Movasin, pills 7.5mg, 20pcs

Composition

Active ingredient:

meloxicam (in terms of 100% substance) 7.5 mg;

Auxiliary substances:

povidone-12.6 thousand(polyvinylpyrrolidone low molecular weight medical 12600± 2700),

lactose monohydrate (milk sugar),

crospovidone (collidone CL, collidone CL-M),

potato starch,

talc,

magnesium stearate,

microcrystalline cellulose.

Pharmacological action

Meloxicam – NSAIDs. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in prostaglandin biosynthesis in the inflammatory region.

When prescribed in high doses, long-term use and individual characteristics of the body, selectivity for COX-2 decreases. Inhibits prostaglandin synthesis in the area of inflammation to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2. Less often causes erosive and ulcerative diseases of the gastrointestinal tract. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandins that protect the gastrointestinal mucosa and take part in the regulation of blood flow in the kidneys.

Pharmacokinetics

Suction

After oral use, meloxicam is well absorbed from the gastrointestinal tract, with an absolute bioavailability of 89%. Simultaneous intake with food does not change the absorption. The concentration of meloxicam when taking the drug orally at doses of 7.5 and 15 mg is proportional to the dose.

After intravenous use, the relative bioavailability is almost 100%. After intravenous use of the drug at a dose of 5 mg, the Cmax is 1.62 mcg / ml and is reached within approximately 60 minutes.

Meloxicam demonstrates linear pharmacokinetics at doses of 7.5-15 mg when administered intravenously.

Css distribution is achieved within 3-5 days of regular admission. With prolonged use of the drug (more than 1 year), the concentrations are similar to those observed after the first achievement of a stable state of pharmacokinetics. Binding to plasma proteins (especially albumin) is more than 99%.

The range of differences between the maximum and basal concentrations of the drug after taking it 1 time/day is relatively small and amounts to 0.4-1 mcg / ml when using a dose of 7.5 mg, and 0.8-2 mcg/ml when using a dose of 15 mg (Cmin and Cmax values are shown, respectively).

Meloxicam penetrates through histohematic barriers, the concentration in synovial fluid reaches 50% of the maximum concentration of the drug in plasma.

The Vd is low and is 11 liters. Interindividual differences are 30-40%.

Metabolism

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

Deduction

It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines, and only trace amounts of the drug are detected unchanged in the urine. T1 / 2 of meloxicam after oral use is 15-20 hours, with intramuscular use-20 hours. Plasma clearance averages 8 ml / min

. Pharmacokinetics in special clinical cases

In the elderly, the clearance of the drug decreases.

Moderate hepatic or renal insufficiency does not significantly affect the pharmacokinetics of meloxicam.

Indications

Symptomatic therapy:

• osteoarthritis;
• rheumatoid arthritis;
• ankylosing spondylitis (ankylosing spondylitis).

Contraindications

• status after conducting coronary artery bypass grafting;
• decompensated heart failure;
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance of acetylsalicylic acid and other NSAIDs (including in the anamnesis);
• erosive and ulcerative changes in the mucous membrane of the stomach or duodenal ulcers, active gastrointestinal bleeding;
• inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
• cerebrovascular bleeding or other bleeding;
• severe hepatic impairment or active liver disease;
• chronic renal failure patients not undergoing dialysis (KK less than 30 ml/min), progressive kidney disease (including confirmed hyperkalemia);
• children up to age 12 years (for tablets);
• children up to age 18 years (for a solution for the/m introduction);
• pregnancy;
• lactation (breastfeeding);
• hypersensitivity to meloxicam and other components of the drug.

The drug contains lactose in tablet form, so patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug.

Caution

• ischemic heart disease;
• cerebrovascular disease;
• compensated heart failure;
• dyslipidemia/hyperlipidemia;
• diabetes mellitus;
• peripheral arterial disease;
• Smoking;
• KK 30-60 ml/min;
• anamnestic information about the development of ulcerative lesions of the gastrointestinal tract;
• infection Helicobacter pylori;
• older age;
• long-term use of NSAIDs;
• frequent alcohol consumption;
• severe somatic disease;
• concomitant therapy with the following drugs: anticoagulants (e. g., warfarin); antiplatelet agents (e. g., acetylsalicylic acid, clopidogrel); oral corticosteroids (e. g., prednisone); selective serotonin reuptake inhibitors (e. g., citalopram, fluoxetine, paroxetine, sertraline).

