Feburic 80mg Astellas treat chronic hyperuricemia (3 blisters x 10 tablets)

Dosage form Box of 3 blisters x 10 tablets
Specifications Febuxostat

Ingredient

Composition information	Content
Febuxostat	80mg

Uses

Indications

Treatment of chronic hyperuricemia hyperuricemia in conditions of urate deposition (including a history or currently urate and/or arthritis in gout).

Feburic is indicated in adults.

Pharmacology

Group of Pharmacological Therapy: Preparations for gout treatment, inhibited preparation of uric acid production.

Mechanism of action:

Uric acid is the final product of human purin metabolism and is formed in uric hypoxanthin acid hypoxanthin acid. Both steps in the above shift are catalyzed by xanthin oxidase (XO).

Febuxostat is a 2 -year -old derivative - Arylthiazol achieves the therapeutic effect that reduces serum uric acid levels by inhibiting Xanthin oxidase selection. Febuxostat is a selective inhibitor Xanthin Oxidase without purin (NP - Sixo) with a value of inhibitors in vitro inhibitors under 1 nanomol.

Febuxostat has been shown to be strongly inhibited both oxidation and reducing form of xanthin oxidase, at treatment concentration, Febuxostat does not inhibit other enzymes involved in the metabolism of purin or pyrimidine, ie guanin deaminase, hypoxanthin guanin phosphoribosyltransferase, orotate Phosphoribosyltransferase, OROTIDIN monophosphate decarboxylase or purin nucleosid phosphorylase.

Clinical efficiency and safety:

The effect of Febuxostat has been shown in 3 key phase 3 studies (2 key APEX and Fact and additional Confirms studies described below) which have been conducted in 4101 patients with hyperuricemia and gout.

In every key phase 3 study, Febuxostat has shown the ability to dominate and maintain serum uric acid levels compared to allopurinol. The main evaluation criteria for the effectiveness of APEX and FAT studies are the proportion of patients with 3 values of serum uric acid concentration of the last month

In the additional 3 -phase confils research, with the result after the circulation license for Febuxostat was first issued, the main criterion of effective evaluation was that the proportion of patients with serum urate concentration

APEX research:

Research on the effectiveness of Febuxostat is controlled with allopurinol and placebo (Allopurinol and Placebo - ControlLed Efficacy Study of Febuxostat - Apex) is a 28 -week study, phase 3, random, double blind, multi -center. A thousand seventy -two (1,072) patients are randomly selected: placebo (n = 134), Febuxostat 80mg, 1 time/day (n = 267), Febuxostat 120mg, 1 time/day (n = 269), Febuxostat 240mg, 1 time/day (N - 134) or Allopurinol (300mg, 1 time/day (N = 258) Initial serum creatinine 1.5 mg/dl and

APEX research shows that the statistically significant in both febuxostat 80mg, 1 time/day and Febuxostat 120mg, 1 time/day compared to the usual dose of Allopurinol (N = 258)/100mg (N = 10) in reducing the concentration of serum uric acid (Sua) below 6mg/DL (357 mol).

Fact research:

Febuxostat test research is controlled with Allopurinol (Febuxostat Allopurinol Controlled Trial - Fact) is a 52 -week study, phase 3, random, double blind, multi -center. Seven hundred sixty (760) patients are randomly selected: Febuxostat 80mg, 1 time/day (n = 256), Febuxostat 120mg, 1 time/day (n = 251) or Allopurinol 300 mg, 1 time/day (n = 253).

Fact research shows that the statistical significance of both groups of Febuxostat 80mg 1 time/day and Febuxostat 120mg, 1 time/day compared to the common dose of Allopurinol in the reduction and maintenance of Uric acid levels of Thanh/DL (357 mol/l).

