Nestle Skin Health R&D, Sophia Antipolis, France.
Clinique Pasteur Toulouse, INSERM 1048, Toulouse, France.
Drugs R D. 2018 Mar;18(1):87-90. doi: 10.1007/s40268-018-0227-y.
Topical α-adrenergic agonist therapy has been developed to treat the persistent erythema of rosacea patients. Brimonidine and oxymetazoline are both topical α-adrenergic agonists.
The objective of this in vitro safety pharmacology study was to compare the potential safety profiles of brimonidine and oxymetazoline.
Brimonidine and oxymetazoline underwent pharmacological profiling with a standard panel of 151 assays, including α-adrenergic receptors and 5-hydroxytryptamine (5-HT) receptors. A valvular interstitial cell (VIC) proliferation assay was performed with oxymetazoline hydrochloride.
Brimonidine was highly selective for the α adrenergic receptors, specifically α, 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-HT receptor, whereas oxymetazoline had significant 5-HT receptor agonist activity and caused proliferation of mitral VICs in vitro.
As the 5-HT 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.
为了治疗酒渣鼻患者的持续性红斑，已经开发出了局部 α-肾上腺素能激动剂疗法。 溴莫尼定和羟甲唑啉都是局部 α-肾上腺素能激动剂。
本体外安全药理学研究的目的是比较溴莫尼定和羟甲唑啉的潜在安全性特征。
用包括 α-肾上腺素能受体和 5-羟色胺（5-HT）受体在内的 151 个检测试剂盒对溴莫尼定和羟甲唑啉进行了药理学分析。用盐酸羟甲唑啉进行了瓣膜间质细胞（VIC）增殖测定。
溴莫尼定对 α 肾上腺素能受体具有高度选择性，特别是 α1 受体，而羟甲唑啉的选择性则低得多，对广泛的靶标具有高度活性。溴莫尼定在 5-HT 受体上几乎没有活性，而羟甲唑啉具有显著的 5-HT 受体激动剂活性，并在体外导致二尖瓣 VIC 增殖。
由于 5-HT 受体可能与药物引起的瓣膜病有关，因此应仔细考虑其获益/风险比，特别是在患有心血管疾病或其他合并症的患者中。
