Brimonidine Tartrate Gel Research Articles

Efficiency of complex topical therapy and broadband pulsed non-coherent light in the treatment of erythematotelangiectatic subtype of rosacea

Rosacea is a chronic inflammatory dermatosis of facial localization. Treatment tactics for patients with rosacea is a complex task, since it depends on the severity and individual characteristics of the patient. Numerous studies determine the relevance of this problem. Observation of 22 patients, 11 of whom received only topical treatment with the erythematotelangiectatic subtype of rosacea treatment in the form of 15% azelaic acid, 0.5 % brimonidine tartrate gel, and 1 % metronidazole cream. In 11 other patients, topical treatment was combined with phototherapy – broadband incoherent pulsed light at intervals of 1 time in 4 weeks, 3 procedures per course. Evaluation of the effectiveness of therapy was carried out using the Antera 3D visualization and skin diagnostics device. Also, the dermatological index GSS (Global Severity Score) and the dermatological index of symptom scale (DISS) were used as clinical evaluation methods. The combination of 15 % azelaic acid, 0.5 % brimonidine tartrate gel, with broadband pulse therapy (3 procedures) showed higher efficiency than monotherapy with topical agents. The obtained results, indicating higher efficiency of the combined treatment method, can be explained by the synergistic effect of the combination of the physiotherapeutic factor and external drugs affecting the pathogenetic mechanisms of disease development.

Rosacea.

Rosacea is a common cutaneous condition affecting predominantly the face. It is historically characterised into four subtypes: erythematotelangiectatic, papulopustular, phymatous and ocular rosacea. This article describes the pathophysiology, clinical features and current treatment options for rosacea, and discusses updated diagnostic criteria. General guidance is required on the need to avoid possible triggers including dietary and environmental triggers. The strongest evidence supports the use of 0.75% metronidazole, topical azelaic acid or topical ivermectin for inflammatory rosacea. Erythema should be treated with brimonidine tartrate gel, oral medication such as beta blockers or vascular laser and light-based therapy. Oral doxycycline 40 mg modified release can be used as monotherapy or in combination with other treatments for recalcitrant disease. Further understanding of the pathogenesis of rosacea could allow identification and targeted avoidance of triggers and the development of new treatment modalities.

ЕRYTHEMATOTELANGIECTATIC ROSACEA: THE OPTIMIZATION OF DIAGNOSTICS AND THERAPY

Presents the modern classification, definition and differential diagnostic criteria of the clinical picture of rosacea. The social significance of dermatosis, the importance and the ability to eliminate the symptoms of the disease in the early stages, achieve a sustainable clinical effect to the ”Clear“ skin condition. The article presents the first domestic positive experience in the complex treatment of the erythematotelangiectatic rosacea, using broadband pulsed light radiation using a 0.5% brimonidine tartrate gel (Mirvazo Derm®). The effectiveness of the method is estimated using a multispectral analysis of the skin, which allows real-time to see the morphological structure of the pathological process, as well as create a map of the distribution of hemoglobin and measure its concentration in the lesions. During research there were 60 patients aged 26 to 55 years with an established diagnosis of erythematotelangiectatic rosacea. The duration of the disease ranged from 6 months to 12 years. We have demonstrated the high efficiency and tolerability of the combined method, the absence of side and undesirable effects in patients with rosacea with an erythematotelangiectatic subtype.

INNOVATIONS TO TOPICAL THERAPY OF ROSACEA

The main pathogenetic aspects of rosacea, various classifications of dermatosis and the modern clinical classification are presented. The symptoms that differentiate rosacea from other dermatoses are described. Contradictory of modern scientific concepts of different researchers, approaches to etiology, pathogenesis and treatment has been noted. The social significance of rosacea, the importance and possibility of eliminating the symptoms of the disease at early stages, the achievement and prolongation of remission are shown. The main triggers for the manifestation of rosacea, which should be taken into account to achieve the maximum effect in the treatment of the disease, are indicated. The domestic and foreign clinical recommendations on the treatment of the disease are considered in view of the appearance of new external drugs. The results of several studies in the USA and Canada on the efficacy of 1% ivermectin cream and 0.5% brimonidine tartrate gel compared to placebo are shown. The first domestic positive experience of self-study with 1% ivermectin cream (Solantra®) and 0.5% brimonidine tartrate gel (Mirvazo Derm®) is presented. The high efficacy and very good tolerability of this drugs, as well as the absence of any side effects in patients with moderate to severe rosacea are shown.

Update on the Management of Rosacea.

