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Flurbiprofen (Tablet, Film Coated)

Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1931

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Flurbiprofen (Tablet, Film Coated)
dailymed-instance:dosage
Carefully consider the potential benefits and risks of FLURBIPROFEN Tablets and other treatment options before deciding to use FLURBIPROFEN Tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals . After observing the response to initial therapy with FLURBIPROFEN Tablets, the dose and frequency should be adjusted to suit an individual patient's needs. For relief of the signs and symptoms of rheumatoid arthritis or osteoarthritis, the recommended starting dose of Flurbiprofen Tablets is 200 to 300 mg per day, divided for administration two, three, or four times a day. The largest recommended single dose in a multiple-dose daily regimen is 100 mg.
dailymed-instance:descripti...
Flurbiprofen is a member of the phenylalkanoic acid derivative group of nonsteroidal anti-inflammatory drugs. Flurbiprofen Tablets are white, oval, film coated tablets for oral administration. Flurbiprofen is a racemic mixture of (+)S- and (-)R- enantiomers. Flurbiprofen is a white or slightly yellow crystalline powder. It is slightly soluble in water at pH 7.0 and readily soluble in most polar solvents. The chemical name is [1,1'-biphenyl]-4-acetic acid, 2-fluoro-alpha-methyl-, (��)-. The molecular weight is 244.26. Its molecular formula is CHFOand it has the following structural formula: The inactive ingredients in flurbiprofen (both strengths) include carnauba wax, colloidal silicon dioxide, croscarmellose sodium, hypromellose, lactose, magnesium stearate, microcrystalline cellulose, propylene glycol, and titanium dioxide. In addition, the 100 mg tablet contains FD&C Blue No. 2.
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Pharmacodynamics: Flurbiprofen Tablets contain flurbiprofen, a nonsteroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of flurbiprofen, like that of other nonsteroidal anti-inflammatory drugs, is not completely understood but may be related to prostaglandin synthetase inhibition.<br/>Pharmacokinetics:<br/>Absorption: The mean oral bioavailability of flurbiprofen from Flurbiprofen Tablets 100 mg is 96% relative to an oral solution. Flurbiprofen is rapidly and non-stereoselectively absorbed, with peak plasma concentrations occurring at about 2 hours (see Table 1). Administration of Flurbiprofen Tablets with either food or antacids may alter the rate but not the extent of flurbiprofen absorption. Ranitidine has been shown to have no effect on either the rate or extent of flurbiprofen absorption.<br/>Distribution: The apparent volume of distribution (Vz/F) of both R- and S-flurbiprofen is approximately 0.12 L/Kg. Both flurbiprofen enantiomers are more than 99% bound to plasma proteins, primarily albumin. Plasma protein binding is relatively constant for the typical average steady-state concentrations (���10��g/mL) achieved with recommended doses. Flurbiprofen is poorly excreted into human milk. The nursing infant dose is predicted to be approximately 0.1 mg/day in the established milk of a woman taking Flurbiprofen Tablets 200 mg/day .<br/>Metabolism: Several flurbiprofen metabolites have been identified in human plasma and urine. These metabolites include 4'-hydroxy-flurbiprofen, 3',4' dihydroxy-flurbiprofen, 3'-hydroxy-4'-methoxy-flurbiprofen, their conjugates, and conjugated flurbiprofen. Unlike other aryl propionic acid derivatives (eg, ibuprofen), metabolism of R-flurbiprofen to S-flurbiprofen is minimal. In vitro studies have demonstrated that cytochrome P450 2C9 plays an important role in the metabolism of flurbiprofen to its major metabolite, 4'-hydroxy-flurbiprofen. The 4'-hydroxy-flurbiprofen metabolite showed little anti-inflammatory activity in animal models of inflammation. Flurbiprofen does not induce enzymes that alter its metabolism. The total plasma clearance of unbound flurbiprofen is not stereoselective, and clearance of flurbiprofen is independent of dose when used within the therapeutic range<br/>Excretion: Following dosing with Flurbiprofen Tablets, less than 3% of flurbiprofen is excreted unchanged in the urine, with about 70% of the dose eliminated in the urine as parent drug and metabolites. Because renal elimination is a significant pathway of elimination of flurbiprofen metabolites, dosing adjustment in patients with moderate or severe renal dysfunction may be necessary to avoid accumulation of flurbiprofen metabolites. The mean terminal disposition half-lives (t 1/2) of R- and S-flurbiprofen are similar, about 4.7 and 5.7 hours, respectively. There is little accumulation of flurbiprofen following multiple doses<br/>Special Populations:<br/>Pediatric: The pharmacokinetics of flurbiprofen has not been investigated in pediatric patients.