Meloxicam Description

Meloxicam (oxicam derivative) belongs to a family of non-steroidal anti-inflammatory drugs (NSAIDs) that also belong to piroxicam and isoxicam. Meloxicam is indicated for the treatment of signs and symptoms of osteoarthritis and is also used as an analgesic to relieve mild to moderate pain.


Meloxicam administered orally, but can also be administered intramuscularly or rectally. After oral administration, absorption is slow to reaching the highest plasma concentrations 4-5 hours. The absolute bioavailability is 90%. The drug undergoes gastrointestinal recirculation since a maximum concentration of second peak is observed at 12-14 hours. Drug absorption is not affected by the presence of food, but 22% increase in peak plasma concentrations. The drug is extensively bound to plasma proteins (99%) in particular albumin. In synovial fluid concentrations are observed 40-50% plasma concentrations, but due to the lower albumin content of synovial fluid, the greater the free fraction of the drug.

Meloxicam is extensively metabolized by CYP2C9 enzyme system (with a minor contribution of CYP3A4), yielding 4 inactive metabolites. 43% of the administered dose was excreted in urine, mainly as metabolites, while the remainder is excreted in the feces. The percentage of native drug in the urine and feces is 0.2% and 1.6% respectively.

Meloxicam exhibits linear pharmacokinetics, with a half-life of elimination of 15 to 20 hours. The state of equilibrium ("steady state") is reached after five doses (onece a day).

In patients with mild hepatic dysfunction (Child class I plug) or moderate (Child class II-Plug) marked differences in plasma concentrations compared to normal patients are not observed. Nor is it affected the degree of binding to plasma proteins. The pharmacokinetic behavior of meloxicam is unknown in patients with severe hepatic impairment (Child's Class C-Plug).

In patients with renal failure, plasma levels of meloxicam decrease depending on the severity of the dysfunction, although the overall clearance increases due to less drug binding to plasma proteins. Similarly, the free fraction of the drug is greater in patients with end stage renal disease compared to healthy volunteers.

Hemodialysis removes meloxicam circulation.

Women show lower compared with men of the same age plasma concentrations of meloxicam. In equilibrium, the elimination half-life is 17.9 hours for women and 21.4 hours for men. However, peak concentrations are similar for both men and women.

In the elderly, men show a pharmacokinetic profile like that of the young. Conversely women after 65 years show a reduced clearance of meloxicam with a 47% higher AUCs and plasma concentrations more elevated than young women 37%. It is believed that this is because in older women is less the free fraction of the drug.

Indications and Ddosages

Treatment of osteoarthritis


  • Initially, 7.5-15 mg once daily. The minimum effective dose should be individualized. The maximum recommended dose is 15 mg / day. With 30 mg / day significantly increases the risk of adverse reactions


  • start treatment with 7.5 mg / day.

Adolescents and children:

  • The safety and efficacy of meloxicam have not been established

Treatment of rheumatoid arthritis


  • Adults have used doses of 7.5 and 15 mg once daily in controlled clinical studies with naproxen. However, no optimal dose determined in patients with rheumatoid arthritis. The dose of 7.5 mg / day meloxicam, is comparable to the dose of 750 mg / day for naproxen in terms of efficiency, with less adverse effects on the digestive tract. In some studies, doses of 15 mg / day have been more effective than 7.5 mg / day when it refers to morning stiffness and grip strength


  • It is recommended to start treatment with the lowest possible doses

Adolescents and children:

  • Adolescents and children aged 2 to 12 years have used doses of 0.125 mg / kg and 0.25 mg / kg daily in patients with juvenile arthritis. Meloxicam showed comparable efficacy and tolerance of naproxen

Short-term treatment of mild to moderate pain


  • 15 mg / day for 7 days


  • It is recommended to start treatment with the lowest possible doses

Adolescents and children:

  • The safety and efficacy of meloxicam have not been established

Maximum recommended doses


  • 15 mg / day

Adolescents and children:

  • The safety and efficacy of meloxicam have not been established. Doses 0.125 and 0.250 mg / kg / day in the treatment of juvenile arthritis

Hepatic impairment - not necessary adjustments to the dose. However, in patients with severe hepatic impairment the administration of meloxicam is not recommended. Renal impairment - not necessary adjust the dose. However, the administration of meloxicam is not recommended when CrCl <15 ml / min.



Meloxicam is absolutely contraindicated in patients with hypersensitivity to the drug. Neither should be used in patients with hypersensitivity to salicylates or other nonsteroidal anti-inflammatory. There have been reports of serious adverse anaphylactic reactions in these patients.

Meloxicam should be used with caution in patients with asthma showing an increased risk of hypersensitivity to aspirin (Samter triad). These patients may experience severe bronchospasm, even fatal, after receiving aspirin or other NSAIDs.

