Indications
Symptomatic therapy:
- osteoarthritis;
- rheumatoid arthritis;
- ankylosing spondylitis (ankylosing spondylitis).
$9.00
Active ingredient: | |
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Dosage form: |
Symptomatic therapy:
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
To reduce the risk of gastrointestinal adverse events, the minimum effective dose should be used in the shortest possible course.
Active substance:
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.
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.
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.
Symptomatic therapy:
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
To reduce the risk of gastrointestinal adverse events, the minimum effective dose should be used in the shortest possible course.
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.
The drug Movasin is taken orally with meals in a daily dose of 7.5-15 mg. Recommended dosage regimen:
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.
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.
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.
Tablets
Store in a dry place, protected from light, at a temperature not exceeding 25 °C
2 years
Meloxicam
By prescription
Tablets
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