Refining diagnostic criteria has identified key characteristics differentiating rosacea, a chronic skin disorder, from other common cutaneous inflammatory conditions. The current classification system developed by the National Rosacea Society Expert Committee consists of erythematotelangiectatic, papulopustular, phymatous, and ocular subtypes. Each subtype stands as a unique entity among a spectrum, with characteristic symptoms and physical findings, along with an intricate pathophysiology. The main treatment modalities for rosacea include topical, systemic, laser, and light therapies. Topical brimonidine tartrate gel and calcineurin inhibitors are at the forefront of topical therapies, alone or in combination with traditional therapies such as topical metronidazole or azelaic acid and oral tetracyclines or isotretinoin. Vascular laser and intense pulsed light therapies are beneficial for the erythema and telangiectasia, as well as the symptoms (itching, burning, pain, stinging, swelling) of rosacea. Injectable botulinum toxin, topical ivermectin, and microsecond long-pulsed neodymium-yttrium aluminum garnet laser are emerging therapies that may prove to be extremely beneficial in the future. Once a debilitating disorder, rosacea has become a well known and manageable entity in the setting of numerous emerging therapeutic options. Herein, we describe the treatments currently available and give our opinions regarding emerging and combination therapies.

The role of brimonidine tartrate gel in the treatment of rosacea.

Rosacea is a chronic cutaneous condition with a prevalence rate ranging from 9.6% to 22% in recent studies. Facial erythema (transient and permanent) is considered a common denominator that is frequently observed in all subtypes of rosacea and is estimated to affect more than 40 million people worldwide. Brimonidine tartrate is a selective α2-adrenergic receptor agonist and is the first topical treatment approved for facial erythema of rosacea. Clinical trials have demonstrated that brimonidine tartrate provided significantly greater efficacy, compared to vehicle, for the treatment of moderate to severe erythema of rosacea. In addition, brimonidine tartrate has demonstrated a rapid onset of effect, duration of action throughout the day, and good safety profile in studies of up to 1 year. This review critically discusses the role of brimonidine tartrate for the treatment of facial erythema of rosacea by examining both clinical study data and real-world dermatologist experiences across a wide spectrum of treated patients, and concludes that it is a significant therapeutic option in the management of an unmet need of this chronic condition.

The Role of Topical Brimonidine Tartrate Gel as a Novel Therapeutic Option for Persistent Facial Erythema Associated with Rosacea.

Rosacea is a chronic inflammatory skin condition that commonly presents with persistent facial erythema with or without the coincident presence of flushing, telangiectasias, inflammatory papules or pustules, phymatous changes, or ocular involvement. Patients often present with a constellation of various signs and symptoms of the disease, and an individualized treatment plan should be tailored to a patient’s unique clinical presentation. Previously available medications for rosacea have all targeted the inflammatory erythematous papules and pustules frequently associated with the disease, leaving a therapeutic gap for the common manifestation of persistent facial erythema. Brimonidine tartrate 0.33% gel was approved by the US Food and Drug Administration in August 2013 as the first medication available for the topical treatment of persistent facial erythema associated with rosacea. Brimonidine gel is a highly selective α2-adrenergic receptor agonist with potent vasoconstrictive effects, which leads to significant reduction of persistent facial erythema in the majority of patients when applied once daily. Based on large-scale clinical trials and post-marketing reports, brimonidine gel has maintained a good safety profile with a minority of patients experiencing adverse effects from its use, most of which are cutaneous in nature, mild-to-moderate in degree, occur early after initiation of treatment, often resolve spontaneously with continued use, and generally resolve after discontinuation of use. Among the reported adverse effects, two distinct manifestations of worsened erythema have been described. Brimonidine gel can be integrated into a treatment regimen along with concomitant therapies for facial papules and pustules with no increased risk of adverse events with combination therapy. Education about optimal application methods, setting reasonable expectations for treatment, and minimizing inflammation are important factors for the successful use of brimonidine gel as part of a patient’s overall rosacea treatment regimen.Electronic supplementary materialThe online version of this article (doi:10.1007/s13555-015-0078-1) contains supplementary material, which is available to authorized users.

Update on the management of rosacea.

Refining diagnostic criteria has identified key characteristics differentiating rosacea, a chronic skin disorder, from other common cutaneous inflammatory conditions. The current classification system developed by the National Rosacea Society Expert Committee consists of erythematotelangiectatic, papulopustular, phymatous, and ocular subtypes. Each subtype stands as a unique entity among a spectrum, with characteristic symptoms and physical findings, along with an intricate pathophysiology. The main treatment modalities for rosacea include topical, systemic, laser, and light therapies. Topical brimonidine tartrate gel and calcineurin inhibitors are at the forefront of topical therapies, alone or in combination with traditional therapies such as topical metronidazole or azelaic acid and oral tetracyclines or isotretinoin. Vascular laser and intense pulsed light therapies are beneficial for the erythema and telangiectasia, as well as the symptoms (itching, burning, pain, stinging, swelling) of rosacea. Injectable botulinum toxin, topical ivermectin, and microsecond long-pulsed neodymium-yttrium aluminum garnet laser are emerging therapies that may prove to be extremely beneficial in the future. Once a debilitating disorder, rosacea has become a well known and manageable entity in the setting of numerous emerging therapeutic options. Herein, we describe the treatments currently available and give our opinions regarding emerging and combination therapies.

