How Effective Is Meloxicam for Pain?

Meloxicam tablets, the indication is-short-term symptoms treatment when osteoarthritis symptoms worsen. -Long-term treatment of rheumatoid arthritis and ankylosing spondylitis.

Drug Name: Meloxicam

Drug type: Prescription drugs, medicines for medical workers' injuries
Use classification: Enoic acid

Meloxicam tablet ingredients

Meloxicam Chemical Name: 4-hydroxy-2-methyl-N- (5-methyl-2-thiazolyl) -2H-1,2-benzothiazine-3-carboxamide-1,1- Dioxide.
Chemical Structure:

Molecular formula: C ₁₄ H ₁₃ N ₃ O ₄ S ₂
Molecular weight: 351.39

Meloxicam Tablet Properties

This product is a light yellow tablet.

Meloxicam tablets indications

-Short-term treatment of osteoarthritis symptoms.
-Long-term treatment of rheumatoid arthritis and ankylosing spondylitis.

Meloxicam Tablet Specifications

7.5mg

Meloxicam tablets dosage

oral.
-When the symptoms of osteoarthritis worsen: 1 tablet at a time, once a day. If the symptoms do not improve, the dose can be increased to 2 tablets at a time, once a day; 7.5mg per tablet.
-Rheumatoid arthritis and ankylosing spondylitis: 2 tablets at a time, once a day, depending on the response after treatment, the dose can be reduced to 1 tablet at a time, once a day; 7.5 mg per tablet (see "Special Population") .
The daily dose should not exceed 15 mg / day.
The total daily dose should be taken all at once and taken with water or other fluids with food.
Elderly patients in special populations and patients at increased risk of adverse reactions;
For elderly patients, the recommended dose for long-term treatment of rheumatoid arthritis and ankylosing spondylitis is 7.5 mg / day. The starting dose for patients with an increased risk of adverse reactions is 7.5 mg / day.
Patients with renal insufficiency:
In patients with severe renal failure who need dialysis, the dose should not exceed 7.5 mg / day.
Patients with mild and moderate renal insufficiency do not need to adjust the dose (eg, the patient's creatinine clearance is greater than 25ml / min).
For patients with severe renal failure who do not require dialysis, see [Contraindications].
Patients with liver dysfunction:
Patients with mild and moderate hepatic insufficiency do not need to adjust the dose.
For patients with severe liver dysfunction, see [Contraindications].
child:
This product should not be used by children under 15 years of age. Meloxicam is available in other dosage forms and may be suitable.

Adverse reactions to meloxicam

a) General Some of the adverse reactions reported below may be related to the use of meloxicam. The frequencies listed below were obtained in clinical trials, and the corresponding causality was not investigated. This information is based on clinical trials conducted on 3750 patients over 18 months, with patients taking meloxicam tablets or capsules daily at a dose of 7.5 or 15 mg (the average time for treatment is 127 days). Includes reports of adverse reactions that may have been related to the use of meloxicam after receiving this product.
The following convention is used to indicate the incidence of adverse reactions:
Very common (1 / 10); common (1 / 100, <1/10);
Rare (1 / 1000, <1/100): Rare (1 / 10000, <1/1000);
Very rare (<1/10000).
b) Adverse reactions Blood and lymphatic disorders:
Common: Anemia.
Rare: Imbalanced blood count, leukopenia, thrombocytopenia, agranulocytosis (see section c).
Immune system disorders:
Rare: allergic / allergic reaction.
Mental disorders:
Rare: mood disorders, insomnia, and nightmares.
Neurological disorders:
Common: slight dizziness, headache.
Rare: dizziness, tinnitus, drowsiness.
Rare: Chaos.
Eye disorders:
Rare: Visual impairment includes blurred vision.
Cardiac disorders:
Rare: palpitations.
Vascular disorders:
Rare: elevated blood pressure, flushing.
Respiratory, thorax, and mediastinal disorders:
Rare: Individual patients have asthma attacks after taking aspirin or other nonsteroidal anti-inflammatory drugs.
Gastrointestinal:
Common: Indigestion, nausea and vomiting symptoms, abdominal pain, constipation, flatulence, diarrhea.
Rare: gastrointestinal bleeding, peptic ulcer, esophagitis. Stomatitis.
Rare: gastrointestinal perforation, gastritis, colitis, peptic ulcer, perforation or gastrointestinal bleeding are sometimes severe, especially for elderly patients.
Hepatobiliary disorders:
Rare: transient abnormal liver function indicators (such as elevated aminotransferase or bilirubin).
Rare: hepatitis.
Skin and subcutaneous tissue disorders:
Common: itching, rash.
Rare: urticaria.
Rare: Steven-Johnson syndrome and lax toxic epidermal necrosis, angioedema, bullous reactions such as erythema polymorpha, photosensitivity.
Kidney and urinary disorders:
Rare: abnormal renal function indicators (such as elevated serum creatinine or urea).
Rare: renal failure.
Whole body system
Common; Edema includes edema of the lower extremities.
c) Individual and specific serious and / or possible adverse reactions. Individuals have reported agranulocytosis after meloxicam and other potentially myelotoxic drugs.

