[Hypolipidemic treatment under special conditions: posttransplant and/or immunosuppressive therapy].
There are limited data regarding the use of hypolipidemic agents concomitantly with immunosuppressive drugs. Best evidence is provided for the use of statins and cyclosporine. In terms of pharmacodynamics, these two drugs have different substrates. In respect to pharmacokinetics, statins usually do not modify serum concentrations of cyclosporine, however when combined with any statin a careful monitoring of cyclosporine levels is recommended, due to a narrow therapeutic window of the immunosuppressive agent. Conversely, cyclosporine does affect the area under the curve for many statins, by inhibiting the CYP450 3A4, thus increasing systemic exposure to statins. Pravastatin appears to be the safest compound, once it is glucuronized. The area under the curve for the other statins (simvastatin, lovastatin, atorvastatin, cerivastatin, and rosuvastatin) can be increased in variable degrees according to the site of metabolization, liver extraction by OATP-C transporter, biliary secretion, renal excretion, and drug extrusion by the MDR system.
Izar
Maria Cristina de Oliveira
MC
Setor de Lípides, Aterosclerose e Biologia Vascular, UNIFESP-EPM.
D016572:Cyclosporine / Q000009:adverse effects / Q000627:therapeutic use*; D005464:Fluorobenzenes / Q000009:adverse effects / Q000627:therapeutic use; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000627:therapeutic use*; D007166:Immunosuppressive Agents / Q000009:adverse effects / Q000627:therapeutic use*; D016030:Kidney Transplantation / Q000009:adverse effects / Q000276:immunology; D008148:Lovastatin / Q000009:adverse effects / Q000627:therapeutic use; D017035:Pravastatin / Q000009:adverse effects / Q000627:therapeutic use; D011743:Pyrimidines / Q000009:adverse effects / Q000627:therapeutic use; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides / Q000009:adverse effects / Q000627:therapeutic use
D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D007166:Immunosuppressive Agents; D011743:Pyrimidines; D013449:Sulfonamides; D016572:Cyclosporine; D000068718:Rosuvastatin Calcium; D008148:Lovastatin; D017035:Pravastatin