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IDARAC®
Sanofi
Floctafenine
Anti-inflammatory - Analgesic
 
Action And Clinical Pharmacology: Floctafenine, an anthranilic acid derivative, is a nonsteroidal anti-inflammatory agent with analgesic and anti-inflammatory properties. The analgesic activity is comparable to that of other mild analgesics in the relief of acute pain. Floctafenine has been shown to inhibit in vitro biosynthesis of prostaglandins PGE2 and PGF2a. Gastrointestinal bleeding determined by daily fecal blood loss, was shown in one clinical trial to be approximately 1.2 mL after 1 600 mg/day of floctafenine compared to 10.4 mL after 2 400 mg/day of ASA.

In normal volunteers, floctafenine was well absorbed after oral administration and peak plasma levels of floctafenine acid, the active metabolite, were attained 1 to 2 hours after administration and declined in a biphasic manner, with an initial (a phase) half-life of approximately 1 hour and a later (b phase) half-life of approximately 8 hours. Floctafenine and its metabolites do not accumulate following oral administration of multiple doses.

After oral and i.v. administration of 4 labelled floctafenine, urinary excretion accounted for 40% and fecal and biliary excretion accounted for 60% of recovered radioactivity. The main urinary metabolites are floctafenic acid and its conjugate with minimal amounts of free floctafenine.

Indications And Clinical Uses: For short-term use in acute pain of mild and moderate severity.

Contra-Indications: As with other NSAIDs, floctafenine is contraindicated in patients with peptic ulcer or any other active inflammatory disease of the gastrointestinal tract.

Floctafenine should not be used where there is a known or suspected hypersensitivity to the drug. Because of the possibility of cross-sensitivity, floctafenine should not be used in patients in whom acetylsalicylic acid (ASA) or other nonsteroidal anti-inflammatory agents induce acute asthmatic attacks, urticaria, rhinitis or other allergic manifestations. Fatal anaphylactoid reactions may occur. On occasion, it has been observed that intermittent use may have resulted in increased sensitivity. Since severe cases of hypersensitivity reactions have been reported with floctafenine, its use in severe cardiac insufficiency and ischemic cardiomyopathy is contraindicated.

Manufacturers' Warnings In Clinical States: Peptic ulceration, perforation and gastrointestinal bleeding, sometimes severe and occasionally fatal, have been reported during therapy with nonsteroidal anti-inflammatory drugs and may occur with floctafenine.

Elderly and debilitated individuals are most susceptible to adverse events from nonsteroidal anti-inflammatory drugs, the incidence of which increases with dose and duration of treatment. For such individuals, consideration should be given to a starting dose lower than usual, with individual adjustment when necessary and under close supervision (see Precautions for further information).

Floctafenine should be given under close medical supervision to patients prone to gastrointestinal tract irritation, particularly those with a history of peptic ulcer, diverticulosis or other inflammatory disease of the gastrointestinal tract. In these cases the physician must weigh the benefits of treatment against the possible hazards.

Patients taking any nonsteroidal anti-inflammatory drug including floctafenine should be instructed to contact a physician immediately if they experience symptoms of signs suggestive of peptic ulceration or gastrointestinal bleeding. These reactions can occur at any time during treatment.

Pregnancy: As floctafenic acid crosses the placental barrier, the use in women of childbearing potential requires that the likely benefit of the drug be weighed against the possible risk to the mother and fetus.

Lactation: It has been shown that floctafenic acid is slightly secreted in breast milk. Therefore, use of floctafenine in women who are nursing is not recommended.

Children: Safety and efficacy in children have not been established and therefore its use in this age group is not recommended.

The safety and efficacy of long-term use have not been clearly established.

Precautions: Renal Effects: As with other drugs that inhibit prostaglandin synthesis, floctafenine should be used with caution in patients with impaired renal function. In clinical trials dysuria, without apparent changes in renal function, was reported. The incidence of dysuria was greater in males than in females and occurred primarily in the first morning voiding. It has not been established whether dysuria is related to dose and/or duration of drug administration.

Long-term administration of nonsteroidal anti-inflammatory drugs to animals has resulted in renal papillary necrosis and other abnormal renal pathology. In humans, there have been reports of acute interstitial nephritis with hematuria, proteinuria and occasionally nephrotic syndrome.

Renal toxicity has been seen in patients treated with nonsteroidal anti-inflammatory drugs who had pre-renal conditions leading to the reduction in renal blood flow or blood volume, where the renal prostaglandins have a supportive role in the maintenance of renal perfusion. In these patients, administration of a nonsteroidal anti-inflammatory drug may cause a dose-dependent reduction in prostaglandin formation and may precipitate overt renal decompensation. Patients at greatest risk of this reaction are those with impaired renal function, heart failure, liver dysfunction, those taking diuretics, and the elderly. Discontinuation of nonsteroidal anti-inflammatory therapy is usually followed by recovery to the pretreatment state.

Floctafenine and its metabolites are eliminated from plasma by the kidneys. Therefore, in patients with impaired renal function (creatine clearance <10 mL/min), lower doses of floctafenine should be used and patients monitored.

