Rilmenidine is an imidazoline derivative that appears to lower blood pressu
re (BP) by an interaction with imidazoline (I-1) receptors in the brainstem
(and kidneys). Rilmenidine is as effective in monotherapy as all other fir
st-line classes of drugs, including diuretics, beta -blockers, angiotensin
converting enzyme (ACE) inhibitors, and calcium antagonists. It is well tol
erated and can be taken in combination for greater efficacy. Sedation and d
ry mouth are not prominent side effects and withdrawal hypertension is not
seen when treatment is stopped abruptly.
Recently, in addition to a reduction in BP, this agent has been shown to im
prove glucose tolerance, lipid risk factors. and insulin sensitivity. These
changes would be consistent with a reduction in long-term cardiovascular r
isk, as would recently described actions on the heart (reducing left ventri
cular hypertrophy) and the kidney (reducing microalbuminuria). Although no
data are yet available from prospective long-term outcome studies, rilmenid
ine could represent an important new development in antihypertensive therap
y and the prevention of cardiovascular disease. (C) 2001 American Journal o
f Hypertension, Ltd.