Pharmacokinetic and pharmacological effects and safety profile of eptazocine were investigated after an intravenous administration of eptazocine at doses of 60mg and 90mg under nitrous oxide, oxygen and enflurane anesthesia.
The pharmacokinetic data were well fitted to a three-compartment model. Its area under the curve (AUC) showed dose dependency (60mg:119.1μg·min/ml; 90mg:143.6μg·min/ml), although half-life (60mg:108.9min; 90mg:110.3min) and volume of distribution (60mg:76.6l; 90mg:70.1l) remained unchanged.
Blood pressure was slightly elevated after the administration of eptazocine. However, there were no clinically significant changes in pulse rate.
In recovery phase from the anesthesia, respiratory depression was not found. But at dose of 90mg, the time from the end of the anesthesia to the extubation was prolonged, being compared with at dose of 60mg, and the psychological status at the termination of anesthesia was drowsy at the doses of 60mg and 90mg.
From the above results, eptazocine at doses of 60mg and 90mg was confirmed to be safe under nitrous oxide, oxygen and enflurane anesthesia.
Furthermore, it was suggested that the property of eptazocine on the anesthetic effects of enflurane was additive.
