What are the primary uses of allopurinol. How should allopurinol be dosed. What are the common and serious side effects of allopurinol. How does allopurinol interact with other medications.

Understanding Allopurinol: A Comprehensive Overview

Allopurinol is a widely prescribed medication that plays a crucial role in managing various conditions related to elevated uric acid levels in the body. This article delves into the essential aspects of allopurinol, including its uses, dosage recommendations, potential side effects, and important interactions with other medications.

The Primary Uses of Allopurinol

Allopurinol is primarily used to treat conditions associated with high uric acid levels in the blood and urine. These conditions include:

• Gout
• Recurrent kidney stones
• Elevated serum uric acid levels
• Kidney damage
• Complications from cancer chemotherapy
• Psoriasis-related uric acid buildup

The medication works by inhibiting xanthine oxidase, an enzyme responsible for uric acid production. By reducing uric acid levels, allopurinol helps prevent the formation of uric acid crystals that can lead to painful gout attacks and kidney stones.

Can allopurinol be used preventatively?

Yes, allopurinol can be prescribed as a preventive measure for individuals at high risk of developing gout or recurrent kidney stones. It is particularly beneficial for those with a history of these conditions or those undergoing treatments that may increase uric acid levels, such as certain chemotherapies.

Dosage Guidelines for Allopurinol

Allopurinol is available in oral tablet form and as an intravenous injection. The oral tablets are marketed under brand names such as Zyloprim and Lopurin, as well as in generic form. Dosage recommendations vary based on the condition being treated and individual patient factors.

How is the appropriate dosage determined?

The appropriate dosage is determined by several factors, including:

• The specific condition being treated
• The severity of uric acid elevation
• The patient’s kidney function
• Individual response to the medication

Typically, treatment begins with a lower dose, which may be gradually increased to achieve the desired uric acid levels. Regular blood tests are essential to monitor uric acid levels and adjust the dosage as needed.

Common and Serious Side Effects of Allopurinol

Like all medications, allopurinol can cause side effects. It’s crucial for patients to be aware of both common and potentially serious adverse reactions.

What are the most common side effects of allopurinol?

The more frequently reported side effects include:

• Skin rash (mild)
• Diarrhea
• Nausea
• Changes in liver function test results
• Gout flare-up (particularly at the beginning of treatment)

These side effects are generally mild and often resolve on their own as the body adjusts to the medication. However, if they persist or worsen, it’s important to consult a healthcare provider.

What serious side effects require immediate medical attention?

While rare, some serious side effects of allopurinol can occur and require immediate medical intervention. These include:

1. Severe skin rash: This can be life-threatening and may present with symptoms such as itchy hives, red or purple-colored spots, scaly skin, fever, chills, trouble breathing, or swelling of the face or throat.
2. Liver injury: Symptoms may include fatigue, loss of appetite, weight loss, pain in the upper right abdomen, dark urine, or yellowing of the skin or eyes (jaundice).

If any of these serious side effects occur, patients should stop taking allopurinol immediately and seek emergency medical care.

Allopurinol Interactions with Other Medications

Allopurinol can interact with various medications, potentially altering their effectiveness or increasing the risk of side effects. It’s crucial for patients to inform their healthcare providers about all medications, supplements, and herbs they are taking.

Which medications are known to interact with allopurinol?

Some notable interactions include:

• Azathioprine and mercaptopurine: Allopurinol can increase the levels of these immunosuppressants, potentially leading to severe toxicity.
• Warfarin: Allopurinol may enhance the anticoagulant effect of warfarin, increasing the risk of bleeding.
• Certain antibiotics: The combination of allopurinol with ampicillin or amoxicillin may increase the risk of skin rash.
• Diuretics: Some diuretics can increase uric acid levels, potentially counteracting the effects of allopurinol.

Healthcare providers may need to adjust dosages or consider alternative medications to manage these interactions effectively.

Precautions and Special Considerations

While allopurinol is generally safe and effective when used as prescribed, certain precautions and special considerations are important to ensure optimal treatment outcomes and minimize risks.

What precautions should patients take when using allopurinol?

Important precautions include:

• Adequate hydration: Patients should drink at least 3.4 liters (14 cups) of fluids daily to help prevent uric acid crystal formation and promote urine flow.
• Monitoring drowsiness: Allopurinol can cause drowsiness, so patients should avoid driving or operating machinery until they know how the medication affects them.
• Regular check-ups: Periodic liver function tests and uric acid level monitoring are essential to ensure the medication is working effectively and not causing liver damage.
• Allergic reaction awareness: Patients should be vigilant for signs of allergic reactions, particularly skin rashes, and seek immediate medical attention if they occur.

Are there specific populations that require special consideration?

