Azathioprine

Azathioprine is imidazolyl derivative of mercaptopurine. It functions as a structural analog or antimetabolite. As an immunosuppressant, Azathioprine is commonly used in transplant patients but also is useful in the treatment of rheumatoid arthritis, lupus nephritis, and psoriatic arthritis. Azathioprine is being investigated as an agent to prevent the development of diabetes mellitus. It was originally approved by the FDA in 1968. Adverse effects include bone marrow depression.

Brands
AZAFRINE IMURAN AZOPRINE AMORIN AMORIN PHARMAZORINE AZATHIOPRINE AZATHIOPRINE
Adult Dose
Dose: 50 to 300 mg
Single Dose: 180 (175)
Frequency: As recommended.
Route: IV
Instructions: Initially for once
Neonatal
Dose: 1 to 4 mg/kg
Single Dose: 2.5 (2.5)
Frequency: 24 hourly
Route: Intra Venous
Instructions:
Paedriatic
Dose: 1 to 4 mg/kg
Single Dose: 2.5 (2.5)
Frequency: 24 hourly
Route: Intra Venous
Instructions:
Characteristics
. It is of Synthetic origin and belongs to Purine Imidazole. It belongs to Antimetabolites (DNA acting) pharmacological group on the basis of mechanism of action and also classified in Antidotes and Immunosuppressant Agent pharmacological group.The Molecular Weight of Azathioprine is 277.30. Its pKa is 8.2.
Contraindications
Azathioprine is contraindicated in conditions like Renal failure,Impaired hepatic function.
Effects
The severe or irreversible adverse effects of Azathioprine, which give rise to further complications include Liver damage, Pancreatitis.Azathioprine produces potentially life-threatening effects which include Hematological reactions, Carcinogenicity, Infection, GI reactions. which are responsible for the discontinuation of Azathioprine therapy.The signs and symptoms that are produced after the acute overdosage of Azathioprine include Leucopenia, Bone marrow suppression.The symptomatic adverse reactions produced by Azathioprine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Alopecia, Myalgia, Skin RashX, Arthralgia.
Indications
Azathioprine is primarily indicated in conditions like Autoimmune conditions, Derangement of immune system, Nausea and vomiting (prevention), Postmenopausal osteoporosis, Rejection of organ transplants, Suppression of transplant rejection, and can also be given in adjunctive therapy as an alternative drug of choice in Moderate to severe rheumatoid arthritis, Prevention of post-operative nausea and vomiting.
Interactions
Azathioprine is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAllopurinolAllopurinol 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.Balsalazide SodiumPossible increased risk of leucopenia when Balsalazide given with Azathioprine. N/ACaptoprilAzathioprine increases risk of leucopenia with captopril.CyclophosphamideCoadministration results in hepatotoxicity,,hepatocellular necrosis and bone marrow suppression.ModerateClose monitoring for signs and symptoms of hepatotoxicity and myelotoxicity is needed.DidanosineDue to overlapping toxicity profile hematological adverse effects may be observed during their coadministration.ModerateCoadministration should be avoided.Extreme caution and clinical monitoring is advised if they are used together.DiphtheriaTetanus-Acellular Pertussis VaccineMoexiprilConcurrent use may increase the blood pressure or heart rate.Mumps VaccineConcurrent use may weaken the immune system.Pancuronium (Br)Azathioprine decreases or reverse the effects of pancuronium by inhibiting phosphodiestrase in motor nerve terminals.MinorPatient should monitored for neuromuscular blockade and dose adjustment is necessary.PenicillaminePentostatinThe concomitant use of azathioprine and other myelosuppressive or myelotoxic agents may potentiate the risk of hematologic adverse reactions due to overlapping toxicity profiles of these drugs.MinorConcomitant use should generally be avoided. Extreme caution and clinical and laboratory monitoring for hematologic toxicity is advised if these drugs must be used together.TrimethoprimCoadministration increases the risk of bone marrow supression,thrombocytopenia and neutropenia in renal transplant patient.ModerateClose clinical monitoring for hematological adverse effects is recommended during and after therapy.Vecuronium (Br)Warfarin (Na)Azathioprine may diminish the anticoagulant effect of Warfarin. ModerateMonitor for decreased therapeutic effects of Warfarin if Azathioprine is initiated/dose increased, or increased effects if Azathioprine is discontinued/dose decreased. An adjustment in Warfarin dosage may 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, 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, Inj Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.
Warnings
Azathioprine should be used with caution in patients with medical history especially, liver disease, kidney disease, blood disorders, any infection or any allergy. Azathioprine is not recommended during pregnancy or lactation. Hepatic function should be carefully assessed in patients receiving azathioprine especially in patients with pre-existing hepatic disease. Determination of serum alkaline phosphatase, bilirubin and aminotransferase concentration should be performed periodically.
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