Drug General Information (ID: DDIGR25LB6)
  Drug Name Cyclosporine Drug Info Orlistat Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Antiviral Agents Antiobesity Agents
  Structure

 Mechanism of Cyclosporine-Orlistat Interaction (Severity Level: Major)
     Altered Fat-soluble drugs absorption Click to Show/Hide Mechanism Graph
      Drug Name Cyclosporine Orlistat
      Mechanism Fat-soluble agent Decrease fat-soluble agent absorption
      Key Mechanism Factor 1
Factor Name Pharmacokinetic
Factor Description Alters the absorption of the drug, leading to changes in the plasma concentration of the drug and affecting the pharmacological effects.
      Mechanism Description
  • Decreased absorption of Cyclosporine caused by Orlistat 

Recommended Action
      Management Given the risk of organ rejection associated with inadequate drug levels, orlistat should preferably not be used in transplant patients treated with cyclosporine. If concomitant therapy is necessary, separating the doses by at least 2 hours may help minimize the potential for an interaction. Cyclosporine blood levels should be closely monitored and patients should be monitored for signs of rejection.

References
1 Colman E, Fossler M "Reduction in blood cyclosporine concentrations by orlistat." N Engl J Med 342 (2000): 1141. [PMID: 10766596]
2 Nagele H, Petersen B, Bonacker U, Rodiger W "Effect of orlistat on blood cyclosporin concentration in an obese heart transplant patient." Eur J Clin Pharmacol 55 (1999): 667-9. [PMID: 10638396]