Yes, certain groups may require additional monitoring or dosage adjustments:

• Patients with kidney disease: Dosage may need to be reduced due to decreased drug clearance.
• Pregnant or breastfeeding women: The safety of allopurinol during pregnancy and breastfeeding is not well-established, and its use should be carefully weighed against potential risks.
• Elderly patients: They may be more susceptible to side effects and may require lower initial doses.
• Patients with a history of liver disease: Close monitoring of liver function is crucial.

Maximizing the Benefits of Allopurinol Therapy

To achieve the best results from allopurinol treatment, patients should adhere to certain guidelines and lifestyle modifications in addition to taking the medication as prescribed.

How can patients optimize their allopurinol treatment?

Consider the following strategies:

1. Consistent medication adherence: Take allopurinol at the same time each day to maintain steady blood levels.
2. Dietary modifications: Reduce intake of high-purine foods and beverages, such as red meat, organ meats, and alcohol, especially beer.
3. Weight management: Maintain a healthy weight, as excess weight can contribute to elevated uric acid levels.
4. Regular exercise: Engage in moderate physical activity to help control weight and improve overall health.
5. Stress reduction: Practice stress-management techniques, as stress can potentially trigger gout attacks.

By combining these lifestyle changes with proper medication use, patients can significantly enhance the effectiveness of their allopurinol therapy.

Long-term Outlook and Management

Allopurinol is often a long-term treatment, and understanding the long-term outlook and management strategies is crucial for patients and healthcare providers alike.

What is the long-term prognosis for patients on allopurinol?

For most patients, the long-term outlook with allopurinol therapy is positive. When used consistently and in combination with appropriate lifestyle changes, allopurinol can effectively control uric acid levels, reduce the frequency of gout attacks, and prevent complications such as kidney stones. However, it’s important to note that:

• Allopurinol is not a cure for gout or other uric acid-related conditions, but rather a management tool.
• Long-term use requires ongoing monitoring and potential dosage adjustments.
• Some patients may experience an initial increase in gout attacks when starting treatment, but this typically subsides as uric acid levels stabilize.

How should long-term allopurinol therapy be managed?

Effective long-term management involves:

1. Regular check-ups: Schedule periodic appointments with your healthcare provider to assess treatment efficacy and monitor for potential side effects.
2. Uric acid level monitoring: Regular blood tests to ensure uric acid levels remain within the target range.
3. Liver and kidney function tests: Periodic testing to detect any potential organ damage early.
4. Medication review: Regular evaluation of all medications to check for potential interactions with allopurinol.
5. Lifestyle maintenance: Continual adherence to dietary and lifestyle modifications that support uric acid control.

By maintaining open communication with healthcare providers and actively participating in their treatment plan, patients can achieve optimal long-term outcomes with allopurinol therapy.

Side Effects, Dosage, Uses & More

Highlights for allopurinol

1. Allopurinol oral tablet is available as a generic drug and as brand-name drugs. Brand names: Zyloprim and Lopurin.
2. Allopurinol is also given as an injection by a healthcare professional in the hospital.
3. Allopurinol oral tablet is used to treat gout, elevated serum uric acid levels, and recurrent kidney stones.

• Severe skin rash: This drug may cause a severe, life-threatening skin rash. If you have itchiness, trouble breathing, or swelling of your face or throat, stop taking this drug and call your doctor right away.
• Liver injury: This drug may cause changes in liver function test results and liver failure. This may be fatal. If you develop liver problems, your doctor may have you stop taking allopurinol.
• Drowsiness: This drug can cause drowsiness. You shouldn’t drive, use machinery, or do other tasks that require alertness until you know how it affects you.
• Fluid intake: You should drink at least 3.4 liters (14 cups) of fluids each day. This will help you urinate at least 2 liters (2 quarts) per day. This can help prevent uric acid crystals from forming and blocking your urine flow. Ask your doctor how to measure how much you urinate.

Allopurinol oral tablet is a prescription drug that’s available as the brand-name drugs Zyloprim and Lopurin. It’s also available as a generic drug. Generic drugs usually cost less. In some cases, they may not be available in every strength or form as the brand-name version.

Allopurinol also comes in an intravenous (IV) form, which is only given by a healthcare professional.

Allopurinol may be used as part of a combination therapy. This means you may need to take it with other medications.

Why it’s used

Allopurinol is used to decrease uric acid levels in the blood and urine of people with high uric acid levels. High uric acid levels may be caused by the following:

• gout
• kidney stones, kidney damage, or treatment with dialysis
• cancer chemotherapy
• psoriasis
• use of diuretics (water pills)
• a diet high in soft drinks, beef, steak, salami, or beer

How it works

Allopurinol belongs to a class of drugs called xanthine oxidase inhibitors. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

Allopurinol decreases blood and urine uric acid levels by blocking xanthine oxidase. This is an enzyme that helps make uric acid. High levels of uric acid in your blood or urine can cause gout or kidney stones.