Table: The proportion of patients with serum uric acid levels Research Febuxostat 80mg, 1 time/day

Febuxostat 120 mg, 1 time/day apex (28 weeks) (n = 262) 65%* ’# (n = 269) 22% (n = 268) (n = 251) Collaborative results 51%* (n = 517) 63%*,# (n = 519) 22%(n = 519) Serum creatinine> 1.5 and * p

The decrease in serum uric acid levels Figure 1: Negative acid concentration Note: 509 patients are treated with Allopurinol 300mg, 1 time/day, 10 patients with serum creatinine levels> 1.5 and Confirms research: Confirms research is a 26 -week, 3, random, control study to evaluate the safety and effectiveness of Febuxostat 40mg and 80mg compared to allopurinol 300mg or 200mg in patients with gout and hyperuricemia. 2269 patients were randomly selected: Febuxostat 40mg, 1 time/day (n = 757), Febuxostat 80mg, 1 time/day (n = 756), or allopurinol 300/200 mg, 1 time/day (n = 756). At least 65% of patients with mild - medium renal failure (with creatinine clearance 30 - 89ml/minute). Preventive treatment for gout outbreaks is mandatory in 26 weeks. The proportion of patients with serum urate concentration The main evaluation criteria for patients with renal failure: APEX research has evaluated the effectiveness of 40 patients with renal impairment (for example, the initial serum creatinine level> 1.5mg/dl and 2.0mg/DL). For kidney failure objects selected randomly into the treatment group with Allopurinol, the dose is limited to 100mg, 1 time/day. Febuxostat has achieved the main evaluation criteria for effectiveness in 44% of patients (80mg, 1 time/day), 45% of patients (120mg, 1 time/day) and 60% of patients (240mg, 1 time/day) compared to 0% in the group using allopunnol 100mg, 1 time/day and the placebo group. There is no clinical difference in terms of percentage reduction for serum uric acid levels in healthy objects regardless of renal function (58% in normal kidney function groups and 55% in severe kidney dysfunction group). Analysis in patients with gout and kidney failure is determined over time in the Confirms research and shows that Febuxostat is more effective in reducing serum urate levels The main evaluation criterion for patients with serum uric acid levels (Sua)> 10 mg/dl: About 40% of patients (APEX and Facting research) have initial uric acid levels> 10 mg/dl. In this subgroup Febuxostat has achieved the main evaluation criteria for effective (serum uric acid level (sua) In the Confirms research, the proportion of patients achieving the main criteria for effective evaluation (serum uric acid concentration (sua) 10mg/dl treated with Febuxostat 40mg, 1 time/day of 27% (66/249), with Febuxostat 80mg, 1 day, 1 time 49% (125/254) and with Allopurinol 300mg/200mg, 1 time/day is 31% (72/230), corresponding. Clinical results: The proportion of patients need to treat gout outbreaks APEX research: During the 8 -week prophylaxis treatment, a larger percentage of subjects in the Febuxostat 120mg (36%) treatment group require gout outbreaks compared to Febuxostat 80mg (28%), Allopurinol 300mg (23%) and placebo (20%). Gout outbreaks increase after the prevention and decrease over time. 46% to 55% of subjects have been treated for gout outbreaks from week 8 to 28 weeks. The gout out of the last 4 weeks of the study (24 - 28 weeks) was observed in 15% of the object (Febuxostat 80mg, 120mg), 14% of subjects (Allopurinol 300mg) and 20% of the subjects. Fact research: During the 8 -week prophylaxis treatment, a larger percentage of subjects in the Febuxostat 120mg (36%) treatment group required gout outbreaks compared to both Febuxostat 80mg (22%) and allopurinol 300mg (21%). After 8 weeks of prophylaxis, the rate of outbreaks increased and decreased over time (64% and 70% of subjects were treated for gout outbreaks from 8 - 52 weeks). The outbreaks of gout in the last 4 weeks of the study (week 49 - 52) were observed in 6 - 8% of subjects (Febuxostat 80mg, 120mg) and 11% of objects (Allopunnol 300mg). The ratio of objects that need to be treated with gout outbreaks (APEX and Fact research) decreased in terms of quantity in groups that have achieved average serum urate concentration after the initial level 6.0mg/dl in the last 32 weeks of the period of the last 32 weeks of treatment periods ( By week 49 - 52). In the Confirms research, the proportion of patients need to treat gout outbreaks (1 to 6 months) is 31% for Febuxostat 80mg and 25% for Allopurinol. Not observing the difference in the proportion of patients who need to treat gout outbreaks between the group using Febuxostat 80mg and the group using Febuxostat 40mg. Label expansion studies: Excel research (C02 - 021): Excel research is a 3 -year expansion study of safety, phase 3, open label, multicolored, random, control with allopurinol in patients who have completed key 3 -phase studies (Apex or Fact). A total of 1086 patients were included in the study: Febuxostat 80mg, 1 time/day (n = 649), Febuxostat 120mg, 1 time/day (n = 292) and Allopurinol 300/100mg, 1 time/day (n = 145). About 69% of patients do not need to change treatment to achieve final stable treatment. Patients with 3 serum uric acid levels (consecutive) site> 6mg/dl are withdrawn from the study. Urat concentration is maintained over time (ie 91% of the initial treatment patients with Febuxostat 80mg and 93% of the initial treatment patients with Febuxostat 120mg have serum uric acid level 3 -year data shows a decrease in the rate of gout outbreaks with less than 4% of patients who need to treat outbreaks (i.e. more than 96% of patients who do not need treatment for outbreaks) in the 16th - 24th month and 30 - 36 months. 