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El metabolismo de primer paso de la ciclosporina por el intestino
J C Kolars1, W M Awni, R M Merion
1Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor.
Lancet (London, England)
|December 14, 1991
Resumen
La ciclosporina se metaboliza principalmente en el hígado. Sin embargo, este estudio encontró una descomposición significativa de la ciclosporina en el intestino delgado, lo que explica su mala absorción oral y las interacciones farmacológicas.
Área de la Ciencia:
- Farmacología Farmacología.
- Gastroenterología y Gastroenterología.
- Medicina del trasplante Medicina del trasplante
Sus antecedentes:
- La ciclosporina (también conocida como ciclosporina) es un fármaco inmunosupresor.
- Se cree ampliamente que el hígado es el único sitio del metabolismo de la ciclosporina.
- Comprender el metabolismo de la ciclosporina es crucial para optimizar su uso terapéutico y controlar los efectos adversos.
Objetivo del estudio:
- Para investigar el papel del intestino delgado en el metabolismo de la ciclosporina.
- Para determinar si la ciclosporina se descompone en el tracto gastrointestinal antes de la circulación hepática.
Principales métodos:
- Administración de ciclosporina directamente en el intestino delgado de dos pacientes trasplantados de hígado.
- Recolección de muestras de sangre venosa portal durante la fase anhepática (cuando se extrae el hígado).
- Análisis de la sangre venosa portal para detectar la presencia de metabolitos de la ciclosporina.
Principales resultados:
- Los metabolitos de la ciclosporina se detectaron fácilmente en la sangre venosa portal.
- La presencia de metabolitos en la sangre portal indica que el metabolismo intestinal ocurrió antes de llegar al hígado.
Conclusiones:
- El intestino delgado es un sitio significativo para el metabolismo de la ciclosporina.
- El metabolismo intestinal puede contribuir a la biodisponibilidad oral variable de la ciclosporina.
- Este hallazgo podría explicar las interacciones farmacológicas observadas con ciclosporina.
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