Arkoksia - instructions for use, reviews, analogs and formulations (tablets 30 mg, 60 mg, 90 mg and 120 mg) drugs for the treatment of arthrosis and arthritis in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Arkoxia. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Arkoksia in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Arkoksia in the presence of existing structural analogs. Use for the treatment of arthrosis and arthritis in adults, children, as well as during pregnancy and lactation.Composition and interaction of the drug with alcohol.

Arkoxia non-steroidal anti-inflammatory drug (NSAID). The selective inhibitor of COX-2, at therapeutic concentrations, blocks the formation of prostaglandins and has anti-inflammatory, analgesic and antipyretic effects. Selective oppression of COX-2 is accompanied by a decrease in the severity of clinical symptoms associated with the inflammatory process, with no effect on the function of platelets and the mucosa of the gastrointestinal tract.

Etorikoksib (the active substance of the preparation Arkoksia) has a dose-dependent effect of COX-2 inhibition, without affecting COX-1 when applied at a daily dose of up to 150 mg. Arkoksia has no effect on the production of prostaglandins in the mucous membrane of the stomach and at the time of bleeding. In the conducted studies, there was no decrease in the level of arachidonic acid and platelet aggregation caused by collagen.

Composition

Etoricoxib + excipients.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the digestive tract. Bioavailability with oral administration is about 100%.Eating does not have a significant effect on the severity and rate of absorption of etorikoksiba when taken in a dose of 120 mg. Reception of antacids does not affect the pharmacokinetics of the drug. Etorikoksib penetrates the placental barrier and through the blood-brain barrier (BBB). Intensively metabolized in the liver, with the participation of cytochrome P450 isoenzyme (CYP) and the formation of 6-hydroxymethyl-etoricoxib. Elimination of etorikoksib occurs in the form of metabolites by the kidneys. Less than 1% of the drug is excreted in the urine unchanged.

With a single intravenous administration of healthy volunteers with a labeled radioactive preparation containing etorikoksib in a dose of 25 mg, it was demonstrated that 70% of the drug is excreted by the kidneys, 20% through the intestine, mainly in the form of metabolites. Less than 2% is found unchanged.

There are no pharmacokinetic differences in men and women.

Pharmacokinetics in the elderly (65 years and older) are comparable to those in young people, and there is no need to adjust the dose of the drug in the elderly.

The pharmacokinetic parameters of etorikoksib in children younger than 12 years have not been studied. In comparative pharmacokinetic studies, comparable data were obtained with the use of etorikoksib in the group(from 12 to 17 years) with a body weight of 40-60 kg at a dose of 60 mg per day in a similar age group and with a body weight of more than 60 kg - 90 mg per day, and in adults with admission 90 mg per day.

Indications

Symptomatic therapy of the following diseases and conditions:

• osteoarthritis;
• rheumatoid arthritis;
• ankylosing spondylitis;
• pain and inflammatory symptoms associated with acute gouty arthritis;
• therapy of moderate and severe acute pain after dental operations.

Forms of release

Tablets coated with 30 mg, 60 mg, 90 mg and 120 mg.

Other dosage forms, whether injections in ampoules, ointment or gel, do not exist.

Instructions for use and dosing regimen

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

With osteoarthritis, the recommended dose is 60 mg 1 time per day. The daily dose for osteoarthritis should not exceed 60 mg.

In rheumatoid arthritis and ankylosing spondylitis, the recommended dose is 90 mg once a day. The daily dose for 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 a day.The daily dose for acute gouty arthritis should not exceed 120 mg.

The duration of use of the drug at a dose of 120 mg is not more than 8 days. A minimum effective dose should be used with the minimum possible short course.

The average therapeutic dose for pain is only 60 mg once.

Acute pain after dental operations: the recommended dose is 90 mg once a day. In the treatment of acute pain, the drug Arkoksia should be used only in the acute symptomatic period, limited to no more than 8 days. The daily dose for pain relief after dental operations should not exceed 90 mg.