46% of the final stable treatment patients with Febuxostat 80mg, 1 time/day and 38% of patients treated the final stable stable with Febuxostat 120mg, 1 time/day there is a complete reduction in primary urate hotels from the beginning until the last visit. Focus research (TMX - 01 - 005) is a 5 -year expansion study in safety, phase 2, open label, multicolored, for patients who have completed 4 weeks using Febuxostat by the double blind method in TMX - 004. 62% of patients do not need to adjust the dose to maintain serum uric acid levels The proportion of patients with serum urate concentration In phase 3 clinical studies, observed abnormalities of mild liver function tests in patients treated with Febuxostat (5.0%). This ratio is similar to the rate reported when using allopurinol (4.2%). The increased TSH values (> 5.5microiu/ml) have been observed in patients with long -term treatment with Febuxostat (5.5%) and patients treated with allopurinol (5.8%) in long -term expansion studies. Dynamic pharmacokinetics in healthy objects, maximum concentrations in plasma (cmax) and area under the plasma concentration curve over time (AUC) of Febuxostat increases proportional to the dosage after single dose and multiple doses of 10mg to 120mg. For doses from 120mg to 300mg, observing a greater increase in proportional to the dose of AUC for Febuxostat. There is no significant accumulation when using 10mg to 240mg every 24 hours. Febuxostat has a sale time (T1/2) The average terminal phase is about 5 - 8 hours. The pharmacokinetic/pharmacokinetic analysis of population has been conducted in 211 patients with hyperuricemia and gout, treated with Febuxostat 40 - 240mg, 1 time/day. In general, Febuxostat pharmacokinetics parameters are estimated by these analysis in accordance with the pharmacokinetic parameters achieved from healthy subjects indicating that healthy objects represent the pharmacokinetic/pharmacokinetic assessment in patients with gout. absorption: Febuxostat is quickly absorbed (TMAX 1.0 - 1.5 hours) and is well absorbed (at least 84%). After taking a single dose and multiple doses of 80mg and 120mg, 1 time/day, cmax is about 2.8 - 3.2g/ml for 80mg, 1 time/day and 5.0 - 5.3g/ml for 120mg, 1 time/day. The absolute bioavailability of the Febuxostat tablet formula has not been studied. After taking multiple doses of 80mg, 1 time/day or a single -dose of 12mg with a high -fat meal, a 49% cmax reduction for 80mg and 38% cmax doses for 120mg, 18% of AUC for 80mg and 16% for AUC for 120mg dose. However, it is not observed that the clinical change is clinically significant for a percentage reduction for serum uric acid levels during testing (multiple doses of 80mg). So Febuxostat can be used not related to food. Distribution: Expected distribution volume in the stable state (VSS/F) of Febuxostat is about 29 - 75 liters after taking oral doses of 10 - 300mg. The cohesion of Febuxostat with plasma protein is about 99.2% (mainly with albumin) and does not change on the range of concentrations achieved at a dose of 80mg and 120mg. The cohesion of active metabolites with plasma proteins from about 82% to 91%. Biological Change: Febuxostat is strongly metabolized due to the conjugate through the uridin diphosphate glucuronosyltransferase system (UDPGT) and oxidation through the Cytochrom P450 (CYP) system. 4 Hydroxyl metabolites with pharmacological activity have been identified, of which 3 substances are found in human plasma. In vitro studies with human liver microsom shows that the above oxidant metabolites are formed mainly by CYP1A1, CYP1A2, CYP2C8 or CYP2C9 and Febuxostat Glucuronid formed mainly by UGT 1A1, 1A8 and 1A9. Era: Febuxostat is eliminated through both liver and kidneys. After taking a dose of 80mg Febuxostat with 14C marked, about 49%of the dose found in urine in the form of Febuxostat does not change (3%), acglucuronide of active ingredient (30%), its known oxidant metabolites and unnamed substances (13%) and other unknown substances (3%). In addition to the excretion of urine, about 45%of the dose found in feces in the form of febuxostat does not change (12%), acyl glucuronid of the active ingredient (1%), its known oxidant metabolites and unnamed (25%) and other unknown substances (7%). kidney failure: After taking multiple doses of Febuxostat 80mg in patients with mild, medium or severe renal impairment, Febuxostat's CMAX does not change compared to those with normal kidney function. The average AUC total of Febuxostat increases about 1.8 times from 7.5 g - hour/ml in the group with normal kidney function to 13.2g - hour/ml in the severe kidney dysfunction group. CMAX of metabolites increases 2 times and AUC of metabolites increases 4 times. However, it is not necessary to adjust the dose in patients with mild or medium renal failure. Hepatic failure: After taking multiple doses of Febuxostat 80mg in patients with mild liver failure (Child - PUGH type A) or medium (Child - PUGH type B), CMAX and AUC of Febuxostat and its metabolites are not changed compared to those with normal liver function objects. No research has been conducted in patients with severe liver failure (Child - Pugh type C). Age: There is no significant change in the AUC of Febuxostat or its metabolites after many doses of Febuxostat in elderly subjects compared to healthy young people. Sex: After taking multiple febuxostat oral doses, CMAX is 24% higher than in women and AUC is 12% higher than in women. However, CMAX and AUC are adjusted the same weight between gender. No need to adjust the dose based on gender.

