Allopurinol

Allopurinol is isomer of hypoxanthine, a purine. An alternative to increasing uric acid excretion in the treatment of gout is to reduce its synhtesis by inhibiting xanthine oxidase with it. It reduces elevated blood uric acid levels caused by certain conditions such as those associated with malignancies or in kidney diseases.


Adult Dose
Dose: 300 to 600 mg
Single Dose: 450 (450)
Frequency: 24 hourly
Route: PO
Instructions:
Neonatal
Dose: 10 to 20 mg/kg
Single Dose: 15 (15)
Frequency: 24 hourly
Route: oral
Instructions:
Paedriatic
Dose: 10 to 20 mg/kg/day
Single Dose: 15 (15)
Frequency: As recommended.
Route: Oral
Instructions: For under 15 years of age: maximum 400 mg/day in neoplastic condition, enzymes disorder.
Characteristics
. It is of Synthetic origin and belongs to Pyrazolol. It belongs to Analgesics and Anti-inflammatory Agents pharmacological group.The Molecular Weight of Allopurinol is 136.10. Its pKa is 10.2.
Contraindications
Allopurinol
Effects
The severe or irreversible adverse effects of Allopurinol, which give rise to further complications include Granulomatous hepatitis.Allopurinol produces potentially life-threatening effects which include Stevens Johnson syndrome, Stevens Johnson syndrome, Hepatitis, Eosinophilia, Lymphadenopathy, Interstitial nephritis. which are responsible for the discontinuation of Allopurinol therapy.The signs and symptoms that are produced after the acute overdosage of Allopurinol include GI intolerance.The symptomatic adverse reactions produced by Allopurinol are more or less tolerable and if they become severe, they can be treated symptomatically, these include Skin rashes, Pruritus, Skin rashes.
Indications
Allopurinol is primarily indicated in conditions like Acute uric acid nephropathy, Calcium oxalate/ phosphate renal stones, Hypothyroidism (myxoedema), Idiopathic gout, Myeloproliferative disorders, Neoplastic disease, Uric acid lithiasis.
Interactions
Allopurinol is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAminophyllineAmpicillinIncreased risk of rash when allopurinol given with ampicillin.AzathioprineAllopurinol inhibits the hepatic and intestinal metabolism of thiopurine results in increased plasma level leads to enhanced pharmacological and toxic effects such as bone marrow depression.MajorDose of thiopurine should be reduce approximately 1/4 to 1/3 of the usual dose.Closely monitor for hematologic toxicity. Patient should notify to physician if experience thiopurine toxicity.BamifyllineBendrofluazideCaptoprilIncreased risk of toxicity when Allopurinol given with Captopril especially in renal impairment. Captopril may enhance the potential for allergic or hypersensitivity reactions to Allopurinol. MajorImmediate (Sequence important)ChlorothiazideChlorpropamideAllopurinol reduces the renal excretion and prolong the half-life of chlorpropamide.MinorMonitor blood sugar of patient regularly.ChlorthalidoneCop-FluampicilCyclophosphamideAllopurinol induces the hepatic metabolism of cyclophosphamide or decrease its renal clearenceresult in enhanced myelosuppressive side effects.ModerateClosely monitor for myelosuppression, hemorrhagic cystitis, cardiotoxicity, interstitial pneumonitis and bleeding.Cyclosporin AAllopurinol possibly increases plasma concentration of ciclosporin (risk of nephrotoxicity).DidanosineAllopurinol possibly increases plasma concentration of didanosine.Enalapril (Maleate)FluorouracilFosphenytoinHydrochlorothiazideconcomitant administeration can lead to impaired renal functionHydroflumethiazideMercaptopurine (Monohydrate)Allopurinol enhances effects and toxicity of azothiaprine.Reduice doses of Mercaptopurine.MoexiprilOxtriphylline (Choline Theophyllinate)Phenytoin (Na)Probenecidprobencid promotes the excretion of allopurinols active metaboliteSulphinpyrazoneSultamicillinThe concurrent administration of allopurinol and ampicillin increases substantially the incidence of rashes in patients receiving both drugs Avoid concurrent useTamoxifen (Citrate)TheophyllineAllopurinol possibly increases plasma concentration of theophylline by inhibiting its metabolism results in increased toxicity.MinorClosely monitor for theophylline toxicity.Vidarabine (Monohydrate)Vincristine (Sulphate)Coadministration of these agents may enhanced the risk of peripheral neuropathy.ModerateClosely monitor for the symptoms of neuropathy. Reduce the dose or discontinue drug if symptoms of peripheral neuropathy appear.Warfarin (Na)Allopurinol may enhance the anticoagulant effect of Warfarin by inhibiting its metabolism.ModerateMonitor increased prothrombin times (PT)/therapeutic effects of Warfarin if allopurinol is initiated/dose increased, or decreased effects if Allopurinol is discontinued/dose decreased. Reductions in Warfarin dosage will likely be needed. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, Geriatrics, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.
Warnings
Periodically perform liver and kidney function and complete blood counts, especially during first few months of therapy. Allopurinol should be used with caution in patients with renal (kidney) impairment. Initially give low doses of allopurinol to patients and increase at weekly intervals by 100 mg until serum uric acid level of 6 mg/dl or less is attained with out exceeding maximum recommended dose.
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