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Pharmacokinetics of intrarectal nalbuphine in children undergoing general anaesthesia
Author(s) -
Bessard G.,
Alibeu JP,
Cartal M.,
Nicolle E.,
Debeauvais F Serre,
Devillier P.
Publication year - 1997
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/j.1472-8206.1997.tb00180.x
Subject(s) - nalbuphine , pharmacokinetics , rectal administration , analgesic , anesthesia , medicine , absorption (acoustics) , drug administration , high performance liquid chromatography , pharmacology , chemistry , chromatography , opioid , physics , receptor , acoustics
Summary— The pharmacokinetics of nalbuphine (0.3 mg/kg) administered by the rectal route were studied in ten children undergoing general anaesthesia for minor surgery. Blood sampling was carried out for 8 h after rectal administration and plasma drug concentrations were measured by high performance liquid chromatography using electrochemical detection after an optimized solid‐phase extraction procedure. The mean time to achieve the maximum plasma concentration (C max = 24 ± 15 ng/mL) was 25 ± 11 min and the elimination half‐life was 2.7 ± 0.7 h. The coefficients of variation for C max and the concentration‐time curve (AUC) were 62 and 68%, respectively. Although rectal absorption is considered irregular, the large intersubject variability is also explainable by a variable hepatic bypass for a drug, like nalbuphine, that undergoes extensive first‐pass metabolism. No problem of analgesic efficacy or of local tolerance was reported. In conclusion, the rectal route of administration provides a rapid and reliable absorption of nalbuphine.