111011-63-3

Usage

Uses

Used in Pharmaceutical Industry:
Efonidipine is used as an antihypertensive medication for the treatment of high blood pressure. Its dual mechanism of action, targeting both L-type and T-type calcium channels, makes it highly effective in lowering blood pressure and reducing the risk of complications associated with hypertension.
Used in Cardiovascular Health:
Efonidipine is used to improve cardiovascular health by relaxing the blood vessels, allowing blood to flow more easily and reducing the strain on the heart. This helps in managing and preventing the progression of hypertension and its associated complications, such as heart disease, stroke, and kidney damage.
Used in Combination Therapy:
Efonidipine can be prescribed in combination with other antihypertensive drugs to enhance the overall effectiveness of blood pressure management. This combination therapy may be beneficial for patients who require additional support in controlling their blood pressure levels.
Used in Oral Medication:
Efonidipine is typically taken orally, making it a convenient and accessible option for patients with high blood pressure. Its oral administration allows for easy incorporation into daily routines and helps ensure consistent medication adherence.

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Related news

Original contributionEffect of EFONIDIPINE (cas 111011-63-3) and ACE inhibitors on proteinuria in human hypertension with renal impairment08/29/2019

BackgroundAlthough several lines of recent studies fail to demonstrate the beneficial action of calcium antagonists, a novel dihydropyridine efonidipine, which possesses dilatory action of both afferent and efferent arterioles and, therefore, shares the renal microvascular action with angiotensi...detailed

Full PaperEffect of EFONIDIPINE (cas 111011-63-3) on TGF-β1–Induced Cardiac Fibrosis Through Smad2-Dependent Pathway in Rat Cardiac Fibroblasts08/28/2019

.Transforming growth factor beta-1 (TGF-β1) plays a critical role in progression of cardiac fibrosis, which may involve intracellular calcium change. We examined effects of efonidipine, a dual T-type and L-type calcium channel blocker (CCB), on TGF-β1–induced fibrotic changes in neonatal rat ...detailed

Effects of the iron chelator deferiprone and the T-type calcium channel blocker EFONIDIPINE (cas 111011-63-3) on cardiac function and Ca2+ regulation in iron-overloaded thalassemic mice08/26/2019

Although disturbance of cardiac Ca2+ regulation is involved in the pathophysiology of iron-overload cardiomyopathy, the obvious mechanisms involved in the dysregulation of iron-induced cardiac Ca2+ are unclear. Moreover, the roles of the iron chelator deferiprone and the T-type calcium channel b...detailed

The Ca2 + channel inhibitor EFONIDIPINE (cas 111011-63-3) decreases voltage-dependent K+ channel activity in rabbit coronary arterial smooth muscle cells08/25/2019

The effect of efonidipine, a commercially available antihypertensive drug and Ca2 + channel inhibitor, on voltage-dependent K+ (Kv) channels was studied in freshly isolated rabbit coronary arterial smooth muscle cells using the whole-cell patch clamp technique. The amplitude of Kv current was de...detailed

A chiral LC–MS/MS method for the stereospecific determination of EFONIDIPINE (cas 111011-63-3) in human plasma08/24/2019

Efonidipine hydrochloride is a new generation dihydropyridine Ca2+ channel blocker designed to inhibit both T-type and L-type Ca2+ channels. Efonidipine possesses a chiral carbon and is clinically administered as a racemate. In the present study, an enantioselective and sensitive LC–MS/MS metho...detailed

Determination of EFONIDIPINE (cas 111011-63-3) in human plasma by LC–MS/MS for pharmacokinetic applications08/23/2019

Efonidipine hydrochloride is a new generation dihydropyridine calcium channel blocker designed to inhibit both T-type and L-type calcium channels. For the first time, a simple and robust LC–MS/MS method was developed for the determination of efonidipine in human plasma over the range of 0.100–...detailed

Research paperIncreased bioavailability of EFONIDIPINE (cas 111011-63-3) hydrochloride nanosuspensions by the wet-milling method08/22/2019

The aim of this study was to improve the oral bioavailability of a practically insoluble drug, efonidipine hydrochloride (EFH), by agglomeration in acid solution/gastric fluid. The EFH nanosuspension was prepared by the wet-milling method with F68 as a dispersing agent, SDS as an auxiliary stabi...detailed

Relevant academic research and scientific papers

THERAPY FOR COMPLICATIONS OF DIABETES

A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.

ANTIHYPERTENSIVE THERAPY

A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.

Method for treating resistant hypertension

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Synthesis of 1,4-dihydropyridine-5-phosphonates and their calcium-antagonistic and antihypertensive activities

The effect of the 3-carboxylic-ester variation in 2,2-dimethyltrimethylene 3-alkoxycarbonyl-4-aryl-1,4-dihydro-2,6-dimethyl-5-pyridinephosphonate s (1) was investigated with relation to the calcium-antagonistic and antihypertensive activities: the analogs containing the alkyl groups of not more than 12 carbons and an amino functionality in the carboxylic-ester moiety were synthesized to be examined for biological activities. Among them, 2-[benzyl(phenyl)amino]-ethyl 5-(5,5-dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-di methyl-4-(3-nitrophenyl)-3-pyridine-carboxylate hydrochloride ethanol (NZ-105) showed particularly beneficial activities and was selected for further pharmacological studies and clinical development. Some aspects of the structure-activity relationships and solid-state structure of NZ-105 by X-ray crystallographic analysis were described.