Allopurinol oral tablet may cause drowsiness. You shouldn’t drive, use machinery, or do other tasks that require alertness until you know how allopurinol affects you. It can also cause other side effects.

More common side effects

The more common side effects of allopurinol oral tablet can include:

• skin rash
• diarrhea
• nausea
• changes in your liver function test results
• gout flare-up (if you have gout)

If you develop a skin rash, talk your doctor right away. You should not continue taking allopurinol if you develop a rash. Other mild side effects may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk with your doctor or pharmacist.

Serious side effects

Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

• Severe skin rash. Symptoms can include:
  • itchy hives (raised bumps on your skin)
  • red or purple-colored spots on your skin
  • scaly skin
  • fever
  • chills
  • trouble breathing
  • swelling of your face or throat
• Liver injury. Symptoms can include:
  • tiredness
  • lack of appetite
  • weight loss
  • right upper abdominal area pain or discomfort
  • jaundice (dark-colored urine or yellowing of your skin or the whites of your eyes)

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare professional who knows your medical history.

Allopurinol oral tablet can interact with other medications, vitamins, or herbs you may be taking. An interaction is when a substance changes the way a drug works. This can be harmful or prevent the drug from working well.

To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk with your doctor or pharmacist.

Interactions that increase your risk of side effects

• Side effects from allopurinol: Taking allopurinol with certain medications raises your risk of side effects from allopurinol. This is because the amount of allopurinol in your body is increased. Examples of these drugs include:
  • Ampicillin or amoxicillin. You may have an increased risk of a skin rash.
  • Thiazide diuretics, such as hydrochlorothiazide. You may have an increased risk of allopurinol side effects. These include skin rash, diarrhea, nausea, changes in your liver function test results, and gout flare-ups.
• Side effects from other drugs: Taking allopurinol with certain medications raises your risk of side effects from these drugs. Examples of these drugs include:
  • Mercaptopurine. Allopurinol can increase the blood levels of mercaptopurine in your body. It does this by blocking one of the enzymes used to break down mercaptopurine. This can cause severe side effects from mercaptopurine. Your doctor may reduce your mercaptopurine dose.
  • Azathioprine. Allopurinol can increase the blood levels of azathioprine in your body. It does this by blocking one of the enzymes used to break down azathioprine. This can cause severe side effects from azathioprine. Your doctor may reduce your azathioprine dosage.
  • Cyclosporine. Taking allopurinol with cyclosporine may increase cyclosporine levels in your body. Your doctor should monitor your cyclosporine levels and adjust your dose if needed.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions. This information is not a substitute for medical advice. Always speak with your healthcare professional about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.

This drug comes with several warnings.

Allergy warning

Allopurinol can cause a severe allergic reaction. Symptoms can include:

• itchy hives (raised bumps on your skin)
• red or purple-colored spots on your skin
• scaly skin
• fever
• chills
• trouble breathing
• swelling of your face or throat

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call 911 or go to the nearest emergency room. Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

When to call your doctor

Call your doctor if your gout symptoms get worse while you’re taking this drug. When you first start taking this medication, it can cause your gout to flare up. Your doctor may give you nonsteroidal anti-inflammatory drugs (NSAIDs) or colchicine to treat the flare-up and prevent more flares. You may need to take these drugs for up to 6 months.

Warnings for certain groups

For people with kidney problems: If you have kidney problems or a history of kidney disease, you may not be able to clear this drug from your body well. This may increase the levels of allopurinol in your body and cause more side effects. This medication may also decrease your kidney function. This would make your kidney disease worse.

For pregnant women: Allopurinol is a category C pregnancy drug. That means two things:

1. Research in animals has shown adverse effects to the fetus when the mother takes the drug.
2. There haven’t been enough studies done in humans to be certain how the drug might affect the fetus.

Talk with your doctor if you’re pregnant or planning to become pregnant. This drug should only be used if the potential benefit justifies the potential risk to the fetus.

For women who are breastfeeding: Allopurinol passes into breast milk and may cause side effects in a child who is breastfed. Talk with your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

For seniors: The kidneys of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stays in your body for a longer time. This raises your risk of side effects.

For children: This medication hasn’t been studied and shouldn’t be used in people younger than 18 years for the treatment of gout or kidney stones.

This dosage information is for allopurinol oral tablet. All possible dosages and drug forms may not be included here. Your dosage, drug form, and how often you take the drug will depend on:

• your age
• the condition being treated
• how severe your condition is
• other medical conditions you have
• how you react to the first dose

Forms and strengths

Generic: Allopurinol

• Form: oral tablet
• Strengths: 100 mg, 300 mg

Brand: Zyloprim

• Form: oral tablet
• Strengths: 100 mg, 300 mg

Brand: Lopurin

• Form: oral tablet
• Strengths: 100 mg, 300 mg

Dosage for gout

Adult dosage (ages 18–64 years)

• Typical starting dose: 100 mg per day
• Dose adjustments: Your doctor may increase your dose by 100 mg per week until you’ve reached the desired level of serum uric acid.
• Usual dose:
  • Mild gout: 200–300 mg per day
  • Moderate to severe gout: 400–600 mg per day
• Maximum dose: 800 mg per day taken in divided doses

Child dosage (ages 0–17 years)

This medication hasn’t been studied and shouldn’t be used in people younger than 18 years for this condition.

