Each tablet contains: Meloxicam, USP 15 mg.
Pharmacology: Meloxicam is a non-steroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mode of action of Meloxicam may be related to prostaglandin synthetase (cyclooxygenase) inhibition.
Pharmacokinetics: Absorption: Absolute bioavailability of a single oral dose is 89%. Neither the rate nor the extent of absorption is affected by multiple dose administration. Administration with food does not affect the extent of absorption.
Distribution: VolD-10 L. Penetration into red blood cells is less than 10%. Concentrations in synovial fluid after a single oral dose range from 40% to 50% of those in plasma. The free fraction in synovial fluid is 2.5 times higher than in plasma, due to the lower albumin content in synovial fluid.
Protein binding: Very high (99.4%).
Biotransformation: Almost completely metabolized to 4 pharmacologically inactive metabolites. Metabolized largely by cytochrome P450 2C9.
Half-life: Elimination 15 to 20 hours.
Time to peak concentration: 5 to 6 hours.
Peak serum concentration: 1.05 micrograms/mL in healthy male adults at steady state, with a 7.5 mg dose.
Elimination: Only traces of unchanged parent compound are excreted in the urine (0.2%) and feces (1.6%). Excretion is predominantly in the form of metabolites and occurs to an equal extent in the urine and feces.
Arthritis, juvenile rheumatoid (treatment): Meloxicam is indicated for relief of the signs and symptoms of pauciarticular or polyarticular course Juvenile Rheumatoid Arthritis in patients 2 years of age and older.
Arthritis, rheumatoid (treatment): Meloxicam is indicated for the relief of the signs and symptoms of rheumatoid arthritis.
Osteoarthritis (treatment): Meloxicam is indicated for the relief of the signs and symptoms of osteoarthritis.
Adult dose: Osteoarthritis or rheumatoid arthritis: 7.5 mg once a day. Some patients receive additional benefit by increasing the dose to 15 mg once daily.
Adult prescribing limits: Up to 15 mg once a day.
Pediatric dose: For treatment of osteoarthritis and rheumatoid arthritis: Safety and efficacy have not been established.
Juvenile rheumatoid arthritis: Recommended dose of 0.125 mg per kg of body weight once daily.
Pediatric prescribing limits: Up to 7.5 mg once daily.
Geriatric dose: See usual adult dose.
Clinical effects: Note: The following symptoms describe overdose of nonsteroidal anti-inflammatory drugs (NSAIDs) in general. Anaphylactoid reaction; cardiac arrest; convulsions; drowsiness; lethargy; epigastric pain; gastrointestinal bleeding; hepatic dysfunction; hypertension; nausea or vomiting; acute renal failure; respiratory depression.
Treatment of overdose: Forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion may not be useful due to high protein binding. Patients should be managed with symptomatic and supportive care, possibly including: To decrease absorption: Activated charcoal - recommended for patients who present 1 to 2 hours after overdose; Cholestyramine; Gastric lavage - if performed within one hour of overdose. Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.
Except under special circumstances, this medication should not be used when the following medical problem exists: Coronary artery bypass graft (CABG) surgery (Meloxicam is contraindicated for the treatment of peri-operative pain in the setting of CABG) surgery. Hypersensitivity to Meloxicam. Nasal polyps associated with bronchospasm, Aspirin-induced (high risk of severe allergic reaction). Previous allergic/anaphylactic reaction to aspirin or other NSAIDs.
Risk-benefit should be considered when the following medical problems exist: Gastrointestinal bleeding, active, or pre-existing. Peptic ulcer disease, active or Risk factors for CV disease (may be at greater risk of serious CV thrombotic events; lowest effective dose of Meloxicam for shortest duration should be used with physicians and patients remaining alert for development of signs and symptoms of such events). Renal function impairment, severe (long-term studies have not been done in patients with severe renal function impairment; use of Meloxicam is not recommended in these patients; however, if Meloxicam is used in patients with severe renal impairment, close monitoring is recommended).
Absolute contraindications: Not to be given to those patients who have 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.
Cross-sensitivity and/or related problems: Patients who have experienced asthma, urticaria, or allergic-type reactions after taking Aspirin or other NSAIDs should not be given Meloxicam; severe, anaphylactic-like reactions to NSAIDs have been reported in such patients.
Carcinogenicity: No carcinogenic effect of Meloxicam was observed in rats given oral doses up to 0.8 mg/kg/day (approximately 0.4-fold the human dose of 15 mg/day for a 50 Kg adult based on body surface area conversion) for 104 weeks or in mice given oral doses up to 8.0 mg/Kg/day (approximately 2.2 - fold the human dose) for 99 weeks.
Mutagenicity: Meloxicam was not mutagenic in an Ames assay. No clastogenic effect was observed in the chromosome aberration assay with human lymphocytes or in the in vivo micronucleus test in mouse bone marrow.
Pediatrics: For treatment of osteoarthritis and rheumatoid arthritis: No information is available on the relationship of age to the effects of Meloxicam in children up to 18 years of age. Safety and efficacy have not been established.
