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Azathioprine is an immunosuppressant (purine antimetabolite) taken by mouth that pharmacies may compound, including as an oral suspension, on a prescriber's order.
Azathioprine is an immunosuppressant in the thiopurine class. The body converts it to mercaptopurine and then to thioguanine nucleotides, which are built into DNA and slow the growth and activation of immune cells (lymphocytes). Manufactured products include Imuran and Azasan tablets, generic azathioprine tablets, and azathioprine sodium for injection. The Imuran label lists two uses: as an add-on to prevent rejection after kidney transplant, and to reduce signs and symptoms of active rheumatoid arthritis. No commercial liquid form exists, and a stability study in the International Journal of Pharmaceutical Compounding examined compounded azathioprine oral suspensions. A prescriber might order azathioprine compounded as a liquid or in a strength or form that is not manufactured. Compounded preparations are not FDA-approved and require a prescription.
Imuran carries a boxed warning for malignancy: long-term immunosuppression raises cancer risk, including lymphoma after transplant and hepatosplenic T-cell lymphoma in people with inflammatory bowel disease. It can cause severe drops in blood cells, so regular blood counts are needed; people with low TPMT or NUDT15 enzyme activity face a higher risk. Serious infections can occur, and sun exposure should be limited because of skin cancer risk. Allopurinol or febuxostat can raise azathioprine to toxic levels; ACE inhibitors, co-trimoxazole and ribavirin can worsen low blood counts; azathioprine may weaken warfarin. Do not use it if you are allergic to it, or for rheumatoid arthritis during pregnancy; people with rheumatoid arthritis previously treated with alkylating drugs such as cyclophosphamide may face a prohibitive cancer risk. The label says it can cause fetal harm and is not recommended while nursing; LactMed reports low or unmeasurable levels in milk and says many experts consider it acceptable during breastfeeding. Report unusual bleeding, bruising or fever right away. For other side effects, talk to your prescriber or pharmacist.
Azathioprine is metabolized to 6-mercaptopurine (6-MP), which is activated through HGPRT to 6-thioguanine nucleotides (6-TGN); incorporation of 6-TGN into DNA contributes to cytotoxicity. 6-MP is inactivated by TPMT (to 6-MeMP) and xanthine oxidase (to 6-thiouric acid), and NUDT15 converts 6-TGNs to inactive monophosphates. Oral bioavailability is variable (StatPearls); azathioprine and 6-MP are about 30% protein bound, and clinical effect tracks tissue thiopurine nucleotide levels rather than plasma levels. Labeled indications (Imuran tablets): adjunct for prevention of rejection in renal homotransplantation, and active rheumatoid arthritis; the label does not recommend combined use with other DMARDs. The label contraindicates use for rheumatoid arthritis in pregnant women and warns of prohibitive malignancy risk in RA patients previously treated with alkylating agents. StatPearls describes use in autoimmune hepatitis, SLE, ANCA-associated vasculitis and inflammatory myopathies, which are not FDA-approved indications. Prescribers have ordered compounded azathioprine oral suspension; a 2023 IJPC study reported physical, chemical and microbiological stability of such suspensions under refrigerated and room-temperature storage. Dosing is per prescriber; the label advises alternative therapy in homozygous TPMT or NUDT15 deficiency, reduced dosing in heterozygous deficiency, dose reduction with allopurinol, and avoiding febuxostat. Monitor CBC with platelets weekly in the first month, twice monthly in months two and three, then monthly; StatPearls adds baseline liver and renal tests, hepatitis B and C and tuberculosis screening, and TPMT/NUDT15 testing.
Compounded at Bayview
Patient guides for the preparations we make most often. Each one is compounded to order and requires a prescription.
We do not have a patient page for this ingredient yet. That does not mean we cannot make it. Bayview compounds this ingredient to a prescriber's order, and our full compounding formulary lists every preparation we make. Viewing the formulary requires a prescriber account.
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Every preparation in our formulary that contains this ingredient. Strength, base and dose form are set by the prescription.
Other salt forms of this molecule, and ingredients commonly compounded alongside it.
This page describes an active pharmaceutical ingredient, not a finished drug product. Bayview Pharmacy compounds preparations containing it only on a prescriber's order for an individual patient.
Compounded preparations are not FDA-approved, and the FDA has not evaluated them for safety, effectiveness, or manufacturing quality. Nothing on this page is a claim that any preparation is effective for any condition.
A valid prescription is required. Availability depends on Bayview's licensure in your state. This page is general information, not medical advice. Discuss your situation with a licensed healthcare provider.
Our pharmacists work with prescribers to build preparations around a patient's dose, form and tolerances. Ask us what is possible with this ingredient.
