Premium
Single‐Dose Kinetics and Bioavailability of Ketobemidone
Author(s) -
Anderson P.,
Arnér S.,
Bondesson U.,
Boréus L. O.,
Hartvig P.
Publication year - 1982
Publication title -
acta anaesthesiologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.738
H-Index - 107
eISSN - 1399-6576
pISSN - 0001-5172
DOI - 10.1111/j.1399-6576.1982.tb01848.x
Subject(s) - medicine , bioavailability , rectal administration , anesthesia , oral administration , pharmacokinetics , pharmacology , surgery
The single‐dose kinetics and the oral and rectal bioavailability of ketobemidone have been studied in patients after surgery. Plasma concentrations were determined following intravenous administration of Ketogin® 2 ml, containing ketobemidone chloride 10 mg and the spasmolytic substance N, N‐dimethyl‐3, 3‐diphenyl‐l‐methylallylamine chloride 50 mg and following oral or rectal administration of Ketogin. Ketobemidone was analyzed by gas chromatography‐mass spectrometry using a deuterated internal standard. Ketobemidone disappeared rapidly from plasma after i.v. or oral administration, yielding a mean plasma half‐life between 2.25 and 2.45 h. After rectal administration the plasma half‐life was somewhat prolonged (3.27 h), probably due to late absorption. The bioavailability of oral ketobemidone was 34%±16% s.d. (n=6), and when given rectally 44%±9% s.d. (n = 5). In contrast to earlier investigations performed without plasma analysis, ketobemidone was found to have a rapid elimination when given intravenously, orally or rectally.