Systemic exposure of topical erythromycin in comparison to oral administration and the effect on cytochrome P450 3A4 activity.

ABSTRACT:

Aims

Erythromycin is a macrolide antibiotic, which is frequently used as a topical formulation for the treatment of acne. It is also known as an inhibitor of the cytochrome P450 (CYP) isoenzyme 3A4. In this study, the systemic availability of topical erythromycin, hence the influence on the activity of CYP3A, is evaluated in comparison to orally administered erythromycin.

Methods

Sixteen healthy volunteers received consecutively topical (two applications of 800 mg) and oral erythromycin (two dose groups, 250 and 1000 mg, with n = 8) to assess erythromycin pharmacokinetics. A microdose of midazolam (3 μg orally) was used to determine the effect on CYP3A activity.

Results

After topical administration, erythromycin was detected in the plasma of every participant without

SUBMITTER: Carls A 

PROVIDER: S-EPMC4256632 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature