The P-I-E-N-O Parkinsn's List Drug Database
ibuprofen /AdvilTM , ExcedrinTM , IBTM , MotrinTM , NuprinTM , ProvelTM , RufenTM
NON-STEROIDAL ANTIINFLAMMATORY:
Description: Ibuprofen is an oral, nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Ibuprofen is indicated for the treatment of rheumatoid arthritis, osteoarthritis, and dysmenorrhea. It also is used for its antipyretic effects and for the alleviation of mild to moderate pain. In addition, clinical studies have demonstrated its effectiveness in the treatment of ankylosing spondylitis, gout, and psoriatic arthritis. Ibuprofen was approved by the FDA in 1974.
Mechanism of Action: The exact mechanism of action of NSAIDs is not known, but antiinflammatory effects are believed to be secondary to inhibition of synthesis and/or release of prostaglandins. Ibuprofen probably has a peripheral rather than central action as an analgesic. Higher doses are required for an antiinflammatory effect than for analgesia. Antipyretic activity may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Pharmacokinetics: Ibuprofen is administered orally and is approximately 80% absorbed from the gut; the suspended form is absorbed at about twice the rate of the tablet form. Although absorption is slower if the drug is taken with food, the extent of absorption is not affected. Peak serum concentrations are reached 1-2 hours after a dose. In children, the antipyretic effect begins within 1 hour and peaks within 2-4 hours. In treatment for inflammation, a few days to 2 weeks is generally required before a therapeutic response occurs. Ibuprofen is highly protein-bound (about 90-99%) and undergoes biotransformation in the liver. Plasma half-life is between 2 and 4 hours. Ibuprofen is excreted in the urine, 50-60% as metabolites and approximately 10% as unchanged drug. Excretion is usually complete within 24 hours of oral administration.
CONTRAINDICATIONS/PRECAUTIONS: Chronic use of ibuprofen can result in gastritis, ulceration with or without perforation, and/or GI bleeding, which can occur at any time, often without preceding symptoms. Therefore, ibuprofen is contraindicated in patients with a history of or active GI disease including peptic ulcer disease, ulcerative colitis, or GI bleeding. Such patients should be monitored closely, with special caution in tobacco smoking patients or in patients with alcoholism. All patients receiving prolonged treatment should be routinely monitored for potential GI ulceration and bleeding (see Adverse Reactions).
Liver dysfunction can occur during therapy with NSAIDs, resulting in jaundice and fatal hepatitis. Ibuprofen should be prescribed cautiously to patients with preexisting hepatic disease. Most NSAIDs are metabolized in the liver and accumulation can occur, increasing risk of toxicity.
Ibuprofen and its metabolites are renally excreted. Accumulation of parent drug and metabolites can occur in patients with renal impairment, increasing risk of potential toxicity. Dosage adjustment may be necessary.
Conditions associated with fluid retention, such as congestive heart failure, can be exacerbated with ibuprofen therapy since peripheral edema has been observed in some patients. Hypertension may be exacerbated by the NSAID-induced fluid retention. Reduced renal blood flow caused by inhibition of prostaglandin synthesis can result in overt renal decompensation. Patients with renal disease, hepatic disease, congestive heart failure, diabetes mellitus, systemic lupus erythematosus (SLE), edema, extracellular volume depletion, sepsis, those taking diuretics or nephrotoxic drugs, and the elderly are at the highest risk for this reaction.
Patients with aspirin hypersensitivity, nasal polyps, and a history of asthma can be susceptible to bronchospasm when given ibuprofen.
Ibuprofen should be used cautiously in patients with preexisting coagulopathy or hemophilia due to the effect of the drug on platelet function and vascular response to bleeding. Like other NSAIDs, ibuprofen can prolong bleeding time. Anemia may be exacerbated with the used of NSAIDs.
Intramuscular injections should be administered cautiously to patients receiving ibuprofen. IM injections may cause bleeding, bruising, or hematomas due to platelet effects secondary to ibuprofen therapy.
