Azathioprine is a Generic formof brand name AZAPURE.
AZAPURE isbelonging to immunosuppressant which may be needed with other immunosuppressant drugs to block organ refusal after a liver transplant.
AZAPURE is a prescription drug provided under the supervision of medical practioners.
Prescribed as an addition for the prevention of rejection in renal homotransplantations.
Prescribed for the management of active rheumatoid arthritis to reduces signs and symptoms.
MECHANISM OF ACTION
Azathioprine belongs to imidazole derivative of 6-mercaptopurine (6-MP). Azathioprine is fastly broken down inside into 6-MP and a methyl nitroimidazole molecules. While the correct modes of activity remain to be exemplified, some suggested mechanisms contain:
• The discharge of 6-MP which acts as a purine antimetabolite;
• The potentialstoppage of -SH groups by alkylation;
• The prevention of many pathways in nucleic acid biosynthesis, hence inhibitingmultiplication of cells contains in determination and amplification of immune response;
• Destroy to deoxyribonucleic acid (DNA) via incorporation of purine thioanalogues.
Well absorbed, and high plasma radioactivity is 1-2 hours.
Bounding to plasm protein is 30%.
Primarily azathioprine changed to the active metabolites 6-mercaptopurine and 6-thioinosinic acid via a non-enzymatic process and glutathione transferases. Activation of 6-mercaptopurine happen via hypoxanthine-guanine phosphoribosyl transferase (HGPRT) and a set of multi-enzymatic processes involving kinases to form 6-thioguanine nucleotides (6-TGNs) as active metabolites.
Fastly eliminated from blood and in urine after 8 hours has no azathioprine or mercaptopurine is detectable.
For oral dosage form – for kidney transplant rejection :
In adults the prescribed dose is based on body weight and should be driven by doctor
Commonly starting 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. Inform 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 based on body weight and should be driven by doctor.
Normallystarting dose is 1 milligram (mg) per kilogram (kg) of body weight per day administer as a single dose once a day or split into two doses. Inform the doctor may adjust your dose as necessary. Even though the dose is generally not greater than 2.5 mg per kg of body weight per day.
In children the drug usage and dose should be discussed by doctor. Overdose :
If overdose occurs, then please seek emergency department. Avoid the overdose, have the drug properly
While on treatment with AZAPURE is a Chronic immunosuppression with this purine antimetabolite raises neoplasia risk, mutagenic risk, and hematologic toxicities
Using of medication AZAPURE, Resulted with malignancies contain posttransplant lymphoma and hepatosplenic T-cell lymphoma (HSTCL) in patients with inflammatory bowel disease
Prescribing physicians must be familiar with mutagenic potential and with possible hematologic toxicities
Serious side effects :
Nausea or vomiting
Bacterial, fungal, protozoal, viral infections
Bone marrow suppression
Sweet syndrome (acute febrile neutrophilic dermatosis)
AZAPURE combination with adalimumab will have high immunosuppressive effects and risk of infections occurs. Avoid usage both combination.
AZAPURE combination with allopurinol will have high levels of azathioprine by reducing metabolism and increased risk of bone marrow toxicity.
AZAPURE concomitant use with cyclosporine both increase immunosuppressive effects. Avoid the using
Concomitant use with captopril will show pharmacodynamic synergism and use with caution and will have risk of neutropenia.
AZAPURE Concomitant use with zidovudine will either increases toxicity of the other by pharmacodynamic synergism and will increased risk of myelosuppression. Use with caution
AZAPURE is contraindicated to patients.
Pregnancy while treatment for rheumatoid arthritis
Pregnancy category is D
Administration of AZAPURE to pregnant women without careful weighing of risk versus benefit due to it will cause harm to fetal
Most of evidence show the breastfeeding is safe but proper discussion with doctor before using AZAPURE tablet
- Store the drug at 20°C-25°C
• Protect the drug in dry place and from light
If dose is forgotten, have immediately before next dose reaches or swap the dose and follow normal timing
Please Consult with the doctor