Posts Tagged ‘Allopurinol’

Zyloric (Allopurinol)

Zyloric 100 mg and 300 mg tablets

Allopurinol

1 What Zyloric is and what it is used for

Zyloric tablets contain a medicine called Allopurinol. It works by slowing down the speed of certain chemical reactions in your body. Zyloric is used:

•  to prevent gout. This is a disease where your body produces too much of a substance called ‘uric acid’. The uric acid builds up in your joints and tendons as crystals. These crystals cause an inflammatory reaction. The inflammation causes the skin around certain joints to become swollen, tender and sore when only slightly touched. You can also fine you get severe pain when the joint is moved.

•  to prevent other conditions where there is a build up of uric acid in the body. These include kidney stones and certain other types of kidney problem and when you are having treatment for cancer.

2 Before you take Zyloric

Do not take Zyloric if:

•  you are allergic (hypersensitive) to Allopurinol or any of the other ingredients of Zyloric. Do not take Zyloric if the above applies to you. If you are not sure, talk to your doctor or pharmacist before taking Zyloric.

Take special care with Zyloric

Check with your doctor or pharmacist before taking your medicine if:

•  you have problems with your liver or kidneys. Your doctor may give you a lower dose or ask you to take it less often than each day. They will also monitor you more closely

•  You have heart problems or high blood pressure

•  you are currently having an attack of gout

•  you have been told by your doctor that you have an intolerance to lactose. Zyloric tablets contain a small amount of lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicinal product.

If you are not sure if any of the above applies to you, talk to your doctor or pharmacist before taking Zyloric.

Taking other medicines

Tell your doctor or pharmacist if you are taking any of the following:

•  aspirin

•  theophylline, used for breathing problems

•  medicines used for fits (epilepsy)

•  antibiotics

•  didanosine, used to treat HIV infection

•  medicines for cancer

•  medicines used to reduce your immune response (immunosuppressants)

•  medicines used to treat diabetes

•  medicines for heart problems or high blood pressure such as ‘ACE inhibitors’ or water tablets (diuretics)

•  medicines used to thin your blood (anticoagulants), such as warfarin

•  any other medicine to treat gout.

Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines. This includes medicines obtained without a prescription, including herbal medicines. This is because Zyloric can affect the way some medicines work. Also some other medicines can affect the way Zyloric works. Taking Zyloric with food and drink Take Zyloric with food and water.

Pregnancy and breast-feeding

Talk to your doctor before taking this medicine if you are pregnant, might become pregnant or are breast-feeding.

Driving and using machines

You may feel drowsy, giddy or have problems with your co-ordination. If this happens, do not drive or use any tools or machines.

3 How to take Zyloric

Always take Zyloric exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.

Taking this medicine

•  Swallow the tablet with a drink of water.

•  Take with or just after food. Children (under 15 years)

•  The usual dose ranges from 100 to 400 mg each day. Adults (over 18 years)

•  The usual dose ranges from 100 to 900 mg each day.

You will usually start on a dose of 100 to 300 mg each day. Elderly (over 65 years)

•  Your doctor will prescribe the lowest dose of Zyloric tablets that best controls your symptoms.

If you have a serious kidney problem

•  you may be asked to take less than 100 mg each day

•  or you may be asked to take 100 mg at longer intervals than one day.

If you have dialysis two or three times a week, your doctor may prescribe a dose of 300 or 400 mg which is to be taken straight after your dialysis.

If you take more Zyloric than you should

If you take more Zyloric than you should, talk to a doctor or go to hospital straight away. Take the medicine pack with you.

If you forget to take Zyloric

•  If you forget a dose, take it as soon as you remember it. However, if it is nearly time for the next dose, skip the missed dose.

•  Do not take a double dose to make up for a forgotten dose. If you stop taking Zyloric

Do not stop taking your Zyloric without talking to your doctor.

If you have any further questions on the use of this product, ask your doctor or pharmacist.

4.  Possible side effects

Like all medicines, Zyloric can cause side effects, although not everybody gets them. The following side effects may happen with this medicine:

Allergic reactions (affects less than 1 in 10,000 people) If you have an allergic reaction, stop taking Zyloric and see a doctor straight way. The signs may include:

•   skin rash, flaking skin, boils or sore lips and mouth

•   very rarely signs may include sudden wheeziness, fluttering or tightness in the chest and collapse.

Do not take any more tablets unless your doctor tells you to do so.

If you experience any of the following, stop your tablets and tell your doctor as soon as possible:

Rare (affects less than 1 in 1000 people)

•  joint pain or painful swelling in your groin, armpits or neck

•   yellowing of the skin and eyes (jaundice)

• liver or kidney problems

•   feeling sick (nausea) or being sick (vomiting), occasionally    with blood

. •   you notice any changes to your skin, for example blisters or   peeling

•   fever and chills, aching muscles and generally feeling unwell

•   bleeding in the lips, eyes, mouth, nose or genitals Very rare (affects less than 1 in 10,000 people)

•   bruising more easily than usual, or you may develop a sore throat or other signs of an infection. Tell your doctor as soon as possible. Occasionally Zyloric tablets may affect your blood or lymph system. These effects usually occur in people with liver or kidney problems

•   high temperature

•   blood in your urine (haematuria)

•   high levels of cholesterol in your blood (hyperlipidaemia)

•   a general feeling of being unwell

•   weakness, numbness, unsteadiness on your feet, feeling unable to move muscles (paralysis) or loss of consciousness

•   headache, dizziness, drowsiness or disturbance of your vision

•   chest pain, high blood pressure or a slow pulse

•   male infertility or erectile dysfunction

•   enlargement of the breasts, in men as well as women

•   a change in your normal bowel habit

•   a change in taste

•   cataracts

•   hair loss or discolouration

•   fits (convulsions)

•   depression

•   build up of fluid leading to swelling (oedema) particularly of your ankles

•   feeling thirsty, tired and losing weight; these may be symptoms of diabetes. Your doctor may wish to measure the level of sugar in your blood to check if this is happening.

If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

5. How to store Zyloric

•   Keep out of the reach and sight of children.

•   Do not use Zyloric after the expiry date which is stated on the carton after ‘EXP’. The expiry date refers to the last day of that month.

•   Keep your tablets in the original packaging.

•   Do not store above 25°C.

•   Medicines should not be disposed of via wastewater or household waste.

•   Return any unused or unwanted tablets to your pharmacist for disposal. Only keep them if your doctor tells you to. These measures will help to protect the environment.

6. Further information

What Zyloric contains

•  The active substance is Allopurinol.

•  The other ingredients are lactose, maize starch, povidone and magnesium stearate.

What Zyloric looks like and contents of the pack

Zyloric tablets contain 100 or 300 mg Allopurinol. Each 100 mg tablet is white, round and marked with a score line, ‘GXCM2′.

Each 300 mg tablet is white, round and marked with a score line, ‘GXCM7′.

