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Transcript
TACROLIMUS prepared by Turkeyah Al-Backer Tacrolimus is a potent macrolide immunosuppressant derived from streptomyces tsukubaensis,and has similar actions to those of cyclosporine.It is used to prevent or reserve rejection in patients receiving organ transplants. Mechanism of Action: *Tacrolimus binds to FK-binding protein,inhibiting cacineurin, a cytoplasmic phosphatase. *Calineurin regulates the ability of the nuclear factor of activated T cells to translocate the nucleus and increase the production of cytokines. *By this way,tacrolimus inhibit the synthesis of cytokines that normaly occur in response to T cell activation.. Pharmacokinetics: *administrated orally or intravenously. *oral absorption is in complete *absorption is decrease if drug is taken with high fat or high carbohydrate meals. *highly bound to serum protein. *highly concentrated in the erythrocyte. *metabolized in the liver by CYTP3A4 *most of the drug and its metabolites are found in the feces *renal excretion is very low Clinical Uses: *organ transplantation especially in kidney and liver transplantation *oral psoriasis *atopic dermatitis *glomerular kidney disease *hepatitis *inflammatory bowel disease *mysthenia gravis Adverse Effects: *cacinogenicity *sever anemia due to selective depression of erythropiosis *post transplant diaetes mellitus *hypertrophic cardiomyopathy *nephrotoxicity *peripheral neuropathy *lentigines(small pigmented macules in the skin) Drug-Drug Ineraction: *anti-bacterial drugs.e.g.erythromycin *anti-viral drugs *calcium channels blockers.e.g.nifedipine *danazole *all these drugs increase the level of tacrolimus THANK YOU