Allopurinol 300mg Stella Pharm reduces the formation of uric acid, treating gout (10 blisters x 10 tablets)

Dosage form Box of 10 blisters x 10 tablets
Specifications Allopurinol
Ingredient Stella

Ingredient

Composition information	Content
Allopurinol	300mg

Uses

indications

Allopurinol 300 is indicated in the following cases:

Reducing urate/uric acid formation in urate/uric acid deposits (such as gout arthritis, urate in the skin, kidney stones) or clinical risks that can be predicted (such as the treatment of malignant malignant diseases that can lead to acute kidney disease due to uric acid). The main conditions that can cause urate/uric acid deposits are: Gout is idiopathic; Uric acid stones in the kidneys; Acute kidney disease due to uric acid; Cancer and bone marrow hypertrophy, of which high urate concentration occurs spontaneously or after cytotoxic treatment; Some disorder enzymes lead to excessive urate production such as hypoxanthine-guanine phosphoribosyltransferase (including lesch-anyhan syndrome), glucose-6-phosphate (including glycogen reserves), phosphoribosyl-pyrophosphate synthetase Amido-transferase, adenine phosphoribosyl-gsferase.

Treatment of kidney stones 2.8-dihydroxyadenine (2.8-dha) is associated with the activity decline of adenine phosphoribosyltransferase.

Treatment of recurrent mixed calcium oxalate kidney stones is encountered in urinary hyperurgery when compensation, diet and similar measures.

Pharmacokology

Pharmacological group: Gout treatment drugs; Uric acid production inhibitors.

ATC code: M04AA1.

Allopurinol is a Xanthine-Oxidase inhibitor. Allopurinol and its main metabolites oxipurinol reduces uric acid levels in plasma and urine by inhibiting xanthine oxidase, enzymes catalyzing hydroxide oxidation into xanthine and xanthine into uric acid. In addition, the drug inhibits purine catalosis in some patients with hyperuricemia, and reduces purine biosynthesis through the mechanism of reverse inhibiting hypoxanthine-guanine phosphoribosyltransferase. Other metabolites of allopurinol include Allopurinol-Riboside and Oxipurinol-7 Riboside.

Dynamic pharmacokinetics

allopurinol is active when used orally and quickly absorbed through the above digestive tract. Studies have found Allopurinol in the blood after 30-60 minutes of medication. Born is estimated to change from 67% to 90%. The peak concentration of Allopurinol is usually reached after about 1.5 hours of taking the drug, but it decreases rapidly and it is almost impossible to find after 6 hours. The peak concentration of oxipurinol in plasma is usually reached after 3-5 hours of using allopurinol and is maintained longer.

distribution

Allopurinol is negligible with plasma proteins and therefore changes in links with proteins are not thought to be significantly changing clearance. Allopurinol's distribution integral is about 1.6 l/kg, showing the relatively spacious absorption by tissues. Allopurinol levels in tissue have not been reported in humans, but capable Allopurinol and oxipurinol will be at the highest concentration in the liver and mucous membranes of the active in the active place of xanthine-olidase.

transformation

The main metabolites of allopurinol are oxipurinol. Other metabolites of allopurinol include Allopurinol-Riboside and Oxipurinol-7-Riboside.

Elimination

About 20% Allopurinol after taken is excreted in the feces. Allopurinol elimination is mainly by converting into oxipurinol by xanthine-oidase and aldehyde oxidase, less than 10% of non-metabolic drugs are eliminated in urine. Allopurinol has a semi -discharged time in plasma about 0.5 - 1.5 hours.

oxipurinol is a lesser Xanthine-Oxidase inhibitor than allopurinol, but the semi-waste time in the plasma of oxipurinol is much longer.

Estimates from 13 - 30 hours in humans. Therefore, the Xanthine-Oxidase inhibitor is maintained for about 24 hours after taking a daily dose of Allopurinol. Patients with normal kidney function will accumulate oxipurinol slowly until the concentration of oxipurinol in plasma is stable.

Such patients, using Allopurinol 300 mg/day, will have oxipurinol levels in plasma is 5 - 10 mg/l.

oxipurinol is eliminated in the form of non -metabolized urine but has long semi -exhaust time due to the process of reabsorption in the renal tubules.

The values are reported on the sale time between 13.6 - 29 hours.

