AZR

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.

Azathioprine

AZR

50mg

Ipca




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.

Pharmacological action

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.



Pharmacokinetic

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.




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AZR 50mg
Brand AZR
Ingredients Azathioprine
Strength 50mg
Manufactured Ipca laboratories
Rating

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

Precautions

  • 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

Drug interaction with AZR tablet

  • AZR interaction with adalimumab will increase immunosuppressive effects and risk of infections occurs. Avoid usage both combination.
  • AZR interaction with allopurinol will increases levels of azathioprine by decreasing metabolism and increased risk of bone marrow toxicity.
  • AZR combination with cyclosporine both increase immunosuppressive effects. Avoid the using.
  • AZR combination with everolimus and tacrolimus both increase immunosuppressive effects. Avoid the using.
  • Interaction with captopril will show pharmacodynamic synergism and use with caution and will have risk of neutropenia.
  • AZR interaction with zidovudine will either increases toxicity of the other by pharmacodynamic synergism and will increased risk of myelosuppression. Use with caution.

Contraindications

AZR is contraindicated to patients having hypersensitivity to the drug. While AZR using for treatment for rheumatoid arthritis, avoid it if patient is pregnant



Pregnancy category is D AZR should not have administrated to pregnant without careful weighing of risk versus benefit because it will cause harm to fetal

Most of evidence show the breastfeeding is safe but proper discussion with doctor before using AZR tablet

If overdose occurs, then please seek emergency department. Avoid the overdose, have the drug properly Storage conditions of AZR tablet Store the drug at 20°-25°C Protect the drug in dry place and from light

If dose is missed, have it soon before next dose reaches or skip the dose and follow normal timing Please Consult with the doctor

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