Comparative pharmacokinetics and bioavailability of brimonidine following ocular and dermal administration of brimonidine tartrate ophthalmic solution and gel in patients with moderate‐to‐severe facial erythema associated with rosacea. (16th July 2014)

• Record Type: Journal Article
• Authors: Benkali, K.; Leoni, M.; Rony, F.; Bouer, R.; Fernando, A.; Graeber, M.; Wagner, N.
• Is Part Of: British journal of dermatology. Volume 171:Number 1(2014:Jul.)
• Page Start: 162
• Page End: 169
• Publication Date: 2014-07-16
• Subjects: Dermatology -- Periodicals; Skin -- Diseases -- Periodicals; 616.5
• DOI: 10.1111/bjd.12881
• Languages: English
• ISSNs: 0007-0963

Abstract

<abstract abstract-type="main" id="bjd12881-abs-0001"> <title>Summary</title> <sec id="bjd12881-sec-0001" sec-type="section"> <title>Background</title> <p>Persistent facial erythema is the most common primary pathological feature of rosacea, the only treatment for which is brimonidine tartrate (BT) gel.</p> </sec> <sec id="bjd12881-sec-0002" sec-type="section"> <title>Objectives</title> <p>To assess the relative bioavailability of topical BT gel in comparison with the ophthalmic BT solution.</p> </sec> <sec id="bjd12881-sec-0003" sec-type="section"> <title>Methods</title> <p>A pharmacokinetic study was conducted to compare intraindividual systemic exposures after dermal application of BT gel (0·07%, 0·18% and 0·5%) under maximal use conditions in patients with moderate‐to‐severe facial erythema associated with rosacea, and administration of BT ophthalmic solution 0·2%.</p> </sec> <sec id="bjd12881-sec-0004" sec-type="section"> <title>Results</title> <p>Patients who received BT ophthalmic solution 0·2% three times a day for 1 day had a mean <italic>C</italic><sub>max</sub> of 54 ± 28 pg mL<sup>−1</sup> and a mean 0–24‐h area under the curve (AUC<sub>0–24 h</sub>) of 568 ± 277 pg h mL<sup>−1</sup>. Topical application of BT gel for 29 days resulted in quantifiable systemic exposure in 22%, 48%, 71% and 79% of patients who received BT gel 0·07% twice daily, 0·18% once daily, 0·18% twice daily and 0·5% once daily, respectively. The mean <italic>C</italic><sub>max</sub> values for the BT gels ranged between 13 and 25 pg mL<sup>−1</sup>, and mean AUC<sub>0–24 h</sub> values ranged between 42 and 290 pg h mL<sup>−1</sup>. Systemic exposure increased with applied dose, with no drug accumulation for the duration of treatment. The systemic exposure observed with the highest dose of BT gel (0·5% once daily) was significantly lower than the systemic levels observed for the ophthalmic solution. 0·2% apply for all the concentrations.</p> </sec> <sec id="bjd12881-sec-0005" sec-type="section"> <title>Conclusions</title> <p>The systemic safety profile of BT gel may be considered better than that of the ophthalmic solution.</p> </sec> </abstract>