Meloxicam taboo

In the following cases, this product is disabled:
-Pregnant or breastfeeding (see [Medication for pregnant and lactating women]);
-People who are allergic to the active ingredient meloxicam or its excipients or those allergic to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs. This product is not suitable for patients with asthma, nasal polyps, angioedema or urticaria after using acetylsalicylic acid or other non-steroidal anti-inflammatory drugs
-Patients with active peptic ulcers or patients with a history of recurrent peptic ulcers;
-Severe liver dysfunction;
-Non-dialysis severe renal insufficiency;
-Gastrointestinal bleeding. Patients with cerebral hemorrhage or other bleeding disorders;
-Severe uncontrolled heart failure.

Precautions for Meloxicam

-Patients with esophagitis, gastritis and / or peptic ulcer should ensure that these diseases are cured before using this product. The use of meloxicam in patients with a history of this type should be regularly noted for the possibility of recurrence of these diseases.
-Patients with gastrointestinal symptoms or a history of gastrointestinal disorders (eg ulcerative colitis. Localized ileitis) should be monitored for symptoms of gastrointestinal discomfort, especially gastrointestinal bleeding.
-As with other nonsteroidal anti-inflammatory drugs, gastrointestinal bleeding or ulcers / perforations can occur at any stage of treatment with this product, in some cases fatal, with or without aura symptoms, and patients may or may not have A history of severe gastrointestinal disorders. The consequences of gastrointestinal bleeding or ulcers / perforations in older patients are more severe.
-Stop using this product if peptic ulcer or gastrointestinal bleeding occurs.
-Non-steroidal anti-inflammatory drugs including meloxicam are known to cause severe skin adverse reactions and severe life-threatening allergic reactions (such as allergic reactions). In these cases, stop using this product and observe it carefully.
-Rarely, nonsteroidal anti-inflammatory drugs may cause interstitial nephritis. Glomerulonephritis, renal medulla necrosis or nephrotic syndrome.
-As with most other nonsteroidal anti-inflammatory drugs, occasional reports of elevated serum transaminase, elevated serum bilirubin, or other parameters of liver function, including serum creatinine, blood urinary nitrogen, and other laboratory abnormalities. Most cases are only transient and minor anomalies. If this abnormality is significant or persistent, the product should be discontinued and followed up.
-Use of non-steroidal anti-inflammatory drugs may cause sodium, potassium, and water retention and affect the natriuretic effect of diuretics, exacerbating symptoms in patients with heart failure or hypertension.
-Nonsteroidal anti-inflammatory drugs have an inhibitory effect on the prostaglandin synthesis that supports the maintenance of renal perfusion. For patients with reduced renal blood flow and blood volume, the use of nonsteroidal anti-inflammatory drugs may cause decompensation of underlying renal failure. However, treatment with non-steroidal anti-inflammatory drugs stopped and returned to the state before treatment. This risk may be associated with elderly patients, patients with congestive heart failure, patients with cirrhosis, patients with nephrotic syndrome or renal failure, and patients treated with diuretics, as well as those with reduced blood volume due to major surgery patient. The diuretic capacity and renal function of these patients should be carefully monitored at the beginning of treatment.
-Elderly patients, frail or debilitated patients are generally less tolerant of side effects, and these patients should be carefully monitored. As with other nonsteroidal anti-inflammatory drugs, care should be taken when treating older patients who are more vulnerable to kidney, liver, or heart damage.
-Do not exceed the maximum recommended daily dose or add another non-steroidal anti-inflammatory drug to the treatment, even if you do not get a satisfactory therapeutic effect, because this will increase the toxic effect and the effect may not increase. If symptoms do not improve after several days of treatment, the effect of treatment should be re-evaluated.
-Meloxicam, like other nonsteroidal anti-inflammatory drugs, may mask symptoms of underlying infectious diseases.
-The use of meloxicam, like any drug known to inhibit cyclooxygenase / prostaglandin synthesis, may damage fertility, so women who are preparing to conceive are not recommended to use this product. Meloxicam should be discontinued in women who have difficulty in conception or are undergoing infertility testing.
Impact on the ability to drive and operate machines No special studies have been conducted on the impact on the ability to drive and operate machines. Based on its pharmacodynamic properties and reported adverse drug reactions, meloxicam should have little or no effect on this ability. However, in the event of visual impairment or drowsiness, dizziness, or other central nervous system disorders, it is recommended to avoid driving and operating machines.