<br/>Race: No pharmacokinetic differences due to race have been identified<br/>Geriatric: Flurbiprofen pharmacokinetics was similar in geriatric arthritis patients, younger arthritis patients, and young healthy volunteers receiving Flurbiprofen Tablets 100 mg as either single or multiple doses.<br/>Hepatic insufficiency: Hepatic metabolism may account for>90% of flurbiprofen elimination, so patients with hepatic disease may require reduced doses of Flurbiprofen Tablets compared to patients with normal hepatic function. The pharmacokinetics of R- and S-flurbiprofen were similar, however, in alcoholic cirrhosis patients (N=8) and young healthy volunteers (N=8) following administration of a single 200 mg dose of Flurbiprofen Tablets. Flurbiprofen plasma protein binding may be decreased in patients with liver disease and serum albumin concentrations below 3.1 g/dL .<br/>Renal insufficiency: Renal clearance is an important route of elimination for flurbiprofen metabolites, but a minor route of elimination for unchanged flurbiprofen (���3% of total clearance). The unbound clearances of R- and S-flurbiprofen did not differ significantly between normal healthy volunteers (N=6, 50 mg single dose) and patients with renal impairment (N=8, inulin clearances ranging from 11 to 43 mL/min, 50 mg multiple doses). Flurbiprofen plasma protein binding may be decreased in patients with renal impairment and serum albumin concentrations below 3.9 g/dL. Elimination of flurbiprofen metabolites may be reduced in patients with renal impairment . Flurbiprofen is not significantly removed from the blood into dialysate in patients undergoing continuous ambulatory peritoneal dialysis.<br/>Drug-Drug Interactions:<br/>Antacids: Administration of Flurbiprofen Tablets to volunteers under fasting conditions or with antacid suspension yielded similar serum flurbiprofen-time profiles in young adult subjects (n=12). In geriatric subjects (n=7), there was a reduction in the rate but not the extent of flurbiprofen absorption.<br/>Aspirin: Concurrent administration of Flurbiprofen Tablets and aspirin resulted in 50% lower serum flurbiprofen concentrations. This effect of aspirin (which is also seen with other nonsteroidal anti-inflammatory drugs) has been demonstrated in patients with rheumatoid arthritis (n=15) and in healthy volunteers (n=16) .<br/>Beta-adrenergic blocking agents: The effect of flurbiprofen on blood pressure response to propranolol and atenolol was evaluated in men with mild uncomplicated hypertension (n=10). Flurbiprofen pretreatment attenuated the hypotensive effect of a single dose of propranolol but not atenolol. Flurbiprofen did not appear to affect the beta-blocker-mediated reduction in heart rate. Flurbiprofen did not affect the pharmacokinetic profile of either drug .<br/>Cimetidine, Ranitidine: In normal volunteers (n=9), pretreatment with cimetidine or ranitidine did not affect flurbiprofen pharmacokinetics, except for a small (13%) but statistically significant increase in the area under the serum concentration curve of flurbiprofen in subjects who received cimetidine.<br/>Digoxin: In studies of healthy males (n=14), concomitant administration of flurbiprofen and digoxin did not change the steady state serum levels of either drug.<br/>Diuretics: Studies in healthy volunteers have shown that, like other nonsteroidal anti-inflammatory drugs, flurbiprofen can interfere with the effects of furosemide. Although results have varied from study to study, effects have been shown on furosemide-stimulated diuresis, natriuresis, and kaliuresis. Other nonsteroidal anti-inflammatory drugs that inhibit prostaglandin synthesis have been shown to interfere with thiazide and potassium-sparing diuretics .<br/>Lithium: In a study of 11 women with bipolar disorder receiving lithium carbonate at a dosage of 600 to 1200 mg/day, administration of 100 mg Flurbiprofen Tablets every 12 hours increased plasma lithium concentrations by 19%. Four of 11 patients experienced a clinically important increase (>25% or>0.2 mmol/L). Nonsteroidal anti-inflammatory drugs have also been reported to decrease the renal clearance of lithium by about 20% .<br/>Methotrexate: In a study of six adult arthritis patients, coadministration of methotrexate (10 to 25 mg/dose) and Flurbiprofen Tablets (300 mg/day) resulted in no observable interaction between these two drugs.<br/>Oral Hypoglycemic Agents: In a clinical study, flurbiprofen was administered to adult diabetics who were already receiving glyburide (n=4), metformin (n=2), chlorpropamide with phenformin (n=3), or glyburide with phenformin (n=6). Although there was a slight reduction in blood sugar concentrations during concomitant administration of flurbiprofen and hypoglycemic agents, there were no signs or symptoms of hypoglycemia.
