Smoothie. Some people are better able to. This agent has little effect on established graft rejections or secondary responses. Others: Additional side effects of low frequency have been reported. The drug suppresses hypersensitivities of the cell-mediated type and causes variable alterations in antibody production. Azathioprine can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. The easiest way to lookup drug information, identify pills, check interactions and set up your own personal medication records. [9] In 2018, it was the 358th most commonly prescribed medication in the United States, with more than 800,000 prescriptions. Blood and urine tests may be needed to check for unwanted effects. Drug information provided by: Merative, Micromedex. Azathioprine may be administered in a single dose or twice-daily doses. Because of the risk of toxicity, patients with TPMT or NUDT15 deficiency require alternative therapy or dose modification (see DOSAGE AND ADMINISTRATION). The use of Azathioprine in nursing mothers is not recommended. This document does not contain all possible drug interactions. Accurate phenotyping (red blood cell TPMT activity) results are not possible in patients who have received recent blood transfusions (see CLINICAL PHARMACOLOGY, WARNINGS: Cytopenias, ADVERSE REACTIONS and DOSAGE AND ADMINISTRATION sections). Check with your doctor as soon as possible if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination. Renal Homotransplantation: The dose of Azathioprine required to prevent rejection and minimize toxicity will vary with individual patients; this necessitates careful management. Subscribe to Drugs.com newsletters for the latest medication news, new drug approvals, alerts and updates. This effect can cause anemia, decrease your body's ability to fight an infection, or cause easy bruising/bleeding. However, acute myelogenous leukemia as well as solid tumors have been reported in patients with rheumatoid arthritis who have received Azathioprine. Effects on the neonate of prednisone and Azathioprine administered to the mother during pregnancy. Azathioprine is usually given as a single daily dose on the day of, and in a minority of cases 1 to 3 days before, transplantation. Keep all medical and lab appointments. Azathioprine, an immunosuppressive antimetabolite, is available in tablet form for oral administration. Careful monitoring by your doctor may decrease your risk. These patients have subnormal responses to vaccines, low numbers of T-cells, and abnormal phagocytosis by peripheral blood cells, but their mitogenic responses, serum immunoglobulins, and secondary antibody responses are usually normal. It is recommended that a further dose reduction or alternative therapies be considered for patients with low or absent TPMT activity receiving Azathioprine and xanthine oxidase inhibitors because both TPMT and XO inactivation pathways are affected (see CLINICAL PHARMACOLOGY, WARNINGS, PRECAUTIONS: Laboratory Tests and ADVERSE REACTIONS sections). Each scored tablet contains 50 mg azathioprine and the inactive ingredients lactose monohydrate, pregelatinized starch, povidone, corn starch, magnesium stearate, and stearic acid. Guidelines and recommendations for safe handling of antineoplastic agents. Recommendations for the safe handling of parenteral antineoplastic drugs. Schusziarra V, Ziekursch V, Schlamp R, et al. Azathioprine oral tablet is used to treat rheumatoid arthritis and to keep your immune system from attacking a new kidney after a transplant. It is a pale yellow solid with a slightly bitter taste and a melting point of 238245C. Each scored tablet contains 50 mg, 75 mg or 100 mg Azathioprine, USP and the inactive ingredients anhydrous lactose, magnesium stearate, povidone, pregelatinized starch (corn starch), and stearic acid. Ribavirin is known to inhibit IMDH, thereby leading to accumulation of an Azathioprine metabolite, 6-methylthioionosine monophosphate (6-MTITP), which is associated with myelotoxicity (neutropenia, thrombocytopenia, and anemia). It is very important that your doctor check your progress at regular visits for any problems that may be caused by this medicine. [48] They presented with a very aggressive disease course, and with one exception, died of the lymphoma. [59], Traditionally, as for all cytotoxic drugs, the manufacturer advises not to breastfeed whilst taking azathioprine, but the "lactation risk category" reported by Thomas Hale in his book Medications and Mothers' Milk lists azathioprine as "L3", termed "moderately safe". [77] Following the work done by Sir Peter Medawar and Gertrude Elion in discovering the immunological basis of rejection of transplanted tissues and organs, and Schwartz's researches on 6-MP, Sir Roy Calne, the British pioneer in transplantation, introduced 6-MP as an experimental immunosuppressant for kidney and heart transplants. Make your tax-deductible gift and be a part of the cutting-edge research and care that's changing medicine. Azathioprine is also used to treat symptoms of rheumatoid arthritis. The risks of secondary infection and malignancy are also significant (see WARNINGS). 