Arthrozan, tablets 15 mg 20 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug

ATX code: M01AC06

Pharmacological properties

Pharmacodynamics

Artrosan

sup>® is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic effects.

It belongs to the class of oxycams and is a derivative of enolic acid.

The mechanism of action is related to inhibition of prostaglandin synthesis due to selective inhibition of enzymatic activity of cyclooxygenase of the second type (COX-2), which takes part in biosynthesis of prostaglandins in inflammatory areas. When prescribed in high doses, prolonged use and individual characteristics of the body, selectivity against COX-2 is reduced. To a lesser extent, it acts on cyclooxygenase type 1 (COX-1), which is involved in the synthesis of prostaglandins that protect the mucosa of the gastrointestinal tract and is involved in the regulation of blood flow in the kidneys. Due to the above selective inhibition of COX-2 activity, the drug less often causes erosive-ulcerative lesions of the gastrointestinal tract.

Pharmacokinetics

Highly absorbed from the gastrointestinal tract, the absolute bioavailability is 89%. Simultaneous intake of food does not change the absorption of the drug. When using the drug orally in doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Equilibrium concentrations are reached within 3-5 days of treatment. In long-term use of the drug (more than 1 year) concentrations are similar to those observed after the first achievement of steady state pharmacokinetics.

Binding to plasma proteins is 99%. At a dose of 7.5 mg, the minimum concentration (C_min) is 0.4 µg/mL, the maximum concentration (C_max) is 1.0 µg/mL; when using a 15 mg dose, C_min is 0.8 µg/mL, C_max is 2.0 µg/mL. It is almost completely metabolized in the liver to form four 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 CYP 2C9 isoenzyme plays an important role in this metabolic transformation, CYP3A4 isoenzyme has additional importance. Peroxidase plays an important role in the formation of the other two metabolites (which are, respectively, 16% and 4% of the drug dose), whose activity probably varies.

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

Plasma clearance is on average 8 ml/min. In elderly persons the drug clearance is decreased. The volume of distribution is low and averages 11 L. Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.

It is excreted in equal proportions in the feces and urine, 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. The half-life (T_1/2) of meloxicam is 15-20 hours.

Indications

Symptomatic therapy:

Active ingredient

Composition

On 1 tablet:

the active ingredient: meloxicam – 7.5 mg or 15.0 mg;

excipients:

for 7.5 mg dosage: potato starch – 64.5 mg, lactose monohydrate – 100.0 mg, povidone (polyvinylpyrrolidone, povidone K-25) – 3.2 mg, sodium citrate – 18.8 mg, magnesium stearate – 2.0 mg, colloidal silicon dioxide (aerosil) – 4.0 mg;

For dosing 15.0 mg: potato starch – 94.5 mg, lactose monohydrate – 150.0 mg, povidone (polyvinylpyrrolidone, povidon K-25) – 4.5 mg, sodium citrate – 27.0 mg, magnesium stearate – 3.0 mg, colloidal silica (aerosil) – 6.0 mg.

How to take, the dosage

At the mouth.

The drug is taken with meals in a daily dose of 7.5-15 mg.

Recommended dosing regimen:

Rheumatoid arthritis:

15 mg daily. If necessary, the dose may be reduced to 7.5 mg per day.

Osteoarthritis, Osteochondrosis and other inflammatory and degenerative diseases of the musculo-articular system accompanied by pain syndrome:

7.5 mg per day. If ineffective, the dose may be increased to 15 mg daily.

Ankylosing spondylitis:

15 mg daily.

The maximum daily dose should not exceed 15 mg.

In patients at increased risk of side effects, and in patients with significant renal impairment who are on hemodialysis, the dose should not exceed 7.5 mg daily.

Interaction

Special Instructions

Influence on ability to drive vehicles, mechanisms

.Due to the possibility of headache, dizziness and somnolence, during the treatment, patients should avoid driving vehicles and performing other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

Synopsis

Contraindications

Side effects

In terms of frequency of adverse effects within the system-organ classes, the following categories are used: very common (≥ 1/10); common (≥ 1/100, < 1/10); infrequent (≥ 1/1,000, < 1/100); rare (≥ 1/10,000, < 1/1,000); very rare (< 1/10,000); not established.

Blood and lymphatic system disorders:

not infrequently: anemia;

rarely: Changes in blood cell count, including changes in the leukocyte formula, leukopenia, thrombocytopenia.

From the immune system:

infrequent: Other immediate-type hypersensitivity reactions;

frequency unknown: anaphylactic shock, anaphylactoid/anaphylactic reactions.

Mental side:

often: mood changes;

frequency unknown: confusion, disorientation.

Nervous system side:

often: Headache;

infrequent: dizziness, drowsiness.

Visual side:

frequently: conjunctivitis, visual disturbances, including blurred vision.

Hearing organ and labyrinth disorders:

frequent: vertigo;

frequent: tinnitus.

Cardiac side:

frequently: palpitations.

vascular side:

infrequent: increase in blood pressure, “rushes” of blood to the face.

Respiratory system, chest and mediastinum:

rarely: bronchial asthma in patients allergic to acetylsalicylic acid or other NSAIDs.

Gastrointestinal tract:

often: abdominal pain, dyspepsia, diarrhea, nausea, vomiting;

frequently: latent or overt gastrointestinal bleeding, gastritis, stomatitis, constipation, abdominal bloating, belching;

rarely: gastroduodenal ulcers, colitis, esophagitis;

very rarely: gastrointestinal perforation.

From the liver and biliary tract:

infrequent: Transient changes in liver function parameters (e.g., increased transaminase or bilirubin activity);

very frequently: hepatitis.

Skin and subcutaneous tissue:

not infrequently: angioedema, pruritus, skin rash;

rarely: toxic epidermal necrolysis, Stevens-Johnson syndrome, urticaria;

very rarely: bullous dermatitis, erythema multiforme;

frequency unknown: photosensitization.

Kidney and urinary tract disorders:

infrequent: Changes in renal function parameters (increased serum creatinine and/or urea levels), urinary disorders, including acute urinary retention;

very frequently: acute renal failure.

Combined use with medications that depress bone marrow (e.g., methotrexate) may provoke cytopenia. Gastrointestinal bleeding, ulceration or perforation may be fatal.

As with other NSAIDs do not exclude the possibility of interstitial nephritis, glomerulonephritis, renal medullary necrosis, nephrotic syndrome.

Overdose

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

Treatment:no specific antidotes or antagonists. In case of overdose of the drug – gastric lavage, administration of 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.

Pregnancy use

Similarities