Delving into the Latest Updates on Lercanidipine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Carmen, Corifeo, Lercadip

+ [25]

Target

Cav2.1

Mechanism

Cav2.1 inhibitors(calcium voltage-gated channel subunit alpha1 A inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Meda AB

Active Organization

Recordati SpA

Gador SA

Orient Europharma Co. Ltd.

+ [11]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

SE (28 Mar 1998),

Hypertension

RegulationPriority Review (CN)

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Structure

Molecular FormulaC36H42ClN3O6

InChIKeyWMFYOYKPJLRMJI-UHFFFAOYSA-N

CAS Registry132866-11-6

Lercanidipine in reducing doxorubicin-induced neuroinflammation and maintaining the expressions of choline acetyltransferase. Thirty-two adult Wistar albino female rats were divided into four groups as Control, DOX (20 mg/kg intraperitoneally), DOX + LRD 0.5 (0.5 mg/kg orally), and DOX + LRD2(2 mg/kg orally). Twenty-four hours after the last drug administration (9th day), brain tissues were taken for histopathological, immunohistochemical (choline acetyltransferase [CHAT], interleukin-10 [IL-10], and caspase-3 [Cas-3] staining), biochemical (total antioxidant status [TAS], total oxidant status [TOS], and oxidative stress index [OSI]), and genetic analyzes (PI3K/AKT/HIF1-α and IL-6 gene expressions). Histopathological analyses revealed hyperemia, slight hemorrhage, degeneration, neuronal loss, gliosis in the cerebellum, and neuronal loss in the brain cortex and hippocampus in the DOX group. According to other analyzes, decreased CHAT, PI3K, AKT, HIF1-α and increased IL-6, IL-10, Cas-3 expression were observed in the DOX group.

CONCLUSIONS:

Both LRD doses reversed all these findings, but LRD2 was observed to be more effective. In conclusion, we determined that LRD has potential therapeutic effect by reducing DOX-induced neuroinflammation, oxidative stress and apoptosis in brain tissues.

01 Nov 2024·European journal of hospital pharmacy : science and practice

Evaluation of drug interaction between cyclosporine and lercanidipine: a descriptive study

Article

Author: Tecen-Yucel, Kamer ; Erdem, Yunus ; Yıldırım, Tolga ; Bayraktar-Ekincioglu, Aygin ; Demirkan, Kutay

OBJECTIVES:

Cyclosporine is an immunosuppressive drug with a high potential for drug interactions that is frequently used in renal transplant patients. The purpose of this study was to assess the change in cyclosporine concentration in patients taking cyclosporine and lercanidipine concurrently.

METHODS:

The potential drug interactions in renal transplant patients who received lercanidipine and cyclosporine concurrently in a university hospital between January 2008 and January 2018 were evaluated retrospectively. Patients had renal transplantation from deceased donors or living related donors. The Drug Interaction Probability Scale (DIPS) criteria were used to assess the causality of cyclosporine and lercanidipine drug interaction.

RESULTS:

The study included six renal transplant patients. The median cyclosporine concentration before lercanidipine use was 325 ng/mL (min-max 101-356) and 592.5 ng/mL (min-max 198-799) thereafter (p=0.028). Serum creatinine and proteinuria levels did not change significantly during lercanidipine treatment (p=0.686 and p=0.116, respectively). According to the DIPS evaluation, cyclosporine and lercanidipine interaction was classified as "possible (score 3)".

CONCLUSIONS:

Concomitant use of cyclosporine and lercanidipine increases the concentration of cyclosporine, which may result in side effects during effective treatment in renal transplant patients. Therefore, cyclosporine concentrations should definitely be monitored while patients are taking lercanidipine.

13 Jul 2024·Cureus Journal of Medical Science

Unveiling the Preparation and Characterization of Lercanidipine Hydrochloride in an Oral Solid Self-Nanoemulsion for Enhancing Oral Delivery

Article

Author: Abdul Hussein, Haneen M ; Ghareeb, Mowafaq M

INTRODUCTION:

Chronic kidney disease (CKD) is becoming increasingly prevalent worldwide, particularly among the elderly, along with an increase in the incidence of hypertension and cardiovascular disorders. Developing lipid-based oral dosage forms with a higher expected bioavailability of antihypertensive drugs with nephroprotective effects poses a challenge. Lercanidipine hydrochloride (LRCH) is a newer type of third-generation dihydropyridine calcium channel blocker that functions as an antihypertensive and has significant nephroprotective effects. Due to its extensive first-pass metabolism, its bioavailability is about 10% and increases to 3-4 times when taken with a high-fat meal. Targeting this drug to the lymphatic system using the solid self-nano-emulsifying drug delivery system (SSNEDDS) is a promising approach for improving LRCH's bioavailability and dispersion rate. SSNEDDS combines the benefits of both liquid self-emulsifying and solid dosage forms, improving drug stability and extending storage time.

MATERIALS AND METHODS:

In this study, liquid SNEDDS composed of 10% peppermint oil, 67% Tween 20, and 22.5% propylene glycol was solidified using two adsorbent agent mixtures (SSNEDDS1: Avicel PH 101 and Aerosil 200) and (SSNEDDS2: Avicel PH 102 and Aerosil 200) separately. The prepared formulations were evaluated for powder flow, drug content, and an in-vitro dispersion test in comparison to the brand-marketed tablet as a standard or pure drug. DSC and X-ray diffraction analysis were also used.

RESULTS:

The SSNEDDS2 shows excellent flowability, a higher drug content (99.761%), and a significantly higher and faster dispersion rate of 100% within 10 minutes compared to 92% of the marketed LRCH tablet and 18.1% of the pure drug for 60 minutes. The solid-state characterization of the formulation composed of SSNEDDS2 confirmed that the LRCH was in an amorphous form inside the solidified nano system without interacting with the excipient.

CONCLUSION:

This study successfully prepared LRCH using the promising strategy of SSNEDDS as a hard gelatin capsule with a higher dispersion rate. It improved its stability and expected bioavailability compared to the brand-marketed tablet as the standard.

100 Deals associated with Lercanidipine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D01849	Lercanidipine Hydrochloride	C08CA13	DB00528

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	SE	Meda AB	28 Mar 1998

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01093807 (Pubmed \| J Hypertens)	Phase 2	Hypertension	1,039	Placebo	iyjyvrvroy(mczokuqtxx) = athsyxoaop uhwkoighig (prjqawypwf ) View more	-	01 Jan 2016
				Lercanidipine 10mg	iyjyvrvroy(mczokuqtxx) = vqeakjjjrk uhwkoighig (prjqawypwf ) View more