Zyloric 100 mg tablets come in 4 strips of 25 tablets.

Zyloric 300 mg tablets come in calendar packs of 2 x 14 tablets.

 

Allopurinol Tablets BP (Allopurinol)

Allopurinol Tablets BP 100mg

(Allopurinol)

1. What Allopurinol 100mg tablets is used for

Allopurinol belongs to a group of medicines called enzyme inhibitors which is used for the long term prevention of gout, the prevention of kidney stones and the treatment of high levels of uric acid associated with tumours and their treatment, certain enzyme disorder in particular Lesch Nyhan syndrome.

The Tablets are only given to children with cancer especially leukaemia (cancer of the blood) and certain enzyme disorders (e.g. Lesch Nyhan disorders).

2. Before you take Allopurinol 100mg Tablets

Do not take Allopurinol 100mg Tablets

•    If you are sensitive or allergic to allopurinol or any of the ingredients in the tablets.

Do not take Allopurinol tablets if the above applies to you. If you are not sure, talk to your doctor or pharmacist before taking Allopurinol tablets

Take special care with Allopurinol 100mg tablets

Check with your doctor before taking Allopurinol 100mg tablets:

•   If you have problems with your liver or kidneys. Your doctor may give you a lower dose or ask you to take it less often than each day. They will also monitor you more closely

•   If you have heart problems or high blood pressure.

•   If you are currently having an attack of gout.

If you are not sure if any of the above applies to you, talk to your doctor or pharmacist before taking Allopurinol tablets.

Taking other medicines

Please inform your doctor if you are taking or have recently taken any other medicines, including those obtained without a prescription.

Before taking Allopurinol 100mg tablets, tell your doctor if you are already   taking any of the following:

•  6-mercaptopurine used to treat cancer of the blood cells.

•  Anticoagulants (drugs to prevent blood clotting such as Warfarin).

Other products used to treat high levels of uric acid e.g. probenecid.

•  Some drugs used to reduce excess water in the body (thiazide diuretics) ampicillin (antibiotic),

•  aspirin

•  theophylline.used for breathing problems

•  medicines used for fits (epilepsy)

•  didanosine.used to treat HIV infection

•  medicines used to treat diabetes

•  medicines used to reduce your immune response(immunosuppressant)

•  medicines for heart problems or high blood pressure such as ‘ACE inhibitors’ or water tablets(diuretics)

Pregnancy and breast-feeding

If you are planning to become pregnant, or are pregnant do not take Allopurinol 10Omg tablets an contact your doctor for further advice. If you are planning to breastfeed your baby ask your doctor or pharmacist for advice.

Ask your doctor or pharmacist for advice before taking any medicine.

Driving and using machines

Allopurinol 100mg tablets may cause drowsiness or affect your vision. If you experience these symptoms you should avoid driving or operating machinery.

Important information about some of the ingredients

These tablets contain lactose. If your doctor has told you that you have an intolerance to some sugars then do not take these tablets until you have consulted with your doctor.

3. How to take Allopurinol 10Omg Tablets

Always take Allopurinol 10Omg tablets exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.

For oral use only. Allopurinol 100mg Tablets should be swallowed, without chewing, with half a glassful of water during or after meals.

Adults:(Over 18 years)

The usual dose ranges from 100 to 900 mg each day. Initially 100 to 300mg per day taken as a single dose.

Children:(under 15 years)

The recommended dose is 10 to 20mg/kg body weight/day up to a maximum of 400mg daily.

Use in the elderly: (over 65 years)

The lowest dosage possible will be given as recommended by your doctor.

Use in patients with kidney damage:

The level and frequency of dosage should be recommended by your doctor. The dose may need to be decreased depending on blood uric acid levels due to kidney damage which mean it takes longer to excrete Allopurinol.

Use in patients on kidney dialysis:

Allopurinol and its by-products are removed by dialysis. If dialysis is done frequently 300 to 400mg of Allopurinol may be given after each dialysis with none in the interim.

The dose should be adjusted by checking blood uric acid and/or urinary uric acid levels at appropriate intervals which will be done by your doctor. It might take one to three weeks for blood and/or urinary uric acid to return to the desired levels.

If you take more Allopurinol 100mg Tablets than you should

If you or someone else swallow several of these tablets together, contact your doctor or nearest hospital emergency department immediately. Always take the box, this leaflet and any tablets that are left over with you, if you can.

If you forget to take Allopurinol 100mg Tablets

If you miss a dose, take it as soon as you remember and carry on as before. If it is almost time for your next dose, skip the forgotten dose and continue as usual. Do not take a double dose to make up for a forgotten dose.

If you stop taking Allopurinol 100mg Tablets

Do not stop taking Allopurinol 10Omg tablets without first discussing it with your doctor. If you have any further questions on the use of this product, ask your doctor or pharmacist.

4. Possible side effects

Like all medicines Allopurinol 100mg Tablets can cause side effects although not everybody gets them.

An allergic (hypersensitive) reaction may occur with symptoms such as skin rash, flaking skin, fever, boils or sore lips and mouth and in extreme cases hepatitis.

Very rarely signs may include sudden wheeziness, fluttering or tightness in the chest and collapse. In this case stop taking the tablets immediately and contact your doctor or hospital emergency department immediately.

If you experience any of the following, stop your tablets and tell your doctor as soon as possible:

•     Joint pain or painful swelling in your groin, armpits or neck

•     Yellowing of the skin and eyes (jaundice)

•     Liver or kidney problems

•     Feeling sick (nausea) or being sick (vomiting),occasionally with blood

•     Bruising more easily than usual or you may develop a sore throat or other signs of an infection.

•     High temperature

•     Blood in your urine (haematuria)

•     High levels of cholesterol in your blood (hyperlipidaemia)

•     A general feeling of being unwell

•     Weakness,numbness,unsteadiness on your feet, feeling unable to move

•     muscles (paralysis) or loss of consciousness

•     headache,dizziness,drowsiness or disturbance of your vision

•     chest pain, high blood pressure or a slow pulse

•     male infertility or erectile dysfunction

•     enlargement of the breasts, in men as well as women

•     a change in your normal bowel habit

•     a change in taste

•     cataracts

•     hair loss or discolouration

•     fits (convulsions)

•     depression

•     build up of fluid leading to swelling (oedema) particularly of your ankles

•     feeling thirsty, tired and losing weight; these may be symptoms of diabetes. Your doctor may wish to measure the level of sugar in your blood to check if this is happening

If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

5. How to store Allopurinol 100mg Tablets

Keep out of the reach and sight of children.

Do not store above 25°C. Store in the original package and keep containers tightly closed. Do not use the tablets after the expiry date is stated on the label.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.

6. Further information

  • What Allopurinol 100mg Tablets contains

The active ingredient is Allopurinol.

The other substances are Lactose monohydrate, Maize Starch, Povidone K30,    Sodium Starch Glycollate and Magnesium Stearate (See Section 2 ‘Important information about some of the ingredients of Allopurinol 100mg tablets)’.

