First-pass metabolism of cyclosporin by the gut

JC Kolars, PB Watkins, RM Merion, WM Awni - The Lancet, 1991 - Elsevier
JC Kolars, PB Watkins, RM Merion, WM Awni
The Lancet, 1991Elsevier
Cyclosporin is thought to be exclusively metabolised in the liver. We instilled cyclosporin into
the small bowel of 2 patients during the anhepatic phase of liver transplantation; cyclosporin
metabolites were readily detected in portal venous blood. Our findings indicate that the small
intestine is a major site of cyclosporin breakdown: such intestinal metabolism might help to
explain the poor oral bioavailability and drug interactions of cyclosporin.
Abstract
Cyclosporin is thought to be exclusively metabolised in the liver. We instilled cyclosporin into the small bowel of 2 patients during the anhepatic phase of liver transplantation; cyclosporin metabolites were readily detected in portal venous blood. Our findings indicate that the small intestine is a major site of cyclosporin breakdown: such intestinal metabolism might help to explain the poor oral bioavailability and drug interactions of cyclosporin.
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