| Attributes | Values |
|---|
| rdf:type
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| http://linked.open...gbank/description
| - A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. Cyclosporine is produced as a metabolite by the fungus species Cordyceps militaris. (From Martindale, The Extra Pharmacopoeia, 30th ed). (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Lichtiger S, Present DH, Kornbluth A, Gelernt I, Bauer J, Galler G, Michelassi F, Hanauer S: Cyclosporine in severe ulcerative colitis refractory to steroid therapy. N Engl J Med. 1994 Jun 30;330(26):1841-5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8196726 # Synthesis Information "Link":http://www.patentgenius.com/patent/6927208.html # "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9323029 (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
| - Biphasic and variable, approximately 7 hours (range 7 to 19 hours) in children and approximately 19 hours (range 10 to 27 hours) in adults. (en)
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| http://linked.open...ugbank/indication
| - For treatment of transplant (kidney, liver, and heart) rejection, rheumatoid arthritis, severe psoriasis. (en)
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| http://linked.open...bank/manufacturer
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Cyclosporine binds to cyclophilin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporine also inhibits lymphokine production and interleukin release. In ophthalmic applications, the precise mechanism of action is not known. Cyclosporine emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
| |
| http://linked.open...outeOfElimination
| - Elimination is primarily biliary with only 6% of the dose (parent drug and metabolites) excreted in the urine. Only 0.1% of the dose is excreted in the urine as unchanged drug. (en)
|
| http://linked.open.../drugbank/synonym
| - Ciclosporin (en)
- Cyclosporin A (en)
- CsA (en)
- CyA (en)
|
| http://linked.open...drugbank/toxicity
| - The oral LD<sub>50</sub> is 2329 mg/kg in mice, 1480 mg/kg in rats, and > 1000 mg/kg in rabbits. The I.V. LD<sub>50</sub> is 148 mg/kg in mice, 104 mg/kg in rats, and 46 mg/kg in rabbits. (en)
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| http://linked.open...umeOfDistribution
| - The steady state volume of distribution during intravenous dosing has been reported as 3 to 5 L/kg in solid organ transplant recipients. Cyclosporine is excreted in human milk. (en)
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| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...k/foodInteraction
| - Red wine may reduce cyclosporine levels due to increased metabolism, therefore it appears prudent to avoid red wine (white wine does not appear to affect cyclosporine metabolism). (en)
- Avoid salt substitutes containing potassium. (en)
- Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product. (en)
- When taken with a meal, AUC and Cmax of cyclosporine modified decreased. (en)
|
| http://linked.open...nk/proteinBinding
| - In the plasma, approximately 90% is bound to proteins, primarily lipoproteins. In blood, the distribution is concentration dependent. Approximately 33% to 47% is in plasma, 4% to 9% in lymphocytes, 5% to 12% in granulocytes, and 41% to 58% in erythrocytes. (en)
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| http://linked.open...ynthesisReference
| - Hans Dietl, "Pharmaceutical preparation containing cyclosporine(s) for intravenous administration and a process for its production." U.S. Patent US5527537, issued October, 1990. (en)
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| http://linked.open...y/mesh/hasConcept
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
| |
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