Meloxicam tablets for pregnant and lactating women

Pregnant women-animal tests have lethal doses higher than clinical doses;
-It is recommended not to take meloxicam during the first six months of pregnancy;
-In the last trimester of pregnancy, all prostaglandin synthesis inhibitors can cause cardiopulmonary (pulmonary hypertension with premature closure of arterial ducts) and kidney toxicity to the fetus or inhibit uterine contractions. This effect on the uterus is associated with an increased chance of dystocia and delayed births in animals. Therefore, the use of nonsteroidal anti-inflammatory drugs is absolutely prohibited in the last trimester of pregnancy.
Non-steroidal anti-inflammatory drugs enter breast milk of lactating women. Therefore, breastfeeding women should avoid nonsteroidal anti-inflammatory drugs.

Meloxicam tablets for children

This product should not be used by children under 15 years of age. Meloxicam is available in other formulations and may be suitable.

Meloxicam tablets for the elderly

Compared with young people, the average steady-state plasma clearance of the elderly is slightly reduced.
For elderly patients, the recommended dose for long-term treatment of rheumatoid arthritis and ankylosing spondylitis is 7.5 mg / day.
Elderly patients are generally less tolerant of side effects and should be carefully examined.

Meloxicam tablets drug interactions

Pharmacodynamic Interactions:
Other non-steroidal anti-inflammatory drugs include salicylate (acetylsalicylic acid 3g / day):
Concurrent use of several nonsteroidal anti-inflammatory drugs may increase the likelihood of gastrointestinal ulcers and bleeding through synergistic effects. The combination of meloxicam with other nonsteroidal anti-inflammatory drugs is not recommended.
Diuretics:
Treatment with nonsteroidal anti-inflammatory drugs has the potential to cause acute renal failure in dehydrated patients. Patients using this product and diuretics should be provided with sufficient water, and renal function should be monitored before treatment begins.
Oral anticoagulants:
Inhibiting platelet function and destroying the gastroduodenal mucosa increases the risk of bleeding. The combination of nonsteroidal anti-inflammatory drugs and oral anticoagulants is not recommended. If it cannot be avoided, the INR needs to be carefully monitored.
Thrombolytics and antiplatelet drugs:
Inhibiting platelet function and destroying the gastroduodenal mucosa increases the risk of bleeding.
ACE inhibitors and angiotensin II receptor antagonists:
Nonsteroidal anti-inflammatory drugs and angiotensin II receptor antagonists have a synergistic inhibitory effect on glomerular filtration, and symptoms can worsen when renal function is affected. For elderly patients and or dehydrated patients, the combination of the two may cause acute renal failure due to a direct impact on glomerular filtration. Renal function should be monitored at the beginning of treatment and patients should be regularly hydrated. In addition, the combined use will reduce the antihypertensive effect of ACE inhibitors and angiotensin II receptor citrin inhibitors, leading to a partial loss of efficacy (due to the vasodilation effect of prostaglandins).
Other antihypertensive drugs (such as beta receptor blockers):
Beta-blockers have reduced antihypertensive effects (due to the vasodilation effect of prostaglandins).
