Arcoxia, 60 mg 14 pcs

Arcoxia is a nonsteroidal anti-inflammatory drug. It is a selective COX-2 inhibitor, in therapeutic concentrations it blocks formation of prostaglandins and has anti-inflammatory, analgesic and antipyretic effects.

Selective inhibition of COX-2 is accompanied by decrease of severity of clinical symptoms related to the inflammatory process with no effect on platelet function and gastrointestinal mucosa.

Etoricoxib has a dose-dependent effect of COX-2 inhibition with no effect on COX-1 when used in daily doses up to 150 mg.

Arcoxia has no effect on the production of prostaglandins in the gastric mucosa and on bleeding time. In the studies conducted, there was no decrease in arachidonic acid levels and collagen-induced platelet aggregation.

Indications

Symptomatic therapy for the following diseases and conditions:

Active ingredient

Composition

1 tablet contains:

Active substance:

Etoricoxib 60 mg;

Auxiliary substances:

Calcium hydrophosphate;

Cellulose microcrystalline;

Croscarmellose sodium;

Magnesium stearate.

How to take, the dosage

The drug is taken orally, regardless of meals, with a small amount of water.

In osteoarthritis the recommended dose is 60 mg once daily. The daily dose in osteoarthritis should not exceed 60 mg.

In rheumatoid arthritis and ankylosing spondylitis the recommended dose is 90 mg once daily. The daily dose in rheumatoid arthritis and ankylosing spondylitis should not exceed 90 mg.

In acute gouty arthritis the recommended dose in the acute period is 120 mg once daily. The daily dose in acute gouty arthritis should not exceed 120 mg.

The duration of use of the drug in a dose of 120 mg is not more than 8 days. The minimum effective dose should be used for the shortest possible course.

The average therapeutic dose for pain syndrome is a single dose of 60 mg.

Acute pain after dental surgery: The recommended dose is 90 mg once daily. In the treatment of acute pain, the drug Arcoxia® should be used only in the acute symptomatic period, limited to a duration of not more than 8 days. The daily dose for pain relief after dental surgery should not exceed 90 mg.

In patients with hepatic impairment (Child-Pugh score 5-9) it is recommended that the daily dose not exceed 60 mg.

Interaction

Pharmacodynamic interaction

In patients receiving warfarin, Arcoxia® at a dose of 120 mg/day was associated with an increase of approximately 13% in MHO and prothrombin time. In patients receiving warfarin or similar drugs, MHO values should be monitored at the start of therapy or change of the dosing regimen of Arcoxia®, especially in the first few days.

There are reports that non-selective NSAIDs and selective COX-2 inhibitors may weaken the hypotensive effect of ACE inhibitors. This interaction should be taken into account when treating patients taking Arcoxia® simultaneously with ACE inhibitors. In patients with impaired renal function (e.g., in dehydration or elderly patients) this combination may aggravate functional renal failure.

Arcoxia® may be used concomitantly with acetylsalicylic acid at low doses intended for prevention of cardiovascular disease. However, concomitant administration of low-dose acetylsalicylic acid and Arcoxia® may result in an increased incidence of GI ulceration and other complications compared to administration of Arcoxia® alone. After reaching equilibrium, administration of etoricoxib at a dose of 120 mg once daily has no effect on the antiplatelet activity of low-dose acetylsalicylic acid (81 mg/day). The drug does not replace the prophylactic effect of acetylsalicylic acid in cardiovascular diseases.

Cyclosporine and tacrolimus increase the risk of nephrotoxicity with Arcoxia®.

Pharmacokinetic interaction

There is evidence that non-selective NSAIDs and selective COX-2 inhibitors may increase the plasma concentration of lithium. This interaction should be taken into consideration when treating patients taking Arcoxia® concomitantly with lithium.

Two studies investigated the effects of Arcoxia® in doses of 60, 90 and 120 mg once daily for seven days in patients who received once weekly methotrexate in doses of 7.5 to 20 mg for rheumatoid arthritis. Arcoxia® at doses of 60 and 90 mg had no effect on plasma concentrations (AUC) and renal clearance of methotrexate. In one study, Arcoxia® at a dose of 120 mg had no effect on plasma concentrations (AUC) and renal clearance of methotrexate. In another study, Arcoxia® at a dose of 120 mg increased plasma concentration of methotrexate by 28% (by AUC) and decreased renal clearance of methotrexate by 13%. When concomitant administration of Arcoxia® in doses above 90 mg/day and methotrexate, the possible occurrence of toxic effects of methotrexate should be monitored.

