Felxicam

Felxicam is 4-Hydroxy-2-methyl-N-2-pyridinyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, an oxicam. Members of the oxicam family are not carboxylic acids, but they are acidic by virtue of the enolic 4-hydroxy substituent. Felxicam occurs as a white crystalline solid, sparingly soluble in water, dilute acid and most organic solvents. It is slightly soluble in alcohols and in aqueous alkaline solution. It exhibits a weakly acidic 4-hydroxy proton (pKa 5.1) and a weakly basic pyridyl nitrogen (pKa 1.8).

It has a molecular formula of C₁₅H₁₃N₃O₄S and molecular weight of 331.35.

Carefully consider the potential benefits and risks of Felxicam and other treatment options before deciding to use Felxicam. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.

Felxicam is indicated:

• For relief of the signs and symptoms of osteoarthritis.
• For relief of the signs and symptoms of rheumatoid arthritis.

Felxicam is in a group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). Felxicam works by reducing hormones that cause inflammation and pain in the body.

Felxicam is used to treat pain or inflammation caused by arthritis.

Felxicam may also be used for other purposes not listed in this medication guide.

Undesirable effects may be minimized by using the minimum effective dose for the shortest duration necessary to control symptoms.

Rheumatoid Arthritis, Osteoarthritis (Arthrosis, Degenerative Joint Disease) and Ankylosing Spondylitis: The recommended starting dose 20 mg given as a single daily dose. The majority of patients will be maintained on 20 mg daily. A relatively small group of patients may be maintained on 10 mg daily.

Acute Gout: Because of its GI safety profile, Felxicam should not be used in first-line treatment for acute gout when an NSAID is indicated. For same reason, it should be used to treat acute gout in patients most at risk of developing serious GI adverse events. Therapy should be initiated by a single dose of 40 mg, followed on the next 4-6 days with 40 mg daily, given in single or divided doses. Felxicam is not indicated for the long term management of gout.

Acute Musculoskeletal Disorders: Because of its GI safety profile, Felxicam should not be used in first-line treatment for acute musculoskeletal disorders when an NSAID is indicated. For the same reason, it should not be used to treat acute musculoskeletal disorders in patients most at risk of developing serious GI adverse events. Therapy should be initiated with 40 mg daily for the first two days given in single or divided doses. For the remainder of the 7 to 14 day treatment period, the dose should be reduced to 20 mg daily.

Postoperative and Post-traumatic Pain: The recommended dose is 20 mg given in a single daily dose.

Dysmenorrhea: Because of its GI safety profile, Felxicam should not be used in first-line treatment for dysmenorrhea when NSAID is indicated. For the same reason, it should not be used to treat dysmenorrhea in patients most at risk of developing serious GI adverse events. The treatment of primary dysmenorrhea is initiated at the earliest onset of symptoms with a recommended starting dose of 40 mg given in a single daily dose for the first two days. Treatment may be continued thereafter with a single daily dose of 20 mg for the next one to three days as necessary.

Upper Respiratory Tract Inflammation: The adult dosage is 10 mg or 20 mg once daily for five to seven days.

Juvenile Rheumatoid Arthritis (JRA): The recommended dosage for children with JRA are based on body weight as follows: Children less than or equal to 15 kg: 5 mg. 16 to 25 kg: 10 mg. 26 to 45 kg: 15 mg. Greater than or equal to 46 kg: 20 mg.

The drug should be taken once daily. The dispersible tablet may be used to obtain the exact dose required.

Administration:

Oral (Capsules, Fast Dissolving): Felxicam (Felxicam Flash) fast-dissolving tablets may be swallowed with water or placed on the tongue to disperse and then swallowed with saliva or water as a suspension. Felxicam fast-dissolving tablet dissolves almost instantly in the mouth in the presence of water or saliva.

Combined Administration: The total daily dosage of Felxicam administered as capsule and fast dissolving tablet should not exceed the maximum recommended daily dosage as indicated previously.

See also:
What is the most important information I should know about Felxicam?

This medicine can increase your risk of life-threatening heart or circulation problems, including heart attack or stroke. This risk will increase the longer you use Felxicam. Do not use this medicine just before or after having heart bypass surgery (also called coronary artery bypass graft, or CABG).

Seek emergency medical help if you have symptoms of heart or circulation problems, such as chest pain, weakness, shortness of breath, slurred speech, or problems with vision or balance.

