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Journal of veterinary pharmacology and therapeutics1999; 22(3); 174-180; doi: 10.1046/j.1365-2885.1999.00200.x

Comparison of the pharmacokinetics of moxidectin (Equest) and ivermectin (Eqvalan) in horses.

Abstract: A study was undertaken in order to evaluate and compare plasma disposition kinetic parameters of moxidectin and ivermectin after oral administration of their commercially available preparations in horses. Ten clinically healthy adult horses, weighing 390-446 kg body weight (b.w.), were allocated to two experimental groups of five horses. Group I was treated with an oral gel formulation of moxidectin (MXD) at the manufacturers recommended therapeutic dose of 0.4 mg/kg bw. Group II was treated with an oral paste formulation of ivermectin (IVM) at the manufacturers recommended dose of 0.2 mg/kg b.w. Blood samples were collected by jugular puncture at different times between 0.5 h and 75 days post-treatment. After plasma extraction and derivatization, samples were analysed by HPLC with fluorescence detection. Computerized kinetic analysis was carried out. The parent molecules were detected in plasma between 30 min and either 30 (IVM) or 75 (MXD) days post-treatment. Both drugs showed similar patterns of absorption and no significant difference was found for the time corresponding to peak plasma concentrations or for absorption half-life. Peak plasma concentrations (Cmax) of 70.3+/-10.7 ng/mL (mean +/- SD) were obtained for MXD and 44.0+/-23.1 ng/mL for IVM. Moreover, the values for area under concentration-time curve (AUC) were 363.6+/-66.0 ng x d/mL for the MXD treated group, and 132.7+/-47.3 ng x d/mL for the IVM treated group. The mean plasma residence times (MRT) were 18.4+/-4.4 and 4.8+/-0.6 days for MXD and IVM treated groups, respectively. The results showed a more prolonged residence of MXD in horses as demonstrated by a four-fold longer MRT than for IVM. The longer residence and the higher concentrations found for MXD in comparison to IVM could possibly explain a more prolonged anthelmintic effect. It is concluded that in horses the commercial preparation of MXD presents a pharmacokinetic profile which differs significantly from that found for a commercial preparation of IVM. To some extent these results likely reflect differences in formulation and doses.
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Publication Date: 1999-08-14 PubMed ID: 10447828DOI: 10.1046/j.1365-2885.1999.00200.xGoogle Scholar: Lookup
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Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research compares how the horse body responds to absorption, distribution, and excretion of two commercial drugs, moxidectin (MXD) and ivermectin (IVM), used as deworming medications. It reveals that moxidectin stays in the horses’ systems longer and at higher concentrations compared to ivermectin, which could suggest moxidectin’s potentially prolonged worm-fighting effects.

Experiment Setup

  • In the experiment, researchers studied 10 clinically healthy adult horses, separated into two equal groups.
  • One group received the standard dose of moxidectin adapted to their weight, whereas the other group was given a standard dose of ivermectin.
  • Horses’ blood samples were collected over time (from 0.5 hours to 75 days following administration). The samples were then processed and analyzed using High-Performance Liquid Chromatography with fluorescence detection.
  • The analysis’ main intent was to evaluate the pharmacokinetic characteristics of the two drugs, specifically the concentration over time and how long it remained in the horse’s system.

Pharmacokinetics Comparison

  • The plasma drug residues for both moxidectin and ivermectin were detected between 30 minutes and up to 30 days for ivermectin and 75 days for moxidectin post-treatment. This indicates that moxidectin stays in the horses’ system significantly longer.
  • The absorption pattern and speed were similar for both drugs, as indicated by peak plasma concentrations achieved and their absorption half-lives
  • Moxidectin reached higher peak concentrations and had much larger area under concentration-time curve (AUC) values, indicating a higher overall exposure to the drug.

Observations and Conclusions

  • The mean plasma residence times were significantly different in the two groups. Moxidectin had a residence time of about 18.4 days, four times longer than ivermectin, which had an average of 4.8 days.
  • The longer residence and higher concentrations of moxidectin could potentially explain a more extended anti-parasitic effect compared to ivermectin.
  • It was concluded that the commercial preparation of moxidectin presents a different pharmacokinetic profile than that of ivermectin, likely reflecting differences in the formulation and doses used.