Before taking Feburic 80mg Astellas treat chronic hyperuricemia (3 blisters x 10 tablets)

How to use

Feburic 80mg medicine is taken orally.

Should drink feburic oral and can be taken with or not with food.

Dosage

The recommended oral dose of Feburic is 80mg, 1 time/day is not related to food. If serum uric acid concentration> 6mg/dl (357mol/l) after 2-4 weeks, can be considered for 120mg, 1 time/day.

Feburic works quickly enough to allow the test of serum uric acid after 2 weeks. The goal of treatment is to reduce and maintain serum uric acid levels below 6mg/dl (357 mol/l).

Recommendations for preventive treatment for gout out for at least 6 months.

Elderly

Unnecessary adjustment of the dose in the elderly.

kidney failure

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

Unsurting dose adjustment in patients with mild or medium renal failure.

Hepatic failure

The efficiency and safety of Feburic has not been studied in patients with severe liver failure (Child Pugh type C).

recommended dose in mild liver failure patients is 80mg.

Existing information is limited in patients with average liver failure.

Group of children's patients

The safety and effectiveness of Feburic in children under 18 have not been determined. There is no data.

What do

do when overdose?

What to do when you forget the dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Do not drink twice as prescribed.

Side Effects

Safety summary

The most commonly reported side effects in clinical trials (4072 subjects are treated at least at 10mg to 300mg) and in after -sales experience are gout outbreaks, liver function abnormalities, diarrhea, nausea, headache, rash and edema.

These side effects are mostly mild or medium. Serious hypersensitivity reactions are rare for Febuxostat, some reactions that are related to systemic symptoms have occurred in after -sales experience.

List of side effects

Common side effects (1/100 to

In each frequency group, side effects are presented in the order of severity of severity.

