Effectiveness and Safety of Modified-Release Doxycycline Capsules Once Daily for Papulopustular Rosacea Monotherapy Results from a Large Community-Based Trial in Subgroups Based on Gender

June 2012 | Volume 11 | Issue 6 | Original Article | 703 | Copyright © 2012

Abstract

This article is a prospective planned analysis of data evaluating the effectiveness and safety of modified-release doxycycline capsules (30 mg immediate-release and 10 mg delayed-release beads) used once daily for up to 12 weeks in subgroups of males and females with papulopustular (subtype 2) rosacea from a large, open-label, multicenter, community-based study. A total of 1421 patients participated in the study. The per-protocol population comprised 826 patients on monotherapy, with 28.5% male participants (n=235) and 71.5% female participants (n=591). Rosacea was assessed on a 5-point investigator's global assessment (IGA) scale (0=clear, 1=near clear, 2=mild, 3=moderate, 4=severe). Erythema was also assessed on a 5-point clinician's erythema assessment (CEA) scale (0=none, 1=mild, 2=moderate, 3=significant, 4=severe). At baseline, males had a higher percentage of IGA scores of 3 (116 per 235; 49.4% versus 273 per 591; 46.2% in females) and 4 (32 per 235; 13.6% versus 35 per 591; 5.9% in females). Significant improvements in severity rating and erythema were observed in males and females as demonstrated by shifts in the distribution of IGA and CEA scores between baseline and week 12 (P<.001). Treatment success (IGA score of 0 or 1) at week 12 was achieved in 172 per 235 (73.2%) of males and in 444 per 591 (75.2%) of females. Adverse events (primarily mild or moderate gastrointestinal events) were reported in 9.9% of males and 12.8% of females. Anti-inflammatory dose doxycycline, which is administered as a 40 mg modified-release capsule once daily was effective and safe as monotherapy for papulopustular rosacea in both the female (n=591) and male (n=235) study groups. This specific 40 mg capsule delivers 30 mg immediate-release and 10 mg as delayed release using specially designed beads, and is subantimicrobial with both single and repeated dosing.

J Drugs Dermatol. 2012;11(6):703-707

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INTRODUCTION

Doxycycline 40 mg modified-release capsules (30 mg immediate-release and 10 mg delayed-release beads), administered at a daily dosage of one capsule daily, is the first and only oral medication approved by the US Food and Drug Administration (FDA) for the treatment of papulopustular (PP) rosacea, also referred to as subtype 2 rosacea. This formulation has been specifically referred to as anti-inflammatory dose doxycycline in the peer-reviewed medical literature, including in the pivotal phase III study publication, as its pharmacokinetic (PK) and microbiologic profiles demonstrate absence of antibiotic selection pressure with a lack of emergence of antibiotic-resistant bacterial strains.1-4 Specifically, this modified-release oral 40 mg capsule formulation administered once daily differs in PK profile from immediate-release doxycycline tablets, capsules, and liquids, and from other delayed-release oral formulations of doxycycline, such as enteric-coated pellets embedded in a tablet or capsule hull. Importantly, this specific doxycycline 40 mg capsule allows for immediate release of 30 mg of doxycycline, followed later during intestinal transit by release of 10 mg of doxycycline from delayed-release beads, providing a PK profile that is unique and not bioequivalent to other doxycycline products.1 In addition, the plasma concentrations of doxycycline achieved with oral intake of this modified-release doxycycline 40 mg capsule once daily are in the range which provides anti-inflammatory effects unrelated to antibiotic activity, and are below those required to achieve minimum inhibitory concentrations needed to suppress bacteria.1-4 Thus, this specific modified-release doxycycline 40 mg capsule formulation (30 mg immediate release and 10 mg delayed release beads) coupled with once daily administration, hereafter referred to as anti-inflammatory dose doxycycline, was intentionally designed to achieve anti-inflammatory effects while at the same time avoiding the antibiotic effects that occur with other doxycycline formulations dosed at equal to or greater than 50 mg daily.2-5 Another advantage of anti-inflammatory dose doxycycline demonstrated in a randomized, double-blind, active-control, comparative 16-week study is the nearly identical speed of onset and magnitude of effectiveness in patients with predominantly moderate PP rosacea based on lesion count reductions and investigator's global assessment (IGA), but with a five-fold lower incidence of gastrointestinal adverse events as compared to doxycycline 100 mg once daily.5

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