azathioprine

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Related to Azothioprine: methotrexate

azathioprine

 [a″zah-thi´o-prēn]
a mercaptopurine derivative used as an immunosuppressive agent for prevention of transplant rejection in organ transplantation; as a disease-modifying antirheumatic drug for treatment of severe, progressive rheumatoid arthritis unresponsive to other agents; and for treatment of a number of autoimmune diseases; administered orally as the base or intravenously as the sodium salt.

azathioprine

Apo-Azathioprine (CA), Azasan, Gen-Azathioprine (CA), Immunoprin (UK), Imuran, Novo-Azathioprine (CA)

Pharmacologic class: Purine antagonist

Therapeutic class: Immunosuppressant

Pregnancy risk category D

FDA Box Warning

• Drug may cause chronic immunosuppression, increasing neoplasia risk. Physicians using it should be familiar with this risk and with possible hematologic toxicities and mutagenic potential in both sexes.

Action

Prevents proliferation and differentiation of activated B and T cells by interfering with synthesis of purine, DNA, and RNA

Availability

Injection: 100-mg vial

Tablets: 50 mg, 75 mg, 100 mg

Indications and dosages

To prevent rejection of kidney transplant

Adults and children: Initially, 3 to 5 mg/kg/day P.O. or I.V. as a single dose. Give on day of transplantation or 1 to 3 days before day of transplantation; then 3 to 5 mg/kg/day I.V. after surgery until patient can tolerate P.O. route. Maintenance dosage is 1 to 3 mg/kg/day P.O.

Rheumatoid arthritis

Adults and children: Initially, 1 mg/kg P.O. or I.V. in one or two daily doses. Increase dosage in steps at 6 to 8 weeks and thereafter at 4-week intervals; use dosage increments of 0.5 mg/kg/day, to a maximum dosage of 2.5 mg/kg/day. Once patient stabilizes, decrease in decrements of 0.5 mg/kg/day to lowest effective dosage.

Dosage adjustment

• Renal disease
• Concurrent allopurinol therapy
• Elderly patients

Off-label uses

• Crohn's disease
• Myasthenia gravis
• Chronic ulcerative colitis

Contraindications

• Hypersensitivity to drug
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• chickenpox, herpes zoster, impaired hepatic or renal function, decreased bone marrow reserve
• previous therapy with alkylating agents (cyclophosphamide, chlorambucil, melphalan) for rheumatoid arthritis
• elderly patients
• women of childbearing age.

Administration

• Give after meals.
• Be aware that I.V. administration is intended for use only when patients can't tolerate oral medications.

Adverse reactions

CNS: malaise

EENT: retinopathy

GI: nausea, vomiting, diarrhea, stomatitis, esophagitis, anorexia, mucositis, pancreatitis

Hematologic: anemia, thrombocytopenia, leukopenia, pancytopenia

Hepatic: jaundice, hepatotoxicity

Musculoskeletal: muscle wasting, joint and muscle pain

Skin: rash, alopecia

Other: chills, fever, serum sickness, neoplasms, serious infection

Interactions

Drug-drug.Allopurinol: increased therapeutic and adverse effects of azathioprine

Angiotensin-converting enzyme (ACE) inhibitors, co-trimoxazole: severe leukopenia

Anticoagulants, cyclosporine: decreased actions of these drugs

Atracurium, pancuronium, tubocurarine, vecuronium: reversal of these drugs' actions

Drugs affecting bone marrow and bone marrow cells (such as ACE inhibitors, co-trimoxazole): severe leukopenia

Drug-diagnostic tests.Alanine aminotransferase, alkaline phosphatase, amylase, aspartate aminotransferase, bilirubin: increased levels

Albumin, hemoglobin, uric acid: decreased levels

Urine uric acid: decreased level

Drug-herbs.Astragalus, echinacea, melatonin: interference with immunosuppressant action

Patient monitoring

Monitor CBC, platelet level, and liver function test results.
• Assess for signs and symptoms of hepatotoxicity (clay-colored stools, pruritus, jaundice, and dark urine).
• Watch for signs and symptoms of infection.
• Monitor for bleeding tendency and hemorrhage.

Patient teaching

Tell patient that drug lowers resistance to infection. Instruct him to immediately report fever, cough, breathing problems, chills, and other symptoms.

Instruct patient to immediately report unusual bleeding or bruising.
• Tell patient that drug effects may not be obvious for up to 8 weeks in immunosuppression and up to 12 weeks for rheumatoid arthritis relief.