Table: Auxiliary reactions in expanded, long -term, 3 combined and after -sales experience

Blood disorders and lymphatic systems rare: reducing all bloody platelets, platelets; Giap in the blood

Uncommon: diabetes, hypergyang blood lipids, decreased appetite, weight gain;

Rare: Losing weight, increasing appetite, anorexia;

Rare: restlessness;

Less: dizziness, paresthesia, hemiplegia, drowsiness, change taste, reduce sensation, reduce smell;

Eye disorders rare: blurred vision; (ECG); Chemistry Common: diarrhea **, nausea;

Uncommon: abdominal pain, abdominal distention, gastroesophageal reflux disease - esophagus, vomiting, dry mouth, indigestion, constipation, defecation many times, flatulence, discomfort with digestive tract;

Rare: Pancreatitis, mouth ulcers;

Uncommon: gallstones;

Rare: hepatitis, jaundice*, liver damage*;

Skin disorders and subcutaneous tissue Common: Ban (including the types of boards reported with lower frequencies, see below);

Uncommon: dermatitis, urticaria, itching, skin discoloration, skin damage, hemorrhagic spots, rash, rash, lumpy, lumpy;

Rare: Poisoned epidermis*, Stevens - Johnson*, angioedema*, Drug reaction with acidic white blood cells and systemic symptoms (Dress syndrome)*, systemic rash (serious)*, erythema, scales, acne acne rash, blister rash, pustules, itchy skin, skin red rash, measles rash;

Rare: Pepper pattern*, stiffness, musculoskeletal stiffness;

Rare: interstitial renal tubular inflammation*, urinating;

Reproductive disorders and mammary glands less common: erectile dysfunction;

Less: fatigue, chest pain, uncomfortable chest;

Rare: Thirst;

Testing Uncommon: increased blood amylase, reduces the number of platelets, reduces the number of white blood cells, reduces the number of lymphocytes, increases blood creatinine, increases blood creatinine, reduces hectares Dehydrogenase in the blood, hyperkalemia;

Rare: increased blood glucose, thromboplastin time for prolonged activation, reducing the number of red blood cells, increasing alkaline phosphatase in the blood;

** Diarrhea is not caused by infection during treatment and testing of abnormal liver function in phase -3 studies more common in patients treated simultaneously with colchicin.

*** See the pharmacological properties of the rate of gout outbreaks in randomly random phase studies.

Describe selective side effects

Serious hypersensitivity reactions rare with Febuxostat, including Stevens - Johnson syndrome, poisoned epidermal necrosis and anaphylactic/shocking reaction, occurred in after -sales experience.

Stevens - Johnson syndrome and poisoned epidermal necrosis are characterized by progressive skin rashes that come with water balls or mucosal damage and eye irritation.

Hypersensitivity reaction to Febuxostat may be associated with the following symptoms: The skin reaction is characterized by the contaminated rash, body rash or peeling, in addition to skin damage, face, fever, hematological abnormalities such as platelet reduction and acid leukocytes and related to one or more organs (liver and kidneys include interstitial kidney inflammation).

Gout outbreaks are often observed immediately after the beginning of treatment and in the first months. After that, the frequency of gout outbreaks in time depends on time. Recommended prophylactic treatment of gout outbreaks.

Notify the doctor with unwanted effects when using the drug.

Warnings

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

Contraindicated

Feburic medicine is contraindicated in the following cases:

Hypersensitivity to any ingredients of the drug.

Be cautious when taking the drug

Read the instructions carefully before use. If you need more information, please consult your doctor.

This drug is only used by a doctor.

cardiovascular disorders

Do not recommend Febuxostat treatment in patients with ischemia or congestive heart failure.

Observed a larger percentage in terms of the number of cardiovascular events according to APTC reported by the researcher (the criteria determined by the platelet anti -platelet testing group (APTC) including cardiovascular death, non -fatal myocardial infarction, non -fatal stroke) among the total number of febuxostat groups compared to the group of Allopurinol in APEX and Facting (1.3 Variables/Fact. Human/year (PYS) compared to 0.3 events/100 patients/year), but not observed in the Confirms research.

The rate of cardiovascular events by APTC in phase 3 combined studies reported by researchers (APEX, Fact and Confirms studies) are 0.7 events/100 patients/year compared to 0.6 events/100 patients/year.

In long -term expansion studies, the proportion of APTC events reported by the researcher is 1.2 events/100 patients/year for Febuxostat and 0.6 events/100 patients/year for allopurinol.

There is no statistical difference and there is no causal relationship with Febuxostat. The risk factors for these patients are medical history of atherosclerosis and/or myocardial infarction or congestive heart failure.

allergies/hypersensitivity to drugs

Rare reports on severe allergic/hypersensitivity reactions, including Stevens - Johnson syndrome, poisoned epidermal necrotic and acute anaphylactic/acute shock reaction, have been collected in after -sales experience.

