RiteMED Meloxicam

Meloxicam 7.5 mg is a yellow-colored round tablet, one side scored, and two sides of the score are engraved with "IS".
Meloxicam 15 mg is a yellow-colored round tablet, one side scored, and two sides of the score are engraved with "IN".
Each tablet contains: Meloxicam 7.5 mg or 15 mg.

Non-Steroidal Anti-inflammatory Drug (NSAID).
Pharmacology: Pharmacodynamics: Meloxicam is an oxicam derivative non-steroidal anti-inflammatory drug (NSAID) which exhibits analgesic, antipyretic and anti-inflammatory activities by inhibiting cyclooxygenase (COX)-1 and COX-2 isoenzymes resulting in inhibition of prostaglandin synthesis.
Meloxicam inhibits the COX-2 isoform of prostaglandin endoperoxide synthase more than it inhibits the COX-1 isoform as shown in in vitro and in vivo studies. However, Meloxicam is classified as a "preferential" rather than a "selective" COX-2 inhibitor since its COX-2 selectively is dose-dependent and is diminished at higher doses.
Pharmacokinetics: Meloxicam is almost completely absorbed after oral administration with an absolute bioavailability of 89% compared with IV bolus injection. Meloxicam's bioavailability is not markedly affected by concomitant food intake. Maximum plasma concentration (C_max) after a 30 mg oral dose is reached in about 9 to 11 hours while C_max for a 15 mg dose is achieved in about 2.5 to 7 hours. Steady state blood concentrations of Meloxicam are achieved only after 3 to 4 days after oral administration because of its long half-life (around 20 to 24 hours).
Meloxicam is about 99% bound to plasma proteins. Its apparent volume of distribution after oral administration is about10 to 15 L. Meloxicam readily penetrates the synovial fluid with concentrations reaching about 45-57% of plasma concentrations.
Meloxicam is extensively metabolized in the liver to four inactive metabolites. In in vitro studies, Meloxicam is mainly metabolized by the CYP450 2C9 with minor involvement of the CYP3A4 isoenzyme.
Meloxicam is excreted equally in both the urine and feces mainly as metabolites. Its apparent oral clearance ranges from 0.42 to 0.7 L/h.
Meloxicam's pharmacokinetic profile is not significantly altered in elderly patients or in those with mild renal impairment. Meloxicam's pharmacokinetic parameters were also found to be similar in patients with hepatic cirrhosis and healthy volunteers.

For symptomatic treatment of osteoarthritis such as arthrosis and degenerative joint disease, rheumatoid arthritis, ankylosing spondylitis, and similar conditions that respond to anti-inflammatory therapy.
For the relief of signs and symptoms of pauciarticular or polyarticular course juvenile rheumatoid arthritis.

Meloxicam tablet may be taken without regard to food or antacids.
As with other NSAIDs, the lowest effective dose of Meloxicam should be used for the shortest possible time. Therefore, after observing the response to initial therapy with this product, the dose and frequency should be adjusted to suit individual patients needs. (See table.)

Click on icon to see table/diagram/image

There is limited experience with meloxicam overdose.
Acute NSAID overdosage may present with symptoms including lethargy, drowsiness, nausea, vomiting, and epigastric pain. These symptoms are usually reversible with supportive care. Gastrointestinal bleeding may occur. Severe poisoning may result in hypertension, acute renal failure, hepatic dysfunction, respiratory depression, coma, convulsions, cardiovascular collapse, and cardiac arrest. Anaphylactoid reactions may also occur.
Manage patients with symptomatic and supportive care following overdosage with an NSAID. Gastric lavage followed by activated charcoal is recommended in acute overdosage but gastric lavage performed more than one hour after an overdose has little benefit. Activated charcoal is recommended in patients who present one to two hours after overdose. Administer activated charcoal repeatedly in substantial overdose or severely symptomatic patients. Removal of Meloxicam is accelerated with 4 g oral doses of cholestyramine given thrice daily. Meloxicam is highly protein bound. Thus, forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion may not be useful.

Known hypersensitivity to Meloxicam or to any ingredient in the product.
Patients who have experienced asthma, urticaria or allergic reactions after taking aspirin or other NSAIDs.
Patients with previous or active peptic ulcer.
Contraindicated in the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

Cardiovascular Risk: NSAIDs, including meloxicam, may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. The risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk.
Meloxicam is contraindicated in patients who have a history of: Stroke: cerebrovascular accident (CVA); Heart attack: myocardial infarction (MI); Coronary artery bypass graft (CABG); Uncontrolled hypertension; Congestive heart failure (CHF) NYHA II-IV.
Gastrointestinal Risk: NSAIDs, including Meloxicam, 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.

