Meloflex Rompharm solution 10mg/ml 1.5ml ampoules, 3pcs

Composition

1 ml:

meloxicam 10 mg

Auxiliary substances:  

meglyumin – 6.25 mg,

glycofurfural-100 mg,

poloxamer

188-50 mg, glycine-5 mg,

sodium chloride-3.5 mg,

sodium hydroxide solution of 1 M-pH 8.6-9,

d/i water-up to 1 ml

Pharmacological action

: NSAIDs.

Pharmacology: Meloflex Rompharm is an NSAID, belongs to the derivatives of enolic acid and has anti-inflammatory, analgesic and antipyretic effects.

The pronounced anti-inflammatory effect of meloxicam was 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 prostaglandin synthesis at the site of inflammation to a greater extent than in the gastric mucosa or kidneys. These differences are associated with more selective inhibition of cyclooxygenase-2 (COX-2) compared to cyclooxygenase-1 (COX-1).

It is believed that COX-2 inhibition provides a therapeutic effect of NSAIDs, while inhibition of the constantly present COX-1 isoenzyme can cause side effects from the stomach and kidneys.

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

Ex vivo found that meloxicam (in doses of 7.5 mg and 15 mg) actively inhibited COX-2, providing a greater inhibitory effect on the production of prostaglandin E 2, stimulated by lipopolysaccharide (reaction-controlled COX-2) than on the production of thromboxane, which is involved in blood clotting (reaction-controlled COX-1). These effects were dose-dependent.

Ex vivo studies showed that meloxicam at the recommended doses did not affect platelet aggregation and bleeding time, in contrast to Indometacin, diclofenac, ibuprofen and naproxen, which significantly suppressed platelet aggregation and increased bleeding time.

Pharmacokinetics:

Suction and distribution

Binding to plasma proteins is 99%. Passes through histohematic barriers, penetrates synovial fluid. The synovial fluid concentration is 50% of the plasma concentration.

Metabolism and elimination

It is metabolized in the liver to inactive metabolites.

It is excreted through the intestines and kidneys (approximately in equal parts), unchanged – 5% of the daily dose (through the intestines). T1 / 2-20 hours Plasma clearance is on average 8 ml / min (decreases in the elderly).

Indications

• Osteoarthritis;

• rheumatoid arthritis;

• ankylosing spondylitis (Ankylosing spondylitis).

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

Use during pregnancy and lactation

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

The drug penetrates into breast milk, so Meloflex Rompharm is contraindicated during lactation. Breast-feeding should be stopped for the duration of taking the drug.

Contraindications

• The combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid and medicines pirazolona range;
• ulcer disease of stomach and duodenum (in the phase of exacerbation);
• severe hepatic insufficiency;
• chronic renal failure in patients not undergoing dialysis (KK less than 30 ml/min);
• active gastrointestinal bleeding;
• progressive kidney disease;
• severe hepatic impairment or active liver disease;
• status after conducting coronary artery bypass grafting;
• confirmed hyperkalemia;
• inflammatory bowel disease;
• children up to age 18 years;
• hypersensitivity (including to other NSAIDs).

With caution in

• the elderly;
• coronary artery disease;
• congestive heart failure;
• cerebrovascular disease;
• dyslipidemia/hyperlipidemia;
• diabetes mellitus;
• peripheral arterial disease;
• Smoking;
• chronic renal failure (CC 30-60 ml/min);
• ulcerative lesions of the gastrointestinal tract in history;
• the presence of Helicobacter pylori infection;
• long-term use of NSAIDs;
• alcohol;
• severe somatic disease;
• concomitant use of oral corticosteroids (e. g. prednisone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel)selective reuptake inhibitors of serotonin (including citalopram, fluoxetine, paroxetine, and sertraline).

Side effects

Frequency of side effects: common (more than 1%); infrequent (0.1-1%); rare (0.01-0.1%); very rarely (less than 0.01%).

From the digestive system: often-dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequently-transient increase in the activity of hepatic transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including hidden), stomatitis; rarely – perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.

From the hematopoietic organs: often-anemia; infrequently-changes in the blood formula, including leukopenia, tromocytopenia.

From the skin: often-pruritus, skin rash; infrequently-urticaria; rarely-photosensitization, bullous rashes, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the respiratory system: infrequently-the occurrence of asthma attacks in people who are allergic to acetylsalicylic acid or other NSAIDs.

