Pharmacokinetics of fentanyl delivered transdermally in healthy adult horses–variability among horses and its clinical implications.
Abstract: The safety and pharmacokinetics of fentanyl, delivered transdermally at a dosage of 60-67 microg/kg, were investigated in six healthy adult horses. Three transdermal fentanyl patches (Duragesic), each containing 10 mg of fentanyl citrate, were applied to the mid-dorsal thorax of each horse and left in place for 72 h. Plasma fentanyl concentrations were periodically measured throughout this period and for 12 h after patch removal. After an initial delay of approximately 2 h, the plasma fentanyl concentration rose rapidly in a fairly linear fashion, reaching a peak at around 12 h; thereafter, it gradually declined in a roughly linear manner over the next 72 h. There was much individual variation, however. The initial delay ranged from 0 to 5.1 h (mean, 1.91+/-2.0 h), Tcmax ranged from 8.5 to 14.5 h (mean, 11.4+/-2.7 h) and Cmax ranged from 0.67 to 5.12 ng/mL (mean, 2.77+/-1.92 ng/mL). In two horses, the plasma fentanyl concentration failed to reach even 1 ng/mL, whereas in the other four horses it was >1 ng/mL for at least 40 h and for at least 72 h in two of these horses. No adverse effects attributable to fentanyl were observed in any of the horses, indicating that this dosage is safe in systemically healthy adult horses. However, it failed to achieve plasma fentanyl concentrations generally considered to be analgesic (>or=1 ng/mL) in about one-third of horses.
Publication Date: 2006-11-07 PubMed ID: 17083458DOI: 10.1111/j.1365-2885.2006.00796.xGoogle Scholar: Lookup
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- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
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The research investigates the safety and pharmacokinetics of transdermal fentanyl patches in adult horses. Differing responses among individual horses raise implications for clinical use.
Transdermal Fentanyl Patches: Administration and Quantification
- The study looked into administering fentanyl, a potent opioid analgesic, through transdermal patches to six healthy adult horses. The patches, with a dosage of 60-67 microg/kg, were placed on the mid-dorsal thorax of each horse and left for 72 hours.
- The researchers periodically measured plasma fentanyl concentrations during the application of the patch and for 12 hours post-removal.
- The initial 2-hour delay in absorption was observed after which the plasma fentanyl concentration increased fairly linearly, reaching its peak at around 12 hours. A subsequent decline was observed gradually over the next 72 hours.
Individual Variation in Horses
- There was significant variability in the responses among horses. The initial delay ranged between 0 to 5.1 hours, time to reach peak concentration varied from 8.5 to 14.5 hours, and the peak plasma concentration ranged from 0.67 to 5.12 ng/mL.
- In two horses, the plasma fentanyl concentration didn’t exceed 1 ng/mL, whereas it inflicted a higher concentration in the other four. In two of these four horses, the higher concentration of fentanyl was maintained for the full 72 hours.
Safety and Clinical Implications
- No adverse effects were linked to the usage of fentanyl, establishing that its dosage applied in the study is safe in healthy adult horses.
- However, the effectiveness of the drug as an analgesic is questionable. Around one-third of the horses did not achieve the plasma concentration considered effective for pain relief (1 ng/mL or more). This emphasizes the variability among individual horses and signals potential issues in achieving consistent clinical outcomes.
Cite This Article
APA
Orsini JA, Moate PJ, Kuersten K, Soma LR, Boston RC.
(2006).
Pharmacokinetics of fentanyl delivered transdermally in healthy adult horses–variability among horses and its clinical implications.
J Vet Pharmacol Ther, 29(6), 539-546.
https://doi.org/10.1111/j.1365-2885.2006.00796.x Publication
Researcher Affiliations
- Department of Clinical Studies, New Bolton Center, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, PA, USA. orsini@vet.upenn.edu
MeSH Terms
- Administration, Cutaneous
- Analgesics, Opioid / administration & dosage
- Analgesics, Opioid / blood
- Analgesics, Opioid / pharmacokinetics
- Animals
- Area Under Curve
- Female
- Fentanyl / administration & dosage
- Fentanyl / blood
- Fentanyl / pharmacokinetics
- Horses / metabolism
Citations
This article has been cited 3 times.- Bahrami F, Rossi RM, Defraeye T. Predicting transdermal fentanyl delivery using physics-based simulations for tailored therapy based on the age.. Drug Deliv 2022 Dec;29(1):950-969.
- Dmitrović P, Vanaga J, Dupont J, Franck T, Gougnard A, Detilleux J, Kovalcuka L, Salciccia A, Serteyn D, Sandersen C. Effect of Fentanyl Infusion on Heart Rate Variability and Anaesthetic Requirements in Isoflurane-Anaesthetized Horses.. Animals (Basel) 2021 Oct 9;11(10).
- Buchholz T, Hildebrand M, Heider A, Stenger V, Arens D, Spadavecchia C, Zeiter S. Transdermal Fentanyl Uptake at Two Different Patch Locations in Swiss White Alpine Sheep.. Animals (Basel) 2020 Sep 17;10(9).
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