Single-dose pharmacokinetics of orally and rectally administered misoprostol in adult horses.
Abstract: To characterize the pharmacokinetics of a clinically relevant dose of misoprostol administered PO or per rectum (PR) to horses. Methods: 8 healthy adult horses. Methods: In a randomized 3-way crossover design, horses received a single dose of misoprostol (5 μg/kg) administered PO (with horses fed and unfed) and PR, with a minimum 3-week washout period separating the experimental conditions. Blood samples were obtained before and at various points after drug administration (total, 24 hours), and plasma concentrations of misoprostol free acid were measured. Results: Mean maximum plasma concentration of misoprostol was significantly higher in the PR condition (mean ± SD, 967 ± 492 pg/mL) and unfed PO condition (655 ± 259 pg/mL) than in the fed PO condition (352 ± 109 pg/mL). Mean area under the concentration-versus-time curve was significantly lower in the PR condition (219 ± 131 pg•h/mL) than in the unfed (1,072 ± 360 pg•h/mL) and fed (518 ± 301 pg•h/mL) PO conditions. Mean time to maximum concentration was ≤ 30 minutes for all conditions. Mean disappearance half-life was shortest in the PR condition (21 ± 29 minutes), compared with values for the unfed (170 ± 129 minutes) and fed (119 ± 51 minutes) PO conditions. No adverse effects were noted. Conclusions: Misoprostol was rapidly absorbed and eliminated regardless of whether administered PO or PR to horses. Rectal administration may be a viable alternative for horses that cannot receive misoprostol PO, but this route may require more frequent administration to maintain therapeutic drug concentrations.
Publication Date: 2019-10-24 PubMed ID: 31644339DOI: 10.2460/ajvr.80.11.1026Google Scholar: Lookup
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- Journal Article
- Randomized Controlled Trial
- Veterinary
Summary
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The study investigates how a clinically relevant dose of misoprostol, a medication often used for stomach ulcers, gets absorbed and dispensed when administered orally (PO) or rectally (PR) in horses. It found out that while misoprostol was absorbed faster when given rectally, the drug left the system quickest when using this method, which may require more frequent applications for maintaining therapeutical drug levels.
Methods
- The researchers conducted this study using a randomized 3-way crossover design where each horse was subjected to each of three different conditions: misoprostol administered orally while fed, orally while unfed, and rectally.
- This method ensured that any individual characteristics of specific horses did not influence the overall results.
- Eight healthy adult horses were involved in this study, and they were given a three-week period between treatments to wash out any remaining medication in their systems.
- Blood samples were collected at specified intervals for 24 hours after drug administration and assessed for levels of misoprostol free acid, the active medication compound.
Results
- The research found out that the concentration of misoprostol in the horses’ bloodstream peaked faster when the drug was administered rectally or orally while the horse was unfed.
- However, when administered rectally, the concentration of the drug decreased faster as well. This was reflected by a significantly lower area under the concentration-time curve in the PR condition when compared to PO conditions.
- Moreover, when fed, the oral administration resulted in slower absorption and lower maximum concentration of the drug in the horses’ system.
- In terms of the drug’s disappearance, it was found to disappear fastest when the drug was administered rectally than when given orally (whether the horse was fed or not).
Conclusions
- In summary, the research found out that misoprostol gets rapidly into the equally fast leave the horses’ systems when given rectally.
- Oral administration with food slowed down both the drug’s absorption and dispensation.
- The study concluded that rectal administration could be an alternative for horses who can’t receive the drug orally. However, the rapid dispensation of the drug via this method may require more frequent dosages to maintain effective drug concentrations.
Cite This Article
APA
Lopp CT, McCoy AM, Boothe D, Schaeffer DJ, Lascola K.
(2019).
Single-dose pharmacokinetics of orally and rectally administered misoprostol in adult horses.
Am J Vet Res, 80(11), 1026-1033.
https://doi.org/10.2460/ajvr.80.11.1026 Publication
Researcher Affiliations
MeSH Terms
- Administration, Oral
- Administration, Rectal
- Animals
- Area Under Curve
- Cross-Over Studies
- Female
- Half-Life
- Horses / metabolism
- Male
- Misoprostol / administration & dosage
- Misoprostol / pharmacokinetics
Citations
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