Anne Ravix MSc, Verena Gotta PhD, Marc Pfister PhD, Christoph Berger PhD, Antonia Glauser PhD, Paolo Paioni MD, Chantal Csajka PhD, Monia Guidi PhD
{"title":"阿莫西林在儿童莱姆病治疗中的剂量评价与优化。","authors":"Anne Ravix MSc, Verena Gotta PhD, Marc Pfister PhD, Christoph Berger PhD, Antonia Glauser PhD, Paolo Paioni MD, Chantal Csajka PhD, Monia Guidi PhD","doi":"10.1002/jcph.6190","DOIUrl":null,"url":null,"abstract":"<p>Amoxicillin is commonly used to treat erythema migrans in the first stage of Lyme disease in children, with a recommended dose of 50 mg/kg/day, administered three times a day (q8h). This model-based simulation study aimed to determine whether splitting the same daily dose into two administrations (q12h) would provide comparable drug exposure. A pharmacokinetic model suitable for a pediatric population (age: 1 month to 18 years, weight: 4-80 kg) was selected through a literature review. Simulations were performed with 15,000 virtual patients receiving 16.67 mg/kg/dose q8h, 25 mg/kg/dose q12h, or other q12h dosing variations. The target therapeutic level was defined by the percentage of time that the unbound drug concentration remained above the minimum inhibitory concentration (% fT > MIC) specific to <i>Borrelia burgdorferi</i>, with MICs of 0.06, 0.25, 1, 2, and 4 mg/L, requiring at least 40% and 50% of time for effective treatment. Probability of target attainment (PTA) was considered acceptable if it exceeded 50%, allowing for comparison of dosing schedules. Results indicated that the 50 mg/kg/day divided q12h regimen provided similar drug exposure to the q8h regimen for MICs below 2 mg/L (PTAs >50%). For a MIC of 2 mg/L, PTA was achieved with a higher dose of 30 mg/kg/dose q12h. However, for a MIC of 4 mg/L, the PTA criterion was not met. These findings suggest that a twice-daily dosing of 25 mg/kg/dose provides comparable bactericidal activity to the thrice-daily regimen for MICs between 0.06 and 1 mg/L. This simplified regimen may improve adherence and treatment implementation in children.</p>","PeriodicalId":22751,"journal":{"name":"The Journal of Clinical Pharmacology","volume":"65 6","pages":"742-750"},"PeriodicalIF":0.0000,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Dose Evaluation and Optimization of Amoxicillin in Children Treated for Lyme Disease\",\"authors\":\"Anne Ravix MSc, Verena Gotta PhD, Marc Pfister PhD, Christoph Berger PhD, Antonia Glauser PhD, Paolo Paioni MD, Chantal Csajka PhD, Monia Guidi PhD\",\"doi\":\"10.1002/jcph.6190\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>Amoxicillin is commonly used to treat erythema migrans in the first stage of Lyme disease in children, with a recommended dose of 50 mg/kg/day, administered three times a day (q8h). This model-based simulation study aimed to determine whether splitting the same daily dose into two administrations (q12h) would provide comparable drug exposure. A pharmacokinetic model suitable for a pediatric population (age: 1 month to 18 years, weight: 4-80 kg) was selected through a literature review. Simulations were performed with 15,000 virtual patients receiving 16.67 mg/kg/dose q8h, 25 mg/kg/dose q12h, or other q12h dosing variations. The target therapeutic level was defined by the percentage of time that the unbound drug concentration remained above the minimum inhibitory concentration (% fT > MIC) specific to <i>Borrelia burgdorferi</i>, with MICs of 0.06, 0.25, 1, 2, and 4 mg/L, requiring at least 40% and 50% of time for effective treatment. Probability of target attainment (PTA) was considered acceptable if it exceeded 50%, allowing for comparison of dosing schedules. Results indicated that the 50 mg/kg/day divided q12h regimen provided similar drug exposure to the q8h regimen for MICs below 2 mg/L (PTAs >50%). For a MIC of 2 mg/L, PTA was achieved with a higher dose of 30 mg/kg/dose q12h. However, for a MIC of 4 mg/L, the PTA criterion was not met. These findings suggest that a twice-daily dosing of 25 mg/kg/dose provides comparable bactericidal activity to the thrice-daily regimen for MICs between 0.06 and 1 mg/L. This simplified regimen may improve adherence and treatment implementation in children.</p>\",\"PeriodicalId\":22751,\"journal\":{\"name\":\"The Journal of Clinical Pharmacology\",\"volume\":\"65 6\",\"pages\":\"742-750\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2025-01-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"The Journal of Clinical Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/jcph.6190\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"The Journal of Clinical Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/jcph.6190","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Dose Evaluation and Optimization of Amoxicillin in Children Treated for Lyme Disease
Amoxicillin is commonly used to treat erythema migrans in the first stage of Lyme disease in children, with a recommended dose of 50 mg/kg/day, administered three times a day (q8h). This model-based simulation study aimed to determine whether splitting the same daily dose into two administrations (q12h) would provide comparable drug exposure. A pharmacokinetic model suitable for a pediatric population (age: 1 month to 18 years, weight: 4-80 kg) was selected through a literature review. Simulations were performed with 15,000 virtual patients receiving 16.67 mg/kg/dose q8h, 25 mg/kg/dose q12h, or other q12h dosing variations. The target therapeutic level was defined by the percentage of time that the unbound drug concentration remained above the minimum inhibitory concentration (% fT > MIC) specific to Borrelia burgdorferi, with MICs of 0.06, 0.25, 1, 2, and 4 mg/L, requiring at least 40% and 50% of time for effective treatment. Probability of target attainment (PTA) was considered acceptable if it exceeded 50%, allowing for comparison of dosing schedules. Results indicated that the 50 mg/kg/day divided q12h regimen provided similar drug exposure to the q8h regimen for MICs below 2 mg/L (PTAs >50%). For a MIC of 2 mg/L, PTA was achieved with a higher dose of 30 mg/kg/dose q12h. However, for a MIC of 4 mg/L, the PTA criterion was not met. These findings suggest that a twice-daily dosing of 25 mg/kg/dose provides comparable bactericidal activity to the thrice-daily regimen for MICs between 0.06 and 1 mg/L. This simplified regimen may improve adherence and treatment implementation in children.