From the central nervous system: often – dizziness, headache; infrequently-vertigo, tinnitus, drowsiness; rarely-confusion, disorientation, emotional lability.

From the cardiovascular system: often-peripheral edema; infrequently-increased blood pressure, palpitations, flushes of blood to the skin of the face.

From the urinary system: infrequently-hypercreatininemia and / or increased serum urea concentration; rarely – acute renal failure; association with meloxicam intake has not been established – interstitial nephritis, albuminuria, hematuria.

From the sensory organs: rarely-conjunctivitis, visual impairment, including blurred vision. Allergic reactions: rarely-angioedema, anaphylactoid / anaphylactic reactions.

Interaction

Pharmacodynamic interaction:

Concomitant use of several NSAIDs (including salicylates) may increase the risk of erosive and ulcerative lesions of the gastrointestinal tract due to the synergistic effect, so the use of meloxicam with other NSAIDs is not recommended.

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

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

With the combined use of thrombolytic and antithrombotic drugs with meloxicam, an increased risk of bleeding may occur (periodic monitoring of blood clotting parameters is necessary).

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

Meloxicam enhances the nephrotoxic effect of cyclosporine.

Meloxicam may reduce the effectiveness of contraceptives.

Pharmacokinetic interaction:

NSAIDs can increase the concentration of lithium in the blood serum to a toxic level (a decrease in the excretion of lithium by the kidneys). Therefore, the simultaneous use of meloxicam with lithium preparations is not recommended.

If their combined use is necessary, the lithium content in the blood serum should be carefully monitored before, during and after the course of therapy with meloxicam and lithium preparations. When used concomitantly with methotrexate, the negative effect on the hematopoietic system increases (the risk of anemia and leukopenia).

Periodic monitoring of the hemogram is required.

Colestyramine accelerates the elimination of meloxicam, increasing the clearance of meloxicam by 50%, reducing its T1 / 2 by 13±3 hours. This interaction is of clinical significance.

No significant clinical interactions have been reported with antacids, cimetidine, and digoxin concomitantly.

NSAIDs reduce the effectiveness of contraceptive intrauterine devices.

When meloxicam is co-administered with 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 should 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.

How to take, course of use and dosage

The drug is administered deep in/m. Intravenous use is contraindicated.

Intravenous use of Meloflex Rompharm is indicated only during the first days of treatment. In the future, treatment is continued with the use of oral forms (tablets).

Acute osteoarthritis – 7.5 mg / day, if the condition does not improve, you can increase the dose 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. Do not exceed the daily dose of meloxicam 15 mg.

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

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

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

Overdose

Increased 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, and hemodialysis are ineffective due to the high degree of meloxicam binding to plasma proteins. There is no specific antidote.

Special instructions

Caution should be exercised when treating patients with a history of gastrointestinal diseases. Patients with gastrointestinal symptoms should be monitored regularly. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, Meloflex Rompharm should be discontinued.

As with other NSAIDs, gastrointestinal bleeding, ulcers, and perforations that are potentially life-threatening may occur at any time during treatment, either in the presence of alarming symptoms or in the absence of a history of serious gastrointestinal complications. The consequences of these complications are generally more serious in the elderly.

Special attention should be paid to patients who report the development of adverse events from the skin and mucous membranes. In such cases, discontinuation of Meloflex Rompharm should be considered.

Patients with reduced BCC and reduced glomerular filtration rate (dehydration, chronic heart failure, cirrhosis of the liver, nephrotic syndrome, clinically expressed kidney diseases, diuretics, dehydration after major surgical operations) may experience clinically expressed chronic renal failure, which is completely reversible after discontinuation of the drug (in such patients, daily diuresis and renal function should be monitored at the beginning of treatment).

If there is a persistent and significant increase in transaminases and changes in other indicators of liver function, the drug should be discontinued and control tests should be performed.

In patients with an increased risk of side effects, treatment begins with a dose of 7.5 mg. In end-stage chronic renal failure in patients undergoing dialysis, the dose should not exceed 7.5 mg / day.

Influence on the ability to drive motor vehicles and manage mechanisms

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

Form of production

Solution for intramuscular use.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

4 years

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

For adults as directed by your doctor

Indications

Sciatica, Osteoarthritis and Arthritis, Sciatica, Rheumatoid Arthritis, Osteoarthritis, Osteochondrosis, Lumbago, Periarthritis