Year 2019 / Volume 26 / Number 6

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Special Article

Key factors governing spinal cord opioid bioavailability in the management of acute pain

Rev. Soc. Esp. Dolor. 2019; 26(6): 359-367 / DOI: 10.20986/resed.2019.3737/2019

Borja Mugabure Bujedo


ABSTRACT

Although there is no either ideal analgesic or route of neuraxial administration, clinicians alike continue to search for compounds with qualities which may approach this idea. However, it´s a demonstrated fact that spinal administration of an opioid drug does not always guarantee segmental and selective analgesia into the spinal cord. This point is valid due to partial reuptake of the drug to systemic blood circulation reaching specific brain opioid receptors, rather than the differences are explained by variations in the clearance rate from the cerebrospinal fluid. Published evidence from either human or animal experimental studies indicates that bioavailability in the spinal cord biophase is negatively correlated with liposolubility. Therefore, opioid spinal cord bioavailability is higher for hydrophilic opioids like morphine, than for lipophilic ones such as fentanyl, sufentanil or alfentanil.



RESUMEN

Aunque no existe un analgésico ni una vía de administración neuroaxial ideal, los clínicos continúan buscando compuestos con cualidades que puedan acercarse a esta idea. Sin embargo, se ha demostrado que la administración espinal de un medicamento opioide no siempre garantiza una analgesia segmentaria y selectiva en la médula espinal. Este punto es cierto debido a la recaptación parcial del fármaco a la circulación sistémica sanguínea que alcanza receptores opioides cerebrales específicos, además de las diferencias que se explican por las variaciones en la tasa de eliminación del líquido cefalorraquídeo. La evidencia publicada de estudios experimentales en humanos o animales indica que la biodisponibilidad en la biofase medular está
correlacionada negativamente con la liposolubilidad. Por lo tanto, la analgesia espinal es mayor para los opioides hidrófilos como la morfina, que para los lipófilos como el fentanilo, el sufentanilo o el alfentanilo.





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Mugabure Bujedo B. Key factors governing spinal cord opioid bioavailability in the management of acute pain. Rev Soc Esp Dolor 2019; 26(6): 359-367 / DOI: 1020986/resed20193737/2019


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Recibido: 08/04/2019

Aceptado: 31/05/2019

Prepublicado: 09/10/2019

Publicado: 11/12/2019

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