Myrlox, 15 mg tablets, 20 pcs.

Pharmgroup:

NSAIDs.

Pharmaceutical action:

Mirlox is a non-steroidal anti-inflammatory drug (NSAID). It has anti-inflammatory, analgesic and antipyretic effects.

The anti-inflammatory effect is associated with inhibition of COX-2 enzymatic activity, which is involved in the biosynthesis of prostaglandins in the inflamed area. To a lesser extent, it acts on COX-1, which is involved in the synthesis of prostaglandin, which protects the mucous membrane of the digestive tract and is involved in the regulation of blood flow in the kidneys.

Pharmacokinetics:

Intake
After oral administration is well absorbed from the gastrointestinal tract. The absolute bioavailability of meloxicam is 89%. Simultaneous intake of food does not change absorption.

When Mirlox is taken orally in doses of 7.5 mg and 15 mg the plasma concentration of meloxicam is proportional to the dose.

The range of difference between Cmax and Cmin in plasma after a single dose is relatively small and with a dose of 7.5 mg is 0.4-1 mcg/ml, and with a dose of 15 mg – 0.8-2 mcg/ml (the values of both Cmin and Cmax are given, respectively).

Distribution
Css is reached within 3-5 days. With long-term use of the drug (more than 1 year), concentrations are similar to those observed after first reaching the equilibrium state.

The binding to plasma proteins is more than 99%. Vd is small and averages 11 liters.

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

Metabolism
Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive metabolites. The main metabolite, 5′-carboxymeloxicam (60% of the dose taken), is formed by oxidation of the intermediate metabolite, 5′-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose taken). 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 (which are 16% and 4% of the dose of the drug, respectively).

Elimation
T1/2 of meloxicam is 15-20 h. It is excreted in the feces and urine, mainly as metabolites. Less than 5% of the daily dose is excreted unchanged in the feces, the drug is excreted unchanged in the urine only in trace amounts. Plasma clearance is on average 8 ml/min.

Pharmacokinetics in special clinical cases

The clearance of Mirlox is decreased in elderly persons.

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

Indications

– symptomatic treatment of osteoarthritis;
– symptomatic treatment of rheumatoid arthritis;
– symptomatic treatment of ankylosing spondylitis (Behterev disease).

Active ingredient

Composition

1 tablet contains:

Meloxicam 15 mg

Associates:

Lactose,

Corn starch,

sodium citrate,

/p>

maltodextrin,

crospovidone micronized,

magnesium stearate.

How to take, the dosage

The drug is taken orally with meals once a day.

In rheumatoid arthritis: The recommended dose is 15 mg/day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg/day.

In osteoarthritis: Recommended dose is 7.5 mg/day. If ineffective, the dose can be increased to 15 mg/day.

In ankylosing spondylitis: The dose is 15 mg/day. The maximum daily dose should not exceed 15 mg.

In patients at increased risk of side effects, and in patients with severe renal failure on hemodialysis: The dose should not exceed 7.5 mg/day.

For ease of dosing, it is possible to use the drug: Mirlox tablets 7.5 mg disp. 20 Grodziski Pharmaceutical Plant Polfa d.o.o.

Preferral of Mirlox tablets 7.5 mg.

Interaction

Concomitant use with other NSAIDs (as well as with acetylsalicylic acid ) increases the risk of erosive ulcerative lesions and bleeding from the gastrointestinal tract.

When used concomitantly with antihypertensive drugs, the effectiveness of the latter may be reduced.

Simultaneous use with lithium preparations may lead to cumulation of lithium and an increase in its toxic effects (we recommend that the lithium concentration in the blood be controlled).

In case of concomitant use with methotrexate the side effect of the latter on the hematopoietic system increases (danger of anemia and leukopenia; periodic control of total blood count is indicated).

Concomitant use with diuretics and with cyclosporine increases the risk of renal failure.

Concomitant use with intrauterine contraceptives may decrease the effectiveness of the latter.

In concomitant use with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic agents (streptokinase, fibrinolysin) the risk of bleeding increases (periodic monitoring of blood clotting is necessary).

In concomitant use with colestiramine, as a result of binding of meloxicam, its excretion through the gastrointestinal tract is increased.

Special Instructions

The drug should be used with caution in patients with a history of peptic ulcer disease and duodenal ulcer, as well as in patients receiving anticoagulant therapy. In these patients the risk of gastrointestinal erosive-ulcer lesions is increased.

The drug should be used with caution and under control of renal function parameters in elderly patients, patients with chronic heart failure with circulatory insufficiency, patients with cirrhosis of liver as well as in patients with hypovolemia because of surgical operations.

In patients with renal insufficiency if CKG is more than 25 ml/min, dosage regimen adjustment is not required.

In patients on dialysis, the maximum dose of the drug is 7.5 mg/day.

Patients taking diuretics and meloxicam at the same time should get enough fluids.

If allergic reactions (itching, skin rash, urticaria), as well as photosensitization occurred during treatment, the patient should consult a physician to decide whether to discontinue the drug.

Hypatic disorders: Contraindicated in severe hepatic insufficiency.

Application in renal impairment: In patients with increased risk of side effects and in patients with severe renal impairment who are on hemodialysis, the dose should not exceed 7.5 mg/day.

Impact on the ability to drive and operate vehicles: The use of the drug may cause adverse effects in the form of headache and dizziness, drowsiness. If the above mentioned effects occur it is necessary to refrain from driving vehicles, operating machines and mechanisms.

Contraindications

– “Aspirin” asthma.
– Gastric and duodenal ulcer in the acute phase.
– Severe hepatic failure.
– Severe renal failure (if hemodialysis is not carried out).
– Children under 15 years of age.
– Pregnancy.
– Lactation (breast-feeding).
– Hypersensitivity to the drug components.

The drug should be used with caution in elderly patients with gastrointestinal erosive lesions in past history.

Side effects

Gastrointestinal system disorders: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, gastrointestinal erosive and ulcerative lesions, gastric or intestinal perforation, gastrointestinal bleeding (hidden or overt), increased liver enzyme activity, hepatitis, colitis, stomatitis, dry mouth, esophagitis.

Cardiovascular system: tachycardia, increased BP, feeling of hot flashes.

Respiratory system disorders: exacerbation of bronchial asthma, cough.

CNS disorders: headache, dizziness, tinnitus, disorientation, mental confusion, sleep disorders.

Urinary system disorders: edema, interstitial nephritis, renal medullary necrosis, urinary tract infection, proteinuria, hematuria, renal failure.

An organ of vision: conjunctivitis, blurred vision.

Hematopoietic system disorders: anemia, leukopenia, thrombocytopenia.

Dermatological reactions: itching, skin rash, increased photosensitivity.

Allergic reactions: urticaria, anaphylactoid reactions (including anaphylactic shock), edema of the lips and tongue, allergic vasculitis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Others: fever.

Overdose

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

Treatment: gastric lavage, administration of activated charcoal (within the next hour after intake), symptomatic therapy. Colestyramine accelerates excretion of meloxicam from the body. Forced diuresis, urine alkalinization, hemodialysis are ineffective due to the high binding of meloxicam with blood proteins. There is no specific antidote.

Pregnancy use

The drug is contraindicated in pregnancy and lactation.

Similarities