CYCLOSPORINE Uses, Side Effects, and More

 CYCLOSPORINE

BRAND NAME:-  IMUSPORIN 25,50,100mg soft gelatin capsules. , Sandimmun neoral, Panimun Bioral 25,50,100mg caps ., Sandimmun, Panimun 100mg/ml inj in 1ml ,5ml, 50 ml vial.

PHARMACOKINETICS:-

Ciclosporin is a cyclic peptide of 11 amino acids; it contains a single D-amino acid, which is rarely encountered in nature. Unlike most peptides, ciclosporin is not synthesized by ribosomes.

Ciclosporin is highly metabolized in humans and animals after ingestion. The metabolites, which include cyclosporin B, C, D, E, H, and L,have less than 10% of ciclosporin's immunosuppressant activity and are associated with higher kidney toxicity.Individual ciclosporin metabolites have been isolated and characterized but do not appear to be extensively studied.

PHARMACODYNAMIC:-

Cyclosporine exerts potent immunosuppressive actions on T cells, thereby prolonging survival following organ and bone marrow transplants. This drug prevents and controls serious immune-mediated reactions including allograft rejection, graft versus host disease, and inflammatory autoimmune disease.

Some notable effects of cyclosporine are hypertrichosis, gingival hyperplasia, and hyperlipidemia. There is also some debate about this drug causing nephrotoxicity.

 MECHANISM OF ACTION:- 

Cyclosporine is a calcineurin inhibitor that inhibits T cell activation. Its binding to the receptor cyclophilin-1 inside cells produces a complex known as cyclosporine-cyclophilin. This complex subsequently inhibits calcineurin, which in turn stops the dephosphorylation as well as the activation of the nuclear factor of activated T cells (NF-AT) that normally cause inflammatory reactions. NF-AT is a transcription factor that promotes the production of cytokines such as IL-2, IL-4, interferon-gamma and TNF-alpha, all of which are involved in the inflammatory process. Specifically, the inhibition of IL-2, which is necessary for T cell activation or proliferation, is believed to be responsible for cyclosporine's immunosuppressive actions. In addition to the above, the inhibition of NF-AT leads to lower levels of other factors associated with T helper cell function and thymocyte development.

USED:- 

Cyclosporine is used to prevent organ rejection in people who have received a liver, kidney, or heart transplant. It is usually taken along with other medications to allow your new organ to function normally. 

SIDE EFFECTS:-

Shaking, headache, dizziness, unusual growth of body hair, nausea/vomiting, diarrhea, stomach upset, or flushing may occur.

 DOSE:-

10-15mg /kg/day with milk or fruit juice till 1-2 weeks after transplantation, gradually reduced to maintenance dose of 2-6 mg / kg/day. Therapy may be strated with 3-5mg/kg i.v. infusion.