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| Clinical data | |
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| Trade names | Mobic, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601242 |
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| Pregnancy category | |
| Routes of administration | By mouth,intravenous |
| Drug class | Nonsteroidal anti-inflammatory drug (NSAID) |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | 89%[9] |
| Protein binding | 99.4%[9] |
| Metabolism | Liver (CYP2C9 and3A4-mediated)[9] |
| Eliminationhalf-life | 20 hours[9] |
| Excretion | Urine andfeces equally[9] |
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| DrugBank |
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| PDB ligand | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.113.257 |
| Chemical and physical data | |
| Formula | C14H13N3O4S2 |
| Molar mass | 351.40 g·mol−1 |
| 3D model (JSmol) | |
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Meloxicam, sold under the brand nameMobic among others, is anonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation inrheumatic diseases andosteoarthritis.[10][11] It is taken by mouth or given byinjection into a vein.[11][12] It is recommended that it be used for as short a period as possible and at a low dose.[11]
Common side effects include abdominal pain, dizziness, swelling, headache, and a rash.[11] Serious side effects may includeheart disease,stroke, kidney problems, andstomach ulcers.[11] Use is not recommended in thethird trimester of pregnancy.[11] It blockscyclooxygenase-2 (COX-2) more than it blockscyclooxygenase-1 (COX-1).[11] It is in theoxicam family of chemicals and is closely related topiroxicam.[11]
It is available as ageneric medication.[11] In 2023, it was the 27th most commonly prescribed medication in the United States, with more than 20 million prescriptions.[13][14] An intravenous version of meloxicam (Anjeso) was approved for medical use in the United States in February 2020.[15][12] Meloxicam is available in combination with bupivacaine asbupivacaine/meloxicam and in combination with rizatriptan asmeloxicam/rizatriptan.
Meloxicam isindicated for the treatment ofosteoarthritis,rheumatoid arthritis, andjuvenile rheumatoid arthritis.[3]
Meloxicam use can result ingastrointestinal toxicity and bleeding, headaches, rash, andvery dark or black stool (a sign of intestinal bleeding). It has fewer gastrointestinal side effects thandiclofenac,[16]piroxicam,[17]naproxen,[18] and perhaps all other NSAIDs which are not COX-2 selective.[16]
In October 2020, the USFood and Drug Administration (FDA) required theprescribing information to be updated for all nonsteroidal anti-inflammatory medications to describe the risk of kidney problems in unborn babies that result in low amniotic fluid.[19][20] They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy.[19][20]
Like otherNSAIDs, its use is associated with an increased risk of cardiovascular events such asheart attack andstroke.[21] Although meloxicam inhibits formation ofthromboxane A, it does not appear to do so at levels that would interfere withplatelet function.[22][23] 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 ofthromboembolic complications than the NSAID diclofenac (0.2% versus 0.8% respectively) but a similar incidence of thromboembolic events to naproxen and piroxicam.[24]
People withhypertension,high cholesterol, ordiabetes are at risk for cardiovascular side effects. People with family history of heart disease, heart attack, or stroke should tell their treating physician as the potential for serious cardiovascular side effects is significant.[11][25]
NSAIDs cause an increase in the risk of seriousgastrointestinal adverse events including bleeding,ulceration, and perforation of the stomach or intestines, which can be fatal. Elderly patients are at greater risk for serious gastrointestinal events.[11]
Meloxicam blockscyclooxygenase (COX), theenzyme responsible for convertingarachidonic acid intoprostaglandin H2—the first step in the synthesis ofprostaglandins, which are mediators of inflammation.Meloxicam has been shown, especially at lowtherapeutic doses, to selectively inhibitCOX-2 overCOX-1.[9]
X-ray crystallographic analyses and molecular modelling studies of meloxicam´s binding to cyclooxygenase isoforms showed that the methyl group of the thiazole ring in meloxicam exploits the „flexible extra space" at the top of the COX-2 chanel. The substitution of the second shell amino acid residue Ile434 in COX-1 by Val in COX-2 allows the side chain of Phe518 (a residue at the active side) to open „extra space“, which favors the binding of meloxicam to COX-2. Site-directed mutagenesis studies in which Ile434 was substituted for Val434 in COX-2 confirmed this hypothesis.[26] Other oxicams also occupy this binding site, albeit nonselectively because of the missing methyl group in the side chain.[27]
