生物活性

• 描述Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. However, nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension^[3]. Lercanidipine is a lipophilic third-generation DHP-CCB (Dihydropyridine-Calcium channel blocker), characterized by high vascular selectivity and persistence in the smooth muscle cell membranes. Lercanidipine prevents renal damage induced by angiotensin II and demonstrates anti-inflammatory, antioxidant, and anti-atherogenic properties through an increasing bioavailability of endothelial nitric oxide. It is associated with a regression of microvascular structural modifications in hypertensive patients. Lercanidipine produces a sustained blood pressure-lowering activity with a high rate of responder/normalized patients, associated with a favorable tolerability profile^[4]. Lercanidipine and lercanidipine/enalapril for stage 1 or 2 hypertension highly improves office SBP and DBP, overall 24-hour BP (blood pressure), daytime BP, and nighttime BP, also reducing BPV (BP variability) with few adverse effects^[5]. Lercanidipine was associated with a lower risk of peripheral edema and a lower risk of treatment withdrawal because of peripheral edema than were the first-generation, but not the second-generation, dihydropyridine CCBs^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00741585	Essential Hypertension ... more >> Cardiovascular Disease Stroke Chronic Kidney Disease Collapse <<	Phase 4	Completed	-	Spain ... more >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 Collapse <<
  NCT01180413	Essential Hypertension ... more >> High Blood Pressure Collapse <<	Phase 4	Completed	-	Denmark ... more >> Aarhus University Hospital - dept. cardiology (A) Aarhus, Denmark, 8000 Collapse <<
  NCT00424801	Microvascular Angina ... more >> Hypertension Collapse <<	Not Applicable	Terminated(Due to recent findi... more >>ngs relating MRI contrast to nephrogenic systemic fibrosis) Collapse <<	December 2008	Denmark ... more >> Aarhus Hospital Aarhus, Denmark, 8000 Collapse <<

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• 参考文献

• [1] Tawakkol S M, Farouk M, et al. Stability Study of the Calcium Channel Blocker Lercanidipine and its Determination by Reversed Phase Chromatography in Pharmaceutical Formulation and Plasma[J] . Analytical Chemistry Letters, 2014, 4(4):255-266.

  [2] Canavesi M, Baldini N, et al. In vitro inhibitory effect of lercanidipine on cholesterol accumulation and matrix metalloproteinases secretion by macrophages. J Cardiovasc Pharmacol. 2004 Oct;44(4):416-22.

  [3] Ranpise NS, Korabu SS, Ghodake VN. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride. Colloids Surf B Biointerfaces. 2014; 116:81‐87

  [4] Grassi G, Robles NR, Seravalle G, Fici F. Lercanidipine in the Management of Hypertension: An Update. J Pharmacol Pharmacother. 2017; 8(4):155‐165

  [5] Rayner B. The effect of lercanidipine or lercanidipine/enalapril combination on blood pressure in treatment-naïve patients with stage 1 or 2 systolic hypertension. Pragmat Obs Res. 2019;10:9‐14. Published 2019 Jan 22

  [6] Makarounas-Kirchmann K, Glover-Koudounas S, Ferrari P. Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers [published correction appears in Clin Ther. 2010 Feb;32(2):401-2]. Clin Ther. 2009; 31(8):1652‐1663

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