Advil (ibuprofen)

What is ibuprofen? How does it work (mechanism of action)?

Ibuprofen belongs to a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). Other members of this class include aspirin, naproxen (Aleve), indomethacin (Indocin), nabumetone (Relafen) and several others. These drugs are used for the management of mild to moderate pain, fever, and inflammation. Pain, fever, and inflammation are promoted by the release in the body of chemicals called prostaglandins. Ibuprofen blocks the enzyme that makes prostaglandins (cyclooxygenase), resulting in lower levels of prostaglandins. As a consequence, inflammation, pain and fever are reduced. The FDA approved ibuprofen in 1974.

What are the uses for ibuprofen?

Ibuprofen is used for the treatment of mild to moderate pain, inflammation and fever caused by many and diverse diseases. It is used for treating menstrual cramps (dysmenorrhea), osteoarthritis, rheumatoid arthritis, and juvenile idiopathic arthritis. Intravenous ibuprofen is used for treating patent ductus arteriosus.

What are the side effects of ibuprofen?

The most common side effects from ibuprofen are:

• rash,
• ringing in the ears,
• headaches,
• dizziness,
• drowsiness,
• abdominal pain,
• nausea,
• diarrhea,
• constipation, and
• heartburn.

NSAIDs reduce the ability of blood to clot and therefore increase bleeding after an injury.
Ibuprofen may cause ulceration of the stomach or intestine, and the ulcers may bleed. Sometimes, ulceration can occur without abdominal pain; and due to bleeding, the only signs or symptoms of an ulcer may be black, tarry stools, weakness, and dizziness upon standing (orthostatic hypotension).
Sometimes, ulceration can occur without abdominal pain, due to the bleeding, and the only signs or symptoms of an ulcer are:

• black, tarry stools,
• weakness, and
• dizziness upon standing (orthostatic hypotension)

NSAIDs reduce the flow of blood to the kidneys and impair function of the kidneys. The impairment is most likely to occur in patients who already have impaired function of the kidney or congestive heart failure, and use of NSAIDs in these patients should be cautious.
People who are allergic to other NSAIDs, including aspirin, should not use ibuprofen.
Individuals with asthma are more likely to experience allergic reactions to ibuprofen and other NSAIDs.
Other serious side effects associated with NSAIDs are:

• fluid retention (edema),
• blood clots,
• heart attacks,
• hypertension (high blood pressure), and
• heart failure.

NSAIDs (except low- dose aspirin) may increase the risk of potentially fatal heart attacks, stroke, and related conditions in people with or without heart disease or risk factors for heart disease. The increased risk of heart attack or stroke may occur as early as the first week of use and the risk may increase with longer use and is higher in patients who have underlying risk factors for heart and blood vessel disease. Therefore, NSAIDs should not be used for the treatment of pain resulting from coronary artery bypass graft (CABG) surgery.

What is the dosage for ibuprofen?

• For minor aches, mild to moderate pain, menstrual cramps, and fever, the usual adult dose is 200 or 400 mg every 4 to 6 hours.
• Arthritis is treated with 300 to 800 mg 3 or 4 times daily.
• When under the care of a physician, the maximum dose of ibuprofen is 3.2 g daily. Otherwise, the maximum dose is 1.2 g daily.
• Individuals should not use ibuprofen for more than 10 days for the treatment of pain or more than 3 days for the treatment of a fever unless directed by a physician.
• Children 6 months to 12 years of age usually are given 5-10 mg/kg of ibuprofen every 6-8 hours for the treatment of fever and pain. The maximum dose is 40 mg/kg daily.
• Juvenile arthritis is treated with 20 to 40 mg/kg/day in 3-4 divided doses.
• Ibuprofen should be taken with meals to prevent stomach upset.

Which drugs or supplements interact with ibuprofen?

Ibuprofen is associated with several suspected or probable interactions that can affect the action of other drugs.