For treatment of juvenile rheumatoid arthritis: Safety and effectiveness in pediatric patients from 2 to 17 years of age have been evaluated.
Geriatrics: As with any NSAID, caution should be exercised in treating the elderly (65 years and older). Elderly patients are at greater risk for serious gastrointestinal events. Plasma concentrations of Meloxicam and steady state pharmacokinetics in elderly men (≥65 years of age) were similar to those in young males. Elderly females (≥65 years of age) had a 47% higher AUC and 32% higher Cmax when compared to younger females (≤55 years of age). Despite the difference in total concentrations, the adverse event profiles were comparable in elderly men and elderly women.
Pregnancy: Adequate and well-controlled studies in humans have not been done. Meloxicam may cause premature closure of the ductus arteriosus. Therefore, use of Meloxicam is not recommended during pregnancy, especially late pregnancy.
Meloxicam crosses the placenta.
Meloxicam caused an increased incidence of septal defect of the heart at an oral dose 64.5-fold the human dose (15 mg/day for a 50 Kg adult based on body surface area conversion) and embryolethality at oral doses greater than 5.4 times the human dose in rabbits treated throughout organogenesis. Meloxicam was not teratogenic in rats at a dose equivalent to 2.2 times the human dose when given throughout organogenesis. An increased incidence of stillbirths occurred in rats given doses ≥1 mg/Kg/day throughout organogenesis. When female rats were given Meloxicam at half the human dose 2 weeks before mating and during early embryonic development, there was increased incidence of embryolethality. The birth index, the number of live births, and neonatal survival were reduced in rats given oral doses ≥0.125 mg/Kg/day (0.07-fold the human dose) during the late gestation and lactation periods.
Breastfeeding: Studies of distribution of Meloxicam into human breast milk have not been done. However, Meloxicam has been found in the milk of lactating rats at concentrations higher than those in plasma. Because many drugs are distributed in human milk and because of the potential for serious adverse reactions in nursing infants from Meloxicam, 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.
Fertility: Meloxicam did not impair male and female fertility in rats at oral doses up to 9 and 5 mg/Kg/day, respectively (4.9-fold and 2.5-fold the human dose of 15 mg/day for a 50 Kg adult based on body surface area conversion).
Labor and delivery: Studies in rats with Meloxicam showed an increased incidence of stillbirths, increased length of delivery time, and delayed parturition at doses 0.5-fold the human dose of 15 mg/day for a 50 Kg adult based on body surface area conversion, and decreased pup survival at an oral dose of 2.1-fold the human dose given throughout organogenesis.
Similar results were observed in rats at 0.07-fold the human dose given during late gestation and lactation period.
Those indicating need for medical attention: Less frequent:
Albuminuria; Allergic reaction; Angina pectoris; Angioedema; Arrhythmia; Asthma; Bilirubinemia; Bronchospasm; Bullous eruption; Cardiac failure; Colitis; Convulsions; Duodenal ulcer; Dyspnea; Face edema; Gastric ulcer; Hematemesis; Hematuria; Hemorrhagic duodenal or gastric ulcer; Hepatitis; Hypertension; Hypotension; Intestinal perforation; Leukopenia; Melena; Myocardial infarction; Palpitation; Pancreatitis; Perforated duodenal or gastric ulcer; Photosensitivity reaction; Pruritus; Purpura; Renal failure; Stomatitis ulcerative; Syncope; Tachycardia; Thrombocytopenia; Tremor; Urticaria; Vasculitis.
Agranulocytosis; Anaphylactoid reaction; Anemia; Erythema multiforme; Exfoliative dermatitis; Gastrointestinal bleeding or hemorrhage; Interstitial nephritis; Jaundice; Liver failure; Shock; Steven-Johnson syndrome; Toxic epidermal necrolysis.
Those indicating need for medical attention only if they continue or are bothersome: Incidence more frequent:
Diarrhea; Dyspepsia; Flatulence.
Incidence less frequent or rare:
Abdominal pain; Abnormal dreaming; Abnormal vision; Alopecia; Anxiety; Appetite increased; Confusion; Conjunctivitis; Constipation; Dehydration; Depression; Dry mouth; Eructation; Esophagitis; Fatigue; Fever; Gastritis; Gastroesophageal reflux; Hot flushes; Malaise; Nausea and/or vomiting; Nervousness; Paresthesia; Somnolence; Sweating increased; Taste perversion; Tinnitus; Vertigo; Weight decreased or increase.
Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.
Aspirin (concurrent administration of low-dose Aspirin and Meloxicam may result in an increased rate of gastrointestinal ulceration or other complications).
Lithium (Meloxicam can elevate plasma lithium level and reduce renal lithium clearance; patients on lithium treatment should be closely monitored when Meloxicam is introduced or withdrawn).
Store at a temperature not exceeding 30°C.
M01AC06 - meloxicam ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, oxicams.