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Physician
Patient

Allopurinol
(Tablets of 100 mg or 300 mg)

Composition:
Each tablet contains:
Allopurinol...............................100 mg or 300 mg.
 
Properties:
Allopurinol acts on purine catabolism, without disrupting the biosynthesis of purines. It reduces the production of uric acid by inhibiting the biochemical reaction immediately preceding its formation. Allopurinol is a structural analogue of the natural urine base, hypoxanthine. It is an inhibitor of xanthene oxidase enzyme which is responsible for the conversion of hypoxanthine----->Xanthene ------>uric acid , the end product of purine metabolism in man.
Allopurinol is metabolized to the corresponding xanthene analogue,oxipurinol ( alloxanthine ), which is also an inhibitor of  xanthene oxidase. Allopurinol is approximately 90% absorbed from the gastro- intestinal tract. Peak plasma levels generally occurs at 1.5 hours & 4.5 hours for Allopurinol & oxipurinol. Approximately 20% of the ingested Allopurinol is excreted in the feces.
Allopurinol has a long plasma half-life, approximately 15.0 hours & therefore effective xanthene oxidase inhibition is maintained over a 24 hours period with a single daily dose of Allopurinol.
 
Indications:
To treat primary or secondary hyperuricemia associated with chronic gout, uric acid nephropathy, recurrent uric acid stone formation, enzyme disorders, blood disorders & cancer therapy.
 
Contraindications:
Patients who have developed a severe reaction to Allopurinol should not be restarted on the drug.
 
Precautions:
Allopurinol should not be used for the treatment of an acute attack of gout.
Allopurinol should be administered with care with renal or hepatic impairment.
 
Use during pregnancy & lactation:
Allopurinol should be used during pregnancy only if clearly needed.
Caution should be exercised when Allopurinol is administered to a nursing mother since it is excreted in the breast milk.

 

Drug interaction:
Allopurinol prolongs the half-life of the anticoagulant, dicoumarol. This should be noted when Allopurinol is given to patients on dicoumarol therapy.


In patients receiving mercaptopurine or azathioprine, the concomitant administration of 300-600 mg Allopurinol daily will require a reduction in dose to approximately one-third to one-fourth of the usual dose of mercaptopurine or azathioprine.

Concomitant use of Allopurinol and thiazide diuretics may contribute to enhancement of Allopurinol toxicity in some patients.

Renal function should be monitored in patients on thiazide diuretics and Allopurinol dosage levels should be adjusted if diminished renal function is detected.

Concomitant administration of uricosuric agents and Allopurinol has been associated with a decrease in oxypurine secretion and an increase in urinary uric acid excretion compared with that observed with Allopurinol alone.
 

Dosage & route of administration & duration:
To reduce the possibility of precipitating acute gout:
Dose of 100 mg daily may be given initially and increased by 100 mg daily at weekly intervals until the concentration of uric acid in plasma is about 60 mcg per ml.
The average daily dose is 200 to 300 mg for those with mild gout & 400 to 600 mg for those with moderately to severe gout.
Up to 300 mg may be taken as a single daily dose, larger amount should be taken in divided doses.
Allopurinol is best taken after meals. Doses should be reduced in patients with impaired renal function, 100 to 200 mg daily should be used if the creatinine clearance is between 10 & 20 ml per minute & not more than 100 mg daily if the creatinine clearance is less.

 
Adverse effects:
The most common side effect of allopurinol is skin rash which may occur more frequently in patients with renal failure. Treatment with Allopurinol should be discontinued immediately if a rash develops.

Other side effects of less serious nature include peripheral neuritis, nausea, vomiting, abdominal pain diarrhea, headache & drowsiness.
 
Storage:
Keep at temp. not exceeding 30°C.
Keep medicine out of reach of children.
 
Presentation:
ox of 30 or 1000 tablets (100 mg)
Box of 20 or 1000 tablets(300 mg)

 

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