Names and pronunciation
(ay-za-thye′oh-preen) Azasan, Imuran
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Drug reference
(ay-za-thye′oh-preen) Azasan, Imuran
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Func. class.: Immunosuppressant
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Chem. class.: Purine antagonist
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Do not confuse: azaTHIOprine/azaCITIDine
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ACTION: Produces immunosuppres- sion by inhibiting purine synthesis in cells
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USES: Renal transplants to prevent graft rejection, refractory rheumatoid arthritis
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Unlabeled uses: Chronic ulcerative colitis, Crohn’s disease, autoimmune hepatitis, dermatomyositis, thrombocyto- penic purpura, lupus nephritis, polymyo- sitis, pulmonary fibrosis, systemic lupus erythematosus (SLE), Wegener’s granu- lomatosis, vasculitis, atopic dermatitis
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CONTRAINDICATIONS: Preg- nancy, hypersensitivity, breastfeeding Precautions: Severe renal/hepatic dis- ease, geriatric patients, thiopurine methyltransferase deficiency, infection, bone marrow suppression; must be used by an experienced clinician
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Black Box Warning: Neoplastic disease
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SIDE EFFECTS CNS: Progressive multifocal leukoen- cephalopathy EENT: Retinopathy Resp: Pulmonary edema GI: Nausea, vomiting, stomatitis, esoph- agitis, pancreatitis, hepatotoxicity, jaun- dice, hepatic veno-occlusive disease HEMA: Leukopenia, thrombocytopenia, anemia, pancytopenia, bleeding INTEG: Rash, alopecia MISC: Serum sickness, Raynaud’s symp- toms, secondary malignancy, infection, chills, fever MS: Arthralgia, muscle wasting
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INTERACTIONS Increase: leukopenia—ACE inhibitors, sulfamethoxazole-trimethoprim; monitor for increased leukopenia Increase: myelosuppression—cycloSPO- RINE, antineoplastics; monitor for increased myelosuppression Increase: action of azaTHIOprine—allo- purinol; decrease dose of allopurinol, or avoid using Decrease: immune response—vaccines, toxoids Drug/herb Decrease: product’s effect—cat’s-claw, echinacea; avoid concurrent use Drug/Lab Test Increase: LFTs Decrease: uric acid Interference: CBC, differential count
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DOSAGE AND ROUTES Immunosuppression in kidney transplantation • Adult and child: PO/IV 3-5 mg/kg/ day, then maintenance (PO) of ≥1-3 mg/ kg/day Child/adolescent (unlabeled): PO 1-2 mg/ kg/day with tacrolimus and corticoste- roids Renal dose A • Adult: PO Give lower dose in tubular necrosis in immediate postcadaveric transplant period Refractory rheumatoid arthritis • Adult: PO 1 mg/kg/day, may increase dose after 2 mo by 0.5 mg/kg/day and then q4wk, max 2.5 mg/kg/day Lupus nephritis/SLE/Wegener’s granulomatosis/idiopathic pulmonary fibrosis/multiple sclerosis (unlabeled) • Adult: PO 2-3 mg/kg/day Atopic dermatitis (unlabeled) • Adult/adolescent ≥16 yr: PO 2.5 mg/ kg/day Crohn’s disease, ulcerative colitis (unlabeled) • Adult/child: PO 50 mg/day; may in- crease by 25 mg/day q1-2wk up to 2-3 mg/kg/day, if tolerated
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Available forms: Tablets 50, 75, 100 mg; powder for injection 50 mg , 100 mg/vial
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Administer: • For several days before transplant surgery • All medications PO if possible; avoid IM injection because bleeding may occur PO route • With meals to reduce GI upset IV route • Prepare in biologic cabinet with gown, gloves, mask Direct IV • Dilute to 10 mg/mL with 0.9% NaCl, 0.45% NaCl, D5W, give over 5 min Intermittent IV INFUSION route • Reconstitute 100 mg/10 mL of sterile water for injection; rotate to dissolve; further dilute with 50 mL or more saline or glucose in saline, give over ½-1 hr Y-site compatibilities: Alfentanil, atracu- rium, atropine, benztropine, calcium glu- conate, cycloSPORINE, enalaprilat, epoe- tin alfa, erythromycin, fentaNYL, fluconazole, folic acid, furosemide, glyco- pyrrolate, heparin, insulin, mannitol, mechlorethamine, metoprolol, naloxone, nitroglycerin, oxytocin, penicillin G, potas- sium chloride, propranolol, protamine, SUFentanil, trimethaphan, vasopressin
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Assess: • For infection: increased temperature, WBC; sputum, urine, vital signs baseline and during treatment • I&O, weight daily, report decreasing urine output; toxicity may occur • Bone marrow suppression: severe leukopenia, pancytopenia, thrombocytope- nia; HB, WBC, platelets during treatment monthly; if leukocytes are <3000/mm3 or platelets <100,000/mm3, product should be discontinued, CBC • Hepatotoxicity: if dark urine, jaun- dice, itching, light-colored stools, in- creased LFTs, product should be dis- continued; hepatic studies: alkaline phosphatase, AST, ALT, bilirubin • Arthritis: pain; ROM; swelling; mobil- ity before, during treatment
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Evaluate: • Therapeutic response: absence of graft rejection, immunosuppression in autoimmune disorders
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take as prescribed; not to miss doses; if dose is missed on daily regimen, to skip dose; if taking multiple doses/day, to take as soon as remembered • That therapeutic response may take 3-4 mo with RA; to continue with pre- scribed exercise, rest, other medica- tions • To report fever, rash, severe diarrhea, chills, sore throat, fatigue because seri- ous infections may occur; report unusual bleeding, bruising; signs/symptoms of renal/hepatic toxicity • To avoid vaccinations, bring up to date before use • To avoid crowds to reduce risk for infection • That treatment is ongoing to prevent transplant rejection • To avoid use with OTC, herbals, supplements unless approved by pre- scriber • RA: Advise patient to continue with other prescribed treatment, other medi- cations, physical therapy
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PHARMACOKINETICS Metabolized in liver, excreted in urine (active metabolite), crosses placenta, half-life 3 hr
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• Adult/adolescent ≥16 yr: PO 2.5 mg/ kg/day Crohn’s disease, ulcerative colitis (unlabeled)
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