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Allopurinol - Uses, Dosage, Side Effects, Precautions, and Warnings

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Allopurinol helps to treat gout. Learn about its uses, how it works, dosage, side effects, and precautions.

Medically reviewed by

Dr. Sunny Kumar Yadav

Published At January 5, 2023
Reviewed AtJanuary 10, 2023

What Is Allopurinol Used For?

Allopurinol is a class of medication that inhibits the activity of xanthine oxidase and treats gout and specific kidney stones. The drug is often used to manage leukemia, lymphoma, and malignancies which may cause elevated serum and uric acid levels. Allopurinol can manage patients with recurrent calcium kidney stones and elevated uric acid levels. Allopurinol is a Food and Drug Administration (FDA)-approved medication that prevents tumor lysis syndrome.

How Does Allopurinol Work?

Allopurinol helps to reduce uric acid production by inhibiting biochemical reactions. Allopurinol is metabolized in the liver into its active metabolite or oxypurinol. The oxypurinol inhibits the xanthine oxidase enzyme in the purine catabolism pathway and converts hypoxanthine to xanthine to uric acid. Allopurinol increases the reuse of hypoxanthine and xanthine for nucleotide and nucleic acid synthesis. This causes increased nucleotide concentration resulting in decreased urine and serum uric acid concentration. The half-life of Allopurinol is one to two hours, and oxypurinol is about 15 hours. Therefore, the kidney primarily eliminates Allopurinol and its metabolites.

How to Take Allopurinol?

Allopurinol is available as an oral tablet to be taken once or twice a day, preferably after a meal. The medicine should be taken at the same time each day. It is advised to take eight to ten glasses of fluid daily to reduce the risk of kidney stones. It may be required to have regular blood tests to monitor uric acid levels. There may be more gout attacks initially when Allopurinol is started, and it may take up to two to six weeks for symptoms of gout to reduce. When taken regularly, Allopurinol can lower the number of gout attacks and help to prevent damage to the joints.

What Is the Dosage of Allopurinol?

The recommended dose of Allopurinol is 100 mg to 300 mg a day. Allopurinol is usually started on a low dose. The duration and the dosage depend on

  • Age.

  • The condition that is being treated.

  • The severity of the condition.

  • Other medical conditions.

  • Reaction to the first dose.

Dosage of Allopurinol

What Precautions to Be Taken When Taking Allopurinol?

  • Allergies - Allopurinol can cause severe allergic reactions. The drug should be avoided if you have ever been allergic to Allopurinol or other similar medicines.

  • Pregnancy and Breastfeeding - Allopurinol is a category C pregnancy drug and can cause adverse effects on the fetus. The drug passes into human breastmilk and may cause side effects in the child.

  • Geriatrics - Kidney function deteriorates with age causing older adults to be more susceptible to side effects while taking Allopurinol.

  • Children - Allopurinol should be given with caution in children as there can be an increased risk of side effects such as a rash, itchy skin, hives, fever with chills, or blood in urine or stool.

  • Liver Disease - Allopurinol may cause changes in the liver function test results and liver disease, which may be fatal.

  • Kidney Problems - Allopurinol should be administered cautiously in patients with kidney problems or a history of kidney disease. There can be an increase in the levels of Allopurinol in the body because of delayed clearing of the drug from the body.

  • Alertness - Allopurinol can cause drowsiness and should not be taken when driving, handling machinery, or other activity that requires alertness.

  • Alcohol - Drinking alcohol can increase the level of uric acid in the blood and can trigger an attack of gout.

What Are the Side Effects of Allopurinol?

Allopurinol can cause serious drug reactions that may affect many parts of your body.

Some of the side effects may include

  • Rash.

  • Drowsiness.

  • Fever and chills.

  • Nausea.

  • Diarrhea.

  • Joint pain.

  • Painful urination.

  • Easy bruising.

  • Numbness, tingling, burning pain.

  • Loss of appetite.

  • Weight loss.

  • Irritation of the eyes.

  • Swelling of lips or mouth.

