Opedulox 40 OPV treat chronic uric acid hypertrophy (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Febuxostat

Ingredient

Composition information	Content
Febuxostat	40mg

Uses

indications

Opedulox 40 drugs are indicated in the following cases:

Treatment of chronic uric acid in adults has occurred urate deposition (including people with a history or being urate and/or gout arthritis).

Pharmacological

Febuxostat is a gout treatment, uric acid production inhibitors.

In humans, uric acid is the final product of the purin metabolism and is created in step by step hypoxanthin → xanthin → uric acid. Both metabolic steps are catalyzed by xanthin oxidase. Febuxostat is a derivative of 2 - Arylthiazol, its treatment effect is to reduce serum uric acid by inhibiting Xanthin oxidase selection. At the treatment concentration, Febuxostat does not inhibit enzymes involved in the metabolism of purin or pyrimidine, namely guanin deaminase, hypoxanthin guanin phosphoribosyltransferase, OROTATIATH phosphoribosyltransferase, OROTIDIIN MONOMHOSPHAT DECOMOXYLASE phosphorylase.

Pharmacokinetics

absorption

After drinking, Febuxostat is well absorbed and fast. Peak concentration in plasma is about 2.8 - 3.2 µg/ml and 5.0 - 5.3 µg/ml after taking the dose of 80 mg and 120 mg once/day respectively. Time to reach peak concentration in plasma 1.0 - 1.5 hours. Febuxostat can be taken without caring for food.

Distribution

The distribution volume in the stable state of Febuxostat is about 29 - 75 liters after taking the dose of 10 - 300 mg. Febuxostat ratio is linked to plasma proteins about 99.2% (mainly albumin). The ratio of metabolites with active activity associated with plasma protein is about 82% to 91%.

Metabolism

Febuxostat is expanded by conjugated through the uridin diphosphate glucuronosyltransferase (UGT) and oxidation through the Cytochrom P450 (CYP). In human liver microscopy, In vitro studies show that oxidative metabolites are formed mainly by CYP1A1, CYP1A2, CYP208 or CYP2C9 and Glucuronic Febuxostat formed mainly by UGT 1A1, 1A8, and 1A9.

Elimination

Febuxostat is eliminated through the liver and kidneys. When taking the dose of Febuxostat 80 mg, about 49%of the dose is found in urine in the form of Febuxostat (3%), Acyl Glucuronic Febuxostat (30%), oxidative and combined metabolites (13%), other unknown metabolites (3%). In addition to the excretion of urine, about 45%of the dose is found in the form of Febuxostat (12%), Acyl Glucuronic Febuxostat (1%), oxidative and conjugated substances (25%), other unknown metabolites (7%). The final half -life of Febuxostat is about 5 - 8 hours.

Patients with renal failure

After taking multiple doses of 80 mg Febuxostat in patients with mild, medium or severe renal failure, Febuxostat's CMAX does not change compared to those with normal renal function. The average total AUC of Febuxostat increased by about 1.8 times from 7.5 µg. Element/ml in the group with normal kidney function to 13.2 µg. Annes/ml in the group with severe kidney dysfunction. CMAX and AUC of metabolic substances have increased activity to 2 to 4 times. However, it is not necessary to adjust the dose for patients with mild or medium renal failure.

Patients with liver failure

After taking multiple doses of 80 mg of Febuxostat in patients with mild liver impairment (Child - Pugh group A) or average (Child - PUGH group B), CMAX and AUC of Febuxostat and its metabolites do not change clearly compared to people with normal liver function. There is no study conducted in patients with severe liver failure (Child - Pugh Group C).

Age

Do not observe clear changes on the AUC of Febuxostat or its metabolites after taking multiple Febuxostat doses in older people than healthier people.

Gender

After taking multiple doses of Febuxostat, CMAX and AUC, 24% and 12% are higher than women. However, CMAX and AUC in the same volume in men and women. No need dose by gender.

Before taking Opedulox 40 OPV treat chronic uric acid hypertrophy (3 blisters x 10 tablets)

How to use

Take oral use. The drug can be taken or not with food.

Dosage

Adults

80 mg/1 time/day. The dose of 120 mg/day may be used if the concentration of serum uric acid is> 6 mg/dl (357 umol/l) after 2-4 weeks of treatment.

Elderly

No dose adjustment.

Patients with renal failure

Efficiency and safety have not been fully evaluated in patients with severe renal impairment (creatinine clearance

Patients with liver failure

Effective and safety has not been studied in patients with severe liver failure. The recommended dose in patients with mild liver failure is 80 mg. There is no information in patients with average liver failure.

Children

Safety and effectiveness of Opedulox 40 drug in children under 18 have not been determined. There is no information.

