Paracetamol disposition in normal subjects and in patients treated with antiepileptic drugs.
- 1 February 1979
- journal article
- clinical trial
- Published by Wiley in British Journal of Clinical Pharmacology
- Vol. 7 (2), 201-206
- https://doi.org/10.1111/j.1365-2125.1979.tb00922.x
Abstract
1 The serum concentration profile of paracetamol has been determined after administration of single 1000 mg intravenous and oral doses in six normal subjects and six epileptic patients on chronic antiepileptic drug therapy. The urinary excretion of free and conjugated paracetamol has also been determined. 2 Following intravenous administration, serum paracetamol concentration declined with first‐order kinetics. Both elimination rate and total body clearance were higher in the epileptic patients, although in neither case was the difference statistically significant. 3 The oral bioavailability (mean +/‐ s.e. mean) was significantly lower in the epileptic patients than in the normal subjects (0.77 +/‐ 0.03 and 0.89 +/‐ 0.02 respectively, P less than 0.01), whereas the urinary excretion total (free+conjugated) paracetamol was almost identical in the two groups. 4 It is suggested that the lower bioavailability of paracetamol in the epileptic patients results from enhancement of first‐pass metabolism, secondary to enzyme induction.Keywords
This publication has 32 references indexed in Scilit:
- Effects of alteration of hepatic microsomal enzyme activity on liver blood flow in the ratBiochemical Pharmacology, 1976
- Increased Clearance of Antipyrine and d-Propranolol after Phenobarbital Treatment in the MonkeyJCI Insight, 1974
- Primate Biliary Physiology VIII. THE EFFECT OF PHENOBARBITAL UPON BILE SALT SYNTHESIS AND POOL SIZE, BILIARY LIPID SECRETION, AND BILE COMPOSITIONJCI Insight, 1973
- Influence of Route of Administration on Drug AvailabilityJournal of Pharmaceutical Sciences, 1972
- Studies of Y and Z, two hepatic cytoplasmic organic anion-binding proteins: effect of drugs, chemicals, hormones, and cholestasisJCI Insight, 1971
- Changes in liver blood flow during enzyme inductionBiochemical Pharmacology, 1971
- Gas-liquid chromatographic estimation of paracetamolJournal of Pharmacy and Pharmacology, 1971
- Influence of First-Pass Effect on Availability of Drugs on Oral AdministrationJournal of Pharmaceutical Sciences, 1971
- The gas-liquid chromatographic estimation of phenacetin and paracetamol in plasma and urineJournal of Pharmacy and Pharmacology, 1971
- Drugs and Enzyme InductionAnnual Review of Pharmacology, 1969