Peroral contraceptives: taking Arcoxia® in a dose of 120 mg with oral contraceptives containing 35 mcg of ethinylestradiol and 0.5 to 1 mg of norethindrone for 21 days, simultaneously or 12 hours apart, increases the steady-state AUC0-24 of ethinylestradiol by 50-60%. However, norethisterone concentrations are not usually increased to a clinically significant degree. This increase in ethinylestradiol concentration should be taken into account when choosing an appropriate oral contraceptive for concomitant use with Arcoxia®. Such a fact may lead to an increased incidence of thromboembolism, due to increased exposure to ethinylestradiol. No significant pharmacokinetic interaction with GCS was found.

Etoricoxib has no effect on the AUC0-24 in equilibrium or elimination of digoxin. However, etoricoxib increases Cmax (by an average of 33%), which may be important in the development of digoxin overdose.

The concomitant administration of Arcoxia® and rifampicin (a potent inducer of hepatic metabolism) leads to a 65% reduction of AUC of etoricoxib in plasma. This interaction should be considered when concomitant administration of Ancoxia® with rifampicin.

The antacids and ketoconazole (potent CYP3A4 inhibitor) have no clinically significant effect on the pharmacokinetics of Arcoxia®.

Special Instructions

Administration of the drug Arcoxia® requires close monitoring of BP. All patients should have their BP monitored during the first two weeks of treatment and periodically thereafter.

Hep and renal function should also be monitored regularly.

The drug should be discontinued if hepatic transaminases increase 3-fold or more relative to HGH.

With increasing risk of adverse effects with increasing duration of use, the need to continue the drug and the possibility of reducing the dose should be periodically assessed.

The drug should not be used concomitantly with other NSAIDs.

The film of Arcoxia® contains a small amount of lactose; this must be considered when prescribing the drug in patients with lactase deficiency.

Influence on driving and operating machinery

At the time of treatment, caution should be exercised while driving motor transport and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions. Patients who have had episodes of dizziness, drowsiness or weakness should refrain from activities requiring concentration.

Contraindications

Side effects

Digestive system disorders: often – epigastric pain, heartburn, nausea, diarrhea, dyspepsia, flatulence; infrequent – bloating, belching, increased peristalsis, constipation, dry oral mucosa, gastritis, gastric or duodenal ulcer, irritable bowel syndrome, esophagitis, oral mucosa ulcers, vomiting; very rare – gastrointestinal ulcers (with bleeding or perforation), hepatitis.

Nervous system disorders:often – headache, dizziness, weakness; infrequently – taste disorders, drowsiness, sleep disorders, sensory disturbances, including paresthesia/hyperesthesia, anxiety, depression, concentration disorders; very rarely – hallucinations, confusion.

Sensory organs: infrequent – blurred vision, conjunctivitis, tinnitus, vertigo.

Urinary system disorders: infrequent – proteinuria; very rare – renal failure, usually reversible upon discontinuation of the drug.

Allergic reactions:very rarely – anaphylactic/anaphylactoid reactions, including marked BP decrease and shock.

Cardiovascular system:often – palpitations, increased BP; infrequently – hot flashes, impaired cerebral circulation, atrial fibrillation, congestive heart failure, non-specific ECG changes; myocardial infarction; very rare – hypertensive crisis.

In the respiratory system: infrequent – cough, dyspnea, nasal bleeding; very rare – bronchospasm.

Dermatological reactions:often – ecchymosis; infrequently – facial swelling, skin itching, rash; very rarely – urticaria, Stevens-Johnson syndrome, Lyell’s syndrome.

Infectious complications: infrequent – gastroenteritis, infections of the upper respiratory tract, urinary tract.

Muscular system disorders:infrequent – muscle cramps, arthralgia, myalgia.

Metabolic disorders:often – edema, fluid retention; infrequently – changes in appetite, weight gain.

From the side of laboratory tests: often – increased activity of hepatic transaminases; infrequent – increased nitrogen in blood and urine, increased CPK activity, decreased hematocrit, decreased hemoglobin, hyperkalemia, leukopenia, thrombocytopenia, increased serum creatinine, increased uric acid; rare – increased serum sodium.

Others:often – flu-like syndrome; infrequently – chest pain.

Overdose

No overdose of Arcoxia® has been reported in clinical trials. In clinical trials, single administration of Arcoxia® in a single dose up to 500 mg or multiple administration up to 150 mg/day for 21 days caused no significant toxic effects.

Symptoms:In overdose of the drug, there may be adverse effects on the gastrointestinal, cardiovascular and renal systems.

Treatment:Symptomatic therapy is carried out. Etricoxib is not excreted by hemodialysis; excretion of the drug in peritoneal dialysis has not been studied.

Similarities