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Meloxicam


Category:

Anti-inflammatory Drugs, Nonsteroidal (NSAIDs)

Composition:

Each tablet contains: Meloxicam 7.5 or 15 mg

Chemistry:

Molecular formula: C14H13N3O4S2 =351.4 [Martindale 35]

Mechanism of Action:

Meloxicam is a nonsteroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, antipyretic activities. The mechanism of action may be related to prostaglandin synthesis inhibition. [USP DI 2007]

Pharmacokinetics:

Meloxicam is well absorbed (bioavalability= 89%) after oral doses. It is 99% bound to plasma proteins (Vd ~ 10 Lit.).the fraction of protein binding decreases to ~ 99% in patients with renal disease. meloxicam is completely metabolized to four pharmacologically inactive metabolites. Cytochrome P-450 2C9 plays an important role in this metabolic pathway, with the minor contribution of the CYP 3A4 isoenzyme. Peroxidase enzyme may inactivate 4 to 16% of administered dose. [PDR 2008] Meloxicam has a plasma-elimination half-life of about 15 to 20 hours. It is extensively metabolized mainly by oxidation and excreted in similar amounts in the urine and in the feces; less than 3% of a dose is excreted unchanged. The volume of distribution is increased in renal failure. [Martindale 35]

Indications:

Meloxicam is used in the management of rheumatoid arthritis, for the short-term symptomatic treatment of acute exacerbations of osteoarthritis, and for the symptomatic treatment of ankylosing spondylitis. It may also be used in the treatment of juvenile idiopathic arthritis. [Martindale 35] However, it is recommended that the use of meloxicam is limited to those patients considered to be at high risk of developing serious gastrointestinal problems if given a non-selective NSAID.

Contraindications:

  • Meloxicam is contraindicated in patients with known hypersensitivity to meloxiam or any of its components. Also it is contraindicated for patients who have experienced asthma, urticaria, or allergic-type reaction after taking aspirin or other NSAIDs.
  • It is contraindicated for treatment peri-operative pain in the setting of coronary artery bypass graft surgery (CABG).

Warnings:

Cardiovascular effect: Cardiovascular thrombotic events. Clinical trials have shown an increased risk of serious cardiovascular (CV) thrombotic events, myocardial infarction and stroke, which can be fatal.
Hypertension: NSAIDs can lead to onset of new hypertension or worsening of pre-existing hypertension, either of witch may contribute to increased risk of CV events. Congestive heart failure and edema: Fluid retention has been observed in some patients. Gastrointestinal effects- risk of GI ulceration, bleeding and perforation: NSAIDs can cause serious GI adverse effects including inflammation, bleeding, ulceration and perforation witch can be fatal.
Renal effects: Long-term administration of NSIADs can result in renal papillary necrosis, renal insufficiency, acute renal failure and other renal injury. Advanced renal disease: If meloxicam therapy is initiated, close monitoring of patient's renal function is advisable. Anaphylactoid
reactions: As with other NSAIDs, anaphylactoid reactions have occurred in patients without prior exposure to meloxicam.
Skin reactions: NSADs can cause serious skin reactions such as dermatitis, Steven's Johnson syndrome, toxic epidermal necrolysis, which can be fatal. Usage in pregnancy: pregnancy category C. Breast-feeding: Because of the potential of serious adverse effect, a decision should be made whether to discontinue nursing or to discontinue the drug. Geriatrics: Caution should be exercised in treating the elderly (65 years and older). [PDR 2008]

Precautions:

Meloxicam should be avoided in severe hepatic impairment, in bleeding disorders, and in patients with renal failure unless receiving dialysis. [Martindale 35] Pre-existing asthma: Patients with asthma may have aspirin-sensitive asthma. Since cross-sensitivity has been reported in some patients (between aspirin and other NSAIDs), meloxicam should not be used in patients with this form of aspirin-sensitivity and should be used with caution in patients with pre-existing asthma. [PDR 2008]

Drug Interactions:

  • ACE-inhibitors: NSAIDs may diminish the hypertensive effect of ACE-inhibitors
  • Asprin: Co-administration of asprin and meloxicam is not recommended because of potential for increased adverse effects.
  • Cholestyramine: Pretreatment for 4 days with cholestyramine significantly increased the clearance of meloxicam by 50%. The clinical relevance of this interaction has not been established.
  • Furosemide: NSAIDs can reduce the natriuretic effect of furosemide and thiazides in some patients.
  • Lithium: Patients on lithium treatment should be monitored closely for signs of lithium toxicity when meloxicam is introduced, adjusted or withdrawn.
  • Warfarin: The effects of warfarin and NSAIDs on GI bleeding are synergistic. Caution should be used when meloxicam is administered in patients on warfarin.

Side effects:

Heart attack, stroke, high blood pressure, heart failure from body swelling, kidney problems including kidney failure, bleeding and ulcers in the stomach and intestine, anemia, life-threatening skin reactions, life-threatening allergic reactions, liver problems including liver failure, asthma attacks in people who have asthma, Stomach pain, constipation, diarrhea, gas, nausea, vomiting, dizziness. [PDR 2008]

Overdosage:

There is limited experience with meloxicam overdose. Symptoms following acute NSAID overdose usually limited to lethargy, nausea, vomiting, and epigastric pain, witch are 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 NSADIs and may occur following an overdose. Patients should be managed with symptomatic and supportive care following an NSAID overdose. In case of acute overdose, gastric lavage followed by activated charcoal is recommended. Gastric lavage performed more than one hour after overdose has little benefit in the treatment of overdose. Administration of activated charcoal is recommended for patients who present11-2 hours after overdose. For substantial overdose or severely symptomatic patients, activated charcoal may be administered repeatedly. Accelerated remove of meloxicam by 4 gram oral doses of cholestyramine given three times a day was demonstrated in a clinical trial. Administration of cholestyramine may be useful following an overdose. Forced duresis, alkalinization of urine, hemodialysis, or hemoperfusion may not be useful due to high protein binding.

Dosage and Administration:

In the treatment of rheumatoid arthritis and ankylosing spondylitis, meloxicam is given by mouth in a usual dose of 15 mg daily as a single dose. Those with an increased risk of adverse reactions should be started on 7.5 mg daily. A dose of 7.5 mg daily is recommended for long-term treatment in the elderly. In the treatment of acute exacerbations of osteoarthritis the usual daily dose of meloxicam by mouth is 7.5 mg, increased if necessary to a maximum of 15 mg daily given as a single dose. BNFC has suggested the following oral doses, according to body-weight, in those aged 12 to 18 years who are intolerant of other NSAIDs:
  • Less than 50 kg, 7.5 mg once daily.
  • Over 50 kg, 15 mg once daily.
Meloxicam is normally contra-indicated in patients with severe renal impairment. However, in dialyzed patients, meloxicam may be given in a dose of 7.5 mg daily by mouth or by rectal suppository.

Storage:

Store below 30 °C, in dry place.
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