Myocardial and vascular effects of efonidipine in vitro as compared with nifedipine, verapamil and diltiazem

Tanaka, Hikaru; Masumiya, Haruko; Sekine, Toshiyuki; Sijuku, Toshinori; Sugahara, Motoko; Taniguchi, Haruyori; Terada, Miyuki; Saito, Wataru; Shigenobu, Koki

doi:10.1016/0306-3623(95)02065-9

Cited by 21 publications

(10 citation statements)

References 17 publications

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“…24 It has been reported that bradycardia depends on stimulation/frequency; that is, inhibitors of HR are more dramatically effective when the HR is initially high. 25 Thus, in the present study, in the high-HR group of healthy adults, HR significantly decreased after single-dose administration of efonidipine hydrochloride, but there were no marked changes in the low-HR group.…”

Section: Circulation Journal Vol67 February 2003mentioning

confidence: 99%

“…These agents may be appropriate for patients with hypertension or angina pectoris. 13,24,29 Previous studies have reported the effects of T-type Ca channel inhibitors on autonomic nervous activity. Though nifedipine, which is selective for L-type channels, inhibits parasympathetic nervous activity, the T-type Ca channel inhibitor, mibefradil, has been reported to enhance parasympathetic nervous activity and favorably influence the autonomic nervous system.…”

Section: Circulation Journal Vol67 February 2003mentioning

confidence: 99%

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Clinical Efficacy of Efonidipine Hydrochloride, a T-type Calcium Channel Inhibitor, on Sympathetic Activities. Examination Using Spectral Analysis of Heart Rate/Blood Pressure Variabilities and 123I-Metaiodobenzylguanidine Myocardial Scintigraphy.

Harada¹,

Nomura²,

Nishikado³

et al. 2003

Circ J

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Section: Circulation Journal Vol67 February 2003mentioning

confidence: 99%

Section: Circulation Journal Vol67 February 2003mentioning

confidence: 99%

Clinical Efficacy of Efonidipine Hydrochloride, a T-type Calcium Channel Inhibitor, on Sympathetic Activities. Examination Using Spectral Analysis of Heart Rate/Blood Pressure Variabilities and 123I-Metaiodobenzylguanidine Myocardial Scintigraphy.

Harada¹,

Nomura²,

Nishikado³

et al. 2003

Circ J

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“…This was indeed the case with efonidipine in isolated myocardial preparations. In case of nifedipine and verapamil, the potencies of the chronotropy and inotropy expressed in terms of EC 30 values were about the same, while in the case of efonidipine, the potency of inotropy was 1 / 300 of the potency of chronotropy (38,39).…”

Section: Camentioning

confidence: 93%

Pathophysiological Significance of T-type Ca2+ Channels: T-type Ca2+ Channels and Drug Development

Tanaka

Shigenobu

2005

J Pharmacol Sci

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Abstract. T-type Ca2+ channels are present in cardiovascular, neuronal, and endocrine systems; and they are now receiving attention as novel therapeutic targets. Many drugs and compounds non-specificaly block T-type Ca 2+ channels. Certain dihydropyridine compounds, such as efonidipine, have blocking activity on both L-type and T-type Ca 2+ channels which possibly underlies their excellent clinical profiles such as minimum reflex tachycardia and renal protection. Selective inhibitors of T-type Ca 2+ channels, such as non-hydrolyzable mibefradil and R(−)-efonidipine, are powerful pharmacological tools for further studies and may lead to the development of novel therapeutic strategies.

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“…These effects were initially attributed to the slow onset of efonidipine's action (19,30,65). However, since efonidipine has been shown to have potent negative chronotropic effects on isolated right atria (32,56), we thought that the drug might have direct effects on the sinoatrial node. Thus, we performed standard glass microelectrode recordings of spontaneous action potentials in isolated sinoatrial node tissue from the rabbit and guinea pig and examined the effects of various Ca 2+ channel blockers including efonidipine (33).…”

Section: Effect On Cardiac Pacemakingmentioning

confidence: 99%

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

Tanaka

Shigenobu

2002

Cardiovascular Drug Reviews

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T-type Ca 2+ channels have properties different from those of the L-type and are involved in cardiac pacemaking and regulation of blood flow, but not in myocardial contraction. Efonidipine is an antihypertensive and antianginal drug with dihydropyridine structure that was recently found to block both L-and T-type Ca 2+ channels. In isolated myocardial and vascular preparations, efonidipine has potent negative chronotropic and vasodilator effects but only a weak negative inotropic effect. In experimental animals and patients, reduction of blood pressure by the drug was accompanied by no or minimum reflex tachycardia leading to improvement of myocardial oxygen balance and maintenance of cardiac output. Efonidipine increased glomerular filtration rate without increasing intraglomerular pressure. By relaxing both the afferent and efferent arterioles, efonidipine markedly reduced proteinuria. Thus, efonidipine, an L-and T-type dual Ca 2+ channel blocker, appears to have an ideal profile as an antihypertensive and antianginal drug with organ-protective effects in the heart and kidney.

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Myocardial and vascular effects of efonidipine in vitro as compared with nifedipine, verapamil and diltiazem

Cited by 21 publications

References 17 publications

Clinical Efficacy of Efonidipine Hydrochloride, a T-type Calcium Channel Inhibitor, on Sympathetic Activities. Examination Using Spectral Analysis of Heart Rate/Blood Pressure Variabilities and 123I-Metaiodobenzylguanidine Myocardial Scintigraphy.

Clinical Efficacy of Efonidipine Hydrochloride, a T-type Calcium Channel Inhibitor, on Sympathetic Activities. Examination Using Spectral Analysis of Heart Rate/Blood Pressure Variabilities and 123I-Metaiodobenzylguanidine Myocardial Scintigraphy.

Pathophysiological Significance of T-type Ca2+ Channels: T-type Ca2+ Channels and Drug Development

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

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Myocardial and vascular effects of efonidipine in vitro as compared with nifedipine, verapamil and diltiazem

Cited by 21 publications

References 17 publications

Clinical Efficacy of Efonidipine Hydrochloride, a T-type Calcium Channel Inhibitor, on Sympathetic Activities. Examination Using Spectral Analysis of Heart Rate/Blood Pressure Variabilities and 123I-Metaiodobenzylguanidine Myocardial Scintigraphy.

Clinical Efficacy of Efonidipine Hydrochloride, a T-type Calcium Channel Inhibitor, on Sympathetic Activities. Examination Using Spectral Analysis of Heart Rate/Blood Pressure Variabilities and 123I-Metaiodobenzylguanidine Myocardial Scintigraphy.

Pathophysiological Significance of T-type Ca2+ Channels: T-type Ca2+ Channels and Drug Development

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca2+ Channels

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Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels