Meloflex Rompharm, 10 mg/ml 1.5 ml 3 pcs.

Pharmgroup: NSAIDs.

Pharmaceutical effect: Meloflex Rompharm is an NSAID, refers to enolic acid derivatives and has anti-inflammatory, analgesic and antipyretic effects.

The pronounced anti-inflammatory effect of meloxicam has been established in all standard models of inflammation. The mechanism of action of meloxicam is its ability to inhibit the synthesis of prostaglandins – known mediators of inflammation.

In vivo meloxicam inhibits the synthesis of prostaglandins at the site of inflammation to a greater extent than in the gastric mucosa or kidneys. These differences are due to more selective inhibition of cyclooxygenase-2 (COX-2) compared to cyclooxygenase-1 (COX-1).

The inhibition of COX-2 is thought to provide the therapeutic effect of NSAIDs, whereas inhibition of the ever-present COX-1 isoenzyme may cause gastric and renal side effects.

The selectivity of meloxicam against COX-2 has been confirmed in various test systems, both in vitro and ex vivo. The selective ability of meloxicam to inhibit COX-2 was shown when human whole blood was used as a test system in vitro.

Ex vivo, meloxicam (at doses of 7.5 mg and 15 mg) was found to be more active in inhibiting COX-2, having a greater inhibitory effect on lipopolysaccharide-stimulated prostaglandin E2 production (COX-2-controlled response) than on thromboxane production involved in blood clotting (COX-1-controlled response). These effects were dose-dependent.

Ex vivo, meloxicam at the recommended doses was shown to have no effect on platelet aggregation and bleeding time, unlike indomethacin, diclofenac, ibuprofen and naproxen, which significantly inhibited platelet aggregation and increased bleeding time.

Pharmacokinetics:

Absorption and distribution

Binding with plasma proteins is 99%. Passes through histohematic barriers, penetrates the synovial fluid. Concentration in synovial fluid is 50% of the concentration in plasma.

Metabolism and excretion

Metabolized in the liver to inactive metabolites.

Extracted through the intestine and the kidneys (approximately equal parts), unchanged – 5% of the daily dose (through the intestine). T1/2 – 20 h. Plasma clearance – on average 8 ml/min (decreases in old age).

Indications

Osteoarthritis;

Rheumatoid arthritis;

Ankylosing spondylitis (Bechterew’s disease).

Purposed for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Active ingredient

Composition

1 ml:

meloxicam 10 mg

Excipients:

meglumine – 6.25 mg,

glycafurfural – 100 mg,

poloxamer 188 – 50 mg,

glycine – 5 mg,

sodium chloride – 3.5 mg,

sodium hydroxide solution 1M – pH 8.6-9,

d/i water – up to 1 ml.

How to take, the dosage

The drug is administered deeply in m/m. V/v is contraindicated.

Introduction of Meloflex Romfarm is indicated only during the first days of treatment. Later the treatment is continued using oral forms (tablets).

Osteoarthritis in the acute phase – 7.5 mg/day; if the condition does not improve the dose can be increased up to 15 mg/day.
Rheumatoid arthritis, ankylosing spondylitis – 15 mg/day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg/day. The daily dose of meloxicam 15 mg should not be exceeded.

In elderly patients, the recommended dose for long-term therapy of rheumatoid arthritis or ankylosing spondylitis is 7.5 mg/day. In elderly patients with an increased risk of side effects, therapy should be started with 7.5 mg/day.

In patients on dialysis with severe renal impairment, the daily dose of meloxicam 7.5 mg should not be exceeded. In patients with mild to moderately severe renal impairment (creatinine clearance greater than 25 ml/min) there is no need to reduce the dose.

In patients with mild to moderately severe hepatic impairment, there is no need to reduce the dose of Meloflex Rompharm.

Interaction

Pharmacodynamic interaction:

The simultaneous use of several NSAIDs (including salicylates) may increase the risk of gastrointestinal erosive ulcers due to synergistic effects, therefore it is not recommended to use meloxicam with other NSAIDs.

When using meloxicam with diuretics, the patient should drink sufficient fluids, and regular medical monitoring of renal function before and during treatment is required.

Combined use with indirect anticoagulants increases the risk of bleeding due to inhibition of platelet function and damage to the gastrointestinal mucosa. Therefore, combined use with NSAIDs and indirect anticoagulants is not recommended.

When combined use of thrombolytics and antithrombotic drugs with meloxicam an increased risk of bleeding is possible (periodic monitoring of blood clotting is necessary).

Simultaneous use with ACE inhibitors and other hypotensive drugs in elderly patients with symptoms of dehydration may provoke acute renal failure. In addition, combined use with meloxicam may reduce their hypotensive effect.

Meloxicam increases the nephrotoxic effect of cyclosporine.

