The 40M Quaylox ARMEPHACO medicine treatment for chronic uric acid (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Febuxostat

Ingredient

Composition information	Content
Febuxostat	40mg

Uses

indications

Vairilox is used to treat chronic uric acid in case of urate deposits that have occurred (including cases with a history or currently being tophi and/or gout arthritis). The drug is only for adults.

Pharmacokic

Uric acid is the last product of purine metabolism in people with hypoxanthine cycle -> xanthine -> uric acid. Both steps above are catalyzed by Xanthine Oxidase (XO), Febuxostat is a 2-an4thiazole derivative that reduces uric acid in the blood due to selective inhibition. Febuxostat has the ability to inhibit both oxidation and reduction of enzymes.

In the treatment dose, Febuxostat has no effect on inhibiting the catalytic enzymes that metabolize the process of purine or pyrimidine metabolism such as guanine deaminase, hypoxanthine guanine phosphoribosyltransferase, OROTATE phosphoribosyltransferase, OROTIDINE monophosphate decarboxylase phosphorylase.

Dynamic pharmacokinetics

In healthy people, peak concentration (C) and the area under the curve (AUC) of Febuxostat increases proportional to the dosage when taking single and multi -dose from 10mg to 120 mg.

With the dose from 120mg to 300mg, AUC increases more than the dose. The drug is not significantly accumulated from 10mg to 240mg every 24 hours. Febuxostat waste sale time is about 5 to 8 hours.

absorption

Febuxostat absorbs fast (from 1.0 - 1.5 hours) and is good (at least 84%). After using single or oral doses from 80mg to 120mg/day, equivalent to 2.8 - 3.2 mg/ml and 5.0 - 5.3 mg/ml. Absolute bioavailability of Febuxostat tablets has not been studied. After drinking 80mg multiple doses, 1 time or single daily dose of 120mg with high -fat meals, CMAX decreased by 49% and 38%, respectively; AUC decreased by 18% and 16% respectively. However, there is no clinical change in uric acid levels (80 mg multi -dose). Therefore, Febuxostat can be taken before or after ǎn.

distribution

Calculate the number of stable status of Febuxostat ranges from 29 to 75L after taking the dose from 10 to 300 mg. Protein bond is about 99.2%, mainly with albumin, and stable in the dose range from 80 to 120mg. The metabolites have active cohesion with plasma proteins from 82% to 91%.

Biological metabolism

Febuxostat is metabolized mainly by binding with urrin diphosphate glucuronosyltransferase (UDPGT) and oxidized by the cytochrome P450 enzyme system (CYP). The four hydroxyl metabolites have biological activity, of which 3 substances are found in human plasma. In vitro studies with microenme people show that oxidized metabolites are formed mainly thanks to the enzymes CYP1A1, CYP1A2, CYP2C8 or CYP2C9 and Febuxostat Alicuronic weak due to UGT1A1, 1A8, and 1A9.

Elimination

Febuxostat is eliminated both through the kidneys and liver. After taking the dose of 80 mg, C-Febuxostat marks, about 49%of the dose found in the urine in the form of constant (3%), the form of febuxostat acyl glucuronide (30%), their known oxidant metabolites (13%), and unknown metabolites (3%). In addition to the renal excretion, about 45%of the dose is excreted through the non -variable form (12%), the form of febuxostat acyl glucuronide (1%), known oxidant metabolites, their types of links (25%), and unknown metabolites (7%).

Patients with renal failure

After taking multiple doses of Febuxostat 80 mg, high value, unchanged for patients with mild, medium or severe renal impairment compared to patients with normal kidney function. The total AUC average of Febuxostat increases about 1.8 times from 7.5mg.h/ml in people with normal kidney function to 13.2 mg.h/ml. In people with severe kidney failure CMAX and AUC of metabolites increased by 2 and 4 times. However, do not need to adjust the dose for patients with mild or medium renal failure.

Patients with liver failure

After giving patients with a mild or medium-sized liver (Child-Pugh Class A), Febuxostat 80mg, C and AUC of Febuxostat and its metabolites have not changed significantly compared to patients with normal liver function. There is no study with patients with severe liver failure (Childpugh class c).

Before taking The 40M Quaylox ARMEPHACO medicine treatment for chronic uric acid (3 blisters x 10 tablets)

How to use

oral medication. Can be taken with or not with food.

Dosage

The recommended dose of Febuxostat is 80 mg (1 tablet of Vaidilox 80 or 2 Vaidilox 40 tablets), once a day. The drug can be taken when hungry or full. If the concentration of uric acid in the blood> 6 mg/dl (357 µmol/l) after 2-4 weeks, it is possible to consider using 120 mg, once a day (3 vsidilox 40 tablets).

Patients need to be tested for uric acid levels in the blood after 2 weeks of treatment. The goal of treatment is to bring and maintain uric acid levels in the blood level below 6 mg/dL (357 mol/l).

For the elderly: No dose adjustment.

Patients with renal failure: Effective and safe treatment has not been established with patients with severe renal failure (clearing creatinine below 30 ml/minute). No dose adjustments for patients with mild or medium renal failure.