Ibuprofen should be used with caution in patients with dental disease. All NSAIDs may rarely cause myelosuppression (leukopenia, thrombocytopenia) and there may be an increased risk of infection. Dental work should be performed prior to initiating ibuprofen therapy or deferred until blood counts return to normal. Patients should be instructed on proper oral hygiene.
Ibuprofen is classified as a pregnancy category B drug: no studies have linked ibuprofen use during pregnancy and congenital defects. Although ibuprofen has not been shown in studies to cause fetal harm early on in pregnancy, use of ibuprofen should be avoided unless the potential therapeutic benefits justify its use during pregnancy. Ibuprofen is classified as a pregnancy category D drug if used during the third trimester, due to the potential for prostaglandin synthetase inhibitors to cause in utero constriction of the fetal ductus arteriosus. Persistent pulmonary hypertension due to ductus arteriosus constriction has occured in neonates whose mothers received prostaglandin synthetase inhibitors during pregnancy. Prostaglandin synthetase inhibitors also have the potential to prolong pregnancy and inhibit labor if taken during the third trimester.
DRUG INTERACTIONS: Ibuprofen should be used cautiously in patients receiving anticoagulants (e.g., heparin or warfarin) or thrombolytic agents (e.g., streptokinase) because NSAIDs can cause GI bleeding, inhibit platelet aggregation, and prolong bleeding time. Ibuprofen does not, however, displace warfarin from protein-binding sites or independently prolong the prothrombin time.
Corticosteroids can increase the potential for NSAID-induced toxicity. Although some patients may need to be given both types of agents concomitantly, which can be done successfully for short periods of time without sequelae, prolonged concomitant administration should be avoided. When ibuprofen is given concomitantly with other NSAIDs, the risk of GI toxicity is increased. Ethanol also can potentiate ibuprofen-induced GI side effects.
Ibuprofen can reduce the renal clearance of lithium, causing serum lithium concentrations to increase. Because of the potential for lithium toxicity and its serious nature, frequent monitoring of lithium concentrations is recommended when ibuprofen is prescribed to patients receiving lithium.
When taken with oral hypoglycemics, ibuprofen can potentiate hypoglycemic effects because of the influence of prostaglandins on glucose metabolism. Little is known, however, about a drug-drug interaction between NSAIDs and oral hypoglycemics.
Nephrotoxicity can occur during concomitant treatment with diuretics and NSAIDs. This interaction is well described for the combination of indomethacin and triamterene. In these patients, reversible renal insufficiency occurred after several days of combination therapy. Manifestations included azotemia, hyperkalemia, and hyperuricemia, and patients most often were elderly and/or were receiving NSAID therapy for treatment of acute gouty arthritis. Because of the contribution of renal vasodilatory prostaglandins to renal perfusion, NSAIDs should be used cautiously in patients receiving diuretics, especially if the patient is in a dehydrated state.
NSAIDs can reduce the renal elimination of methotrexate. In patients receiving high-dose methotrexate therapy, NSAIDs can lead to life-threatening methotrexate toxicity. All NSAIDs should be avoided in patients receiving high-dose methotrexate therapy.
ADVERSE REACTIONS: Nausea/vomiting, diarrhea, constipation, flatulence, and abdominal pain could represent a minor adverse reaction to ibuprofen therapy in some patients or serious GI toxicity in others. These symptoms correlate poorly with the degree of mucosal injury. When feasible, monitor stool for blood loss. During chronic administration, more serious effects, such as peptic ulcer disease and gastritis, leading to GI bleeding or even perforation can occur at any time, with or without warning. These effects can be potentiated by alcohol and smoking. An orally administered prostaglandin, misoprostil, is approved for use in the prevention of NSAID-related gastritis; however, this agent has not been shown to significantly reduce the incidence of ulceration. Although ulcers can heal even when NSAID therapy is continued, in general, ibuprofen therapy is not advised in those with active peptic ulcer disease. Pancreatitis has been reported in < 1% of patients on ibuprofen.
