Premium
The kinetics of amylobarbitone metabolism in healthy men and women
Author(s) -
BALASUBRAMANIAM K.,
LUCAS S. B.,
MAWER G. E.,
SIMONS P. J.
Publication year - 1970
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1970.tb10364.x
Subject(s) - kinetics , metabolism , psychology , chemistry , endocrinology , medicine , physics , quantum mechanics
1 Sodium amylobarbitone (3·54 mg/kg) was given by intravenous injection to seven healthy men and nine healthy women who were not receiving other drugs. Serum amylobarbitone and urine hydroxyamylobarbitone concentrations were measured by gas‐liquid chromatography. There was no significant difference between the groups either in the serum amylobarbitone concentration/time curves or in the urinary excretion of hydroxyamylobarbitone. 2 The serum amylobarbitone concentration decayed over 48 h as a double exponential function of time; the first exponential component had a mean half‐time of 0·6 h (males 0·56 ± 0·06 h, females 0·62 ± 0·08 h, ± s.e. ) and the second exponential component had a mean half time of 21 h (males 22·7 ± 1·6 h, females 20·0 ± 1·0 h, ± s.e. ). 3 The urinary excretion of hydroxyamylobarbitone over 48 h accounted for 34% of the dose (males 33·8 ± 3·2%, females 35·2 ± 3·0%, ± s.e. ). One male and two female subjects excreted hydroxyamylobarbitone partly as a conjugate which was readily hydrolysed in acid. 4 An elimination constant ( k el ) derived from the serum concentration/time curve by the application of a two compartment model was approximately proportional to β (h −1 ), the rate constant of the second exponential component. There was a positive correlation ( r =0·78, P<0·001) between β and the mean rate of urinary excretion of hydroxyamylobarbitone during the 24 to 48 h period.