To reduce the risk of gastrointestinal adverse events, the minimum effective dose should be used in the shortest possible course.

Side effects

From the digestive system:  more than 1% – dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1% – transient increase in the activity of” hepatic ” transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, gastrointestinal bleeding (including hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis.

From the side of hematopoietic organs:  more than 1% – anemia; 0.1-1% – changes in the blood formula, including leukopenia, thrombocytopenia.

From the side of the skin:  more than 1% – pruritus, skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitization, bullous rashes, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

Respiratory system disorders:  less than 0.1% – bronchospasm.

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

From the cardiovascular system (CVS):  more than 1% – peripheral edema; 0.1-1% – increased blood pressure( BP), palpitations, “flushes” of blood to the skin of the face.

From the urinary system:  0.1-1% – hypercreatininemia and / or increased serum urea; less than 0.1% – acute renal failure; no association with meloxicam has been established – interstitial nephritis, albuminuria, hematuria.

From the side of the senses:  less than 0.1% – conjunctivitis, visual impairment, including blurred vision.

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

Interaction

• with simultaneous use with other NSAIDs (or acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and bleeding in the gastrointestinal tract;
• while the use of Novasina with antihypertensive drugs may reduce their effectiveness;
• with the simultaneous use with lithium preparations may develop accumulation of lithium and increase its toxic effect (it is recommended to monitor the concentration of lithium in the blood);
• while the use of Novasina with methotrexate increases adverse effect on the hematopoietic system (the risk of anemia and leukopenia shows periodic monitoring of complete blood count);
• with simultaneous use with diuretics and cyclosporine increases the risk of renal failure;
• while the use of Novasina with intrauterine contraceptives may reduce the effectiveness of the latter;
• with the simultaneous use of anticoagulants (heparin, tiklopidin, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (requires periodic monitoring of indicators of blood coagulation);
• while the use of Novasina with kolestiraminom accelerated excretion of the drug from the body;
• concomitant use with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

How to take, course of use and dosage

The drug Movasin is taken orally with meals in a daily dose of 7.5-15 mg. Recommended dosage regimen:

• rheumatoid arthritis: 15 mg of Movasin per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.
• osteoarthritis: 7.5 mg of Movasin per day. If ineffective, the dose can be increased to 15 mg per day.
• ankylosing spondylitis: 15 mg of Movasin per day.

The maximum daily dose is 15 mg. In patients with an increased risk of side effects, as well as in patients with severe renal insufficiency who are on hemodialysis, the dose should not exceed 7.5 mg of Movasin per day.

Overdose

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

Treatment: there is no specific antidote; in case of overdose of the drug, gastric lavage, taking activated charcoal (within the next hour), and symptomatic therapy should be performed. Forced diuresis, urine alkalinization, and hemodialysis are ineffective due to the high binding of the drug to blood proteins.

Special instructions

• caution should be exercised when using Movasin in patients with a history of gastric and duodenal ulcers, as well as in patients undergoing anticoagulant therapy. These patients are at increased risk of erosive and ulcerative diseases of the gastrointestinal tract;
• use caution and monitor the indicators of renal function with use of the drug Mohsin from elderly patients, patients with chronic heart failure (CHF) with symptoms of circulatory failure in patients with cirrhosis, and in patients with hypovolemia as a result of surgical interventions;
• patients with slight or moderate decrease in renal function (QC more than 30 ml/min) does not require correction of dosing regimen;
• patients concurrently receiving diuretics and meloxicam, should take plenty of fluids;
• if in the course of treatment had an allergic reaction (itching, skin rash, urticaria, photosensitivity), you must consult a doctor to solve the issue of termination of drug Mohsin;
• meloxicam, like other NSAIDs, may mask the symptoms of infectious diseases;
• the use of meloxicam, like other drugs that block prostaglandin synthesis, may impair fertility and is not recommended for women who wish to conceive.

Driving vehicles, servicing machines and mechanismsapplication of the drug Movasin can cause undesirable effects in the form of headaches and dizziness, drowsiness, so during the period of taking the drug, you should stop driving vehicles and servicing machines and mechanisms that require concentration of attention.

Form of production

Tablets

Storage conditions

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

Shelf life

2 years

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

Tablets