Melox

Melox

meloxicam

Manufacturer:

Medochemie

Distributor:

Medochemie
Full Prescribing Info
Contents
Meloxicam.
Description
Each tablet also contains the following excipients: Sodium citrate, lactose, microcrystalline cellulose, colloidal silicon dioxide, povidone, crospovidone and magnesium stearate.
Action
Pharmacotherapeutic Group: Nonsteroidal anti-inflammatory drug.
Pharmacology: Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam group, possessing analgesic, anti-inflammatory and antipyretic activity. In common with other NSAIDs, although the exact mechanism of action remains unknown, it is known that the inhibition of prostaglandin synthesis, known inflammation mediators, plays a role in the anti-inflammatory activity.
Pharmacokinetics: Following oral administration, meloxicam is well absorbed from the gastrointestinal tract and it has an absolute bioavailability of about 90%. Peak serum levels are reached after 7-8 hrs following a single oral dose, with steady-state concentration being achieved after 3-5 days administration. Plasma concentrations are proportional to dose over the 7.5- to 15-mg dosage range.
Plasma protein-binding, principally to albumin, is high (99%).
Meloxicam undergoes extensive metabolism, principally via oxidation of the methyl group of the thiazolyl ring.
Excretion of administered dose is 50% in the urine and 50% in the faeces, principally as metabolites, with only about 3% of the dose being excreted as unchanged meloxicam.
Mean elimination t½ is approximately 20 hrs. Mean plasma clearance is about 8 mL/min and clearance is reduced in the elderly. Meloxicam has a low volume of distribution, about 11 L, although there is considerable interindividual variation.
Patients with terminal renal failure have an increased volume of distribution, and the stipulated maximum daily dosage of 7.5 mg must not be exceeded.
Toxicology: Preclinical Safety Data: Meloxicam exhibits a similar toxicological profile to other NSAIDs. Preclinical studies in animals using chronic administration of high doses resulted in gastrointestinal erosion and ulceration, and renal papillary necrosis. Depending upon the animal species, nontoxic doses were 3-10 times greater than those used clinically.
Reproductive toxicological studies in animals demonstrated foetotoxic effects at doses greatly in excess of those used clinically. Foetotoxic effects at the end of the gestation period common to all prostaglandin synthesis inhibitors were found, cardiopulmonary and renal toxic effects.
In vitro and in vivo studies have not shown any evidence of mutagenic or carcinogenic potential.
Indications/Uses
Short-term symptomatic therapy of acute exacerbations of osteoarthritis, long-term symptomatic therapy of rheumatoid arthritis (chronic polyarthritis), and the symptomatic therapy of ankylosing spondylitis.
Dosage/Direction for Use
Melox tablets are for oral administration only. The total daily dose should be taken as a single dose, with water or another liquid, during a meal. The maximum daily dose is 15 mg. Do not exceed this dose.
Adults: Recommended Dose: Acute Exacerbations of Osteoarthritis: 7.5 mg. If necessary and depending upon the severity of symptoms, dosage may be increased to 15 mg daily.
Rheumatoid Arthritis: 15 mg/day. Patients at increased risk for adverse reactions should initiate therapy at 7.5 mg/day.
Ankylosing Spondylitis: 15 mg/day. Patients at increased risk for adverse reactions should initiate therapy at 7.5 mg/day.
Elderly: In elderly patients being treated for rheumatoid arthritis, the recommended dose for long-term treatment is 7.5 mg/day.
Hepatic Impairment: Meloxicam is contraindicated in severe hepatic impairment (see Contraindications). Caution should be exercised in patients with lesser degrees of hepatic impairment. These patients should be closely monitored. Diuresis and renal function should be carefully monitored during meloxicam therapy (see Precautions).
Renal Impairment: Meloxicam is contraindicated in nondialysed severe renal failure (see Contraindications). Patients with severe renal failure undergoing dialysis should not exceed a dose of 7.5 mg/day. Diuresis and renal function should be carefully monitored during meloxicam therapy (see Precautions).