Meloxicam concentrations insynovial fluid range from 40% to 50% of those inplasma. The free fraction in synovial fluid is 2.5 times higher than in plasma, due to the lower albumin content in synovial fluid compared to plasma. The significance of this penetration is unknown,[11] but it may account for the fact that it performs exceptionally well in treatment of arthritis in animal models.[28]
Thebioavailability of meloxicam is decreased when administered orally compared to an equivalent IV bolus dose. Different oral formulations of meloxicam are notbioequivalent.[11] Use of oral meloxicam following a high-fat breakfast increases the mean peak drug levels by about 22%; however, the manufacturer does not make any specific meal recommendations. In addition, the use ofantacids does not show pharmacokinetic interactions.[3] With chronic dosing, the time to maximum plasma concentration following oral administration is approximately 5–6 hours.[29]
The mean volume of distribution of meloxicam is approximately 10 L. It is highly protein-bound, mainly toalbumin.[23][29]
Meloxicam is extensively metabolized in the liver by the enzymesCYP2C9 andCYP3A4 (minor) into four inactive metabolites.Peroxidase activity is thought to be responsible for the other two remaining metabolites.[11][3]
Meloxicam is predominantly excreted in the form of metabolites and occurs to equal extents in the urine and feces.[3] Traces of unchanged parent drug are found in urine and feces.[3] The mean elimination half-life ranges from 15 to 20 hours.[3]
Adverse events are dose-dependent and associated with length of treatment.[3][30]
In the 1970s, chemists at Dr. Karl Thomas GmbH, a subsidiary of Boehringer-Ingelheim in Germany, synthesized a variety of enol carboxamides with the aim of obtaining active ingredients with anti-inflammatory or antithrombotic properties.[31] A compound belonging to the oxicams (UH-AC 62, meloxicam) stood out, exhibiting antiinflammatory activity in the pharmacological adjuvant arthritis model, but only low antithrombotic efficacy as measured by platelet aggregation.[23] Dr. Karl Thomas GmbH filed the German basic patent DE2756113 (1979) and Boehringer Ingelheim US patent 4,233,299 (1980) and patents in many other countries.[32]
Meloxicam is used inveterinary medicine mainly to treat dogs,[33][34] but also seesoff-label use in other animals such as cattle and exotics.[35][36] In the European Union and other countries it is not considered off-label and can be used in cattle, pigs, horses, dogs, cats and guinea pigs.[37] It has also been investigated as an alternative todiclofenac by theRoyal Society for the Protection of Birds (RSPB) to prevent deaths ofvultures.[38]
Depending on the animal species, each country or union of countries applies different guidelines or legal frameworks for the use of the drug, as well as different recorded side effects. The most common side effects in dogs include gastrointestinal irritation (vomiting, diarrhea, andulceration).[33] As far as the perioperative administration is concerned, in healthy dogs given meloxicam, no perioperative adverse effects on the cardiovascular system have been reported at recommended dosages.[39] Perioperative administration of meloxicam to cats did not affect postoperative respiratory rate nor heart rate.[40]
The issue of using meloxicam in cats involves conflicting guidelines, differing legislation, and a narrow therapeutic safety margin that can easily turn the drug from cure to poison. More specifically:
The USFood and Drug Administration (FDA) approves the use of meloxicam in cats only in injectable form and only as a one-time injection given before surgery.[41][42] It does not approve meloxicam oral suspension for cats and it does not approve meloxicam spray for cats because after reviewing numerous reports of meloxicam side effects in cats, it has identified many cases ofacute renal failure anddeath and has added the following boxed warning to the prescription label: "Repeated use of meloxicam in cats has been associated with acute renal failure and death. Do not administer additional injectable or oral meloxicam to cats. See Contraindications, Warnings, and Precautions for detailed information."[43]
In contrast, in the European Union and other continents or countries, the use of the drug in cats is allowed with no such warning.[44][45] The product instruction leaflet for meloxicam for cats in the form of oral suspension 0.5 mg/ml states that: "Typical adverse reactions ofNSAIDs such as loss of appetite, vomiting, diarrhoea, faecal occult blood, apathy, and renal failure have occasionally been reported. These side effects are in most cases transient and disappear following termination of the treatment but in very rare cases may be serious or fatal."[46]
The data sheets for meloxicam products for cats also state that: "Meloxicam has a narrow therapeutic safety margin in cats and clinical signs of overdose may be seen at relatively small overdose levels."[46]
