Uloxoric 80mg Herabiopharm medicine for hyperuricemia (3 blisters x 10 tablets)
Dosage form Box of 3 blisters x 10 tablets
Specifications Hera Pharmaceutical Company Limited
Uses
indications
Uloxoric 80mg drug indicated in the following cases:
ATC code: m04aa03.
Active mechanism:
Uric acid is the final product of the human metabolism and is formed according to the hypoxanthin process → xanthin → uric acid.
The above changes are catalyzed by xanthin oxidase enzymes. Febuxostat is a 2-anlthiazol derivative that effectively reduces serum uric acid content by inhibiting Xanthin Oxidase enzyme selection.
Febuxostat is a Non-Purin selective inhibiting Xanthin oxidase enzyme with ki value in Vitro in Vitro research less than a nanomolar.
Febuxostat inhibits oxidation and formation of xanthin oxidase.
During Febuxostat treatment, do not inhibit other enzymes involved in purin or pyrimidine metabolism, specifically, guanin deaminase, hypoxanthin guanin phosphoribosyltransferase, phosphoribosyltransferase OROTAT, OROTIDIN decarboxylase monophate nucleosid phosphorylase.
Dynamic pharmacokinetics
in healthy people, maximum concentrations in plasma (cmax) and the area under the curve (AUC) of Febuxostat increases in proportion to the dosage when using the dosage and multiple doses from 10 mg to 120 mg.
For the dose of 120 mg and 300 mg, the area under the curve (AUC) of Febuxostat increases larger rate. There is no significant accumulation when taking 10 mg to 240 mg orally orally orally. Febuxostat waste time (TFRAC12;) is about 5-8 hours.
Pharmacokinetics/Pharmacokinetic analysis has been conducted in 211 patients with symptoms of hyperuricemia and gout, treatment with Febuxostat 40-240 mg per day.
In general, Febuxostat pharmacokinetic parameters are estimated by the analysis in accordance with the results obtained in healthy subjects, showing that healthy people represent the evaluation of pharmacokinetics/pharmacokinetics in the collection of patients with gout.absorption:
Febuxostat absorbs quickly (t max after 1.0-1.5 h) and good absorption (at least 84%). After taking single-dose or multi-dose 80 and 120 mg once a day, the peak concentration (CMAX) corresponds to about 2.8-3.2 µg/ml and 5.0-5.3 µg/ml. The absolute bioavailability of the form of Febuxostat has not been studied.
After taking 80 mg doses once a day or a single -dose of 120 mg with a high -fat meal, there is a decrease in CMAX, equivalent to 49% and 38% and AUC reduction, equivalent 18% and 16%.
However, the change in blood uric acid concentration is not clinically significantly observed in the test (using 80 mg multi -dose). Thus, Febuxostat can be used without a meal.
Distribution:
The actual distribution voltage in the stable state (VSS/F) of Febuxostat is about 29-75 l after the oral dose of 10-300 mg.
Febuxostat plasma protein bound is about 99.2%, (mainly with albumin), and unchanged when using the dose of about 80 mg and 120 mg. The protein bond of metabolites is active between 82% to 91%.
Metabolism:
Febuxostat is widely metabolized by a combination through the uridin diphosphate glucuronosyltransferase (UDPGT) system and oxidation through the Cytochrom P450 system (CYP).
Four pharmacological hydroxyl metabolites have been identified, in which three processes occur in a human plasma. In In vitro study with human liver microsom shows that oxidative metabolites are formed mainly by CYP1A1, CYP1A2, CYP2C8 or CYP2C9 and Glucuronid Febuxostat formed mainly by UGT 1A1, 1A8 and 1A9.
Era:
Febuxostat is eliminated by both liver and kidney. After taking a dose of 80 mg Febuxostat marking the 14C isotope, about 49%of the dosage is recovered in the urine in the form of febuxostat unchanged (3%), active ingredient glucuronid acyl (30%), its oxidant metabolites and combinations (13%), and other unknown metabolites (3%).