This medicine can also increase your risk of serious effects on the stomach or intestines, including bleeding or perforation (forming of a hole). These conditions can be fatal and gastrointestinal effects can occur without warning at any time while you are taking Felxicam. Older adults may have an even greater risk of these serious gastrointestinal side effects.

Call your doctor at once if you have symptoms of bleeding in your stomach or intestines. This includes black, bloody, or tarry stools, or coughing up blood or vomit that looks like coffee grounds.

Do not use any other over-the-counter cold, allergy, or pain medication without first asking your doctor or pharmacist. Many medicines available over the counter contain aspirin or other medicines similar to Felxicam (such as ibuprofen, ketoprofen, or naproxen). If you take certain products together you may accidentally take too much of this type of medication. Read the label of any other medicine you are using to see if it contains aspirin, ibuprofen, ketoprofen, or naproxen.

Do not drink alcohol while taking Felxicam. Alcohol can increase the risk of stomach bleeding caused by Felxicam.

Avoid exposure to sunlight or artificial UV rays. Felxicam can make your skin more sensitive to sunlight and sunburn may result.

Use Felxicam as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Felxicam comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Felxicam refilled.
• Take Felxicam by mouth. It may be taken with food if it upsets your stomach. This may not lower the risk of stomach or bowel problems (eg, bleeding, ulcers). Talk with your doctor if you have persistent stomach upset.
• Take Felxicam with a full glass (8 oz [240 mL]) of water as directed by your doctor.
• If you miss a dose of Felxicam and you are taking it regularly, take it as soon as possible. If it is almost time for your next dose, skip the missed dose. Go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Felxicam.

Use: Labeled Indications

Arthritis: Relief of signs and symptoms of osteoarthritis and rheumatoid arthritis.

Off Label Uses

Ankylosing spondylitis

In a systematic review and metaanalysis of trials evaluating the treatment of ankylosing spondylitis, the use of Felxicam was shown to be safe and effective (Kroon 2015). The American College of Rheumatology/Spondylitis Association of America/Spondyloarthritis Research and Treatment Network recommend NSAIDS in the treatment of ankylosing spondylitis (Ward 2016).

See also:
What other drugs will affect Felxicam?

Acetylsalicylic Acid: As with other NSAIDs, the use of Felxicam in conjunction with acetylsalicylic acid or the concomitant use of 2 NSAIDs is not recommended because data are inadequate to demonstrate that the combination produces greater improvement than that achieved with the drug alone and the potential for adverse reactions is increased.

Studies in man have shown that the concomitant administration of Felxicam and acetylsalicylic acid resulted in a reduction of plasma levels of Felxicam to about 80% of the normal values.

Felxicam interferes with the antiplatelet effect of low-dose aspirin, and thus may interfere with aspirins prophylactic treatment of cardiovascular disease.

Anticoagulants: Bleeding has been reported rarely when Felxicam has been administered to patients on coumarin type anticoagulants. Patients should be monitored closely if Felxicam and oral anticoagulants are administered together.

Felxicam, like other NSAID, decreases platelet aggregation and prolongs bleeding time. This effect should be kept in mind when bleeding times are determined.

Antacids: Concomitant administration of antacids had no effect on Felxicam plasma levels.

Antihypertensives Including Diuretics, Angiotensin-Converting Enzyme (ACE) Inhibitors and Angiotensin II Antagonists (AIIA) and β-Blockers: NSAIDs can reduce the efficacy of diuretics and other antihypertensive drugs including ACE inhibitors, AIIA and β-blockers.

In patients with impaired renal function (eg, dehydrated patients or elderly patients with the renal function compromised), the co-administration of an ACE inhibitor or an AIIA with a cyclooxygenase inhibitor can increase the deterioration of the renal function, including the possibility of acute renal failure, which is usually reversible.

The occurrence of these interactions should be considered in patients taking Felxicam with an ACE inhibitor or an AIIA and/or diuretics. Therefore, the concomitant administration of these drugs should be done with caution, especially in elderly patients. Patients should be adequately hydrated and the need to monitor the renal function should be assessed in the beginning of the concomitant treatment and periodically thereafter.

Cardiac Glycosides (Digoxin and Digitoxin): NSAIDs may exacerbate cardiac failure, reduce glomerular filtration rate (GFR) and increase plasma glycoside levels. Concomitant administration of digoxin or digitoxin had no effect on the plasma levels of Felxicam or either drug.