Senior dosage (ages 65 years and older)

The kidneys of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stays in your body for a longer time. This raises your risk of side effects.

Your doctor may start you on a lowered dose or a different dosing schedule. This can help keep levels of this drug from building up too much in your body.

Special considerations

• For people with kidney disease: Depending on how well your kidneys are working, your doctor will lower your dosage. Your doctor will decide your dosage based on your creatinine clearance. This is a measure of your kidney function.

Dosage for elevated serum uric acid levels due to cancer treatments

Adult dosage (ages 18–64 years)

600–800 mg per day for 2 or 3 days.

Child dosage (ages 11–17 years)

600–800 mg per day for 2 or 3 days

Child dosage (ages 6–10 years)

300 mg per day. Your doctor will adjust your dose as needed based on your serum uric acid level.

Child dosage (ages 0–5 years)

150 mg per day. Your doctor will adjust your child’s dose as needed based on your serum uric acid level.

Senior dosage (ages 65 years and older)

The kidneys of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stays in your body for a longer time. This raises your risk of side effects.

Your doctor may start you on a lowered dose or a different dosing schedule. This can help keep levels of this drug from building up too much in your body.

Special considerations

• For people with kidney disease: Depending on how well your kidneys are working, your doctor will lower your dose. Your doctor will decide your dosage based on your creatinine clearance. This is a test that measures your kidney function.

Dosage for recurrent kidney stones

Adult dosage (ages 18–64 years)

Typical dosage is 200–300 mg per day taken in a single or divided doses.

Child dosage (ages 0–17 years)

This medication hasn’t been studied and shouldn’t be used in people younger than 18 years for this condition.

Senior dosage (ages 65 years and older)

The kidneys of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stays in your body for a longer time. This raises your risk of side effects.

Your doctor may start you on a lowered dose or a different dosing schedule. This can help keep levels of this drug from building up too much in your body.

Special considerations

• For people with kidney disease: Depending on how well your kidneys are working, your doctor will lower your dose. Your doctor will decide your dosage based on your creatinine clearance. This is a test that measures your kidney function.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always to speak with your doctor or pharmacist about dosages that are right for you.

Allopurinol oral tablet is used for long-term treatment. It comes with serious risks if you don’t take it as prescribed.

If you stop taking the drug suddenly or don’t take it at all: The uric acid levels in your blood or urine will stay high. If you have gout or kidney stones, you’ll still have symptoms of your condition.

If you miss doses or don’t take the drug on schedule: Your medication may not work as well or may stop working completely. For this drug to work well, a certain amount needs to be in your body at all times.

If you take too much: You could have dangerous levels of the drug in your body. Symptoms can include:

• skin rash
• diarrhea
• nausea
• changes in your liver function test results
• gout flare-up (if you have gout)

If you think you’ve taken too much of this drug, call your doctor or local poison control center. If your symptoms are severe, call 911 or go to the nearest emergency room right away.

What to do if you miss a dose: Take your dose as soon as you remember. But if you remember just a few hours before your next scheduled dose, take only one dose. Never try to catch up by taking two doses at once. This could result in dangerous side effects.

How to tell if the drug is working: Your doctor will test your uric acid levels to check if this drug is working. Your blood uric acid levels will decrease about 1–3 weeks after you start taking this drug. Your doctor will also ask you about how much fluids you drink and how much fluids you urinate.

Right after you start taking this drug, you may have gout flares. Over time, your symptoms of gout may start to go away.

Keep these considerations in mind if your doctor prescribes allopurinol oral tablet for you.

General

• Take this drug at the time(s) recommended by your doctor.
• You can take allopurinol with or without food.
• Taking this drug after a meal and with lots of water may reduce your chance of upset stomach.
• You can cut or crush the allopurinol tablet.
• Not every pharmacy stocks this drug. When filling your prescription, be sure to call ahead to make sure your pharmacy carries it.

Storage

• Store allopurinol at room temperature. Keep it between 68°F and 77°F (20°C and 25°C).
• Keep it away from light.
• Don’t store this medication in moist or damp areas, such as bathrooms.

Refills

A prescription for this medication is refillable. You should not need a new prescription for this medication to be refilled. Your doctor will write the number of refills authorized on your prescription.