In addition to the excretion in the urine, about 45%of the dose found in the feces is the initial Febuxostat (12%), the active ingredient Glucuronid Acyl (1%), its oxidative and synchronized metabolites (25%), and other unknown metabolites (7%).
kidney failure:
After taking 80 mg of Febuxostat multi -dose in patients with mild, medium or severe renal failure, the peak concentration (CMAX) of Febuxostat does not change compared to patients with normal renal function.
The total area under the average curve (AUC) of Febuxostat increases about 1.8 times compared to 7.5 mg/ml in the normal kidney function to 13.2 μg.h/ml in the severe kidney dysfunction group. The value of C Max and AUC of active metabolites increases to 2 and 4 times respectively. However, do not need to adjust the dose in patients with mild or medium renal failure.
liver failure:
After taking 80 mg of Febuxostat multi-dose in patients with mild hepatic impairment (Child-Pugh Class A) or average (Child-Pugh Class B), CMAX and AUC of Febuxostat and its metabolites does not change significantly compared to those with normal liver function. No studies have been conducted in patients with severe liver (Child-Pugh Class C).
Age:
There is no significant change observed in the AUC of Febuxostat or its metabolites when taking Febuxostat in the elderly compared to healthy young people.
Sex:
After taking multiple doses of Febuxostat, CMAX and AUC in women are 24% and 12% are higher than men. However, CMAX and AUC are adjusted to the same volume as the same gender. No need to adjust the dose based on gender.
Before taking Uloxoric 80mg Herabiopharm medicine for hyperuricemia (3 blisters x 10 tablets)
How to use
oral medication. Patients can use the drug with food or not.
Dosage
Dosage in case of gout patients: Febuxostat recommended dose is 80 mg/time/day does not depend on meals. If blood uric acid> 6 mg/dl (357 μmol/l) after 2-4 weeks, recommend the use of Febuxostat at a dose of 120 mg/time/day.
Febuxostat is quick to check the blood uric acid concentration in the blood after 2 weeks. Treatment goals to reduce and maintain blood uric acid levels below 6 mg/dL (357μmol/l).
Recommended prevention of gout outbreaks for at least 6 months.
Tumor solving syndrome: Febuxostat recommended dose is 120 mg/time/day does not depend on meals. Febuxostat should be treated 2 days before the beginning of cytotoxic treatment and continue to treat at least 7 days, but treatment may last up to 9 days over time of chemotherapy based on clinical assessment.
Elderly:
No need to adjust the dosage in the elderly.
Patients with renal failure:
Efficiency and safety have not been fully evaluated in patients with severe renal failure (creatinine clearance
No need to adjust the dosage in patients with mild or medium renal failure.
Patients with liver failure:
Efficiency and safety of Febuxostat has not been studied in patients with severe liver failure (Child Pugh Class C).
Gout: The recommended dose in patients with mild liver failure is 80 mg. Restricted information for patients with average liver failure.
Tumor solving syndrome: In phase III of the test, eliminate the object of severe liver failure. Do not require adjusting the dose compared to patients with normal liver function.
Children:
The safety and effectiveness of Febuxostat in children aged between 18 and 18 have not been determined. No data available.
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 clinical trials (4072 subjects are treated at least at a dose from 10 mg to 300 mg) and reports during the circulation period are acute gout, abnormal liver function, diarrhea, nausea, headache, rash and edema.
usually light side effects. Rarely serious sensitive reactions, some of which are related to systemic symptoms, occurred during circulation.
Classification of frequency of the effects of not wanting to include: Common (≥1/100 to
Common, 1/100 ≤ ADR
Metabolism and nutrition: Acute gout.
Neurology: Pain.
Digestive: diarrhea **, nausea.
Liver: Abnormal liver function **.
skin and subcutaneous organization: rash.
Body: edema.
less common, 1/1000 ≤ ADR
Endocrine: Thyroid blood stimulates hormones.
Metabolism and nutrition: diabetes, hyperlipidemia, reduced appetite, weight gain.
Mental: Reduce libido, insomnia.
Neurological: dizziness, uncomfortable feeling, hemiplegia, sleeping, changing taste, reducing tactile, reducing irritation.