In patients with hepatic insufficiency (5-9 points on the Child-Pugh scale), it is recommended not to exceed the daily dose of 60 mg.

Side effect

• epigastric pain;
• nausea, vomiting;
• diarrhea;
• dyspepsia;
• flatulence;
• bloating;
• eructation;
• increased peristalsis;
• constipation;
• dryness of the oral mucosa;
• gastritis;
• ulcer of the mucous membrane of the stomach or duodenum;
• irritable bowel syndrome;
• esophagitis;
• ulcers of the oral mucosa;
• Gastrointestinal ulcers (with bleeding or perforation);
• headache;
• dizziness;
• weakness;
• a taste disorder;
• drowsiness;
• sleep disorders;
• sensitivity disorders, incl. paresthesia / hyperesthesia;
• anxiety;
• depression;
• hallucinations;
• confusion of consciousness;
• blurred vision;
• conjunctivitis;
• noise in ears;
• renal failure, usually reversible with withdrawal of the drug;
• anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock;
• palpitation;
• increased blood pressure;
• tides;
• impaired cerebral circulation;
• atrial fibrillation;
• congestive heart failure;
• hypertensive crisis;
• cough;
• dyspnea;
• nose bleed;
• bronchospasm;
• swelling of the face;
• itching;
• rash;
• hives;
• Stevens-Johnson syndrome;
• Lyell's syndrome;
• infection of the upper respiratory tract, urinary tract;
• muscle cramps;
• arthralgia;
• myalgia;
• edema, fluid retention;
• changes in appetite;
• weight gain;
• leukopenia, thrombocytopenia;
• influenza-like syndrome;
• pain in the chest.

Contraindications

• complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis);
• erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding;
• inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;
• hemophilia and other bleeding disorders;
• severe heart failure (2-4 NYHA functional classes);
• severe hepatic impairment (more than 9 on the Child-Pugh scale) or active liver disease;
• renal failure of severe degree (QC less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;
• period after aortocoronary shunting; diseases of peripheral arteries, cerebrovascular diseases, clinically expressed coronary artery disease;
• persistently persisting values ​​of blood pressure greater than 140/90 mm Hg. Art. with uncontrolled arterial hypertension;
• pregnancy;
• lactation period (breastfeeding);
• children's age till 16 years;
• hypersensitivity to any component of the drug.

Application in pregnancy and lactation

The drug is contraindicated in pregnancy and lactation.

The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.

Use in children

Contraindicated in children and adolescents under the age of 16 years.

special instructions

Admission of the drug Arkoksia requires careful monitoring of blood pressure. All patients should be monitored during the first two weeks of treatment and periodically thereafter.

Also, the liver and kidney function indicators should be monitored regularly.

In the case of an increase in the level of hepatic transaminases 3 times or more relative to VGN, the drug should be withdrawn.

Given the increased risk of developing unwanted effects with an increase in the duration of admission, it is necessary to periodically assess the need to continue taking the drug and the possibility of reducing the dose.

Do not use the drug simultaneously with other non-steroidal anti-inflammatory drugs.

Use with caution when taking alcohol frequently.

The shell of the drug Arkoksia contains lactose in a small amount, which should be taken into account when prescribing the drug to patients with lactase deficiency.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Patients who have had episodes of dizziness, drowsiness, or weakness should refrain from occupations requiring concentration.

Drug Interactions

Pharmacodynamic interaction

In patients receiving warfarin, taking Arcoxia at a dose of 120 mg per day was accompanied by an increase of approximately 13% in MHO and prothrombin time. In patients receiving Warfarin or similar drugs, MHO should be monitored when starting therapy or changing the dosage regimen of Arkoxia, especially in the first few days.

There have been reports that non-selective NSAIDs and selective inhibitors of COX-2 can weaken the hypotensive effect of ACE inhibitors. This interaction should be taken into account in the treatment of patients taking Arkoxia concomitantly with ACE inhibitors. In patients with impaired renal function (for example, with dehydration or in old age), a similar combination can aggravate functional kidney failure.