Overdosage
Symptoms: Symptoms following acute NSAID overdose are usually limited to lethargy, drowsiness, nausea, vomiting and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Severe poisoning may result in hypertension, acute renal failure, hepatic dysfunction, respiratory depression, coma, convulsions, cardiovascular collapse and cardiac arrest.
Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs and may occur following an overdose.
Treatment: There is no known antidote to meloxicam, therefore, treatment of overdose is symptomatic and supportive. Cholestyramine administration, 4 g 3 times daily, may enhance the elimination of meloxicam. Antacids and H2-receptor antagonists may be used for the treatment of severe gastrointestinal lesions. In cases of acute overdose, gastric lavage followed by activated charcoal is recommended. Gastric lavage performed >1 hr after overdose has little benefit in the treatment of overdose. Administration of activated charcoal is recommended for patients who present 1-2 hrs after overdose. For substantial overdose or severely symptomatic patients, activated charcoal may be administered repeatedly. Forced diuresis, alkalinization of urine, haemodialysis or haemoperfusion may not be useful due to high protein-binding of meloxicam.
Contraindications
Hypersensitivity to meloxicam or to any other components of Melox.
The possibility of cross-sensitivity of meloxicam with other NSAIDs or aspirin exists. Therefore, meloxicam is also contraindicated in patients who have developed asthma, nasal polyps, angioneurotic oedema, urticaria or any other hypersensitivity reaction following administration of any NSAID or aspirin.
Active peptic ulcer or a history of recurrent peptic ulcer disease; severe hepatic impairment or renal impairment (without dialysis); cerebrovascular and gastrointestinal bleeding, or any other bleeding disorder.
Special Precautions
Before initiating therapy with meloxicam in patients with a history of oesophagitis, gastritis or peptic ulcer, freedom from these conditions must be established. Routine attention should be given to the possibility of recurrence of these conditions in meloxicam-treated patients with a history of these conditions.
Monitoring for digestive disturbances, particularly gastrointestinal bleeding, should be done in patients with gastrointestinal symptoms, or a history of gastrointestinal disease.
In common with other NSAIDs, gastrointestinal bleeding, or ulceration and/or perforation, has been reported with meloxicam at any stage of treatment, in rare instances resulting in fatalities. These events can occur with or without any warning symptoms, and in patients with or without a previous history of serious gastrointestinal events. The elderly generally experience more serious consequences of gastrointestinal bleeding or ulceration and/or perforation.
In the rare instances where gastrointestinal bleeding or ulceration occurs in patients on meloxicam therapy, the drug should be withdrawn promptly.
In the event of severe cutaneous or mucosal adverse effects occurring, meloxicam withdrawal must be considered. The possible occurrence of severe skin reactions and hypersensitivity reaction that are severe and life-threatening is known to occur with NSAIDs, including oxicams.
NSAIDs may cause glomerulonephritis, interstitial nephritis, nephritic syndrome or renal medullary necrosis in rare cases.
In common with the majority of NSAIDs, there are occasional reports of increases in serum transaminase levels, serum bilirubin, other liver function parameters, serum creatinine and blood urea nitrogen, and other laboratory test disturbances. In most cases, these have been transitory and minor abnormalities. However, if such an abnormality be significant or persist, meloxicam should be withdrawn and appropriate clinical investigation performed.
NSAIDs may cause the retention of sodium, potassium and water, and may interfere with the natriuretic effects of diuretics. This may result in consequential exacerbation of the condition of patients with cardiac insufficiency or hypertension.
In patients with decreased renal blood flow and blood volume, synthesis of renal prostaglandins responsible for maintenance of renal perfusion may be inhibited by NSAIDs. Administration of NSAIDs in such patients may cause the decompensation of latent renal failure, although renal function reverts to original status following therapy withdrawal. This risk affects all elderly patients, patients with congestive heart failure, cirrhosis, nephritic syndrome or renal failure. Patients who have undergone major surgery resulting in hypovolaemia, or on diuretic therapy are similarly affected. Diuresis and renal function should be carefully monitored during meloxicam therapy (see Dosage & Administration).