Serious gastric bleeding with ulceration and perforation without notice in patients treated with NSAIDs may result. Patients should be warned of this possibility and monitored to check for bleeding, even in the absence of noticeable symptoms. In the case of meloxicam they have been reported serious hemorrhages and perforations of the digestive tract.

NSAIDs in general and in particular meloxicam should be prescribed with caution in patients who have a history of ulcers, perforation or gastrointestinal bleeding. Patients elderly and debilitated patients are more susceptible to digestive effects of meloxicam. To minimize these effects, we recommend starting treatment with the lowest possible dose. Other factors may be additive in relation to digestive effects of meloxicam are alcohol and snuff, and use of corticosteroids or anticoagulants.

In patients treated with NSAIDs (including meloxicam) it was observed in 15% of cases marked elevations in transaminases. Rarely this condition has progressed to a more severe hepatic reaction (jaundice, fulminant hepatitis and hepatic necrosis). If signs and symptoms suggestive of liver dysfunction advirtiesen, the patient should be carefully monitored discontinuing treatment if they are kept or worse.

Chronic administration of NSAIDs has occasionally produced papillary necrosis and other renal injury. In patients with some form of renal impairment inhibition of renal prostaglandins and therefore the reduction of renal perfusion, produced by meloxicam may precipitate renal decompensation. In general, these patients regain their previous state when the anti-inflammatory is removed.

Meloxicam can induce peripheral edema and fluid retention, caution is recommended in patients with heart failure, fluid retention or hypertension.

If you start a treatment in dehydrated patients there should be a proper hydration before administering meloxicam.

Meloxicam, like other NSAIDs can worsen a state of preexisting anemia. It is recommended that these patients be periodically evaluated certain levels of hemoglobin and hematocrit.

Meloxicam is classified in category C pregnancy risk. Although meloxicam did not alter fertility in rats at doses between 2.5 and 5 times the human dose, an increase in lethality in embryos when the drug was administered to pregnant females, particularly during the period of organogenesis was observed. There have been no controlled studies in human pregnancy so that the drug will only be used if the potential benefit to the mother justifies the potential risk to the fetus. In particular its use should be avoided during the third trimester to avoid a defective closure of the ductus arteriosus.

Meloxicam is excreted in the milk of laboratory animals, not knowing if so does in humans. Because of the potential adverse effects that the drug may cause a nursing its use is not recommended during breastfeeding, having to seek alternatives to it (drug discontinuation or artificial feeding.


Drug Interaction

The potential effects of enzyme inducers or inhibitors of cytochrome P450 metabolism of meloxicam is unknown.

There are following interactions of meloxicam with other drugs:

ACE inhibitors: the nonsteroidal anti-inflammatories including meloxicam, can reduce the antihypertensive effect of inhibitors converting enzyme inhibitors, can cause uncontrolled hypertension

Aspirin administration of 1 g of aspirin twice daily to healthy volunteers AUC increased slightly (10%) and Cmax (24%) of meloxicam. The clinical significance of this interaction is unknown. However, concomitant administration of meloxicam and aspirin (or other nonsteroidal anti-inflammatory) is not recommended because the side effects may be additive.

Cholestyramine: administration of cholestyramine for 4 days before starting treatment with meloxicam increases clearance of the latter by 50% with a parallel reduction of the AUCs and elimination half-life. It has been suggested that this interaction could be useful in cases of overdose of meloxicam

Cimetidine despite cimetidine be a known inhibitor of CYP2C9 and CYP2D6 enzyme systems administration at a dose of 200 mg four times a day it did not affect the pharmacokinetics of a dose of 30 mg meloxicam.

Digoxin: Administration of meloxicam 15 mg / day did not affect plasma concentrations of digoxin. Nor it has found no interaction between meloxicam and digoxin as regards binding to plasma proteins.

Furosemide: the non-steroidal anti-inflammatories, including meloxicam, can reduce the natriuretic effect of furosemide and thiazide diuretics. This effect is due to the inhibiting effects of NSAIDs on renal prostaglandins. Although the studies conducted have not been observed interactions between furosemide and meloxicam, it is recommended to monitor renal function if meloxicam is administered concomitantly with diuretics.

Lithium: meloxicam administration induces an elevation of plasma lithium levels and reduced renal clearance. This effect is attributed to the effects of meloxicam on renal prostaglandins. It is recommended to monitor plasma levels of lithium if meloxicam is administered concomitantly.

Methotrexate has not been proven any interaction between methotrexate and meloxicam, while other NSAIDs reduce the clearance of the first with the corresponding risk of toxicity.

