শুধুমাত্র তথ্যমূলক — চিকিৎসা পরামর্শ নয়। সর্বদা লাইসেন্সপ্রাপ্ত স্বাস্থ্যসেবা প্রদানকারীর পরামর্শ নিন।

MedBD
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Community data Updated 2 মাস আগে

ইঙ্গিত

Imruza is used as an immunosuppressant antimetabolite, either on its own or, more commonly, together with other agents (usually corticosteroids) and procedures that influence the immune response. Its therapeutic effect may become evident only after weeks or months of treatment and can include a steroid-sparing effect, which in turn reduces the toxicity associated with high doses and prolonged use of corticosteroids. In combination with corticosteroids and/or other immunosuppressive agents and procedures, Imruza is indicated to improve the survival of organ transplants, including renal, cardiac and hepatic transplants. It also reduces the corticosteroid requirements of renal transplant recipients. Imruza is indicated for the treatment of moderate to severe inflammatory bowel disease (IBD), namely Crohn's disease or ulcerative colitis, in patients who require corticosteroid therapy, in patients who cannot tolerate corticosteroid therapy, or in patients whose disease does not respond to other standard first-line therapy. Used either alone or, more usually, in combination with corticosteroids and/or other medicinal products and procedures, Imruza has been shown to provide clinical benefit (which may include a reduction in the dose, or discontinuation, of corticosteroids) in a proportion of patients with the following conditions: severe active rheumatoid arthritis, systemic lupus erythematosus, dermatomyositis and polymyositis, autoimmune chronic active hepatitis, pemphigus vulgaris, polyarteritis nodosa, autoimmune haemolytic anaemia, and chronic refractory idiopathic thrombocytopenic purpura.

⚠️ কোনো ওষুধ গ্রহণের আগে সর্বদা নিবন্ধিত চিকিৎসকের পরামর্শ নিন।

ফার্মাকোলজি

Azathioprine is an immunosuppressive antimetabolite, chemically 6-[(1-methyl-4-nitro-1H-imidazol-5-yl)thio]-1H-purine. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound.Azathioprine is an imidazole derivative of 6-mercaptopurine (6-MP). It is rapidly broken down in vivo into 6-MP and amethylnitroimidazole moiety. The 6-MP readily crosses cell membranes and is converted intracellularly into a number of purine thioanalogues, which include the main active nucleotide, thioinosinic acid. The rate of conversion varies from one person to another. Nucleotides do not traverse cell membranes and therefore do not circulate in body fluids. Irrespective of whether it is given directly or is derived in vivo from azathioprine, 6-MP is eliminated mainly as the inactive oxidised metabolite thiouric acid. This oxidation is brought about by xanthine oxidase, an enzyme that is inhibited by allopurinol. The activity of the methylnitroimidazole moiety has not been defined clearly. However, in several systems it appears to modify the activity of azathioprine as compared with that of 6-MP. Determination of plasma concentrations of azathioprine or 6-MP have no prognostic value as regards effectiveness or toxicity of these compounds.Because of these mechanisms, the therapeutic effect of azathioprine may be evident only after several weeks or months of treatment. Azathioprine appears to be well absorbed from the upper gastro-intestinal tract. Plasma levels of azathioprine and 6-mercaptopurine do not correlate well with the therapeutic efficacy or toxicity of azathioprine.Absorption: Azathioprine is well absorbed following oral administration. Although there are no food effect studies with azathioprine, pharmacokinetic studies with 6-mercaptopurine have been conducted that are relevant to azathioprine. The mean relative bioavailability of 6-mercaptopurine was approximately 27% lower following administration with food and milk compared to an overnight fast. 6-mercaptopurine is not stable in milk due to the presence of xanthine oxidase (30% degradation within 30 minutes). Azathioprine may be taken with food or on an empty stomach, but patients should standardise the method of administration. The dose should not be taken with milk or dairy products.After oral administration of [35S]-azathioprine, the maximum plasma radioactivity occurs at 1-2 hours and decays with a half-life of 4-6 hours. This is not an estimate of the half-life of azathioprine itself, but reflects the elimination from plasma of azathioprine and the [35S]-containing metabolites of the drug. Azathioprine is principally excreted as 6-thiouric uric acid in the urine. 1-methyl-4-nitro-5-thioimidazole has also been detected in urine as a minor excretory product. A small proportion of the drug may be cleaved between the S atom and the purine ring. Only a small amount of the dose of azathioprine administered is excreted unmetabolised in the urine.Biotransformation: Thiopurine S-Methyl Transferase (TPMT): TPMT activity is inversely related to red blood cell 6-mercaptopurine derived thioguanine nucleotide concentration, with higher thioguanine nucleotide concentrations resulting in greater reductions in white blood cell and neutrophil counts. Individuals with TPMT deficiency develop very high cytotoxic thioguanine nucleotide concentrations.

