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Veterinary parasitology2010; 170(1-2); 120-126; doi: 10.1016/j.vetpar.2010.01.041

Comparative plasma disposition, bioavailability and efficacy of ivermectin following oral and pour-on administrations in horses.

Abstract: Pour-on formulations of endectocides decrease the risk of injury for both user and animal, and are particularly convenient for animal owners who can apply the product. This study was designed to investigate the plasma disposition and efficacy of ivermectin (IVM) following pour-on, per os and intravenous administrations. Eighteen female horses weighing 510-610 kg were used in this study. The animals were allocated into three groups (per os, pour-on and intravenous groups). The equine paste, bovine pour-on and bovine injectable formulations of IVM were administered orally, topically and intravenously at the dose rates of 0.2, 0.5 and 0.2mg/kg bodyweight, respectively. Heparinized blood samples and hair samples were collected at various times between 1h and 40 days. The samples were analysed by high performance liquid chromatography with fluorescence detector. Faecal strongyle egg counts (EPG) were performed by a modified McMaster's technique before and at weekly intervals during 10 weeks after treatment. The results indicated that the plasma concentration and systemic availability of IVM was lower but the plasma persistence was prolonged after pour-on administration compared with per os route. IVM (paste) reduced the EPG by >95% for 10 weeks, whereas the reduction in pour-on group varied from 82 to 97%. EPG reduction in pour-on group was lower than that of per os group. Degradation on the application site, cutaneous biotransformation, binding of IVM to the haircoat and/or sebum are probably responsible for the relatively lower bioavailability of IVM in horses after pour-on administration. In conclusion, the poor plasma availability observed after pour-on administration could result in subtherapeutic plasma concentrations, which may promote the development of drug resistance in parasites.
Publication Date: 2010-02-04 PubMed ID: 20181429DOI: 10.1016/j.vetpar.2010.01.041Google Scholar: Lookup
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  • Comparative Study
  • Journal Article

Summary

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The research evaluates the effectiveness of using pour-on, oral, and intravenous methods to administer the antiparasitic drug ivermectin in horses. It shows that the pour-on method leads to longer-lasting, but overall less absorption of the drug. This could contribute to parasite drug-resistance if the drug concentration in the horse’s system is not high enough to fully eliminate the parasites.

Research Design

  • This study involved eighteen female horses, each weighing between 510-610 kg. The horses were divided into three groups receiving ivermectin through three different methods – pour-on, oral (per os), and intravenous.
  • Depending on the groups they belonged to, the horses were administered doses of ivermectin paste, pour-on (designed for use in cattle), and injectable formulations at dose rates of 0.2, 0.5, and 0.2mg/kg bodyweight respectively.
  • Researchers collected heparinized blood and hair samples at various times ranging from 1 hour to 40 days post-treatment. These samples underwent analysis using high-performance liquid chromatography with a fluorescence detector.
  • The researchers also obtained fecal strongyle egg counts (EPG) using a modified McMaster’s technique before and at weekly intervals for 10 weeks post-treatment to assess the efficacy of the drug’s delivery method.

Findings and Implications

  • The results indicated that the skin-application (pour-on) method yielded lower plasma concentration and systemic availability of ivermectin, but provided prolonged plasma persistence compared to the oral administration method.
  • The oral administration method reduced the strongyle egg counts by over 95% for 10 weeks, while the pour-on method lead to reductions ranging from 82 to 97% with the pour-on group showing lower reduction levels than the per os group.
  • The lower bioavailability of ivermectin in horses after pour-on administration could be attributed to degradation at the application site, cutaneous biotransformation, or binding of the drug to the horse’s hair or sebum.
  • These results suggest that while pour-on administration is more convenient and lowers the risk of injury during treatment, it could lead to subtherapeutic plasma concentrations of the drug, potentially promoting the development of drug-resistant parasites.