Arkoksia can be used simultaneously with Acetylsalicylic acid in low doses, designed to prevent cardiovascular diseases. However, simultaneous administration of acetylsalicylic acid in low doses and Arkoksia can lead to an increase in the frequency of ulcerative gastrointestinal lesions and other complications compared with the administration of one Arkoksia. After reaching the equilibrium state, taking etorikoksib in a dose of 120 mg once a day does not affect the antiplatelet activity of acetylsalicylic acid in low doses (81 mg per day). The drug does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

Cyclosporine and tacrolimus increase the risk of developing nephrotoxicity with Arkoxia.

Pharmacokinetic interaction

There are data that nonselective NSAIDs and selective inhibitors of COX-2 can increase the concentration of lithium in plasma. This interaction should be taken into account in the treatment of patients taking Arkoxia concomitantly with lithium.

Two studies examined the effects of Arkoxia at a dose of 60, 90 and 120 mg once daily for seven days in patients who received Methotrexate at a dose of 7.5 to 20 mg once a week for rheumatoid arthritis. Arkoksia in a dose of 60 and 90 mg did not affect the plasma concentration (AUC) and renal clearance of methotrexate. In one study, 120 mg of arkoxia had no effect on plasma concentration (AUC) and renal clearance of methotrexate. In another study, 120 mg of arkoxia increased the plasma methotrexate concentration by 28% (AUC) and reduced the renal clearance of methotrexate by 13%. If concomitant administration of Arkoksa in doses above 90 mg per day and methotrexate should be monitored for the possible emergence of toxic effects of methotrexate.

Oral contraceptives: reception of Arkoksia in a dose of 120 mg with oral contraceptives,containing 35 μg of ethinyl estradiol 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, the concentration of norethisterone usually does not increase to a clinically significant extent. This increase in the concentration of ethinylestradiol should be taken into account when choosing the appropriate oral contraceptive for simultaneous use with arkoxia. This fact can lead to an increase in the frequency of thromboembolism, by increasing the exposure of ethinylestradiol. No significant pharmacokinetic interaction with GCS was found.

Etorikoksib does not affect AUC0-24 in the equilibrium state or the elimination of digoxin. However, etorikoksib increases Cmax (an average of 33%), which may be important in the development of an overdose of digoxin.

Simultaneous administration of Arkoxia and rifampicin (a powerful inducer of hepatic metabolism) leads to a 65% decrease in AUC etorikoksib in plasma. This interaction should be considered with the simultaneous administration of arkoxia with rifampicin.

Antacids and Ketoconazole (a potent inhibitor of CYP3A4) do not have a clinically significant effect on the pharmacokinetics of arkoxia.

Analogues of the drug Arkoksia

There are no structural analogs to the active substance of the drug Arkoksia.

Analogues on the curative effect (agents for the treatment of arthrosis):

• Actasulide;
• Alflutop;
• Apranaks;
• Arthra;
• Artradol;
• Arthrovit;
• Arthrotheca;
• Aulin;
• Brufen;
• Butadione;
• Beliefed;
• Voltaren Emulgel;
• Glucosamine sulfate 750;
• Dexazone;
• Dexamethasone phosphate;
• Diklobene;
• Dicluberl;
• Dicloran;
• Diclofen;
• Diclofenac;
• Dimexide;
• Diprospan;
• Dolgit;
• DONA;
• Donalgin;
• Zinaksin;
• Ibuprofen;
• Indomethacin;
• Kartilag Vitrum;
• Ketonal;
• Coxib;
• Mesulide;
• Miolastane;
• Movasin;
• Naproxen;
• Nimesil;
• Orthophene;
• Piroxicam;
• Rheumatic Gel;
• Ronidase;
• Rumalon;
• Sabelnik Evalar;
• Sanaprox;
• Tenikam;
• Tenoktil;
• Triamsinolone;
• Fastum gel;
• Feloran;
• Floiled;
• Chondramine;
• Chondrolon;
• Cefexon;
• Cigapan;
• The Unium.

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