  • What Allopurinol 100mg Tablets looks like and contents of the pack

Allopurinol 100mg Tablets are white, round, biconvex tablets embossed with MAL100 on one side and plain on the reverse.

The product is available in containers of 1000, 500, 250, 100, 84, 70, 56, 42, 28, 21,15 and 14 tablets. They are also available in blister packs of 84, 70, 56, 42, 28, 21,15 and 14 tablets (not all pack sizes may be marketed).

 

Probenecid

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Probenecid; Probenecidas; Probenecidum; Probenesidi
BAN: Probenecid
INN: Probenecid [rINN (en)]
INN: Probenecid [rINN (es)]
INN: Probénécide [rINN (fr)]
INN: Probenecidum [rINN (la)]
INN: Пробенецид [rINN (ru)]
Chemical name: 4-(Dipropylsulphamoyl)benzoic acid
Molecular formula: C13H19NO4S =285.4
CAS: 57-66-9
ATC code: M04AB01
Read code: y031N

Pharmacopoeias. In China, Europe, International, Japan and US.

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Probenecid). A white or almost white crystalline powder or small crystals. Practically insoluble in water; sparingly soluble in dehydrated alcohol; soluble in acetone.

The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Probenecid). A white or practically white, fine, practically odourless, crystalline powder. Practically insoluble in water and in dilute acids; soluble in alcohol, in acetone, in chloroform, and in dilute alkali.

Adverse Effects and Treatment

Probenecid may cause nausea, vomiting, anorexia, headache, sore gums, flushing, alopecia, dizziness, anaemia, and urinary frequency. Hypersensitivity reactions, with fever, dermatitis, pruritus, urticaria, and, rarely, anaphylaxis, and Stevens-Johnson syndrome have occurred. There have been reports of leucopenia, hepatic necrosis, nephrotic syndrome, and aplastic anaemia. Haemolytic anaemia has also occurred, and may be associated with G6PD deficiency. When used in chronic gout, and particularly during the first few months of therapy, probenecid may precipitate acute attacks. Uric acid renal calculi, with or without haematuria, costovertebral pain and renal colic may occur.

In massive overdosage probenecid causes stimulation of the CNS, with convulsions and death from respiratory failure. Severe overdosage should be managed by lavage and symptomatic treatment.

Precautions

Probenecid therapy should not be started during an acute attack of gout; however treatment is usually continued when acute attacks occur in patients already receiving the drug, and the acute attack is treated separately. Probenecid is also unsuitable for the control of hyperuricaemia secondary to cancer or cancer chemotherapy. Probenecid should not be given to patients with a history of uric acid renal calculi or blood disorders. It should be used with caution in patients with a history of peptic ulceration. Probenecid should not be used as an antibacterial adjunct in patients with known renal impairment, and it is ineffective in gout in patients with severe renal impairment. To reduce the risk of uric acid renal calculi in patients with gout an adequate fluid intake (2 to 3 litres daily) is required, and, if necessary, especially during the first few months of treatment, sodium bicarbonate or potassium citrate may be given to render the urine alkaline. A reducing substance has been found in the urine of some patients taking probenecid, and may give false positive results with some tests for glucose in the urine. Probenecid reduces the excretion of some iodinated contrast media and may interfere with laboratory tests by decreasing the excretion of aminohippuric acid, phenolsulfonphthalein, and sulfobromophthalein.

Abuse. It has been alleged that some athletes using banned anabolic steroids have taken probenecid in an attempt to inhibit the urinary excretion of steroid metabolites in order to avoid detection by urine screening tests.

Porphyria. Probenecid is considered to be unsafe in patients with porphyria although there is conflicting experimental evidence of porphyrinogenicity.

Interactions

The dose of probenecid may need to be increased if patients are also given drugs, such as diuretics or pyrazinamide, that increase the blood concentration of uric acid. Salicylates, including aspirin, and probenecid are mutually antagonistic and should notbe given together. Probenecid may also affect many other drugs. By inhibiting renal tubular secretion, it has the potential to increase the toxicity and/or to enhance the therapeutic efficacy of drugs excreted by that route. In some instances a reduction in dose is essential to counteract an increase in toxicity, as is the case with methotrexate. Some combinations, such as that with ketorolac, should be avoided. Conversely, probenecid may be given with some antibacterials such as the penicillins and cephalosporins to increase their effects.

Altered excretion may also increase serum concentrations of other antibacterials (aminosalicylic acid, conjugated sulfonamides, dapsone, meropenem, some quinolones, rifampicin), some antivirals (aciclovir, ganciclovir, zalcitabine, zidovudine, and possibly famciclovir), some benzodiazepines (adinazolam, lorazepam, and nitrazepam), some ACE inhibitors (captopril and enalapril), some NSAIDs (diflunisal, indometacin, ketoprofen, meclofenamate, naproxen), paracetamol, and sulfonylurea hypoglycaemic drugs. The clinical significance of such interactions is not entirely clear although the possibility of the need for a reduction in dosage of these drugs should be borne in mind.

It has been reported that patients receiving probenecid require lower doses of thiopental for induction of anaesthesia. Probenecid may increase the speed of induction of anaesthesia with midazolam.

Reducing the urinary concentration of some drugs could diminish their activity in certain diseases as might happen with nitrofurantoin or some quinolones in urinary-tract infections and penicillamine in cystinuria.

Allopurinol. Probenecid may increase the clearance of allopurinol despite an increased hypouricaemic effect when these 2 drugs are given together (see Antigout Drugs, under Allopurinol).

Pharmacokinetics

Probenecid is completely absorbed from the gastrointestinal tract with peak plasma concentrations achieved 2 to 4 hours after a dose. It is extensively bound to plasma proteins (85 to 95%). The plasma half-life is dose-dependent and ranges from less than 5 to more than 8 hours. Probenecid crosses the placenta. It is metabolised by the liver, and excreted in the urine mainly as metabolites. Excretion of unchanged probenecid is increased in alkaline urine.

Uses and Administration

Probenecid is a uricosuric drug used to treat hyperuricaemia associated with chronic gout; it has also been used to treat hyperuricaemia caused by diuretic therapy. It is also used as an adjunct to some antibacterials to reduce their renal tubular excretion and is given with the antiviral cidofovir to reduce nephrotoxicity.

Probenecid is used in chronic gout and hyperuricaemia to inhibit the renal tubular reabsorption of uric acid so increasing the urinary excretion of uric acid, lowering plasma-urate concentrations, and eventually reducing urate deposits in the tissues. Probenecid is therefore of value in hyperuricaemia caused by decreased uric acid excretion rather than increased urate production, and is notused for hyperuricaemia associated with cancer or cancer therapy.

Probenecid has no analgesic or anti-inflammatory action and is of no value in acute gout. Initially it may increase plasma concentrations of urate and uric acid by dissolving deposits. This can trigger or exacerbate acute attacks, hence probenecid should not be started until an acute attack has completely subsided, and an NSAID or colchicine may be given during the first few months.

