Meloxicam has been shown, especially at low therapeutic doses, to selectively 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. Pharmacokinetics
Absorption
The bioavailability of meloxicam is decreased when administered orally compared to an equivalent IV bolus dose. 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 of antacids does not show pharmacokinetic interactions. Distribution
The mean volume of distribution of meloxicam is approximately 10L. It is highly protein-bound, mainly to albumin. Metabolism
Meloxicam is extensively metabolized in the liver by the enzymes CYP2C9 and CYP3A4 (minor) into four inactive metabolites. Peroxidase activity is thought to be responsible for the other two remaining metabolites. Excretion
Meloxicam is predominantly excreted in the form of metabolites and occurs to equal extents in the urine and feces. Traces of unchanged parent drug are found in urine and feces. The mean elimination half-life ranges from 15 to 20 hours. Specific populations
Geriatrics
Use of meloxicam is not recommended in people with peptic ulcer disease or increased gastrointestinal bleed risk, including those over 75 years of age or those taking medications associated with bleeding risk.
Meloxicam, sold under the brand name Mobic among others, is a nonsteroidal anti-inflammatory medication (NSAID) used to treat pain and inflammation in rheumatic diseases and osteoarthritis. It is used by mouth or by injection into a vein. It is recommended that it be used for as short a period as possible and at a low dose.Common side effects include abdominal pain, dizziness, swelling, headache, and a rash. Serious side effects may include heart disease, stroke, kidney problems, and stomach ulcers. Use is not recommended in the third trimester of pregnancy. It blocks cyclooxygenase-2 (COX-2) more than it blocks cyclooxygenase-1 (COX-1). It is in the oxicam family of chemicals and is closely related to piroxicam.Meloxicam was patented in 1977 and approved for medical use in the United States in 2000. It was developed by Boehringer Ingelheim; however, it is also available as a generic medication. In 2020, it was the 28th most commonly prescribed medication in the United States, with more than 19 million prescriptions. An intravenous version of meloxicam (Anjeso) was approved for medical use in the United States in February 2020. Adverse 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.