Meloxicam DS, 10 mg/ml 1.5 ml 3 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drugs

ATC code: M01AC06

Pharmacodynamics:

Meloxicam is a non-steroidal anti-inflammatory drug with analgesic anti-inflammatory and antipyretic effect. Anti-inflammatory activity is associated with inhibition of enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the inflammation. To a lesser extent meloxicam acts on cyclooxygenase-1 (COX-1) involved in the synthesis of prostaglandin protecting the mucosa of the gastrointestinal tract and is involved in the regulation of blood flow in the kidneys.

Pharmacokinetics:

Relative bioavailability is nearly 100%. After an intravenous injection of 5 mg, the Cmax is 1.62 mcg/mL and is reached within approximately 60 minutes. Meloxicam binds well to plasma proteins, especially to albumin (99%). Penetrates into synovial fluid The concentration in synovial fluid is approximately 50% of the plasma concentration. Vd is low, averaging 11 L. Interindividual variation is 30-40%.

Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive derivatives. The main metabolite 5′-carboxymeloxicam (60% of the dose value) is formed by oxidation of the intermediate metabolite 5′-hydroxymethylmeloxicam which is also excreted but to a lesser extent (9% of the dose value). In vitro studies have shown that CYP2C9 isoenzyme plays an important role in this metabolic transformation, and CYP3A4 isoenzyme has additional importance. Peroxidase activity of which probably varies individually takes part in the formation of two other metabolites (which are 16% and 4% of the drug dose, respectively).

It is excreted equally in the feces and urine, mainly as metabolites. Less than 5% of daily dose is excreted unchanged in the feces, and only trace amounts of the drug are excreted in the urine. Mean T1/2 is 20 hours. Plasma clearance averages 8 ml/min.

Meloxicam exhibits linear pharmacokinetics at doses of 7.5-15 mg when administered by injection.

Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.

Indications

– Symptomatic treatment of osteoarthritis;

– Symptomatic treatment of rheumatoid arthritis;

– Symptomatic treatment of ankylosing spondylitis (Bechterew’s disease).

Active ingredient

Composition

1 ampoule contains:

The active ingredient:

meloxicam – 15 mg;

Additional ingredients: ethanol, poloxamer 188, sodium chloride, glycine, meglumine, sodium hydroxide, water for injection.

How to take, the dosage

Intramuscularly. Intramuscular administration of the drug is indicated only during the first 2-3 days. Subsequently, treatment is continued with oral forms (tablets).

The recommended dose is 7.5 mg or 15 mg once daily depending on the intensity of the pain and the severity of the inflammatory process.

The drug is administered deeply intramuscularly. Intravenous administration of the drug is prohibited!

In patients with an increased risk of adverse reactions, the daily dose should not exceed 7.5 mg.

In patients with end-stage renal failure on hemodialysis, the dose should not exceed 7.5 mg. In patients with mild to moderate renal impairment (CKD greater than 30 ml/min) the dose should not exceed 7.5 mg.

The dosage regimen of the drug for intramuscular injection in children and adolescents has not been defined; this dosage form can only be used in adult patients. The maximum recommended daily dose is 15 mg.

In case of combined use of different dosage forms of the drug, its maximum daily dose in suppositories tablets and solution for injection is 15 mg.

Interaction

– Concomitant use with other NSAIDs (as well as acetylsalicylic acid) increases the risk of erosive ulcerative lesions and gastrointestinal bleeding;

– Concomitant use with hypotensive drugs may reduce the effectiveness of the latter;

– Concomitant use with lithium preparations may cause cumulation of lithium and increase its toxic effect (it is recommended to control lithium concentration in blood);

– Concomitant use with methotrexate may increase side effects of the latter on the hematopoietic system (periodic monitoring of general blood count is recommended for risk of anemia and leukopenia);

Concomitant use with diuretics and with cyclosporine increases the risk of renal impairment.

Concomitant use with intrauterine contraceptives may decrease the effectiveness of the latter.

– Concomitant use with anticoagulants (heparin ticlopidine warfarin) antiaggregants (acetylsalicylic acid clopidogrel) as well as with fibrinolytic drugs (streptokinase fibrinolysin) increases the risk of bleeding (periodic monitoring of blood clotting is necessary);

– Simultaneous use with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

Special Instructions

– Caution should be exercised when using the drug in patients with a history of peptic ulcer or duodenal ulcer as well as in patients on anticoagulant therapy. These patients have an increased risk of gastrointestinal erosive ulcers.