It is usual to start treatment for gout with oral doses of 250 mg twice daily increased after a week to 500 mg twice daily and later, if the therapeutic effects are inadequate, by increments of 500 mg every 4 weeks, up to 2 g daily. Probenecid may not be effective in chronic renal impairment particularly when the glomerular filtration rate is less than 30 mL/minute. An adequate fluid intake is required to reduce the risk of uric acid renal calculi.

When the patient has been free from acute attacks for at least 6 months, and provided that the plasma-urate concentration is within acceptable limits, the daily dose may be gradually reduced, by 500 mg every 6 months, to the lowest effective maintenance dose which is then given indefinitely

Probenecid may also be used as an adjunct to antibacterial therapy particularly when treating severe or resistant infections. It reduces the tubular excretion of penicillins and most cephalosporins and may increase their plasma concentrations up to fourfold. The usual dosage for reducing tubular excretion of penicillins and cephalosporins is 500 mg four times daily, or less in elderly patients with suspected renal impairment. When renal impairment is sufficient to retard the excretion of antibacterials, probenecid should not be given. The dosage for children over 2 years of age and weighing less than 50 kg is 25 mg/kg (700 mg/m) initially, followed by 10 mg/kg (300 mg/m) every 6 hours.

Single oral doses of probenecid 1 g are given with a suitable oral antibacterial, or at least 30 minutes before an injected antibacterial, in the single-dose treatment of gonorrhoea.

Preparations

British Pharmacopoeia 2008: Probenecid Tablets;

The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Ampicillin and Probenecid for Oral Suspension; Probenecid and Colchicine Tablets; Probenecid Tablets.

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Australia: Benemid¤; Pro-Cid; Canada: Benemid¤; Benuryl; Finland: Probecid¤; France: Benemide; Greece: Benemid; India: Bencid; Ireland: Benemid¤; Italy: Solpurin¤; Urocid¤; Mexico: Benecid; Netherlands: Benemid¤; Norway: Probecid; New Zealand: Benemid¤; South Africa: Benemid¤; Proben; Sweden: Probecid; Switzerland: Benemid¤; Thailand: Bencid; Benemid¤; United Kingdom: Benemid¤; United States: Benemid; Probalan¤

Multi-ingredient Preparations

Spain: Agilex¤; United States: ColBenemid; Proben-C¤

Adjuvant to Preparations

Brazil: Ampicler com Probenecide¤; Degona¤; Emicilin; Gonocilin¤; Gonol; Gonorrels¤; Probecilin¤; Canada: Ampicin-PRB¤; France: Prototapen¤; Spain: Blenox; United States: Polycillin-PRB¤; Principen with Probenecid¤

Allopurinol

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Allopurinol; Allopurinoli; Allopurinolum; Alopurinol; Alopurinolis; BW-56-158; HPP; NSC-1390
BAN: Allopurinol
USAN: Allopurinol
INN: Allopurinol [rINN (en)]
INN: Alopurinol [rINN (es)]
INN: Allopurinol [rINN (fr)]
INN: Allopurinolum [rINN (la)]
INN: Аллопуринол [rINN (ru)]
Molecular formula: C5H4N4O =136.1
CAS: 315-30-0 (allopurinol); 17795-21-0 (allopurinol sodium)
ATC code: M04AA01
Read code: y0318

Description. Allopurinol is a tautomeric mixture of 1H-pyrazolo[3,4-d]pyrimidm-4-ol and l,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one.

Pharmacopoeias. In China, Europe , International, Japan, and US

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Allopurinol). A white or almost white powder. Very slightly soluble in water and in alcohol; dissolves in dilute solutions of alkali hydroxides.

The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Allopurinol). A fluffy white to off-white powder having only a slight odour. Very slightly soluble in water and in alcohol; practically insoluble in chloroform and in ether; soluble in solutions of potassium and sodium hydroxides.

Incompatibility. Allopurinol sodium as a 3 mg/mL solution in 0.9% sodium chloride was visually incompatible with amikacin sulfate, amphotericin B, carmustine, cefotaxime sodium, chlormethine hydrochloride, chlorpromazine hydrochloride, cimetidine hydrochloride, clindamycin phosphate, cytarabine, dacarbazine, daunorubicin hydrochloride, diphenhydramine hydrochloride, doxorubicin hydrochloride, doxycycline hyclate, droperidol, floxuridine, gentamicin sulfate, haloperidol lactate, hydroxyzine hydrochloride, idarubicin hydrochloride, imipenem with cilastatin sodium, methylprednisolone sodium succinate, metoclopramide hydrochloride, minocycline hydrochloride, nalbuphine hydrochloride, netilmicin sulfate, ondansetron hydrochloride, pethidine hydrochloride, prochlorperazine edisilate, promethazine hydrochloride, sodium bicarbonate, streptozocin, tobramycin sulfate, and vinorelbine tartrate.

Adverse Effects

The most common adverse effect of allopurinol is skin rash. Rashes are generally maculopapular or pruritic, sometimes purpuric, but more serious hyper sensitivity reactions may occur and include exfoliative rashes, the Stevens-Johnson syndrome, and toxic epidermal necrolysis. It is therefore recommended that allopurinol be withdrawn immediately if a rash occurs (see Precautions, below). Further symptoms of hypersensitivity include fever and chills, lymphadenopathy, leucopenia or leucocytosis, eosinophilia, arthralgia, and vasculitis leading to renal and hepatic damage and, very rarely, seizures. These hypersensitivity reactions may be severe, even fatal, and patients with hepatic or renal impairment are at special risk.

Hepatotoxicity and signs of altered liver function may also be found in patients who are not hypersensitive. Haematological effects include thrombocytopenia, aplastic anaemia, agranulocytosis, and haemolytic anaemia.

Many other adverse effects have been noted rarely and include paraesthesia, peripheral neuropathy, alopecia, gynaecomastia, hypertension, taste disturbances, nausea, vomiting, abdominal pain, diarrhoea, headache, malaise, drowsiness, vertigo, and visual disturbances.

Patients with gout may have an increase in acute attacks on beginning treatment with allopurinol, although attacks usually subside after several months.

Incidence of adverse effects. A Boston Collaborative Drug Surveillance Program involving 29 524 hospitalised patients found that, with the exception of skin reactions, 33 of 1835 patients treated with allopurinol (1.8%) had adverse effects. These effects were dose-related and the most frequent were haematological (11 patients, 0.6%), diarrhoea (5 patients, 0.3%), and drug fever (5 patients, 0.3%). Hepatotoxicity was reported in 3 patients (0.2%). Two patients developed possible hypersensitivity reactions to allopurinol.

A further analysis involving 1748 outpatients indicated no instances of acute blood disorders, skin diseases, or hypersensitivity that warranted hospital treatment. Liver disease, although found, was not considered to be associated with allopurinol.

