Ibuprofen (Advil, Motrin): Drug Whys


Generic name: Ibuprofen (multiple manufacturers)
Common U.S. brand names: Advil (Wyeth Consumer Healthcare), Motrin (McNeil Consumer Healthcare) — both over the counter (OTC) non-prescription strengths
Popularity: Eighteenth most commonly prescribed drug between 2002-2006 (U.S.)
Class: Antipyretic, NSAID (non-steroidal anti-inflammatory drug)

Treatment Uses — For treatment of fever — ibuprofen is comparable to aspirin or acetaminophen. For pain syndromes including minor aches, headaches (including migraines and tension headaches), head and neck cancer pain, dental pain, postepisiotomy pain, pain and inflammation associated with sports-related injuries, and discomfort (as well as fever) associated with common colds. Effective for treatment of osteoarthritis, rheumatoid arthritis, primary dysmenorrhea (menstrual pain), and pain associated with systemic lupus erythematosus (SLE). May reduce gastrointestinal and injection site pain but not fever in children receiving DTP vaccination. Evidence seems to show ibuprofen slows progression of pulmonary decline in children with cystic fibrosis. In one very small study, ibuprofen was effective in reducing menstrual blood flow caused by intrauterine devices (IUDs). Some studies suggest regular use of aspirin or ibuprofen reduces risk of malignant melanoma among women. However, further research is needed to make this finding conclusive.

Studies using ibuprofen for prevention of colorectal cancer have had mixed results. The U.S. Preventive Services Task Force (USPSTF) recommends against aspirin or NSAID use for colorectal cancer prevention in adults with average risk factors and no symptoms. Ibuprofen may be useful for foot pain associated with diabetic peripheral neuropathy, but data are limited at best. There is some evidence to suggest an NSAID protective effect against development of Alzheimer's disease or improving symptoms in Alzheimer's patients but clinical trials to date have not shown any of these benefits. Ibuprofen is ineffective for preventing recurrent febrile seizure in susceptible children. It is also not effective for treatment of fibromyalgia syndrome. Older studies touted ibuprofen in combination with caffeine as a superior remedy for high altitude headache but NSAIDs have at least theoretically been implicated in causing or accelerating high altitude pulmonary edema (HAPE). More recent data show acetaminophen as effective as ibuprofen in relieving high altitude headache, without the HAPE risks.

Dosing and Administration — Prescribers are cautioned to weighs risks and benefits of treatment before starting any NSAID, including ibuprofen. To reduce risks of serious adverse effects, the lowest effective dose of ibuprofen should be used for the shortest duration possible. Once a response to treatment is seen, the dose and frequency should be adjusted to each particular patient’s needs. OTC ibuprofen should not be taken for longer than 10 days without consulting a health care practitioner. For adults with mild to moderate pain, fever and common cold, the recommended oral starting dose is 200 to 400 milligrams every four to six hours as needed with a daily maximum of 1,200 milligrams. Individual doses above 400 milligrams do not provide any greater analgesic action. For arthritis, the recommended dosing range in adults is 1,200 to 3,200 milligrams daily, given as 300 milligrams four times daily or as 400, 600 or 800 milligrams three or four times each day. For primary dysmenorrhea, treatment should begin with the start of pain at 400 milligrams taken orally every four hours as needed.

Pediatric dosing for fever and pain are based on age and weight. From six months to 12 years old, the recommended oral dosing is 5 to 10 milligrams per kilogram of body weight every six to eight hours as needed with a maximum of four doses per day. For children older than 12 years, recommended oral dosing is 200 to 400 milligrams every four to six hours as needed, not to exceed 1,200 milligrams per day. As with adult patients, higher doses are recommended for pediatric arthritis. Liquid oral formations of ibuprofen are available. The maximum pediatric dose of ibuprofen should not exceed 50 milligrams per kilogram per day.

No dose adjustments are recommended for patients with kidney dysfunction or failure. Supplemental ibuprofen is not needed during or following dialysis. Studies also suggest dose adjustments are not needed in patients with liver dysfunction. Morbidly obese patients do require higher ibuprofen doses but no change in dosing intervals.

An intravenous form of ibuprofen called ibuprofen lysine is available and used for indications not covered in this monograph. Ibuprofen is also available in topical gel formulations. Several sustained release oral ibuprofen preparations are available which are no more effective than regular release ibuprofen but offer longer durations of action with fewer fluctuations in drug concentration in the body.

Food affects absorption of ibuprofen but these effects have no clinical significance. Ibuprofen can be taken without regard to meals and is best taken with food or milk to reduce gastrointestinal irritation.

Most ibuprofen overdoses are asymptomatic. Deaths are rare. Toxicity is typically becomes evident within four hours of poisoning. Treatment is supportive, directed at presenting symptoms. Mild symptoms include GI effects, drowsiness, headache and tinnitus (ringing in the ears). More severe effects include apnea and/or seizures (particularly common in pediatric patients), coma, renal failure, lung injury and acidosis. Seizures resulting from ibuprofen toxicity are usually brief and terminate without benzodiazepines. Generally, ingestion of up to 200 milligrams per kilogram does not manifest symptoms and requires only observation. For overdoses exceeding 200 milligrams per kilogram, GI decontamination is recommended although little drug will be captured if elapsed time from ingestion exceeds one hour. Because pediatric overdoses may induce seizures, emesis should not be induced in younger patients. Overdoses exceeding 400 milligrams per kilogram typically require hospital admission/observation and blood chemistry monitoring. Overdoses of up to 48 grams (that's 48,000 milligrams) have been well tolerated in healthy adults. Hemodialysis is not effective for removing ibuprofen from the body.