• Ibuprofen may increase the blood levels of lithium (Eskalith, Lithobid) by reducing the excretion of lithium by the kidneys. Increased levels of lithium may lead to lithium toxicity.
• Ibuprofen may reduce the blood pressure-lowering effects of drugs that are given to reduce blood pressure. This may occur because prostaglandins play a role in the regulation of blood pressure.
• When ibuprofen is used in combination with methotrexate (Rheumatrex, Trexall) or aminoglycosides (for example, gentamicin) the blood levels of the methotrexate or aminoglycoside may increase, presumably because their elimination from the body is reduced. This may lead to more methotrexate or aminoglycoside-related side effects.
• Ibuprofen increases the negative effect of cyclosporine on kidney function.
• Individuals taking oral blood thinners or anticoagulants, for example, warfarin (Coumadin), should avoid ibuprofen because ibuprofen also thins the blood, and excessive blood thinning may lead to bleeding.
• If aspirin is taken with ibuprofen there may be an increased risk for developing an ulcer.
• Persons who have more than three alcoholic beverages per day may be at increased risk of developing stomach ulcers when taking ibuprofen or other NSAIDs.
• Combining SSRIs or selective serotonin reuptake inhibitors (for example, fluoxetine [Prozac], citalopram [Celexa], paroxetine [Paxil, Paxil CR, Pexeva) with NSAIDs may increase the likelihood of upper gastrointestinal bleeding.

Is ibuprofen safe to take if I'm pregnant or breastfeeding?

There are no adequate studies of ibuprofen in pregnant women. Therefore, ibuprofen is not recommended during pregnancy. Ibuprofen should be avoided in late pregnancy due to the risk of premature closure of the ductus arteriosus in the fetal heart.
Ibuprofen is excreted in breast milk but the American Academy of Pediatrics states that ibuprofen is compatible with breastfeeding.

What brand names are available for ibuprofen?

• Advil
• Pediatric Advil
• Advil/Motrin
• Advil Migraine
• Medipren
• Motrin
• Nuprin
• PediaCareChildren’s Pain Reliever/Fever Reducer
• PediaCare Infant’s Pain Reliever/Fever Reducer Fever
• Caldolor
• Duexis
• IBU-Tab
• Neoprofen (ibuprofen lysine)
• Many others

What else should I know about ibuprofen?

Ibuprofen preparations

• Tablets: 100, 200, 400, 600, and 800 mg
• Chewable tablets: 50 and 100 mg; Suspension: 100 mg/5 ml and 40 mg/ml
• Intravenous solution: 10 mg/ml, 100 mg/ml

How ibuprofen should be stored

• Ibuprofen should be stored at room temperature, between 15 C to 30 C (59 F to 86 F).

OTC and prescription availability

• You need a prescription from your doctor or other healthcare professional to obtain 400 to 800 mg strengths and injection.
• Lower doses of ibuprofen are available over-the-counter (OTC, without a prescription).

Summary

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) used to reduce mild to moderate pain, inflammation, and fever. Ibuprofen works by blocking an enzyme that makes prostaglandin (a hormone-like substance that participates in a variety of body functions), which results in lower levels of prostaglandins in the body. Lower levels of prostaglandins reduce pain, inflammation, and fever.
Ibuprofen is prescribed to treat diseases and conditions that cause mild to moderate pain, fever, and inflammation. For example, Pain from strains and sprains; pain from cuts, scrapes, and puncture wounds; muscle aches and pains; tooth pain; common cold; mild headache; some arthritis conditions; joint pain; and to reduce fever.
Common side effects of ibuprofen include, diarrhea, constipation, nausea, heartburn, belly pain, drowsiness, headaches, tinnitus (ringing in the ears), and mild rash.
More serious side effects and adverse effects include, increased bleeding after injury, stomach ulcers, impaired kidney function, severe allergic reaction (anaphylaxis), blood clots, heart attack, heart failure, and high blood pressure.
The maximum dose prescribed under a doctor's care is 3.2 g daily. Otherwise, the over-the-counter (OTC) maximum daily dose is 1.2 g daily. Dosage depends upon the age, weight, and any current medical conditions of the patient. Several drugs interact with ibuprofen so check with your doctor, pharmacist, or other health care professional with questions in regard to this drug. Doctors don't know if it is safe to take ibuprofen if your are pregnant, therefore it is not recommended if you are pregnant. According to the American Academy of Pediatrics, ibuprofen is safe to take while breastfeeding.
REFERENCE: FDA Prescribing Information.