Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and fever reducer effects. It is an oxicam closely related to piroxicam, and falls in the enolic acid group of NSAIDs. It was developed by Boehringer-Ingelheim. Meloxicam starts to relieve pain about 30-60 minutes after administration.
As of 2015 the cost for a typical month of medication in the United States is less than $25 USD.
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Side effects
Meloxicam use can result in gastrointestinal toxicity and bleeding, headaches, rash, and very dark or black stool (a sign of intestinal bleeding). Like other NSAIDs, its use is associated with an increased risk of cardiovascular events such as heart attack and stroke. It has fewer gastrointestinal side effects than diclofenac, piroxicam, naproxen, and perhaps all other NSAIDs which are not COX-2 selective. Although meloxicam inhibits formation of thromboxane A, it does not appear to do so at levels that would interfere with platelet function.
A pooled analysis of randomized, controlled studies of meloxicam therapy of up to 60 days duration found that meloxicam was associated with a statistically significantly lower number of thromboembolic complications than the NSAID diclofenac (0.2% versus 0.8% respectively) but a similar incidence of thromboembolic events to naproxen and piroxicam.
Cardiovascular side effects
Persons with hypertension, high cholesterol, or diabetes are at risk for cardiovascular side effects. Persons with family history of heart disease, heart attack, or stroke must tell their treating physician as the potential for serious cardiovascular side effects is significant.
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Mechanism of action
Meloxicam blocks cyclooxygenase (COX), the enzyme responsible for converting arachidonic acid into prostaglandin H2--the first step in the synthesis of prostaglandins, which are mediators of inflammation. Meloxicam has been shown, especially at its low therapeutic doses, selectively to inhibit COX-2 over COX-1.
Meloxicam concentrations in synovial fluid 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 as compared to plasma. The significance of this penetration is unknown, but it may account for the fact that it performs exceptionally well in treatment of arthritis in animal models.
Veterinary use
Meloxicam is used in veterinary medicine, most commonly in dogs and cats, but also sees off-label use in other animals such as cattle and exotics.
Side effects in animals are similar to those found in humans; the principal side effect is gastrointestinal irritation (vomiting, diarrhea, and ulceration). Rarer but important side effects include liver and kidney toxicity.
A peer-reviewed journal article cites feline overdose of NSAIDs, including meloxicam, as being a cause of severe kidney damage in cats.
Meloxicam has been investigated as an alternative to Diclofenac by the RSPB to prevent deaths of vultures.
Pharmacokinetics
In dogs, the absorption of meloxicam from the stomach is not affected by the presence of food, with the peak concentration (Cmax) of meloxicam occurring in the blood 7-8 hours after administration. The half-life of meloxicam is approximately 24 hours in dogs.
In the koala (Phascolarctos cinereus), very little meloxicam is absorbed into the blood after oral administration (that is, it has poor bioavailability).
Legal status
United States
Since 2003, meloxicam has been approved in the U.S. for use in dogs for the management of pain and inflammation associated with osteoarthritis, as an oral (liquid) formulation of meloxicam. In January 2005, the product insert added a warning in bold-face type: "Do not use in cats." An injectable formulation for use in dogs was approved by the FDA in November 2003.
In October 2004, a formulation for use in cats was approved for use prior to surgery only. This is an injectable meloxicam, indicated for as a single, one-time dose only, with specific and repeated warnings not to administer a second dose.
In 2005, the U.S. Food and Drug Administration sent a Notice of Violation to the manufacturer for its promotional materials which included promotion of the drug for off-label use.
European Union
In Europe, where the product has been available since the early 1990s, it is licensed for other anti-inflammatory benefits including relief from both acute and chronic pain in dogs. In June 2007, an oral version of meloxicam was licensed for the long-term relief of pain in cats. Meloxicam is also licenced for use in horses, to relieve the pain associated with musculoskeletal disorders.
Other countries
As of June 2008, meloxicam is registered for long-term use in cats in Australia, New Zealand, and Canada.
Source of the article : Wikipedia
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