Cimetidine: Results of 2 separate studies indicate a slight increase in the absorption of Felxicam following cimetidine administration but no significant changes in elimination parameters. Cimetidine increases the AUC_0-120hrs and C_max of Felxicam by approximately 13-15%. Elimination rate constants and t_½ show no significant differences. The small but significant increase in absorption is unlikely to be clinically significant.

Cholestyramine: Cholestyramine has been shown to enhance the oral clearance and decrease the t_½ of Felxicam. To minimize this interaction, it is prudent to administer Felxicam at least 2 hrs before or 6 hrs after cholestyramine.

Corticosteroids: Increased risk of gastrointestinal ulceration or bleeding.

Cyclosporine: Increased risk of nephrotoxicity.

Lithium and Other Protein-Bound Agents: Felxicam is highly protein-bound and therefore, might be expected to displace other protein-bound drugs. The physician should closely monitor patients for change in dosage requirements when administering Felxicam to patients on highly protein-bound drugs. NSAID, including Felxicam, have been reported to increase steady-state plasma lithium levels. It is recommended that these levels be monitored when initiating, adjusting and discontinuing Felxicam.

Methotrexate: When methotrexate is administered concurrently with NSAIDs, including Felxicam, NSAIDs may decrease elimination of methotrexate resulting in increased plasma levels of methotrexate. Caution is advised, especially in patients receiving high doses of methotrexate.

Tacrolimus: Possible increased risk of nephrotoxicity when NSAIDs are given with tacrolimus.

See also:
What are the possible side effects of Felxicam?

Felxicam is generally well tolerated. Gastrointestinal symptoms are the most commonly encountered side effects but in most instances do not interfere with the course of therapy.

Objective evaluations of gastric mucosal appearances and intestinal blood loss show that Felxicam 20 mg/day administered either in single or divided daily doses is significantly less irritating to the gastrointestinal tract than acetylsalicylic acid.

Blood and Lymphatic System Disorders: Anemia, aplastic anemia, eosinophilia, hemolytic anemia, leucopenia, thrombocytopenia.

Immune System Disorders: Anaphylaxis, serum sickness.

Metabolism and Nutrition Disorders: Anorexia, hyperglycemia, hypoglycemia, fluid retention.

Psychiatric Disorders: Depression, dream abnormalities, hallucinations, insomnia, mental confusion, mood alterations, nervousness.

Nervous System Disorders: Aseptic meningitis, dizziness, headache, paresthesia, somnolence, vertigo.

Eye Disorders: Blurred vision, eye irritations, swollen eyes.

Ear and Labyrinth Disorders: Hearing impairment, tinnitus.

Cardiac Disorders: Palpitations.

Vascular Disorders: Vasculitis, hypertension.

Respiratory, Thoracic and Mediastinal Disorders: Bronchospasm, dyspnea, epistaxis.

Gastrointestinal Disorders: Abdominal discomfort and pain, constipation, diarrhea, epigastric distress, flatulence, gastritis, gastrointestinal bleeding (including hematemesis and melena), indigestion, nausea, pancreatitis, perforation, stomatitis, ulceration, vomiting.

Hepatobiliary Disorders: Fatal hepatitis, jaundice. Although such reactions are rare, if abnormal liver function tests persist or worsen, if clinical signs and symptoms consistent with liver disease develop, or if systemic manifestations occur (eg, eosinophilia, rash), Felxicam should be discontinued.

Reproductive System and Breast Disorders: Decreased female fertility.

Skin and Subcutaneous Tissue Disorders: Alopecia, angioedema, dermatitis exfoliative, erythema multiforme, non-thrombocytopenic purpura (Henoch-Schonlein), onycholysis, photoallergic reactions, pruritus, skin rash, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's disease), urticaria, vesiculo bullous reactions.

Renal and Urinary Disorders: Nephrotic syndrome, glomerulonephritis, interstitial nephritis; renal failure.

General Disorders and Administration Site Conditions: Edema (mainly of the ankle), local adverse reactions (burning sensation) or tissue damage (sterile abscess formation, fatty tissue necrosis) at the site of injection, malaise, transient pain upon injection.

Investigations: Positive ANA, reversible elevations of BUN and creatinine, decreases in hemoglobin and hematocrit unassociated with obvious gastrointestinal bleeding, increased serum, transaminase levels, increased and decreased weight.