1987. Mayo Clinic does not endorse companies or products. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Azathioprine (AZA) is a medication used in the management and treatment of active rheumatoid arthritis (RA) and the prevention of kidney transplant rejection. Tell your doctor about all your current medicines. [35][37] Certain genetic variations within the TPMT gene can lead to decreased or absent TPMT enzyme activity, and individuals who are homozygous or heterozygous for these types of genetic variations may have increased levels of TGN metabolites and an increased risk of severe bone marrow suppression (myelosuppression) when receiving azathioprine. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose). To help you remember, take it at the same time(s) each day. A gastrointestinal hypersensitivity reaction characterized by severe nausea and vomiting has been reported. As usual for patients with increased risk for skin cancer, exposure to sunlight and ultraviolet light should be limited by wearing protective clothing and using a sunscreen with a high protection factor. Portions of this document last updated: Feb. 01, 2023. Azathioprine can be discontinued abruptly, but delayed effects are possible. Tallent et al described an infant with a large myelomeningocele in the upper lumbar region, bilateral dislocated hips, and bilateral talipes equinovarus. Azathioprine tablets should not be given to patients who have shown hypersensitivity to the drug. If you miss a dose, take it as soon as you remember. Early drug discontinuation may be considered in patients with abnormal CBC results that do not respond to dose reduction (see CLINICAL PHARMACOLOGY, WARNINGS: Cytopenias, and PRECAUTIONS: Laboratory Tests). [8] It is on the World Health Organization's List of Essential Medicines. Package insert / product label A single case has been reported of a renal transplant patient who ingested a single dose of 7500 mg Azathioprine. [13], Azathioprine has been used in the management of moderate to severe chronically active Crohn's disease,[17] to maintain clinical remission (absence of disease activity) in corticosteroid-dependent patients,[18] and to provide benefit in people with fistulizing Crohn's disease. The majority occurred in patients with inflammatory bowel disease. AMA Council on Scientific Affairs. Hepatotoxicity manifest by elevation of serum alkaline phosphatase, bilirubin, and/or serum transaminases is known to occur following Azathioprine use, primarily in allograft recipients. In the US - Call your doctor for medical advice about side effects. Concerns about increased risk of malignancy has led to a decreased use, yet it is still used in maintenance treatment for people who frequently relapse. Your doctor may adjust your dose as needed. Also call your doctor at once if you have: signs of infection (fever, chills, weakness, flu symptoms, sore throat, cough, pain or burning when you urinate); dark urine, jaundice (yellowing of the skin or eyes). Azathioprine is metabolized to 6-mercaptopurine (6-MP). thiopurine nucleotides can help to optimize the efficacy and safety. Jones RB, Frank R, Mass T. Safe handling of chemotherapeutic agents: a report from The Mount Sinai Medical Center. hair loss. AdultsDose is based on body weight and must be determined by your doctor. [10], Azathioprine is used alone or in combination with other immunosuppressive therapy to prevent rejection following organ transplantation, and to treat an array of autoimmune diseases, including rheumatoid arthritis, pemphigus, systemic lupus erythematosus, Behet's disease, and other forms of vasculitis, autoimmune hepatitis, atopic dermatitis, myasthenia gravis, neuromyelitis optica (Devic's disease), restrictive lung disease, and others. Azathioprine tablets are indicated as an adjunct for the prevention of rejection in renal homotransplantation. You may not be able to continue taking other arthritis medications together with azathioprine. Your doctor will perform blood tests to make sure you do not have conditions that would prevent you from safely using azathioprine. You should not become pregnant while using azathioprine. It dissolves in alkaline aqueous solutions, where it hydrolyzes to 6-mercaptopurine.