Brimonidine

Active substance from the group of selective α2-adrenoceptor agonists; primary use in the therapy of glaucoma. Brimonidine has a vasoconstrictive effect. A 0.33% gel is approved in adults for the symptomatic treatment of facial redness in rosacea.

In clinical trials conducted by the manufacturer, brimonidine gel had achieved significantly greater improvements in facial redness in rosacea than placebo. The tests included two 4-week phase 3 trials with a total of 553 patients. There is also a long-term (12 months) trial with 449 patients.

The most common side effects (incidence ≥ 1%) during short-term treatment were flushing, erythema, burning of the skin and contact dermatitis. The most common side effects during long-term use (incidence: ≥4%) were: flushing (10%), redness (8%), worsening rosacea (5%), nasopharyngitis (5%), burning of the skin (4%), increased intraocular pressure (4%) and headache (4%).

The gel is applied daily in approximately pea-size amounts to the affected areas. The effect is expected within 30 minutes.

• In a long-term study, 15% of patients complained of paradoxical effects such as increased erythema (initially diminishing effect of the preparation, then increased erythema after a few hours), flushing or burning.
• The rate of contact allergies is estimated at <1%.

Brimonidine gel 0.33% ( Mirvaso®) .

1. Del Rosso JQ (2014) Management of cutaneous rosacea: emphasis on new medical therapies. Expert Opinion Pharmacother 15:2029-2038
2. Moore A Long-term safety and efficacy of once-daily topical brimonidine tartrate gel 0.5% for the treatment of moderate to severe facial erythema of rosacea: results of a 1-year open-label study.J Drugs Dermatol 13:56-61
3. Piwnica D et al (2014) Vasoconstriction and anti-inflammatory properties of the selective α-adrenergic receptor agonist brimonidine. J Dermatol Sci 75:49-54.
4. Tong LX et al (2014) Brimonidine tartrate for the treatment of facial flushing and erythema in rosacea. Expert Rev Clin Pharmacol 7:567-577.