Ronaghinia Amir Atabak, Birch Julie Melsted, Frandsen Henrik Lauritz, Toutain Pierre-Louis, Damborg Peter, Struve Tina
Department of Veterinary and Animal Sciences, University of Copenhagen, Stigbøjlen 4, 1870, Frederiksberg C, Denmark.
Kopenhagen Diagnostics, Department of Health and Diagnostics, Kopenhagen Fur a.m.b.a., Langagervej 60, 2600, Glostrup, Denmark.
Vet Res. 2021 Feb 27;52(1):34. doi: 10.1186/s13567-021-00906-0.
Staphylococcus delphini is one of the most common pathogens isolated from mink infections, especially dermatitis. Tylosin (TYL) is used frequently against these infections, although no evidence-based treatment regimen exists. This study aimed to explore the dosage of TYL for infections caused by S. delphini in mink. Two animal experiments with a total of 12 minks were conducted to study the serum pharmacokinetic (PK) characteristics of TYL in mink after 10 mg/kg IV and oral dosing, respectively. The concentration of TYL in serum samples collected before and eight times during 24 h after TYL administration was quantitated with liquid chromatography quadrupole time-of-flight mass spectrometry, and the TYL disposition was analyzed using non-linear mixed effect analysis. The pharmacodynamics (PD) of TYL against S. delphini were studied using semi-mechanistic modeling of in vitro time-kill experiments. PKPD modeling and simulation were done to establish the PKPD index and dosage regimen. The disposition of TYL was described by a two-compartmental model. The area under the free concentration-time curve of TYL over the minimum inhibitory concentration of S. delphini (fAUC/MIC) was determined as PKPD index with breakpoints of 48.9 and 98.7 h for bacteriostatic and bactericidal effect, respectively. The calculated daily oral dose of TYL was 2378 mg/kg, which is 238-fold higher than the currently used TYL oral dosage regimen in mink (10 mg/kg). Accordingly, sufficient TYL concentrations are impossible to achieve in mink plasma, and use of this drug for extra-intestinal infections in this animal species must be discouraged.
海豚葡萄球菌是从水貂感染尤其是皮炎中分离出的最常见病原体之一。泰乐菌素(TYL)经常用于对抗这些感染,尽管尚无循证治疗方案。本研究旨在探索TYL用于水貂海豚葡萄球菌感染的剂量。进行了两项动物实验,共12只水貂,分别研究了10mg/kg静脉注射和口服给药后TYL在水貂体内的血清药代动力学(PK)特征。在TYL给药前及给药后24小时内8次采集的血清样本中TYL浓度,采用液相色谱四极杆飞行时间质谱法定量,并使用非线性混合效应分析来分析TYL的处置情况。利用体外时间杀菌实验的半机制模型研究了TYL对海豚葡萄球菌的药效学(PD)。进行PKPD建模和模拟以建立PKPD指数和给药方案。TYL的处置情况用二室模型描述。将TYL游离浓度-时间曲线下面积与海豚葡萄球菌最低抑菌浓度的比值(fAUC/MIC)确定为PKPD指数,抑菌和杀菌作用的断点分别为48.9和98.7小时。计算得出的TYL每日口服剂量为2378mg/kg,比目前水貂使用的TYL口服给药方案(10mg/kg)高238倍。因此,在水貂血浆中不可能达到足够的TYL浓度,必须不鼓励在该动物物种中使用这种药物治疗肠道外感染。