Arcoxia pills 90 mg 28 pcs
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Active ingredients
Etoricoxib
Release form
Pills
Composition
Active ingredient: etoricoxibActivating agents: calcium phosphate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate. Active substance concentration (mg): 90 mg
Pharmacological effect
NSAIDs. Selective inhibitor of COX-2, in therapeutic concentrations, blocks the formation of prostaglandins and has anti-inflammatory, analgesic and antipyretic effects. Selective inhibition of COX-2 is accompanied by a decrease in the severity of clinical symptoms associated with the inflammatory process, with no effect on platelet function and gastrointestinal mucosa. Etorikoksib has a dose-dependent effect of inhibition of COX-2, without affecting COX-1 when used in a daily dose 150 mg. Arcoxia does not affect the production of prostaglandins in the gastric mucosa and for the time of bleeding. In the conducted studies, no decrease in arachidonic acid and platelet aggregation caused by collagen was observed.
Pharmacokinetics
AbsorptionAfter ingestion is rapidly absorbed from the gastrointestinal tract. Bioavailability when administered is about 100%. After taking the drug by adults on an empty stomach at a dose of 120 mg Cmax is 3.6 mcg / ml, the time to reach Cmax is 1 hour after ingestion. Food intake does not have a significant effect on the severity and rate of absorption of Etoricoxib when taken at a dose of 120 mg. At the same time, there is a decrease in Cmax values by 36% and an increase in Tmax by 2 hours. Acceptance of antacids does not affect the pharmacokinetics of the drug. Distribution The average geometric AUC0-24 was 37.8 μg × h / ml. The pharmacokinetics of etoricoxib within the range of therapeutic doses is linear. The binding to plasma proteins exceeds 92%. Vd in equilibrium is about 120 l. Etorikoksib penetrates through the placental barrier and through the BBB. Metabolism Intensively metabolized in the liver, with the participation of the cytochrome P450 isoenzyme (CYP) and the formation of 6-hydroxymethyl-etoricoksib. 5 metabolites of etoricoxib were detected, the main ones - 6-hydroxymethyl-ethoroxib and its derivative - 6-carboxy-acetyl-etoricoxib. The major metabolites do not affect COX-1 and are completely inactive or inactive with respect to COX-2. Intake Excretion of etoricoxib occurs in the form of metabolites by the kidneys.Less than 1% of the drug is excreted in the urine unchanged. With a single IV injection to healthy volunteers, a labeled radioactive drug containing Etoricoxib at a dose of 25 mg has been demonstrated that 70% of the drug is excreted by the kidneys, 20% through the intestine, mainly in the form of metabolites. Less than 2% was found unchanged. An equilibrium state is reached after 7 days with a daily dose of 120 mg, with a cumulation factor of about 2, which corresponds to T1 / 2 - about 22 hours. The plasma clearance is about 50 ml / min. Pharmacokinetics in special In clinical cases, pharmacokinetic differences in men and women are absent. The pharmacokinetics in the elderly (65 years and older) is comparable to those in the young, and there is no need to adjust the dose of the drug in the elderly. Passage differences do not affect the pharmacokinetics ethoricoxib parameters. In patients with minor hepatic impairment (5-6 points on the Child-Pugh scale), a single dose of 60 mg / day of etoricoxib was accompanied by an increase in AUC by 16% compared with healthy individuals. In patients with moderately impaired liver function (7-9 points on the Child-Pugh scale) who took the drug at a dose of 60 mg every other day, the AUC value was the same as in healthy individuals who took the drug daily at the same dose. Clinical and pharmacokinetic studies in patients with severe impairment ne functions There are no results (more than 9 points on the Child-Pugh scale). The pharmacokinetic parameters of single dose administration of Etoricoxib 120 mg in patients with moderate to severe renal failure and end-stage chronic renal failure on hemodialysis did not differ significantly from those in healthy individuals. . Hemodialysis had little effect on elimination (clearance of dialysis - about 50 ml / min). The pharmacokinetic parameters of etoricoxib in children under 12 years of age have not been studied. In comparative pharmacokinetic studies, comparable data were obtained when using etoricoxib in a group of adolescents (12 to 17 years old) with a body weight of 40-60 kg at a dose of 60 mg / day, in the same age group and with a body weight of more than 60 kg - 90 mg / day , and in adults when taking 90 mg / day.
