What Is Azathioprine?
Azathioprine is an imidazole derivative of thiopurine, which breaks down into thiopurine in the body and functions. Its immune mechanism is the same as that of thiopurine, that is, it has purine antagonism. Because immunoactive cells require purines in the proliferation period after antigen stimulation, at this time, purine antagonism can inhibit the synthesis of DNA, RNA and protein, thereby inhibiting The proliferation of lymphocytes, that is, preventing the antigen-sensitive lymphocytes from being transformed into immune blasts, which produces an immune effect.
Basic Information
- Chinese name
- Azathioprine
- Foreign name
- Azathioprine
- Sodium content
- Approximately 4.5 mg
- Character
- tablet
- CAS number
- 446-86-6
- Molecular formula
- C9H7N7O2S
- Molecular weight
- 277.27
- EINECS number
- 207-175-4
Azathioprine indications
- It is mainly used for anti-rejection reaction during organ transplantation. It is mostly used in combination with corticosteroids or anti-lymphocyte globulin (ALG). It is also widely used in rheumatoid arthritis, systemic lupus erythematosus, active chronic hepatitis, ulcerative colitis, myasthenia gravis, scleroderma and other autoimmune diseases. For chronic nephritis and nephrotic syndrome, its efficacy seems to be less than cyclophosphamide. Due to its many adverse reactions, it is not the first choice for the treatment of the above diseases, and it is usually used when the corticosteroid alone cannot control it.
Azathioprine clinical application
- This product must be swallowed with plenty of water after a meal. The dose for organ transplantation depends on the immunotherapy regimen used, usually the first day dose is up to 5 mg per kilogram of body weight per day. The maintenance dose should be adjusted according to clinical needs and tolerability of the blood system, and is generally 1 to 4 mg per kilogram of body weight per day.
- Therapeutic dose for other diseases: Generally, the starting dose of this product is 1 ~ 3mg / kg / day, during the continuous treatment, according to the clinical response (may not have a response for months or weeks) and the tolerance of the blood system The sexual situation is adjusted accordingly within this range. When the treatment effect is obvious, the dosage should be reduced to the lowest dose that can maintain the curative effect as a maintenance dose. If the condition does not improve within 3 months, you should consider discontinuing this product.
- The maintenance dose of this product ranges from less than 1 mg per kilogram of body weight to 3 mg per kilogram of body weight per day, depending on the need for clinical treatment and the individual response of the patient, including the tolerance of the blood system.
Azathioprine adverse reactions
- 1. Toxic reaction is similar to thiopurine. Large doses and prolonged administration may cause severe bone marrow suppression, which can lead to granulocytopenia and even aplastic anemia, which usually occurs after 6 to 10 days. There may also be toxic hepatitis, pancreatitis, hair loss, mucosal ulcers, peritoneal bleeding, retinal hemorrhage, pulmonary edema, and anorexia, nausea, stomatitis and so on.
- 2. Increase susceptibility to bacterial, viral and fungal infections.
- 3. May cause teratogenicity. In addition can still induce cancer.
Azathioprine precautions
- This product can cause bone marrow suppression, liver function damage, teratogenicity, etc. This product must not be opened or shattered, and it should not be accepted after the outer packaging is broken. It is harmless to hold the film coat intact, and no other protection measures are required. Or as directed by your doctor.
- Patients with renal insufficiency should be appropriately reduced. When the drug is overdose, symptomatic treatment is generally used. In severe cases, dialysis can be considered.
Contraindications to azathioprine
- Liver impairment is disabled. Use with caution in pregnant women.
Azathioprine Drug Interactions
- 1. Allopurinol, oxypurinol or thiopurine can inhibit the metabolism of this product, increase the efficacy and toxicity of this product, so the dose of this product should be reduced by 3/4.
- 2. This product can enhance the neuromuscular block effect of succinylcholine.
- 3. This product attenuates the neuromuscular block effect of tuber poison.
- Note: The above content is only for introduction, the drug use must be carried out by a regular hospital under the guidance of a doctor.