[68]. There is no general agreement that all of the procedures recommended in the guidelines are necessary or appropriate. Azathioprine was synthesized by George Herbert Hitchings and Gertrude Elion in 1957 (named BW57-322) to produce 6-MP in a metabolically active, but masked form, and at first used as a chemotherapy drug. These cases have had a very aggressive disease course and have been fatal. Use with Other Agents Affecting Myelopoesis: Use with Angiotensin-Converting Enzyme Inhibitors: We comply with the HONcode standard for trustworthy health information. Taking this medication after meals may help lessen these effects. Azathioprine sometimes causes nausea or vomiting. The TPMT*2, TPMT*3A, and TPMT*3C alleles account for about 95% of individuals with reduced levels of TPMT activity. Clinically, most hospitals resort to on-exchange LC-MS (liquid chromotography mass spectrometry) but the newly developed approach of porous graphitic carbon based chromatography hyphenated with mass spectrometry appears superior with respect to patient care in this respect. Ask your healthcare professional how you should dispose of any medicine you do not use. Available for Android and iOS devices. Usual doses produce blood levels of Azathioprine, and of mercaptopurine derived from it, which are low (<1 mcg/mL). Begins to work in 30 minutes, the effect lasts for 4-5 hours. Tell your doctor right away if you develop any of the following symptoms: unusual tiredness, pale skin, signs of infection (such as sore throat that doesn't go away, fever, chills), easy bruising/bleeding. . Azathioprine is used to prevent organ rejection in people who have received a kidney transplant. However, in some patients, nausea and vomiting may be severe and may be accompanied by symptoms such as diarrhea, fever, malaise, and myalgias (see PRECAUTIONS). Overview of medical management of high-risk, adult patients with moderate to severe Crohn disease. Azathioprine is well absorbed following oral administration. Do not increase your dose or use this drug more often or. Cote CJ, Meuwissen HJ, Pickering RJ. Avoid contact sports or other situations where bruising or injury could occur. [4] Use during pregnancy may result in harm to the baby. Azathioprine (Imuran) is a medication that treats diseases that have to do with your immune system. Hematologic toxicities are dose-related and may be more severe in renal transplant patients whose homograft is undergoing rejection. [58], Azathioprine can cause birth defects. Azathioprine sometimes causes nausea or vomiting. It may take up to 8 weeks before your symptoms improve. Use in Renal Dysfunction: Relatively oliguric patients, especially those with tubular necrosis in the immediate postcadaveric transplant period, may have delayed clearance of Azathioprine or its metabolites, may be particularly sensitive to this drug, and are usually given lower doses. It is usually taken along with other medications to allow your new kidney to function normally. Gastrointestinal: Nausea and vomiting may occur within the first few months of therapy with Azathioprine, and occurred in approximately 12% of 676 rheumatoid arthritis patients. Azathioprine may cause a rare type of lymphoma (cancer) of the liver, spleen, and bone marrow that can be fatal. This is not an estimate of the half-life of Azathioprine itself, but is the decay rate for all 35 S-containing metabolites of the drug. The father was on long-term Azathioprine therapy 7. This medication may increase your risk of getting a rare but very serious (possibly fatal) brain infection (progressive multifocal leukoencephalopathy-PML). In one completed study, the rate of lymphoproliferative disease in RA patients receiving higher than recommended doses of Azathioprine (5 mg/kg per day) was 1.8 cases per 1,000 patient-years of follow-up, compared with 0.8 cases per 1,000 patient-years of follow-up in those not receiving Azathioprine. When given for kidney transplant, azathioprine is usually given right before or on the day of transplant. Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances. However, Viagra can interact with Doxazosin to cause low blood pressure. They should be informed of the danger of infection while receiving Azathioprine and asked to report signs and symptoms of infection to their physician. Tell your doctor if you are pregnant or plan to become pregnant. Consult your pharmacist or local waste disposal company. Keep all medical and lab appointments. Experience with over 16,000 transplants shows a 5-year patient survival of 35% to 55%, but this is dependent on donor, match for HLA antigens, anti-donor or anti-B-cell alloantigen antibody, and other variables. Approximately 0.3% (1:300) of patients of European or African ancestry have two loss-of-function alleles of the TPMT gene and have little or no TPMT activity (homozygous deficient or poor metabolizers), and approximately 10% of patients have one loss-of-function TPMT allele leading to intermediate TPMT activity (heterozygous deficient or intermediate metabolizers). Azathioprine is very similar to mercaptopurine. Pharmacokinetics of Azathioprine under haemodialysis. The cytotoxicity of Azathioprine is due, in part, to the incorporation of 6-TGN into DNA. Using this medicine while you are pregnant can harm your unborn baby. 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