Oral antibiotic therapy for acne vulgaris: pharmacokinetic and pharmacodynamic perspectives

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.