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Brand Name :
No Data Available.
Synonyms :
Azatioprina, azathioprinum
Class :
Anticancer & antimetabolites
Dosage forms & Strengths
Solution reconstituted, Injection
100 mg
Tablet, Oral
75 mg
100 mg
50 mg
Refer to adult dosing
Azathioprine converted into the active metabolites like thioguanine (6-TGN) and mercaptopurine (6-MP) by the activity of TPMT.
It inhibits the synthesis of purines. Metabolites of azathioprine can cause immunosuppressive and toxic effects.
Frequency defined:
>10%:
Nausea (30%)
Vomiting (30%)
Weight loss
Increased liver enzymes (14%)
Myelosuppression (11%)
Leukopenia
infection
decreased CrCl (16%)
<1%
Lymphoma
Frequency not defined:
Alopecia
Arthralgia
Diarrhea
Hepatotoxicity
Sweat syndrome
Thrombocytopenia
Rash
Myelosuppression
Elevate the risk of mutagenesis, hematologic toxicity, neoplasia may occur because of the chronic immunosuppression with azathioprine.
Contraindication:
Hypersensitivity
Rheumatoid arthritis
Pregnancy
Lactation
Caution:
The risk of neoplasia elevates with chronic usage
Hepatotoxicity
Thrombocytopenia
Severe leukopenia
Severe myelosuppression
Pregnancy consideration: azathioprine is fall under pregnancy category D. Avoid during pregnancy.
Lactation: excreted in breast milk at very low levels, avoid use during lactation
Pregnancy category:
Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or the later trimester.
Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh risks over benefits. These category drugs should be prohibited for pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology:
Azathioprine is a purine analog. It is an immunosuppressive drug and used to treat rheumatoid arthritis and prevent rejection of kidney transplant.
Pharmacodynamics:
Azathioprine regulates rac1 to cause apoptosis of T cells and immunosuppressive effects.
Pharmacokinetics:
Absorption
Azathioprine is absorbed properly in oral administration. The duration of maximum concentration is about 1 to 2 hours. The peak plasma concentration is below 1 mcg/ml.
Distribution
About 30% of the azathioprine is protein bounded.
Metabolism
Azathioprine goes for hepatic metabolism.
6-thiouric acid and 6-mercaptopurine are the 2Â Â metabolites.
Elimination and excretion
Azathioprine is eliminated through urine.
Half-life:
5 hours
A pharmacist must combine the suspension before the oral administration.
Tablets must be taken orally after the meal to decrease the effect of GI tract. IV administration with an Iv push may be administrated for 5 minutes at concentration of not greater than 5 mg/ml.
Why do we use Azathioprine?
It is an immunosuppressant medication. It is used for different diseases where immune suppression system is important.
Autoimmune diseases: Azathioprine is used to treat chronic autoimmune diseases like:
Rheumatoid arthritis
Systemic lupus erythematosus (SLE)
Inflammatory bowel diseases like Crohn’s disease and ulcerative colitis
Myasthenia gravis
Organ transplantation: It is used to stop the rejection in patients who have received organ transplantation specifically kidney transplantation. Azathioprine prevents he body to attack the transplanted organ by suppressing the immune response.
Dermatological conditions: Azathioprine is used to treat skin diseases like pemphigus vulgaris, atopic dermatitis, and psoriasis.