Pharmacokinetics of the oral narcotic analgesic bezitramide and preliminary observations on its effect on experimentally induced pain.

Article Details

Citation
Copy to clipboard

Meijer DK, Hovinga G, Versluis A, Broring J, van Aken K, Moolenaar F, Wesseling H

Pharmacokinetics of the oral narcotic analgesic bezitramide and preliminary observations on its effect on experimentally induced pain.

Eur J Clin Pharmacol. 1984;27(5):615-8.

PubMed ID
6519169 [ View in PubMed
]
Abstract

The oral absorption of bezitramide 5 mg was studied in 7 human volunteers, using a specific radioimmuno-assay which measured both bezitramide and its active metabolite R-4618. A lag time of 0.5-1.0 h and a Cmax of 5.4 ng/ml plasma were found, the latter occurring 2.5-3.5 h after administration. The apparent elimination half-life varied from 11 to 24 h. Less than 0.3% of the dose was excreted unchanged in the urine. High concentrations in the faeces of some individuals indicate incomplete absorption and/or biliary secretion. The analgesic effect, using a standardized superficial electrical stimulation method, reached its maximum between 2.5 and 3.5 h after dosing, in accordance with the absorption phase. The duration of the effect was highly variable. Experiments in rats (n = 6, 3H-bezitramide 2.5 micrograms), demonstrated extensive biliary excretion (up to 70% of total radioactivity) and less than 3% of the label was removed by urinary excretion.

DrugBank Data that Cites this Article

Drugs