The acute effects of sublingual 17β-estradiol on the cardiovascular system

Abstract The beneficial effects of estrogen in postmenopausal women have been well documented. Cardioprotection by estrogen, which is probably the result of several metabolic alterations, appears after 2 or more years of constant use. However, acute administration of estrogen (intravenous or intracoronary) was found to improve cardiac hemodynamics and function through various non-genomic mechanisms. This article reviews data on the consequences of sublingual administration of estrogen, a non-invasive and simple dosing route which is associated with rapid absorption and prompt cardiovascular reactions. It appears that sublingual estradiol at 1 or 2 mg may improve ischemia and exercise performance in women with coronary artery disease, and augment the aortic and brachial blood flow as a result of vasodilation, whereas larger doses (4 mg) may lead to a decrease in myocardial contractility and aortic blood flow, and a slight drop in blood pressure. More data are needed to evaluate the actual clinical significance of sublingual estradiol in healthy women, in situations when endothelial dysfunction is anticipated (diabetes, hypertension) and in women with diagnosed coronary artery disease.