There were only 2 patients in whom renal disease could possibly have been caused by allopurinol.

Effects on the blood. In addition to the haematological abnormalities of leucopenia, thrombocytopenia, haemolytic anaemia, and clotting abnormalities noted in the Boston Collaborative Drug Surveillance Program, aplastic anaemia has also been reported, sometimes in patients with renal impairment. Pure red cell aplasia has also been reported.

Effects on the eyes. Some case reports have suggested an association between allopurinol use and the development of cataracts, but a detailed ophthalmological survey involving 51 patients who had taken allopurinol failed to confirm this. However, a large retrospective case-control study in elderly patients concluded that long-term, or high-dose, allopurinol therapy did increase the risk of cataract extraction.

Effects on the skin. Skin reactions are the most common adverse effects of allopurinol.

One report calculated that of 215 adverse effects noted over a 16-year period 188 (87.4%) were related to the skin or mucous membranes. An analysis by the Boston Collaborative Drug Surveillance Program of data on 15 438 patients hospitalised between 1975 and 1982 detected 6 allergic skin reactions attributed to allopurinol among 784 recipients of the drug. Desensitisation protocols and alternative drugs have been used after cutaneous reactions to allopurinol.

Serious skin reactions to allopurinol may occur as part of a generalised hypersensitivity reaction. A review of the literature between 1970 and the end of 1990 revealed 101 cases of allopurinol hypersensitivity syndrome, 94 of which involved the skin. Skin reactions included erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necro lysis, or a diffuse maculopapular or exfoliative dermatitis; 27 of the 101 patients died. The relative risk of toxic epidermal necro lysis or Stevens-Johnson syndrome occurring with allopurinol was high (calculated to be 5.5) in a case-control study including 13 patients with these cutaneous reactions who had received allopurinol. This risk was not constant over time, being higher during the first 2 months of treatment. During these 2 months the estimated excess risk was 1.5 cases per million users per week. Another case-control study, involving 379 patients with Stevens-Johnson syndrome or toxic epidermal necro lysis, found that allopurinol was the drug most frequently associated with these reactions. The risk again appeared to be restricted to short-term use (less than 8 weeks) and was greater in patients taking 200 mg or more daily.

Precautions

Allopurinol should not be used for the treatment of an acute attack of gout; additionally, allopurinol therapy should not be begun for any purpose during an acute attack. However, allopurinol is continued when acute attacks occur in patients already receiving the drug, and the acute attack is treated separately. Treatment should be stopped immediately if any skin reactions or other signs of hypersensitivity develop. A cautious reintroduction at a low dose may be attempted when mild skin reactions have cleared (see Effects on the Skin, above); allopurinol should not be reintro-duced in those patients who have experienced other forms of hypersensitivity reaction. Dosage should be reduced in renal or hepatic impairment. Care is advised in patients being treated for hypertension or cardiac insufficiency, who may also have renal impairment. To reduce the risk of renal xanthine deposition an adequate fluid intake (2 to 3 litres daily) is required. In addition, a neutral or slightly alkaline urine may be desirable.

Breast feeding. Allopurinol and its metabolite, oxipurinol, are distributed into breast milk, and licensed product information recommends that allopurinol should be used with caution in breast-feeding women. Although oxipurinol was detected in the plasma of a breast-fed infant, no adverse effects were noted in the infant during 6 weeks of maternal treatment with allopurinol. The American Academy of Pediatrics noted that there had been no documented problems with allopurinol and considered its use to be usually compatible with breast feeding.

Interactions

Drugs that can increase uric acid concentrations may decrease the efficacy of allopurinol. Aspirin and the salicylates possess this activity and should generally be avoided in hyperuricaemia and gout. An increase in hypersensitivity reactions, and possibly also other adverse effects, has been reported in patients taking allopurinol with ACE inhibitors orthiazide diuretics, particularly in patients with renal impairment. The metabolism of azathioprine and mercaptopurine is inhibited by allopurinol and their doses should be markedly reduced when either of them is given with allopurinol to avoid potentially life-threatening toxicity. There have also been reports of allopurinol enhancing the activity of, and possibly increasing the toxicity of, a number of other drugs including some antibacte-rials, some anticoagulants, some other antineoplastics, ciclosporin, some sulfonylurea antidiabetics, theophyl-line, and vidarabine.

ACE inhibitors. An apparent interaction between allopurinol and captopril has been reported in patients with chronic renal failure. In one patient it was suggested that the development of fatal Stevens-Johnson syndrome after the introduction of allopurinol was due to potentiation by captopril. In the second patient hypersensitivity, characterised by fever, arthralgia, and myalgia, occurred and was believed to be due to captopril, or one of its metabolites, potentiated by the addition of allopurinol. Care is advised if allopurinol is used with captopril, especially in patients with chronic renal failure.

Antacids. Allopurinol failed to reduce blood-uric-acid concentrations when given at the same time as aluminium hydroxide in 3 patients on chronic haemodialysis. However, if allopurinol was given 3 hours before aluminium hydroxide the expected decrease in uric acid concentration did occur.

Antibacte rials. Although an increased incidence of skin rashes has been noted when allopurinol has been used with ampicillin or amoxicillin, data currently available are insufficient to confirm whether this is due to allopurinol or not. For further details, see Ampicillin.

Anticoagulants. For the effect of allopurinol on dicoumarol, phenprocoumon, or warfarin, see Warfarin.

Antiepileptics. For a report of allopurinol possibly inhibiting the metabolism of phenytoin, see under Antigout Drugs.

Antigout drugs. Uricosuric drugs are likely to increase the renal elimination of oxipurinol (the major active metabolite of allopurinol). For example, benzbromarone lowered plasma concentrations of oxipurinol by about 40% when used with allopurinol, although plasma concentrations of allopurinol itself were not affected. The interaction was not of concern, since the combination was more effective than allopurinol alone in lowering serum concentrations ofuric acid. Licensed product information recommends reassessing the dosage of allopurinol on an individual basis when a uricosuric drug is added. Probenecid has been reported to decrease the clearance of oral allopurinol riboside. In a pharmacokinetic study in healthy subjects, giving allopurinol and probenecid together significantly reduced oxipurinol concentrations; however, this combination had a greater hypouricaemic effect than either drug given alone.

Antineoplastics. Allopurinol inhibits the metabolism of mercaptopurine and marked dosage reduction of this drug to one-quarter to one-third of the usual dose is required if it is used with allopurinol. There are also reports of interactions between allopurinol and other antineoplastics. Mild chronic allopurinol-induced hepatotoxicity has been reported in a male patient to have been exacerbated by tamoxifen. Hypersensitivity vasculitis resulting in the death of a patient receiving allopurinol and pentostatin has been described. Although it could not be ascertained whether this effect was due to one of the drugs alone or to an interaction it was believed that this combination should not be used.

