Pronunciation: EYE-bue-PROE-fen
Class: NSAID

Trade Names

Advil
- Tablets 200 mg

Advil Liqui-Gels
- Capsules 200 mg

Advil Migraine
- Capsules 200 mg

Caldolor
- Injection, solution 100 mg/mL

Children's Advil
- Suspension 100 mg per 5 mL

Children's Motrin
- Tablets, chewable 50 mg
- Suspension, oral 100 mg per 5 mL

Ibuprofen
- Capsules 200 mg
- Tablets 200 mg
- Tablets 400 mg
- Tablets 600 mg
- Tablets 800 mg
- Tablets, chewable 100 mg

Ibutab
- Tablets 200 mg

Infant's Motrin
- Drops, oral 40 mg/mL

Junior Strength Motrin
- Tablets 100 mg
- Tablets, chewable 100 mg

Motrin Migraine Pain
- Tablets 200 mg

PediaCare Fever
- Suspension, oral 100 mg per 5 mL
- Drops, oral 40 mg/mL

Pediatric Advil Drops
- Suspension, oral 100 mg per 2.5 mL

Apo-Ibuprofen (Canada)
Apo-Ibuprofen Prescription (Canada)
Motrin IB Extra Strength (Canada)
Motrin IB Super Strength (Canada)

Pharmacology

Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

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Pharmacokinetics

Absorption

T _max is 1 to 2 h (oral). Bioavailability is less than 80% (oral). C _max is 39.2 mcg/mL and 72.6 mcg/mL for a 400 and 800 mg IV dose, respectively.

Distribution

Highly protein bound.

Elimination

Plasma half-life is 1.8 to 2 h (oral) and 2.22 to 2.44 h (IV). 45% to 79% is eliminated through the urine (oral). Cl is 3 to 35 L/h (oral).

Indications and Usage

IV : In adults for the management of mild to moderate pain and as an adjunct to opioid analgesics in the management of moderate to severe pain. PO : Relief of signs and symptoms of rheumatoid arthritis and osteoarthritis, mild to moderate pain, primary dysmenorrhea, reduction of fever, migraine.

Contraindications

Treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery; patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; hypersensitivity to any component of the product.

Dosage and Administration

Fever Reduction
Adults

IV 400 mg followed by 400 mg every 4 to 6 h or 100 to 200 mg every 4 h as necessary (max, 3,200 mg/day).

Children 1 to 12 y of age

PO : 39.2°C (102.5°F) and less, recommended dose 5 mg/kg; more than 39.2°C (102.5°F), recommended dose 10 mg/kg; max daily dose 40 mg/kg.

Mild to Moderate Pain
Adults

PO 400 mg every 4 to 6 h as needed. IV 400 to 800 mg every 6 h as necessary (max, 3,200 mg/day).

Primary Dysmenorrhea
Adults

PO 400 mg every 4 h as needed.

Rheumatoid Arthritis and Osteoarthritis
Adults

PO 300 to 800 mg 3 to 4 times daily, not to exceed 3.2 g/day.

OTC Use (Minor Aches/Pains, Dysmenorrhea, Fever Reduction)

PO 200 mg every 4 to 6 h. Do not exceed 1.2 g in 24 h or take for pain for more than 10 days or for fever for more than 3 days. Use smallest effective dose.

OTC Use (Migraine)
Adults

PO 400 mg with a glass of water. Advise patient to contact health care provider if symptoms persist or worsen . Do not exceed 400 mg in 24 h or for longer than 10 days.

OTC Use (Children)

PO If possible, use weight to dose; otherwise, use age. May repeat dose every 6 to 8 h. Do not use more than 4 times per day.

• Children 12 to 17 lb or 6 to 11 mo of age, give 50 mg.
• Children 18 to 23 lb or 12 to 23 mo of age, give 75 mg.
• Children 24 to 35 lb or 2 to 3 y of age, give 100 mg.
• Children 36 to 47 lb or 4 to 5 y of age, give 150 mg.
• Children 48 to 59 lb or 6 to 8 y of age, give 200 mg.
• Children 60 to 71 lb or 9 to 10 y of age, give 250 mg.
• Children 72 to 95 lb or 11 y of age, give 300 mg.

General Advice

• Injection
• For IV administration only. Infusion time should be no less than 30 min.
• Must be diluted before administration in sodium chloride 0.9% injection (normal saline), dextrose 5% injection, or Ringer's lactate solution. For an 800 mg dose, dilute 8 mL of ibuprofen in no less than 200 mL of diluent; for a 400 mg dose, dilute 4 mL of ibuprofen in no less than 100 mL of diluent.
• Visually inspect parenteral drug products for particulate matter and discoloration prior to administration, whenever solution and container permit. If visibly opaque particles, discoloration, or other foreign particulates are observed, do not use the solution.