Travel

When traveling with your medication:

• Always carry your medication with you. When flying, never put it into a checked bag. Keep it in your carry-on bag.
• Don’t worry about airport X-ray machines. They can’t hurt your medication.
• You may need to show airport staff the pharmacy label for your medication. Always carry the original prescription-labeled box with you.
• Don’t put this medication in your car’s glove compartment or leave it in the car. Be sure to avoid doing this when the weather is very hot or very cold.

Clinical monitoring

You and your doctor should monitor certain health issues. This can help make sure you stay safe while you take this drug. These issues include:

• Kidney function. Your doctor may do blood tests to check how well your kidneys are working. If your kidneys aren’t working well, your doctor may lower your dose of this drug.
• Liver function. Your doctor may do blood tests to check how well your liver is working. If your liver isn’t working well, your doctor may lower your dose of this drug.
• Uric acid levels. Your doctor may do blood tests to check your uric acid. This will help your doctor tell how well this drug is working.

Your diet

If you have repeat kidney stones, your doctor may tell you to eat a special diet. This diet will be low in animal protein (meat), sodium, sugar, and oxalate-rich foods (such as, spinach, beets, celery, and green beans).

Your diet should also be high in fiber, and you should drink plenty of water. You may also need to watch your calcium intake.

There are other drugs available to treat your condition. Some may be better suited for you than others. Talk with your doctor about other drug options that may work for you.

Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Allopurinol: MedlinePlus Drug Information

pronounced as (al oh pure’ i nole)

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Allopurinol is used to treat gout (a type of arthritis in which uric acid, a naturally occurring substance in the body, builds up in the joints and causes sudden attacks of redness, swelling, pain, and heat in one or more joints). Allopurinol is also used to treat high levels of uric acid that builds up in the blood as tumors break down in people with certain types of cancer who are being treated with chemotherapy medications. It is also used to treat kidney stones that have come back in people who have high levels of uric acid in their urine. Allopurinol is in a class of medications called xanthine oxidase inhibitors. It works by reducing the production of uric acid in the body. High levels of uric acid may cause gout attacks or kidney stones. Allopurinol is used to prevent gout attacks, not to treat them once they occur.

Allopurinol comes as a tablet to take by mouth. It is usually taken once or twice a day, preferably after a meal. To help you remember to take allopurinol, take it around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take allopurinol exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Your doctor will probably start you on a low dose of allopurinol and gradually increase your dose, not more than once a week.

It may take several months or longer before you feel the full benefit of allopurinol. Allopurinol may increase the number of gout attacks during the first few months that you take it, although it will eventually prevent attacks. Your doctor may prescribe another medication such as colchicine to prevent gout attacks for the first few months you take allopurinol. Continue to take allopurinol even if you feel well. Do not stop taking allopurinol without talking to your doctor.

This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.

Before taking allopurinol,

• tell your doctor and pharmacist if you are allergic to allopurinol, any other medications, or any of the ingredients in allopurinol tablets. Ask your pharmacist for a list of the ingredients.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking while you are taking allopurinol. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• tell your doctor if you have or have ever had high blood pressure, diabetes, kidney or liver disease or heart failure.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking allopurinol, call your doctor.
• you should know that allopurinol may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
• ask your doctor about the safe use of alcoholic beverages while you are taking allopurinol.

Drink at least eight 8-ounce (240-milliter) cups of water or other liquids each day while taking allopurinol unless directed to do otherwise by your doctor.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Allopurinol may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• nausea
• diarrhea
• drowsiness

Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them, stop taking allopurinol and call your doctor immediately or get emergency treatment:

• rash, itching, or hives
• peeling, blistering, or shedding skin
• red or purple spots on skin
• painful urination
• blood in the urine
• irritation of the eyes
• swelling of the lips or mouth
• fever or flu-like symptoms
• swollen glands
• yellowing of the skin or eyes, pain in the upper right part of the stomach, nausea, vomiting, itching, or extreme tiredness

Allopurinol may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www. fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

• Lopurin^®
• Zyloprim^®

Last Revised – 07/15/2022

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Allopurinol – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English name

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Allopurinol

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• The use of the substance Allopurinol

• Contraindications

• Application restrictions

• Use during pregnancy and lactation

• Side effects of Allopurinol

• Interaction

• Overdose

• Dosage and administration

• Precautionary measures

• Trade names with the active substance Allopurinol

Structural formula

Russian name

Allopurinol

English name

Allopurinol

Latin name

Allopurinolum ( born Allopurinoli)

Chemical name

1,5-Dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

General formula

C ₅ H _{4 9 0074 N 4 O}

Pharmacological group of the substance Allopurinol

Drugs affecting the metabolism of uric acid

Nosological classification

ICD-10 code list

• E79Purine and pyrimidine metabolism disorders

• E79. 1 Lesch-Nychen syndrome

• L40 Psoriasis

• M10 Gout

• M10.0 Idiopathic gout

• M10. 4 Other secondary gout

• N20.9 Urinary stones, unspecified

• T94.1 Sequelae of injuries, unspecified

• Y42.0 Glucocorticoids and their synthetic analogues

• Z51. 0 Course of radiotherapy

• Z51.1 Chemotherapy for neoplasm

CAS code

315-30-0

Pharmacological action

Pharmacological action –

hypouricemic , antigout .

