Antihypertensive effects and cerebral circulation of NZ-105, a novel dihydropyridine calcium antagonist

Kurimoto, Tadashi; Jin, Hiromasa; Ito, Sigeru; Furuichi, Hiroyasu; Takemasa, Toshihiko; Sato, Ryuichi; Tagashira, Eijiro

doi:10.1016/0014-2999(90)94432-w

Cited by 2 publications

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“…These effects were compared with those of nicardipine or nimodipine in isolated basilar, middle cerebral, superior mesenteric, and femoral arteries of dogs (10). The selectivity of efonidipine for the basilar artery was 49 times higher than for the superior mesenteric and 25 times higher than for the femoral arteries.…”

Section: Effects On Vascular and Cardiac Preparationsmentioning

confidence: 98%

“…but not nicardipine, significantly increased renal blood flow. In anesthetized cats the local cerebral blood flow (cortical, hippocampal, amygdaline, hypothalamic, and cerebellar), measured by a hydrogen clearance method, was increased by efonidipine (10). In open-chest dogs, efonidipine produced no significant change in the maximal rate of elevation of the left ventricular pressure (28).…”

Section: Hernodynamic Effectsmentioning

confidence: 99%

“…The hemodynamic effects of efonidipine were investigated in anesthetized dogs (10,29). By intravenous administration efonidipine (3-30 p g k g ) decreased arterial pressure and significantly increased vertebral (VBF) and coronary blood flow (CBF), but had no effect on femoral blood flow.…”

Section: Hernodynamic Effectsmentioning

confidence: 99%

“…In various rabbit blood vessels (basilar, coronary, superior mesenteric, renal and femoral arteries, and saphenous vein), depolarized with a high-K + solution, efonidipine produced a nonparallel depression of the concentration-response curves for CaC1,-induced contractions (12); its effect was strongest in the basilar artery. These effects were compared with those of nicardipine or nimodipine in isolated basilar, middle cerebral, superior mesenteric, and femoral arteries of dogs (10). The selectivity of efonidipine for the basilar artery was 49 times higher than for the superior mesenteric and 25 times higher than for the femoral arteries.…”

Section: Effects On Vascular and Cardiac Preparationsmentioning

confidence: 99%

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Efonidipine Hydrochloride: A New Calcium Antagonist

Masuda¹,

Tanaka²

1994

Cardiovascular Drug Reviews

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Efonidipine hydrochloride (NZ-105; Fig. 1) is a new phosphonate, long-acting calcium antagonist that has recently been marketed for the treatment of hypertension in Japan. In clinical trials, 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 (27,(41)(42)(43)46). Once-daily therapy with efonidipine is highly efficacious and leads to few minor side effects. In patients with essential hypertension, efonidipine significantly increased renal blood flow, decreased renal vascular resistance, and had a tendency to increase glomerular filtration rate (38). It also significantly increased urinary output and Na+/K+ ratio. Moreover, in hypertensive patients with renal impairment, efonidipine improved proteinuria, i.e., it decreased urinary excretion of proteins. Phase I11 clinical trials for angina pectoris and phase I1 trials for cerebral vasodilation are underway in Japan.It is well known that many 1 ,Cdihydropyridine derivatives are subject to the first-pass effect, and that the primary metabolism step of most derivatives involves oxidation of the dihydropyridine ring to the corresponding pyridine analog (15,17,18,28,39). 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 (32).Slow-onset and long-lasting antihypertensive effects and a favorable renal effect of efonidipine were shown in experiments with rats (14) and dogs (30). Tachycardia, which accompanied the hypotensive effect of efonidipine, was weaker than that induced by nicardipine, another calcium antagonist. In in vitro experiments with vascular preparations, efonidipine possessed selective calcium-antagonizing properties which were slow in

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Section: Effects On Vascular and Cardiac Preparationsmentioning

confidence: 98%

Section: Hernodynamic Effectsmentioning

confidence: 99%

Section: Hernodynamic Effectsmentioning

confidence: 99%

Section: Effects On Vascular and Cardiac Preparationsmentioning

confidence: 99%

See 2 more Smart Citations