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Expert Opinion on Pharmacotherapy Jan 2019Brimonidine tartrate is a commonly used eyedrop for short- and long-term lowering of intraocular pressure. Its use has been popularized due to its effects on aqueous... (Review)
Review
Brimonidine tartrate is a commonly used eyedrop for short- and long-term lowering of intraocular pressure. Its use has been popularized due to its effects on aqueous suppression and uveoscleral outflow, as well as the suggestion of neuroprotection. Although available with alternative preservative vehicles, brimonidine is associated with high rates of local allergy and is contraindicated in breastfeeding women, neonates, young children, and the elderly due to risk of central nervous system depression. Other topical agents with differing advantages have challenged brimonidine's role in the treatment algorithm of ocular hypertension and glaucoma. Areas covered: The authors review the development of topical alpha-adrenergic agonists, with particular attention to the currently available formulations of brimonidine tartrate. Its mechanism of action, pharmacodynamics and safety, and clinical efficacy are analyzed. Expert opinion: Despite clinical familiarity with brimonidine after two decades of use, agents that offer daily dosing, nocturnal effect, and more favorable ocular and systemic side effect profiles have ultimately led to brimonidine's adjunctive use in patients with elevated intraocular pressure or high- or low-tension glaucomas. Still, brimonidine may be advantageous in patients undergoing laser trabeculoplasty or iridotomy, in certain forms of glaucoma, or in pregnant individuals prior to the last trimester, underscoring its clinical importance.
Topics: Adrenergic alpha-Agonists; Brimonidine Tartrate; Glaucoma; Humans; Intraocular Pressure; Ocular Hypertension; Ophthalmic Solutions; Treatment Outcome
PubMed: 30407890
DOI: 10.1080/14656566.2018.1544241 -
Expert Review of Clinical Pharmacology Aug 2022Ocular redness, or conjunctival hyperemia, is a common ophthalmic sign associated with reduced quality of life. For redness without apparent underlying pathology,... (Review)
Review
INTRODUCTION
Ocular redness, or conjunctival hyperemia, is a common ophthalmic sign associated with reduced quality of life. For redness without apparent underlying pathology, topical ophthalmic decongestants have been widely used.
AREAS COVERED
Brimonidine tartrate was approved in 2017 as a topical vasoconstrictor at a 0.025% concentration for relief of ocular redness. Since then, investigators have reported on efficacy and safety findings from studies evaluating low-dose brimonidine for reducing ocular redness.
EXPERT OPINION
Brimonidine is highly selective for α-adrenergic receptors. Clinical trials have so far shown that the drug in low doses significantly reduces ocular redness in comparison to vehicle for up to 8 hours. Brimonidine-treated eyes did not present side effects of other vasoconstrictors, such as hypotension, cardiac arrhythmia, or drowsiness. Ocular adverse events, such as allergic reactions and redness rebound, were also minimal. In this review, we examine in detail published literature on the mechanism of brimonidine tartrate and its efficacy and safety in relieving conjunctival hyperemia.
Topics: Adrenergic alpha-Agonists; Brimonidine Tartrate; Erythema; Humans; Hyperemia; Nasal Decongestants; Ophthalmic Solutions; Quality of Life; Quinoxalines; Receptors, Adrenergic
PubMed: 35951740
DOI: 10.1080/17512433.2022.2112948 -
Expert Review of Clinical Pharmacology Sep 2014Rosacea is a chronic inflammatory dermatologic condition that can often be disfiguring with significant negative impact on patients' quality of life. Sanrosa... (Review)
Review
Rosacea is a chronic inflammatory dermatologic condition that can often be disfiguring with significant negative impact on patients' quality of life. Sanrosa (brimonidine tartate) is a novel therapeutic agent targeting the facial flushing and erythema of rosacea through its α₂ adrenergic receptor agonist activity. The goal of this article is to discuss current treatment options for rosacea and the properties of brimonidine tartate as well as the evidence surrounding its efficacy and safety profile.