Pregnancy & Breastfeeding

Teratogenicity: Evidence for the teratogenicity of azathioprine in humans is inconclusive. As with any cytotoxic chemotherapy, both partners should be advised to use adequate contraceptive precautions while either one is receiving azathioprine.

Mutagenicity: Chromosomal abnormalities that disappear over time have been found in the lymphocytes of children born to patients treated with azathioprine. Except in extremely rare cases, no visible physical abnormalities have been observed in these offspring. Azathioprine combined with long wave ultraviolet light has shown a synergistic clastogenic effect in patients treated with azathioprine for various disorders.

Fertility: The specific effect of azathioprine therapy on human fertility is not known.

Pregnancy: Azathioprine and its metabolites are known to cross the placenta and amniotic membrane in substantial amounts, passing from mother to fetus. Azathioprine falls under Pregnancy Category D. It should not be given to patients who are pregnant or likely to become pregnant soon without a careful assessment of the risks against the benefits. As noted above, evidence for its teratogenicity in humans is inconclusive, and adequate contraceptive precautions should be used by either partner during treatment.

Women of childbearing potential and contraception for men and women: Because of azathioprine's genotoxic potential, women of childbearing potential should use effective contraception during treatment and for one month after finishing it. Men are advised to use effective contraception and avoid fathering a child while receiving azathioprine and for three months after completing treatment.

Lactation: Mothers receiving azathioprine are advised not to breastfeed, since 6 mercaptopurine has been detected in the colostrum and breast milk of women treated with the drug.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

ডোজ নির্দেশিকা

⚠️ শুধুমাত্র সরকারি উৎস থেকে নির্দেশিকা পরিসীমা। ব্যক্তিগতকৃত ডোজের জন্য আপনার ডাক্তারের পরামর্শ নিন।

Adults: Transplants: Depending on the immunosuppressive regimen used, a dose of up to 5 mg/kg body weight per day may be given by mouth or intravenously on the first day of treatment. The maintenance dose should range from 1 to 4 mg/kg body weight per day and must be adjusted according to clinical need and how well the blood counts tolerate the drug. Evidence indicates that azathioprine treatment should be continued indefinitely, even if only low doses are needed, because of the risk of graft rejection. Other indications: In general, the starting dose is 1 to 3 mg/kg body weight per day, adjusted within these limits according to the clinical response (which may not be evident for weeks or months) and blood count tolerance. Once a therapeutic response is evident, reducing the maintenance dose to the lowest level that keeps that response should be considered. If the patient's condition has not improved within three months, withdrawing azathioprine should be considered. However, for patients with inflammatory bowel disease (IBD), a treatment duration of at least twelve months should be considered, and a response to treatment may not become clinically apparent until after three to four months. The maintenance dose needed may range from less than 1 mg/kg body weight per day to 3 mg/kg body weight per day, depending on the condition being treated and the individual patient's response, including blood count tolerance. Overweight children: Children considered overweight may need doses at the higher end of the range, so close monitoring of the response to treatment is recommended. Elderly: There is limited experience with giving azathioprine to elderly patients. Although the available data do not show that side effects are more common in elderly patients than in other patients treated with azathioprine, doses at the lower end of the range are recommended. Renal impairment: In patients with reduced kidney function, a dose reduction should be considered. Hepatic impairment: In patients with reduced liver function, a dose reduction should be considered.

পার্শ্বপ্রতিক্রিয়া ও পারস্পরিক ক্রিয়া

পার্শ্বপ্রতিক্রিয়া

No side-effect data recorded yet.