  • Blood in urine or stool.

  • Sore throat.

  • Muscle aches.

  • Little or no urination.

  • Yellowing of the skin or eyes.

  • Severe skin rash or redness can develop into a life-threatening skin condition called Stevens-Johnson syndrome, which may cause flu-like symptoms followed by red or purple rash or blister.

What Will Happen If You Stop Taking Allopurinol?

Allopurinol should not be stopped suddenly as there is an increased risk of worsening gout or serious side effects. The doctor will reduce the dose gradually.

What Are the Interactions of Allopurinol?

Drug Interactions:

  • Azathioprine.

  • Mercaptopurine.

  • Chlorpropamide.

  • Cyclosporine.

  • Antibiotics such as Ampicillin or Amoxicillin.

  • Anticoagulants such as Warfarin, Coumadin, or Jantoven.

  • Diuretics such as Furosemide.

  • Enalapril.

  • Ramipril.

Food Interaction:

  • Coffee - Drinking coffee in moderation can reduce the risk of gout as it can lower the rate at which uric acid is formed.

  • Vitamin C - High vitamin C intake can increase plasma ascorbate in Allopurinol patients. Vitamin supplements or food rich in vitamin C can significantly reduce serum uric acid levels.

Interaction with Diseases:

  • Bone Marrow Suppression - Therapy with Allopurinol should be administered with caution to patients with or predisposed to bone marrow suppression as it can cause suppression in these people as early as six weeks to as long as six years.

  • Dehydration - It is important to be adequately hydrated during Allopurinol therapy to prevent the formation of xanthine calculi and renal precipitation of urates.

  • Liver Disease - Therapy with Allopurinol should be administered cautiously in patients with liver disease as there can be asymptomatic elevated serum transaminase and alkaline phosphatase levels. Periodic monitoring of liver function is recommended in these patients during the early stages of therapy.

  • Renal Dysfunction - Patients with decreased renal function may require a lower dose of Allopurinol. Individuals with preexisting renal disease should be monitored regularly with periodic renal function tests.

  • Thyroid Problems - Increased thyroid-stimulating hormone levels can be observed in patients receiving long-term Allopurinol treatment.

Conclusion:

Allopurinol can be used for the long-term treatment of gout. It is important to monitor certain health issues like kidney and liver function tests and uric acid tests while taking Allopurinol to stay safe while taking this medicine. Eating a diet low in animal protein and oxalate-rich foods such as spinach, beets, celery, and green beans is recommended to check uric acid levels.

Frequently Asked Questions

1.

How Can Allopurinol Be Eliminated From Our Bodies?

Allopurinol is primarily eliminated from the body through the kidneys. The time taken for complete elimination from the body depends on various factors such as dosage, duration of use, and individual metabolic rate.  Allopurinol may take several days to weeks to be eliminated from the body.

2.

What Is the Route of Administration for Allopurinol?

Allopurinol is generally taken orally as it comes in tablet form. The tablet is taken as the doctor prescribes, commonly once or twice a day. The doctor will start with a low allopurinol dose and gradually increase the dosage. The dosage may vary based on the individual’s medical condition.

3.

What Is the Shelf Life of Allopurinol?

Allopurinol is a medication with a long shelf life when stored properly. The specific shelf-life depends on the formulation and manufacturer of the product. It is necessary to store in a cool, dry place, away from direct sunlight and out of reach of children. The manufacturer, pharmacist, or doctor provides proper guidance on storage and disposal.

4.

How Does Allopurinol Act Against Gout?

Allopurinol is used to treat gout. It acts by inhibiting the enzyme xanthine oxidase, which is involved in uric acid production. Allopurinol works by reducing uric acid production in the body. Allopurinol prevents gout by reducing uric acid build-up, particularly in patients under chemotherapy. Allopurinol does not treat gout.

5.

What Is the Time Frame for Allopurinol to Reduce Uric Acid Levels?