Daily dosage recommendations should not be exceeded if there is inadequate therapeutic efficacy.
Additional NSAIDs should not be added to the dosage regimen as toxicity may be increased, and therapeutic efficacy has not been demonstrated.
Effects on the Ability to Drive or Operate Machinery: Patients may experience drowsiness, vertigo, visual disturbances and other central nervous system disturbances during meloxicam therapy (see Adverse Reactions). Patients should be cautioned as to the possibility of such effects and advised not to drive or operate machinery if such disturbances occur.
Use in pregnancy: Lethal effects on the foetus have been reported in animal studies using doses higher than those administered clinically. It is recommended that the use of meloxicam be avoided during pregnancy. In the final trimester of pregnancy, the use of any prostaglandin synthesis inhibitor may result in foetal cardiopulmonary toxicity, pulmonary hypertension and premature closure of the ductus arteriosus, and renal toxicity. Uterine contraction may also be inhibited and in animals, this has been associated with dystocia incidence elevation and delayed parturition. Meloxicam, in common with all NSAIDs, is absolutely contraindicated during the final trimester of pregnancy.
Use in lactation: NSAIDs are excreted in maternal breast milk, therefore, administration should be avoided in women who are breastfeeding as a precaution.
Use in children: The safety and efficacy of meloxicam have not been established in children <15 years.
Use in the elderly: Elderly, fragile or weakened patients are often less tolerant of adverse effects and therefore, require careful monitoring during therapy. In common with other NSAIDs, particular caution should be exercised with the elderly, who frequently have impairment of cardiac, hepatic and renal functions.
Use In Pregnancy & Lactation
Use in pregnancy: Lethal effects on the foetus have been reported in animal studies using doses higher than those administered clinically. It is recommended that the use of meloxicam be avoided during pregnancy. In the final trimester of pregnancy, the use of any prostaglandin synthesis inhibitor may result in foetal cardiopulmonary toxicity, pulmonary hypertension and premature closure of the ductus arteriosus, and renal toxicity. Uterine contraction may also be inhibited and in animals, this has been associated with dystocia incidence elevation and delayed parturition. Meloxicam, in common with all NSAIDs, is absolutely contraindicated during the final trimester of pregnancy.
Use in lactation: NSAIDs are excreted in maternal breast milk, therefore, administration should be avoided in women who are breastfeeding as a precaution.
Adverse Reactions
Cardiovascular System: Oedema, lower limb oedema, elevated blood pressure (see also Precautions), palpitations and flushes.
Central Nervous System: Drowsiness, headache, lightheadedness, tinnitus and vertigo may occur. Rare instances of confusion, insomnia and nightmares.
Dermatological: Reports of skin rash, pruritus, urticaria and photosensitivity reactions. Very rarely, erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis, or other bullous reactions.
Gastrointestinal System: Abdominal pain, constipation, diarrhoea, dyspepsia, flatulence, nausea, oesophagitis, stomatitis and vomiting may occur. Rare instances of peptic ulceration, perforation or gastrointestinal bleeding, sometimes severe, particularly in the elderly (see Precautions). Reports of rare cases of gastritis.
Genitourinary System: Laboratory tests of renal function may be disturbed eg, elevated creatinine or urea.
Haematological System: Reports of blood count disturbances in patients taking meloxicam, some of which have been attributed to therapy; anaemia, leucocytopenia, and thrombocytopenia. There are isolated reports of agranulocytosis in patients taking meloxicam and other drugs with myelotoxic potential.
Hepatic System: Liver function tests may show transitory disturbance eg, elevation of bilirubin or transaminase levels.
Immunological: Rare reports of angioedema and anaphylactic or anaphylactoid reactions.