Topics: Adrenergic alpha-2 Receptor Agonists; Animals; Brimonidine Tartrate; Erythema; Humans; Quality of Life; Quinoxalines; Rosacea; Treatment Outcome
PubMed: 25091290
DOI: 10.1586/17512433.2014.945910 -
Profiles of Drug Substances,... 2023Brimonidine is a highly selective 2-adrenoceptor agonist that lowers intraocular pressure (IOP) by decreasing aqueous humor production and increasing aqueous humor...
Brimonidine is a highly selective 2-adrenoceptor agonist that lowers intraocular pressure (IOP) by decreasing aqueous humor production and increasing aqueous humor outflow via the uveoscleral route. Brimonidine is used to treat glaucoma and other eye conditions. Brimonidine is a topical medication that is used mainly to treat open-angle glaucoma and ocular hypertension in the eyelids. The purpose of this chapter is to provide a comprehensive discussion of Brimonidine's nomenclature, physiochemical properties, preparation methods, identification procedures, and numerous qualitative and quantitative analytical techniques, as well as its ADME profiles and pharmacological effects. In addition, the chapter contains numerous approaches for separating brimonidine from other medications in combination formulations utilizing chromatographic techniques and other spectroscopic approaches.
Topics: Humans; Brimonidine Tartrate; Glaucoma, Open-Angle; Adrenergic alpha-Agonists; Quinoxalines; Ophthalmic Solutions; Glaucoma; Antihypertensive Agents
PubMed: 37061271
DOI: 10.1016/bs.podrm.2022.11.001 -
Journal of Cosmetic Dermatology Apr 2022Post-acne erythema (PAE) is a common sequela of acne inflammation, and it refers to telangiectasia and erythematous lesions remaining after the acne treatment. Although... (Review)
Review
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.
Topics: Acne Vulgaris; Brimonidine Tartrate; Erythema; Humans; Lasers, Dye; Lasers, Solid-State; Treatment Outcome
PubMed: 35076997
DOI: 10.1111/jocd.14804 -
Dermatologic Surgery : Official... Jan 2018
Review
Topics: Brimonidine Tartrate; Erythema; Facial Dermatoses; Female; Gels; Humans; Laser Therapy; Male; Middle Aged; Vasoconstrictor Agents; Young Adult
PubMed: 29077635
DOI: 10.1097/DSS.0000000000001389 -
Skin Therapy Letter Jul 2021The diagnosis and classification of rosacea has been modified to reflect presenting features. On exclusion of differentials, the diagnosis of rosacea is based on the...
The diagnosis and classification of rosacea has been modified to reflect presenting features. On exclusion of differentials, the diagnosis of rosacea is based on the presence of either (1) phymatous changes, or (2) centrofacial persistent erythema. In their absence, diagnosis can be established by presence of any two of: flushing/transient erythema, papules and pustules, telangiectases, or ocular manifestations. Management of rosacea depends on presenting feature(s), their severity, and impact. General management includes gentle skin care, sun protection, and trigger avoidance. Evidence-based treatment recommendations include topical brimonidine and oxymetazoline for persistent erythema; topical azelaic acid, ivermectin, metronidazole, minocycline and oral doxycycline, tetracycline and isotretinoin for papules and pustules; vascular lasers and light devices for telangiectases; and omega-3 fatty acids and cyclosporine ophthalmic emulsion for ocular rosacea. While surgical or laser therapy can be considered for clinically noninflamed phyma, there are no trials on their utility. Combination therapies include topical brimonidine with topical ivermectin, or topical metronidazole with oral doxycycline. Topical metronidazole, topical ivermectin, and topical azelaic acid are appropriate for maintenance therapy. In conclusion, the updated phenotype approach, based on presenting clinical features, is the foundation for current diagnosis, classification, and treatment of rosacea.
