Drug Information 


 






Allopurinol

  
















 
Pharmacokinetics



After oral Intake it is
absorbed relatively rapidly. It is converted to alloxanthine which is
active.


 
Indication
& Dosage


  

Oral : 

PRIMARY GOUT(ACUTE ATTACKS,
TOPHI, ARTHRITIS, URIC ACID STONES OR
NEPHROPATHY) :



  200-600mg/day according to severity. Upto 800mg/day may be given if
required. Higher than 300mg should be given in divided doses after meals.
Enough fluids should be taken to ensure urine output of atleast 2
liters/day.



PREVENTION OF URIC ACID NEPHROPATHY IN PATIENTS RECEIVING HIGH DOSES
OF ANTINEOPLASTIC DRUGS (SECONDARY GOUT) : 


  600-800mg/day for 2 or 3 days with high fluid intake. Discontinue
after the potential for uric acid nephropathy no longer exists.


Children :
(6-10yrs)-300mg/day, less than 6yrs-150mg/day. Dosage may be
adjusted based on the response. 



MANAGEMENT OF RECURRENT CALCIUM OXALATE STONES IN PATIENTS WITH HIGH
EXCREATION OF URIC ACID : 200-300mg/day.
Action

  

Allopurniol is an inhibitor of the enzyme xanthine Oxidase
which converts hypoxanthin to xanthine and uric acid. The reduced
production of uric acid relieves all symptoms associated with
hyperuricaemia and gout. Inhibition of xanthine Oxidase leads to
accumulation of its substrates hypoxanthine and xanthine but since their
renal clearance is more than 10 times that of uric acid, there is no risk
of nephrolithiasis. Omipurinol the metabolite of allopurinol also inhibits
Xanthine Oxidase.

 

Interactions

ACE inhibitors /
Risk of hypersensitivity reactions

Aluminum salts /
Effect of allopurinol


Ampicillin / Risk
of ampicillin-induced skin rashes


Anticoagulants, oral /
Effect of anticoagulant due to
breakdown by liver


Azathioprine /
Effect of azathioprine due to
breakdown by liver


Cyclophosphamide /
Risk of bleeding or infection due to
myelosuppressive effects of cyclophosphamide


Iron preparations / Allopurinol
hepatic iron concentrations


Mercaptopurine /
Effect of mercaptopurine due to
breakdown by liver


Theophylline / Allopurinol
plasma theophylline levels
possible toxicity


Thiazide diuretics /
Risk of hypersensitivity reactions to allopurinol


Uricosuric agents /
Effect of oxipurinol due to
rate of excretion


Adverse
Effect & Precaution




Hypersensitivity reactions, maculopapapular rash,
uriticaria, myalgia, malaise fever, transiet leucopenia or leukocytosis,
hepatic damage, nausea, vomiting, diarrhoea, headache, drowsiness.


Preacution: Hepatic or renal
dysfucntion, ensure adequate hydration

Pregnancy: Use with caution

Breast Feeding: Contraindicated

Man: Use with caution
  

 

Brand
available in Market




 






Allgoric

Kamron
TAB 100mg 10 12.03
Zyloric

Burroughs Wellcome
TAB 100mg 10 12.04





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Allopurinol
  

 

Pharmacokinetics

After oral Intake it is absorbed relatively rapidly. It is converted to alloxanthine which is active.
 

Indication & Dosage
  
Oral : 
PRIMARY GOUT(ACUTE ATTACKS, TOPHI, ARTHRITIS, URIC ACID STONES OR NEPHROPATHY) :
  200-600mg/day according to severity. Upto 800mg/day may be given if required. Higher than 300mg should be given in divided doses after meals. Enough fluids should be taken to ensure urine output of atleast 2 liters/day.

PREVENTION OF URIC ACID NEPHROPATHY IN PATIENTS RECEIVING HIGH DOSES OF ANTINEOPLASTIC DRUGS (SECONDARY GOUT) : 
  600-800mg/day for 2 or 3 days with high fluid intake. Discontinue after the potential for uric acid nephropathy no longer exists.
Children : (6-10yrs)-300mg/day, less than 6yrs-150mg/day. Dosage may be adjusted based on the response. 

MANAGEMENT OF RECURRENT CALCIUM OXALATE STONES IN PATIENTS WITH HIGH EXCREATION OF URIC ACID : 200-300mg/day.

Action
  
Allopurniol is an inhibitor of the enzyme xanthine Oxidase which converts hypoxanthin to xanthine and uric acid. The reduced production of uric acid relieves all symptoms associated with hyperuricaemia and gout. Inhibition of xanthine Oxidase leads to accumulation of its substrates hypoxanthine and xanthine but since their renal clearance is more than 10 times that of uric acid, there is no risk of nephrolithiasis. Omipurinol the metabolite of allopurinol also inhibits Xanthine Oxidase.

 

Interactions

ACE inhibitors / Risk of hypersensitivity reactions Aluminum salts / Effect of allopurinol Ampicillin / Risk of ampicillin-induced skin rashes Anticoagulants, oral / Effect of anticoagulant due to breakdown by liver Azathioprine / Effect of azathioprine due to breakdown by liver Cyclophosphamide / Risk of bleeding or infection due to myelosuppressive effects of cyclophosphamide Iron preparations / Allopurinol hepatic iron concentrations Mercaptopurine / Effect of mercaptopurine due to breakdown by liver Theophylline / Allopurinol plasma theophylline levels possible toxicity Thiazide diuretics / Risk of hypersensitivity reactions to allopurinol Uricosuric agents / Effect of oxipurinol due to rate of excretion

Adverse Effect & Precaution

Hypersensitivity reactions, maculopapapular rash, uriticaria, myalgia, malaise fever, transiet leucopenia or leukocytosis, hepatic damage, nausea, vomiting, diarrhoea, headache, drowsiness.
Preacution: Hepatic or renal dysfucntion, ensure adequate hydration
Pregnancy: Use with caution
Breast Feeding: Contraindicated
Man: Use with caution
  

 

 

Allgoric

Kamron

TAB

100mg

10

12.03

Zyloric

Burroughs Wellcome

TAB

100mg

10

12.04


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By |2022-07-20T16:44:52+00:00July 20, 2022|Uncategorized|Comments Off on Allopurinol

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