Heart: Atrial fibrillation, fast heartbeat, electrocardi disorders.
Blood vessels: Hypertension, red skin, heating.
Respiratory system: Difficulty breathing, bronchitis, upper respiratory tract infection, cough.
Digestive: abdominal pain, bloating, gastroentricular disease, vomiting, dry mouth, indigestion, constipation, frequent, flatulence, gastrointestinal disorders.
Liver-stones: gallstones.
Skin and subcutaneous organization: dermatitis, urticaria, itching, skin pigmentation, damage, hemorrhage, yellow rash, papules, small acne in the skin.
musculoskeletal and connective tissue: joint pain, arthritis, muscle pain, muscle pain, muscle weakness, muscle spasm, muscle tension, epidemic inflammation.
Kidney and urinary: kidney failure, kidney stones, bleeding, urination, protein.
Reproduction and mammary gland: erectile dysfunction.
Body: fatigue, chest pain, chest tightness.
Hematology: Increasing blood starch, platelets decreases, decreasing leukocytes, decreasing lymphocytes, increased blood creatin, increased blood creatinin, decreasing hemoglobin, increased blood urea, increased bloodceride, increased blood cholesterol, red blood cells decreases, lactat dehydrogenase in blood increases, increased blood.
rare, 1/10000 ≤ ADR
Blood and lymphatic system: decreased by three lines of peripheral blood cells, platelets.
The immune system: Anaphylactic reaction *, sensitivity *.
Eyes: blurred vision.
Metabolism and nutrition: Losing weight, increasing appetite, anorexia.
Mental: Stress.
ears: tinnitus.
Digestive: Pancreatitis, mouth ulcers.
Liver: Hepatitis, jaundice*, liver damage*.
Skin and subcutaneous organization: Poisoned epidermal necrosis*, Stevens-Johnson syndrome*, angioedema*, Symptoms of drug reactions with eosinophilia and body*, whole rash (serious)*, erythema, flaky skin rash, ovulation rash, redness blisters, pustules, rashes*, sweat rash, measles rash, measles rash.
musculoskeletal and connective tissue: muscle pattern*, stiffness, musculoskeletal muscle.
Kidney and urinary tract: Pepper pattern*, stiffness, musculoskeletal muscle.
Body: Thirst.
Hematology: Glucose in the blood increases, prolongs blood clotting, reduces the number of red blood cells, high blood alkalin content in the blood.
*Side reactions in the circulation process.
** Emergency treatment for emergency diarrhea without infection and abnormal liver function in combining phase 3 studies is more frequent in patients who use Colchicin at the same time.
Unwanted treatment (ADR)
To prevent acute gout occurs during treatment, it is advisable to start treatment with Febuxostat when acute gout attacks have completely dropped.
If acute gout occurs during febuxostat treatment, patients should not stop the drug. Acute gout control suitable for each patient.
Continue to treat with Febuxostat to reduce the frequency and intensity of acute gout.
Must stop Febuxostat immediately when appearing in the skin, accompanied by more severe allergy symptoms, especially those with kidney damage or taking thiazide diuretics.
Patients must be instructed on signs and symptoms and closely monitor the symptoms of allergic/hypersensitivity reactions.
Febuxostat treatment should be stopped immediately if allergic/hypersensitivity reactions, including Stevens-Johnson syndrome, the early stopping will have better prognosis.
If the patient has developed allergic/hypersensitivity reactions, including Stevens-Johnson syndrome and acute anaphylactic reaction/reaction/stop use Febuxostat in this patient at any time.
Treatment of hypersensitivity reactions with glucocorticoids, severe reactions must be used for prolonged use. In some patients, if a mild skin reaction can be used carefully with low doses, but immediately stop if the reaction reappears.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Uloxoric 80mg contraindications in the following cases:
Be cautious when using
need to be very careful when taking the drug for patients in the following cases:
cardiovascular disorders:
Treatment of chronic hyperuricemia:
Prevention and treatment of hyperuricemia in patients at risk of TLS (tumor syndrome):
allergies, hypersensitivity to drugs:
very few reports on severe allergic/hypersensitivity reactions, including the life-threatening syndrome of Stevens-Johnson, poisoned epidermal necrosis and acute anaphylaxis, have been collected during circulation.