Indications
Symptomatic therapy of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, pain and inflammatory symptoms associated with acute gouty arthritis.
Contraindications
Hypersensitivity to any component of the drug, a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including history), erosive and ulcerative changes of the gastric mucosa or 12 duodenal ulcer , active gastrointestinal bleeding; cerebrovascular or other bleeding; inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase; hemophilia and other bleeding disorders; severe heart failure (NYHA II-IV); severe hepatic insufficiency (more than 9 points on the Child-Pugh scale) or active liver disease, severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia; period after coronary artery bypass surgery; peripheral arterial diseases, cerebrovascular diseases, clinically expressed coronary heart disease, persistently maintained blood pressure values exceeding 140/90 mm Hg. st. with uncontrolled hypertension, pregnancy, breastfeeding period, children under 16 years of age.
Precautionary measures
With caution, the drug is used in the presence of anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, Helicobacter pylori infection, in elderly people, in patients who have long used NSAIDs, who often drink alcohol, in severe somatic diseases, dyslipidemia / hyperlipidemia, in diabetes, hypertension, edema and fluid retention, smoking, in patients with QA less than 60 ml / min, with concomitant therapy with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (for example p, acetylsalicylic acid, clopidogrel), corticosteroids (e.g., prednisone), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).
Use during pregnancy and lactation
The drug is contraindicated during pregnancy and lactation. The use of the drug can adversely affect female fertility and is not recommended for women planning a pregnancy.
Dosage and administration
Inside, regardless of the meal, with a small amount of water. Osteoarthritis: The recommended dose is 60 mg once a day. Rheumatoid arthritis and ankylosing spondylitis: The recommended dose is 90 mg once a day. Acute gouty arthritis: The recommended dose in the acute period is 120 mg once a day. The duration of use of the drug at a dose of 120 mg is not more than 8 days. You should use the minimum effective dose of the shortest possible short course. The average therapeutic dose for pain syndrome is 60 mg per day.
Side effects
Very often> 10%, often -1-10%; infrequently - 0.1-1%; rarely 0.01–0.1%; very rarely - less than 0.01%, including some cases. On the part of the digestive system: often - epigastric pain, nausea, diarrhea, dyspepsia, flatulence; infrequently - abdominal distension, belching, increased peristalsis, constipation, dryness of the oral mucosa, gastritis, gastric or duodenal ulcers, irritable bowel syndrome, esophagitis, ulcers of the oral mucosa, vomiting; very rarely - gastrointestinal ulcers (with bleeding or perforation). On the part of the hepatobiliary system: very rarely - hepatitis. The nervous system: often - headache, dizziness, weakness; infrequently - a violation of taste, drowsiness, sleep disturbances, a violation of sensitivity, incl. paresthesia / hyperesthesia, anxiety, depression, impaired concentration, very rarely - hallucinations, confusion. On the part of the senses: infrequently - blurred vision, conjunctivitis, tinnitus, vertigo. From the urinary system: infrequently - proteinuria; very rarely - renal failure, usually reversible with drug withdrawal. Allergic reactions: very rarely - anaphylactic / anaphylactoid reactions, including marked reduction in blood pressure and shock; Since the cardiovascular system: often - heartbeat, increased blood pressure; infrequently - hot flashes, cerebrovascular accident, atrial fibrillation, congestive heart failure, non-specific ECG changes; myocardial infarction, very rarely - hypertensive crisis. On the part of the respiratory system: Infrequently - cough, shortness of breath, nosebleeds; very rarely - bronchospasm.On the part of the skin: often - ecchymosis; infrequently - swelling of the face, itchy skin, rash; very rarely - urticaria, Stevens-Johnson syndrome, Lyell's syndrome. Infections: infrequently - gastroenteritis, infections of the upper respiratory tract, urinary tract. From the musculoskeletal system: infrequently - muscle cramps, arthralgia, myalgia. Metabolic disorders: often - edema, fluid retention; infrequently - changes in appetite, weight gain. Others: often - flu-like syndrome; infrequently - chest pains. The results of laboratory tests: often - increased "liver" transaminases; infrequently - an increase in nitrogen in the blood and urine, increased activity of creatine phosphokinase, decrease in hematocrit, decrease in hemoglobin, hyperkalemia, leukopenia, thrombocytopenia, increase in serum creatinine, increase in uric acid; rarely, an increase in serum sodium.
