Generic form Azathioprine is sold under the brand name of AZR. AZR is a drug required in certain autoimmune conditions AZR belongs to group of immunosuppressive antimetabolite pro-drug. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are like those of the parent compound. AZR (Azathioprine) is converted into 6-mercaptopurine in the body where it stops purine metabolism and DNA synthesis.
Usage of AZR tablet
AZR tablet are indicated as an addition for the prevention of rejection in renal homotransplantations. AZR tablet also used for the management of active rheumatoid arthritis to decrease signs and symptoms.
Azathioprine antagonizes belongs to purine metabolism and may prohibit development of DNA, RNA, and proteins. It may also block cellular metabolism and stops mitosis. Its mechanism of action is likely due to inclusion of thiopurine analogues into the DNA structure, leads to chain termination and cytotoxicity.
While oral administration the drug is well absorbed, and peak plasma radioactivity is 1-2 hours.
The metabolite and AZR are moderately bound to plasm protein is 30%.
Mainly azathioprine converted to the active metabolites 6-mercaptopurine and 6-thioinosinic acid through a non-enzymatic process and glutathione transferases. Activation of 6-mercaptopurine happen through hypoxanthine-guanine phosphoribosyl transferase (HGPRT) and a set of multi-enzymatic processes containing kinases to form 6-thioguanine nucleotides (6-TGNs) as important metabolites.
Rapidly eliminated from blood and in urine after 8 hours has no azathioprine or mercaptopurine is detectable.
Posology of AZR (dosage)
For oral dosage form – for kidney transplant rejection:
In adults the dose is depends on body weight and should be driven by doctor Generally initial dose is 3 to 5 milligrams (mg) per kilogram (kg) of body weight per day given as a single dose once a day. The first dose is initiate either 1 to 3 days before the transplant or on the day of the transplant. Your doctor may adjust your dose as needed. In children the drug usage and dose should be discussed by doctor.
For rheumatoid arthritis:
In adults the dose is depends on body weight and should be driven by doctor Generally initial dose is 1 milligram (mg) per kilogram (kg) of body weight per day given as a single dose once a day or divided into two doses. Your doctor may adjust your dose as needed. Although the dose is commonly not more than 2.5 mg per kg of body weight per day. In children the drug usage and dose should be discussed by doctor.
Side effects caused by AZR tablet
Serious side effects
Leukopenia (28-50%), Infection (20%), Lymphoma
Incident not known
Fever, Hepatotoxicity, Macrocytic Anemia, Myalgia, Nausea or vomiting, Rash, Skin cancer, Steatorrhea, Abdominal pain, Alopecia, Arthralgia, Bacterial, fungal, protozoal, viral infections, Bone marrow suppression, Diarrhoea, Sweet syndrome (acute febrile neutrophilic dermatosis) Thrombocytopenia
- Chronic immunosuppression with this purine antimetabolite raises neoplasia risk, mutagenic risk, and hematologic toxicities
- Resulted with malignancies include posttransplant lymphoma and hepatosplenic T-cell lymphoma (HSTCL) in patients with inflammatory bowel disease
- Recommending physicians should be familiar with mutagenic probable and with possible hematologic toxicities