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

Persistent facial erythema is the most common primary pathological feature of rosacea, the only treatment for which is brimonidine tartrate (BT) gel. To assess the relative bioavailability of topical BT gel in comparison with the ophthalmic BT solution. 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%. Patients who received BT ophthalmic solution 0·2% three times a day for 1 day had a mean Cmax of 54 ± 28 pg mL(-1) and a mean 0-24-h area under the curve (AUC0-24 h ) of 568 ± 277 pg h mL(-1) . 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 Cmax values for the BT gels ranged between 13 and 25 pg mL(-1) , and mean AUC0-24 h values ranged between 42 and 290 pg h mL(-1) . 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. The systemic safety profile of BT gel may be considered better than that of the ophthalmic solution.

Current drug therapies for rosacea: a chronic vascular and inflammatory skin disease.

Rosacea is a chronic skin disorder that presents with abnormal vascular and inflammatory conditions. Clinical manifestations include flushing, facial erythema, inflammatory papules and pustules, telangiectasias, edema, and watery or irritated eyes. To discuss the evolving pathophysiology of rosacea, factors involved in promoting the chronic vascular and inflammatory abnormalities seen in rosacea, and the available drug therapies for the condition. Chronic inflammation and vascular changes are believed to be underlying factors in the pathophysiology of rosacea. Aberrant cathelicidin expression, elevated kallikrein 5 (KLK5) proteolytic activity, and altered toll-like receptor 2 (TLR2) expression have been reported in rosacea skin leading to the production of proinflammatory cytokines. Until recently, drug therapies only targeted the inflammatory lesions (papules and pustules) and transient erythema associated with these inflammatory lesions of rosacea. Brimonidine tartrate gel 0.5% was recently approved for the treatment of persistent (nontransient) facial erythema of rosacea, acting primarily on the cutaneous vascular component of the disease. Rosacea is a chronic vascular and inflammatory skin disease. Understanding the role of factors that trigger the onset of rosacea symptoms and exacerbate the condition is crucial in treating this skin disease.

Getting the Red Out, Office Style

The U.S. Food and Drug Administration approved brimonidine tartrate gel 0.5% g (BT) for the treatment of the erythema associated with

Efficacy and safety of once-daily brimonidine tartrate gel 0.5% for moderate to severe facial erythema of rosacea: Two randomized, double-blind, and vehicle-controlled phase III studies

Efficacy and safety of once-daily brimonidine tartrate gel 0.5% for moderate to severe facial erythema of rosacea: Two randomized, double-blind, and vehicle-controlled phase III studies

A single application of brimonidine tartrate gel significantly reduces moderate to severe facial erythema associated with rosacea

A single application of brimonidine tartrate gel significantly reduces moderate to severe facial erythema associated with rosacea

Once-daily topical brimonidine tartrate gel 0.5% is safe and efficacious in the treatment of moderate to severe persistent facial erythema associated with rosacea

Once-daily topical brimonidine tartrate gel 0.5% is safe and efficacious in the treatment of moderate to severe persistent facial erythema associated with rosacea

Once-daily topical brimonidine tartrate gel 0·5% is a novel treatment for moderate to severe facial erythema of rosacea: results of two multicentre, randomized and vehicle-controlled studies

Erythema of rosacea is thought to result from abnormal cutaneous vasomotor activity. Brimonidine tartrate (BT) is a highly selective α(2) -adrenergic receptor agonist with vasoconstrictive activity. To determine the optimal concentration and dose regimen of topical BT gel for the treatment of erythema of rosacea and to evaluate its efficacy and safety. In study A, 122 subjects were randomized to receive a single application of BT 0·07%, 0·18%, 0·5% or vehicle. In study B (4-week treatment and 4-week follow-up), 269 subjects were randomized to receive BT 0·5% once daily, BT 0·18% once daily, vehicle once daily, BT 0·18% twice daily or vehicle twice daily. Evaluations included Clinician's Erythema Assessment (CEA), Patient's Self-Assessment (PSA), Chroma Meter measurements and adverse events. In study A, a single application of topical BT gel reduced facial erythema in a dose-dependent fashion. A significant difference between BT 0·5% and vehicle in Chroma Meter redness value was observed from 30min to 12h after application. In study B, BT 0·5% once daily had a statistically superior success profile (defined as a two-grade improvement on both CEA and PSA over 12h) compared with vehicle once daily on days 1, 15 and 29 (all P<0·001). No tachyphylaxis, rebound of erythema or aggravation of other disease signs (telangiectasia, inflammatory lesions) was observed. All regimens were safe and well tolerated with similarly low incidence of adverse events. Once-daily BT gel 0·5% is well tolerated and provides significantly greater efficacy than vehicle gel for the treatment of moderate to severe erythema of rosacea.