Overdose
In clinical trials, Arcoxia overdose was not reported. In clinical trials, a single dose of Arcoxia in a single dose of up to 500 mg or multiple intakes of up to 150 mg / day for 21 days did not cause significant toxic effects. Symptoms: an overdose of the drug may cause undesirable effects from the gastrointestinal tract, cardiovascular system and kidneys. Treatment: conduct symptomatic therapy. Etotrikoksib is not excreted by hemodialysis, the removal of the drug during peritoneal dialysis has not been studied.
Interaction with other drugs
Pharmacodynamic interaction In patients receiving warfarin, Arcoxia intake at a dose of 120 mg / day was accompanied by an increase of about 13% MPE and prothrombin time. In patients receiving warfarin or similar drugs, MHO should be monitored when starting therapy or changing the Arcoxia dosing regimen, 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 in the treatment of patients taking Arcoxia simultaneously with ACE inhibitors. In patients with impaired renal function (for example, during dehydration or in old age), such a combination may exacerbate the functional insufficiency of the kidneys. Arcoxia can be used simultaneously with acetylsalicylic acid in low doses intended for the prevention of cardiovascular diseases.However, the simultaneous appointment of acetylsalicylic acid in low doses and Arcoxia can lead to an increase in the frequency of ulcerative lesions of the gastrointestinal tract and other complications compared with Arcoxia alone. After reaching equilibrium, the administration of etoricoxib at a dose of 120 mg 1 time / day does not affect the antiplatelet activity of acetylsalicylic acid at low doses (81 mg / day). The drug does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases. Cyclosporine and tacrolimus increase the risk of nephrotoxicity while receiving Arcoxia. This interaction should be taken into account when treating patients taking Arcoxia at the same time as lithium. In two studies, the effects of Arcoxia at 60, 90, and 120 mg were tested once a day for seven days in patients who received methotrexate 1 dose per week. 7.5 to 20 mg for rheumatoid arthritis. Arcoxia at a dose of 60 and 90 mg did not affect the plasma concentration (by AUC) and the renal clearance of methotrexate. In one study, Arcoxia at a dose of 120 mg had no effect on plasma concentration (AUC) and renal clearance of methotrexate. In another study, Arcoxia at a dose of 120 mg increased plasma concentration of methotrexate by 28% (according to AUC) and decreased the renal clearance of methotrexate by 13%. With the simultaneous appointment of Arcoxia in doses above 90 mg / day and methotrexate, it should be monitored for the possible toxic effects of methotrexate. day, at the same time or with a difference of 12 hours, increases the stationary ethylene estradiol AUC0-24 by 50-60%. However, the concentration of norethisterone usually does not increase to a clinically significant extent. This increase in ethinyl estradiol concentration should be taken into account when selecting the appropriate oral contraceptive for simultaneous use with Arcoxia. This fact can lead to an increase in the frequency of thromboembolism, due to the increased exposure to ethinyl estradiol.No significant pharmacokinetic interaction with GCS was found. Etorikoksib does not affect AUC0-24 in the equilibrium state or the elimination of digoxin. At the same time, etoricoxib increases Cmax (by an average of 33%), which can be important if digoxin overdose develops. Simultaneous administration of Arcoxia and rifampicin (a powerful inducer of hepatic metabolism) results in a 65% decrease in plasma AUC of etrikoxib. This interaction should be considered when administering Arcoxia with rifampicin at the same time. Antacids and ketoconazole (a potent CYP3A4 inhibitor) do not have a clinically significant effect on Arcoxia pharmacokinetics.
special instructions
Taking Arcoxia requires careful monitoring of blood pressure. All patients in the appointment of the drug should be monitored blood pressure during the first two weeks of treatment and periodically in the future. You should also regularly monitor indicators of liver and kidney function. In case of increased levels of hepatic transaminases, 3 times or more with VGN, the drug should be canceled. Considering the increase the risk of adverse effects with increasing duration of administration, it is necessary to periodically assess the need to continue taking the drug and the possibility of reducing the dose. It is necessary to use the drug simultaneously with other NPVS. The capsule of Arcoxia contains a small amount of lactose, which should be taken into account when prescribing the drug to patients with lactase deficiency. Impact on the ability to drive vehicles and control mechanisms activities requiring increased concentration and psychomotor speed reactions. Patients with episodes of dizziness, drowsiness or weakness should refrain from activities that require concentration.