Patients with hepatic impairment: Effective and safe treatment of Febuxostat has not been studied in patients with severe liver (Child-Pugh Class C). For patients with mild liver failure, the recommended dose of Febuxostat is 80mg/day. There is not much information about the dosage for patients with average liver failure.

Children: Safe and effective treatment of Febuxostat with patients under 18 years old has not been established, there is no treatment for this group of patients.

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 using overdose?

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

The most common side effects

In 3 controlled randomized clinical studies that last from 6 to 12 months, the side effects listed below are related to drug use. The table below lists side effects over 1% in the drug and is at least 0.5% higher than the Placebo group:

Side effects Plassbo

Febuxostat (n = 757) daily dose 80 mg
(n = 1279) (n = 1277) joints 0% 1.1% 0.7% 0.7%
In addition, over 1% of patients suffer from dizziness when using Febuxostat but the rate is not higher than 0.5% higher than the group using Placbo.
Side effects are less common
The following side effects occur below 1% of patients using Febuxostat in phase 2 and 3 clinical studies with a dose from 40mg to 240mg below:

Blood and lymphatic system: Anemia, thrombocytopenia, hemorrhage, increased leukemia, enlarged spleen, reducing all bloody hemoglobin. Blurred. Abnormal sensation, gait disorders, symptoms like influenza, mass, pain, thirst. Blood, hyperglycemia, hyperlipidemia, hyperglyceride, hypokalemia, decrease/weight gain. Glassing the blood, tremor. Male. Itching, hemorrhage, skin color change/skin pigmentation, skin damage, abnormal smell, urticaria. Triglyceride increases, amylas increases, increased potassium, increased TSH, platelets decreases, hematocrit decreases, hemoglobin decreases, increased MCV, RBC decreases, increased creatinine, increased blood urea, increased bun/creatinine ratio, creatine phosphokinase (CPI) increase, increased phosphate alkaline alkaline increase, pSA increases Lymphocytes decreased, leukocytes increased/decreased, abnormal blood clots, increased LDL, long prothrombin time, positive urine with leukocytes and proteins.

Warnings

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

contraindicated

Vaidilox drugs contraindicated in the following cases:

There is a history of sensitivity to the ingredients of the drug.

Be cautious when using

cardiovascular disease: It is not recommended to use Febuxostat for patients with ischemia or congested heart disease.

Hypersensitivity allergies: A few reports recorded life -threatening allergy/hypersensitivity, including Stevens - Johnson syndrome, super -infected necrosis (Ten) and acute anaphylaxis shock. In most cases, these reactions occur in the first month of treatment with Febuxostat. Some of them suffer from renal failure and/or have a sensitive reaction to allurinol. Some cases of hypersensitivity accompanied by kidney or liver.

A warning of patients should be warned and symptoms and must be strictly controlled for symptoms of hypersensitivity reactions. Febuxostat must be discontinued as soon as possible if the allergy/hypersensitivity occurs, including Stevens - Johnson syndrome. Do not reuse Febuxostat for patients in the case of patients with hypersensitivity reactions.

Acute gout: Do not indicate treatment with Febuxostat until the gout is gone. Gout can occur during the starting process of Febuxostat due to changes in the blood uric acid levels in the blood, leading to tissue urate transfer. In at least the first 6 months of treatment with Febuxostat, carefully preventing gout with NSAI or Colchicine drugs.

Do not stop the drug if the acute gout occurs during Febuxostat treatment. The acute gout can be controlled by a appropriate measure for each patient. Continuing treatment with Febuxostat will reduce the frequency and level of acute gout.

Xanthine deposits: For patients where urate formation rate increases much (such as in malignant diseases and treatment processes, lesch-anyhan syndrome), the increased Xanthine concentration in urine can lead to xanthine deposits on urinary tract. Because there is no experience with Febuxostat, the use of drugs for this group of patients does not recommend.

mercaptopurinelazathopring: It is not recommended to use Febuxostat for patients who are being treated with mercaptopurine/azathioprine. In case of unavoidable treatment, it is necessary to monitor patients closely. Mercaptopurine or azathioprine should be reduced to avoid hematological reactions. For patients with organ transplantation: Because there is no experience in using the drug, it is not recommended to use Febuxostat for these patients.

Theophyllline: Be careful when using Febuxostat for patients who are being treated with theophyllline and theophyllline concentration to be monitored when starting with Febuxostat.

Liver damage: In clinical studies 3 combined, abnormalities in mild liver function test are recorded in patients using Febuxostat (5.0%). Patients should be tested for liver function before starting treatment with Febuxostat and periodically based on clinical evaluation.

Some reports during the circulation of the drug record the case of liver failure leading to death or not in patients using Febuxostat, although reports are not enough information to determine the cause.

In control clinical trials, increasing transaminase more than 3 times compared to the above limit recorded. Do not record the correlation between the dose and this transaminase increasing phenomenon.