Pulmonary System: Patients allergic to aspirin or other NSAIDs have experienced asthma attacks.
Sensory System: Rare reports of visual disturbances, including blurred vision.
Drug Interactions
Simultaneous administration of meloxicam with the following drugs mandates careful supervision and monitoring of the clinical and laboratory status of the patient.
The following combinations are inadvisable: Other NSAIDs, High Dosages of Salicylates: The risk of gastrointestinal ulceration and/or gastrointestinal bleeding is increased when administering several NSAIDs together due to synergistic effects.
Lithium: Blood lithium levels are increased by NSAIDs due to decreased renal excretion of lithium. Consequently, lithium levels may reach toxic levels, therefore, blood lithium levels should be monitored during initiation, dose titration and withdrawal of meloxicam.
Oral Anticoagulants, Ticlopidine, Parenteral Heparin: Due to inhibition of platelet function and gastroduodenal mucosa damage, there is an increased risk of bleeding. In the event that use of such combinations is unavoidable, the effect of the anticoagulants must be closely monitored.
High Dosage Methotrexate (≥15 mg/week): NSAIDs decrease the renal clearance of methotrexate resulting in increased haematological toxicity of methotrexate. Although causality has not been confirmed, there is a report of agranulocytosis in a patient treated with methotrexate and meloxicam. Prescription of such combination requires caution and close monitoring of the blood cell count is recommended in such an instance (see also text as follows).
Simultaneous administration of meloxicam with the following drugs requires precautions: Cyclosporin: NSAIDs may enhance the nephrotoxicity of cyclosporin due to renal prostaglandin-mediated effects. Renal function must be measured during combination therapy.
Diuretics: NSAIDs therapy results in decreased renal prostaglandin synthesis with consequent decreased glomerular filtration resulting in an elevated risk of acute renal failure in dehydrated patients. Use of meloxicam with a diuretic means it is essential to ensure the patient is adequately hydrated and to closely monitor renal function at the initiation of such therapy.
Low Dosage Methotrexate (<15 mg/week): NSAIDs decrease the renal clearance of methotrexate resulting in increased haematological toxicity of methotrexate. Blood count should be monitored weekly during the 1st few weeks of such combination therapy. In elderly patients, and those with even slight renal impairment, require increased monitoring and close supervision.
Pentoxifylline: There is an increased risk of bleeding, and general clinical monitoring and verification of bleeding time should be of increased frequency.
Zidovudine: Due to effects on the reticulocytes, there is an increased risk of greater red cell line toxicity effects, with severe anaemia resulting 1 week after NSAID therapy is initiated. The CBC and reticulocyte count should be checked 1 or 2 weeks post-NSAID therapy initiation.
Simultaneous administration of meloxicam with the following drugs requires caution and appropriate precautions should be taken: Antihypertensives (β-blockers, angiotensin-converting enzyme inhibitors, diuretics): NSAID therapy inhibits prostaglandin synthesis and may result in a decrease of the antihypertensive effect.
Intrauterine Devices (IUD): There is a possible risk of impaired efficacy, and additional contraceptive precautions may be required.
Thrombolytics: There is an elevated risk of bleeding.
Others: Antacids, H2-Receptor Agonists (Cimetidine, Ranitidine), Furosemide, β-Acetyl Digoxin: Concomitant administration with meloxicam has not resulted in any significant pharmacokinetic interactions.
Cholestyramine: The elimination of meloxicam is accelerated due to binding in the digestive tract.
Oral Antidiabetics: The possibility of interactions cannot be excluded; such patients should be closely monitored and supervised.
Storage
Store below 25°C in the original blister.
Shelf-Life: 24 months.
ATC Classification
M01AC06 - meloxicam ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, oxicams.
Presentation/Packing
Tab (light yellow, round, flat, scored on one side, 7 mm diameter) 7.5 mg x 10 x 10's, 100 x 10's.
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