The iontophoresis of fentanyl citrate in humans

M. A. Ashburn, J. Streisand, J. Zhang, G. Love, Mark Rowin, S. Niu, J. K. Kievit, J. R. Kroep, M. J. Mertens

Research output: Contribution to journalArticle

65 Citations (Scopus)

Abstract

Background: Iontophoresis is a method of transdermal administration of ionizable drugs in which the electrically charged components are propelled through the skin by an external electric field. This study was designed to determine whether iontophoresis could be used to deliver clinically significant doses of fentanyl in humans and whether there is a charge-dose relation in the delivery of fentanyl by iontophoresis. Methods: Five adult volunteers were tested three times on separate days, once receiving passive treatment of 0.O mA for 2 h (0 mA · min), iontophoresis 1.0 mA for 2 h (120 mA · min), and iontophoresis 2.0 mA for 2 h (240 mA · min) in an open, randomized, crossover design. Respiratory rate, heart rate, blood pressure, and hemoglobin oxygen saturation were monitored throughout the study. Plasma fentanyl concentrations were measured several times before, during, and after iontophoresis. Plasma fentanyl concentrations were measured by radioimmunoassay. Results: No fentanyl was detected after passive (0.0-mA) fentanyl delivery. The following results were obtained for the 1.0- and 2.0- mA deliveries, respectively. Mean times to detectable concentrations of plasma fentanyl were 33 and 19 min; mean times to maximum concentration were 122 and 119 min; maximum concentrations were 0.76 and 1.59 ng/ml(P = 0.010); mean areas under the curve of the plasma fentanyl concentration versus time relation were 233 and 474 ng · ml-1 · min (P = 0.003); and mean elimination half-lives were 354 and 413 min (P = 0.326). Only minor adverse side effects related to iontophoresis occurred. However, typical opioid- related effects occurred frequently in the 1.0- and 2.0-mA administration groups. Conclusions: Clinically significant doses of fentanyl can be administered by iontophoresis for delivery periods of 2 h. A charge-dose relation exists after administration with currents of 1.0 and 2.0 mA. Future research into the iontophoresis of fentanyl as a method of potent opioid administration is indicated.

Original languageEnglish (US)
Pages (from-to)1146-1153
Number of pages8
JournalAnesthesiology
Volume82
Issue number5
DOIs
StatePublished - Jan 1 1995
Externally publishedYes

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Iontophoresis
Fentanyl
Opioid Analgesics
Cutaneous Administration
Respiratory Rate
Cross-Over Studies
Area Under Curve
Radioimmunoassay
Volunteers
Hemoglobins
Heart Rate
Oxygen
Blood Pressure

All Science Journal Classification (ASJC) codes

  • Anesthesiology and Pain Medicine

Cite this

Ashburn, M. A., Streisand, J., Zhang, J., Love, G., Rowin, M., Niu, S., ... Mertens, M. J. (1995). The iontophoresis of fentanyl citrate in humans. Anesthesiology, 82(5), 1146-1153. https://doi.org/10.1097/00000542-199505000-00009

The iontophoresis of fentanyl citrate in humans. / Ashburn, M. A.; Streisand, J.; Zhang, J.; Love, G.; Rowin, Mark; Niu, S.; Kievit, J. K.; Kroep, J. R.; Mertens, M. J.

In: Anesthesiology, Vol. 82, No. 5, 01.01.1995, p. 1146-1153.

Research output: Contribution to journalArticle

Ashburn, MA, Streisand, J, Zhang, J, Love, G, Rowin, M, Niu, S, Kievit, JK, Kroep, JR & Mertens, MJ 1995, 'The iontophoresis of fentanyl citrate in humans', Anesthesiology, vol. 82, no. 5, pp. 1146-1153. https://doi.org/10.1097/00000542-199505000-00009
Ashburn MA, Streisand J, Zhang J, Love G, Rowin M, Niu S et al. The iontophoresis of fentanyl citrate in humans. Anesthesiology. 1995 Jan 1;82(5):1146-1153. https://doi.org/10.1097/00000542-199505000-00009
Ashburn, M. A. ; Streisand, J. ; Zhang, J. ; Love, G. ; Rowin, Mark ; Niu, S. ; Kievit, J. K. ; Kroep, J. R. ; Mertens, M. J. / The iontophoresis of fentanyl citrate in humans. In: Anesthesiology. 1995 ; Vol. 82, No. 5. pp. 1146-1153.
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AU - Streisand, J.

AU - Zhang, J.

AU - Love, G.

AU - Rowin, Mark

AU - Niu, S.

AU - Kievit, J. K.

AU - Kroep, J. R.

AU - Mertens, M. J.

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N2 - Background: Iontophoresis is a method of transdermal administration of ionizable drugs in which the electrically charged components are propelled through the skin by an external electric field. This study was designed to determine whether iontophoresis could be used to deliver clinically significant doses of fentanyl in humans and whether there is a charge-dose relation in the delivery of fentanyl by iontophoresis. Methods: Five adult volunteers were tested three times on separate days, once receiving passive treatment of 0.O mA for 2 h (0 mA · min), iontophoresis 1.0 mA for 2 h (120 mA · min), and iontophoresis 2.0 mA for 2 h (240 mA · min) in an open, randomized, crossover design. Respiratory rate, heart rate, blood pressure, and hemoglobin oxygen saturation were monitored throughout the study. Plasma fentanyl concentrations were measured several times before, during, and after iontophoresis. Plasma fentanyl concentrations were measured by radioimmunoassay. Results: No fentanyl was detected after passive (0.0-mA) fentanyl delivery. The following results were obtained for the 1.0- and 2.0- mA deliveries, respectively. Mean times to detectable concentrations of plasma fentanyl were 33 and 19 min; mean times to maximum concentration were 122 and 119 min; maximum concentrations were 0.76 and 1.59 ng/ml(P = 0.010); mean areas under the curve of the plasma fentanyl concentration versus time relation were 233 and 474 ng · ml-1 · min (P = 0.003); and mean elimination half-lives were 354 and 413 min (P = 0.326). Only minor adverse side effects related to iontophoresis occurred. However, typical opioid- related effects occurred frequently in the 1.0- and 2.0-mA administration groups. Conclusions: Clinically significant doses of fentanyl can be administered by iontophoresis for delivery periods of 2 h. A charge-dose relation exists after administration with currents of 1.0 and 2.0 mA. Future research into the iontophoresis of fentanyl as a method of potent opioid administration is indicated.

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