Cardiovascular Effects: Cardiovascular Thrombotic Events: Clinical trials using COX-2 selective and nonselective NSAIDs of up to three years duration show an increased risk of cardiovascular (CV) thrombotic events, myocardial infarction and stroke, which can be fatal. Risk for these events is greater in patients with known CV disease or risk factors for CV disease. Use the lowest effective NSAID dose for the shortest possible time to minimize the potential risk for an adverse CV event. Even in the absence of previous CV symptoms, physicians and patients should be alert for the development of such events. Inform patients about signs and/or symptoms of serious CV events and the steps to take if they occur.
There is no consistent evidence that concurrent use of Aspirin mitigates the increased risk of serious CV thrombotic events associated with NSAID use.
Clinical trials of a COX-2 selective NSAID for the treatment of pain in the first 10-14 days after CABG surgery found an increased incidence of myocardial infarction and stroke.
Hypertension: NSAIDs, including Meloxicam, can lead to the onset of new hypertension or worsening of pre-existing hypertension, either of which may contribute to the increased incidence of CV events. Use Meloxicam with caution in patients with hypertension. Impaired response to therapies such as thiazides or loop diuretics may occur in patients taking NSAIDs, including Meloxicam. Monitor blood pressure closely during initiation of NSAID treatment and throughout the course of therapy.
Congestive Heart Failure and Edema: Fluid retention and edema (including peripheral edema) have been seen in some patients taking NSAIDs. Use Meloxicam with caution in patients with fluid retention, hypertension or heart failure.
Gastrointestinal (GI) Effects: NSAIDs should be prescribed with extreme caution in those with a prior history of ulcer disease and/or gastrointestinal bleeding since such patients have a greater than 10-fold increased risk for developing a GI bleed when they use NSAIDs compared with patients with neither of these risk factors. Other factors that increase the risk for 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. Elderly or debilitated patients, in particular, are at greater risk for serious gastrointestinal events; special care should be taken in treating this population.
The lowest effective dose should be used for the shortest possible duration to minimize the potential risk for an adverse GI event. Physicians and patients should remain alert for signs and symptoms of GI ulceration and bleeding during NSAID therapy and promptly initiate additional evaluation and treatment if a serious GI adverse event is suspected. This should include discontinuation of the NSAID until a serious GI adverse event is ruled out. Alternate therapies that do not involve NSAIDs should be considered especially for high-risk patients.
Renal Effects: Renal papillary necrosis and other renal injury may result from long-term administration of NSAIDs. In patients in whom renal prostaglandins have a compensatory role in the maintenance of renal perfusion, renal toxicity may occur with NSAID use because of the dose-dependent reduction in prostaglandin and renal blood flow which may precipitate overt renal decompensation. Elderly patients, those with impaired renal function, heart failure, liver dysfunction, those taking diuretics, ACE inhibitors and angiotensin II receptor antagonists are at greatest risk for this reaction. Recovery to the pretreatment state usually follows discontinuation of NSAID therapy.
Meloxicam is not recommended in patients with advanced renal disease.
Use caution when initiating Meloxicam treatment in patients with considerable dehydration. Rehydrate patients first before starting Meloxicam therapy.
Anaphylactoid Reactions: Anaphylactoid reactions may occur in patients without known prior exposure to NSAIDs. Asthmatic patients who experience rhinitis with or without nasal polyps, or who exhibit severe, potentially fatal bronchospasm after taking Aspirin or other NSAIDs are at an increased risk of this symptom complex. Seek emergency help when an anaphylactoid reaction occurs.
Skin reactions: As with other NSAIDs, Meloxicam can cause serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson Syndrome (SJS), and toxic epidermal necrolysis (TEN), which can be fatal. Since these serious events may occur without warning, inform patients about the signs and symptoms of serious skin manifestations and advice them to discontinue the drug at the first appearance of skin rash or any other sign of hypersensitivity.
Hepatic Effects: Elevations of one or more liver function tests and rare cases of severe hepatic reactions including jaundice and fatal fulminant hepatitis, liver necrosis and hepatic failure, which may be fatal, have been reported with NSAID use.
Evaluate patients with signs and/or symptoms suggesting liver dysfunction or abnormal liver test for evidence of the development of more severe hepatic reaction while on Meloxicam therapy.
Discontinue Meloxicam treatment if clinical signs and symptoms consistent with liver disease develop or if systemic manifestations such as eosinophilia or rashes occur.
Hematological Effects: Anemia, which may be due to fluid retention, occult or gross gastrointestinal blood loss, or an incompletely described effect upon erythropoiesis have been seen in patients receiving NSAIDs. Periodically determine hemoglobin values in patients with initial hemoglobin values of 10 g or less who are to receive a longer duration of meloxicam therapy.
NSAIDs generally inhibit platelet aggregation and may prolong bleeding time in some patients but this effect on platelet function, compared with Aspirin, is quantitatively less, of shorter duration, and reversible. Carefully monitor patients on Meloxicam therapy who may be adversely affected by alterations in platelet function (e.g., those with coagulation disorders or patients receiving anticoagulants).
Preexisting Asthma: Asthmatic patients 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. Do not administer Meloxicam to patients with Aspirin sensitivity since cross reactivity between Aspirin and other NSAIDs have been reported. Administer Meloxicam with caution in patients with preexisting asthma.
General Precautions: Meloxicam is not a corticosteroid substitute and cannot be used to treat corticosteroid insufficiency.
The antipyretic and anti-inflammatory actions of Meloxicam may diminish the use of these diagnostic signs in detecting complications of presumed non-infectious, non-inflammatory painful conditions.
Use in Pregnancy & Lactation: See Use in Pregnancy & Lactation section for further information.
Use in Children: The safety and efficacy in children below 2 years old have not been established. The use in children 2-17 years old with juvenile rheumatoid arthritis has been established.
Use in the Elderly: As with any NSAID, exercise caution in treating the elderly (65 years and older).