Pharmacology/Pharmacokinetics/Stability — Oral ibuprofen is rapidly absorbed. Initial response to regular release ibuprofen taken for pain or fever is seen within 15 to 25 minutes with peak response within 90 minutes. Taken for arthritis, initial response is seen within a few days to one week and peak response within two weeks. The average half-life (time needed for half the active drug to be eliminated from the body) of ibuprofen in the body is 1.8 to two hours. Most ibuprofen is excreted by the kidneys.

Use of ibuprofen during pregnancy is not recommended. For minor aches, pains or fever, acetaminophen, used short term at normal doses, appears safer for the fetus. Ibuprofen is compatible with breastfeeding. No studies to date have been able to detect ibuprofen in breast milk of nursing mothers.

Ibuprofen most likely produces anti-inflammatory, fever reducing and analgesic effects by inhibiting prostaglandin synthesis in the body. Prostaglandins are chemical messengers that activate inflammatory responses, create pain and raise body temperature. Ibuprofen also inhibits platelet aggregation, increasing risk for bleeding.

Ibuprofen oral tablets come in 200, 400, 600 and 800 milligram strengths. Ibuprofen oral suspension comes in a variety of strengths, most commonly available as 100 milligrams per 5 milliliters. Chewable tablets are available for children in a variety of lower dose strengths. Color, shape, and size of tablets vary by manufacturer. Tablets should be stored at room temperature between 68-77 F and protected from light. Occasional temperature variations to 59-86 F are permitted.

Cautions and Warnings — Severe, even fatal, allergic reactions have been reported in patients taking ibuprofen who have experienced asthma, hives or other allergic reactions to aspirin or other NSAID agents. Ibuprofen should not be taken by patients with allergic type reactions (including asthma or rash) to aspirin or other NSAIDs. Patients with the "aspirin triad" (aspirin allergy, nasal polyps and asthma) should not take ibuprofen.

There is an increased risk of bleeding with ibuprofen, particularly in the gut. Bleeding, ulceration or perforation of the stomach or intestines can occur without warning. Elderly, very ill patients and people taking steroids have the highest risk for this potential complication. Consumption of more than three alcoholic beverages daily significantly increases the risk for GI bleeding with ibuprofen.

All NSAIDs including ibuprofen were labeled in October 2005 with a "Black Box Warning" from the U.S. Food and Drug Administration (FDA). Data at that time revealed that all NSAIDs excluding aspirin (both prescription and over the counter agents) increase the risk of cardiovascular (CV) events and pose serious risk of potentially life threatening gastrointestinal bleeding. The FDA also requested that NSAID package inserts include a contraindication for patients immediately post operative from coronary artery bypass (CABG) surgery since this group has more serious risk of adverse CV events than the general population. For patients with high risk features for cardiovascular disease (males over 45, females over 55, family history, smokers, hypertensive, obese, high cholesterol, etc.), risks of taking ibuprofen or any NSAID besides aspirin may outweigh the benefits.

One important caveat from the FDA data is that the risk of adverse CV events from NSAIDs appears increased with higher doses and long durations of therapy. The available data do not show increased risk of serious CV events for the short-term, low dose use of NSAIDs available over the counter.

Since ibuprofen is largely metabolized in the liver where many essential clotting factors are manufactured, it should be used carefully in patients with liver dysfunction. A theoretical increased risk of bleeding exists. The same is true for patients with kidney dysfunction given that ibuprofen is renally eliminated. A theoretical risk of prolonged elimination resulting in higher than usual levels of ibuprofen in the body exists.

Important Side Effects and Interactions — The most commonly reported side effects of ibuprofen are gastrointestinal. Up to 16 percent of patients report at least one GI symptom such as nausea, belly pain or heartburn. Rash, dizziness and tinnitus occur in 3 to 9 percent of patients. Edema, headache and itching are reported by 1 to 3 percent of patients taking ibuprofen. Up to 15 percent of patients taking ibuprofen experience increases in liver function tests although the clinical significance of this is unknown.

Seventy drugs or drug classes are reported to interact with ibuprofen; most lack substantial evidence. The antiplatelet effect of aspirin is significantly reduced by ibuprofen (hence the FDA Black Box Warning). In patients who occasionally use ibuprofen and are taking daily aspirin for cardioprotective effects, aspirin should be taken at least 30 minutes before or eight hours after the ibuprofen. Regular use of ibuprofen most likely negates any cardioprotective effects of aspirin and switching to acetaminophen, another NSAID, or a COX-2 inhibitor is recommended. Ibuprofen should not be taken with other NSAIDs because of the increased risk of bleeding. Consumers should carefully read OTC labels to understand the ingredients. It is not uncommon for patients to unknowing take multiple NSAID containing medications. Concurrent use of warfarin and ibuprofen appears safe, especially at ibuprofen doses of less than 600 milligrams per day. Ibuprofen may increase cyclosporine, digoxin, lithium and methotrexate (MTX) serum concentrations. NSAIDs may worsen adverse renal effects of ACE inhibitors.

Average Costs — U.S.
600 mg and 800 mg tablet (generic)
Patient cost: $0.26 and $0.33 each*
Large Hospital cost: $0.03 and $0.08 each
*($4.00 at Wal Mart® and Target for one month supply)


References:
1. MICROMEDEX® Healthcare Series: Thomson Micromedex, Greenwood Village, Colorado (accessed December, 2007).
2. Albany Medical Center Pharmacy, Albany, New York.

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