Leyden James J, Del Rosso James Q
J Clin Aesthet Dermatol. 2011 Feb;4(2):40-7.
To review data on pharmacokinetic factors that influence the absorption and tissue distribution for individual antibiotic agents to better inform clinicians on rational dosing considerations of oral antibiotics for the treatment of acne vulgaris. The focus is placed on the most commonly prescribed oral antibiotics for acne vulgaris, the tetracyclines. Dose-response is also reviewed.
This review describes factors affecting the absorption, distribution, and target tissue penetration of the most frequently prescribed oral antibiotics for the treatment of acne vulgaris, the tetracyclines. Articles cited were identified by a search of PubMed covering the period from January 1, 2000, to November 15, 2010. Reference lists in articles identified in this search were searched manually for additional references of interest.
Pharmacokinetic factors that may influence outcomes in antibiotic therapy for acne vulgaris include drug solubility, gastrointestinal permeability, systemic absorption, tissue distribution, and target tissue penetration. In particular, drugs that are highly soluble and highly permeable are well absorbed and widely distributed. Drugs that are more lipophilic are believed to penetrate better into the lipid-rich sebaceous follicular tissues, where the therapeutic target, Propionibacterium acnes, resides. Food intake and differences in patient body weight can also alter antibiotic absorption and distribution, potentially resulting in differences in efficacy and tolerability. Dose-response data with oral antibiotics, including the tetracyclines, is scant. Pharmacokinetic studies completed with extended-release minocycline have allowed for assessment of interindividual differences in drug absorption, a consideration that may influence therapeutic response and/or predilection for adverse effects. Dose-response pharmacokinetic data is not currently available with other tetracyclines.
An understanding of the differences in absorption (with and without meals or other ingestants), distribution, and target tissue penetration among oral tetracyclines is valuable for clinicians, as such factors may influence outcomes in patients treated for acne vulgaris.
回顾影响个体抗生素吸收和组织分布的药代动力学因素，以便更好地为临床医生提供关于治疗寻常痤疮口服抗生素合理给药考虑的信息。重点关注治疗寻常痤疮最常用的口服抗生素——四环素类。同时也回顾了剂量反应情况。
本综述描述了影响治疗寻常痤疮最常用的口服抗生素——四环素类吸收、分布及靶组织渗透的因素。通过检索2000年1月1日至2010年11月15日期间的PubMed确定引用的文章。手动检索该检索中确定的文章的参考文献列表以获取其他相关参考文献。
可能影响寻常痤疮抗生素治疗效果的药代动力学因素包括药物溶解度、胃肠道通透性、全身吸收、组织分布和靶组织渗透。特别是，高溶解度和高通透性的药物吸收良好且分布广泛。亲脂性更强的药物被认为能更好地渗透到富含脂质的皮脂腺滤泡组织中，而治疗靶点痤疮丙酸杆菌就存在于该组织中。食物摄入和患者体重差异也会改变抗生素的吸收和分布，可能导致疗效和耐受性的差异。包括四环素类在内的口服抗生素的剂量反应数据很少。用缓释米诺环素完成的药代动力学研究使得能够评估个体间药物吸收的差异，这一因素可能影响治疗反应和/或不良反应倾向。目前其他四环素类药物尚无剂量反应药代动力学数据。
了解口服四环素类药物在吸收（有无食物或其他摄入物）、分布和靶组织渗透方面的差异对临床医生很有价值，因为这些因素可能影响寻常痤疮患者的治疗效果。