Ibuprofen can cause adverse ocular effects including amblyopia (blurred vision or visual impairment). Vision generally improves when the drug is discontinued. The mechanism for visual disturbances is unclear. Other changes in the special senses include tinnitus and hearing loss.
NSAIDs have been associated with nephrotoxicity. It is well known that vasodilatory renal prostaglandins and the potent vasoconstrictor angiotensin II work in concert to maintain renal blood flow. Inhibition of renal prostaglandins by NSAIDs can cause renal insufficiency. This problem can be manifest as hyperkalemia, hyperuricemia, or azotemia. With some NSAIDS, renal papillary necrosis, nephrotic syndrome, hematuria, proteinuria, and interstitial nephritis has been reported.
NSAIDs have been associated with hepatotoxicity such as hepatitis or jaundice. Usually, this is an infrequent occurrence, but patients should be monitored closely if elevated hepatic enzymes are observed during therapy.
NSAIDs have been shown to cause platelet dysfunction; this effect, however, is transient and reversible. Since inhibition of platelet aggregation appears to correlate with plasma concentrations of the drug, the individual half-life of each NSAID determines the duration of this effect. Other adverse hematologic effects include neutropenia, agranulocytosis, aplastic anemia, and hemolytic anemia.
Peripheral edema and heart failure can occur with most other NSIADs and caution should be exercised when administering ibuprofen to patients with congestive heart failure or other conditions predisposing to fluid retention.
Maculopapular rash and urticaria have been reported in 1-3% of patients taking NSAIDs. Other dermatologic reactions occur less frequently, including bullous rash, toxic epidermal necrolysis and vasculitis.
PATIENT INFORMATION:
What do ibuprofen tablets or capsules do?
Ibuprofen (MotrinTM , AdvilTM , RufenTM , NuprinTM ) is a nonsteroidal antiinflammatory drug (NSAID). Ibuprofen reduces inflammation and eases mild to moderate pain. It reduces fever and relieves the symptoms of rheumatoid arthritis (rheumatism), osteoarthritis, menstrual cramps or premenstrual pain and swelling. Generic ibuprofen tablets and caplets are available.
What should my doctor, dentist, or pharmacist know before I take ibuprofen?
They need to know if you have any of these conditions:
How should I take this medicine?
Take ibuprofen tablets or caplets by mouth. Follow the directions on the prescription label. Swallow the tablets or caplets whole with a full glass of water. It is better to take ibuprofen with food. Take your doses at regular intervals. Do not take your medicine more often than directed.
Special precautions for use in children:
This medicine is not for infants under 6 months old. The suspension form is better than tablets for children under 6 years old.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What other medicines can interact with ibuprofen?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking ibuprofen?
Elderly patients are more likely to get side effects.
Serious side effects with ibuprofen include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with ibuprofen include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take ibuprofen?
Let your doctor know if your pain continues, do not take with other pain-killers without advice. Do not treat yourself for a fever with ibuprofen for more than 3 days, or for pain for more than 10 days without asking your doctor for advice. You may be covering up a more serious illness.
To reduce unpleasant effects on your throat and stomach, take ibuprofen with a full glass of water and never just before lying down.
You may get dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how ibuprofen affects you. Do not sit or stand up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.
Do not smoke cigarettes or drink alcohol; these increase irritation to your stomach and can make it more susceptible to damage from ibuprofen.
If you get black, tarry stools or vomit up what looks like coffee grounds, call your doctor at once. You may have a bleeding ulcer.
If you are going to have surgery, tell your doctor or dentist that you are taking ibuprofen. Ibuprofen can cause blood problems. This can mean slow healing and a risk of infection. Problems can arise if you need dental work, and in the day to day care of your teeth. Try to avoid damage to your teeth and gums when you brush or floss your teeth.
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30C (59 and 86F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
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