Melox

Meloxicam.

MELOX (7.5 MG TABLET): Each tablet contains Meloxicam 7.5 mg.
MELOX (15 MG TABLET): Each tablet contains Meloxicam 15 mg.

Pharmacology: Pharmacodynamics: Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID), an oxicam derivative. It inhibits the biosynthesis of prostaglandins as inflammatory mediators. It has inhibitory effect to 2 isoenzymes of cyclooxygenases (COXs or prostaglandin endoperoxide syntases): COX-1 and COX-2. The normal dose of Meloxicam is preferential inhibitor of COX-2, associated with anti-inflammatory effect, than COX-1, associated with adverse gastrointestinal effect.
Pharmacokinetics: Meloxicam is well absorbed after oral doses. Timing of meals or concomitant use of antacids does not affect the drug pharmacokinetics. Maximum plasma concentration (C_max) is reached within 5-10 hours of administration. It is about 99% bound to plasma proteins. The volume of distribution is increased in renal failure.
Meloxicam is extensively metabolized in the liver principally via cytochrome P450 (CYP) 2C9 isoenzyme, with minor contribution by CYP3A4, to inactive metabolites including 5'-carboxymeloxicam as the major metabolite. Both drug and its metabolites are excreted in the similar amounts in the urine and in the feces; small amount is excreted unchanged (< 5%). Second maximum plasma concentration occurs prolongedly around 12-14 hours of administration, as some amount of the biliary excretion has enterohepatic recirculation. It has an elimination half-life of about 15-20 hours.

Symptomatic treatment of osteoarthritis (arthrosis or degenerative joint disease).
Symptomatic treatment of rheumatoid arthritis.
Symptomatic treatment of juvenile arthritis.
Symptomatic treatment of ankylosing spondylitis.

Use the lowest possible effective dosage and shortest duration of therapy to avoid risk of adverse drug reactions.
This drug should be taken with meals or after meals.
Take the recommended dosages or according to medical prescription.
Adult dosage: Symptomatic treatment of osteoarthritis (arthrosis or degenerative joint disease): 7.5 mg taken once daily. For additional benefit, dosage may be increased to 15 mg once daily.
Symptomatic treatment of rheumatoid arthritis: 7.5 mg taken once daily. For additional benefit, dosage may be increased to 15 mg once daily.
Symptomatic treatment of ankylosing spondylitis: 7.5 mg taken once daily. For additional benefit, dosage may be increased to 15 mg once daily.
The maximum recommended daily dosage is 15 mg.
Children and adolescent dosage (12-18 years old): Symptomatic treatment of juvenile arthritis: dosage according to body weight: less than 50 kg: 7.5 mg taken once daily; 50 kg and above: 15 mg taken once daily.
Renal impairment: Closely monitor renal function of the patients with renal impairment using Meloxicam or other NSAIDs.
No dose adjustment is required in patients with mild to moderate renal impairment (creatinine clearance of greater than 25 mL/minute).
In patients with hemodialysis, a maximum daily dosage of 7.5 mg is recommended.
Meloxicam is contraindicated in patients with severe renal impairment.
Hepatic impairment: No dose adjustment is required in patients with mild to moderate hepatic impairment.
There are inadequate studies in patients with severe hepatic impairment.

Patients with overdosage may experience effects which are reversible with supportive care including lethargy, drowsiness, nausea, vomiting, epigastric pain; gastrointestinal bleeding may occur. Severe cases such as acute renal failure, hepatic dysfunction, respiratory depression, convulsion, cardiovascular failure, cardiac arrest, anaphylactoid reaction, may occur.
Symptomatic and supportive care are recommended. For acute overdosage, gastric lavage is suggested within 1 hour after overdosage, followed by activated charcoal within 1-2 hours; repeat administration may be useful following substantial overdose or those with severe symptoms. It is also suggested to take cholestyramine orally 4 g 3 times a day to accelerate the drug removal.
Forced diuresis, alkalinization of urine, hemodialysis or hemoperfusion may not be useful due to high protein binding.

1. Patients with known hypersensitivity to Meloxicam or any ingredient in the formulation, aspirin, and other nonsteroidal anti-inflammatory drugs (NSAIDs).
2. Patients with gastrointestinal hemorrhage, intracranial hemorrhage, and bleeding in different parts of the body.
3. Patients with gastrointestinal ulcers, or history of gastrointestinal diseases.
4. Patients with severe hepatic impairment or severe renal impairment.
5. The treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
6. Last trimester pregnancy (30 weeks or more) or nursing mothers, unless prescribed by a physician.
7. Patients with dengue hemorrhagic fever.

1. It is contraindicated in patients with hypersensitivity to this drug, or patients with asthma, urticaria or acute nasal cavity inflammation after taking aspirin or NSAIDs.
2. Avoid the drug during pregnancy in last trimester, unless prescribed by a physician.
3. It is contraindicated in patients with gastrointestinal hemorrhage or perforation.
4. It is contraindicated in patients with severe hepatic or renal diseases.
5. It is contraindicated in patients with dengue hemorrhagic fever.
6. If rash or flu-like symptoms occur during taking this drug, stop the drug immediately and consult a doctor.
7. This drug may increase the risk of gastrointestinal hemorrhage or ulceration.
8. This drug may increase the risk of ischemic stroke and ischemic heart disease, especially with prolonged use.
9. This drug may cause an adverse effect of edema. Use with caution in patients with heart disease and renal impairment.
10. Use with caution in patients with hypertension or elderly.
11. This drug may affect the platelet aggregation. Avoid use in patients with dengue hemorrhagic fever, or other thrombosis disorders.
12. When using this drug if the following symptoms, such as fever, vesicle, peeling of the skin and mucous membranes including mouth, nose, throat, reproductive organs and conjunctivitis appear, stop medication and consult a doctor because it may be Stevens-Johnson syndrome.

NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. Use the drug with caution in patients with cardiovascular disease or risk factors for cardiovascular disease.
NSAIDs can lead to onset of new hypertension or worsening existing hypertension, therefore increase the incidence of cardiovascular events. Use the drug with caution and closely monitor blood pressure during the initiation of NSAIDs treatment and throughout the course.
Long-term use of NSAIDs can result in renal papillary necrosis and renal medullary changes; as the prostaglandin formation and renal blood flow are reduced. Patients at risk are those with impaired renal function, heart failure, liver dysfunction, the elderly, those taking diuretics, ACE inhibitors, and angiotensin II antagonists.
Monitoring for signs or symptoms of gastrointestinal tract hemorrhage and anemia is suggested. For long-term treatment, patients should have complete blood count test (CBC) and chemistry profile check, including hemoglobin or hematocrit.
Discontinue the drug in case of signals and symptoms associated with the development of hepatic or renal disease, systemic manifestations, persistent or worsening of abnormal liver test.
Use in Children: Safety and efficacy of Meloxicam has not been established in children younger than 2 years old.
Use in the Elderly: Increased concentration may occur in elderly patient (particularly in females) because they are at higher risk for serious gastrointestinal ulcer. However, no specific dosage adjustment is recommended.

Safe use of the drug during pregnancy has not been established. It crosses the placenta barrier; therefore it is recommended not to use in pregnancy, except only when the potentials benefit justifies the possible risks to the fetus. Avoid NSAIDs including Meloxicam in the last trimester (30 weeks and above) of pregnancy as premature closure of ductus arteriosus, affecting the lung and heart function of the fetus, may occur.
The drug is distributed in the milk of lactating rats. There are no studies in human; therefore it is not recommended to use in nursing mothers. A decision should be made whether to discontinue nursing or the drug.

Adverse reactions resulting from administration of Meloxicam following: Gastro-intestinal: dyspepsia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhoea, transitory abnormalities of liver function parameters (e.g. raised transaminases or bilirubin), eructation, oesophagitis, gastroduodenal ulcer, occult or macroscopic gastrointestinal bleeding, gastrointestinal perforation, colitis, hepatitis, gastritis.
Haematological: anaemia, disturbances of blood count, including differential white cell count, leukopenia and thrombocytopenia. Concomitant administration of a potentially myelotoxic drug, in particular methotrexate, appears to be a predisposing factor to the onset of a cytopenia.
Dermatological: pruritus, skin rash, stomatitis, urticaria, photosensitisation. On rare occasions bullous reactions, erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis may develop.
Respiratory: cough, pharyngitis, upper respiratory infection, onset of acute asthma has been reported in certain individuals following the administration of aspirin or other NSAIDs, including MELOX.
Central nervous system: lightheadedness, headache, vertigo, tinnitus, drowsiness, insomnia.
Cardiovascular: oedema, increase of blood pressure, palpitations, flush.
Genitourinary: abnormal renal function parameters (increased serum creatinine and/or serum urea), acute renal failure.
Vision disorders: conjunctivitis, visual disturbances including blurred vision.
Other: Flu-like symptoms.

Concomitantly use with angiotensin converting enzyme (ACE) inhibitors, or angiotensin II antagonists may diminish the antihypertensive effect of such drugs.
Concomitantly use with aspirin increases the plasma concentration of Meloxicam, therefore increases adverse drug reactions, especially gastrointestinal ulcers. Coadministration of aspirin or Meloxicam with other NSAIDs is not recommended. Meloxicam is not a substitute for aspirin for cardiovascular prophylaxis.
Concomitantly use with bile acid sequestrants such as cholestyramine can increase plasma clearance of Meloxicam.
Concomitantly use of NSAIDs and diuretics such as furosemide or thiazide can reduce renal blood flow because of decreased prostaglandin synthesis. It is also found reduced natriuresis in some patients. Drug interaction between Meloxicam and furosemide is not found, though. Concomitantly use with diuretics requires closely observing of sign of renal failure as well as diuretic efficacy.
Concomitantly use with lithium increases lithium plasma concentration, following the inhibition of prostaglandin synthesis and decreased renal blood flow, resulting in reduced elimination of lithium.
Closely monitor for sign of lithium toxicity when Meloxicam is introduced, adjusted, or withdrawn.
Concomitantly use of methotrexate and other NSAIDs may increase risk of methotrexate toxicity. Though drug interaction of Meloxicam and methotrexate has not been found, concomitantly use with caution.
Concomitantly use of the drug, as well as other NSAIDs, and warfarin or antiplatelets or anticoagulants, increases the risk of gastrointestinal hemorrhage, and other bleeding. Use with caution and closely monitor prothrombin time and INR, particularly in a first few days after initiating or changing Meloxicam therapy in such patients.
Concomitantly use of the drug, as well as other NSAIDs, with cyclosporine is risk the cyclosporine toxicity; use with caution.
Concomitantly use of the drug and cimetidine or digoxin does not affect pharmacokinetics among the drugs.

Store below 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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