Melox (Tablets) Instructions for Use

Marketing Authorization Holder

Medochemie, Ltd. (Cyprus)

Contact Information

MEDOCHEMIE, Ltd. (Cyprus)

ATC Code

M01AC06 (Meloxicam)

Active Substance

Meloxicam (Rec.INN registered by WHO)

Dosage Forms

	Melox	Tablets 7.5 mg: 10 or 20 pcs.
		Tablets 15 mg: 10 or 20 pcs.

Dosage Form, Packaging, and Composition

Tablets are light yellow in color, round, flat, with a score line on one side; marbling, inclusions, and some surface roughness are acceptable.

Excipients: sodium citrate, lactose, microcrystalline cellulose, colloidal anhydrous silica, povidone, crospovidone, magnesium stearate.

10 pcs. – blister packs (2) – cardboard packs.

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

NSAID

Pharmacological Action

NSAID. Selective COX-2 inhibitor. Belongs to the oxicam class, an enolic acid derivative. It has anti-inflammatory, analgesic, and antipyretic effects.

The mechanism of action is due to the drug’s ability to inhibit the biosynthesis of prostaglandins, which are mediators of inflammation.

Pharmacokinetics

Absorption

After oral administration, Meloxicam is well absorbed from the gastrointestinal tract. After a single dose of 7.5 mg, C_max is reached in 4-6 hours and is about 1000 µg/l.

Bioavailability is about 90%.

Distribution

C_ss is reached after 3-5 days of administration. Plasma protein binding (mainly to albumin) is 99%.

The concentration of meloxicam in the synovial fluid is 40-50% of the plasma concentration.

Metabolism

Meloxicam undergoes biotransformation in the liver, mainly through oxidation under the influence of cytochrome P₄₅₀, forming a 5-carboxy derivative (60% of the administered dose) and a 5-hydroxymethyl derivative. Oxidation of the benzothiazole ring leads to the appearance of an oxamic acid metabolite.

Excretion

Plasma clearance is 8 ml/min.

About 50% is excreted in the urine, mainly as inactive metabolites and about 0.2% unchanged; the remainder is excreted in the feces, with about 1.6% unchanged.

T_1/2 is 15-20 hours.

Indications

Symptomatic treatment of the following diseases

• Rheumatoid arthritis;
• Osteoarthritis;
• Ankylosing spondylitis.

ICD codes

Dosage Regimen

For rheumatoid arthritis, the drug is prescribed at a dose of 15 mg/day. If the therapeutic effect is sufficient, the dose can be reduced to 7.5 mg/day.

For osteoarthritis, the recommended dose is 7.5 mg/day. If necessary, the dose can be increased to 15 mg/day.

For ankylosing spondylitis, Melox is prescribed at a dose of 15 mg/day.

In patients with an increased risk of adverse effects, treatment should be started at a dose of 7.5 mg/day.

The maximum daily dose is 15 mg.

In patients with severe renal failure on hemodialysis, the daily dose should not exceed 7.5 mg. In patients with moderate renal impairment (with CC>25 ml/min), no dose reduction is required.

The tablets should be taken once a day with meals, washed down with water.

Adverse Reactions

From the digestive system: dyspepsia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea, belching, esophagitis, erosive and ulcerative lesions of the gastrointestinal tract, occult or macroscopically visible gastrointestinal bleeding, transient changes in liver function parameters (increased transaminase activity or plasma bilirubin level), stomatitis.

From the hematopoietic system: anemia, leukopenia, thrombocytopenia.

From the respiratory system: bronchospasm (in patients with “aspirin triad”).

From the cardiovascular system: peripheral edema, increased blood pressure, palpitations, flushing.

From the central nervous system: headache, dizziness, tinnitus, drowsiness.

From the urinary system: changes in renal function parameters (increased blood creatinine and/or urea levels).

From the organ of vision: conjunctivitis, visual acuity impairment.

Dermatological reactions: itching, skin rash, urticaria, photosensitivity.

Allergic reactions: angioedema, immediate-type hypersensitivity reactions, including anaphylactic and anaphylactoid reactions.

Contraindications

• Peptic ulcer of the stomach or duodenum in the acute phase;
• Increased bleeding (including gastrointestinal bleeding);
• Severe hepatic failure;
• Severe renal failure (without hemodialysis);
• Children and adolescents under 15 years of age;
• Pregnancy;
• Lactation (breastfeeding);
• Hypersensitivity to acetylsalicylic acid and other NSAIDs;
• Hypersensitivity to meloxicam or other components of the drug.

