Motrin Information
Motrin (Ibuprofen) Description
Motrin (Ibuprofen) tablets contain the active ingredient ibuprofen, which is (±) - 2 - (isobutylphenyl) propionic acid. Ibuprofen is a white powder with a melting point of 74-77° C and is very slightly soluble in water (
The structural formula is represented below:
Motrin (Ibuprofen) tablets, a nonsteroidal anti-inflammatory drug (NSAID), is available in 400 mg, 600 mg, and 800 mg tablets for oral administration. Inactive ingredients: carnauba wax, colloidal silicon dioxide, croscarmellose sodium, hypromellose, lactose, magnesium stearate, microcrystalline cellulose, propylene glycol, titanium dioxide.
Motrin (Ibuprofen) Clinical Pharmacology
Motrin (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, Motrin (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 ). Motrin (Ibuprofen) tablets may be well tolerated in some patients who have had gastrointestinal side effects with aspirin, but these patients when treated with Motrin (Ibuprofen) tablets should be carefully followed for signs and symptoms of gastrointestinal ulceration and bleeding. Although it is not definitely known whether Motrin (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 Motrin (Ibuprofen) tablets whereas frank ulceration was reported in 13 patients in the aspirin group (statistically significant p<.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 Cr-tagged red cells indicate that fecal blood loss associated with Motrin (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, Motrin (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 ) and CNS side effects.
Motrin (Ibuprofen) tablets may be used in combination with gold salts and/or corticosteroids.
Controlled studies have demonstrated that Motrin (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, Motrin (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.
The ibuprofen in Motrin (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 Motrin (Ibuprofen) tablets either under fasting conditions or immediately before meals yields quite similar serum ibuprofen concentration-time profiles. When Motrin (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 Motrin (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-[-(2hydroxymethyl-propyl) phenyl] propionic acid and metabolite B (37%), (+)-2-[-(2carboxypropyl)phenyl] propionic acid; the percentages of free and conjugated ibuprofen were approximately 1% and 14%, respectively.
Motrin (Ibuprofen) Indications And Usage
Carefully consider the potential benefits and risks of Motrin (Ibuprofen) tablets and other treatment options before deciding to use Motrin (Ibuprofen) . Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals (see ).
Motrin (Ibuprofen) tablets are indicated for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis.
Motrin (Ibuprofen) tablets are indicated for relief of mild to moderate pain.
Motrin (Ibuprofen) tablets are also indicated for the treatment of primary dysmenorrhea.
Controlled clinical trials to establish the safety and effectiveness of Motrin (Ibuprofen) tablets in children have not been conducted.
Motrin (Ibuprofen) Contraindications
Motrin (Ibuprofen) tablets are contraindicated in patients with known hypersensitivity to Ibuprofen.
Motrin (Ibuprofen) tablets should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients (see , and ).
Motrin (Ibuprofen) tablets are contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery (see ).
Motrin (Ibuprofen) Warnings
NSAIDs, including Motrin (Ibuprofen) tablets, can cause serious gastrointestinal (GI) adverse events including inflammation, bleeding, ulceration, and perforation of the stomach, small intestine, or large intestine, which can be fatal. These serious adverse events can occur at any time, with or without warning symptoms, in patients treated with NSAIDs. Only one in five patients, who develop a serious upper GI adverse event on NSAID therapy, is symptomatic. Upper GI ulcers, gross bleeding, or perforation caused by NSAIDs occur in approximately 1% of patients treated for 3-6 months, and in about 2-4% of patients treated for one year. These trends continue with longer duration of use, increasing the likelihood of developing a serious GI event at some time during the course of therapy. However, even short-term therapy is not without risk. NSAIDs should be prescribed with extreme caution in those with a prior history of ulcer disease or gastrointestinal bleeding. Patients with a who use NSAIDs have a greater than 10-fold increased risk for developing a GI bleed compared to patients treated with neither of these risk factors. Other factors that increase the risk of GI bleeding in patients treated with NSAIDs include concomitant use of oral corticosteroids or anticoagulants, longer duration of NSAID therapy, smoking, use of alcohol, older age, and poor general health status. Most spontaneous reports of fatal GI events are in elderly or debilitated patients and therefore, special care should be taken in treating this population.
