The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia

Melissa Wheeler*, Patrick K Birmingham, Ralph A. Lugo, Corri L. Heffner, Charles J. Coté

*Corresponding author for this work

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

The bioavailability of oral transmucosal fentanyl citrate (OTFC) in children is similar to that of fentanyl solution administered orally to adults. We hypothesized that administering an oral fentanyl solution to children would result in similar fentanyl plasma concentrations and pharmacokinetic variables as administering comparable doses of OTFC. In this pilot study, 10 healthy children requiring postoperative analgesia were enrolled. Each received the undiluted IV fentanyl formulation orally (approximately 10-15 μg/kg; maximum, 400 μg). Venous blood samples were collected from 15 to 600 min after administration. Pharmacokinetic variables were determined using non-compartmental analysis and were compared with a previously studied population of children who received a similar dose of OTFC. Pharmacokinetic variables for the orally administered IV fentanyl formulation were as follows: time to reach peak concentration = 1.7 ± 1.6 h, peak concentration = 1.83 ± 1.19 ng/mL, half-life = 4.7 ± 2.8 h, area under the plasma concentration time curve = 6.46 ± 3.96 h · ng-1 · mL-1, apparent oral volume of distribution (V/F) = 17.5 ± 7.2 L/kg, apparent oral clearance (CL/F) = 3.33 ± 2.25 L · kg-1 · h-1. Although both OTFC and orally administered IV fentanyl resulted in similar pharmacokinetic variables and plasma concentrations for a given dose, there was marked interpatient variability, particularly in the early hours after oral administration of the IV formulation of fentanyl. This suggests that this method of administration be used with caution until further data are available.

Original languageEnglish (US)
Pages (from-to)1347-1351
Number of pages5
JournalAnesthesia and Analgesia
Volume99
Issue number5
DOIs
StatePublished - Nov 1 2004
Externally publishedYes

Fingerprint

Fentanyl
General Anesthesia
Pharmacokinetics
Analgesia
Biological Availability
Oral Administration
Half-Life

ASJC Scopus subject areas

  • Anesthesiology and Pain Medicine

Cite this

Wheeler, Melissa ; Birmingham, Patrick K ; Lugo, Ralph A. ; Heffner, Corri L. ; Coté, Charles J. / The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia. In: Anesthesia and Analgesia. 2004 ; Vol. 99, No. 5. pp. 1347-1351.
@article{f50afa1b293c4500909c64aae2754cc1,
title = "The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia",
abstract = "The bioavailability of oral transmucosal fentanyl citrate (OTFC) in children is similar to that of fentanyl solution administered orally to adults. We hypothesized that administering an oral fentanyl solution to children would result in similar fentanyl plasma concentrations and pharmacokinetic variables as administering comparable doses of OTFC. In this pilot study, 10 healthy children requiring postoperative analgesia were enrolled. Each received the undiluted IV fentanyl formulation orally (approximately 10-15 μg/kg; maximum, 400 μg). Venous blood samples were collected from 15 to 600 min after administration. Pharmacokinetic variables were determined using non-compartmental analysis and were compared with a previously studied population of children who received a similar dose of OTFC. Pharmacokinetic variables for the orally administered IV fentanyl formulation were as follows: time to reach peak concentration = 1.7 ± 1.6 h, peak concentration = 1.83 ± 1.19 ng/mL, half-life = 4.7 ± 2.8 h, area under the plasma concentration time curve = 6.46 ± 3.96 h · ng-1 · mL-1, apparent oral volume of distribution (V/F) = 17.5 ± 7.2 L/kg, apparent oral clearance (CL/F) = 3.33 ± 2.25 L · kg-1 · h-1. Although both OTFC and orally administered IV fentanyl resulted in similar pharmacokinetic variables and plasma concentrations for a given dose, there was marked interpatient variability, particularly in the early hours after oral administration of the IV formulation of fentanyl. This suggests that this method of administration be used with caution until further data are available.",
author = "Melissa Wheeler and Birmingham, {Patrick K} and Lugo, {Ralph A.} and Heffner, {Corri L.} and Cot{\'e}, {Charles J.}",
year = "2004",
month = "11",
day = "1",
doi = "10.1213/01.ANE.0000132777.00967.A3",
language = "English (US)",
volume = "99",
pages = "1347--1351",
journal = "Anesthesia and Analgesia",
issn = "0003-2999",
publisher = "Lippincott Williams and Wilkins",
number = "5",

}

The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia. / Wheeler, Melissa; Birmingham, Patrick K; Lugo, Ralph A.; Heffner, Corri L.; Coté, Charles J.

