Arcoxia 90mg MSD treatment of osteoarthritis, rheumatoid arthritis (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Etoricoxib
Ingredient Gout, dysmenorrhea, osteoarthritis, joint spondylitis, rheumatoid arthritis

Ingredient

Composition information	Content
Etoricoxib	90mg

Uses

Indications

Arcoxia 90mg is indicated:

Acute and chronic treatment of signs and symptoms of osteoarthritis (Osteoarthritis-OA) and rheumatoid arthritis (Rheumatoid Arthritis-Ra). Arthritis).

Acute and chronic analgesic.

Pharmacokological

Arcoxia is an nonsteroidal anti -inflammatory drug (NSAID) with anti -inflammatory, analgesic, and fever -reducing activity in animal models. Arcoxia is a strong, very selective Cycloxygenase-2 (COX-2) inhibitor, which is active when taken within the scope and is higher than the clinical dose range. Cycloxygenase has been identified: Cycloxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Cox-1 is responsible for normal physiological functions through prostaglandin intermediaries such as protecting the gastric mucosa and platelet aggregation. Cox-1 inhibition due to non-selective NSAIDs is often accompanied by stomach damage and platelet inhibition. The COX-2 has been shown in the synthesis of the intermediate substances of prostanoic acid that causes pain, inflammation and fever. The selective inhibition of COX-2 due to the use of Etoricoxib has reduced these clinical signs and symptoms along with reducing toxicity in the digestive tract without having the effect of platelet function.

In all clinical pharmaceutical studies, Arcoxia has the effect of inhibiting COX-2 depending on the dose of use without inhibiting COX-1 when using the dose up to 150mg daily.

The effect of protecting the gastric mucosa of COX-1 is also assessed in a clinical study with gastric biopsy samples collected from the object or Arcoxia 120mg daily, or Naproxen 500mg twice a day, or Placebo to assess the aggregate prostaglandin. Compared to Placebo, Arcoxia does not inhibit prostaglandin synthesis in the stomach. In contrast, Naproxen inhibits the synthesis of prostaglandin in the stomach up to nearly 80% when compared to Placebo. This data proves the selection of Cox-2 of Arcoxia.

Platelet function

Bleeding time is not affected when using Arcoxia multiple doses of up to 150mg daily for 9 days compared to Placebo. Similarly, bleeding time is not changed in a single dose study with Arcoxia 250 or 500mg. In experimental cells living outside the body (EX Vivo), there is no inhibition of arachidonic acid or platelet aggregation due to collagen induction in a stable state with ARCOXIA doses to 150mg. These findings are consistent with the selection of Etoricoxib for COX-2.

pharmacokinetic

absorption

Etoricoxib is well absorbed by oral. The oral average is nearly 100%oral. After taking the dose of 120mg once a day until the state is stable, the peak concentration in plasma (average cmax cmax = 3.6mcg/ml) is recorded nearly 1 hour (TMAX) after adults take the drug when hungry. Average AC0 - 24 hours is 37.8mcg/hour/ml.

Dynamic pharmacokinetics of linear Etoricoxib with clinical dose range.

Normal meals have no clinical significance to the level or absorption rate of 1 dose of Etoricoxib 120mg. In clinical trials, Etoricoxib is used not related to food.

Etoricoxib's pharmacokinetics in 12 healthy subjects are the same (equivalent to AUC, CMAX within a difference of 20%) when taking alone, when used with antacids containing magnesium/aluminum hydroxide, or antacidic drugs containing calcium carbonate (the ability to neutralize acid approximately 50MEQ).

Distribution

About 92% of the dose of Etoricoxib attached to protein in human plasma when used within the concentration of 0.05 - 5mcg/ml. The distribution voltage in a sustainable state (VDSS) is about 120L in humans. Etoricoxib passes through the placenta in rats and rabbits, and goes through the blood -brain barrier in the rat.

Metabolism

Etoricoxib is strongly metabolized with

There have been 5 metabolites identified in humans. The metabolic substance is mainly derivatives of 6’-carboxylic acids of Etoricoxib, formed from oxidation of 6’-hydroxymethyl derivative. These main metabolites manifest or have no active measurable or only active as COX-2 inhibitors. These metabolites do not inhibit COX-1.