To minimize the potential risk for an adverse GI event in patients treated with an NSAID, the lowest effective dose should be used for the shortest possible duration. Patients and physicians should remain alert for signs and symptoms of GI ulcerations and bleeding during NSAID therapy and promptly initiate additional evaluation and treatment if a serious GI event is suspected. This should include discontinuation of the NSAID until a serious GI adverse event is ruled out. For high-risk patients, alternate therapies that do not involve NSAIDs should be considered.
Motrin (Ibuprofen) Precautions
Motrin (Ibuprofen) tablets cannot be expected to substitute for corticosteroids or to treat corticosteroid insufficiency. Abrupt discontinuation of corticosteroids may lead to disease exacerbation. Patients on prolonged corticosteroid therapy should have their therapy tapered slowly if a decision is made to discontinue corticosteroids.
The pharmacological activity of Motrin (Ibuprofen) tablets in reducing fever and inflammation may diminish the utility of these diagnostic signs in detecting complications of presumed noninfectious, painful conditions.
Borderline elevations of one or more liver tests may occur in up to 15% of patients taking NSAIDs, including Motrin (Ibuprofen) tablets. These laboratory abnormalities may progress, may remain unchanged, or may be transient with continuing therapy. Notable elevations of ALT or AST (approximately three or more times the upper limit of normal) have been reported in approximately 1% of patients in clinical trials with NSAIDs. In addition, rare cases of severe hepatic reactions, including jaundice, fulminant hepatitis, liver necrosis, and hepatic failure, some of them with fatal outcomes have been reported.
A patient with symptoms and/or signs suggesting liver dysfunction, or with abnormal liver test values, should be evaluated for evidence of the development of a more severe hepatic reaction while on therapy with Motrin (Ibuprofen) tablets. If clinical signs and symptoms consistent with liver disease develop, or if systemic manifestations occur (e.g., eosinophilia, rash, etc.), Motrin (Ibuprofen) tablets should be discontinued.
Anemia is sometimes seen in patients receiving NSAIDs, including Motrin (Ibuprofen) tablets. This may be due to fluid retention, occult or gross GI blood loss, or an incompletely described effect upon erythropoiesis. Patients on long-term treatment with NSAIDs, including Motrin (Ibuprofen) tablets, should have their hemoglobin or hematocrit checked if they exhibit any signs or symptoms of anemia.
In two postmarketing clinical studies the incidence of a decreased hemoglobin level was greater than previously reported. Decrease in hemoglobin of 1 gram or more was observed in 17.1% of 193 patients on 1600 mg ibuprofen daily (osteoarthritis), and in 22.8% of 189 patients taking 2400 mg of ibuprofen daily (rheumatoid arthritis). Positive stool occult blood tests and elevated serum creatinine levels were also observed in these studies.
NSAIDs inhibit platelet aggregation and have been shown to prolong bleeding time in some patients. Unlike aspirin, their effect on platelet function is quantitatively less, of shorter duration, and reversible.
Patients receiving Motrin (Ibuprofen) tablets who may be adversely affected by alterations in platelet function, such as those with coagulation disorders or patients receiving anticoagulants should be carefully monitored.
Patients should be informed of the following information before initiating therapy with an NSAID and periodically during the course of ongoing therapy. Patients should also be encouraged to read the NSAID Medication Guide that accompanies each prescription dispensed.
Motrin (Ibuprofen) Adverse Reactions
The most frequent type of adverse reaction occurring with Motrin (Ibuprofen) tablets is gastrointestinal. In controlled clinical trials the percentage of patients reporting one or more gastrointestinal complaints ranged from 4% to 16%.
In controlled studies when Motrin (Ibuprofen) tablets were compared to aspirin and indomethacin in equally effective doses, the overall incidence of gastrointestinal complaints was about half that seen in either the aspirin- or indomethacin-treated patients.
