Cyclosporine A , drug

Pichard L, Eabre I, Fabre G, et al. Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes. Drug Metab Dispos 1990 18(5) 595-606. 

Malaekeh-Nikouei M, Tabassi SAS, Jaafari MR (2008) Preparation, characterization, and mucoadhesive properties of chitosan-coated microspheres encapsulated with cyclosporine A. Drug Dev Ind Pharm 34 492 98... 

CastelaoAM. Cyclosporine A - drug interactions. 2nd IntConf Therapeutic Drug Monitoring Toxicology, Barcelona, Spain 1992. 203-9. 

Certain CYP enzymes may be induced or inhibited by conventional drugs or by compounds in plants, leading to an increase or decrease in the activity of the enzyme. If a CYP enzyme is induced, plasma levels of drugs metabolized by that enzyme may be decreased, which, in turn, may result in plasma levels too low to be effective. For example, the compound hyperforin in St. John s wort induces CYP3A4 and reduces plasma levels of cyclosporine, a drug used... 

X. Dong, W. Shi, G. Yuan, L. Xie, S. Wang, and P. Lin, Intravitreal implantation of the biodegradable cyclosporin A drug delivery system for experimental chronic uveitis, Graefes Arch. Clin. Exp. Ophthalmol, 244 (4), 492-497, 2006. 

Ecample Miller and Rich investigated the conformational consequences of substitutions on an amino acid in cyclosporin A, an important immunosuppressive drug. One of the amino acids in this cyclic undecapeptide is (2, 3r, 4r, 6e)-3-Hydroxy-4-methyl-2-(methylamino)-6-octenoic acid (MeBmt). It is essential for biological activity. 

Immunophillins are abundant proteins that catalyze the cis-trans isomerization of proline residues within proteins, generally to aid in protein folding. Immunophillins are not essential proteins, are the intracellular binding proteins of several immunosuppressive drugs. Cyclosporin A exerts its action after binding to cyclophilin. Tacrolimus and sirolimus predominantly bind to the protein FKBP-12 (FK binding protein-12). 

The HMG-CoA reductase inhibitors have an additive effect when used with the bile acid sequestrants, which may provide an added benefit in treating hypercholesterolemia that does not respond to a single-drug regimen. There is an increased risk of myopathy (disorders of the striated muscle) when the HMG-CoA reductase inhibitors are administered with erythromycin, niacin, or cyclosporin a When the HMG-CoA reductase inhibitors are administered with oral anticoagulants, there is an increased anticoagulant effect. 

Sirolimus is currently the only FDA-approved ToR inhibitor. One of its derivatives, everolimus, is in phase III clinical trials and has been approved for use in some European countries.30 Sirolimus is a macrolide antibiotic that has no effect on cal-cineurin phosphatase.11,31,32 Sirolimus inhibits T cell activation and proliferation by binding to and inhibiting the activation of the mammalian ToR, which suppresses cellular response to IL-2 and other cytokines (i.e., IL-4 and IL-15J.11,31 Studies have shown that sirolimus may be used safely and effectively with either cyclosporine or tacrolimus as a replacement for either azathioprine or mycophenolate mofetil.33 However, when using both sirolimus and cyclosporine as part of a patient s immunosuppressant therapy, because of a drug interaction between the two resulting in a marked increase in sirolimus concentrations, it is recommended to separate the sirolimus and cyclosporine doses by at least 4 hours. Sirolimus also can be used as an alternative agent for patients who do not tolerate calcineurin inhibitors due to nephrotoxicity or other adverse events.34... 

Many drugs have been conjugated to antibodies or their fragments, including daunomycin [113], cyclosporine [114], platinum [115], chlorambucil [116], and vindesine [117], When choosing a drug for this type of... 

Chappell, L.H. and Washing, J.L. (1992) Cyclosporin A antiparasitic drug, modulator of the host-parasite relationship and immunosuppressant. Parasitology 105, S25-S40. 

The immunosuppressant compound170 FK-506, similar in effect to cyclosporin A, the leading drug for use in immune system suppression to prevent rejection of transplanted organs171, has been labelled at carbon atoms 10, 16, 18, 21a, 24 and 26 by fermentative biosynthesis using sodium [l-14C]propionate as a precursor172. The same 13C-labelled positions were derived from [l-13C]propionate. FK-506 producing culture Streptomyces tsukubaenis no 9993 has been utilized in this biosynthesis (120 h incubation at 29 °C). 

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