Efonidipine hydrochloride ethanolate (NZ-105), (±)-2-
[Benzyl(phenyl)amino]ethyl-1,4-dihydro-2,6-dimethyl-5-(5,5-dimethy
-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-4-(3-nitorophen-yl)-3- pyridine carboxylate
hydrochloride ethanol, is a dihydropyridine calcium antagonist with aphosphonate backbone and that was discovered at Nissan Chemical Industries, Ltd. This active drug
ingredient was initially studied for development as a hydrochloride salt
without ethanol, obtained through the addition of hydrochloric acid to
efonidipine acetone solution. It showed an excellent antihypertensive effect in
patients with various kinds of hypertension (essential, severe, renal).
Efonidipine has slow onset and long duration of action.
It is well known that many 1,4-dihydropyridine derivatives are subject
to the first-pass effect, and that the primary metabolismstep of most derivatives
involves oxidation of the dihydropyridine ring to the corresponding pyridine
analogue. However, it has been suggested that efonidipine is less likely to be
subject to the first-pass effect than other dihydropyridine derivatives and
that its dihydropyridine ring is oxidized mainly after metabolism of the side
chain. Additionally, efonidipine has distinct properties when compared with
other calcium channel blockers. The studies indicated that efonidipine therapy
simultaneously improves blood pressure, endothelial function, and metabolic
parameters without substantially altering insulin sensitivity in non-diabetic patients
with hypertension.(Read more)
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