Cite This Article

APA
Pérez R, Cabezas I, García M, Rubilar L, Sutra JF, Galtier P, Alvinerie M. (1999). Comparison of the pharmacokinetics of moxidectin (Equest) and ivermectin (Eqvalan) in horses. J Vet Pharmacol Ther, 22(3), 174-180. https://doi.org/10.1046/j.1365-2885.1999.00200.x

Publication

Journal of veterinary pharmacology and therapeutics
ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 22
Issue: 3
Pages: 174-180

Researcher Affiliations

Pérez, R
  • Laboratorio de Farmacología, Facultad Medicina Veterinaria, Universidad de Concepción, Chillán, Chile.
Cabezas, I
    García, M
      Rubilar, L
        Sutra, J F
          Galtier, P
            Alvinerie, M

              MeSH Terms

              • Administration, Oral
              • Animals
              • Anthelmintics / administration & dosage
              • Anthelmintics / blood
              • Anthelmintics / pharmacokinetics
              • Anti-Bacterial Agents / administration & dosage
              • Anti-Bacterial Agents / blood
              • Anti-Bacterial Agents / pharmacokinetics
              • Antiprotozoal Agents / administration & dosage
              • Antiprotozoal Agents / blood
              • Antiprotozoal Agents / pharmacokinetics
              • Area Under Curve
              • Chemistry, Pharmaceutical
              • Chromatography, High Pressure Liquid / veterinary
              • Horses / metabolism
              • Ivermectin / administration & dosage
              • Ivermectin / blood
              • Ivermectin / pharmacokinetics
              • Macrolides

              Citations

              This article has been cited 9 times.
              1. 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
              2. Prichard R, Ménez C, Lespine A. Moxidectin and the avermectins: Consanguinity but not identity. Int J Parasitol Drugs Drug Resist 2012 Dec;2:134-53.
                doi: 10.1016/j.ijpddr.2012.04.001pubmed: 24533275google scholar: lookup
              3. Cringoli G, Veneziano V, Mezzino L, Morgoglione M, Pennacchio S, Rinaldi L, Salamina V. The effect of moxidectin 0,1% vs ivermectin 0,08% on milk production in sheep naturally infected by gastrointestinal nematodes. BMC Vet Res 2009 Nov 12;5:41.
                doi: 10.1186/1746-6148-5-41pubmed: 19909507google scholar: lookup
              4. Cobb R, Boeckh A. Moxidectin: a review of chemistry, pharmacokinetics and use in horses. Parasit Vectors 2009 Sep 25;2 Suppl 2(Suppl 2):S5.
                doi: 10.1186/1756-3305-2-S2-S5pubmed: 19778466google scholar: lookup
              5. El-Banna HA, Goudah A, El-Zorba H, Abd-El-Rahman S. Comparative pharmacokinetics of ivermectin alone and a novel formulation of ivermectin and rafoxanide in calves and sheep. Parasitol Res 2008 May;102(6):1337-42.
                doi: 10.1007/s00436-008-0915-6pubmed: 18297309google scholar: lookup
              6. Ndong TB, Kane Y, Diouf EH, Alvinerie M. Ivermectin in senegalese peulh sheep: influence of sex on plasma disposition. Vet Res Commun 2007 Aug;31(6):739-47.
                doi: 10.1007/s11259-007-3522-6pubmed: 17260181google scholar: lookup
              7. Buono F, Veneziano V, Veronesi F, Molento MB. Horse and donkey parasitology: differences and analogies for a correct diagnostic and management of major helminth infections. Parasitology 2023 Oct;150(12):1119-1138.
                doi: 10.1017/S0031182023000525pubmed: 37221816google scholar: lookup
              8. Nielsen MK. Anthelmintic resistance in equine nematodes: Current status and emerging trends. Int J Parasitol Drugs Drug Resist 2022 Dec;20:76-88.
                doi: 10.1016/j.ijpddr.2022.10.005pubmed: 36342004google scholar: lookup
              9. Woerde DJ, Martin PA, Govendir M. Susceptibility of rapidly growing mycobacteria isolated from Australian cats to ivermectin, moxidectin, ceftiofur and florfenicol. J Feline Med Surg 2015 Dec;17(12):1065-8.
                doi: 10.1177/1098612X14565497pubmed: 25572306google scholar: lookup
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