Itrakonazol till häst
Itraconazole is a third generation azol, a fungicide which acts by inhibiting ergerosterol synthesis in the fungal cell membrane, and thereby disturbing fungal regeneration. It has proven to be less toxic, to have a broader spectrum of activity and to be more potent than its predecessor ketoconazol...
| Autor principal: | |
|---|---|
| Formato: | Otro |
| Lenguaje: | sueco sueco |
| Publicado: |
2005
|
| Materias: | |
| Acceso en línea: | https://stud.epsilon.slu.se/11526/ |
| _version_ | 1855571889431248896 |
|---|---|
| author | Sonesson, Eva |
| author_browse | Sonesson, Eva |
| author_facet | Sonesson, Eva |
| author_sort | Sonesson, Eva |
| collection | Epsilon Archive for Student Projects |
| description | Itraconazole is a third generation azol, a fungicide which acts by inhibiting ergerosterol synthesis in the fungal cell membrane, and thereby disturbing fungal regeneration. It has proven to be less toxic, to have a broader spectrum of activity and to be more potent than its predecessor ketoconazole. Itraconazole is only available in therapheutics approved for human use. Pharmacokinetic studies has been performed in humans, dogs, cats and laboratory animals. Although itraconazole has been used tentatively with good effect against fungal infections in horses, no pharmacokinetic studies have yet been done.
The aim of this pilot study was to get an indication if itraconazole from a pharmacokinetic point of view is a suitable therapeutic agent in equine mycosis. We wanted to make sure that the bioavailability for oral dosing seamed sufficient and that elimination half-life of itraconazol wasn´t too short for it to be used in a practical manner.
Two healthy horses were given itraconazole (5 mg/kg) intravenously and orally. Bloodsamples were collected for 71 hours and serum analyses of itraconazole were made by high performance liquid chromatography (HPLC). Pharmacokinetic parameters obtained in this study indicate that itraconazole, from a pharmacokinetic aspect, is suitable for treatment of equine mycosis, considering the long treatment often required. Bioavailability was 33 % (mean, n=2) which is sufficient for the drug to be given orally. Terminal half-life after intravenous administration was 50h (mean, n=2) and therefore drug administration once daily would be adequate. Mean value (n=2) of volume of distrubution was 7 l/kg and of clearence 0,11/kg·h. This seems promising and an extended study including a greater number of horses should be performed to optimize dose regimen in horses. |
| format | Otro |
| id | RepoSLU11526 |
| institution | Swedish University of Agricultural Sciences |
| language | Swedish swe |
| publishDate | 2005 |
| publishDateSort | 2005 |
| record_format | eprints |
| spelling | RepoSLU115262017-10-03T10:50:53Z https://stud.epsilon.slu.se/11526/ Itrakonazol till häst Sonesson, Eva Veterinary science and hygiene - General aspects Faculty of Veterinary Medicine and Animal Science Itraconazole is a third generation azol, a fungicide which acts by inhibiting ergerosterol synthesis in the fungal cell membrane, and thereby disturbing fungal regeneration. It has proven to be less toxic, to have a broader spectrum of activity and to be more potent than its predecessor ketoconazole. Itraconazole is only available in therapheutics approved for human use. Pharmacokinetic studies has been performed in humans, dogs, cats and laboratory animals. Although itraconazole has been used tentatively with good effect against fungal infections in horses, no pharmacokinetic studies have yet been done. The aim of this pilot study was to get an indication if itraconazole from a pharmacokinetic point of view is a suitable therapeutic agent in equine mycosis. We wanted to make sure that the bioavailability for oral dosing seamed sufficient and that elimination half-life of itraconazol wasn´t too short for it to be used in a practical manner. Two healthy horses were given itraconazole (5 mg/kg) intravenously and orally. Bloodsamples were collected for 71 hours and serum analyses of itraconazole were made by high performance liquid chromatography (HPLC). Pharmacokinetic parameters obtained in this study indicate that itraconazole, from a pharmacokinetic aspect, is suitable for treatment of equine mycosis, considering the long treatment often required. Bioavailability was 33 % (mean, n=2) which is sufficient for the drug to be given orally. Terminal half-life after intravenous administration was 50h (mean, n=2) and therefore drug administration once daily would be adequate. Mean value (n=2) of volume of distrubution was 7 l/kg and of clearence 0,11/kg·h. This seems promising and an extended study including a greater number of horses should be performed to optimize dose regimen in horses. Itrakonazol är en tredje generationens azol. En fungicid som verkar genom att inhibera ergosterolsyntesen i svampcellens membran och därigenom störa svampens reproduktion. Den har visat sig vara mer potent, ha ett bredare spektrum och vara mindre toxisk än sin föregångare ketokonazol. Itrakonazol finns för närvarande endast i läkemedel godkända för människa. Farmakokinetiska studier har gjorts på människa, hund, katt och små försöksdjur. Även om itrakonazol med viss framgång försöksvis har använts mot svampinfektioner på häst, har hittills inga farmakokinetiska studier gjorts på detta djurslag. Syftet med denna pilotstudie var att få en indikation om itrakonazol, ur en farmakokinetisk synvinkel, är ett lämpligt läkemedel mot mykoser på häst. Vi ville se om biotillgängligheten för oral dosering var tillräckligt hög och om halveringstiden för itrakonazol var tillräckligt lång för att substansen skulle kunna användas rent praktiskt. Två friska hästar gavs itrakonazol (5 mg/kg) intravenöst och oralt. Blodprover togs upp till 71h efter tillförseln, varefter itrakonazol i serum analyserades med hjälp av high performance liquid chromatography (HPLC). De farmakokinetiska parametrar som erhölls i studien indikerar att itrakonazol är lämplig för behandling av mykoser hos häst. Distributionsvolymen var 7 l/kg för båda hästarna och clearence var i snitt 0,11 l/kg·h (n=2). Halveringstiden vid intravenös giva var i snitt 50 timmar och biotillgängligheten vid oral giva var i snitt 33 % (n=2). Dessa resultat visar troligtvis att det är lämpligt att ge itrakonazol oralt till häst och att dosering endast behöver ske en gång per dygn, vilket är önskvärt med tanke på den långa behandlingstid som ofta krävs vid en svampinfektion. Detta verkar lovande inför framtiden och en utökad studie över en längre tid och med fler hästar borde företas för att optimera dosering. 2005-01-17 Other NonPeerReviewed application/pdf sv https://stud.epsilon.slu.se/11526/1/sonesson_e_171003.pdf Sonesson, Eva, 2005. Itrakonazol till häst : en farmakokinetisk möjlighet?. UNSPECIFIED, Uppsala. Uppsala: (VH) > Dept. of Biomedical Sciences and Veterinary Public Health (until 231231) <https://stud.epsilon.slu.se/view/divisions/OID-713.html> urn:nbn:se:slu:epsilon-s-7442 swe |
| spellingShingle | Veterinary science and hygiene - General aspects Faculty of Veterinary Medicine and Animal Science Sonesson, Eva Itrakonazol till häst |
| title | Itrakonazol till häst |
| title_full | Itrakonazol till häst |
| title_fullStr | Itrakonazol till häst |
| title_full_unstemmed | Itrakonazol till häst |
| title_short | Itrakonazol till häst |
| title_sort | itrakonazol till häst |
| topic | Veterinary science and hygiene - General aspects Faculty of Veterinary Medicine and Animal Science |
| url | https://stud.epsilon.slu.se/11526/ https://stud.epsilon.slu.se/11526/ |