In most cases, these reactions occur in the first month of Febuxostat treatment. Some but not all these patients have reported renal failure and/or hypersensitivity to allopurinol.

The severe hypersensitivity reaction, including an acid -loving leukemia reaction and systemic symptoms (Dress syndrome) are associated with fever, hematology, kidney or liver in some cases.

must notify the patient about signs and symptoms and need to closely monitor the symptoms of allergic/hypersensitivity reactions. Febuxostat must be stopped immediately if the allergic/hypersensitivity reactions occur, including Stevens - Johnson syndrome, because the early stopping of the drug is associated with a better prognosis.

If the patient appears allergic/hypersensitivity, including Stevens - Johnson syndrome and acute anaphylaxis and anaphylaxis/shock, must not start using Feburic in this patient at any time.

Acute gout (gout outbreak)

Do not start treatment with Febuxostat until acute gout has decreased completely.

Gout outbreaks can occur during the start of treatment due to changes in serum uric acid levels that lead to urate mobilization from the deposition in the tissues. At the beginning of Febuxostat treatment, it is recommended that preventive treatment for nonsteroidal anti -inflammatory drugs (NSAID) or Colchicin for at least 6 months.

If a gout outbreak occurs during Febuxostat treatment, do not stop the drug. Should handle the outbreak of gout simultaneously appropriate for each patient. The continuous treatment with Febuxostat reduces the frequency and intensity of gout outbreaks.

Xanthin deposits

In patients with rising urate formation rate (for example, its malignant disease and treatment, Lesch - NYHAN syndrome), in rare cases, the absolute concentration of xanthin in the urine may increase enough to allow the deposition in the urinary tract. Due to no experience with Febuxostat, it is not recommended to use Febuxostat in this patient group.

mercaptopurin/azathioprin

It is not recommended to use Feburic in patients treated simultaneously with mercaptopurin/azathioprin. In case of this coordination, it is impossible to monitor patients closely. Recommended reduction of mercaptopurin or azathioprin dose to avoid possible hematological effects.

Patients with organ transplants

Due to no experience in organ transplant patients, it is not recommended to use Feburic in these patients.

Theophyllin

Simultaneous use of Febuxostat 80mg and single doses of 400mg for healthy objects do not show any pharmacokinetics interaction. Febuxostat 80mg can be used for patients treated simultaneously with theophylllin without the risk of increasing serum concentration of theophyllin.

There is no research data for Febuxostat 120mg.

Liver disorders

In combination 3 -phase clinical studies, observed abnormalities of mild liver function tests in patients treated with Febuxostat (5%). Recommended liver function test before starting treatment with Febuxostat and periodically later based on clinical evaluation.

thyroid disorders

Observed an increase in the hormone values stimulating the TSH thyroid (> 5.5iu/ml) in patients with long -term treatment with Febuxostat (5.5%) in long -term open label expansion studies. Be careful when using Febuxostat in patients with changes in thyroid function.

lactose

Feburic tablets contain lactose. Patients with rare genetic problems in tolerance Galactose, Lapp Lactase deficiency or Glucose - Galactose should not use this drug.

The ability to drive and operate machinery

drowsiness, dizziness, abnormal and blurred vision have been reported with the use of Febuxostat. Patients need to be cautious before driving, operate machinery or participate in dangerous activities until they are sure that Feburic does not adversely affect performance.

During pregnancy and lactation

pregnancy

Data on a very limited amount of pregnant women using Febuxostat did not show any adverse effects of Febuxostat for pregnancy or health of pregnancy/infant. Animal studies do not show directly or indirectly harmful effects on pregnancy, the development of embryo/fetus or childbirth.

It is unclear the risks that may occur for humans. Febuxostat should not be used during pregnancy.

Breastfeeding period

It is unclear whether Febuxostat will be excreted in breast milk. Animal studies have shown the excretion of this active ingredient in breast milk and reduce the growth of an animal. Can not rule out the risk for breastfeeding.

Do not use Febuxostat during breastfeeding.

Reproduction

In animals, reproductive studies up to 48 mg/kg/day show that there is no adverse effect depending on the dose for fertility. The influence of Febuxostat is unknown on human fertility.

