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Azathioprine Tablets

Function and Efficacy

This drug is an imidazole derivative of 6-thiopurine and is an anti-metabolite with immunosuppressive effects. It can produce alkylation to block SH groups, inhibit nucleic acid biosynthesis, prevent cell proliferation, and cause DNA damage. Animal experiments have confirmed that this drug can reduce DNA and RNA in the thymus and spleen, affect the synthesis of DNA, RNA, and protein, and mainly inhibit T-lymphocytes to affect immunity, so it can inhibit delayed allergic reactions and organ transplant rejection reactions. The efficacy of this drug will only appear after several weeks or months of treatment. It is better absorbed in the upper digestive tract. The levels of thiopurine and 6-thiopurine in plasma have no correlation with the efficacy and toxicity of this drug.

Ingredients

Each tablet contains 50 mg of azathioprine.

Name Description Content CAS NO. Manufacturer
AzathioprineIngredients

This drug is an imidazole derivative of 6-thiopurine and an antimetabolite with immunosuppressive effects. It can produce alkylation to block SH groups, inhibit nucleic acid biosynthesis, prevent cell proliferation, and cause DNA damage. Animal experiments have confirmed that this drug can reduce DNA and RNA in the thymus and spleen, affect the synthesis of DNA, RNA, and protein, and mainly inhibit T-lymphocytes to affect immunity, so it can inhibit delayed allergic reactions and organ transplant rejection reactions. The efficacy of this drug will only appear after several weeks or months of treatment.

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446-86-6 23

Appearance

It is a round, biconvex, yellow film-coated tablet.

Indication

1. Acute and chronic leukemia, with good short-term efficacy for chronic myeloid leukemia, rapid effect, but short remission period; 2. Acquired hemolytic anemia, idiopathic thrombocytopenic purpura, systemic lupus erythematosus; 3. Chronic rheumatoid arthritis, chronic active hepatitis (hepatitis related to autoimmunity), primary biliary cirrhosis; 4. Hyperthyroidism, myasthenia gravis; 5. Others: chronic nonspecific ulcerative colitis, segmental enteritis, polyradiculitis, lupus nephritis, proliferative nephritis, Wegener's granulomatosis, etc.

Usage and Dosage

The injection is administered intravenously only when oral administration is not possible, and should be discontinued when oral therapy can be tolerated. 5 mg/kg body weight is given on the first day of organ transplantation, either orally or intravenously. The maintenance dose should be adjusted according to clinical needs and tolerance of the blood system, usually 1-4 mg/kg body weight/day. Maintenance therapy should be continued indefinitely. Because if the treatment is interrupted, there is a risk of rejection. The initial dose for other diseases is 1-3 mg/kg body weight/day. It should be based on clinical response and tolerance as shown by hematological indicators. When the therapeutic effect is obvious, the maintenance dose should be reduced to the lowest level that can maintain this therapeutic effect. If the patient's condition does not improve within 3 months, discontinuation should be considered. The required maintenance dose ranges from 1 mg/kg body weight/day to 3 mg/kg body weight/day.

Adverse Reactions

Allergic reactions: such as general malaise, dizziness, nausea, vomiting, diarrhea, fever, chills, myalgia, arthralgia, abnormal liver function and hypotension. The drug should be discontinued immediately and supportive therapy should be given, which can recover in most cases. Hematopoietic function: Dose-related, reversible bone marrow suppression may occur, with common leukopenia, occasional anemia and thrombocytopenic purpura. Infection: Organ transplant recipients who use this drug and adrenal cortical hormones have increased susceptibility to viral, fungal and bacterial infections. Gastrointestinal reactions: Occasionally nausea, which can be relieved by taking the drug after meals. Pancreatitis is rare. Pulmonary reactions: Reversible pneumonia is rare.

Precautions

Patients who are allergic to this drug and 6-mercaptopurine are contraindicated.

Special Population Medication

Precautions for children: See the [Usage and Dosage] section. Precautions for pregnancy and lactation: It can cause teratogenesis, so pregnant women should not use it. Precautions for the elderly: The elderly have limited experience in using this product. Although the existing data do not prove that the incidence of side effects after using this product in the elderly is higher, it is still recommended to use the lower limit of the recommended dose range. Pay extra attention to the hematological indicators of the elderly after taking the drug, and use the lowest clinically effective dose as the maintenance dose.

Drug Interactions

When allopurinol, oxypurinol and/or thiopurinol are used in combination with 6-thiopurine or azathiopurine, the dose of 6-thiopurine and azathiopurine should be reduced to 1/2 of the original dose. This drug can enhance the neuromuscular blocking effect of depolarizing drugs such as succinylcholine and weaken the neuromuscular blocking effect of non-depolarizing drugs such as tubocurarine. It hinders the anticoagulant effect of warfarin. This drug can enhance the bone marrow suppressive effect, leading to serious hematological abnormalities, and can also enhance the bone marrow suppressive effect of cimetidine and indomethacin.

Storage

Keep in a sealed container

Packaging Specification

50 mg

Validity Period

24 months.

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