Pharmacology tacrolimus

Pharmacology Tacrolimus is a macrolide immunosuppressant that prolongs the survival of the host and transplanted graft and inhibits T-lymphocyte activation, although the exact mechanism of action is not known. 

Pharmacology Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. The mechanism of action of tacrolimus in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. Pharmacokinetics ... 

Tacrolimus, a macrolide, derives from a streptomyces species pharmacologically it resembles cyclosporin A, but is more potent and efficacious. 

Spencer CM, Goa KL, Gilhs JC. Tacrolimus. An update of its pharmacology and clinical efficacy in the management of organ transplantation. Drugs 1997 54 925-975. 

CYP3A4 activity, significantly decreasing plasma concentrations and the pharmacologic effect of a number of agents, including alprazolam, amitriptyline, cyclosporine, indinavir, methadone, nevirapine, simvastatin, tacrolimus, and oral contraceptives (69-77). 

Peters DH, Fitton A, Plosker GL, Faulds D. Tacrolimus. A review of its pharmacology, and therapeutic potential in hepatic and renal transplantation. Drugs 1993 46(4) 746-94. 

Tacrolimus, a macrolide derivative, has similar immunosuppressive properties to ciclosporin and has effects on T lymphocytes by inhibiting interleukin-2 production. On a weight basis, tacrolimus is about 100 times more potent than ciclosporin. In view of the outcome of several multicenter trials, it has been used as an alternative to ciclosporin as a baseline regimen for the prophylaxis of renal and liver transplant rejection and in the treatment of acute rejection (SED-13,1130) (SEDA-21, 390) (1). The clinical pharmacology, clinical use, and adverse effects profile of tacrolimus in organ transplantation have been extensively reviewed (2). 

Floren, L.C., Bekersky, I., Benet, L.Z., Mekki, Q., Dressier, D. et al. (1997) Tacrolimus oral bioavailability doubles with coadministration of ketoconazole. Clinical Pharmacology and Therapeutics, 62, 41 19. 

In rheumatoid arthritis (RA), T cells play a critical role in both the cause and long-term maintenance of the disease. Tacrolimus, as a T-cell-specific immunosuppressant, should be effective against RA based on the pharmacological evidences that tacrolimus both inhibits the activation of T cells and blocks cross-talk between T cells and antigen-presenting cells [72]. 

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