Drug interaction

mercaptopurin/azathioprin

Based on the mechanism of action of Febuxostat on the inhibition of xanthin oxidase (XO), it is not recommended to use simultaneously. The inhibition of oxidase xanthin by Febuxostat may increase the concentration of these drugs in plasma, leading to toxicity.

Studies on drug interaction between Febuxostat and drugs metabolized by xanthin oxidase have not been done.

Studies on drug interactions between Febuxostat and chemotherapy has not been conducted. There is no data on the safety of Febuxostat in cytotoxic treatment.

Rosiglitazon and CYP2C8 substrate

Febuxostat is seen as a weak inhibitor on in vitro. In a healthy subject, simultaneously used 120mg of Febuxostat QD with a single dose of 4mg Rosiglitazone without any effect on the pharmacokinetics of Rosiglitazone and metabolite metabolites N - Desmethyl Rosiglitazon, which indicates that Febuxostat is not the enzyme inhibitor of CYP2C8 on Vivo.

Therefore, simultaneous use of Febuxostat with Rosiglitazone and CYP2C8 substrates are thought to be no need to adjust the dose for these preparations.

Theophyllin

A study of drug interactions conducted on healthy people using Febuxostat to evaluate whether Xo inhibitors can cause anhophyllin increase during circulation or not like other submerged inhibitors that have been previously reported.

Research results show that simultaneous use of Febuxostat 80mg QD along with single doophyllin 400mg dose does not affect the pharmacokinetics or the safety of theophyllin.

Therefore, no special caution is given when using Febuxostat 80mg and Theophyllin simultaneously. No data for Febuxostat 120mg.

Naproxen and other glucuronids inhibitors

The metabolism of Febuxostat depends on the enzyme Uridine Glucuronosyl Transferase (UGT). Glucuronids inhibitors such as nonsteroidal anti -inflammatory drugs (NSAID) and probenecid, in theory can affect Febuxostat excretion.

In healthy subjects, simultaneously using Febuxostat and Naproxen 250mg, 2 times/day is associated with an increase in contact with Febuxostat (maximum concentration in plasma (cmax) 28%, area under the plasma concentration curve over time (AUC) 41%and 26%waste sale time.

In clinical studies, the use of Naproxen or NSAID/COX - 2 inhibitors is not related to any increase in clinical significance. Febuxostat can be used simultaneously with Naproxen without adjusting the dose of Febuxostat or Naproxen.

Glucuronid -induced drugs

Powerful drugs that can lead to increased metabolism and reduced efficiency of Febuxostat. Therefore, it is recommended to monitor the concentration of serum uric acid 1-2 weeks after starting treatment with a strong induction medication for glucuronid. In contrast, stopping treatment with an induced drug can lead to increased febuxostat concentration in plasma.

Colchicin/indomethacin/hydrochlorothiazide/warfarin

Febuxostat can be used simultaneously with colchicin or indomethacin without adjusting the dose of febuxostat or active ingredient.

Unnecessary adjustment of Febuxostat dose when used with hydrochlorothiazid.

Unnecessary adjustment of Warfarin dose when used with Febuxostat. The use of Febuxostat (80mg or 120mg, 1 time/day) with warfarin does not affect the pharmacokinetics of warfarin in healthy objects. The international standardization index (INR) and the activity of factor VII are not affected by simultaneous use with Febuxostat.

Desipramin/CYP2D6 mechanical

Febuxostat has shown a weak inhibitor CYP2D6 in vitro. In a study in healthy subjects, Febuxostat 120mg, 1 time/day (QD) led to an average increase of 22% of the AUC of Desipramin - a substrate of CYP2D6 showing the weak inhibited effect of Febuxostat on the enzyme CYP2D6 In Vivo.

Therefore, simultaneous use of Febuxostat with other substrates of CYP2D6 is not expected to need any dose adjustments to these compounds.

antacids

Take the same drink with antacids containing magnesi hydroxid and aluminum hydroxid has been shown to slow down the absorption of Febuxostat (about 1 hour) and reduce CMAX by 32%but do not observe the meaning of AUC. Therefore, Febuxostat can be used not related to the use of antacids.

Storage

Store less than 30 ° C, out of reach of children. Do not use overdue drugs stated on the packaging.

Expiry date: 36 months from the date of manufacture.

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