Allopurinol is used to reduce uric acid levels in the blood, which helps in preventing gout attacks. The time frame depends on the individual, and it may take several weeks or months to decrease uric acid levels after starting the medication. Once allopurinol is started, the uric acid levels are monitored regularly, and the dosage is adjusted to achieve the expected results.

6.

What Is the Efficacy of Allopurinol in Treating Gout?

Allopurinol is used to reduce the uric acid level to prevent gout attacks or kidney stones. It acts by inhibiting xanthine oxidase. Allopurinol is not used to treat gout once they occur but to prevent it due to higher uric acid levels.

7.

What Foods Should Be Avoided While on Allopurinol?

Food to be avoided while taking allopurinol is high in purines such as red meat, organ meat, and seafood. Limit alcohol intake, particularly beer and hard liquor. Drinking adequate water is suggested.

8.

How Much Is Allopurinol Taken for Gout?

The dosage for gout varies based on the severity of the condition and uric acid levels. Typically, the adult dosage is 100mg daily, which will gradually increase as required. Therefore, following the dosage prescribed by the doctor is essential.

9.

Is There an Alternative to Allopurinol for Gout?

Yes. Several alternatives to allopurinol, such as Febuxostat, NSAIDS (non-steroidal anti-inflammatory drugs), and steroids to treat gout pain. Other drugs inlude lesinurad, pegloticase, probenecid.

10.

How Quickly Does Allopurinol Start Its Action Against Gout?

Allopurinol is a slow-acting drug. It takes several months to get benefitted from the drug. It can increase gout attacks in the first few months and prevent them. A drug called Colchicine is prescribed along with allopurinol to prevent gout attacks.

11.

Is It Safe to Increase the Allopurinol Dosage?

The healthcare provider can modify the allopurinol dosage, and it is not allowed to increase it without a doctor’s prescription or advice. Increasing the dosage without a doctor’s approval can cause side effects such as skin rash, liver damage, or kidney problems. Instead, a healthcare provider will gradually increase the dosage to achieve optimal uric acid levels and gout prevention.

12.

What Is the Maximum Safe Dosage of Allopurinol?

The maximum safe dosage for allopurinol depends on the individual’s age, body weight, kidney function, and severity of the condition. The maximum recommended dosage is approximately 800 mg per day for adults. Some doctors can prescribe higher doses in certain cases; however, it is essential to follow the instructions provided by your doctor. Overdose of allopurinol can cause serious side effects such as skin rash or itching, painful urination, blood in the urine, peeling, blistering, or shedding skin.

13.

Is It Allowed to Stop Allopurinol Suddenly?

It is not recommended to stop allopurinol without medical supervision. A healthcare provider will gradually decrease the dosage to prevent gout attacks or other potential side effects. Stooping allopurinol suddenly can increase the risk of gout attacks and complications such as skin rashes or kidney problems.

14.

Is It Allowed to Stop Allopurinol Suddenly?

Allopurinol is primarily metabolized in the liver and is excreted through the kidneys. The majority of the drug is eliminated from the body in the form of metabolites in the urine. However, some amount may be excreted in the feces. The elimination half-life is approximately two hours, depending on the individual’s condition. In case of impaired renal function, the elimination half-life is longer, and dosage needs to adjust accordingly.

15.

What Is the Effect of Allopurinol on the Liver?

The effect of allopurinol on the liver is a rare but well-known cause of acute liver injury that is similar to a hypersensitivity reaction that can be serious and fatal. The immunoallergic manifestations include fever, rash, eosinophilia, lymphadenopathy, atypical lymphocytosis, thrombocytopenia, facial edema, and arthralgias. Allopurinol's effect on the liver has high fatality rates due to acute liver failure, renal dysfunction, vasculitis, pancreatitis, and other complications.

16.

Can Allopurinol Precipitate a Gout Attack?

Initial doses of allopurinol can trigger a gout attack due to the dislodgement of crystal into the joint due to size reduction resulting in an attack. Therefore, another medicine is given along with allopurinol to reduce gout attacks.
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Dr. Sunny Kumar Yadav
Dr. Sunny Kumar Yadav

General Medicine

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