Storage/Stability

Store at 68° to 77°F. Diluted IV solutions are stable for up to 24 h at 68° to 77°F.

Drug Interactions

ACE inhibitors (eg, lisinopril)

Antihypertensive effect of ACE inhibitors may be diminished. Also, the risk of nephrotoxicity associated with ACE inhibitors or ibuprofen may be increased. Closely monitor BP. If BP control deteriorates, consider stopping ibuprofen. Periodic measurement of renal function may be necessary.

Aminoglycosides (eg, amikacin, gentamicin)

The risk of acute renal failure may be increased. Avoid coadministration.

Aspirin

Protein binding of ibuprofen may be reduced; in addition, the risk of gastric erosion and bleeding may be increased. The clinical importance is not known. Avoid concurrent use because of the potential of increased adverse reactions.

Azole antifungal agents (eg, fluconazole, voriconazole)

Ibuprofen plasma concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Monitor the clinical response and adjust the ibuprofen dose as needed.

Beta-blockers (eg, metoprolol)

Antihypertensive effect may be decreased. Closely monitor BP and adjust the beta-blocker dose as needed.

Bisphosphonates (eg, alendronate)

Synergistic action may increase the risk of GI adverse effects (eg, gastric ulceration) when bisphosphonates and ibuprofen are coadministered orally. Use with caution. Closely monitor for possible GI adverse reactions, especially gastric ulceration. Instruct patients to report signs of GI irritation (heartburn, epigastric pain, nausea/vomiting, and sensation of fullness) to their health care provider.

Clopidogrel, prasugrel

The risk of bleeding may be increased. Use with caution. Closely monitor patients and instruct them to report any signs or symptoms of bleeding.

Corticosteroids (eg, prednisone)

The risk of GI bleeding may be increased. Use with caution. Closely monitor patients and instruct them to report any signs or symptoms of bleeding.

Cyclosporine, tacrolimus

The nephrotoxicity of each agent may be increased. Closely monitor renal function and cyclosporine concentrations. If an interaction is suspected, consider decreasing the cyclosporine or tacrolimus dose or stopping ibuprofen.

Heparin

The risk of heparin-induced bleeding may be increased by ibuprofen. If coadministration cannot be avoided, close clinical and laboratory monitoring is warranted.

Lithium

May increase lithium levels, increasing the pharmacologic effects and risk of adverse reactions. Monitor lithium plasma concentrations and the clinical response, as well as for signs of lithium toxicity. Adjust the lithium dose as needed.

Loop diuretics (eg, furosemide), thiazide diuretics (eg, hydrochlorothiazide)

The diuretic effects of loop diuretics may be reduced. In addition, renal toxicity has been reported. Closely observe patients for diuretic efficacy and signs of renal failure.

Methotrexate

May increase methotrexate levels. The risk of methotrexate toxicity may be increased. Use with caution. Consider longer leucovorin rescue when giving NSAIDs and methotrexate at antineoplastic doses. Monitor for renal impairment and methotrexate levels if indicated.

Probenecid

Pharmacologic and toxic effects of ibuprofen may be increased. Closely monitor for signs of ibuprofen toxicity. Adjust the ibuprofen dose as needed.

Quinolones (eg, ciprofloxacin)

Risk of CNS stimulation and seizures from quinolones may be increased. In addition, quinolone plasma concentrations may be increased. Use with caution.

Serotonin reuptake inhibitors (eg, fluoxetine, venlafaxine)

The risk of upper GI bleeding may be increased. If coadministration cannot be avoided, close clinical monitoring for signs of GI bleeding is warranted. Use of acid suppression therapy may be considered. Instruct patients to report any signs or symptoms of bleeding.

Smoking

The risk of bleeding may be increased. Use with caution in patients who smoke. Closely monitor patients and instruct them to report any signs or symptoms of bleeding.

Triamterene

The risk of acute renal failure may be increased. Avoid coadministration. If coadministration cannot be avoided, closely monitor renal function. If renal function decreases, consider stopping one or both drugs.

Warfarin

May increase risk of gastric erosion and bleeding. If coadministration cannot be avoided, use with extreme caution. Closely monitor PT and the patient. Instruct patients to report any signs or symptoms of bleeding.

Adverse Reactions

Cardiovascular

Hypertension, hypotension (10%); edema, fluid retention (greater than 1% and less than 3%).

CNS

Headache (12%); dizziness (3% to 9%); nervousness (greater than 1% and less than 3%).

Dermatologic

Rash, including maculopapular (3% to 9%); pruritus (greater than 1% and less than 3%).

EENT

Tinnitus (greater than 1% and less than 3%).