Cyclosporine:
Non-steroidal anti-inflammatory drugs increase the nephrotoxicity of cyclosporine through renin-prostaglandin-mediated effects. Renal function should be measured during combined use. In elderly patients, renal function needs to be carefully monitored.
Intrauterine contraception:
Nonsteroidal anti-inflammatory drugs have been reported to reduce the effectiveness of intrauterine contraceptive devices.
There have been reports of non-steroidal anti-inflammatory drugs reducing the efficacy of intrauterine contraceptive devices, but further confirmation is needed.
Pharmacokinetic Interactions (Effects of Meloxicam on Pharmacokinetics of Other Drugs)
lithium:
Non-steroidal anti-inflammatory drugs are reported to increase lithium plasma concentrations (by inhibiting the excretion of lithium from the kidneys) and may reach toxic concentrations. Therefore, nonsteroidal anti-inflammatory drugs are not recommended for use with lithium.
If you need to use it, it is recommended to use it. Monitor plasma lithium levels while modulating and discontinuing meloxicam.
Methotrexate:
Non-steroidal anti-inflammatory drugs reduce the excretion of methotrexate from the renal tubules and thereby increase the plasma concentration of methotrexate. Therefore, for patients receiving higher doses of methotrexate (greater than 15 mg / week), non-steroidal anti-inflammatory drugs are not recommended. For patients receiving lower doses of methotrexate, the possibility of interaction between nonsteroidal anti-inflammatory drugs and methotrexate should also be considered, especially for patients with renal insufficiency. If combined, monitor blood counts and renal function. Special care should be taken within 3 days of co-administration of nonsteroidal anti-inflammatory drugs and methotrexate. Plasma methotrexate concentrations may increase and cause increased toxicity.
Although the pharmacokinetics of methotrexate (15 mg / week) was not proportionally affected by the combination of meloxicam, it should be considered that the hematological toxicity of methotrexate may be amplified by the combination of nonsteroidal anti-inflammatory drugs (see above).
Pharmacokinetic Interactions (Effects of Other Drugs on Meloxicam Pharmacokinetics)
Cholestyramine:
By affecting the enterohepatic circulation, cholestyramine accelerates the elimination of meloxicam, the elimination of meloxicam is accelerated by 50%, and the half-life is reduced to 13 ± 3 hours. This interaction is clinically significant. No pharmacokinetic drug interactions were observed clinically when using antacids, cimetidine and digoxin.

Meloxicam tablets overdose

The symptoms of acute overdose of nonsteroidal anti-inflammatory drugs are mainly drowsiness, drowsiness, nausea, vomiting, and epigastric pain. Supportive therapy is usually available to recover. Gastrointestinal bleeding may occur. Severe toxicity may cause hypertension, acute renal failure, liver dysfunction, respiratory depression, coma, convulsions, collapse of the cardiovascular system and cardiac arrest. Allergy-like reactions have been reported with nonsteroidal anti-inflammatory drugs, which may occur in excess.
Patients should be treated symptomatically and supportively after nonsteroidal anti-inflammatory overdose.
Clinical trials have shown that 4 g of cholestyramine taken orally three times a day can accelerate the elimination of meloxicam.

