The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs
The pharmacokinetics of diminazene aceturate following intramuscular (i.m.) administration at 4.2 mg/kg was evaluated in 8 healthy German Shepherd dogs. Blood samples were collected at 19 intervals over a period of 21 days. Diminazene plasma concentrations were measured using a validated HPLC method...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
AOSIS
2005-06-01
|
Series: | Journal of the South African Veterinary Association |
Subjects: | |
Online Access: | https://jsava.co.za/index.php/jsava/article/view/416 |
id |
doaj-4e84e0f8b7314024ba7be2b12cff4751 |
---|---|
record_format |
Article |
spelling |
doaj-4e84e0f8b7314024ba7be2b12cff47512020-11-24T23:22:41ZengAOSISJournal of the South African Veterinary Association1019-91282224-94352005-06-0176314615010.4102/jsava.v76i3.416372The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogsD.M. MillerG.E. SwanR.G. LobettiL.S. JacobsonThe pharmacokinetics of diminazene aceturate following intramuscular (i.m.) administration at 4.2 mg/kg was evaluated in 8 healthy German Shepherd dogs. Blood samples were collected at 19 intervals over a period of 21 days. Diminazene plasma concentrations were measured using a validated HPLC method with UV detection and a sensitivity of 25 ng/m . The in vitro and in vivo binding of diminazene to blood elements was additionally determined. Diminazene pharmacokinetics showed a large inter-individual variation after i.m. administration. It had a short absorption half-life (K01-HL of 0.11 + 0.18 h), resulting in a Cmax of 1849 + 268.7 ng/mℓ at Tmax of 0.37 h and a mean overall elimination half-life (T1/2ß) of 5.31 + 3.89 h. A terminal half-life of 27.5 + 25.0 h was measured. At 1 h after i.m. injection, 75% of the diminazene in whole blood was in the plasma fraction. The results of this study indicate that diminazene is rapidly distributed and sequestered into the liver, followed by a slower terminal phase during which diminazene is both redistributed to the peripheral tissues and/or renally excreted. It is recommended that diminazene administered i.m. at 4.2 mg/kg should not be repeated within a 21-day period.https://jsava.co.za/index.php/jsava/article/view/416Babesia CanisBabesiosisBerenilCanineDiminazeneLiver SequestrationPharmacokineticsPharmacology |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
D.M. Miller G.E. Swan R.G. Lobetti L.S. Jacobson |
spellingShingle |
D.M. Miller G.E. Swan R.G. Lobetti L.S. Jacobson The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs Journal of the South African Veterinary Association Babesia Canis Babesiosis Berenil Canine Diminazene Liver Sequestration Pharmacokinetics Pharmacology |
author_facet |
D.M. Miller G.E. Swan R.G. Lobetti L.S. Jacobson |
author_sort |
D.M. Miller |
title |
The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs |
title_short |
The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs |
title_full |
The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs |
title_fullStr |
The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs |
title_full_unstemmed |
The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs |
title_sort |
pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs |
publisher |
AOSIS |
series |
Journal of the South African Veterinary Association |
issn |
1019-9128 2224-9435 |
publishDate |
2005-06-01 |
description |
The pharmacokinetics of diminazene aceturate following intramuscular (i.m.) administration at 4.2 mg/kg was evaluated in 8 healthy German Shepherd dogs. Blood samples were collected at 19 intervals over a period of 21 days. Diminazene plasma concentrations were measured using a validated HPLC method with UV detection and a sensitivity of 25 ng/m . The in vitro and in vivo binding of diminazene to blood elements was additionally determined. Diminazene pharmacokinetics showed a large inter-individual variation after i.m. administration. It had a short absorption half-life (K01-HL of 0.11 + 0.18 h), resulting in a Cmax of 1849 + 268.7 ng/mℓ at Tmax of 0.37 h and a mean overall elimination half-life (T1/2ß) of 5.31 + 3.89 h. A terminal half-life of 27.5 + 25.0 h was measured. At 1 h after i.m. injection, 75% of the diminazene in whole blood was in the plasma fraction. The results of this study indicate that diminazene is rapidly distributed and sequestered into the liver, followed by a slower terminal phase during which diminazene is both redistributed to the peripheral tissues and/or renally excreted. It is recommended that diminazene administered i.m. at 4.2 mg/kg should not be repeated within a 21-day period. |
topic |
Babesia Canis Babesiosis Berenil Canine Diminazene Liver Sequestration Pharmacokinetics Pharmacology |
url |
https://jsava.co.za/index.php/jsava/article/view/416 |
work_keys_str_mv |
AT dmmiller thepharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT geswan thepharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT rglobetti thepharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT lsjacobson thepharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT dmmiller pharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT geswan pharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT rglobetti pharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs AT lsjacobson pharmacokineticsofdiminazeneaceturateafterintramuscularadministrationinhealthydogs |
_version_ |
1725566862347993088 |