In Vitro Safety Pharmacology Profiling of Topical alpha-Adrenergic Agonist Treatments for Erythema of Rosacea.

Article Details

Citation
Copy to clipboard

Piwnica D, Pathak A, Schafer G, Docherty JR

In Vitro Safety Pharmacology Profiling of Topical alpha-Adrenergic Agonist Treatments for Erythema of Rosacea.

Drugs R D. 2018 Mar;18(1):87-90. doi: 10.1007/s40268-018-0227-y.

PubMed ID
29374829 [ View in PubMed
]
Abstract

BACKGROUND: Topical alpha-adrenergic agonist therapy has been developed to treat the persistent erythema of rosacea patients. Brimonidine and oxymetazoline are both topical alpha-adrenergic agonists. OBJECTIVES: The objective of this in vitro safety pharmacology study was to compare the potential safety profiles of brimonidine and oxymetazoline. METHODS: Brimonidine and oxymetazoline underwent pharmacological profiling with a standard panel of 151 assays, including alpha-adrenergic receptors and 5-hydroxytryptamine (5-HT) receptors. A valvular interstitial cell (VIC) proliferation assay was performed with oxymetazoline hydrochloride. RESULTS: Brimonidine was highly selective for the alpha2 adrenergic receptors, specifically alpha2A, whereas oxymetazoline was found to be much less selective and was highly active against a wide range of targets. Negligible activity was observed with brimonidine at the 5-HT2B receptor, whereas oxymetazoline had significant 5-HT2B receptor agonist activity and caused proliferation of mitral VICs in vitro. CONCLUSION: As the 5-HT2B receptor is potentially involved in drug-induced valvulopathy, the benefit/risk ratio should be carefully considered, especially in patients with cardiovascular disease or other comorbidities.

DrugBank Data that Cites this Article

Drugs