If you stop using Opedulox 40

Do not stop taking Opedulox 40 without a doctor's opinion, even if you feel better. If you stop taking the medication, the level of uric acid may begin to increase and the symptoms may be worse by forming new urate crystals in and around your joints and kidneys. If you have any other questions about using this medication, ask your doctor or pharmacist.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose?

What to do when you forget a dose? If the time is near the next dose, skip the forgotten dose and use the next dose to the normal plan. Do not double the dose to compensate for the forgotten dose.

Side Effects

When using Opedulox 40, you may experience unwanted effects (ADR).

Common, 1/100

Nutrition and metabolic disorders: Acute gout.

Nervous system disorders: headache.

Gastrointestinal disorders: diarrhea, nausea.

Liver disorders: abnormalities of liver function.

Skin and subcutaneous tissue disorders: rash.

Systemic disorders: edema.

Uncommon: 1/1000

Endocrine disorders: Increased thyroid stimulating hormones.

Nutrition and metabolic disorders: diabetes, hyperlipidemia, appetite, weight gain.

Mental disorders: Reducing sexual ability, insomnia.

Nervous system disorders: dizziness, abnormalities, hemiplegia, chicken sleep, change taste, reduce tactile, reduce sense of smell.

News disorders: Atrial fibrillation, brushing chest drum, abnormal electrocardiogram.

Pleeing disorders: Hypertension, flushing, hot.

Respiratory disorders: Difficulty breathing, bronchitis, upper respiratory infections, cough.

Gastrointestinal disorders: abdominal pain, abdominal distention, gastroesophageal reflux, vomiting, dry mouth, indigestion, constipation, frequent defecation, flatulence.

Liver disorders: gallstones.

Skin and subcutaneous tissue disorders: dermatitis, urticaria, itching, skin color change, skin damage, hemorrhagic spots, rash.

musculoskeletal disorders and connective tissue: joint pain, arthritis, muscle pain, musculoskeletal pain, muscle weakness, muscle spasm, muscle tension, epidemic inflammation.

Spirit and urinary disorders: kidney failure, kidney stones, bleeding, burning, proteinuria.

Reproductive disorders: erection dysfunction.

Systemic disorders: fatigue, chest pain, uncomfortable chest.

Rare: 1/10000

Blood disorders and lymphatic systems: Reducing all bloody, platelets.

Immune system disorders: Anaphylactic reaction, hypersensitivity to the drug.

visual disorders: blurred vision.

Nutrition and metabolic disorders: Losing weight, increasing appetite, anorexia.

Mental disorders: agitation.

Disorders of mesmerizing and ears: Tinnitus.

Digestive disorders: Pancreatitis, mouth ulcers.

Hepatitis: hepatitis, jaundice, liver damage.

Skin and subcutaneous tissue disorders: toxic skin necrosis syndrome, Stevens - Johnson syndrome, angioedema, erythema, rash, hair loss, increased sweating.

musculoskeletal disorders and connective tissue: muscle pattern, stiffness, musculoskeletal stiffness.

Magic and urinary disorders: Kidney inflammation, urine.

Systemic disorders: thirst.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Opedulox 40 contraindicated drug in the following cases:

Hypersensitivity to Febuxostat or any ingredients of the drug.

Be cautious when using

cardiovascular disorders: It is not recommended to use Febuxostat in patients with myocardial anemia or congestive heart failure.

Rarely reports on serious hypersensitivity reactions, including Stevens - Johnson's life -threatening syndrome, toxic skin necrosis syndrome and acute anaphylactic shock. Patients need advice on signs, symptoms and closely monitor the symptoms of hypersensitivity reactions. Do not reuse drugs in patients who are sensitive to the drug.

Do not start treatment with Febuxostat until acute gout attacks have completely decreased. Acute gout may occur at the beginning of treatment with Febuxostat. Continue treatment with Febuxostat if acute gout attacks occur during treatment.

Do not use Febuxostat in patients with malignant diseases and the treatment of malignant diseases, patients with Lesch - Nyhan syndrome.

The person who has been transplanted with the organ: is not recommended to use Febuxostat in this patient.

Theophylin: Febuxostat 80 mg can be used simultaneously with theophylin without the risk of increasing plasma concentration. There is no information for Febuxostat 120 mg.

Liver dysfunction: Check and periodically evaluate liver function when starting treatment with Febuxostat.

Thyroid disorders: Be cautious when using Febuxostat in patients with changes in thyroid function.

This drug contains lactose. Patients with rare Galactose Genetics problems, Lapp Lactase or Glucose - Galactose should not use this drug.