For a report of an increased incidence of bone-marrow toxicity in patients given allopurinol with cyclophosphamide.

Antivirals. For the effect of allopurinol on didanosine.

Immunosuppressants. Allopurinol inhibits the metabolism of mercaptopurine, the metabolite of azathioprine, and marked dosage reduction of azathioprine to one-quarter to one-third of the usual dose is required if it is used with allopurinol. Similar caution is also required with mercaptopurine itself (see Antineoplastics, above). The effects of allopurinol on ciclosporin concentrations (a marked increase) are reported.

Xanthines. For the effect of allopurinol on the pharmacokinetics of caffeine and theophylline.

Pharmacokinetics

Up to 90% of an oral dose of allopurinol is rapidly absorbed from the gastrointestinal tract; its plasma half-life is about 1 to 2 hours. Allopurinol’s major metabolite is oxipurinol (alloxanthine), which is also an inhibitor of xanthine oxidase with a plasma half-life of about 15 or more hours in patients with normal renal function, although this is greatly prolonged by renal impairment. Both allopurinol and oxipurinol are conjugated to form their respective ribonucleosides. Allopurinol and oxipurinol are not bound to plasma proteins. Excretion is mainly through the kidney, but it is slow since oxipurinol undergoes tubular reabsorption. About 70% of a daily dose may be excreted in the urine as oxipurinol and up to 10% as allopurinol; prolonged use may alter these proportions, as allopurinol inhibits its own metabolism. The remainder of the dose is excreted in the faeces. Allopurinol and oxipurinol have also been detected in breast milk.

Uses and Administration

Allopurinol is used to treat hyperuricaemia associated with chronic gout, acute uric acid nephropa-thy, recurrent uric acid stone formation, certain enzyme disorders, or cancer and its treatment (see Tumour Lysis Syndrome). It is notused for asymptomatic hyperuricaemia. Allopurinol is also used in the management of renal calculi caused by the deposition of calcium oxalate (in the presence of hyperuricosuria) and of 2,8-dihydroxyadenine (see Renal Calculi, below). It may have the potential to reduce oxidative stress by blocking the production of free radicals and is an ingredient of kidney preservation solutions. In addition allopurinol has antiprotozoal activity and has been used in leishmaniasis and American trypanosomiasis.

Allopurinol is used in gout and hyperuricaemia to inhibit the enzyme xanthine oxidase, thus preventing the oxidation of hypoxanthine to xanthine and xanthine to uric acid. The urinary purine load, normally almost entirely uric acid, is thereby divided between hypoxanthine, xanthine, and uric acid, each with its independent solubility. This results in the reduction of urate and uric acid concentrations in plasma and urine, ideally to such an extent that deposits of monosodium urate monohydrate or uric acid are dissolved or prevented from forming. At low concentrations allopurinol acts as a competitive inhibitor of xanthine oxidase and at higher concentrations as a non-competitive inhibitor. However, most of its activity is due to the metabolite oxipurinol which is a non-competitive inhibitor of xanthine oxidase.

Allopurinol is used in chronic gout to correct hyperuricaemia, reduce the likelihood of acute attacks, and prevent the sequelae of chronic gout. Initially, it may increase plasma-concentrations of urate and uric acid by dissolving deposits. This can trigger or exacerbate acute attacks, hence allopurinol should not be started until an acute attack has completely subsided, and treatment should be started with a low dose increased gradually; an NSAID (but not aspirin or salicylates) or colchicine should also be given for at least 1 month after hyperuricaemia is corrected, usually 3 months. It may take several months to deplete the uric acid level sufficiently to control acute attacks.

A suggested oral starting dose of allopurinol is 100 mg daily, gradually increased by 100 mg for example at weekly intervals until the concentration of urate in plasma is reduced to 0.36 mmol/litre (6 mg per 100 mL) or less. A daily dose range of 100 to 300 mg may be adequate for those with mild gout and up to 600 mg for those with moderately severe tophaceous gout. The maximum recommended daily dose is 800 mg in the USA and 900 mg in the UK. Up to 300 mg may be taken as a single daily dose; larger amounts should be taken in divided doses to reduce the risk of gastric irritation. Taking allopurinol after food will also minimise gastric irritation. Patients should maintain an adequate fluid intake to prevent renal xanthine deposition.

Doses of allopurinol should be reduced in patients with renal impairment (see below)

When used for the prevention of uric acid nephropathy associated with cancer therapy 600 to 800 mg may be given daily, generally for 2 or 3 days before starting the cancer treatment. A high fluid intake is essential. In hyperuricaemia secondary to cancer or cancer chemotherapy, maintenance doses of allopurinol are similar to those used in gout and are given according to the response.

The main use of allopurinol in children is for hyperuricaemia associated with cancer or cancer chemotherapy or with enzyme disorders. The dosage used may vary: in the UK a dose of 10 to 20 mg/kg daily up to a maximum of 400 mg daily is recommended for children under 15 years of age, while in the USA the dose is 150 mg daily for children under 6 years of age and 300 mg daily for those aged 6 to 10 years, adjusted if necessary after 48 hours.

Allopurinol sodium has been given by intravenous infusion in sodium chloride 0.9% or glucose 5% to patients (usually cancer patients) unable to take allopurinol orally. The recommended dose in adults is the equivalent of allopurinol 200 to 400 mg/m daily up to a maximum of 600 mg daily. Allopurinol sodium 116.2 mg is equivalent to 100 mg of allopurinol.

Administration in renal impairment. Excretion of allopurinol and its active metabolite oxipurinol is primarily via the kidneys and therefore the dosage should be reduced in renal impairment according to creatinine clearance (CC).

In the USA the following doses are suggested for oral and intravenous use:

• CC 10 to 20 mL/mmute: 200 mg daily

• CC less than 10 mL/minute: no more than 100 mg daily

• CC less than 3 mL/minute: consider also a longer dosage interval

In the UK a maximum initial oral daily dosage of 100 mg is recommended for those with renal impairment, increased only if the response is inadequate. Doses less than 100 mg daily or 100 mg at intervals longer than 1 day are recommended for those with severe renal insufficiency. Because of the imprecision of low creatinine clearancevalues, it is suggested that, if facilities are available for monitoring, the allopurinol dose should be adjusted to maintain plasma-oxipurinol concentrations below 100 micromoles/litre (15.2 micrograms/mL). A suggested alternative dose for patients requiring dialysis two or three times weekly is 300 to 400 mg allopurinol immediately after dialysis only.

The difficulties of maintaining an appropriate dose in such patients were illustrated by a study in New Zealand involving 227 allopurinol-treated patients. The guidelines used suggested maintenance doses based on CC as follows:

• less than 10 mL/minute: 100 mg every 3 days

• 10 mL/minute: 100 mg every 2 days

• 20 mL/minute: 100 mg daily

• 40 mL/minute: 150 mg daily

• 60 mL/minute: 200 mg daily

The recommended dose or less was used in the majority of cases (183 of 227). However, of 214 patients for whom serum-uric acid concentrations were available, only 48 achieved values of 0.36 mmol/litre or less. The proportion of patients achieving acceptable serum-uric acid concentrations was higher (38%) in patients given higher than recommended doses than in those on doses recommended by the guidelines (19%). Although guidelines might be useful for initial dosing, longer term use could lead to inadequate control of hyperuricaemia.

