Arcoxia coated pills 60mg N28

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Active ingredients

Etoricoxib

Release form

Pills

Composition

Ingredients 1 tablet: active ingredient: etoricoxib. Excipients: calcium hydrophosphate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate. The composition of the shell: opadry II white 39K18305, carnauba wax. The composition of the film shell: lactose monohydrate, hypromellose, titanium dioxide, triacetin.

Pharmacological effect

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, and there is no effect on the function of platelets and the mucous membrane of the gastrointestinal tract. Etoricoxib has a dose-dependent effect of inhibiting COX-2, without affecting COX-1 when used in a daily dose of up to 150 mg. Arcoxia does not affect the production of prostaglandins in the gastric mucosa and for the time of bleeding. In the studies conducted, no decrease in arachidonic acid and platelet aggregation caused by collagen was observed.

Pharmacokinetics

Absorption After ingestion is rapidly absorbed from the gastrointestinal tract. Bioavailability when administered is about 100%. After the drug is taken by adults on an empty stomach at a dose of 120 mg Cmax is 3.6 mcg / ml, Tmax -1 h after administration. Eating does not have a significant effect on the severity and rate of absorption of Etoricoxib when taken in a dose of 120 mg. At the same time, Cmax values ​​are reduced by 36% and Tmax is increased by 2 hours. Taking antacids does not affect the pharmacokinetics of the drug. Distribution The geometric mean AUC0-24 was 37.8 mcg x h / ml. The pharmacokinetics of etoricoxib within the range of therapeutic doses is linear. Plasma protein binding exceeds 92%. Vd in equilibrium is about 120 l. Etoricoxib crosses the placental and blood-brain barrier. Metabolism Intensively metabolized in the liver, with the participation of the cytochrome P450 isoenzyme (CYP) and the formation of 6-hydroxymethyl-etoroksiba. 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 towards COX-2. Withdrawal Withdrawal of etoricoxib occurs as metabolites through the kidneys. Less than 1% of the drug is excreted in the urine unchanged. With a single on / in the introduction of healthy volunteers labeled radioactive drug containing etoricoxib at a dose of 25 mg, demonstrated that 70% of the drug is excreted through the kidneys, 20% through the intestine, mainly in the form of metabolites. Less than 2% was found unchanged. The 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 approximately 50 ml / min. Pharmacokinetics in special clinical situations Pharmacokinetic differences in men and women are absent. 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. Racial differences do not affect the pharmacokinetic parameters of etoricoxib. In patients with minor impaired liver function (5-6 points on the Child-Pugh scale), a single dose of etoricoxib at a dose of 60 mg / day 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. Data from clinical and pharmacokinetic studies in patients with severely impaired liver function (more than 9 points on the Child-Pugh scale) are missing. The pharmacokinetic indices of single use of Etoricoxib at a dose of 120 mg in patients with moderate and severe renal insufficiency and with end-stage chronic renal insufficiency (CRF) 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 have not been studied in children under 12 years of age. 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

Arcoxia is used for the symptomatic treatment of such diseases and conditions as: rheumatoid arthritis; acute gouty arthritis; ankylosing spondylitis; osteoarthritis. The drug is also prescribed after dental surgery for the treatment of severe acute and moderate pain. Contraindications Absolute: exacerbations of inflammatory bowel diseases (ulcerative colitis and Crohn's disease); severe renal failure (creatinine clearance less than 30 ml / min), confirmed hyperkalemia, progressive renal diseases; active gastrointestinal, cerebrovascular or other bleeding; erosive and ulcerative lesions of the mucous membrane of the duodenum or stomach; severe liver failure, liver disease in the active phase; persistently maintained high blood pressure with uncontrolled hypertension; bleeding disorders (including hemophilia); clinically significant ischemic heart disease, cerebrovascular diseases and diseases of the peripheral arteries, the period after CABG (coronary artery bypass grafting); severe heart failure; incomplete or complete combination of the following diseases (including history): recurrent polyposis of the nose or paranasal sinuses, bronchial asthma and intolerance to acetylsalicylic acid and other NSAIDs; children and adolescents up to 16 years; During pregnancy and breastfeeding; hypersensitivity to any of the components of the drug. Relative (Arcoxia used with caution): severe somatic diseases; history of the development of ulcerative lesions of the gastrointestinal tract and Helicobacter pylori infection; arterial hypertension; diabetes; swelling and fluid retention; dyslipidemia / hyperlipidemia; renal failure (with creatinine clearance less than 60 ml / min); smoking; frequent use of alcohol; elderly age; prolonged use of NSAIDs; concomitant therapy with antiplatelet agents, glucocorticosteroids, anticoagulants and selective serotonin reuptake inhibitors

Contraindications

A complete or incomplete combination of asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (includingin history); - erosive and ulcerative changes of the mucous membrane of the stomach or duodenum, 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 classification II-IV functional classes); - severe liver failure (more than 9 points on the Child-Pugh scale) or active liver disease; - renal failure severe (CC less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia; - the period after coronary artery bypass surgery; peripheral artery disease, cerebrovascular disease, clinically severe coronary artery disease; - persistently maintained blood pressure values ​​greater than 140/90 mm Hg. st. with uncontrolled arterial hypertension; - pregnancy, - lactation period (breastfeeding); - children's age up to 16 years; - Hypersensitivity to any component of the drug. 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).