Gastrointestinal: If peptic ulceration is suspected or confirmed, or if gastrointestinal bleeding or perforation occurs, floctafenine should be discontinued, an appropriate treatment instituted and patient closely monitored.

Hepatic Effects: As with other nonsteroidal anti-inflammatory drugs, borderline elevations of one or more liver tests may occur. These abnormalities may progress, may remain essentially unchanged, or may be transient with continued therapy. A patient with symptoms and/or signs suggesting liver dysfunction, or in whom an abnormal liver test has occurred, should be evaluated for evidence of the development of more severe hepatic reactions while on therapy with this drug. Severe hepatic reactions including jaundice and cases of fatal hepatitis have been reported with nonsteroidal anti-inflammatory drugs. Although such reactions are rare, if abnormal liver tests persist or worsen, if clinical signs and symptoms consistent with liver disease develop, or if systemic manifestations occur (e.g., eosinophilia, rash, etc.), floctafenine should be discontinued.

If floctafenine is to be used in the presence of impaired liver function, it must be done under strict observation.

Fluid and Electrolyte Balance: Fluid retention and edema have been observed in patients treated with floctafenine. Therefore, as with many other nonsteroidal anti-inflammatory drugs, the possibility of precipitating congestive heart failure in elderly patients or in those with compromised cardiac function should be borne in mind. Floctafenine should be used with caution in patients with heart failure, hypertension or other conditions predisposing to fluid retention.

Hematology: Drugs inhibiting prostaglandin biosynthesis do interfere with platelet function to some degree; therefore, patients who may be adversely affected by such an action should be carefully observed when floctafenine is administered.

Blood dyscrasias associated with the use of nonsteroidal anti-inflammatory drugs are rare, but could have severe consequences.

Infection: In common with other anti-inflammatory drugs, floctafenine may mask the usual signs of infection.

Geriatrics: As with other NSAIDs, floctafenine should be used with caution in the elderly, and the dosage adjusted individually (see Warnings).

Drug Interactions: Nonsteroidal anti-inflammatory drugs are known to be extensively bound to serum albumin. This may lead to interaction with anticoagulants, sulfonylurea, hypoglycemic agents, sulfonamides, phenytoin, lithium and certain chemotherapeutic agents such as methotrexate. Therefore, caution should be observed when these drugs are used concurrently.

Floctafenine may cause water retention and therefore could interfere with diuretics in the treatment of hypertension.

Concomitant administration of acetylsalicylic acid results in decreased peak serum concentration of nonsteroidal anti-inflammatory drugs and slight increases in both clearance and apparent half-life. The clinical significance of these changes is unknown.

In patients receiving concomitant steroid therapy, any reduction in steroid dosage should be gradual to avoid the possible complications of sudden steroid withdrawal.

No interaction with antacids has been observed.

Adverse Reactions: The most commonly occurring side effects reported during therapy were:

CNS: drowsiness, dizziness, headache, insomnia, nervousness, irritability.

Gastrointestinal: nausea, diarrhea, abdominal pain or discomfort, heartburn, constipation, abnormal liver function, gastrointestinal bleeding.

Urogenital: dysuria, burning micturition, polyuria, strong smelling urine, urethritis and cystitis.

Other less frequently occurring side effects were: tinnitus, blurred vision, dry mouth, thirst, bitter taste, anorexia, stomach cramps, flatulence, hot flushes and sweating, tachycardia, weakness and tiredness.

Allergic-type Reactions: maculopapular skin rash, pruritus, urticaria, redness and itching of the face and neck. Cases of anaphylactic shock and angioedema have been reported in clinical use.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: A few cases of overdose have been reported with floctafenine. No common symptoms resulting from overdosing could be distinguished among these patients. In all cases the outcome was favorable and the patients recovered well. Standard procedures to evacuate gastric contents, maintain urinary output and provide general supportive care should be employed in cases of overdose. tag_DosageDosage

Dosage And Administration: Adults: 200 to 400 mg every 6 to 8 hours as required. The maximum recommended daily dose is 1 200 mg. Floctafenine is recommended for short-term management of acute pain.

The tablets should be taken with a glass of water.

Floctafenine is not recommended for use in children.



SuppliedSupplied: 200 mg: Each round, biconvex, creamy white tablet, with "W" on one side and "I" with "200" below on the other, contains: floctafenine 200 mg. Nonmedicinal ingredients: cellulose microcrystalline, cornstarch, docusate sodium, magnesium stearate and povidone. Gluten-, lactose-, sucrose-, sulfite- and tartrazine-free. Energy: 0.88 kJ (0.21 kcal). Bottles of 100 and 500.

400 mg: Each round, biconvex, creamy white tablet, with "W" on one side and "I" with "400" below on the other, contains: floctafenine 400 mg. Nonmedicinal ingredients: cellulose microcrystalline, cornstarch, docusate sodium, magnesium stearate and povidone. Gluten-, lactose-, sucrose-, sulfite- and tartrazine-free. Energy 1.72 kJ (0.41 kcal). Bottles of 100 and 500.

Store at room temperature, protect from light. (Shown in Product Recognition Section)