Meloxicam-Solopharm Politvist 10 mg/ml 1.5 ml, 5 pcs.

Pharmacotherapeutic group:

Non-steroidal anti-inflammatory drug (NSAID)

ICD-10:

XIII.M05-M14.M05 Seropositive rheumatoid arthritis

XIII.M20-M25.M25.5 Joint pain

XIII.M15-M19.M15 Polyarthritis

XIII.M45-M49.M45 Ankylosing spondylitis

ATC:

M.01.A.C.06 Meloxicam

M.01.A.C Oxycams

Pharmacodynamics:

Meloxicam is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic effects. It belongs to the class of oxycams, derivatives of enolic acid. Anti-inflammatory effect is associated with inhibition of enzymatic activity of cyclooxygenase-2, which is involved in the biosynthesis of prostaglandins in the inflamed area. To a lesser extent, meloxicam acts on cyclooxygenase-1, which is involved in the synthesis of prostaglandin, protecting the mucous membrane of the gastrointestinal tract and is involved in the regulation of blood flow in the kidneys.

Pharmacokinetics:

Absorption

The relative bioavailability is approximately 100%. After intramuscular administration of the drug at a dose of 15 mg, the maximum plasma concentration of the drug (Cmax) is 1.62 mcg/mL and is reached within approximately 60 minutes.

Distribution

Meloxicam binds well to plasma proteins, especially to albumin (99%). It penetrates the synovial fluid, the concentration in the synovial fluid is about 50% of the plasma concentration. The volume of distribution is low, approximately 11 liters. Interindividual variation is 30-40%.

Metabolism

Meloxicam is almost completely metabolized in the liver to form four pharmacologically inactive metabolites. 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, CYP3A4 isoenzyme has additional importance. Peroxidase, the activity of which probably varies individually, is involved in the formation of the other two metabolites (constituting, respectively, 16% and 4% of the value of the drug dose).

Extracted equally in the feces and urine, mainly as metabolites. Less than 5% of daily dose is excreted unchanged in feces, in urine the drug is excreted unchanged only in trace amounts. The average half-life of meloxicam is 20 hours. Plasma clearance averages 8 ml/min.

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

There are reports that enterohepatic recirculation is characteristic of meloxicam when administered orally. When using oral dosage forms of meloxicam the average time to reach the maximum plasma concentration of the drug (TSmax) is 5-6 hours, and the violation of enterohepatic recirculation for any reason may increase the elimination of meloxicam and reduce its half-life to 13 hours or more (when taken orally).

Hepatic and/or renal insufficiency

Hepatic insufficiency and mild to moderate renal insufficiency have no significant effect on the pharmacokinetics of meloxicam. In terminal renal failure, increased volume of distribution may lead to higher concentrations of free meloxicam, so in these patients the daily dose should not exceed 7.5 mg.

Elderly patients

In elderly patients, average plasma clearance during equilibrium pharmacokinetics is slightly lower than in younger patients.

Indications

Active ingredient

Composition

1 ml of the drug contains:

Active substance:

Meloxicam – 10.0 mg

Supplementary substances:

Tetrahydrofurfuryl macrogol (glycofurole) – 100.0 mg

Poloxamer 188 – 50.0 mg

Meglumine – 6.25 mg

Elicin – 5.0 mg

Sodium chloride – 3.0 mg

10 M sodium hydroxide solution to pH 8.2-8.9

Water for injection to 1 ml.

Description:

Transparent yellow or greenish-yellow liquid.

How to take, the dosage

Interaction

Special Instructions

Contraindications

– Hypersensitivity to the active ingredient and excipients of the drug, to acetylsalicylic acid or other NSAIDs.

– Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs due to the existing possibility of cross-sensitivity (including a history).

– Erosive ulcerative lesions of the stomach and duodenum in the acute stage or recently suffered.

– Inflammatory bowel disease – Crohn’s disease or ulcerative colitis in the acute stage.

– Severe liver and heart failure.

– Severe renal failure (unless hemodialysis, creatinine clearance less than 30 ml/min), advanced renal disease, including confirmed hyperkalemia.

– Active liver disease.

– Active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of blood clotting disorders.

– Age under 18 years of age.

– Therapy of perioperative pain during coronary artery bypass grafting.

– Concomitant therapy with anticoagulants, since there is a risk of intramuscular hematomas.

– Pregnancy.

– Breastfeeding period.

– Gastrointestinal tract (GIT) diseases in the history (presence of Helicobacter pylori infection).

– Congestive heart failure.

– Renal insufficiency (creatinine clearance 30-60 ml/min).

– Coronary heart disease.

– Cerebrovascular disease.

– Dyslipidemia/hyperlipidemia.

– Diabetes mellitus.

– Concomitant therapy with the following drugs: anticoagulants, oral glucocorticosteroids, antiaggregants, selective serotonin reuptake inhibitors.

– Peripheral arterial disease.

– Older age.

– Prolonged use of NSAIDs.

– Smoking.

– Frequent use of alcohol.

Side effects

Overdose

Similarities