The big difference in these values can be explained by a change in research design and/or creatinine clearance in patients.

Patients with renal failure

The clearance of allopurinol and oxipurinol sharply in patients with impaired renal function leads to higher plasma medication concentrations when chronic treatment. Patients with renal failure, have a creatine clearance from 10 - 20 ml/min, with plasma oxipurinol levels about 30 mg/l after prolonged treatment at 300 mg/day. This is the concentration of approximately the concentration achieved when using a dose of 600 mg/day in people with normal kidney function. Therefore, it is necessary to reduce Allopurinol in patients with renal failure.

Old people

The pharmacokinetics of the drug are not affected but the patient has impaired renal function.

Before taking Allopurinol 300mg Stella Pharm reduces the formation of uric acid, treating gout (10 blisters x 10 tablets)

How to use

allopurinol can be used once a day after meals. The drug is well tolerated, especially after eating. If the daily dose exceeds 300 mg and the digestive system cannot be tolerated, the dose can be divided.

Dosage

adults

Allopurinol should be indicated at low doses such as 100 mg/day to reduce the risk of unwanted effects and only increase the dose when responding to unsatisfactory serum urate. Need to be more cautious in patients with impaired renal function. The recommended dose is as follows:

Mild disease: 100 - 200 mg/day.

If the dose calculation is necessary according to body weight, should be calculated according to the dose 2 - 10 mg/kg/day.

Children

Children under 15 years old: 10 - 20 mg/kg/day, a maximum dose of 400 mg/day. Rarely indicated for children unless malignancy (especially leukemia) and certain enzyme disorders such as lesch-nylos syndrome.

Old people

In case there is no specific data, the lowest dose should be used to reduce Urat satisfactory.

kidney failure

Because Allopurinol and its metabolites are eliminated through the kidneys, the impaired renal function can lead to an increase in the time of preserving the drug and/or its metabolites, thus prolonging the semi -discharged time in plasma. In case of severe renal failure, the dose should be lower than 100 mg/day or a single dose of 100 mg daily. If you can monitor oxipurinol levels, the dose should be monitored to maintain plasma oxipurinol levels at less than 100 umol/l (15.2 mg/l). Allopurinol and its metabolites are excluded by blood separator in the kidneys. If the hemorrhage is needed 2-3 times/week, it is necessary to consider the replacement dose of 300 - 400 mg of Allopurinol after each hemorrhage and do not take the drug during the transition period.

liver failure

Should reduce the dose in patients with liver failure. Recommended testing of liver function in the early stages of treatment.

Treatment of high urate levels such as cancer, lesch-anyhan syndrome

Need to adjust the hyperur with hyperuria and/or increase urinary urery with allopurinol before starting cytotoxic therapy. It is important to ensure adequate drinking of water to maintain the maximum urinary effect and alkaline urine to increase the ability to dissolve urate/urinary uric acid. Allopurinol dose should be a lower dose in the recommended dose range. If kidney disease is caused by urate or other pathologies that impaired kidney function, treatment as in patients with renal failure. These steps may reduce the risk of xanthine and/or oxipurinol deposition, which complicates clinical status.

dose adjustment

Adjust the dose based on serum urate concentration and urate/urinary acid levels at appropriate intervals.

Recommended use of appropriate dosage when using 100 mg, 200 mg and 700 mg.

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?

symptoms

There have been reports on the case of using allopurinol up to 22.5 g without any unwanted effect. Symptoms and manifestations include nausea, vomiting, diarrhea and dizziness have been reported in patients using 20 g of allurinol.

Management

Normal support measures can help recover. The large absorption of Allopurinol can lead to significant inhibition of xanthine-oxidase activity, without causing risk reactions except affecting shared drugs, especially with 6-mercaptopurine and/or azathioprine. Drink adequate water to maintain maximum urology to facilitate the excretion of Allopurinol and its metabolites.

Can hematopathy if necessary.

In case of emergency, call the 115 emergency center immediately or go to the nearest local health station.

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 doses to compensate for missed dose.

Side Effects

When using Allopurinol 300 you may experience unwanted effects (ADR):

Common (1/100 ≤ ADR

Skin and subcutaneous tissue: rash.

immunity: hypersensitivity.

digest: vomiting, nausea.

Liver: Examination of abnormal liver function.

Rare (1/10,000 ≤ ADR

Hepatitis: Hepatitis (including liver necrosis and granular hepatitis).

