Movasin, tablets 7.5 mg 20 pcs

Meloxicam is an NSAID. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is related to inhibition of prostaglandin synthesis as a result of selective inhibition of enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in the biosynthesis of prostaglandins in the area of inflammation.

When administered in high doses, long-term use and individual characteristics of the body, selectivity against COX-2 decreases. Suppresses the synthesis of prostaglandins 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 are involved in the regulation of blood flow in the kidneys.

Pharmacokinetics

Intake

After oral administration of the drug meloxicam is well absorbed from the gastrointestinal tract, the absolute bioavailability is 89%. Concomitant use with food does not change absorption. Magnitude of meloxicam concentration when administered orally in doses of 7.5 and 15 mg is proportional to the dose.

The relative bioavailability is almost 100% after administration in m/m. After an oral dose of 5 mg, Cmax is 1.62 mcg/ml and is reached within approximately 60 minutes.

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

Distribution

Css are achieved within 3-5 days of regular administration. With long-term use of the drug (more than 1 year), concentrations are similar to those observed after first achieving steady state pharmacokinetics. Binding to plasma proteins (especially albumin) is more than 99%.

The range of differences between maximum and basal concentrations of the drug after its administration once daily is relatively small and amounts to 0.4-1 mcg/ml with 7.5 mg dose and 0.8-2 mcg/ml with 15 mg dose (Cmin and Cmax values are given, respectively).

Meloxicam penetrates the 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 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 through the intestine and kidneys, mainly as metabolites. Less than 5% of the daily dose is excreted unchanged in the intestine, the drug is detected only in trace amounts in the urine. T1/2 of meloxicam after oral administration is 15-20 hours, when administered by injection – 20 hours. Plasma clearance averages 8 ml/min.

Pharmacokinetics in special clinical cases

The drug clearance is decreased in elderly persons.

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

Indications

Symptomatic therapy:

Active ingredient

Composition

Active substance:

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

Supplementary substances:

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

lactose monohydrate (milk sugar),

crospovidone (collidone CL, collidone SL-M),

potato starch,

talc,

magnesium stearate,

microcrystalline cellulose.

How to take, the dosage

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

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

Interaction

Special Instructions

Contraindications

Side effects

Gastrointestinal 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, GI bleeding (including hidden gastrointestinal bleeding); less than 0.1

Hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis.

Hematopoietic organs: more than 1% – anemia; 0.1-1% – blood count changes, including leukopenia, thrombocytopenia.

Skin disorders: 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.

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

Cardiovascular system (CVS): more than 1 % – peripheral edema; 0.1-1 % – increase of blood pressure (BP), palpitation, “rushes” of blood to 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.

Sensory organs: less than 0.1% – conjunctivitis, visual impairment, including blurred vision.

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

Overdose

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

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

Similarities