Elimination

After an intravenous injection of a single -dose of 25mg Etoricoxib has radioactive attachment to healthy objects, 70% of radioactive active ingredients are found in urine and 20% in feces, mostly in the form of metabolites. Under 2% of radioactive active ingredients found in non -metabolic drugs.

Most Etoricoxib is excreted mainly through metabolism, then through the excretion in the kidneys. Etoricoxib's concentration in a sustainable state is achieved within 7 days of treatment when taking a dose of 120mg once a day, with an accumulated score of nearly 2, corresponding to the accumulated waste duration of about 22 hours. According to estimates, the removal of drugs in plasma is approximately 50ml/min.

Characteristics in patients (special population)

Sex: Etoricoxib's pharmacokinetics in men and women are the same. Pharmacokinetics in the elderly (> = 65 years) are similar to young people. No dose adjustment in elderly patients.

Race: Race does not create an important effect on the pharmacokinetics of Etoricoxib.

Hepatic failure: In patients with mild liver failure (Child-Pugh 5-6 score), Etoricoxib dose 60mg once a day with an average AUC higher than 16% higher than healthy objects using the same dose mode. Patients with average liver failure (Child-Pugh 7-9 score) using Etoricoxib dose 60mg every 2 days already have average AUC similar to the healthy object using Etoricoxib 60mg once a day, the dose of Etoricoxib 30mg has not been studied once a day in this population. There is no clinical document or pharmacokinetics when taking drugs in patients with severe liver failure (Child-Pugh> 9).

Kidney failure: Etoricoxib pharmacokinetics of a single dose of 120mg in patients with medium - severe renal impairment and patients with end -stage renal disease are undergoing hemolysis is not significant compared to dynamic pharmacokinetics in healthy subjects. Hematoparoology does not contribute significantly to the elimination of drugs (the clearance of drugs through the appraisal of about 50ml/minute).

Children's patients: Etoricoxib's pharmacokinetics in children ( 60kg using Etoricoxib 90mg once a day, it is like a dynamic pharmacology in adults using Etoricoxib 90mg once daily. Etoricoxib's safety and effectiveness has not been established in children's patients.

Before taking Arcoxia 90mg MSD treatment of osteoarthritis, rheumatoid arthritis (3 blisters x 10 tablets)

How to use

Arcoxia is used by oral, can be used or not with food.

arcoxia should be used in the shortest possible time and with the lowest daily dose that is effective.

Dosage

osteoarthritis

The recommended dose for adults is 30mg or 60mg once a day.

rheumatoid arthritis

The recommended dose for adults is 90mg every day.

Jerematitis

The recommended dose for adults is 90mg every day.

acute phong arthritis

The recommended dose for adults is 120mg once a day. ARCOXIA 120mg should only be used in acute symptoms, with a maximum treatment time of 8 days.

Acute pain and abnormal dysmenorrhea

The recommended dose is 120mg once a day. ARCOXIA 120mg should only be used in acute symptoms, with a maximum treatment time of 8 days.

Pain after dental surgery

The recommended dose is 90mg once a day, maximum use for 3 days, some patients may need additional painkillers.

Doses higher than the recommended dose for each of the above indications still do not increase the effectiveness of the drug or have not been studied.

Therefore:

Dosage in osteoarthritis does not exceed 60mg per day.

Dosage in rheumatoid arthritis does not exceed 90mg daily.

Dosage in joint vertebrae should not exceed 90mg per day.

Dosage in acute leprosy disease must not exceed 120mg once a day.

Dosage in acute pain and abolished dysmenorrhea must not exceed 120mg/day.

Dosage in pain after dental surgery must not exceed 90mg daily.

Because cardiovascular risks may increase according to the dose and time of using COX-2 selective inhibitors, therefore should take the drug in the shortest time as possible and use the lowest daily dosage. It is advisable to re -evaluate the demand for symptoms and response to patients (see caution).

Elderly, gender, race: No need to adjust the ARCOXIA dose in the elderly or based on gender or race.

liver failure

In patients with mild liver failure (Child-Pugh 5-6 score), the dose should not exceed 60mg once a day. In patients with average liver failure (Child-Pugh score 7-9), the dose should be reduced, should not exceed the dose of 60mg 2 days once a day, can also consider the dose of 30mg once a day. There is no clinical document or pharmacokinetics when taking drugs in patients with severe liver failure (Child-Pugh score> 9) (see caution)

kidney failure

Do not recommend treatment for arcoxia in patients with progressive renal disease (creatinine clearance ratio

What to do when overdose? There have been reports on the use of acute Etoricoxib, but there is no report on adverse effects that occur in most cases of overdose. The most common adverse effects recorded in accordance with the safety characteristics of Etoricoxib (such as the effects on the gastrointestinal tract, on the kidney blood vessels).

In case of an overdose, reasonable is that it is advisable to apply commonly used support measures, such as removing substances that have not been absorbed from the digestive tract, clinical monitoring and supportive treatment, if necessary.

cannot eliminate Etoricoxib by hemolysis; It is not known whether it is possible to use peritoneal fertilizer to remove Etoricoxib.

What to do when forgetting a dose? However, if it is almost time for the next dose, it is advisable to skip the forgotten dose. Take care not to use double the prescribed dose.

Side Effects

In the application, the following negative impact:

Neurological: headache, dizziness, weakness and indifference, dazzling. Sometimes the tinnitus manifests. Can develop anxiety, depression, reduce attention. Rarely see the appearance of hallucinations or confusion. The amount of platelet. Abdominal pain, increased concentration of transaminase, constipation, dry mouth, taste change, gastritis (gastritis, esophagitis, stomach, hepatitis), formation of gastrointestinal ulcers, development of irritable bowel syndrome, the appearance of ulcers on the mucosa. corn. Weighing, hyper urea, azoturia, increased creatinine, potassium and sodium in the blood, hyperuricemia.

Warnings

Contraindicated

Contraindicated use of Arcoxia in patients:

sensitive to any ingredient of the drug. History of asthma, urticaria or allergic reactions after taking aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs). The brain has been identified (including new patients undergoing coronary artery or blood vessel shaping surgery). Using Arcoxia as a combined therapy with other nonsteroidal anti -inflammatory drugs (NSAID) because there is no sufficient evidence to prove benefits and adverse side effects may encounter.

Precautions when used

Some clinical trials from the drug show that the COX - 2 inhibitors in the composition of Arcoxia 90mg may increase the risk of thrombotic events. Therefore, it is necessary to take the drug in a short time and take the dose in accordance with the doctor's instructions because if you arbitrarily increase the dose can cause high cardiovascular risk.

Patients with diseases of blood pressure, diabetes should be careful to use Arcoxia 90mg.

COX-2 selective inhibitors are not aspirin replacement in cardiovascular disease because it does not work on platelets.

When used to increase the dose of Arcoxia 90mg can cause stomach diseases such as stomach ulcers.

It is not recommended to use Arcoxia therapy for patients with severe renal disease.

If users show signs of dehydration, they need to be supplemented with the amount of water needed before using Arcoxia 90mg.

When using Etoricoxib in the elderly and in patients with kidney, liver or heart dysfunction, it is necessary to maintain the appropriate medical care regime.

The ability to drive and operate machinery

There is no information that suggests Arcoxia affects the ability to drive or operate the machine when the patient is taking the drug.

Pregnant women

like other drugs that inhibit the synthesis of prostaglandin, should avoid using Arcoxia in the last months of pregnancy because it can cause early closing artery. It is recommended to only use Arcoxia 90mg in the first two quarters of pregnancy when the potential benefits are better than the risk that may occur for the fetus.

breastfeeding women

There has been no report on the Arcoxia 90mg medicine that affects the breast milk gland, so the mother who wants to use the drug needs to consult with drug consultants.

Medicinal interaction

Warfarin: In stable objects with chronic Warfarin therapy, Arcoxia 120mg regimen per day is often associated with an increase of about 13% of the international standard chemical ratio in prothrombin time (International Normalized Ratio-inr). It is recommended to regularly check the Inr values when starting or changing treatment with Arcoxia, especially in the first few days in patients using warfarin or similar drugs.