Meloxicam may decrease the effectiveness of contraceptives.

Pharmacokinetic interaction:

NSAIDs may increase serum lithium concentrations to toxic levels (decreased renal excretion of lithium). Therefore, concomitant use of meloxicam with lithium preparations is not recommended.

In case of necessity of their combined use the content of lithium in the blood serum should be carefully monitored before, during and after the end of therapy with meloxicam and lithium preparations.
With concomitant use with methotrexate the negative effect on the hematopoietic system increases (risk of anemia and leukopenia).

Periodic hemogram monitoring is necessary.

Colestyramine accelerates excretion of meloxicam, increasing clearance of meloxicam by 50%, reduces its T1/2 by 13±3 h. This interaction has clinical relevance.

In concomitant administration with antacids, cimetidine and digoxin, no significant clinical interaction has been noted.

NSAIDs reduce the effectiveness of intrauterine contraceptive devices.

When co-administering meloxicam and drugs that have a known ability to inhibit CYP2C9 and/or CYP3A4 (or are metabolized with the participation of these enzymes), the possibility of pharmacokinetic interaction must be taken into account.

The possibility of interaction of meloxicam with oral hypoglycemic agents cannot be excluded.

Concomitant use of meloxicam with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

Special Instructions

Caution should be exercised when treating patients with a history of gastrointestinal diseases. Patients with gastrointestinal symptoms should be monitored regularly. In case of gastrointestinal ulceration or gastrointestinal bleeding Meloflex Romfarm should be discontinued.

As with other NSAIDs, gastrointestinal bleeding, ulcers, and perforations potentially life-threatening to the patient may occur at any time during treatment, either with or without a history of alarming symptoms or serious gastrointestinal complications. The consequences of these complications are generally more serious in the elderly.

Particular attention should be paid to patients who report developing skin and mucosal adverse events. In such cases discontinuation of Meloflex Rompharm should be considered.

. In patients with decreased RBC and glomerular filtration (dehydration, chronic heart failure, liver cirrhosis, nephrotic syndrome, clinically evident renal diseases, use of diuretics, dehydration after major surgery) there may be clinically evident chronic renal failure which is completely reversible after discontinuation of the drug (daily urine output and renal function should be monitored in such patients at the beginning of therapy).

In case of persistent and significant elevation of transaminases and changes in other liver function parameters, the drug should be discontinued and control tests should be performed.

In patients with increased risk of side effects, treatment should be started at a dose of 7.5 mg. In end-stage chronic renal failure patients on dialysis, the dose should not exceed 7.5 mg/day.

Influence on driving and operating machinery

There are no data on the negative effect of the drug on the ability to drive vehicles or operate machinery. In case of CNS disorders (decreased visual acuity, increased fatigue, dizziness or other disorders) these activities are contraindicated.

Contraindications

Side effects

Prevalence of side effects: frequently (more than 1%); infrequently (0.1-1%); rarely (0.01-0.1%); very rarely (less than 0.01%).

Digestive system disorders: often – dyspepsia, including. nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequent – transient increase of liver transaminases activity, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, GI bleeding (including hidden), stomatitis; rarely – GI perforation, colitis, hepatitis, gastritis.

Hematopoietic organs: frequently – anemia; infrequently – changes in the blood count, including leukopenia and thromocytopenia.

The skin: often – itching, skin rash, infrequent – urticaria, rarely – photosensitization, bullous rash, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

Respiratory system disorders: infrequent – occurrence of bronchial asthma attacks in patients with allergy to acetylsalicylic acid or other NSAIDs.

CNS: frequently – dizziness, headache; infrequently – vertigo, tinnitus, somnolence; rarely – confusion, disorientation, emotional lability.

Cardiovascular system: often – peripheral edema; infrequent – increase of blood pressure, palpitations, flushing of blood to the face.

Urinary system: infrequent – hypercreatininemia and/or increased serum urea concentration; rare – acute renal failure; association with meloxicam administration is not determined – interstitial nephritis, albuminuria, hematuria.

Sensory organs: rare – conjunctivitis, visual disturbances, including blurred vision.
Allergic reactions: rare – angioedema, anaphylactoid/anaphylactic reactions.

Overdose

Worsening of dose-dependent side effects.

Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, acute liver failure, respiratory arrest, asystole.

Treatment: symptomatic therapy. Forced diuresis, urine alkalinization, hemodialysis are ineffective due to the high degree of binding of meloxicam with plasma proteins. There is no specific antidote.

Pregnancy use

Suppression of prostaglandin synthesis may have undesirable effects on pregnancy and fetal development. Thus, Meloflex Romfarm is contraindicated during pregnancy.

The drug penetrates into the breast milk, therefore Meloflex Romfarm is contraindicated during lactation. It is necessary to stop breastfeeding while taking the drug.

Similarities