Investigation of plasma concentrations after topical administration selamectin in sheep and goats

Selamektinin koyun ve keçilerde etiket d ı ş ı kullan ı lmas ı n ı takiben plazma konsantrasyonu vefarmakokinetik parametrelerinin belirlenmesi amac ı yla yap ı lan bu çal ı ş mada 1 ya ş ı nda di ş i 12 adetkoyun ile 12 adet keçi kullan ı lm ı ş tı r. Her iki gruba tek doz 12 mg/kg selamektin (Stronghold® %12240 mg) topikal olarak uygulanm ı ş tı r. 35 günlük süre boyunca farkl ı aral ı klarla kan örnekleri al ı nm ı şve gerekli analizler yap ı lm ı ş tı r. Selamektinin plazma konsantrasyonu yüksek bas ı nçl ı s ı v ıkromotografisiyle ölçülmü ş tür (HPLC). Analizler sonucunda ortalama plazma konsantrasyonu,plazma maksimum konsantrasyon (Cmax), e ğ ri altı nda kalan alan (AUC), ortalama kal ı ş süresi(MRT) ve plazma maksimum konsantrasyona ula ş ma süresi (Tmax) koyunlarda s ı ras ı yla1427.27±90.52 pg/mL, 4.78±0.61 ng/mL, 810.35±115.95 ng.saat/mL, 10.86±0.89 gün ve 72 saat;keçilerde ise 1195.03±70.81 pg/mL; 3.27±0.52 ng/mL, 664.42±72.62 ng.saat/mL, 10.46±0.74 günve 72 saat olarak belirlenmi ş tir. Sonuç olarak, selamektinin koyun ve keçilere topikal olarakuygulanmas ı halinde plazma konsantrasyon düzeyi, Cmax ve AUC de ğ erlerinin koyunlarda keçileregöre daha yüksek bulundu ğ u (P0.05) tespit edilmi ş tir.

Topikal Selamektin uygulaması sonrası koyun ve keçilerde plazma konsantrasyonlarının araştırılması

The objective of this study was to investigate of plasma concentration and pharmacokineticparameters after off-label use of selamectin. One years of ago, 12 ewes and 12 female goats wereused in this study. In both groups, a single dose of 12 mg/kg selamectin (Stronghold® 12% 240mg) was administered topically. During the 35 days following administration, blood samples weretaken with different intervals and required analyzes were conducted. Plasma concentrations ofselamectin were analysed by high performance liquid chromatography (HPLC). As a result ofanalyzes, for sheep mean plasma concentration, maximum plasma concentration (Cmax), the areaunder the concentration-time curve (AUC), the mean residence time (MRT) and time to reach peakconcentration (Tmax) values determined as 1427.27±90.52 pg/mL, 4.78±0.61 ng/mL, 810.35±115.95ng.h/mL, 10.86±0.89 days and 72 hours, respectively and for goats these values were determinedas 1195.03±70.81 pg/mL, 3.27±0.52 ng/mL, 664.42±72.62 ng.h/mL, 10.46±0.74 days and 72hours, respectively. As a result, plasma concentration, Cmax and AUC values were found higher insheep compared to goats (P0.05) using selamectin topically in sheep and goats.

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1. Dupuy J, Derlon AL, Sutra JF, et al. Pharmacokinetics of selamectin in dogs after topical application. Vet Res Commun 2004; 28: 407-413.
2. Gokbulut C, Bilgili A, Hanedan B, et al. Sex-related plasma disposition of ivermectin following pour-on administration in goats. Vet Parasitol 2009; 162: 342-345.
3. Novotony MJ, Krautmann MJ, Ehrhart JC, et al. Safety of selamectin in dogs. Vet Parasitol 2000; 91: 377-391.
4. Bishop BF, Bruce CI, Evans NA, et al. Selamectin: A novel broad-spectrum endectocide for dogs and cats. Vet Parasitol 2000; 91: 163-176.
5. Benchaoui HA, Clemence RG, Clements PJM, et al. Efficacy and safety of selamectin against fleas on dogs and cats presented as veterinary patients in Europe. Vet Parasitol 2000; 91: 223-232.
6. Maggie AF, David J. A review of the off-label use of selamectin (stronghold®/ revolution®) in dogs and cats. Acta Vet Scand 2008; 50: 46.
7. McTier TL, Jones RL, Holbert MS, et al. Efficacy of selamectin against adult flea infestations (ctenocephalides felis felis and ctenocephalides canis) on dogs and cats. Vet Parasitol 2000; 91: 187-199.
8. Lo PKA, Fink DW, Williams JB, Blodinger J. Pharmacokinetic studies of ivermectin effects of formulation. Vet Res Commun 1985; 9: 251-268.
9. McKellar QA, Benchaoui HA. Avermectins and milbemycins. J Vet Pharmacol Ther 1996; 19: 331-351.
10. Mugford CA, Kedderis GL. Sex-dependent metabolism of xenobiotics. Drug Metab Rev 1998; 30: 441-498.
11. Bassissi MF, Alvinerie M, Lespine A. Macrocyclic lactones: distribution in plasma lipoproteins of several animal species including humans. Comp Biochem Phys C 2004; 138: 437- 444.
12. Sutra JF, Cadiergues MC, Dupuy J, Franc M, Alvinerie M. Determination of selamectin in dog plasma by high performance liquid chromatography with automated solid phase extraction and fluorescence detection. Vet Res 2001; 32: 455-461.
13. Walker DK, Fenner KS. A sensitive method for the measurement of the novel pet endectocide, selamectin (UK-124,114), in dog and cat plasma by chemical derivatisation and high-performance liquid chromatography with fluorescence detection. J Pharmaceut Biomed 2000; 24: 105-111.
14. Pillai U, Harran L, Blackwell D, Updike L. Toxicokinetics of selamectin in rats and dogs. In: Soback S, McKellar Q. (Editors). Proceeding of the 8 th International Congress of the European Association for Veterinary Pharmacology and Toxicology (EAVPT). J Vet Pharmacol Ther 2000; 23(1).
15. Sarasola P, Jernigan AD, Walker DK, et al. Pharmacokinetics of selamectin following intravenous, oral and topical administration in cats and dogs. J Vet Pharmacol Ther 2002; 25: 265-272.
16. Alvinerie M, Lacoste E, Sutra JF, Chartier C. Some pharmacokinetic parameters of eprinomectin in goats following pour-on administration. Vet Res Commun 1999; 23: 449-455.
17. Alvinerie M, Sutra JF, Cabezas I, Rubilar L, Perez R. Enhanced plasma availability of moxidectin in fasted horses. J Equine Vet Sci 2000; 20: 575-578.
18. Atta AH, Abo-Sh ı hada MN. Comparative pharmacokinetics of doramectin and ivermectin in sheep. J Vet Pharmacol Ther 2000; 23: 49-52.
19. Craven J, Bjorn H, Hennessy DR, Friis C, Nansen P. Pharmacokinetics of moxidectin and ivermectin following intravenous in pigs with different body compositions. J Vet Pharmacol Ther 2001; 24: 99-104.
20. Escudero E, Carceles CM, Diaz MS, et al. Pharmacokinetics of moxidectin and doramectin in goats. Res Vet Sci 1999; 67: 175-179.
21. Nowakowski MA, Lynch MJ, Smith DG, et al. Pharmacokinetic and bio-equivalence of parenterally administered doramectin cattle. J Vet Pharmacol Ther 1995; 18: 290-298.
22. Wilkinson PK, Pope DG, Baylis FP. Pharmacokinetics of ivermectin administered intravenously to cattle. J Pharm Sci 1985; 75: 1105-1107.