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Flurbiprofen Tablets are available as follows: 100 mg: blue, oval, film-coated, imprinted G3724 Bottles of 100 NDC 59762-3724-1 Bottles of 500 N DC 59762-3724-3 Store at controlled room temperature 20��to 25��C(68��to 77��F) [see USP].
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Cardiovascular Risk:<br/>Gastrointestinal Risk:
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General: FLURBIPROFEN 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 FLURBIPROFEN Tablets in reducing fever and inflammation may diminish the utility of these diagnostic signs in detecting complications of presumed noninfectious, painful conditions.<br/>Hepatic effects: Borderline elevations of one or more liver tests may occur in up to 15% of patients taking NSAIDs, including FLURBIPROFEN 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 reportedin 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 FLURBIPROFEN Tablets. If clinical signs and symptomsconsistent with liver disease develop, or if systemic manifestations occur (e.g., eosinophilia, rash, etc.), FLURBIPROFEN Tablets should be discontinued.<br/>Renal effects: Caution should be used when initiating treatment with FLURBIPROFEN in patients with considerable dehydration. It is advisable to rehydrate patients first and then start therapy with FLURBIPROFEN Tablets. Caution is also recommended in patients with pre-existing kidney disease . In clinical studies, the elimination half-life of flurbiprofen was unchanged in patients with renal impairment. Flurbiprofen metabolites are eliminated primarily by the kidneys. Elimination of 4'-hydroxyflurbiprofen was reduced in patients with moderate to severe renal impairment. Therefore, patients with significantly impaired renal function may require a reduction of dosage to avoid accumulation of flurbiprofen metabolites. Such patients should be closely monitored .<br/>Hematological effects: Anemia is sometimes seen in patients receiving NSAIDs, including FLURBIPROFEN. 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 FLURBIPROFEN, should have their hemoglobin or hematocrit checked if they exhibit any signs or symptoms of anemia. 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. FLURBIPROFEN does not generally affect platelet counts, prothrombin time (PT), or partial thromboplastin time (PTT) Patients receiving FLURBIPROFEN who may be adversely affected by alterations in platelet function, such as those with coagulation disorders or patients receiving anticoagulants should be carefully monitored.<br/>Preexisting asthma: Patients with asthma may have aspirin-sensitive asthma. The use of aspirin in patients with aspirin-sensitive asthma has been associated with severe bronchospasm, which can be fatal. Since cross reactivity, including bronchospasm, between aspirin and NSAIDs has been reported in such aspirin-sensitive patients, FLURBIPROFEN Tablets should not be administered to patients with this form of aspirin sensitivity and should be used with caution in patients with preexisting asthma.<br/>Vision changes: Blurred and /or diminished vision has been reported with the use of Flurbiprofen Tablets and other nonsteroidal anti-inflammatory drugs. Patients experiencing eye complaints should have ophthalmologic examinations.<br/>Information For Patients: 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.<br/>Laboratory Tests: Because serious GI tract ulcerations and bleeding can occur without warning symptoms, physicians should monitor for signs of symptoms of GI bleeding. Patients on long-term treatment with nonsteroidal anti-inflammatory drugs should have their CBC and chemistry profile checked periodically. If clinical signs and symptoms consistent with liver or renal disease develop, systemic manifestations occur (eg, eosinophilia, rash etc.), or abnormal liver tests persist or worsen, Flurbiprofen tablets should be discontinued.<br/>Drug Interactions:<br/>ACE-inhibitors: Reports suggest that nonsteroidal anti-inflammatory drugs may diminish the antihypertensive effect of ACE-inhibitors. This interaction should be given consideration in patients taking nonsteroidal anti-inflammatory drugs concomitantly with ACE-inhibitors.<br/>Anticoagulants: The effects of warfarin and NSAIDs on GI bleeding are synergistic, such that users of both drugs together have a risk of serious GI bleeding higher than users of either drug alone. The physician should be cautious when administering Flurbiprofen tablets to patients taking warfarin or other anticoagulants.<br/>Aspirin: Concurrent administration of aspirin lowers serum flurbiprofen concentrations . When FLURBIPROFEN Tablets is administered with aspirin, its protein binding is reduced, although the clearance of free FLURBIPROFEN is not altered. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of FLURBIPROFEN and aspirin is not generally recommended because of the potential for increased adverse effects.<br/>Beta-adrenergic blocking agents: Flurbiprofen attenuated the hypotensive effect of propranolol but not atenolol . The mechanism underlying this interference is unknown. Patients taking both flurbiprofen and a beta-blocker should be monitored to ensure that a satisfactory hypotensive effect is achieved.<br/>Diuretics: Clinical studies, as well as post marketing observations, have shown that FLURBIPROFEN can reduce the natriuretic effect-of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, the patient should be observed closely for signs of renal failure , as well as diuretic efficacy.<br/>Lithium: NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. The mean minimum lithium concentration increased 15% and the renal clearance was decreased by approximately 20%. These effects have been attributed to inhibition of renal prostaglandin synthesis by the NSAID. Thus, when NSAIDs and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity.<br/>Methotrexate: NSAIDs have been reported to competitively inhibit methotrexate accumulation in rabbit kidney slices. This may indicate that they could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.<br/>Pregnancy:<br/>Teratogenic effects: Pregnancy Category C: Reproductive studies conducted in rats and rabbits have not demonstrated evidence of developmental abnormalities. However, animal reproduction studies are not always predictive of human response. There are no adequate and well-controlled studies in pregnant women.<br/>Nonteratogenic effects: Because of the known effects of nonsteroidal anti-inflammatory drugs on the fetal cardiovascular system (closure of ductus arteriosus), use during late pregnancy should be avoided.<br/>Labor and Delivery: In rat studies withNSAIDs, as with other drugs known to inhibit prostaglandin synthesis, an increased incidence of dystocia, delayed parturition, and decreased pup survival occurred. The effects of Flurbiprofen Tablets on labor and delivery in pregnant women are unknown.<br/>Nursing Mothers: Concentrations of flurbiprofen in breast milk and plasma of nursing mothers suggest that a nursing infant could receive approximately 0.10 mg flurbiprofen per day in the established milk of a woman taking Flurbiprofen Tablets 200 mg/day. Because of possible adverse effects of prostaglandin-inhibiting drugs on neonates, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.<br/>Pediatric Use: Safety and effectiveness in pediatric patients have not been established.<br/>Geriatric Use: As with any NSAID, caution should be exercised in treating the elderly (65 years and older). Clinical experience with Flurbiprofen Tablets suggests that elderly patients may have a higher incidence of gastrointestinal complaints than younger patients, including ulceration, bleeding, flatulence, bloating, and abdominal pain. To minimize the potential risk for gastrointestinal events, the lowest effective dose should be used for the shortest possible duration . Likewise, elderly patients are at greater risk of developing renal decompensation . The pharmacokinetics of flurbiprofen does not seem to differ in elderly patients from those in younger individuals . The rate of absorption of Flurbiprofen Tablets was reduced in elderly patients who also received antacids, although the extent of absorption was not affected .
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Symptoms following acute overdoses with nonsteroidal anti-inflammatory drugs are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare. Anaphylactoid reactions have been reported with therapeutic ingestion of nonsteroidal anti-inflammatory drugs, and may occur following anoverdose. Patients should be managed by symptomatic and supportive care following overdose with a nonsteroidal anti-inflammatory drug. There are no specific antidotes. Emesis and/or activated charcoal (60 to 100 g in adults, 1 to 2 g/kg in children) and/or osmotic cathartic may be indicated in patients seen within 4 hours of ingestion with symptoms, or following a large overdose (5 to 10 times the usual dose). Forced diuresis, alkalization of urine, hemodialysis, or hemo-perfusion maynot be useful due to high protein binding.
dailymed-instance:genericMe...
flurbiprofen
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Flurbiprofen (Tablet, Film Coated)
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Carefully consider the potential benefits and risks of FLURBIPROFEN Tablets and other treatment options before deciding to use FLURBIPROFEN Tablets. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals . FLURBIPROFEN Tablets is indicated:
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dailymed-instance:name
Flurbiprofen