Characteristics

White or creamy white fine crystalline powder, insoluble in water and alcohol.

Pharmacology

Inhibits xanthine oxidase, disrupts the conversion of hypoxanthine to xanthine and xanthine to uric acid; thus limits the synthesis of uric acid. Lowers the content of urates in the blood serum and prevents their deposition in tissues, incl. renal. Reduces the excretion of uric acid in the urine and increases the more readily soluble hypoxanthine and xanthine.

Almost completely (90%) absorbed from the gastrointestinal tract. In the liver, under the influence of xanthine oxidase, it turns into alloxanthin, which also prevents the formation of uric acid. max”>C _max of allopurinol is achieved after 1.5 hours, alloxanthin – after 4.5 hours after a single dose. 1/2″> T _1/2 allopurinol is 1-2 hours, alloxanthin – about 15 hours. About 20% of the dose is excreted through the intestines; the rest of allopurinol and its metabolites – by the kidneys.

Application of the substance Allopurinol

Hyperuricemia: primary and secondary gout, urolithiasis with urate formation, diseases accompanied by increased breakdown of nucleoproteins, including hematoblastomas, cytostatic and radiation therapy of tumors, psoriasis, traumatic toxicosis, corticosteroid therapy to prevent uric acid nephropathy, Lesch-Nyhan syndrome, purine disorders metabolism in children, urolithiasis and calcium oxalate stone formation in hyperuricosuria (prevention and treatment).

Contraindications

Hypersensitivity, liver failure, chronic renal failure (azotemia stage), primary (idiopathic) hemochromatosis, asymptomatic hyperuricemia, acute gout attack, pregnancy, breastfeeding.

Restrictions for use

Renal failure, chronic heart failure, diabetes mellitus, arterial hypertension, children’s age (up to 14 years of age, it is prescribed only during cytostatic therapy of leukemia and other malignant diseases, as well as symptomatic treatment of enzyme disorders).

Use in pregnancy and lactation

FDA fetal category – C.

Side effects of the substance Allopurinol

From the gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea , stomatitis, hyperbilirubinemia, cholestatic jaundice, increased activity of hepatic transaminases and alkaline phosphatase; rarely – hepatonecrosis, hepatomegaly, granulomatous hepatitis.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): pericarditis, increased blood pressure, bradycardia, vasculitis, agranulocytosis, anemia, aplastic anemia, thrombocytopenia, eosinophilia, leukocytosis, leukopenia.

From the musculoskeletal system: myopathy, myalgia, arthralgia.

From the nervous system and sensory organs: headache, peripheral neuropathy, neuritis, paresthesia, paresis, depression, drowsiness, taste perversion, loss of taste, visual impairment, cataract, conjunctivitis, amblyopia.

From the genitourinary system: acute renal failure, interstitial nephritis, increased urea concentration (in patients with initially reduced kidney function), peripheral edema, hematuria, proteinuria, reduced potency, infertility, gynecomastia.

Allergic reactions: skin rash, pruritus, urticaria, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), purpura, bullous dermatitis, eczematous dermatitis, exfoliative dermatitis; rarely – bronchospasm.

Other: furunculosis, alopecia, diabetes mellitus, dehydration, epistaxis, necrotizing tonsillitis, lymphadenopathy, hyperthermia, hyperlipidemia.

Interaction

Increases blood concentration and toxicity of azathioprine, mercaptopurine, methotrexate, xanthines (theophylline, aminophylline), hypoglycemic effect of chlorpropamide, anticoagulant – indirect anticoagulants. Pyrazinamide, salicylates, uricosuric agents, thiazide diuretics, furosemide, ethacrynic acid weaken the hypouricemic effect. Against the background of amoxicillin, ampicillin, bacampicillin, the likelihood of a skin rash increases.

Overdose

Symptoms: nausea, vomiting, diarrhea, dizziness, oliguria.

Treatment: forced diuresis, hemo- and peritoneal dialysis.

Dosage and administration

Inside. The dose of the drug is selected individually, the effectiveness of therapy is monitored at the initial stages by re-determining the level of uric acid in the blood (desired level <0.36 mmol / l). A decrease in the level of uric acid under the influence of the drug occurs after 24-48 hours. Beginning with 100 mg / day, once, then the dose is gradually increased. A daily dose of more than 300 mg should be divided into several doses.