Use in Pregnancy and Lactation

Melox is contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

The drug is contraindicated in patients with severe hepatic failure.

If a marked increase in liver transaminase activity or changes in other parameters characterizing liver function occur during the use of Melox, or if these disorders are persistent, the use of Melox should be discontinued and control laboratory tests should be performed.

Use in Renal Impairment

In patients with severe renal failure on hemodialysis, the daily dose should not exceed 7.5 mg. In patients with moderate renal impairment (with CC>25 ml/min), no dose reduction is required.

The drug is contraindicated in patients with severe renal failure not on hemodialysis.

When prescribing Melox, it should be taken into account that the use of NSAIDs in patients with reduced renal blood flow and circulating blood volume may lead to deterioration of renal excretory function, especially in patients with dehydration, congestive heart failure, liver cirrhosis, nephrotic syndrome and severe kidney diseases, in patients receiving diuretics, as well as those who have undergone major surgery leading to hypovolemia. In these categories of patients, careful monitoring of diuresis and renal function must be carried out from the very beginning of treatment. In rare cases, NSAIDs can cause interstitial nephritis, renal medullary necrosis, or nephrotic syndrome. However, after discontinuation of NSAIDs, renal function usually returns to its previous level.

Pediatric Use

The drug is contraindicated in children and adolescents under 15 years of age.

Special Precautions

Melox should be used with caution in patients with a history of upper gastrointestinal tract diseases, as well as in patients receiving anticoagulant therapy. If a peptic ulcer or gastrointestinal bleeding occurs, the drug should be discontinued.

If severe dermatological reactions develop, discontinuation of the drug should also be considered.

When prescribing Melox, it should be taken into account that the use of NSAIDs in patients with reduced renal blood flow and circulating blood volume may lead to deterioration of renal excretory function, especially in patients with dehydration, congestive heart failure, liver cirrhosis, nephrotic syndrome and severe kidney diseases, in patients receiving diuretics, as well as those who have undergone major surgery leading to hypovolemia. In these categories of patients, careful monitoring of diuresis and renal function must be carried out from the very beginning of treatment. In rare cases, NSAIDs can cause interstitial nephritis, renal medullary necrosis, or nephrotic syndrome. However, after discontinuation of NSAIDs, renal function usually returns to its previous level.

If a marked increase in liver transaminase activity or changes in other parameters characterizing liver function occur during the use of Melox, or if these disorders are persistent, the use of Melox should be discontinued and control laboratory tests should be performed.

Melox should be prescribed with caution to elderly patients.

If it is necessary to use Melox while taking oral anticoagulants, ticlopidine, heparin, thrombolytics, blood coagulation parameters should be carefully monitored.

NSAIDs can cause sodium, potassium, and fluid retention and weaken the effect of saluretics, which in the presence of heart failure and arterial hypertension in a patient can lead to the progression of these diseases.

Patients taking Melox in combination with diuretics should receive sufficient fluids. Renal function should be examined before starting combination therapy.

When using Melox concomitantly with cyclosporine, renal function should be monitored.

Use in Pediatrics

The safety and efficacy of Melox in children have not been established.

Effect on the Ability to Drive Vehicles and Operate Machinery

Patients who experience visual acuity impairment, drowsiness, dizziness, headache, or tinnitus while using the drug should not engage in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Overdose

Symptoms: intensification of the described adverse effects is noted.

Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy. There are no specific antidotes. Cholestyramine can be used to accelerate the elimination of meloxicam.

Hemodialysis and forced diuresis are not effective.

Drug Interactions

When Melox is used concomitantly with other NSAIDs (including salicylates) in high doses, due to synergistic interaction, the risk of erosive and ulcerative lesions of the gastrointestinal tract increases.

When Melox is used concomitantly with indirect anticoagulants, ticlopidine, heparin, thrombolytics, the risk of bleeding increases.

When used concomitantly, Melox may enhance the myelodepressive effect of methotrexate (monitoring of blood cell count is necessary).

During the use of Melox, the effectiveness of intrauterine contraceptives may decrease.

In patients with dehydration, when using Melox concomitantly with diuretics, there is a potential risk of developing acute renal failure.

When Melox is used concomitantly with antihypertensive drugs (beta-blockers, ACE inhibitors, vasodilators), their effectiveness may decrease.

When Melox is used concomitantly with cyclosporine, the nephrotoxic effect of the latter may be enhanced.

When Melox is used concomitantly with cholestyramine, the elimination of meloxicam may be accelerated.

Storage Conditions

The drug should be stored in a dry place, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 2 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.