Diagnosis and testing. Deficiency of the enzyme ornithine carbamoyltransferase can result in severe CNS dysfunction or even in death, and identification of women at risk of being carriers of this genetic enzyme deficiency has been described. The enzyme deficiency causes carbamoyl phosphate to accumulate, which stimulates the synthesis of orotidine. The test relies on giving a single dose of allopurinol, which will, in carriers, greatly increase the urinary excretion of orotidine. However, mutation analysis is now more usually used to establish the diagnosis.

Duchenne muscular dystrophy. Controlled studies of the use of allopurinol in an attempt to increase muscle ATP in Duchenne muscular dystrophy failed to show any benefit from treatment.

Epilepsy. Reduction in the frequency of seizures has been described in some patients with severe or intractable epilepsy when allopurinol was added to their existing antiepileptic therapy. Although the mode of action was not known it was noted that the patients were not hyperuricaemic and that allopurinol did not affect plasma concentrations of existing antiepileptics. However, others have seen no benefit.

Organ and tissue transplantation. Allopurinol 25 mg on alternate days has been added to the immunosuppressive treatment for renal transplantation, and is reported to reduce the frequency of acute rejection. One possible explanation for this effect is allopurinors ability to suppress the production of free radicals (see Oxidative Stress, below). Organ and tissue transplantation, and the more usual drugs used in immunosuppressive regimens are discussed. It should be noted that allopurinol interacts with azathioprine (see Immunosuppressants, under Interactions, above) and ciclosporin.

Oxidative stress. Allopurinol, through its inhibition of xanthine oxidase, can block the development of superoxide free radicals during reperfusion after an ischaemic episode. Consequently, the ability of allopurinol to reduce oxidative stress has been investigated in a number of clinical situations. In a small study of patients with idiopathic dilated cardiomyopathy, short-term intracoronary allopurinol improved myocardial efficiency by decreasing the oxygen demand of left ventricular contraction.

In patients undergoing coronary artery bypass graft surgery, perioperative allopurinol reduced hospital mortality, the incidence of arrhythmias, the number of ischaemic events, and the need for inotropic support, although the findings were not consistent in all studies.

Improved endothehal dysfunction has been found in patients with chronic heart failure given allopurinol. A large study in neonates undergoing cardiac surgery found that allopurinol caused a reduction in seizures and cardiac events in those with hypoplastic left heart syndrome. No benefit was found in neonates with less severe forms of congenital heart disease, considered to be at lower risk of adverse surgical outcome or reperfusion injury. Allopurinol also failed to reduce the incidence of periventricular leucomalacia (thought to represent ischaemic infarction of the developing brain) in preterm infants compared with placebo in a large study. Similarly, allopurinol did not reduce the incidence of infarct extension in patients with acute myocardial infarction.

The possibility that allopurinol limits the production of free radicals has also led to allopurinol sodium being included as an ingredient of the University of Wisconsin solution [UW Solution; Belzer UW Solution (commercially available as Viaspan)] which is used for the preservation of organs for transplantation. A pilot study using allopurinol showed a beneficial effect on free radical formation, cerebral blood volume, and electrical brain activity in severely asphyxiated newborns. However, a systematic review of this and 2 other studies in such infants was unable to determine whether allopurinol produced clinically important benefits.

Prostatitis. Although allopurinol has been reported to be of benefit in a small study in patients with chronic prostatitis, a systematic review found no other satisfactory evidence of benefit, and considered that the clinical relevance of the original study results was unclear.

Protozoal infections. Allopurinol has been widely used as an adjunct to pentavalent antimonials in the treatment of Old World visceral leishmaniasis, particularly where resistance to antimony alone is likely, although the degree of benefit has been called into question. It has also been used with other drugs such as pentamidine or azole antifungals, including in transplant patients or those with AIDS, or in whom antimonials were otherwise poorly tolerated. Allopurinol has also been tried alone or with other drugs in both Old World and New World cutaneous or mucocutaneous leishmaniasis; results, particularly in the latter, have been variable. Some beneficial results have been noted in indeterminate and chronic Chagas’ disease (American trypanosomiasis), although it may be less effective than itraconazole. The selective antiparasitic action of allopurinol is believed to be due to its incorporation into the protozoal, but not the mammalian, purine salvage pathway. This leads to the formation of 4-aminopyrazolopyrimidine ribonucleotide triphosphate, a highly toxic analogue of adenosine triphosphate, that is incorporated into ribonucleic acid. This action of allopurinol is shared by allopurinol riboside, one of the minor metabolites in man, but not by oxipurinol, the major human metabolite. Thus, some studies have been conducted with allopurinol riboside, rather than allopurinol, in an attempt to enhance activity by avoiding host-mediated inactivation.

Renal calculi. In conjunction with a reduced dietary purine intake, high fluid intake, and potassium citrate, allopurinol may be used to prevent the recurrence of calcium oxalate renal calculi in patients with hyperuricosuria. The recommended oral dose of allopurinol is 200 to 300 mg daily adjusted on the basis of subsequent 24-hour urinary urate excretion. Allopurinol is also advocated for the management of 2,8-dihydroxyadenine (2,8-DHA) renal stones associated with deficient activity of the enzyme adenine phosphoribosyltransferase.

Sarcoidosis. Although corticosteroids remain the mainstay of drug therapy for sarcoidosis, and other drugs are very much second line, there are reports of benefit in cutaneous disease from the use of allopurinol.

Schizophrenia. Involvement of purinergic neurotransmission has been hypothesised to play some role in schizophrenia, and allopurinol has been investigated as a possible adjunctive treatment, with some evidence of benefit, especially in patients with refractory positive symptoms.

Skin disorders. Reactive perforating collagenosis (RPC) is a condition in which altered collagen is eliminated through the epidermis; it may be inherited or acquired. In 3 of 4 patients with RPC refractory to antibacterials and oral and topical corticosteroids, significant improvement was seen with allopurinol, in terms of reduction of new lesions, improvement of existing lesions, and reduction of pruritus. The fourth patient died from unrelated causes before review.

Preparations

British Pharmacopoeia 2008; Allopurinol Tablets;

The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Allopurinol Oral Suspension; Allopurinol Tablets.

