brimonidine
Regulatory sources consulted
Approved indications
- Symptomatic treatment of facial erythema of rosacea in adults.
Contraindications
Absolute
- Hypersensitivity to brimonidine or excipients.
- Children under 2 years.
- Treatment with MAO inhibitors or tricyclic or tetracyclic antidepressants affecting noradrenergic transmission.
Clinical warnings
- Major warning · It may worsen erythema or cause rebound flushing, especially during the first 2 weeks. Stop if it worsens and test on a small area before restarting. — CIMA/AEMPS, ficha técnica 113904006
- Major warning · Do not apply to irritated skin, after laser treatment, or to wounds. Use cautiously in severe or unstable cardiovascular disease, depression, cerebral or coronary insufficiency, Raynaud phenomenon, orthostatic hypotension, Buerger disease, scleroderma, or Sjögren syndrome. — CIMA/AEMPS, ficha técnica 113904006
Drug interactions
- HighMAO inhibitors and tricyclic or tetracyclic antidepressants
Mechanism: They may affect noradrenergic transmission and potentiate brimonidine effects.
Recommendation: Combination is contraindicated.
CIMA/AEMPS, ficha técnica 113904006https://cima.aemps.es/cima/dochtml/ft/113904006/FT_113904006.html
- ModerateCentral nervous system depressants, antihypertensives, or cardiac glycosides
Mechanism: Additive effects on sedation, blood pressure, or heart rate may occur.
Recommendation: Use cautiously and monitor clinical response.
CIMA/AEMPS, ficha técnica 113904006https://cima.aemps.es/cima/dochtml/ft/113904006/FT_113904006.html
Adverse events
Common (≥1%)
Erythema · Pruritus · Flushing or pallor at the application site · Rosacea · Burning sensation
Rare but serious
Bradycardia · Hypotension · Angioedema
Pregnancy and lactation
Preferably avoid during pregnancy. Do not use while breastfeeding because a risk to the infant cannot be excluded.
Recent literature (PubMed)
Rosacea is a chronic cutaneous disorder affecting primarily the face, characterized by erythema, transient or persistent, telangiectasia, and inflammatory lesions including papulo-pustules and swelling. The essential component of the disease is the persistent erythema of facial skin. Episodes of flushing (acute-subacute intermittent vasodilation) are common. Swelling and erythema of the nose along with dilatation of the pilosebaceous poral orifices, known as rhinophyma, can be noted in chronic cases. Rosacea affects up to 10% of the world population and is especially noted in fair-skinned individuals aged 35-50. Women are affected more often than men. Several treatment modalities including topical medications, systemic drugs, lasers, and light-based therapies have been used for the management of rosacea with variable results. Topical medications such as azelaic acid, metronidazole, and sulfacetamide/sulfur, oral antibiotics such as tetracyclines, and oral retinoids alone or, most commonly, in combination form the mainstay of treatment. Light therapies such as intense pulsed light and pulsed dye laser are best used for the erythemato-telangiectatic type. Topical brimonidine, oxymetazoline, ivermectin, tacrolimus, pimecrolimus, low-dose modified-release tetracyclines and botulinum toxin are the new additions to the therapeutic armamentarium. This article provides a comprehensive review of the various therapies used for rosacea.
Post-acne erythema (PAE) is a common sequela of acne inflammation, and it refers to telangiectasia and erythematous lesions remaining after the acne treatment. Although some PAE lesions may improve over time, persisting PAE might be esthetically undesirable for patients. The efficacy of various treatment options for PAE has been investigated in many studies but there exists no gold standard treatment modality. In this study, we aimed to give a systematic literature review on various treatment options for PAE, the advantage of each modality, and compare their efficacy, safety, and feasibility. By using the selected keywords, we carried out a systematic search for articles published from the inception to 28 April 2021 in PubMed/Medline and Embase databases. Of the 5796 initially retrieved articles, 18 of them were fully eligible to be enrolled in our study. In this study, we found that light and laser-based devices were the most frequently used treatments for PAE. Generally, pulsed-dye lasers were the most commonly used laser devices for PAE. Neodymium:yttrium aluminum-garnet lasers were the second most commonly used modalities in treating PAE. Topical treatments such as oxymetazoline, tranexamic acid, and brimonidine tartrate are promising treatments in reducing PAE lesions. In our study, no severe side effects were found. In conclusion, both laser devices and topical agents seem to be effective for PAE lesions; however, further randomized clinical trials are needed in this field.