Precautionary measures

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 relative to VGN, the drug should becanceled. Considering the increased risk of undesirable 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. You should not use the drug along with other NPVS. lactase deficiency. The effect on the ability to drive motor vehicles and control mechanisms. During the period of treatment it is necessary to Luda caution when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions. Patients with episodes of dizziness, drowsiness or weakness should refrain from activities that require concentration.

Use during 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 a pregnancy.
Dosage and administration
Arcoxia pills are intended for oral administration, regardless of the meal. The drug is washed down with a small amount of water. Recommended doses: rheumatoid arthritis and ankylosing spondylitis: 90 mg once a day (maximum daily dose is 90 mg); acute gouty arthritis: 120 mg once a day (maximum daily dose is 120 mg); osteoarthritis: 60 mg once a day (the maximum daily dose is 60 mg). With pain syndrome, the average therapeutic dose is 60 mg once. When using Arcoxia at a dose of 120 mg, the duration of treatment should be no more than 8 days. It is recommended to use the drug in the minimum effective dose of the shortest possible course. To eliminate acute pain after dental surgery, 90 mg of Etoricoxib is prescribed once a day for no more than 8 days (the maximum daily dose is 90 mg)

Side effects

The digestive system: often - nausea, dyspepsia, heartburn, epigastric pain, flatulence, diarrhea; infrequently - increased peristalsis, ulcers and dryness of the oral mucosa, gastritis,vomiting, belching, esophagitis, irritable bowel syndrome, bloating, constipation, duodenal ulcer or stomach ulcer; very rarely - hepatitis, gastrointestinal ulcers (sometimes with perforation or bleeding); respiratory system: infrequently - nosebleeds, shortness of breath, cough; very rarely - bronchospasm; cardiovascular system: often - increased blood pressure, heartbeat; infrequently - atrial fibrillation, non-specific changes in the electrocardiogram, congestive heart failure, myocardial infarction, cerebrovascular accident, hot flashes; very rarely - hypertensive crisis; nervous system and sense organs: often - weakness, headache and dizziness; infrequently - drowsiness, impaired sensitivity, including hyperesthesia / paresthesia, impaired concentration, anxiety, taste disturbance, depression, sleep disturbances, tinnitus, blurred vision, vertigo, conjunctivitis; very rarely - confusion and hallucinations; musculoskeletal system: infrequently - arthralgia, muscle cramps, myalgia; urinary system: infrequently - detection of protein in the urine; very rarely - renal failure, usually reversible after discontinuation of the drug; metabolism: often - fluid retention, edema; infrequently - weight gain, change in appetite; dermatological and allergic reactions: often - ecchymosis; infrequently - itchy skin, swelling of the face, rash; very rarely - anaphylactoid or anaphylactic reactions, Stevens-Johnson syndrome, urticaria, Lyell's syndrome; laboratory indicators: often - increased activity of liver enzymes; infrequently - decrease in hemoglobin and hematocrit, increased activity of creatine phosphokinase, increased nitrogen in urine and blood, leukopenia, increased uric acid, thrombocytopenia, hyperkalemia, increased serum creatinine; rarely, an increase in serum sodium concentration; infectious complications: infrequently - urinary tract infections and upper respiratory tract infections, gastroenteritis; other reactions: often - flu-like syndrome; infrequently - chest pain

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 doses of up to 150 mg / day for 21 days did not cause significant toxic effects. Symptoms: With an overdose of the drug may cause undesirable effects on the gastrointestinal tract, cardiovascular system and kidneys. Treatment: conduct symptomatic therapy. Etoricoxib is not excreted by hemodialysis, the drug has not been studied for peritoneal dialysis.

Interaction with other drugs

With simultaneous use of Arcoxia with warfarin or similar drugs at the beginning of therapy and with each change in the dosage regimen of the drug, indicators of prothrombin time and INR (international normalized ratio) should be monitored. When administered jointly with ACE inhibitors, the hypotensive effect of ACE inhibitors may be reduced. In cases of impaired renal function, such a combination may further aggravate the functional insufficiency of the kidneys. With the simultaneous use of Arcoxia with cyclosporine and tacrolimus increases the risk of nephrotoxicity of these drugs; with acetylsalicylic acid in low doses - may increase the frequency of ulcerative lesions of the gastrointestinal tract; with lithium preparations - an increase in plasma concentration of lithium may be observed; with methotrexate - toxicity of methotrexate is possible (especially when Arcoxia is used at a dose of 120 mg); with oral contraceptives (especially ethinyl estradiol) - increases the concentration of ethinyl estradiol; with digoxin - digoxin overdose is possible; rifampicin - reduced plasma concentration of Etoricoxib; with antacids and ketoconazole - no clinically significant interaction found

special instructions

During treatment with Arcoxia, regular monitoring of blood pressure is required, especially during the first two weeks. It is also systematically necessary to investigate indicators of renal and liver function. If the level of liver transaminase activity exceeds the upper limit of normal three times or more, the drug should be discontinued. With prolonged use of Etoricoxib, the need for further administration of the drug, as well as the possibility of dose reduction, is periodically assessed.Simultaneous reception with other NSAIDs is not recommended. The shell of the pills in a small amount contains lactose, which must be considered when prescribing Arcoxia to patients with lactase deficiency. During treatment, care must be taken when driving a car or other vehicles and engaging in other potentially dangerous activities. Patients who have developed side effects such as weakness, drowsiness, and dizziness should abandon classes associated with high concentration of attention.

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