Bioavailability of dexmedetomidine after intranasal administration

摘要: The aim of this proof-of-concept study was to characterize the pharmacokinetics and pharmacodynamics intranasal dexmedetomidine compared with its intravenous administration in a small number healthy volunteers. Single doses 84 μg were given once intravenously intranasally seven men. Plasma concentrations measured for 10 h, pharmacokinetic variables calculated standard noncompartmental methods. Heart rate, blood pressure, adrenaline noradrenaline plasma, central nervous system drug effects (with Maddox wing, Bispectral Index, three visual analog scales) monitored assess pharmacological dexmedetomidine. Six individuals included analyses. Following administration, peak plasma reached 38 (15–60) min absolute bioavailability 65% (35–93%) (medians ranges). Pharmacological similar both routes but their onset more rapid after administration. Dexmedetomidine is rather rapidly efficiently absorbed Compared may be feasible alternative patients requiring light sedation.