Topics: Brimonidine Tartrate; Dermatologic Agents; Doxycycline; Humans; Metronidazole; Rosacea
PubMed: 34347259
DOI: No ID Found -
Journal Der Deutschen Dermatologischen... Aug 2022This updated and upgraded S2k guideline deals with the diagnosis and treatment of rosacea, which is a common, chronic inflammatory skin disease mostly affecting the...
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.
Topics: Brimonidine Tartrate; Dermatologic Agents; Erythema; Humans; Ivermectin; Metronidazole; Rosacea
PubMed: 35929658
DOI: 10.1111/ddg.14849 -
Ocular Immunology and Inflammation Nov 2023We reviewed the medical charts of five patients diagnosed with brimonidine tartrate (BT)-related corneal disorders. A fan-shaped corneal opacity was present in four... (Review)
Review
We reviewed the medical charts of five patients diagnosed with brimonidine tartrate (BT)-related corneal disorders. A fan-shaped corneal opacity was present in four patients and limbal corneal infiltrations were present in one patient. confocal microscopy revealed dendritic cells and lipid deposits in the fan-shaped opacity as well as neutrophils in limbal infiltrations. BT instillation was discontinued and topical administration of a corticosteroid was initiated for all patients. The limbal infiltrations improved after BT discontinuation. Conversely, the fan-shaped opacity remained in all affected patients. After a fan-shaped opacity has developed in a patient with a BT-related corneal disorder, the lesion is difficult to resolve. However, limbal infiltrations respond well to treatment. Therefore, BT should be discontinued and anti-inflammatory treatment initiated before a fan-shaped opacity forms.
Topics: Humans; Corneal Diseases; Brimonidine Tartrate; Ophthalmic Solutions; Microscopy, Confocal; Lipids
PubMed: 36306423
DOI: 10.1080/09273948.2022.2137045 -
Eye (London, England) Feb 2021To evaluate the effect of brimonidine tartrate 0.15% ophthalmic solution on pupil size under scotopic condition and upper eyelid position.
BACKGROUND
To evaluate the effect of brimonidine tartrate 0.15% ophthalmic solution on pupil size under scotopic condition and upper eyelid position.
METHODS
This study comprised 72 eyes of 36 healthy subjects. A single drop of brimonidine tartrate 0.15% ophthalmic solution was instilled in the right eye and artificial tear was instilled in the left eye. Pupil size was measured using an infra-red pupillometer under scotopic condition before and at 30 min, 2, 4, 6, 8 and 10 h after instillation. Measurement of margin reflex distance 1 (MRD1) was performed using a millimetre ruler before and after at 10 min after instillation.
RESULTS
The mean age of the subjects was 32.19 ± 11.43 years (range 10-52 years), 17 were female and 19 were male. Before brimonidine instillation, the mean pupil size was 6.09 ± 1.03 mm in the brimonidine eyes and 6.06 ± 1.04 mm in the control eyes. There was a significant decrease in mean pupil size at 30 min (4.45 ± 1.04), 2 h (4.49 ± 1.06), 4 h (4.59 ± 1.06), 6 h (4.89 ± 1.06) and 8 h (5.38 ± 1.02) after instillation compared to before in brimonidine eyes (p < 0.001 for all). There was a significant miosis continued for at least 6 h (5.95 ± 1.03) in control eyes (p < 0.001). There was no significant change in MRD1, before and after instillation both in brimonidine and control eyes.
CONCLUSIONS
Brimonidine tartrate 0.15% had a significant miosis under scotopic condition for at least 8 h after instillation and had a significant miosis on the untreated eye for at least 6 h.
Topics: Adolescent; Adult; Brimonidine Tartrate; Child; Eyelids; Female; Humans; Male; Middle Aged; Ophthalmic Solutions; Pupil; Quinoxalines; Young Adult
PubMed: 32518394
DOI: 10.1038/s41433-020-1007-9