Warfarin: the concomitant administration of meloxicam and warfarin may increase the risk of bleeding in anticoagulated patients. Has occasionally checked INR increased in some subjects treated with warfarin and meloxicam, although in most cases have not been observed pharmacokinetic or pharmacodynamic interactions type. Caution is advised in patients anticoagulated because the meloxicam increases the risk of bleeding. INR monitoring is recommended when the new medication is introduced.

Other gastrolesive drugs: treatment with meloxicam in patients who consume alcohol or receive corticosteroids or other NSAIDs should be carefully monitored. An additive effect of the adverse effects on the digestive tract may occur. Although not specifically evaluated the interaction between meloxicam and alendronate, in a retrospective study, patients treated with both drugs showed an increase of 70% in the risk for gastric bleeding.

Meloxicam, like other anti-inflammatory drugs, possesses a certain antipyretic and analgesic activity can mask the symptoms of an infection, particularly in immunocompromised patients.

Some preclinical observations suggest that drugs that inhibit prostaglandin synthesis may reduce the effectiveness of photodynamic therapy with porfimer or verteporfin

Side Effects

Controlled trials have shown that the incidence of gastrointestinal side effects is lower than that observed with other NSAIDs such as piroxicam, diclofenac or naproxen. However, there have been reports of serious cases of gastrointestinal bleeding and perforation with meloxicam, and adverse reactions were gastrointestinal type who demonstrated more frequently. In a study of 12 months duration, the overall incidence of gastrointestinal adverse reactions was 17.3% at a dose of 7.5 mg / day and 20.1% with the dose of 15 mg. In this study, diclofenac (100 mg / day in a gradual release tablet) produced a 28.1%, while the placebo was 17.2%, that is only slightly less that meloxicam.

The most common gastrointestinal effects observed with doses of 7.5 and 15 mg / day of meloxicam were abdominal pain (1.9% vs. 2.6%), diarrhea (7.8% vs. 3.2%), dyspepsia (4.5% vs. 4.5%) , flatulence (3.2% vs. 3.2%) and nausea / vomiting (3.9% vs. 3.8%).

Other less common gastrointestinal effects (0.1-1.9%) are colitis, dry mouth, peptic ulcer, eructation, esophagitis, gastritis, gastroesophageal reflux, digestive tract bleeding, hematemesis, melena, pancreatitis, gastrointestinal perforations and ulcerative stomatitis.

Up to 15% of patients treated with meloxicam (and other NSAIDs) an elevation of transaminases or bilirubin may develop. These alterations of the representative parameters of liver function may be transient, disappearing with continued treatment or may remain or worsen. For meloxicam, hepatitis have been reported in <2% of patients, while the incidence of jaundice and hepatic failure was <0.1%. If clinical symptoms or systemic symptoms consistent with liver disease (eosinophilia, rash, etc.) are discovered should discontinue treatment with meloxicam.

It has been reported anemia (0-4-1%) and other rare hematological adverse reactions during treatment with meloxicam (leukopenia, purpura, thrombocytopenia). Very rarely (<0.1%) has occurred agranulocytosis. A watch on hematological parameters, particularly hemoglobin and hematocrit if symptoms of anemia or bleeding were complied recommended.

Or respiratory allergic reactions are rare (0.1-1.9%) and include angioedema, asthma, bronchospasm, dyspnea and fever. Very rarely (<0.1) anaphylactic reactions have been reported. Patients with hypersensitivity to aspirin are at an increased risk for these reactions. Patients who develop urticaria, bronchospasm and other symptoms of an anaphylactic reaction should be taken immediately to an emergency department.

Other relatively common (but similar to placebo) adverse effects are dizziness (2.6-3.8% vs. placebo 3.2%), influenza-like symptoms (4.5-5.8% vs. placebo 5.1%), pharyngitis (0.6-3.2% vs. placebo 1.3%) and upper respiratory tract infections (1.9-3.2% vs. placebo 1.9%).

In 2.6% of patients treated with 7.5 mg of meloxicam a nonspecific rash occurred in 0.6% of patients treated with 15 mg / day and 2.5% of those treated with placebo. Other dermatological reactions observed (regardless of causality) were alopecia, bullous rash, pruritus, photosensitivity, increased sweating, and hives. Are few cases in which meloxicam has been associated with erythema multiforme, a toxic epidermal necrolysis or a Stevens-Johnson syndrome.

Edema (in its broadest definition) has been observed in 1.9-4.5% of patients treated with meloxicam. Other rare side effects (0.1-1.9%) related to fluid retention are weight gain, heart failure and hypertension. They also are rare adverse reactions such as renal albuminuria, azotemia, increased serum creatinine, hematuria and renal failure. Interstitial nephritis occurs in <0.1% of cases.