Conduct liver function tests to make reference values before Febuxostat treatment (including ALT, AST, alkaline phosphatase and total bilirubin). For patients with signs of liver failure such as fatigue, appetite/appetite, discomfort in the upper right abdomen, dark urine or jaundice. If the results of abnormal liver function tests with these cases (ALT is 3 times higher than the above limit), it is necessary to stop treatment with Febuxostat to determine the cause. Febuxostat should not be appointed if not found for this liver abnormal abnormalities.

For patients who determine the cause of increased ALT and/or total bilirubin also need to be cautious when treated with Febuxostat.

Thyroid disorders: In open studies, some patients have TSH (> 5.5 IU/ml) when long -term treatment with Febuxostat (5.5%). Caution should be used when using Febuxostat for patients with thyroid function damage.

lactose: Because in the composition of the drug contains lactose, should not be used for patients with rare genetic disorders with Galactose intolerance, lapp-lactase deficiency or reducing glucose-galactose absorption.

The effect of the drug on the ability to drive and operate machinery

drowsiness, dizziness, severe and blurred vision have been reported when using Febuxostat.

Patients need to be cautious when driving, using machines or participating in dangerous activities unless they are sure that Febuxostat does not adversely affect their activities.

Use drugs for women during pregnancy and lactation

Pregnant women

Data obtained from a very few pregnant women who use drugs but does not cause unwanted effects to pregnancy or the health of the fetus/babies. Animal research does not record the harmful reactions of the drug directly or indirectly to the process of pregnancy, the development occurs with the unknown people.

Do not use fobuxostat for pregnant women, and milk or not. Animal research shows that the drug is excreted in milk and the slow development of mice.

breastfeeding women

It is not known whether Febuxostat is excreted. Animal research shows that the drug is excreted through breastfeeding. The risk of slowing the development of breastfed babies is not excluded. Do not use fobuxostat nursing gas.

Interactive drug

mercaptopurinelazathopring

With the Febuxostat inhibiting effect, simultaneous use of the above drugs with Febuxostat is not recommended. Using with Febuxostat can increase the blood concentration of the above drugs leading to poisoning.

Research on drug interactions ofFuxostat with drugs metabolized by XO has not been done.

There are currently no studies on drug interaction between Febuxostat and cytotoxic chemotherapy as well as no data on the safety of Febuxostat in patients being chemotherapy

Theophylline

Although drug interactive studies with Febuxostat have not been conducted, the inhibition of Xo can increase theophyllline concentration in the blood (the metabolism of theophylline is inhibited when used simultaneously with other XO inhibitors). Therefore, it is necessary to be cautious when using the above drugs and theophylline concentration should be monitored when starting treatment with Febuxostat.

Naproxen and glucuronide metabolic inhibitors. Febuxostat elimination depends on the enzyme Uridine Glucuronosyl Transferase (UGT). Glucuronide metabolism inhibitors, such as NSAID and Probenecid, in theory, can affect the metabolism of Febuxostat.

In healthy people, when using simultaneously Febuxost and Naproxen 250mg, 2 times/day increase the concentration of febuxostat in the blood (CMAX 28%, AUC 41%and 26%TMAX). In clinical studies, simultaneous use with Naproxen or other NSAI drugs or COX-2 inhibitors do not increase the side effects of significant clinical significance. Febuxostat can be used simultaneously with Naproxen without adjusting the dose of both drugs.

Glucuronide metabolism stimulants

The drugs that stimulate the enzyme UGT can lead to metabolic increase and reduce the effects of febuxostat. Therefore, it is necessary to monitor uric acid levels in the blood for 1 to 2 weeks after use simultaneously with glucuronide metabolism. In contrast, the discontinuation of treatment with glucuronide metabolism can lead to increased febuxostat levels in the blood.

colchicine/indometacin/hydrochlorothiazide/warfarin

Febuxostat can be indicated simultaneously with Colchicine or Indomethacin without adjusting the dose of both drugs.

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

No need to adjust the dose of warfarin when indicated to be simultaneously used with fobuxostat. The simultaneous use of Tobuxostat (dose of 80 mg or 120 mg, once a day) with warfarin does not affect the pharmacokinetics of warfarin in healthy people, INR and the operation of the VII factor are not affected by the use of Tobuxostat.

desipramine/substrate of the enzyme CYP2D6

On In vitro, Tobuxostat inhibits weak enzyme CYP206. In a healthy clinical study, taking a dose of 120 mg once a day, it increases an average of 22% of the AUC value of the desipramine, a substrate of the CYP2D6 enzyme, showing the mild inhibitor of Tobuxostat's CYP206 enzyme enzyme on in vitro. Therefore, simultaneous use of Febuxostat with drugs is the substrate of the enzyme CYP2D6 does not need to adjust the dose of these drugs.

antacids

Concentrated with antacids containing magnesium hydroxide and aluminum hydroxide slow down the absorption of Febuxostat (nearly 1 hour) and reduced CMAX 32% but does not significantly affect the AUC value. Therefore, the use of Febuxostat may not need to care about the use of antibiotic drugs.

Storage

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

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