Rare (<1%):

• GI bleeding or ulceration

• Tinnitus

• Edema and hypertension

• Elevated liver enzymes

• Rash and pruritus

• Bronchospasm

• Renal impairment

• Hematological changes (anemia, thrombocytopenia)

Severe (rare):

• Anaphylaxis

• Acute renal failure

• Hepatitis

• SJS/TEN

• Aseptic meningitis (more common in autoimmune patients)

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Drug Interactions

Increased Risk of Bleeding:

• Anticoagulants: Warfarin, DOACs (e.g., apixaban)

• Antiplatelets: Aspirin, clopidogrel

• SSRIs/SNRIs: Sertraline, fluoxetine

Reduced Renal Function:

• ACE inhibitors/ARBs + diuretics: Triple whammy effect

• Ciclosporin, tacrolimus: Enhanced nephrotoxicity

Reduced Effectiveness:

• Antihypertensives: May blunt effects of ACEIs, ARBs, beta-blockers

Increased Serum Levels of:

• Methotrexate: Reduced clearance, increased toxicity

• Lithium: Increased levels, potential toxicity

Other Notes:

• NSAIDs interfere with aspirin's antiplatelet effect if taken concurrently

• Avoid alcohol due to additive GI toxicity risk

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Pregnancy and Lactation

Pregnancy:

• Category C (1st and 2nd trimesters), Category D (3rd trimester)

• Avoid in third trimester due to risk of premature ductus arteriosus closure and impaired labor

• Use only if clearly necessary during early pregnancy

Lactation:

• Small amounts excreted in breast milk

• Generally considered safe when used short-term at low doses

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Overdose and Management

Toxic Dose:

• ≥400 mg/kg may cause serious toxicity

• Mild symptoms at lower doses

Symptoms:

• Nausea, vomiting

• Abdominal pain

• Drowsiness, dizziness

• Nystagmus, ataxia

• Rare: seizures, renal failure, metabolic acidosis

Treatment:

• Supportive care

• Activated charcoal if <1 hour post ingestion

• Monitoring of renal function, electrolytes, acid-base status

• Hospitalization if dose >400 mg/kg or symptomatic

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Monitoring Recommendations

• Blood pressure (especially in hypertensive or elderly patients)

• Renal function (baseline and periodically in chronic users)

• Liver function (with prolonged therapy)

• Hemoglobin and hematocrit (in suspected GI blood loss)

• Symptoms of GI toxicity, especially in high-risk groups

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Comparative Notes

NSAID	GI Risk	CV Risk	Duration of Action	Anti-inflammatory Power
Ibuprofen	Moderate	Moderate	Short (~6 hours)	Mild-Moderate
Naproxen	Moderate	Lower than others	Long (~12 hours)	Moderate
Diclofenac	Higher	High	Moderate (~8 hours)	Strong
Celecoxib	Lower GI risk (COX-2 selective)	High	Long (~12 hours)	Moderate-Strong

Patient Counseling Points

• Take with food or milk to reduce stomach upset

• Avoid alcohol to minimize GI irritation

• Do not take other NSAIDs concurrently (e.g., naproxen, diclofenac)

• Do not exceed recommended daily dose

• Report symptoms like black stools, chest pain, shortness of breath, rash, or swelling

• Use only as needed for short durations unless prescribed

• Store at room temperature, away from heat and moisture

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Storage Conditions

• Store below 25°C

• Protect from light and moisture

• Keep out of reach of children