Meloxicam tablets pharmacology and toxicology

Pharmacodynamic properties <br /> Imeloxicam is a non-steroidal anti-inflammatory drug in the Xi Kang family, which has anti-inflammatory, analgesic and antipyretic properties.
Meloxicam has anti-inflammatory activity against all standard inflammation models. As with other nonsteroidal anti-inflammatory drugs, the exact mechanism of action is unknown. But all nonsteroidal anti-inflammatory drugs have at least one common mechanism of action (including meloxicam): inhibition of the prostaglandin biosynthesis, a known inflammatory mediator.
Preclinical safety (toxicology) data < br Preclinical studies have shown that meloxicam has the same toxicological properties as other nonsteroidal anti-inflammatory drugs: gastrointestinal ulcers and erosions, two animal species in long-term toxicity studies Renal nipple necrosis occurs at high doses.
The adversely affected doses occurred when administered at a mg / kg dose (human body weight of 75 kg) 5 to 10 times the clinical dose (7.5-15 mg). As with all prostaglandin synthesis inhibitors, embryonic toxicity has been reported in late pregnancy. Neither in vivo nor in vitro tests showed any mutagenicity. Rats and mice were not found to be carcinogenic at higher clinical doses.

Pharmacokinetics of Meloxicam

Absorption < br The meloxicam is well absorbed through the gastrointestinal tract, and the absolute bioavailability after oral administration (capsules) is 89%. Tablets, oral suspensions and capsules are bioequivalent.
With a single dose of meloxicam, the highest plasma concentration of oral suspension appears within 2 hours, and oral solid preparations appear within 5-6 hours (capsules and tablets). With multiple doses, a stable state can be reached in three to five days. The once-daily dose makes the plasma concentration of the drug fluctuate within a relatively small peak-valley range. The fluctuation range of the 7.5 mg dose is 0.4-1.0 g / ml, and the plasma concentration range of the 15 mg dose is 0.8-2.0 g / ml (respectively stable Cmin and Cmax). The highest plasma concentration of meloxicam when the pair is stable, takes 5-6 hours for tablets, capsules, and oral suspension, respectively. The drug concentration in patients treated continuously for more than one year is similar to that in patients who have entered a stable state for the first time. Taking medication while eating has no effect on absorption.
Distribution < br Almeloxicam almost completely binds to plasma proteins, mainly albumin (99%). Meloxicam penetrates into the synovial fluid at a concentration close to half that in plasma.
The distribution volume is small. The average is 11 liters. Individual differences can reach 30-40%.
Biotransformation < br Romemeloxicam is completely biotransformed in the liver. Four metabolites were obtained in urine, all without pharmacodynamic activity. The main metabolite is 5'-carboxymeloxicam (60% of the dose) is formed by the oxidation of the intermediate product 5'-hydroxymethylmeloxicam, which is also excreted to a lesser extent (9% of the dose) . In vitro experiments show that CYP 2C9 plays an important role in the metabolic pathway, while CYP 3A4 isoenzyme contributes less. The patient's peroxidase activity may be related to the formation of two other metabolites, which accounted for 16% and 4% of the dose taken, respectively.
Elimination < br Almeloxicam is almost completely excreted as a metabolite, with equal amounts excreted via urine or feces. Less than 5% of the daily dose of the original drug is excreted from the feces, and only traces of unaltered original product are excreted from the urine.
The average half-life of meloxicam elimination from the body is 20 hours. The average plasma clearance was 8 ml / min.
Linear / Nonlinear < br The pharmacokinetics of meloxicam administered 7.5 mg and 15 mg were administered orally or intramuscularly.
Special populations < br Liver / renal insufficiency:
Hepatic insufficiency or mild or moderate renal insufficiency had no significant effect on the pharmacokinetics of meloxicam. For patients with advanced renal failure, the increase in distribution volume will lead to an increase in free meloxicam concentration, so it should not exceed the daily 7.5mg dose (see [Dosage and Administration]).
Elderly patients:
Compared with young people, the average steady-state plasma clearance of the elderly is slightly reduced.

Meloxicam tablets storage

Store in a light-proof and sealed environment below 30 ° C!
Keep out of reach of children!

Meloxicam tablet packaging

Packed in aluminum-plastic board, 7 pieces / box, 10 pieces / box.

Expiration Date of Meloxicam

60 months

Meloxicam Tablets

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