This updated and upgraded S2k guideline deals with the diagnosis and treatment of rosacea, which is a common, chronic inflammatory skin disease mostly affecting the face. Initially, rosacea is characterized by recurrent erythema, telangiectasia and flushing. Later, the inflammatory component predominates, with persistent erythema with follicular papules, papulopustules and pustules. The development of phyma, which usually occurs on the acral localizations, is the most severe manifestation. For the treatment of rosacea, the interdisciplinary guideline committee, with representatives of the German Dermatological Society (DDG), the Professional Association of German Dermatologists (BVDD), the German Opthalmological Society (DOG), the Society for Dermopharmacy (GD), the Swiss Society for Dermatology and Venereology (SGDV) and the German Rosacea Aid e. V., recommends the avoidance of trigger factors and topical applications of metronidazole, azelaic acid or ivermectin. For symptomatic treatment of persistent centrofacial erythema, the topical vasoconstrictors brimonidine or oxymetazoline can also be used. Systemic therapy is recommended for therapy-resistant and severe forms of rosacea papulopustulosa. The drug of choice is low-dose doxycycline. Alternatively, low-dose isotretinoin can be recommended. Ocular rosacea should be treated with lid margin hygiene. For topical treatment, ciclosporin eye drops, azithromycin, ivermectin or metronidazole are suggested.
Rosacea is a chronic skin disorder involving central facial erythema secondary to vascular instability and cutaneous inflammation. Rosacea is divided into different subtypes based on the morphology of the rash — erythematotelangiectatic, papulopustular, phymatous, and ocular rosacea. A less-known subtype called neurogenic rosacea has been proposed to categorize patients suffering from rosacea with erythematous flushing and burning sensation that is refractory to traditional treatment. There is minimal data on this subgroup of rosacea patients and its potential treatment options. This review aims to explore current medical literature to define characteristics of neurogenic rosacea and its management. We performed a systematic search of PubMed database and identified 6 articles meeting inclusion criteria with a total of 37 patients with suspected neurogenic rosacea. Combination treatments with topicals (eg, metronidazole, brimonidine), as well as oral medications including vascular (eg, beta blockers), psychiatric (eg, diazepam, duloxetine), neurologic (eg, pregabalin, sumatriptan), and antibiotic agents (eg, rifaximin), were often cited to have better outcomes, but this finding was highly variable between patients. There were isolated reports of effective management with onabotulinumtoxinA intradermal injections and endoscopic thoracic sympathectomy treatment. Current literature supports selecting agents aimed at treating the major symptom pattern (eg, erythema, telangiectasias, burning sensation). Neurogenic rosacea treatment: a literature review. Ivanic MG, Oulee A, Norden A, et al. J Drugs Dermatol. 2023;22(6):566-571. doi:10.36849/JDD.7181  .
Remdesivir, marketed under the brand name Veklury, is an antiviral drug with a broad spectrum of activity. There were various countries where the use of Remdesivir for the treatment of COVID-19 was authorized during the pandemic. Remdesivir was first designed to treat hepatitis C, but it was later tested for Ebola virus sickness and Marburg virus infections. Remdesivir is a prodrug designed to facilitate the intracellular transport of GS-441524 monophosphate and its subsequent biotransformation into GS-441524 triphosphate, a ribonucleotide analogue inhibitor of viral RNA polymerase. The objective of this chapter is to provide a comprehensive review of Remdesivir (GS-5734), including its nomenclature, physiochemical properties, preparation methods, identification procedures, numerous qualitative and quantitative analytical techniques, ADME profiles, and pharmacological effects. In addition, the chapter provides a variety of chromatographic and spectroscopic techniques for separating brimonidine from other drugs in combination formulations.