. . "Following intravenous administration, the blood clearance of cyclosporine (assay: HPLC) is approximately 5 to 7 mL/min/kg in adult recipients of renal or liver allografts. Blood cyclosporine clearance appears to be slightly slower in cardiac transplant patients. The following are clearance parameters (CL/F) for select patient populations: * 593 \u00B1 204 mL/min [De novo renal transplant patients, 597\u00B1174 mg/day] * 492 \u00B1 140 mL/min [Stable renal transplant patients, 344\u00B1122 mg/day] * 577 \u00B1 309 mL/min [De novo liver transplant, 458\u00B1190 mg/day] * 613 \u00B1 196 mL/min [De novo rheumatoid arthritis, 182\u00B155.6 mg/day] * 723 \u00B1 186 mL/min [De novo psoriasis, 189\u00B169.8 mg/day] \t * 285 \u00B1 94 mL/min [Stable Liver Transplant, Age 2 - 8, Dosed T.I.D 101\u00B125 mg/day] * 378 \u00B1 80 mL/min [Stable Liver Transplant, Age 8 - 15, Dosed B.I.D 188\u00B155 mg/day] \t * 171 mL/min [Stable liver transplant, Age 3, Dosed B.I.D 120 mg/day] * 328 \u00B1 121 mL/min [Stable liver transplant, Age 8 - 15, Dosed B.I.D 158\u00B155 mg/day] \t * 418 \u00B1 143 mL/min [Stable renal transplant, Age 7 - 15, Dosed B.I.D 328\u00B183 mg/day] \t"@en . . . . . . . . . . . . . . . . . . . . . . "Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product."@en . . . . . . . . . . . . . . . . . . . . . . "Cyclosporin A"@en . . . . . . . . "For treatment of transplant (kidney, liver, and heart) rejection, rheumatoid arthritis, severe psoriasis. "@en . . . . . "CsA"@en . . . . . . "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 . . . "investigational"@en . . . . "The oral LD₅₀ is 2329 mg/kg in mice, 1480 mg/kg in rats, and > 1000 mg/kg in rabbits. The I.V. LD₅₀ is 148 mg/kg in mice, 104 mg/kg in rats, and 46 mg/kg in rabbits."@en . . . "Hans Dietl, \"Pharmaceutical preparation containing cyclosporine(s) for intravenous administration and a process for its production.\" U.S. Patent US5527537, issued October, 1990."@en . " "@en . . "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 . . "approved"@en . "Cyclosporine"@en . . "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 . . . . . . . "The absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. The extent of absorption is dependent on the individual patient, the patient population, and the formulation. The absolute bioavailability of cyclosproine administered as Sandimmune\u00AE is dependent on the patient population, estimated to be less than 10% in liver transplant patients and as great as 89% in some renal transplant patients. Compared to an intravenous infusion, the absolute bioavailability of the oral solution is approximately 30% based upon the results in 2 patients. The cyclosporine capsules and oral solution are bioequivalent. The time of peak blood concentrations (Tmax) following oral administration of cyclosporine [modified] ranged from 1.5 - 2.0 hours. "@en . . "Ciclosporin"@en . . . . . . "Humans and other mammals"@en . . . . . . . "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 . . "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 . . . "When taken with a meal, AUC and Cmax of cyclosporine modified decreased."@en . . . . . . . . . . "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 . . . . . . . . . . "CyA"@en . . "# 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 . . . . . "59865-13-3"@en . "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 . . . . . . . . . . . . . .