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Alfadiman; Alloboxal¤; Gotir¤; Puritenk; Australia: Allohexal; Alloremed¤; Allorin¤; Allosig; Capurate; Progout; Zygout¤; Zyloprim; Austria: Allostad; Allotyrol; Apurin; Gewapurol; Gichtex; Purinol; Urosin; Zyloric; Belgium: Zyloric; Brazil: Labopurinol; Lopurax; Uricemil; Zyloric; Canada: Alloprin¤; Novo-Purol¤; Purinol¤; Zyloprim; Chile: Talol; Urogotan A; Zyloric; Czech Republic: Apurol; Milurit; Purinol; Denmark: Abopur; Apurin; Hexanurat; Finland: Allonol; Apurin; Arturic; Zyloric; France: Xanturic¤; Zyloric; Germany: Allo-300-Tablinen¤; Allo-Efeka; Allo-Puren; Allo; Allobeta; Allohexal¤; Allop-Gry¤; Allpargin¤; Apulonga¤; Bleminol; Cellidrin; Dabroson¤; dura AL; Embarin¤; Epidropal; Foligan; Jenapurinol; Milurit; Pureduct¤; Remid; Sigapurol¤; Suspendol¤; Uribenz; Uripurinol¤; Urobenyl¤; Urosin¤; Urtias¤; Zyloric; Greece: Soluric; Zylapour; Zyloric; Hong Kong: Allnol¤; Allorin¤; Caplenal¤; Mephanol¤; Milurit; Progout; Zyloric; Hungary: Harpagin; Milurit; India: Ciploric; Zyloric; Ireland: Caplenal¤; Purinol; Tipuric; Zyloric; Israel: Alloril; Zylol; Zyloric; Italy: Allurit; Uricemil¤; Zyloric; Malaysia: Harpagin¤; Uritab¤; Zyloric; Mexico: Acyprin; Apo-Tinole; Atisuril; Aurigen¤; Darzune; Etindrax; Labypurol¤; Oloprim¤; Unizuric; Zyloprim; Netherlands: Apurin; Zyloric; Norway: Allopur; Arturic; Zyloric; New Zealand: Allohexal; Allorin; Progout; Z 300¤; Zyloprim¤; Portugal: Alosfar; Uriprim; Zurim; Zyloric; Russia: Purinol (Пуринол); South Africa: Abburic¤; Be-Uric¤; Ethipurinol¤; Lo-Uric¤; Lonol; Puricos; Pyrazol¤; Ranpuric¤; Redurate; Urinol; Urozyl-SR¤; Zyloprim; Singapore: Allorin¤; Erloric¤; Progout; Valeric¤; Zyloric; Spain: Allopurin¤; Allural¤; Zyloric; Sweden: Zyloric; Switzerland: Allo-300-Tablinen¤; allo-basan; Allopur; Cellidrine; Foligan¤; Lysuron¤; Mephanol; Sigapurol N; Uredimin¤; Uriconorme; Zyloric; Thailand: Alinol; Allopin; Allorin¤; Apnol; Apurol; Loporic¤; Medoric; Mephanol¤; Puricin; Puride; Sigapurol¤; Uricad; Valeric; Xanol; Zyloric; United Kingdom: Aloral¤; Aluline¤; Caplenal; Cosuric; Hamarin¤; Progout¤; Rimapurinol; Xanthomax¤; Zyloric; United States: Aloprim; Lopurin¤; Zyloprim; Venezuela: Aluprol; Aluron; Zyloric

Multi-ingredient Preparations

Argentina: Artrex; Colpuril; Austria: Allobenz; Duovitan¤; Gichtex plus; Uroplus¤; Belgium: Comburic; France: Anurate¤; Desatura¤; Germany: Acifugan¤; Allo.comp.; Allomaron¤; Harpagin; Uricovac comp¤; Italy: Uricodue; Urifugan¤; Portugal: Acifugan¤; South Africa: Allomaron; Spain: Acifugan¤; Biuricowas¤; Facilit¤; Uricina¤; Switzerland: Acifugan¤; Thailand: Allomaron

ALLOPURINOL

ALLOPURINOL (al-oh-PURE-i-nole)

Other Names for this Medication (Brand Names)

7HP, Adenock, Ailural, Allo-Puren, Allohexal, Allopur, Allozym, Allural, Aloprim, Aloral, Alositol, Aluline, Anoprolin, Anzief, Apo-Allopurinol, Apulonga, Apurin, Apurol, Atisuril, Bleminol, Bloxanth, Caplenal, Cellidrin, Cosuric, Dabrosin, Dabroson, Dura Al, Embarin, Epidropal, Epuric, Foligan, Geapur, Gichtex, Gotax, HPP, Hamarin, Hexanuret, Ketanrift, Ketobun-A, Ledopur, Lopurin, Lysuron, Milurit, Miniplanor, Monarch, Nektrohan, Progout, Purinol, Remid, Riball, Sigapurol, Suspendol, Takanarumin, Urbol, Uricemil, Uriprim, Uripurinol, Uritas, Urobenyl, Urolit, Urosin, Urtias, Urtias 100, Xanturat, Zyloprim, Zyloric

Appearance

Oral Tablets – Round tablet containing 100mg (white), 200mg (peach) and 300mg (orange) allopurinol.

Why this Medication is Used

Cancer chemotherapy drugs or radiation therapy are given to kill cancer cells in the body. One of the waste products of the dead cancer cells is uric acid. If uric acid builds up in the body, it can cause kidney damage or joint pain (called gout). Allopurinol helps to prevent the build up of uric acid.

How do you take this Medication

Oral Tablets: It is important to take your medicine regularly as ordered by your doctor.

Precautions

• To help reduce stomach upset, it is best to take this drug after meals.

• Drink at least 8 full glasses of liquids each day unless otherwise directed by your doctor.

• It is best to avoid or limit the amount of alcohol you drink. Alcohol may increase the amount of uric acid in the body.

• Check with your doctor or nurse before you take Vitamin C supplements.

• Tell your doctor if you have a history of kidney disease.

• Allopurinol can interact with other medications (e.g. warfarin, azathioprine, mercaptopurine and others). Tell your doctor or pharmacist about ALL medications you are taking before starting on this medication.

• Store this medicine in a cool dry place. Keep out of the reach of children.

For more information on this medication, please call your doctor, pharmacist or nurse.

SIDE EFFECTS PREVENTION WHAT YOU SHOULD DO
MORE COMMON:
• Skin rash, hives, itching.

• Diarrhea, stomach cramps, nausea and vomiting.

• Take medication with food. • Stop taking the drug and phone your doctor or nurse as soon as possible.

• Eat frequent small meals.

• Eat bland, non-gassy foods.

• If stomach pain and/or nausea and vomiting continue longer than 24-48 hours check with your doctor.

LESS COMMON:
Sleepiness • Maintain regular bedtime hours. • Rest. Don’t drive a car or operate machinery if you are sleepy. Sleepiness may lessen as your body adjusts to the medicine.
RARE:
• Flu-like symptoms including chills, fever, joint pain, sore throat, nausea and vomiting especially if they occur together with a skin rash. • Stop taking the drug and seek medical attention IMMEDIATELY. These effects may be the first sign of a serious reaction to allopurinol.