GI

Nausea (57%); vomiting (22%); flatulence (16%); diarrhea (10%); dyspepsia (4%); epigastric pain, heartburn (3% to 9%); abdominal cramps or pain, abdominal distress, constipation, indigestion (greater than 1% and less than 3%).

Genitourinary

Urinary retention (5%).

Hematologic

Anemia (36%); eosinophilia (26%); bacteremia, neutropenia (13%); blood urea increased, hemorrhage, hypoalbuminemia, LDH increased, thrombocythemia (10%); decreased Hgb, wound hemorrhage (3%).

Metabolic-Nutritional

Hypokalemia (19%); hypoproteinemia (13%); hypernatremia (10%); peripheral edema (3%); decreased appetite (greater than 1% and less than 3%).

Respiratory

Bacterial pneumonia (10%); cough (3%).

Precautions

Warnings NSAIDs may cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with length of therapy. Patients with CV disease or risk factors for CV disease may be at greater risk. Ibuprofen is contraindicated for treatment of perioperative pain in the setting of CABG surgery. NSAIDs cause an increased risk of serious GI adverse reactions, including inflammation, bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur any time during use and without warning symptoms. Elderly patients are at greater risk of serious GI events.

Monitor Follow chronically treated patients for signs and symptoms of GI tract ulceration and bleeding. Monitor LFTs periodically during long-term therapy. Monitor renal function in patients with compromised kidney function. Monitor Hgb in patients with low Hgb and Hct levels. Perform eye examinations if patient experiences visual disturbances. Closely monitor BP during the initiation of treatment and throughout the course of therapy. Carefully monitor patients who may be adversely affected by alterations in platelet function (eg, patients with coagulation disorders or receiving anticoagulant therapy).

Pregnancy

Category C (prior to 30 wk gestation); Category D (starting at 30 wk gestation).

Lactation

Excreted.

Children

Safety and efficacy not established (IV).

Elderly

Increased risk of GI adverse reactions.

Renal Function

Use is not recommended in patients with advanced kidney disease.

Special Risk Patients

Use with caution in patients with fluid retention, dehydration, hypertension, or heart failure.

Administration

Ibuprofen injection must be diluted before administration. Infusion of ibuprofen without dilution can cause hemolysis.

Anaphylactoid reactions

Do not administer to patients with aspirin triad, which occurs typically in asthmatic patients who experience rhinitis with or without nasal polyps, or who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.

Aseptic meningitis

Has been observed with fever and coma. May be more likely to occur in patients with SLE and related connective tissue diseases.

Asthma

Patients with asthma may have aspirin-sensitive asthma, which may be associated with severe and sometimes fatal bronchospasm. Ibuprofen should not be administered to patients with this type of aspirin-sensitivity because of possible cross-reactivity.

Hematologic effects

Anemia may occur and platelet aggregation may be inhibited, which may prolong bleeding time in some patients.

Hepatic effects

Borderline elevations of 1 or more liver tests may occur.

Hypertension

New hypertension or worsening of preexisting hypertension, either of which may contribute to increased risk of CV events, may occur.

Ophthalmic effects

Blurred or diminished vision, scotomata, and changes in color vision have been reported.

Renal effects

Long-term use may result in renal papillary necrosis and other renal injury.

Skin reactions

Serious and sometimes fatal skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and TEN, may occur.

Overdosage

Symptoms

Abdominal pain, acute renal failure, apnea, cyanosis, dizziness, drowsiness, epigastric pain, GI irritation/bleeding, lethargy, metabolic acidosis, nausea, sweating, tinnitus, vomiting.

Patient Information

• Tell patient to take medication soon after meals or with food, milk, or antacids.
• Tell patient to avoid alcohol and medications containing aspirin, such as cold remedies.
• Inform patients that ibuprofen may cause serious CV events, which may result in death.
• Advise patient to discontinue drug and immediately notify health care provider if any of the following occur: bleeding or unusual bruising, bloody or black stools, changes in urine patterns, fever, intestinal flu-like symptoms, joint pain, persistent or recurrent GI upset or stomach pain, rapid weight gain or swelling, skin rash or itching, unexplained tiredness or fatigue, visual changes, vomiting blood, yellowing of the skin or eyes.
• Inform patients that serious skin events, which may result in hospitalization and death, may occur.
• Advise pregnant women to avoid use starting at 30 wk gestation because premature closure of the ductus arterious in the fetus may occur.
• Advise patient to seek emergency medical assistance if any of the following occur: chest pain, shortness of breath or trouble breathing, slurred speech, swelling of the face or throat, weakness in one part or on one side of body.
• Instruct patient not to take OTC preparation for more than 3 days when treating fever or more than 10 days when treating pain, and to notify health care provider if condition does not improve.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

Copyright © 2009 Wolters Kluwer Health.