Infections and parasites: pimples.

Blood and lymph: Laes of granulocytes, anemia, platelets. Sleep, headache, taste disorder.

Eye: cataracts, vision loss, retinal degeneration.

ears and ears: Dizziness.

blood vessels: hypertension.

digest: vomit blood, diarrhea and fat, stomatitis, change the habit of walking.

Skin and subcutaneous tissue: angioedema, drug rash, hair loss, hair color change. Management ADR:

Notify the physician 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

Allopurinol 300 is contraindicated in the following cases:

Hypersensitivity to allopurinol or any ingredients in the formula.

Be cautious when using

need to be very careful when taking the drug for patients in the following cases:

Hypersensitivity syndrome, sjs and ten

Allopurinol's hypersensitivity reactions have many different manifestations, including lumpy rash, hypersensitivity syndrome and SJS/Ten. If these reactions appear anytime during treatment, stop using allopurinol immediately. Allurinol should not be appointed in patients with hypersensitivity syndrome and SJS/Ten. Corticosteroids can be used to treat skin hypersensitivity reactions.

The HLA-B*571

Alen HLA-B*5001 has been shown to be associated with the risk of hypersensitivity syndrome and SJS/Ten due to Allopurinol. The frequency of HLA -B*5001 alen among ethnic groups: up to 20% in Han people, 8-15% in Thai people, about 12% in Koreans and 1-2% in Japanese or European people. Considering the HLA-B*5811 allele screening before starting with allopurinol in patient groups is known to have a high ratio of this allele. Chronic kidney disease may increase the risk in these patients. In the case of patients of Han, Thai or welding people who do not carry HLA-B*5001 alleles, it is necessary to carefully evaluate the benefits and consider higher risks that may occur before starting treatment. The use of drugs in this genotype has not been established in other patients.

If the patient carries HLA-B*581 (especially Han, Thai or Korean people), should not use allopurinol unless no other choice of treatment is more optimal and when the benefits are greater than the risk. It is necessary to be very vigilant for the signs of hypersensitivity syndrome or SJS/Ten and patients need to stop treating as soon as the first symptom appears.

SJS/Ten can still occur in patients who do not carry HLA-B*571 alleles regardless of which ethnic they are.

chronic kidney failure

Patients with chronic renal failure and are taking diuretics, especially Thiazide, may increase the risk of hypersensitivity reactions including SJS/Ten due to Allopurinol. It is necessary to be very vigilant for signs of hypersensitivity syndrome or SJS/Ten and patients need to be notified to stop treatment immediately and permanently when the first symptom appears.

liver failure or kidney failure

Needs to reduce the dose in patients with liver failure or kidney failure. Patients who are treating hypertension or heart failure with diuretics or enzyme inhibitors can be impaired with renal function, allopurinol should be used caution with this group of patients.

Incregent uric acid hyperkemis

Allopurinol is not indicated for asymptomatic hyperuricemia. Change of diet and control risk factors that can adjust this condition.

acute gout

Do not start treating with Allopurinol until acute gout attacks completely decrease because it can cause more gout attacks.

In the early stages of treatment with allopurinol, as well as with urinary urinary drugs, acute gout arthritis may appear. Therefore, it is advisable to prevent appropriate anti -inflammatory drugs or colchicine at least 1 month.

If acute gout attacks in patients who are taking Allopurinol, should continue treatment in the same dosage, and treat acute gout attacks with an appropriate anti -inflammatory drug.

Xanthine deposits

When the urate formation rate increases significantly (such as malignant disease and the treatment of malignant disease, Lesch-Nyhan syndrome), the Xanthine concentration in the urine in some cases may increase enough to cause deposition in the urinary tract. This risk can be minimized by drinking enough water to dilute urine to optimize.

The obstruction of kidney stones caused by uric acid

Treatment is suitable for allopurinol to melt large uric acid stones, the ability to clog ureter is less likely.

thyroid disorders

In a long -term study, TSH increased (> 5.5 IU/ml) in long -term treatment patients with allopurinol (5.8%). Caution should be used when using allopurinol for patients with changes in thyroid function.

excipients

Allopurinol Stella 300 mg contains lactose excipients. Do not use this medication for patients with rare genetic problems galactose intolerance, total lactase enzyme deficiency or poor absorption of glucose-galactose.

