Pharmacokinetics and penetration of danofloxacin from the blood into the milk of cows

Shem-Tov, M.; Rav-Hon, O.; Gil, Ziv; Lavi, Ehud; Glickman, A.; Saran, A.

doi:10.1046/j.1365-2885.1998.00137.x

Cited by 40 publications

(55 citation statements)

References 19 publications

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“…In the case of levels and pharmacokinetic parameters in milk ( Fig. 2; Table 1), our data are in agreement with those previously published by Shem-Tov et al (1998), but only for Y/Y homozygous cows. Levels in the milk of Y/S heterozygous animals were significantly higher when compared with Y/Y homozygous animals at 5 and 11 hours (Fig.…”

Section: Resultssupporting

confidence: 93%

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The Bovine ATP-Binding Cassette Transporter ABCG2 Tyr581Ser Single-Nucleotide Polymorphism Increases Milk Secretion of the Fluoroquinolone Danofloxacin

et al. 2012

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The bovine adenosine triphosphate-binding cassette transporter G2 (ABCG2/breast cancer resistance protein) polymorphism Tyr581Ser (Y581S) has recently been shown to increase in vitro transepithelial transport of antibiotics. Since this transporter has been extensively related to the active secretion of drugs into milk, the potential in vivo effect of this polymorphism on secretion of xenobiotics in livestock could have striking consequences for milk production, the dairy industry, and public health. Our purpose was to study the in vivo effect of this polymorphism on the secretion of danofloxacin, a widely used veterinary antibiotic, into milk. Danofloxacin (1.25 mg/kg) was administered to six Y/Y 581 homozygous and six Y/S 581 heterozygous lactating cows, and plasma and milk samples were collected and analyzed by high-performance liquid chromatography. No differences were found in the pharmacokinetic parameters of danofloxacin in plasma between the two groups of animals. In contrast, Y/S heterozygous cows showed a 2-fold increase in danofloxacin levels in milk. In addition, the pharmacokinetic elimination parameters, mean residence time and elimination half-life, were significantly lower in the milk of the animals carrying the Y/S polymorphism. These in vivo results are in agreement with our previously published in vitro data, which showed a greater capacity of the S581 variant in accumulation assays, and demonstrate, for the first time, an important effect of the Y581S single-nucleotide polymorphism on antibiotic secretion into cow milk. These findings could be extended to other ABCG2 substrates, and may be relevant for the treatment of mastitis and for the design of accurate and novel strategies to handle milk residues. IntroductionThe ATP-binding cassette (ABC) transporter ABCG2 (breast cancer resistance protein) is expressed in a wide range of tissues and organs, including the intestine, liver, blood-brain barrier, and mammary gland (van Herwaarden and Schinkel, 2006). It affects the bioavailability of its substrates and mediates the active secretion of xenobiotics and several vitamins in milk (van Herwaarden et al., 2007). The occurrence of drug residues in milk could lead to the development of bacterial resistance, allergies, or hypersensitivity reactions in consumers (McManaman and Neville, 2003). On the other hand, effective treatments for mastitis may require a considerable transfer of drugs into milk (Escudero et al., 2007). All of these issues are of great concern for general public health, the dairy industry, and veterinary therapeutics. Hence, identification of relevant factors for the transfer of drugs into milk in livestock constitutes a priority.Changes in the expression and/or the function of ABCG2 can lead to dramatic variations in the pharmacokinetics and secretion of its substrates into milk Ni et al., 2010). Several single-nucleotide polymorphisms (SNPs) have been studied in human ABCG2, and of these, Gln141Lys (Q141K) is one of the most important, causing impaired urate transport wh...

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Section: Resultssupporting

confidence: 93%

“…Plasma levels ( Fig. 1) and plasma pharmacokinetic parameters (Table 1) obtained for both groups of animals were very similar to those obtained by Shem-Tov et al (1998) and Shojaee Aliabadi and Lees (2003). Our results showed no significant differences according to the genotype.…”

Section: Resultssupporting

confidence: 86%

The Bovine ATP-Binding Cassette Transporter ABCG2 Tyr581Ser Single-Nucleotide Polymorphism Increases Milk Secretion of the Fluoroquinolone Danofloxacin

et al. 2012

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“…18) (Shem-Tov et al, 1998). Although, there are no references for DAF MIC against S. aureus, it has been proved that enrofloxacin MIC is ≥1 µg.mL -1 (Cester et al, 1992).…”

Section: Danofloxacinmentioning

confidence: 99%

Pharmacokinetic – Pharmacodynamic Considerations for Bovine Mastitis Treatment

Mestorino¹,

Errecalde²

2012

A Bird's-Eye View of Veterinary Medicine

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“…Combination of anti microbial agents for treating infections due to S. aureus used to increase the antibacterial activity and to prevent the emergence of drug resistance 24 . The cefoperazone and danofloxacin antibacterials were selected at t h e present study by their pharmacokinetic and pharmacodynamic characteristics [25][26][27] . Economical considerations require the best possible cure should obtain with the shortest possible withdrawal period as a result the milk can be marketed again as soon as possible 2,18,22 .…”

Section: 23mentioning

confidence: 99%

Sütçü İneklerde S. aureus’un Neden Olduğu Subklinik Mastitisin Sağaltımında Sefoperazon - Danofloksasin Kombinasyonunun Etkinliği

Sekkin¹,

Kum²,

Kırkan³

et al. 2009

Kafkas Univ Vet Fak Derg

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Makale Kodu (Article Code): KVFD-2009-501 SummaryWe report on the effectiveness and profitability of a single-dose intramammary administration of cefoperazone and danofloxacin combination (CDC) against subclinical mastitis in lactating cows. The CDC proved to be effective against Staphylococcus aureus (S. aureus), in vitro checkerboard trials. The presence of mastitis examined on the 892 mammary quarters of 223 lactating cows by bacterial cultures and microscopic somatic cell counting (SCC). Selecting the subjects at random from the 223 animals, twenty-two cows (32 quarters) used for treatment and eleven cows (15 quarters) as controls. Milk samples received one week before the start of treatment and on days 0, 14, 21 and 28 of the experiment. Bacteriological cure examined to the treated quarters. Bacteriological cure defined as no signs of S. aureus after treatment of quarters previously confirmed as infected. The SCC remained unchanged 4 weeks after treatment started, but quarters that were cured (spontaneously or by CDC) showed significant differences on days 21 and 28 (P<0.05). There was no S. aureus in 53.1% of the treated quarters with intramammary CDC, while in the controls there was spontaneous cure of the infection in 13.3% of the untreated quarters with significant (P<0.05) difference. These preliminary results suggest the intramammary application of CDC is an effective and profitable therapy in treating S. aureus infection resulting in subclinical mastitis in lactating cows..

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Pharmacokinetics and penetration of danofloxacin from the blood into the milk of cows

Cited by 40 publications

References 19 publications

The Bovine ATP-Binding Cassette Transporter ABCG2 Tyr581Ser Single-Nucleotide Polymorphism Increases Milk Secretion of the Fluoroquinolone Danofloxacin

The Bovine ATP-Binding Cassette Transporter ABCG2 Tyr581Ser Single-Nucleotide Polymorphism Increases Milk Secretion of the Fluoroquinolone Danofloxacin

Pharmacokinetic – Pharmacodynamic Considerations for Bovine Mastitis Treatment

Sütçü İneklerde S. aureus’un Neden Olduğu Subklinik Mastitisin Sağaltımında Sefoperazon - Danofloksasin Kombinasyonunun Etkinliği

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