Cite This Article

APA
Gokbulut C, Cirak VY, Senlik B, Aksit D, Durmaz M, McKellar QA. (2010). Comparative plasma disposition, bioavailability and efficacy of ivermectin following oral and pour-on administrations in horses. Vet Parasitol, 170(1-2), 120-126. https://doi.org/10.1016/j.vetpar.2010.01.041

Publication

ISSN: 1873-2550
NlmUniqueID: 7602745
Country: Netherlands
Language: English
Volume: 170
Issue: 1-2
Pages: 120-126

Researcher Affiliations

Gokbulut, Cengiz
  • Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Adnan Menderes University, Isikli Koyu, 09100 Aydin, Turkey. cengizgokbulut@yahoo.com
Cirak, Veli Y
    Senlik, Bayram
      Aksit, Dilek
        Durmaz, Murat
          McKellar, Quintin A

            MeSH Terms

            • Administration, Oral
            • Administration, Topical
            • Animals
            • Antiparasitic Agents / administration & dosage
            • Antiparasitic Agents / blood
            • Antiparasitic Agents / pharmacokinetics
            • Area Under Curve
            • Feces / parasitology
            • Female
            • Half-Life
            • Horse Diseases / drug therapy
            • Horse Diseases / parasitology
            • Horses
            • Injections, Intramuscular / veterinary
            • Ivermectin / administration & dosage
            • Ivermectin / blood
            • Ivermectin / pharmacokinetics
            • Parasite Egg Count / veterinary
            • Strongylida Infections / drug therapy
            • Strongylida Infections / parasitology
            • Strongylida Infections / veterinary
            • Strongylus / growth & development

            Citations

            This article has been cited 7 times.
            1. Onyeaka H, Tamasiga P, Agbara JO, Mokgwathi OA, Uwishema O. The use of Ivermectin for the treatment of COVID-19: Panacea or enigma?. Clin Epidemiol Glob Health 2022 Jul-Aug;16:101074.
              doi: 10.1016/j.cegh.2022.101074pubmed: 35694631google scholar: lookup
            2. Leathwick DM, Miller CM, Waghorn TS, Schwendel H, Lifschitz A. Route of administration influences the concentration of ivermectin reaching nematode parasites in the gastrointestinal tract of cattle.. Int J Parasitol Drugs Drug Resist 2020 Dec;14:152-158.
              doi: 10.1016/j.ijpddr.2020.10.006pubmed: 33120249google scholar: lookup
            3. Bazzano M, Di Salvo A, Diaferia M, Veronesi F, Galarini R, Paoletti F, Tesei B, McLean A, Veneziano V, Laus F. Anthelmintic Efficacy and Pharmacokinetics of Ivermectin Paste after Oral Administration in Mules Infected by Cyathostomins.. Animals (Basel) 2020 May 28;10(6).
              doi: 10.3390/ani10060934pubmed: 32481576google scholar: lookup
            4. Sharun K, Shyamkumar TS, Aneesha VA, Dhama K, Pawde AM, Pal A. Current therapeutic applications and pharmacokinetic modulations of ivermectin.. Vet World 2019 Aug;12(8):1204-1211.
            5. Murchie AK, Thompson GM, Clawson S, Brown A, Gordon AW, Jess S. Field Evaluation of Deltamethrin and Ivermectin Applications to Cattle on Culicoides Host-Alighting, Blood-Feeding, and Emergence.. Viruses 2019 Aug 8;11(8).
              doi: 10.3390/v11080731pubmed: 31398840google scholar: lookup
            6. Oksanen A, Åsbakk K, Raekallio M, Nieminen M. The relative plasma availabilities of ivermectin in reindeer (Rangifer tarandus tarandus) following subcutaneous and two different oral formulation applications.. Acta Vet Scand 2014 Nov 25;56(1):76.
              doi: 10.1186/s13028-014-0076-9pubmed: 25421461google scholar: lookup
            7. Pettengill MA, Lam VW, Ollawa I, Marques-da-Silva C, Ojcius DM. Ivermectin inhibits growth of Chlamydia trachomatis in epithelial cells.. PLoS One 2012;7(10):e48456.
              doi: 10.1371/journal.pone.0048456pubmed: 23119027google scholar: lookup