Published online by Cambridge University Press: 06 October 2020
THERAPEUTICS
Brands
• Imuran, Azasan, Azamun, Imurel
Generic?
• Yes
Class
• Immunosuppressant
Commonly Prescribed for
(FDA approved in bold)
• Prophylaxis of organ rejection in patients with allogenic renal transplants
• Reducing signs and symptoms of rheumatoid arthritis
• Myasthenia gravis (MG) (monotherapy or adjunctive)
• Lambert-Eaton myasthenia syndrome
• Inflammatory myopathies: polymyositis (PM) and dermatomyositis (DM)
• Multiple sclerosis (MS)
• Neuromyelitis optica
• Crohn's disease, ulcerative colitis
• Lupus nephritis
How the Drug Works
• Azathioprine, a derivative of 6-mercaptopurine, inhibits the synthesis of purine. This interferes with DNA and RNA synthesis as well as repair and replication of T and B leukocytes
• The mechanism of action in autoimmune diseases is unclear, but it appears to suppress cellular cytotoxicity and blunt hypersensitivity reactions
How Long Until It Works
• At least 3 months. Full effect may occur after 1–2 years
If It Works
• MG: improves strength and muscle fatigue. Often used as an adjunctive to corticosteroids or acute treatment such as immune globulin or plasma exchange. Taper corticosteroids if clinical symptoms Improve
• PM/DM: may allow improvement in strength and discontinuation or reduced dose of corticosteroids. (Corticosteroids are usually tapered first.) Taper slowly over 6 months if clinical remission occurs
• MS: may reduce relapses and new lesions on MRI
If It Doesn't Work
• MG: effectiveness may not occur until 1 year. For patients with severe disability, consider more rapid-acting treatments, such as IV immune globulin
• DM/PM: question the diagnosis (inclusionbody myositis, hypothyroidism, muscular dystrophy), rule out corticosteroid-induced myopathy, and evaluate for undiagnosed malignancy (especially in DM). Change to methotrexate
• MS: if clearly not helpful, change to another agent
Best Augmenting Combos for Partial Response or Treatment-Resistance
• MG: usually combined with corticosteroids or other treatments in MG. Most patients also use symptomatic medication, such as pyridostigmine
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