PHARMACOKINETICS OF INTRANASAL FENTANYL

H.W. Striebel, J. Kramer, I. Luhmann, I. Rohierse-Hohler, and A. Rieger

Der Schmerz (1993) 7:122-125

© Springer-Verlag 1993

 Abstract. Background and aim of the study. Intranasal fentanyl seems to be a promising, non-invasive and rapid-acting new mode of opioid administration that is especially suitable in acute pain syndromes. To date no pharmacokinetic data are available on intranasal fentanyl. In this prospective, randomised and double-blind cross-over study intranasal and intravenous administration of fentanyl were investigated.

Patients and methods. Fentanyl 0.054 mg was administered to eight volunteers (age: 31.5 +/- 7.7 cm; weight 70.8 +/- 9.9 kg). Each volunteer received either 12 sprays (0.054 mg) fentanyl intranasally and simultaneously 12 ml of NaCl 0.9% intravenously, or after a time lag of at least 7 days 12 sprays of NaCl 0.9% intranasally and 12 ml of a diluted fentanyl solution (0.054 mg) intravenously. Venous blood was sampld from a cubital vein 5, 10, 15, 20, 25, 30, 40, 50, 80 and 120 min after dosing.

Results. Following intravenous and intranasal administration the corresponding graphic concentration curves reached their maximal fentanyl concentrations (C max) 5 min after administration. The Cmax following intranasal administration was 58% of the Cmax following intravenous administration. The bioavailability calculated on the basis of the intravenous and intranasal graphic concentration curve was 71%.

Discussion and conclusion. This pharmacokinetic study demonstrates a rapid rise in fentanyl plasma concentrations after intranasal fentanyl as well as a high bioavailability. These pharmacokinetic results are comparable to those obtained with intranasal sufentanil. From a pharmacokinetic point of view, intranasal fentanyl seems suitable for demand-adapted titration.