IBUPROFEN- ibuprofen tablet
Amneal Pharmaceuticals of New York LLC
Cardiovascular Thrombotic Events
- Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use [see WARNINGS and PRECAUTIONS].
- Ibuprofen Tablets are contraindicated in the setting of coronary artery bypass graft (CABG) surgery [see CONTRAINDICATIONS and WARNINGS].
- NSAIDs cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal events [see WARNINGS].
Ibuprofen Tablets, USP contain the active ingredient ibuprofen, which is (±)-2-(p -isobutylphenyl) propionic acid. Ibuprofen is a white powder with a melting point of 74° to 77° C and is very slightly soluble in water (<1 mg/mL) and readily soluble in organic solvents such as ethanol and acetone. The structural formula is represented below:
Ibuprofen Tablets, USP, a nonsteroidal anti-inflammatory drug (NSAID), is available in 800 mg tablets for oral administration. Inactive ingredients: Colloidal Silicon Dioxide, Corn Starch, Hydroxypropyl Cellulose, Hypromellose, Lactose Anhydrous, Magnesium Stearate, Microcrystalline Cellulose, Polyethylene Glycol, Povidone, Sodium Lauryl Sulfate, Sodium Starch Glycolate, Titanium Dioxide.
Ibuprofen Tablets contain ibuprofen which possesses analgesic and antipyretic activities. Its mode of action, like that of other NSAIDs, is not completely understood, but may be related to prostaglandin synthetase inhibition.
In clinical studies in patients with rheumatoid arthritis and osteoarthritis, Ibuprofen Tablets have been shown to be comparable to aspirin in controlling pain and inflammation and to be associated with a statistically significant reduction in the milder gastrointestinal side effects [see ADVERSE REACTIONS]. Ibuprofen Tablets may be well tolerated in some patients who have had gastrointestinal side effects with aspirin, but these patients when treated with Ibuprofen Tablets should be carefully followed for signs and symptoms of gastrointestinal ulceration and bleeding. Although it is not definitely known whether Ibuprofen Tablets causes less peptic ulceration than aspirin, in one study involving 885 patients with rheumatoid arthritis treated for up to one year, there were no reports of gastric ulceration with Ibuprofen Tablets whereas frank ulceration was reported in 13 patients in the aspirin group (statistically significant p<0.001).
Gastroscopic studies at varying doses show an increased tendency toward gastric irritation at higher doses. However, at comparable doses, gastric irritation is approximately half that seen with aspirin. Studies using 51 Cr-tagged red cells indicate that fecal blood loss associated with Ibuprofen Tablets in doses up to 2400 mg daily did not exceed the normal range, and was significantly less than that seen in aspirin-treated patients.
In clinical studies in patients with rheumatoid arthritis, Ibuprofen Tablets have been shown to be comparable to indomethacin in controlling the signs and symptoms of disease activity and to be associated with a statistically significant reduction of the milder gastrointestinal [see ADVERSE REACTIONS] and CNS side effects.
Ibuprofen Tablets may be used in combination with gold salts and/or corticosteroids.
Controlled studies have demonstrated that Ibuprofen Tablets are a more effective analgesic than propoxyphene for the relief of episiotomy pain, pain following dental extraction procedures, and for the relief of the symptoms of primary dysmenorrhea.
In patients with primary dysmenorrhea, Ibuprofen Tablets have been shown to reduce elevated levels of prostaglandin activity in the menstrual fluid and to reduce resting and active intrauterine pressure, as well as the frequency of uterine contractions. The probable mechanism of action is to inhibit prostaglandin synthesis rather than simply to provide analgesia.
In a healthy volunteer study, ibuprofen 400 mg given once daily, administered 2 hours prior to immediate-release aspirin (81 mg) for 6 days, showed an interaction with the antiplatelet activity of aspirin as measured by % serum thromboxane B2 (TxB2) inhibition at 24 hours following the day-6 aspirin dose [53%]. An interaction was still observed, but minimized, when ibuprofen 400 mg given once-daily was administered as early as 8 hours prior to the immediate-release aspirin dose [90.7%]. However, there was no interaction with the antiplatelet activity of aspirin when ibuprofen 400 mg, given once daily, was administered 2 hours after (but not concomitantly, 15 min, or 30 min after) the immediate-release aspirin dose [99.2%].
In another study, where immediate-release aspirin 81 mg was administered once daily with ibuprofen 400 mg given three times daily (1, 7, and 13 hours post-aspirin dose) for 10 consecutive days, the mean % serum thromboxane B2 (TxB2) inhibition suggested no interaction with the antiplatelet activity of aspirin [98.3%]. However, there were individual subjects with serum TxB2 inhibition below 95%, with the lowest being 90.2%.
When a similarly designed study was conducted with enteric-coated aspirin, where healthy subjects were administered enteric-coated aspirin 81 mg once daily for 6 days and ibuprofen 400 mg three times daily (2, 7 and 12 h post-aspirin dose) for 6 days, there was an interaction with the antiplatelet activity at 24 hours following the day-6 aspirin dose [67%] [see PRECAUTIONS, Drug Interactions].
The ibuprofen in Ibuprofen Tablets is rapidly absorbed. Peak serum ibuprofen levels are generally attained one to two hours after administration. With single doses up to 800 mg, a linear relationship exists between amount of drug administered and the integrated area under the serum drug concentration vs time curve. Above 800 mg, however, the area under the curve increases less than proportional to increases in dose. There is no evidence of drug accumulation or enzyme induction.
The administration of Ibuprofen Tablets either under fasting conditions or immediately before meals yields quite similar serum ibuprofen concentration-time profiles. When Ibuprofen Tablets are administered immediately after a meal, there is a reduction in the rate of absorption but no appreciable decrease in the extent of absorption. The bioavailability of the drug is minimally altered by the presence of food.
A bioavailability study has shown that there was no interference with the absorption of ibuprofen when Ibuprofen Tablets were given in conjunction with an antacid containing both aluminum hydroxide and magnesium hydroxide.
Ibuprofen is rapidly metabolized and eliminated in the urine. The excretion of ibuprofen is virtually complete 24 hours after the last dose. The serum half-life is 1.8 to 2.0 hours.
Studies have shown that following ingestion of the drug, 45% to 79% of the dose was recovered in the urine within 24 hours as metabolite A (25%), (+)-2-[p -(2hydroxymethyl-propyl) phenyl] propionic acid and metabolite B (37%), (+)-2-[p -(2carboxypropyl)phenyl] propionic acid; the percentages of free and conjugated ibuprofen were approximately 1% and 14%, respectively.
Carefully consider the potential benefits and risks of Ibuprofen Tablets and other treatment options before deciding to use Ibuprofen Tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals [see WARNINGS].
Ibuprofen Tablets are indicated for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis.
Ibuprofen Tablets are indicated for relief of mild to moderate pain.
Ibuprofen Tablets are also indicated for the treatment of primary dysmenorrhea.
Controlled clinical trials to establish the safety and effectiveness of Ibuprofen Tablets in children have not been conducted.
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