Where is ibuprofen metabolized

It became available by prescription in the United States in , over-the-counter in Britain in , and over-the-counter in the United States in While the exact mechanism remains unknown, ibuprofen is known to be a potent inhibitor of prostaglandin synthesis, which controls pain, inflammation and fever. Ibuprofen is rapidly absorbed, reaching peak serum levels one to two hours after administration, and has a half-life of 1.

Its primary distribution is in plasma albumin, with a volume of distribution of 0. At doses greater than mg, there is an increase in the unbound faction of the drug leading to an increased clearance. The main prescribing precaution for NSAIDs is the risk of gastrointestinal GI tract injuries, which mainly occurs due to blockage of gastroprotective prostaglandin synthesis. It is recommended to take ibuprofen with a meal or a glass of milk if GI upset occurs, and while it has been shown that administering ibuprofen with meals reduces the absorption time, it does not affect the ultimate serum level concentration.

Cardiovascular complications such as worsening hypertension and an increased risk of myocardial infarction are also risks associated with using NSAIDs. As such, ibuprofen usage should be avoided in patients with congestive heart failure, and should be used with caution with patients who have hypertension, as a mean blood pressure increase of 5 mm Hg has been noted with NSAID use.

Use cautiously. Antacids: May decrease absorption of ibuprofen. Patient should take drugs at separate times. Anticoagulants, thrombolytics coumarin derivatives, heparin, streptokinase, urokinase : Increase anticoagulant effects. Monitor coagulation studies. Dosage adjustment may be needed. Antihypertensives, diuretics: May decrease effectiveness of these drugs; diuretics may increase nephrotoxicity.

Aspirin, carbenicillin, cefamandole, cefoperazone, corticosteroids, dextran, dipyridamole, mezlocillin, piperacillin, plicamycin, salicylates, sulfinpyrazone, ticarcillin, valproic acid, other anti-inflammatories: Increases risk of bleeding or adverse GI reactions. Avoid use together. Aspirin: May decrease bioavailability of ibuprofen. Monitor patient for drug effect. Insulin, oral antidiabetics: May potentiate hypoglycemic effects. Lithium, methotrexate: Decreases renal clearance of these drugs.

Use together cautiously. Nifedipine, phenytoin, verapamil: Toxicity may occur. Feverfew: Decreases effectiveness of ibuprofen. Discourage use together.

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