The ability to drive and operate machinery

Sleeping, dizzy, abnormal, blurred vision has been reported when using Febuxostat. Patients should be cautious before driving, operating machinery or participating in dangerous activities.

Pregnancy

The above data is very limited to pregnant women who have used drugs that have not identified any harmful effects of febuxostat in pregnant women or on the health of the fetus/newborn. Animal studies do not identify direct or indirect effects on pregnancy, fetal development or birth. The risk of potential for people. Febuxostat should not be used during pregnancy.

Breastfeeding period

In humans, it is not known whether Febuxostat will excrete through breast milk or not. Animal studies have shown the excretion of this active ingredient in breast milk and the development of a breast -feeding mouse. It is impossible to rule out the risk for infants who are breastfeeding. Febuxostat should not be used while breastfeeding.

Drug interaction

mercaptopurin/azathioprin

Based on the mechanism of the effect of Febuxostat on the inhibition of xanthin oxydase, the simultaneous use of these drugs with Febuxostat is not recommended. The inhibition of xanthin oxydase by Febuxostat may increase the concentration of these drugs in plasma leading to poisoning. Febuxostat interactive studies with drugs metabolized by xanthin oxydase have not been done. Interactive studies of Febuxostat with cytotoxic chemotherapy have not been conducted. There is no data on the safety of Febuxostat in cytotoxic therapy.

Rosiglitazon/substrate of CYP208

Febuxostat is shown to be a weak inhibitor CYP2C8 in vitro. In a study on healthy people, the simultaneous use of 120 mg of Febuxostat once a day with a single dose of 4 mg of Rosiglitazon is not influential on the pharmacokinetics of Rosiglitazon and N - Desmethyl Rosiglitazon metabolites, pointing out that Febuxostat does not inhibit CYP2C8C8 In Vivo. Therefore, it is not required to reduce the dose of Rosiglitazon or other substrates of CYP2C8 when using Febuxostat simultaneously with these substances.

Theophylin

A study of interaction on healthy people has been conducted with Febuxostat to evaluate the inhibition of Xanthin Oxidase (XO) that can increase theophylin level within circulation as reported with other 10 inhibitors. The research results show that Febuxostat 80 mg once daily use with a single doses of 400 mg single dose does not affect the pharmacokinetics or the safety of theophylin. Therefore, there is no special caution when using simultaneously Febuxostat 80 mg and theophylin.

Naproxen and other glucuronic inhibitors

The metabolism of Febuxostat depends on the enzymes of Uidin Glucuronosyl Transferase (UGT). The drugs inhibit glucuronicization, such as NSAID and Probenecids, in theory, can affect Febuxostat excretion. On healthy people, simultaneous use of Febuxostat and Naproxen 250 mg twice a day related to increased contact with Febuxostat (CMAX 28%, AUC 41%and T2 26%). In clinical studies, the use of Naproxen or NSAIDs/other COX -2 inhibitors is not related to any clinical increase of side effects.

Can be used simultaneously Febuxostat with Naproxen without adjusting the dose of Febuxostat or Naproxen.

Glucuronic sensor induction

Strong enzyme -glucuronosyl transferase enzyme enzyme can lead to metabolic increase and reduce the effectiveness of Febuxostat. Check serum uric acid after 1-2 weeks when starting treatment with strong induction substance glucuronicization. In contrast, stop treatment with glucuronicization can lead to increased plasma concentrations of febuxostat.

Colchicin/indometacin/hydrochlorothiazide/warfarin

Can be used simultaneously Febuxostat with Colchicin or Indomethacin without adjusting the dose of Febuxostat or active ingredients simultaneously.

No need to adjust the dose of Febuxostat when used with hydrochlorothiazid.

No need to adjust the Warfarin dose when used with Febuxostat. Use Febuxostat (80 mg or 120 mg once daily) with warfarin that does not affect the dynamics of warfarin in healthy people. Inr and the activity of factor VII are not affected when used in combination with Febuxostat.

Desipramin/substrates of CYP2D6

Febuxostat is a weak inhibitor CYP2D6 in vitro. In a study on healthy people, 120 mg Febuxostat once a day increases the average 22% AUC of Desipramin, a substrate of CYP2D6, showing the weak inhibition of Febuxostat on the CYP2D6 in vivo enzyme. Therefore, do not require adjusting the dose of other substrates of CYP2D6 when used in combination with Febuxostat with these substances.

antacids

Used in combination with an antacids containing magnesium and aluminum hydroxyd shows slowly absorbing Febuxostat (about 1 hour) and reducing 32% CMAX, but there is no significant change in AUC. Therefore, Febuxostat can be taken without caring about antacids.

Storage

At temperatures below 30 ° C, in a dry place, avoiding light.

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