Adverse reactions observed during controlled clinical trials at an incidence greater than 1% are listed in the table. Those reactions listed in Column one encompass observations in approximately 3,000 patients. More than 500 of these patients were treated for periods of at least 54 weeks.
Still other reactions occurring less frequently than 1 in 100 were reported in controlled clinical trials and from marketing experience. These reactions have been divided into two categories: Column two of the table lists reactions with therapy with Motrin (Ibuprofen) tablets where the probability of a causal relationship exists: for the reactions in Column three, a causal relationship with Motrin (Ibuprofen) tablets has not been established.
Reported side effects were higher at doses of 3200 mg/day than at doses of 2400 mg or less per day in clinical trials of patients with rheumatoid arthritis. The increases in incidence were slight and still within the ranges reported in the table.
Motrin (Ibuprofen) Overdosage
Approximately 1½ hours after the reported ingestion of from 7 to 10 Motrin (Ibuprofen) tablets (400 mg), a 19-month old child weighing 12 kg was seen in the hospital emergency room, apneic and cyanotic, responding only to painful stimuli. This type of stimulus, however, was sufficient to induce respiration. Oxygen and parenteral fluids were given; a greenish-yellow fluid was aspirated from the stomach with no evidence to indicate the presence of ibuprofen. Two hours after ingestion the child's condition seemed stable; she still responded only to painful stimuli and continued to have periods of apnea lasting from 5 to 10 seconds. She was admitted to intensive care and sodium bicarbonate was administered as well as infusions of dextrose and normal saline. By four hours post-ingestion she could be aroused easily, sit by herself and respond to spoken commands. Blood level of ibuprofen was 102.9 µg/mL approximately 8½ hours after accidental ingestion. At 12 hours she appeared to be completely recovered.
In two other reported cases where children (each weighing approximately 10 kg) accidentally, acutely ingested approximately 120 mg/kg, there were no signs of acute intoxication or late sequelae. Blood level in one child 90 minutes after ingestion was 700 µg/mL — about 10 times the peak levels seen in absorption-excretion studies.
A 19-year old male who had taken 8,000 mg of ibuprofen over a period of a few hours complained of dizziness, and nystagmus was noted. After hospitalization, parenteral hydration and three days bed rest, he recovered with no reported sequelae.
In cases of acute overdosage, the stomach should be emptied by vomiting or lavage, though little drug will likely be recovered if more than an hour has elapsed since ingestion. Because the drug is acidic and is excreted in the urine, it is theoretically beneficial to administer alkali and induce diuresis. In addition to supportive measures, the use of oral activated charcoal may help to reduce the absorption and reabsorption of Motrin (Ibuprofen) tablets.
Motrin (Ibuprofen) Dosage And Administration
Carefully consider the potential benefits and risks of Motrin (Ibuprofen) tablets and other treatment options before deciding to use Motrin (Ibuprofen) tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals (see ).
After observing the response to initial therapy with Motrin (Ibuprofen) tablets, the dose and frequency should be adjusted to suit an individual patient's needs.
Do not exceed 3200 mg total daily dose. If gastrointestinal complaints occur, administer Motrin (Ibuprofen) tablets with meals or milk.
Motrin (Ibuprofen) How Supplied
Motrin (Ibuprofen) tablets are available in the following strengths, colors and sizes:
Bottles of 100 NDC 0009-7385-01
Bottles of 500 NDC 0009-7385-02
Unit dose blister of 100 NDC 0009-7385-04
Bottles of 90 NDC 0009-7386-05
Bottles of 100 NDC 0009-7386-01
Bottles of 270 NDC 0009-7386-09
Bottles of 500 NDC 0009-7386-02
Unit dose blister of 100 NDC 0009-7386-04
Bottles of 100 NDC 0009-7387-01
Bottles of 270 NDC 0009-7387-08
Bottles of 500 NDC 0009-7387-02
Unit dose blister of 100 NDC 0009-7387-04
Motrin (Ibuprofen)