Emphasize importance of avoiding pregnancy during therapy and for 4 months afterward.
• Caution patient to avoid activities that may cause injury. Tell him to use soft toothbrush and electric razor to avoid gum and skin injury.
• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
• Tell patient he'll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

a·za·thi·o·prine

(ā'ză-thī'ō-prēn),
A derivative of 6-mercaptopurine, used as a cytotoxic and immunosuppressive agent.

azathioprine

/aza·thio·prine/ (az″ah-thi´o-prēn) a 6-mercaptopurine derivative used as the base or the sodium salt as an immunosuppressant for prevention of transplant rejection and for treatment of rheumatoid arthritis and various autoimmune diseases.

azathioprine

(ăz′ə-thī′ə-prēn′)
n.
An immunosuppressive agent used to prevent organ rejection in kidney transplant recipients and to treat severe rheumatoid arthritis.

azathioprine

[az′əthī′ōprēn]
an immunosuppressive.
indications It is prescribed to prevent organ rejection after transplantation and to treat lupus erythematosus and other systemic inflammatory diseases, such as rheumatoid arthritis unresponsive to other agents.
contraindications Known hypersensitivity to this drug prohibits its use. It is contraindicated in rheumatoid arthritis and in pregnant women.
adverse effects Among the most serious adverse reactions are bone marrow depression and hepatotoxicity. Nausea and fever are common.

azathioprine

A thiolated purine analogue/immunosuppressant used to prevent rejection of heart, kidney, lung and other allografts, acting primarily on T cells; it is used in rheumatoid arthritis and myasthenia gravis.

Adverse effects
Dose-related marrow suppression—leukopaenia, thrombocytopaenia, macrocytic anaemia); GI tract—nausea, vomiting, diarrhoea, fever, malaise, myalgia, liver enzyme defects, hepatotoxicity, pancreatitis. Azathiprineshould not be given with allopurinol.

Chemistry
Azathioprine is 6-mercaptopurine with a side chain to protect the labile sulfhydryl group, which is split off in the liver; full metabolic activity follows addition of ribose 5-phosphate from phosphoribosyl pyrophosphate that is metabolised to the cytotoxic derivative 6-mercaptopurine.

azathioprine

Imuran® Immunology An immunosuppressant used to prevent rejection of heart, kidney, lung and other allografts, acting primarily on T-cells; it is used in rheumatoid arthritis, myasthenia gravis Adverse effects BM suppression–leukopenia, thrombocytopenia, macrocytic anemia, GI tract–N&V, diarrhea, fever, malaise, myalgia, LFT abnormalities, hepatotoxicity, pancreatitis; should not be given with allopurinol. See Heart transplant, Kidney transplant, Lung transplant, Transplantation.

azathioprine

A drug used to suppress the immune system so as to avoid rejection of donor transplants. Immune suppression may have serious side effects such as the flare-up of latent infections and an increased risk of malignant tumours such as lymphomas, but azathioprine is safer than other immunosuppressive drugs. Also used to treat rheumatism. The drug is on the WHO official list. A brand name is Imuran.

azathioprine

immunosuppressive agent used in the treatment of autoimmune and chronic inflammatory conditions, e.g. severe rheumatoid arthritis and psoriasis, when corticosteroid treatment alone is no longer effective

immunosuppressants

Drugs that prevent or reduce the immune response. They are used in the treatment of a variety of severe inflammations such as uveitis, scleritis, keratoconjunctivitis sicca, Behçet's syndrome, sympathetic ophthalmia, and to prevent corneal graft rejection. They include the corticosteroids (e.g. prednisolone), ciclosporin (cyclosporine), tacrolimus, and cytotoxic agents (e.g. azathioprine, chlorambucil, cyclophosphamide, methotrexate). It must be noted that immunosuppressants render the patient more susceptible to infection because immunity is reduced.

a·za·thi·o·prine

(ā'ză-thī'ō-prēn)
Derivative of 6-mercaptopurine, used as cytotoxic and immunosuppressive agent.

azathioprine (az´əthīōprēn),

n brand name: Imuran;
drug class: immunosuppressant;
action: inhibits purine synthesis in cells, thereby preventing RNA and DNA synthesis;
uses: renal transplants to prevent graft rejection, refractory rheumatoid arthritis, bone marrow transplants, glomerulonephritis.

azathioprine

a mercaptopurine derivative used as a cytotoxic and immunosuppressive agent in the treatment of leukemia and autoimmune diseases and in transplantation therapy.