dc.contributor.author
Mencke, Norbert
dc.contributor.author
Bäumer, Wolfgang
dc.contributor.author
Fraatz, Kristine
dc.contributor.author
Krebber, Ralph
dc.contributor.author
Schneider, Marc
dc.contributor.author
Blazejak, Katrin
dc.date.accessioned
2024-03-14T08:09:59Z
dc.date.available
2024-03-14T08:09:59Z
dc.identifier.uri
https://refubium.fu-berlin.de/handle/fub188/42804
dc.identifier.uri
http://dx.doi.org/10.17169/refubium-42520
dc.description.abstract
Felpreva® for cats contains the new acaricidal/insecticidal active ingredient tigolaner in a fixed combination with the nematocidal and cestocidal compounds emodepside and praziquantel, respectively. The plasma pharmacokinetics of tigolaner, emodepside, and praziquantel were evaluated in clinically healthy cats following topical (spot-on) treatment as fixed combination Felpreva®. For the determination of bioavailability intravenous administration of single active ingredients was also performed. After a single topical administration of Felpreva® using the target dose volume of 0.148 ml/kg to cats, tigolaner reached mean peak concentrations of 1352 μg/l with a Tmax of 12 days and a mean half-life of 24 days. Simulation of repetitive topical administration every 91 days indicates only a low risk of accumulation after reaching steady state within two to three administrations. The volume of distribution calculated after intravenous dosing was 4 l/kg and plasma clearance was low with 0.005 l/h/kg. Overall plasma exposure was 1566 mg∗h/l after topical administration, providing an absolute bioavailability of 57%. Tigolaner was mainly cleared via the faeces (54% within 28 days), renal clearance was neglectable (< 0.5% within 28 days). Emodepside and praziquantel showed mean peak concentrations of 44 μg/l and 48 μg/l (reached after 1.5 days and 5 h, respectively). Overall plasma exposures were 20.6 and 3.69 mg∗h/l, respectively. The elimination half-life was 14.5 days for emodepside and 10 days for praziquantel after topical administration. After topical administration of Felpreva® using 2.5× and 5× dose multiples an almost proportional increase of plasma exposure was observed for all three active ingredients. With the addition of tigolaner, Felpreva® combines the established pharmacokinetic (PK) characteristics of emodepside and praziquantel contained in Profender® spot-on for cats with the favourable PK of tigolaner suitable for a 3-months protection against fleas and ticks.
en
dc.format.extent
8 Seiten
dc.rights.uri
https://creativecommons.org/licenses/by/4.0/
dc.subject
Praziquantel
en
dc.subject
Pharmacokinetics
en
dc.subject.ddc
600 Technik, Medizin, angewandte Wissenschaften::630 Landwirtschaft::630 Landwirtschaft und verwandte Bereiche
dc.title
Plasma pharmacokinetics of tigolaner, emodepside, and praziquantel following topical administration of a combination product (Felpreva®) and of intravenous administration of the individual active ingredients in cats
dc.type
Wissenschaftlicher Artikel
dcterms.bibliographicCitation.articlenumber
100126
dcterms.bibliographicCitation.doi
10.1016/j.crpvbd.2023.100126
dcterms.bibliographicCitation.journaltitle
Current Research in Parasitology & Vector-Borne Diseases
dcterms.bibliographicCitation.volume
4
dcterms.bibliographicCitation.url
https://doi.org/10.1016/j.crpvbd.2023.100126
refubium.affiliation
Veterinärmedizin
refubium.affiliation.other
Institut für Pharmakologie und Toxikologie

refubium.resourceType.isindependentpub
no
dcterms.accessRights.openaire
open access
dcterms.isPartOf.eissn
2667-114X
refubium.resourceType.provider
WoS-Alert