In most cases, the reactions occurred in the first month of treatment with Febuxostat. Some, but not all patients who have reported previous kidney failure or hypersensitivity to Allopurinol.
A few serious hypersensitivity reactions, including drug reactions with eosinophilia and systemic symptoms combined with fever, hematology, kidney or liver damage in some cases.
Patients must be instructed in signs and symptoms and closely monitor the symptoms of allergic reactions, hypersensitivity.
Febuxostat treatment should be stopped immediately if allergic/hypersensitivity reactions, including Stevens-Johnson syndrome, the early stopping will have better prognosis.
If the patient has developed allergic/hypersensitivity reactions, including Stevens-Johnson syndrome and acute anaphylactic reaction/reaction/stop use Febuxostat in this patient at any time.
Acute gout attacks (gout outbreaks):
Febuxostat treatment should not start until acute gout attacks have completely dropped.
Acute gout may occur at the beginning of treatment due to changes in uric acid levels in the blood leading to urate mobilization from deposition tissue. Febuxostat acute gout prevention should be treated for at least 6 months with NSAID or Colchicin nonsteroidal anti -inflammatory drugs.
If acute gout occurs during Febuxostat treatment, patients should not stop the drug. Control acute gout suitable for each patient. Continue treatment with Febuxostat to reduce the frequency and intensity of acute gout.
Xanthin deposits:
For patients with high urate crystal formation rate (such as malignant disease, lesch -nyhan syndrome) xanthin concentration in urine in very few cases can increase enough to allow accumulation in the urinary tract.
Do not recommend when not experienced with the use of Febuxostat in this case.
mercaptopurin or azathioprin:
Using Febuxostat is not recommended in patients who use simultaneously treated with mercaptopurin/azathioprin.
In case of combination, patients need to be closely monitored. The reduction of the dose of mercaptopurin or azathioprin is recommended to avoid hematological effects that may occur.
The transplanted person:
There is almost no information in organ transplant patients, the use of Febuxostat for these patients is not recommended.
Theophyllin:
Oral combined with Febuxostat 80 mg and theophyllin 400mg in healthy people show that there is no pharmacokinetic interaction. Febuxostat 80 mg can be used in patients who are simultaneously treated with theophylllin without increasing theophyllin level in plasma. There is no data for Febuxostat 120 mg.
Liver disorders:
In the process of combining 3 clinical research stages, there is a mild abnormal in the liver function that has been observed in patients treated with Febuxostat (5.0%). It is recommended to check liver function before starting treatment with Febuxostat and periodically based on clinical evaluation.
thyroid disorders:
Increase TSH value (> 5.5 μi/ml) is observed in long -term patients with Febuxostat (5.5%) in long -term expansion label studies. Be careful when using Febuxostat with patients with changes in thyroid function.
lactose:
Febuxostat tablets contain lactose. Patients with rare genetic problems are galactose intolerance, lactase deficiency or glucose-galactose abutments should not be taken.
Children and teenagers:
Do not use this drug for children under 18 years of age because of safety and effectiveness that has not been established.
Women during pregnancy and lactation
Pregnant women:
Data on a very limited amount of pregnant women not only show any side effects of febuxostat during pregnancy or the health of the fetus/newborn.
Animal research does not show direct or indirect harm to pregnancy, fetal/embryo development or childbirth.
The potential risks to humans are unknown. Febuxostat should not be used during pregnancy.
breastfeeding women:
There is no information that Febuxostat is excreted in breast milk. Animal studies have shown the elimination of this active ingredient in breast milk and the decline of the mice.
Risks for infant breastfeeding is not possible to exclude Febuxostat should not be used when breastfeeding.
Reproduction:
In animals, reproductive research up to 48 mg/kg/day shows no side effects depending on the dose to fertility. The effect of Febuxostat on human fertility is not clarified.
affects the ability to drive or operate machinery
Sleep, dizziness, discomfort and blurred vision can occur when using Febuxostat. Patients should be cautious when driving and operating machinery.