Some additional information about giving meloxicam to cats from researchers is as follows: A peer-reviewed journal article cites NSAIDs, including meloxicam, as causing gastrointestinal upset and, at high doses,acute kidney injury andCNS signs such as seizures and comas in cats. It adds that cats have a low tolerance for NSAIDs.[47][48] Also, in another scientific journal there is talk of research according to which cats that received meloxicam had greaterproteinuria at 6 months than cats that received placebo. It was concluded that meloxicam should be used with caution in cats with chronic kidney disease.[49]
In dogs, theabsorption of meloxicam from the stomach is not affected by the presence of food,[50] with the peak concentration (Cmax) of meloxicam occurring in the blood 7–8 hours after administration.[50] Thehalf-life of meloxicam is approximately 24 hours in dogs.[50] In thekoala (Phascolarctos cinereus), very little meloxicam is absorbed into the blood afteroral administration (that is, it has poorbioavailability).[51]
2003: Meloxicam was approved in the US for use in dogs for the management of pain and inflammation associated withosteoarthritis, as anoral (liquid) formulation of meloxicam.[52]
2003 (November): Aninjectable formulation for use in dogs was approved by the USFood and Drug Administration (FDA).[53]
2004 (October): A formulation for use in cats was approved for use before surgery only.[54] 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.[55]
2005 (January): The product insert added a warning in bold-face type: "Do not use in cats."[56]
2005: The FDA sent a Notice of Violation to the manufacturer for its promotional materials which included promotion of the drug for off-label use.[57]
2020 (February): A meloxicam injection was approved for use in the United States. Specifically, the FDA granted the approval of Anjeso to Baudax Bio.[12][58]
In the European Union, meloxicam is licensed for other anti-inflammatory benefits including relief from bothacute andchronic pain in dogs. Meloxicam is also licensed for use in horses, to relieve the pain associated withmusculoskeletal disorders.[59]
1998 (January): Meloxicam was authorised for use in cattle throughout the European Union, via acentralised marketing authorisation.[60]
2006: The firstgeneric meloxicam product was approved.[60]
2024 (January): EMA issued an 'Opinion'[61] on a change to this medicine's authorisation concerning the follow-up oral treatment after initial injectable administration in cats. This change remains as an 'Opinion', while the medication continues to be approved as usual.[62]
As of June 2008[update], meloxicam was registered for long-term use in cats in Australia, New Zealand, and Canada.[63]
In the United Kingdom, meloxicam is licensed for use in cats, guinea pigs, horses, and livestock including pigs and cattle.[64]
This article incorporates text from this source, which is in thepublic domain. This article incorporates text from this source, which is in thepublic domain.Meloxicam is extensively bound to plasma proteins (99.4%), primarily to albumin. Meloxicam has an apparent volume of distribution (Vd) 10 – 15 L in humans (0.1 – 0.2 L/kg) after oral administration and a mean volume of distribution at steady-state of 0.2 L/kg after intravenous administration."
"None of the meloxicam treatment groups demonstrated inhibition of platelet aggregation to either arachidonic acid (AC) or adenosine diphosphate (ADP). However, there were no significant changes in the platelet count, prothrombin, and activated partial thromboplastin time in any of the meloxicam and indomethacin groups. Other crossover studies also confirmed that meloxicam 15 mg/day caused a major reduction of maximum thromboxane production, but no reduction in collagen- or AC-induced platelet aggregation.
{{cite journal}}: CS1 maint: numeric names: authors list (link)Metacam is a prescription non-steroidal anti-inflammatory drug (NSAID) that is used to control pain and inflammation (soreness) due to osteoarthritis in dogs. Osteoarthritis (OA) is a painful condition caused by "wear and tear" of cartilage and other parts of the joints that may result in the following changes or signs in your dog: Limping or lameness, decreased activity or exercise (reluctance to stand, climb stairs, jump or run, or difficulty in performing these activities), stiffness or decreased movement of joints. Metacam is given to dogs by mouth. Do not use Metacam Oral Suspension in cats.Acute kidney injury and death have been associated with the use of meloxicam in cats.
| pyrazolones / pyrazolidines | |
|---|---|
| salicylates | |
| acetic acid derivatives and related substances | |
| oxicams | |
| propionic acid derivatives (profens) |
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| n-arylanthranilic acids (fenamates) | |
| COX-2 inhibitors (coxibs) | |
| other | |
| NSAID combinations | |
Key:underline indicates initially developed first-in-class compound of specific group;#WHO-Essential Medicines;†withdrawn drugs;‡veterinary use. | |