Adults with mild disease — 100-200 mg/day, with moderate disease — 300-600 mg/day, with severe disease — 700-900 mg/day. Children from 10 to 15 years old – 10-20 mg / kg / day (up to 400 mg / day maximum), up to 10 years old – 5-10 mg / kg / day. In patients with impaired renal excretory function, the daily dose should be reduced. Elderly patients are recommended the lowest doses.

Precautions

Maintain urine output of at least 2 liters per day and neutral or slightly alkaline urine, as this prevents urate precipitation and calculus formation. You should not start therapy until the acute attack of gout is completely relieved; during the first month of treatment, prophylactic NSAIDs or colchicine are recommended; in the event of an acute attack of gout during treatment, anti-inflammatory drugs are additionally prescribed. In case of impaired renal and hepatic function (increased risk of side effects), the dose is reduced. The first 6-8 weeks of treatment requires a regular study of liver function, with blood diseases, regular laboratory monitoring is required.

If a skin rash appears, the drug is canceled, after the disappearance of a mild rash, it is possible to re-administer the drug, if it recurs, the treatment is immediately stopped.

The use of azathioprine or 6-mercaptopurine in the presence of allopurinol allows a 4-fold reduction in their doses. Combine with caution with vidarabine.

Trade names with active substance Allopurinol

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Lek. form
All lek. forms substance-powder tablets

Dosage
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Manufacturer
All manufacturers Avexima Siberia LLC Beijing Tayang Pharmaceutical Industry Co. Irbit Chemical and Pharmaceutical Plant Ozon JSC Organika LLC Organika JSC EGIS JSC Pharmaceutical Plant

Allopurinol instructions for use: indications, contraindications, side effects – description of Allopurinol tab. 300 mg: 30 or 50 pcs. (45612)

