J. vet. Pharmacol. Therap.. 2017;1–7. wileyonlinelibrary.com/journal/jvp
|
1 © 2017 John Wiley & Sons Ltd
Received: 4 April 2016
|
Accepted: 14 February 2017
DOI: 10.1111/jvp.12403
ORIGINAL ARTICLE
Pharmacokinetics of intravenous and transdermal fentanyl in
alpacas
M. Lovasz | T. K. Aarnes | J. A. E. Hubbell | R. M. Bednarski | P. Lerche |
J. Lakritz
Department of Veterinary Clinical Sciences,
College of Veterinary Medicine, The Ohio
State University, Columbus, Ohio, USA
Correspondence
Turi K. Aarnes, Department of Veterinary
Clinical Sciences, College of Veterinary
Medicine, The Ohio State University,
Columbus, Ohio, USA.
Email: aarnes.1@osu.edu
Present address
John A. E. Hubbell, Rood and Riddle Equine
Hospital, Lexington, KY 40580, USA.
Funding information
Morris Animal Foundation, Grant/Award
Number: Grant Number D15LA-301
The purpose of the study was to determine pharmacokinetics of fentanyl after intrave-
nous (i.v.) and transdermal (t.d.) administration to six adult alpacas. Fentanyl was ad-
ministered i.v. (2 μg/kg) or t.d. (nominal dose: 2 μg kg
−1
hr
−1
). Plasma concentrations
were determined using liquid chromatography–mass spectrometry. Heart rate and
respiratory rate were assessed. Extrapolated, zero-time plasma fentanyl concentra-
tions were 6.0 ng/ml (1.7–14.6 ng/ml) after i.v. administration, total plasma clearance
was 1.10 L hr
−1
kg
−1
(0.75–1.40 L hr
−1
kg
−1
), volumes of distribution were 0.30 L/kg
(0.10–0.99 L/kg), 1.10 L/kg (0.70–2.96 L/kg) and 1.5 L/kg (0.8–3.5 L/kg) for V
1
, V
2
,
and V
ss
, respectively. Elimination half-life was 1.2 hr (0.5–4.3 hr). Mean residence time
(range) after i.v. dosing was 1.30 hr (0.65–4.00 hr). After t.d. fentanyl administration,
maximum plasma fentanyl concentration was 1.20 ng/ml (0.72–3.00 ng/ml), which oc-
curred at 25 hr (8–48 hr) after patch placement. The area under the plasma fentanyl
concentration-vs-time curve (extrapolated to infinity) after t.d. fentanyl was 61 ng*hr/
ml (49–93 ng*hr/ml). The dose-normalized bioavailability of fentanyl from t.d. fentanyl
in alpacas was 35.5% (27–64%). Fentanyl absorption from the t.d. fentanyl patch into
the central compartment occurred at a rate of approximately 50 μg/hr (29–81 μg/hr)
between 8 and 72 hr after patch placement.
1 | INTRODUCTION
Fentanyl is a mu receptor opioid agonist commonly used in animals
to provide analgesia. The pharmacokinetics of fentanyl have been de-
scribed after i.v. administration in dogs (Kukanich & Allen, 2014; Sano
et al., 2006), cats (Lee, Papich, & Hardie, 2000; Pypendop, Brosnan,
Majewski-Tiedeken, Stanley, & Ilkiw, 2014), horses (Maxwell, Thomasy,
Slovis, & Kollias-Baker, 2003; Sanchez, Robertson, Maxwell, Zientek, &
Cole, 2007; Thomasy, Mama, Whitley, Steffey, & Stanley, 2007), goats
(Carroll, Hooper, Boothe, Hartsfield, & Randoll, 1999), and sheep
(Ahern, Soma, Rudy, Uboh, & Schaer, 2010). Plasma concentrations of
0.95 ng/ml of fentanyl are associated with analgesia in dogs (Robinson
et al., 1999; Sano et al., 2006). Side effects of fentanyl at relatively
high plasma concentrations include respiratory depression in dogs
(Arndt, Mikat, & Parasher, 1984) and increased locomotor activity in
horses (Kamerling, DeQuick, Weckman, & Tobin, 1985). Documented
use of fentanyl in alpacas is limited to a single case report of a 5 μg/kg
i.v. bolus given to a neonate to facilitate successful placement of a
nasotracheal tube (Tinkler, Mathews, Firshman, & Quandt, 2015).
Fentanyl has been formulated as a transdermal (t.d.) patch to fa-
cilitate sustained drug delivery. The fentanyl t.d. patch is designed to
slowly and consistently release fentanyl (zero-order absorption kinet-
ics) to the skin surface where it is absorbed then distributed system-
ically via the circulation. Rate of absorption can be affected by body
temperature, the amount of body fat present, the location of patch
application, and the species in which it is used. Pharmacokinetics
of t.d. administration have been evaluated in dogs (Kyles, Papich, &
Hardie, 1996; Reed et al., 2011; Schultheiss, Morse, & Baker, 1995),
cats (Lee et al., 2000), sheep (Ahern et al., 2010), goats (Carroll et al.,
1999), llamas (Grubb et al., 2005), and horses (Eberspächer, Stanley,
Rezende, & Steffey, 2008; Maxwell et al., 2003). In llamas, serum fen-
tanyl concentrations were first detectable between 12 and 24 hr after