Allopurinol Stella 300 mg contains Sunset Yellow Lake excipients, which can cause allergic reactions.

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

Due to unwanted effects such as drowsiness, dizziness and loss of movement air conditioning have been reported in patients who are using allopurinol, patients should be cautious before driving, use machinery or participate in dangerous activities until it is sure that Allopurinol does not cause beneficial effects.

Use drugs for women during pregnancy and lactation

Pregnant women

There is no full evidence of Allopurinol's safety in pregnant women, although the drug has been widely used for many years without any obvious bad consequences. Only use drugs in pregnant women when there is no safer replacement therapy and the disease provides a bad risk to the mother or fetus.

breastfeeding women

Allopurinol and its metabolic oxipurinol are excreted through breast milk. Allopurinol levels of 1.4 mg/l and oxipurinol 53.7 mg/l have been found in breast milk in a woman using a dose of 300 mg/day. However, there is no relevant data on Allopurinol effects its substances on breastfeeding. No total recommendations for using allopurinol during breastfeeding.

Drug interaction

6-mercaptopurine and azathioprine: Azathioprine converts into 6-mercaptopurine this substance is inactivated by xanthine oxidase. When using 6-mercaptopurine or azathioprine simultaneously with Allopurinol, only 1/4 of the usual dose of 6-Mercaptopurine or Azathioprine because of the Xanthine Oxidase inhibitors will prolong their effects.

vidarabine (adenine arabinoside): vidarabine's waste time increases when used simultaneously with allopurinol. Be careful when used simultaneously to detect signs of toxicity increased.

salicylate and uric acid elimination drugs through urine: oxipurinol, the main metabolites of allopurinol and have the effect of treatment, excreted through the kidney in the same way as urate. Uric acid excreted drugs such as probenecid or high doses of salicylate can accelerate the excretion of oxipurinol. This may reduce the treatment effect of Allopurinol but the level should be assessed in each case.

chlorpropamide: If Allopurinol is simultaneously used with chlorpropamide when the renal function is poor, it can increase the risk of prolonged hypoglycemia because allopurinol and chlorpropamide can compete in the renal tubules.

Coumarin anti -copper drugs: Rarely report on increasing the effects of warfarin and other anticoagulants when used simultaneously with allopurinol, so patients use anticoagulants should be closely monitored.

Phenytoin: Allopurinol may inhibit phenytoin oxidation in the liver but the clinical significance has not been proven.

Theophyllline: Theophylline's metabolic inhibitor has been reported. The mechanism of interaction can be explained by Xanthine Oxidase involved in theophylline's biological transformation. Theophylline concentration should be monitored in patients starting to treat or when increasing the dose of allurinol.

ampicillin/amoxicillin: The increase in the frequency of skin rash has been reported in patients using ampicillin or amoxicillin simultaneously with allopurinol compared to those who do not take both drugs. The cause is unknown. However, it is recommended that patients who use Allopurinol need to replace ampicillin or amoxicillin if possible.

Cell inhibitors: When using Allopurinol and cell inhibitors (such as cyclophosphamide, doxorubicin, BLEOYMICIN, PROCARBAZINE, Halogen alkyl), blood disorders occur more often than when used individually these substances. Therefore, it is necessary to regularly monitor the blood formula.

ciclosporin: Reports show that plasma ciclosporin levels may increase when treated simultaneously with allopurinol.

Didanosine: In healthy volunteers and HIV patients with Didanosine, the value of cmax and AUC of the didanosine in plasma is approximately the same when treated simultaneously with Allopurinol (300 mg/day) without affecting the sale time. There is no simultaneous use of these 2 drugs. If required to use simultaneously, Didanosine is required and closely monitored.

Diuretics: Interaction between Allopurinol and Furosemide increases the serum urate level and oxipurinol levels in plasma has been reported. Increasing hypersensitivity risk when using allopurinol with diuretics, namely thiazide, especially in patients with renal failure.

Enzyme inhibitors: increased the risk of hypersensitivity when taking allopurinol with transferred enzyme inhibitors, especially in patients with renal failure.

aluminum hydroxyd: If used simultaneously aluminum hydroxyd, allopurinol may be reduced activity. These two drugs should be used at least 3 hours apart.

Storage

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

To be out of reach of children, read the instructions carefully before use.

Other drugs

Disclaimer

Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.