Enhancement of moxidectin bioavailability in lamb by a natural flavonoid: quercetin.

@article{Dupuy2003EnhancementOM,
  title={Enhancement of moxidectin bioavailability in lamb by a natural flavonoid: quercetin.},
  author={Jacques Dupuy and G. Larrieu and Jean François Sutra and Anne Lespine and Michel Alvinerie},
  journal={Veterinary parasitology},
  year={2003},
  volume={112 4},
  pages={
          337-47
        }
}
Influence of verapamil on the pharmacokinetics of the antiparasitic drugs ivermectin and moxidectin in sheep
TLDR
A significant alteration in the plasma disposition of ivermectin in sheep induced by verapamil may have an important impact on efficacy against resistant- or rate-limiting-parasites and on the persistency of its antiparasitic activity.
Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition.
TLDR
An ITZ-induced reduction on the P-gp efflux activity at the intestinal lining may have accounted for the greater absorption and enhanced systemic availability observed for IVM in the intraruminally treated animals.
Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration
TLDR
It is suggested that lipid administration increases the systemic availability of oral moxidectin by enhancing the extent of intestinal lymphatic transport of the drug, and lipid-based formulations should improve the bioavailability of moxIDectin in rabbits.
MODULATION OF THE P-GLYCOPROTEIN-MEDIATED INTESTINAL SECRETION OF IVERMECTIN: IN VITRO AND IN VIVO ASSESSMENTS
TLDR
The results obtained in the current work confirm the relevance of P-gp-mediated transport to the intestinal secretion of ivermectin (IVM), an antiparasitic widely used in human and veterinary medicine.
Loperamide modifies the tissue disposition kinetics of ivermectin in rats
TLDR
The delayed intestinal transit time caused by LPM accounting for an extended plasma–intestine recycling time, and a potential competition between IVM and LPM for the P‐GP‐mediated bile–intestinal secretion processes, may account for the enhanced IVM systemic availability reported in the current study.
Fumagillin, a new P-glycoprotein-interfering agent able to modulate moxidectin efflux in rat hepatocytes.
TLDR
Fumagillin interacts with P-gp function and appears as a promising compound among registered drugs available, which may optimize the therapeutic use of macrocyclic lactones (MLs) in rat hepatocytes.
Quercetin nanoparticles alter pharmacokinetics of bromocriptine, reflecting its enhanced inhibitory action on liver and intestinal CYP 3A enzymes in rats
TLDR
In vivo study revealed that the increased levels of Cmax and AUC were comparatively high in NQC pretreated group than quercetin group, which might be result in higher plasma levels of quERCetin that could inhibit the CYP3A enzyme and enhanced the bioavailability of BRO.
Influence of quercetin on Ochratoxin A toxicokinetics and toxicity in F344 rats
TLDR
It is concluded, that in respect of OTA toxicokinetics in vivo the competitive inhibition of intestinal resecretion and renal tubular secretion by quercetin and OTA, as shown in vitro, was overcome by the upregulation of intestinal and renal efflux transporters and that quercETin was able to diminish OTA-induced pro-oxidative effects on molecular level.
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References

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TLDR
The implication of Pgp in the transport of MOX is demonstrated and prediction of the drug-drug interactions which might modify the bioavailability of endectocides is allowed.
Moxidectin in cattle: correlation between plasma and target tissues disposition.
TLDR
The disposition kinetics of moxidectin (MXD) in plasma and in different target tissues following its subcutaneous administration to cattle are evaluated to contribute to an understanding of the relationship between the kinetic behaviour and the persistence of the antiparasite activity of MXD against different ecto-endoparasites in cattle.
Moxidectin: Absorption, Tissue Distribution, Excretion, and Biotransformation of 14C-Labeled Moxidectin in Sheep
The absorption, tissue distribution, excretion, and biotransformation of moxidectin, a novel endectocide that combats internal and external parasites in sheep, cattle, and horse, were studied in
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TLDR
This hypothesis is consistent with other studies describing verapamil as a blocking agent of P-glycoprotein involved in the efflux of ivermectin in a resistant strain of Haemonchus contortus.
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TLDR
To determine which human cytochrome P450 isoform(s) is responsible for the metabolism of ivermectin, chemical inhibitors including sulphaphenazole, quinidine, furafylline, troleandomycin (TAO) and diethyldithiocarbamate (DDC) were used to evaluate their effect on iverMectin metabolism.
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TLDR
In the low feed intake group the digesta flow was slower than in sheep on high feed intake, which resulted in an extended residence time and greater availability of IVM and its metabolites.
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TLDR
In vivo metabolism of moxidectin was studied in cattle, sheep, and rats with larger quantities of in vitro metabolites prepared from liver microsomal incubations, and in vitro and in vivo metabolites were characterized first by liquid chromatography/mass spectrometry to generate molecular weight information on the unknown metabolites.
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