In: Anesthesia and Analgesia, Vol. 99, No. 5, 01.11.2004, p. 1347-1351.

Research output: Contribution to journalArticle

TY - JOUR

T1 - The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia

AU - Wheeler, Melissa

AU - Birmingham, Patrick K

AU - Lugo, Ralph A.

AU - Heffner, Corri L.

AU - Coté, Charles J.

PY - 2004/11/1

Y1 - 2004/11/1

N2 - The bioavailability of oral transmucosal fentanyl citrate (OTFC) in children is similar to that of fentanyl solution administered orally to adults. We hypothesized that administering an oral fentanyl solution to children would result in similar fentanyl plasma concentrations and pharmacokinetic variables as administering comparable doses of OTFC. In this pilot study, 10 healthy children requiring postoperative analgesia were enrolled. Each received the undiluted IV fentanyl formulation orally (approximately 10-15 μg/kg; maximum, 400 μg). Venous blood samples were collected from 15 to 600 min after administration. Pharmacokinetic variables were determined using non-compartmental analysis and were compared with a previously studied population of children who received a similar dose of OTFC. Pharmacokinetic variables for the orally administered IV fentanyl formulation were as follows: time to reach peak concentration = 1.7 ± 1.6 h, peak concentration = 1.83 ± 1.19 ng/mL, half-life = 4.7 ± 2.8 h, area under the plasma concentration time curve = 6.46 ± 3.96 h · ng-1 · mL-1, apparent oral volume of distribution (V/F) = 17.5 ± 7.2 L/kg, apparent oral clearance (CL/F) = 3.33 ± 2.25 L · kg-1 · h-1. Although both OTFC and orally administered IV fentanyl resulted in similar pharmacokinetic variables and plasma concentrations for a given dose, there was marked interpatient variability, particularly in the early hours after oral administration of the IV formulation of fentanyl. This suggests that this method of administration be used with caution until further data are available.

AB - The bioavailability of oral transmucosal fentanyl citrate (OTFC) in children is similar to that of fentanyl solution administered orally to adults. We hypothesized that administering an oral fentanyl solution to children would result in similar fentanyl plasma concentrations and pharmacokinetic variables as administering comparable doses of OTFC. In this pilot study, 10 healthy children requiring postoperative analgesia were enrolled. Each received the undiluted IV fentanyl formulation orally (approximately 10-15 μg/kg; maximum, 400 μg). Venous blood samples were collected from 15 to 600 min after administration. Pharmacokinetic variables were determined using non-compartmental analysis and were compared with a previously studied population of children who received a similar dose of OTFC. Pharmacokinetic variables for the orally administered IV fentanyl formulation were as follows: time to reach peak concentration = 1.7 ± 1.6 h, peak concentration = 1.83 ± 1.19 ng/mL, half-life = 4.7 ± 2.8 h, area under the plasma concentration time curve = 6.46 ± 3.96 h · ng-1 · mL-1, apparent oral volume of distribution (V/F) = 17.5 ± 7.2 L/kg, apparent oral clearance (CL/F) = 3.33 ± 2.25 L · kg-1 · h-1. Although both OTFC and orally administered IV fentanyl resulted in similar pharmacokinetic variables and plasma concentrations for a given dose, there was marked interpatient variability, particularly in the early hours after oral administration of the IV formulation of fentanyl. This suggests that this method of administration be used with caution until further data are available.

UR - http://www.scopus.com/inward/record.url?scp=6444236948&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=6444236948&partnerID=8YFLogxK

U2 - 10.1213/01.ANE.0000132777.00967.A3

DO - 10.1213/01.ANE.0000132777.00967.A3

M3 - Article

VL - 99

SP - 1347

EP - 1351

JO - Anesthesia and Analgesia

JF - Anesthesia and Analgesia

SN - 0003-2999

IS - 5

ER -