💊 Composition of Allopurinol ✅ Use of Allopurinol Save Search for analogues Interaction Description of the active ingredients of the preparation Allopurinol (Allopurinol) The scientific information provided is general and cannot be used to make decisions. decisions about the use of a particular drug. Update date: 2020.03.30 Marketing authorization holder: ORGANIKA JSC (Russia) ATX code: M04AA01 (Allopurinol) Active substance: allopurinol (allopurinol) Rec.INN registered by WHO Dosage form Allopurinol Tab. 300 mg: 30 or 50 pcs. reg. No.: LP-003429 dated 01/25/16 – Active Date of re-registration: 02. 11.16 Release form, packaging and composition drug Allopurinol Tablets white or almost white, round, flat-cylindrical, with chamfer and notch. Excipients : lactose monohydrate (milk sugar) – 49 mg, microcrystalline cellulose – 20 mg, sodium carboxymethyl starch (primogel) – 20 mg, food gelatin – 5 mg, magnesium stearate – 4 mg, colloidal silicon dioxide (aerosil) – 2 mg. 10 pcs. – cellular contour packings (3) – packs of cardboard. 10 pcs. – cellular contour packings (5) – packs of cardboard. 30 pcs. – jars of dark glass (1) – packs of cardboard. 50 pcs. – jars of dark glass (1) – packs of cardboard. Clinical and pharmacological group: A drug that affects the metabolism of uric acid. Antigout drug Pharmacotherapeutic group: Antigout agent, xanthine oxidase inhibitor Pharmacological action Agent that disrupts the synthesis of uric acid. It is a structural analogue of hypoxanthine. Inhibits the enzyme xanthine oxidase, which is involved in the conversion of hypoxanthine to xanthine and xanthine to uric acid. This is due to a decrease in the concentration of uric acid and its salts in body fluids and urine, which contributes to the dissolution of existing urate deposits and prevents their formation in tissues and kidneys. When taking allopurinol, the excretion of hypoxanthine and xanthine in the urine increases. Pharmacokinetics After oral administration, almost completely (90%) is absorbed from the gastrointestinal tract. It is metabolized with the formation of alloxanthin, which retains the ability to inhibit xanthine oxidase for a sufficiently long time. C max of allopurinol in blood plasma is achieved on average after 1.5 hours, alloxanthin – 4.5 hours after a single dose. T 1/2 allopurinol is 1-2 hours, alloxanthin – about 15 hours. About 20% of the dose taken is excreted through the intestines, the rest – by the kidneys. Indications of the active substances of the drug Allopurinol Treatment and prevention of gout and hyperuricemia of various origins (including in combination with nephrolithiasis, renal failure, urate nephropathy). Recurrent mixed calcium oxalate kidney stones in the presence of hyperuricosuria. Increased formation of urates due to enzyme disorders. Prevention of acute nephropathy with cytostatic and radiation therapy of tumors and leukemia, as well as with complete therapeutic starvation. Open list of ICD-10 codes E79 Purine and pyrimidine metabolism disorders M10 Gout N20 Kidney and ureter stones N21 Lower urinary tract stones Y43. 1 Antitumor antimetabolites Y43.2 Anticancer natural preparations Y43.3 Other anticancer drugs Y84.2 Radiological procedure and radiotherapy Dosing regimen The method of administration and dosing regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. Compliance of the dosage form of a particular drug with indications for use and dosing regimen should be strictly observed. Set individually, under the control of the concentration of urate and uric acid in the blood and urine. Adults when taken orally – 100-900 mg / day, depending on the severity of the disease. The frequency of administration is 2-4 times / day after meals. Children under the age of 15 – 10-20 mg / kg / day or 100-400 mg / day. Maximum doses: for violations of kidney function (including those caused by urate nephropathy) – 100 mg / day. An increase in the dose is possible in cases where, against the background of ongoing therapy, an increased concentration of urates in the blood and urine remains. Side effects From the side of the cardiovascular system: in isolated cases – arterial hypertension, bradycardia. From the digestive system: possible dyspepsia (including nausea, vomiting), diarrhea, transient increase in transaminase activity in the blood serum; rarely – hepatitis; in isolated cases – stomatitis, liver dysfunction (transient increase in transaminases and alkaline phosphatase), steatorrhea. From the side of the central nervous system and peripheral nervous system: in isolated cases – weakness, fatigue, headache, dizziness, ataxia, drowsiness, depression, coma, paresis, paresthesia, convulsions, neuropathy, visual disturbances, cataracts, changes in the visual papilla nerve, taste disturbances. From the hemopoietic system: in some cases – thrombocytopenia, agranulocytosis and aplastic anemia, leukopenia (most likely in patients with impaired renal function). From the urinary system: rarely – interstitial nephritis; in isolated cases – edema, uremia, hematuria. From the endocrine system: in isolated cases – infertility, impotence, gynecomastia, diabetes mellitus. From the side of metabolism: in isolated cases – hyperlipidemia. Allergic reactions: skin rash, flushing, itching; in some cases – angioimmunoblastic lymphadenopathy, arthralgia, fever, eosinophilia, fever, Stevens-Johnson syndrome, Lyell’s syndrome. Dermatological reactions: in isolated cases – furunculosis, alopecia, hair discoloration. Contraindications for use Severe liver and/or kidney dysfunction, pregnancy, lactation, hypersensitivity to allopurinol. Use during pregnancy and lactation Contraindicated for use during pregnancy and lactation (breastfeeding). Use for violations of liver function Contraindication: severe violations of liver function. Allopurinol should be used with caution in violation of liver function (dose reduction is necessary). Use in disorders of kidney function Contraindication: severe impairment of kidney function. With caution, allopurinol should be used for impaired renal function (dose reduction is necessary). Use in children In children, it is used only for malignant neoplasms (especially leukemia), as well as for certain enzyme disorders (Lesch-Nychen syndrome). The dosage regimen is set individually, under the control of the concentration of urates and uric acid in the blood and urine: children under the age of 15 years – 10-20 mg / kg / day or 100-400 mg / day. Special instructions Allopurinol should be used with caution in case of impaired liver and / or kidney function (in both cases, dose reduction is necessary), hypothyroidism. In the initial period of the course of therapy with allopurinol, a systematic assessment of liver function indicators is necessary. During the period of treatment with allopurinol, the daily amount of fluid consumed should be at least 2 liters (under the control of diuresis). An exacerbation of the disease may occur at the beginning of a course of gout treatment. For prophylaxis, NSAIDs or colchicine (0.5 mg 3 times / day) can be used. It should be borne in mind that with adequate allopurinol therapy, it is possible to dissolve large urate stones in the renal pelvis and their subsequent entry into the ureter. Asymptomatic hyperuricemia is not an indication for the use of allopurinol. In children, it is used only for malignant neoplasms (especially leukemia), as well as for certain enzyme disorders (Lesch-Nychen syndrome). For the correction of hyperuricemia in patients with neoplastic diseases, allopurinol is recommended before starting treatment with cytostatics. In such cases, the lowest effective dose should be used. In addition, in order to reduce the risk of xanthine deposition in the urinary tract, measures must be taken to maintain optimal diuresis and alkalinization of the urine. With the simultaneous use of allopurinol and cytostatics, more frequent monitoring of the peripheral blood picture is necessary. Do not drink alcohol while taking allopurinol. Influence on the ability to drive vehicles and mechanisms Use with caution in patients whose activities require a high concentration of attention and fast psychomotor reactions. Drug interactions With the simultaneous use of allopurinol, it enhances the effect of coumarin anticoagulants, adenine arabinoside, and hypoglycemic drugs (especially in case of impaired renal function). High doses of uricosuric agents and salicylates reduce the activity of allopurinol. With the simultaneous use of allopurinol and cytostatics, myelotoxic effects are more likely to occur than with separate use. Leave a Reply Cancel reply Your email address will not be published. Required fields are marked * Comment * Name * Email * Website