Pharmacokinetic Properties of Ethosuximide in Monkeys. I. Single‐Dose Intravenous and Oral Administration
- 1 December 1975
- Vol. 16 (5), 705-716
- https://doi.org/10.1111/j.1528-1157.1975.tb04755.x
Abstract
The pharmacokinetic profile of ethosuximide [an antiepileptic drug] was studied in 6 chronically catheterized male rhesus monkeys at 3 dose levels (30, 60 and 90 mg/kg), i.v. and orally. Plasma and urine levels were assayed by GLC. The i.v. and oral kinetics of ethosuximide were described in terms of a 1-compartment open model with 1st-order elimination (and 1st-order absorption for oral kinetics). Volume of distribution (overall mean .+-. SD = 0.80 .+-. 0.09 l/kg), total body clearance (overall mean .+-. SD = 19.2 .+-. 2.70 ml/h per kg) and elimination half-life (overall mean .+-. SD = 28.98 .+-. 3.35 h and 28.10 .+-. 3.17 h following i.v. and oral administration, respectively) remained constant over the dosage range studied. The bioavailability of the syrup formulation used in the oral studies was essentially complete (overall mean .+-. SD = 96% .+-. 12.0) and dose-independent. The fraction of dose excreted unchanged in urine (overall mean .+-. SD) was 0.32 .+-. 0.07.Keywords
This publication has 5 references indexed in Scilit:
- Pharmacokinetic Evaluation of Anticonvulsants Prior to Efficacy Testing Exemplified by Carbamazepine in Epileptic Monkey ModelEpilepsia, 1974
- Spontaneous Seizure Frequency and Avoidance Conditioning in MonkeysEpilepsia, 1972
- Potential Erroneous Assignment of Nonlinear Data to the Classical Linear Two-Compartment Open ModelJournal of Pharmaceutical Sciences, 1972
- Method of Estimating Relative Absorption of a Drug in a Series of Clinical Studies in Which Blood Levels are Measured After Single and/or Multiple DosesJournal of Pharmaceutical Sciences, 1967
- Per Cent Absorbed Time Plots Derived from Blood Level and/or Urinary Excretion DataJournal of Pharmaceutical Sciences, 1963