Pharmacokinetics and pharmacodynamics of dermorphin in the horse.
J Vet Pharmacol Ther
; 38(4): 321-9, 2015 Aug.
Article
em En
| MEDLINE
| ID: mdl-25376170
ABSTRACT
Dermorphin is a µ-opioid receptor-binding peptide that causes both central and peripheral effects following intravenous administration to rats, dogs, and humans and has been identified in postrace horse samples. Ten horses were intravenously and/or intramuscularly administered dermorphin (9.3 ± 1.0 µg/kg), and plasma concentration vs. time data were evaluated using compartmental and noncompartmental analyses. Data from intravenous administrations fit a 2-compartment model best with distribution and elimination half-lives (harmonic mean ± pseudo SD) of 0.09 ± 0.02 and 0.76 ± 0.22 h, respectively. Data from intramuscular administrations fit a noncompartmental model best with a terminal elimination half-life of 0.68 ± 0.24 (h). Bioavailability following intramuscular administration was variable (47-100%, n = 3). The percentage of dermorphin excreted in urine was 5.0 (3.7-10.6) %. Excitation accompanied by an increased heart rate followed intravenous administration only and subsided after 5 min. A plot of the mean change in heart rate vs. the plasma concentration of dermorphin fit a hyperbolic equation (simple Emax model), and an EC(50) of 21.1 ± 8.8 ng/mL was calculated. Dermorphin was detected in plasma for 12 h and in urine for 48 or 72 h following intravenous or intramuscular administration, respectively.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peptídeos Opioides
/
Cavalos
/
Analgésicos Opioides
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Revista:
J Vet Pharmacol Ther
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Estados Unidos