Pregnancy, Labor, Delivery, and Lactation: Avoid use of Meloxicam during pregnancy (particularly late pregnancy) because of the known effects of NSAIDs on the fetal cardiovascular system (closure of ductus arteriosus). Meloxicam crosses the placental barrier.
Meloxicam's effects on labor and delivery in pregnant women are unknown.
It is not known whether Meloxicam is excreted in human milk. Since many drugs are excreted in human milk and because of the potential for serious adverse reactions from Meloxicam in breastfeeding infants, a decision should be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the drug to the mother.

Body as a whole: Allergic reaction, anaphylactoid reactions including shock, face edema, fatigue, fever, hot flushes, malaise, syncope, weight decrease, weight increase, household accident, edema (including dependent, peripheral and leg edema), fall, influenza-like symptoms.
Cardiovascular: Angina pectoris, cardiac failure, hypertension, hypotension, myocardial infarction, vasculitis, arrhythmia, palpitation, tachycardia.
Gastrointestinal: Colitis, dry mouth, duodenal ulcer, eructation, esophagitis, gastric ulcer, gastritis, gastroesophageal reflux, gastrointestinal hemorrhage, hematemesis, hemorrhagic duodenal ulcer, hemorrhagic gastric ulcer, intestinal perforation, melena, pancreatitis, perforated duodenal ulcer, perforated gastric ulcer, ulcerative stomatitis, abdominal pain, vomiting, diarrhea, dyspepsia (including aggravated dyspepsia, eructation, gastrointestinal irritation), flatulence, nausea.
Respiratory: Upper respiratory tract infection (including laryngitis, pharyngitis, and sinusitis), coughing, asthma, bronchospasm, dyspnea.
Neurologic: Convulsions, paresthesia, tremor, vertigo, dizziness, headache, insomnia, abnormal dreaming, alterations in mood (i.e., mood elevation), anxiety, confusion, depression, nervousness, somnolence.
Dermatologic and Sensitivity Reactions: Rash (including erythematous and maculopapular rash), pruritus, alopecia, angioedema, bullous eruption, erythema multiforme, photosensitivity reaction, exfoliative dermatitis, Stevens-Johnson syndrome, increased sweating, toxic epidermal necrolysis, urticaria.
Hematologic: Agranulocytosis, leukopenia, purpura, thrombocytopenia, anemia.
Urogenital: Frequent micturition, urinary tract infection, acute urinary retention, albuminuria, increased blood urea nitrogen (BUN), increased creatinine, hematuria, interstitial nephritis, renal failure.
Hepatic: Increased alanine aminotransferase (ALT), aspartate aminotransferase (AST) and gamma-glutamyl transpeptidase (GGT); bilirubinemia, hepatitis, jaundice, liver failure.
Musculoskeletal: Arthralgia, back pain.
Metabolic and Nutritional: Dehydration, increased appetite.
Special senses: Abnormal vision, conjunctivitis, taste perversion, tinnitus.

Antihypertensive agents (e.g., ACE-inhibitors, β-blockers, vasodilators): Meloxicam and other NSAIDs may reduce the effect of antihypertensive agents through inhibition of vasodilatory prostaglandins.
Bile acid sequestrants (e.g., cholestyramine): Concomitant administration of bile acid sequestrants and meloxicam may increase the clearance of Meloxicam by 50%.
Aspirin and Other NSAIDs: Concomitant administration of Meloxicam with low-dose aspirin or other NSAIDs may result in increased rate of GI ulceration or other complications.
Ciclosporin: The effects of NSAIDs on renal prostaglandins may increase the nephrotoxicity of Ciclosporin.
Diuretics: As with other NSAIDs, Meloxicam can reduce the natriuretic effect of furosemide and thiazides in some patients due to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, observe patients closely for signs of renal failure, as well as to assure diuretic efficacy.
Lithium: NSAIDs, including Meloxicam, have produced significant elevation of plasma Lithium levels. This effect is attributed to Meloxicam's inhibition of renal prostaglandin synthesis. Closely monitor patients for signs of Lithium toxicity when NSAIDs and Lithium are administered concurrently.
Methotrexate: NSAIDs could enhance the toxicity of Methotrexate. Use caution when NSAIDs are administered concomitantly with methotrexate.
Oral anticoagulants (e.g., Warfarin), antiplatelet drugs, thrombolytics, and systemically administered Heparin: NSAIDs increase the risk of bleeding when co-administered with these agents.
Cimetidine, Digoxin: Pharmacokinetic interaction with Meloxicam is unlikely.

Store at temperatures not exceeding 30°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AC06 - meloxicam ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, oxicams.

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