– Caution should be exercised and renal function parameters should be monitored when using the drug in elderly patients with chronic heart failure with circulatory insufficiency symptoms in patients with cirrhosis and in patients with hypovolemia as a result of surgical interventions.

– In patients with renal insufficiency if creatinine clearance is greater than 30 ml/min does not require dosing adjustments.

– In patients on dialysis, the dosage of the drug should not exceed 75 mg/day.

– Patients taking diuretics and meloxicam at the same time should take sufficient fluids.

– If allergic reactions occurred during treatment (itching, skin rash, urticaria, photosensitization) it is necessary to consult a physician in order to decide whether to discontinue the drug.

– Meloxicam like other nonsteroidal anti-inflammatory drugs can mask the symptoms of infectious diseases.

– The use of meloxicam as well as other drugs that block the synthesis of prostaglandins can affect fertility so it is not recommended for women planning to become pregnant.

Contraindications

– Hypersensitivity to the active substance or excipients;

– contraindicated in the period after coronary artery bypass grafting;

– decompensated heart failure;

– the complete or incomplete combination of bronchial asthma with recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (includingч. history);

– erosive-ulcerative changes of the mucous membrane of the stomach and 12 duodenum – active gastrointestinal bleeding;

– exacerbation of inflammatory bowel disease (non-specific ulcerative colitis Crohn’s disease);

– Cerebrovascular or other bleeding;

– significant hepatic insufficiency or active liver disease;

– significant renal insufficiency in non-dialysis patients (creatinine clearance less than 30 ml/min) advanced renal disease including

– pregnancy, breastfeeding;

– children under 18 years of age.

Ischemic heart disease cerebrovascular disease chronic heart failure dislipidemia/hyperlipidemia diabetes mellitus peripheral artery disease smoking creatinine clearance of 30 to 60 ml/min. Anamnestic evidence of gastrointestinal ulceration presence of Helicobacter pylori infection elderly age long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) frequent use of alcohol severe somatic diseases concomitant therapy with the following drugs:

– Anticoagulants (such as warfarin);

– Antiaggregants (such as acetylsalicylic acid clopidogrel);

– oral glucocorticosteroids (e.g., prednisolone);

– Selective serotonin reuptake inhibitors (e.g., citalopram fluoxetine paroxetine sertraline);

To reduce the risk of GI adverse events, use the lowest effective dose with the shortest course possible.

Side effects

The digestive system: more than 1% – dyspepsia including nausea vomiting abdominal pain constipation flatulence diarrhea; 0.1-1% – transient increase of “liver” transaminases activity hyperbilirubinemia belching esophagitis gastroduodenal ulcer gastroduodenal bleeding (including latent) stomatitis; < 0.1% – perforation of GI colitis; hepatitis gastritis.

The hematopoietic system: more than 1% – anemia; 0.1-1% – changes of blood counts including leukopenia thrombocytopenia.

The skin: more than 1% – itching skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitization bullous rash erythema multiforme including Stevens-Johnson syndrome toxic epidermal necrolysis.

Respiratory system disorders: less than 0.1% – bronchospasm.

CNS disorders: more than 1% – dizziness headache; 0.1-1% – vertigo tinnitus drowsiness; less than 0.1% – confusion disorientation emotional lability.

Cardiovascular system: more than 1% – peripheral edema; 0.1-1% – increase in BP heart palpitations “rushes” of blood to the skin of the face.

Urinary system: 0.1-1% – hypercreatininemia and/or increased serum urea; less than 0.1% – acute renal failure; relationship with meloxicam administration is not determined – interstitial nephritis albuminuria hematuria.

Senses: less than 0.1% – conjunctivitis visual impairment including blurred vision.

Allergic reactions: less than 0.1% – angioedema anaphylactic/anaphylactoid reactions.

Local reactions: more than 1% – swelling at the injection site; less than 1% – painful sensations at the injection site.

Overdose

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

Treatment: no specific antidote; symptomatic therapy. Forced diuresis urine alkalinization hemodialysis – ineffective due to high binding of the drug to blood proteins.

Pregnancy use

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