DefinitionThis section has been translated automatically.
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IndicationThis section has been translated automatically.
- Absolute indications: Systemic lupus erythematosus, mixed collagenosis (overlap syndrome), polymyositis/dermatomyositis, panarteritis nodosa, pemphigus vulgaris, bullous pemphigoid.
- Azathioprine 2nd choice: Wegener's granulomatosis, Behçet's disease, Pyoderma gangraenosum, polymyalgia rheumatica, systemic scleroderma, primary Sjögren's syndrome, rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, essential cryoglobinemia.
- Exceptional indications of azathioprine therapy: persistent erythema exsudativum multiforme, ankylosing spondylitis, infectious arthritis (e.g. Lyme arthritis, reactive arthritis), degenerative diseases, fibromyalgia syndrome.
Limited indicationThis section has been translated automatically.
Dosage and method of useThis section has been translated automatically.
- adults: 1-2,5 mg/kg bw/day p.o.
- children from 1 year: 50-150 mg/day p.o.
- children from 12 years: 100-200 mg/day p.o.
Remember! The daily dose can be divided into three doses (e.g. 3 times/day 50 mg). The onset of effect can be expected after 3-4 weeks, this is recognizable by a "steroid-saving effect"!
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Remember! During the treatment and up to 6 months afterwards, effective contraception must be carried out on both men and women! Blood tests (BB and liver values) in the 1st month weekly, in the 2nd and 3rd month every 14 days, then monthly!
- The therapy can be continued without problems for 4-6 years (after that the risk of hepatocellular carcinoma increases dramatically!)
- The degradation product of azathioprine, 6-thioguanine, is incorporated into the DNA and acts as a UVA-sensitive chromophore, which induces chromosome strand breaks upon UVA irradiation (see also DNA repair).
- It is recommended to have the TPMT status determined before starting!
LiteratureThis section has been translated automatically.
- Brem R et al (2010) DNA breakage and cell cycle checkpoint abrogation induced by a therapeutic thiopurine and UVA radiation. Oncogene 29:3953-3963
- Meggitt SJ et al (2011) Association of Dermatologists' guidelines for the safe and effective prescribing of azathioprine. Br J Dermatol 165:711-734.
TablesThis section has been translated automatically.
Side effects of Azathioprine
Airway organs |
Alveolitis, dyspnoea, flu-like symptoms, cough, rarely interstitial pneumonia |
Blood/lymph |
dose-dependent blood formation disorder, leukopenia (up to 50%), thrombopenia, anemia, pancytopenia, eosinophilia, leukocytosis, bleeding tendency, megaloblast anemia (administration of leukoverin!), acute myeloid leukemia, non-Hodgkin's lymphomas (0.5%) |
Electrolytes, metabolism, endocrinium |
Hyperbilirubinaemia, reticulum cell Ca, breast Ca |
GIT |
Nausea, vomiting, gastro-intestinal disorders, loss of appetite (12%), diarrhoea (depending on the source: 5-20% of patients).), steatorrhoea, intrahepatic cholestasis with increase of AP, GPT, GOT (reversible), intestinal perforation, diverticulitis, dysphagia, toxic hepatitis (1-5%, reversible after discontinuation), Budd-Chiari syndrome (in kidney transplant patients), pancreatitis (reversible), parotitis, primary hepatocellular carcinoma (after many years of therapy) |
Skin |
Urticaria (depending on the source: 2-8% of patients), exanthema (2%), alopecia (reversible), mucous membrane ulcers, bacterial skin infections, verrucae vulgaris, herpes zoster and herpes simplex as well as spinocellular carcinomas (especially at higher dosages) |
Cardiovascular |
cardiac arrhythmia, RR drop, hypotension up to circulatory collapse |
Nervous System |
Neuritis, paresthesias, rigor, dizziness, worsening of a myasthenia gravis up to myasthenic crisis |
Kidney |
Renal dysfunction |
Other |
fever, increased tendency to infections, chromosomal changes (reversible after weaning), teratogenicity |
Support apparatus |
Arthralgia, arthritis, myalgia, myositis |
Interactions of Azathioprine
ACE inhibitors |
severe leukopenia |
Allopurinol |
Azathioprine level ↑, allopurinol effect ↓ (common metabolic pathway via xanthine oxidase) |
Live virus vaccines |
Risk of atypical reactions, avoid combination |
Pancuronium |
Pancuronium effect ↓ |
Penicillamine |
Penicillamine toxicity ↑ |
Suxamethonium |
neuromuscular blockage ↑ |
Inactivated vaccines |
Inactivated vaccine effect ↓, immune response ↓ |
Trimethoprim sulfonamides |
Antifolate activity ↑, trimethoprim sulfonamide toxicity ↑, kidney damage |
Tubocurarin |
Tubocurarin effect ↓ |