Drug interaction
mercaptopurin or azathioprin
Based on the mechanism of operation of Febuxostat is to inhibit the Xanthin oxidase enzyme so it is not used simultaneously. The inhibition of xanthin oxidase enzyme because Febuxostat can cause increased plasma concentrations of these drugs leading to poisoning.
Febuxostat drug interaction research with drugs metabolized by xanthin oxidase enzymes has not been done.
Febuxostat drug interaction research with cytotoxic chemotherapy has not been done. There is no data related to the safety of Febuxostat in cytotoxic treatment.
Rosiglitazon or CYP2C8
Febuxostat is a weak inhibitor CYP2C8 in vitro. In a study in a healthy person, when using the prescription of 120 mg of Febuxostat with a dose of 4 mg Rosiglitazon shows no effect on Rosiglitazon pharmacokinetics and N-Desmethyl Rosiglitazon metabolites, and shows that Febuxostat is not an enzyme inhibitor CYP2C8C8C8 In Vovo.
Therefore, taking Febuxostat at the same time with Rosiglitazon or other CYP2C8 substances will not require any dosage adjustment to those compounds.
Theophyllin
A healthy interactive study has been conducted with Febuxostat to evaluate whether the inhibitor of xanthin oxidase enzyme can cause an increase in theoophylllin level as reported with other Xanthin oxidase inhibitors.
Research results show that oral concurrently Febuxostat 80 mg with theophylllin 400 mg the only dose does not have the effect of pharmacokinetics or the safety of theophyllin.
Therefore there is no special caution that needs to be notified when Febuxostat 80 mg and theophylline are used simultaneously. There is no data for Febuxostat 120 mg.
naproxen and glucuronidation inhibitors
Febuxostat metabolism depends on the uridine glucuronosyl transferase enzyme (UGT). Glucuronid inhibitors, such as NSAID and Probenecid drugs, theoretically can affect the removal of Febuxostat.
For healthy subjects using Febuxostat and Naproxen 250mg twice daily are related to the increase in contact with Febuxostat (C Max 28%, AUC 41%and T 1/2 26%).
In clinical studies using Naproxen or other NSAID/COX-2 inhibitors are not related to any clinical increase in side effects.
Febuxostat can be used with Naproxen without adjusting the dose of Febuxostat or Naproxen.
drug -induced drugs
The strong induction drug of the UGT enzyme can lead to an increase in metabolism and reduce the effectiveness of Febuxostat. Therefore, the quantification of uric acid in the blood is proposed after 1-2 weeks from the beginning of treatment with a strong induction substance with glucuronid.
In contrast, the discontinuation of an induction substance can lead to increased concentration of febuxostat.
colchicin/indometacin/hydrochlorothiazide/warfarin
Febuxostat can be used with Colchicin or Indomethacin without adjusting the dose of febuxostat or taking the active active ingredients if necessary.
No need to adjust the dose for Febuxostat when used with hydrochlorothiazid.
No need to adjust the dosage of warfarin when used with Febuxostat. Take Febuxostat (80 mg or 120 mg once a day) with warfarin that does not affect the pharmacokinetics of warfarin in healthy people. Drinking in combination with Febuxostat does not affect Inr activity and factor VI.
Desipramin/CYP2D6 substrate
Febuxostat is thought to be a poor inhibitor in CYP2D6 in test tubes.
In a healthy study, taking 120 mg of Febuxostat daily gives an average increase of 22% in the area under the curve (AUC) of the Desipramin, a CYP2D6 substrate indicates the potential memory effect of Febuxostat on CYP2D6 enzymes in the body.
Therefore, taking Febuxostat at the same time with other CYP2D6 substrates does not require any adjustments to these compounds.
antacids
When shared antacids containing magnesium hydroxid and aluminum hydroxid are shown to slow down the absorption of Febuxostat (about 1 hour) and cause 32% reduction in peak concentration (CMAX), but observations have not changed any significant changes in AUC.
Therefore, Febuxostat can be used without related to the use of antacids.
Storage
Storage in closed packaging, in a dry place, temperature below 30 ° C.
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