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Home > Cyclosporine



Chemical structure of cyclosporine
Empirical formula C62H111N11O12
Molecular weight 1202.61
Bioavailability variable
Metabolism hepatic
Elimination half life variable
Excretion biliary
ATC code L04AA01
Pregnancy category C ( USA)
C ( Aus)

Cyclosporine or ciclosporin ( INN) or cyclosporin (former BAN), is an immunosuppressant drug. It is used post-allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejectionTransplant rejection is a process by which the immune system of the recipient of an transplant attacks the transplanted organ or tissue. This is because a normal healthy human immune system can distinguish foreign tissues and attempts to destroy them, jus. It has been studied in transplants of skin, heart, kidney, lung, pancreas, bone marrow and small intestine. Cyclosporine is a cyclic nonribosomal peptideNonribosomal peptide s (NRP) are secondary metabolites, usually produced by microorganisms like bacteria and fungi. They are synthesized by nonribosomal peptide synthetases (NRPS) from amino acids. They often have a cyclic and/or branched structure, conta of 11 amino acidIn chemistry, an amino acid is any molecule that contains both amino and carboxylic acid functional groups. In biochemistry, this shorter and more general term is frequently used to refer to alpha amino acids: those amino acids in which the amino and carbs produced by the ascomyceteArchaeascomycetes Hemiascomycetes Euascomycetes Members of the Division Ascomycota are known as the Sac Fungi and are fungi that produce spores in a distinctive type of microscopic sporangium called an ascus (Greek for a "bag" or "wineskin"). This monophy fungusChytridiomycota Zygomycota Ascomycota Basidiomycota The Fungi (singular: fungus are a large group of organisms ranked as a kingdom within the Domain Eukaryota. Included are the conspicuous mushrooms, but also many microscopic forms such as molds and yeast Beauveria nive .

Since 20022002 is a common year starting on Tuesday (see link for calendar). 2002 was the first palindromic year since 1991 and the last until 2112. 2002 was also designated: International Year of Ecotourism and Mountains National Science Year in the United Kingdom a topical emulsionAn emulsion is a mixture of two immiscible substances. One substance (the dispersed phase) is dispersed in the other (the continuous phase). Examples of emulsions include butter, asphalt, mayonnaise and cutting fluid for metalworking. In butter, a continu of cyclosporine for treating dry eye disease (keratoconjunctivitis sicca) has been aggressively marketed under the trade name Restasis®. Cyclosporine is also an antipsoriatic and an antirheumatic , although it is only used in severe cases. It has been investigated in connection with a great many diseases. It is often taken in conjunction with corticosteroids.

The drug is sold by Novartis under the brand names Sandimmune® and Neoral®. Generic cyclosporine drugs have been produced by companies such as Sangstat , Abbott Laboratories and Gengraf . Annual sales of cyclosporine are around $1 billion.

Cyclosporine is thought to bind to the cytosolic protein Cyclophylin (Immunophylin)of immunocompetent lymphocytes, especially T-lymphocytes. This complex of Cyclosporin and Cyclophylin inhibits Calcineurin, which under normal circumstances is responsible for activating the transcription of IL-2. It also inhibits lymphokine production and interleukin release and therefore leads to a reduced function of effector T-cells. It does not effect cytostatic activity.

Treatment has a number of potentially serious side effects and has adverse interactions with a wide variety of other drugs and other materials including grapefruit, although there have been studies to improve the blood level of cyclosporine with grapefruit juice. Side effects can include gum hyperplasia, convulsions, peptic ulcers, pancreatitis, fever, vomiting, diarrhea, confusion, breathing difficulties, numbness and tingling, pruritus, high blood pressure, kidney and liver disfunction, potassium retention and possibly hyperkalemia, hepatotoxicity, nephrotoxicity, and obviously an increased vulnerability to opportunistic fungal and viral infections.

Cyclosporine was discovered in 1970 in a Norwegian soil fungus by Jean F. Borel at Sandoz laboratories and it was approved for use in 1983. The chemical name of cyclosporine is [R-[R*,R*-(E)]]-cyclic(L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl-3-hydroxy-N,4-dimethyl-L-2-amino-6-octenoyl-L-α-amino-butyryl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl) and the empirical formula is C62H111N11O12.

Compare with tacrolimus.



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