Rifampin: Use Arcoxia at the same time as rifampin, a strong induction substance that metabolism through the liver has reduced 65% of the area under the curve (AUC) to represent Etoricoxib concentration in plasma. This interaction should be taken into account when using Arcoxia at the same time as Rifampin.

Methotrexate: There are 2 research tests of Arcoxia effects 60, 90 or 120mg once a day in 7 days in patients taking methotrexate dose of 7.5 - 20mg once a week to treat rheumatoid arthritis. Arcoxia dose 60 and 90mg does not affect methotrexate concentration in plasma (evaluated through AUC) or the removal of drugs through the kidneys. In a test, Arcoxia 120mg does not affect the concentration of methotrexate in plasma (evaluated through AUC) or the removal of drugs through the kidney. In the remaining test, Arcoxia 120mg increases methotrexate levels in plasma by 28% (evaluated through AUC) and reduces the clearance of methotrexate through the kidney by 13%. Methotrexate toxicity should be monitored when using Arcoxia higher than 90mg daily and methotrexate therapy at the same time.

Diuretics, Angiotensin (ACE) and Angiotensin II (AIIAS): NSAIDs suggested reports include COX-2-selective inhibitors that can reduce the treatment of hypertension of diuretics, ACE inhibitors and Angiotensin II antagonists. This interaction should be paid to using Arcoxia at the same time as these drugs. In some patients with reduced renal function (such as elderly patients or patients with loss of circulatory fluid, including patients using diuretic therapy) are taking nonsteroidal anti-inflammatory drugs, including COX-2 selective inhibitors, simultaneous use of ACE inhibitors or Angiotensin II antagonists can worse renal function worse, including acute renal insufficiency. These effects can often be recovered. Therefore, be careful when combining drugs, especially in the elderly.

Lithium: The non-selective NSAIDs suggesting reports and selective inhibitors can increase lithium concentration in plasma. This interaction should be taken into account for patients to use Arcoxia at the same time as Lithium.

Aspirin: Arcoxia can be used at the same time as low -dose aspirin to prevent cardiovascular disease. In sustainable state, Etoricoxib 120mg once a day does not affect the activity of platelet resistance of low -dose aspirin (81mg once a day). However, using low -dose Aspirin simultaneously with Arcoxia increases the rate of gastrointestinal ulcers or other complications compared to the use of single -treatment Arcoxia (see caution at the time of use).

contraceptive pill: Arcoxia 60mg is used at the same time as a 35mcg ethinyl estradiol and 0.5 - 1mg norethindrone in 21 days, increasing the AUC0-24 hours of Ethinyl estradiol in a stable state of up to 37%. The AUC0-24 hours of Ethinyl estradiol in a sustainable state has increased by 50-60% when Arcoxia 120mg is used at the same time or 12 hours from this type of contraceptive pill. It is necessary to take into account the increase in Ethinyl estradiol level when choosing a contraceptive pill with Etoricoxib. Increasing exposure to Ethinyl estradiol may increase the proportion of adverse effects that are often associated with using contraceptives (such as venous thrombosis in risky women).

Hormone replacement therapy: Arcoxia 120mg is used with hormone replacement therapy containing conjugated estrogen (0.625mg premarin tm) for 28 days, increasing the average AUC0-24 hours in the sustainable state of non-conjunctiva (41%), Equilin (76%), and 17-A-Eleriol (22%). The impact of the recommended doses of Arcoxia (30, 60, and 90mg) has not been researched. The impact of Arcoxia 120mg on concentration (AUC 0-24 hours) these estrogen components in premarin is half less than the observed effect when using a single premarin and when the dose increases from 0.625 to 1.25mg. It is still unknown to the clinical significance of these increase and there is no research on the higher dosage premarintm coordination regimen with Arcoxia. It should be taken into account the concentration of estrogen when choosing to replace postmenopausal hormones to use with Arcoxia.

Other drugs: In studies on drug interaction, Arcoxia does not have clinically important effects on pharmacokinetic pharmacokinetics of prednisone/prednisolone or digoxin.

antacids and ketoconazole (1 strong CYP3A4 inhibitor) does not have important effects on Arcoxia clinical pharmacokinetics.

Storage

Leave a cool place, avoid light, temperature below 30⁰C.

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