Neuroprotective Effect of Lercanidipine- A Novel Calcium Channel Blocker in Albino Mice

Selvaraj, Nitya; Adhimoolam, Mangaiarkkarasi; Perumal, Deepa Kameswari; Rajamohammed, Meher Ali

doi:10.7860/jcdr/2015/14085.6801

Cited by 5 publications

(7 citation statements)

References 17 publications

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“…İlacın farelerde kas koordinasyonunu ya da lokomotor aktiviteyi etkilemediği de kaydedilmiştir. Lerkanidipinin olumlu nöroprotektif etkisi nedeniyle, konvülsiyonların tedavisinde, potansiyel bir aday olabileceği vurgulanmaktadır 67 .…”

Section: Finansal çıKar çAkışmasıunclassified

Pleiotropic Effects of Calcium Channel Blockers

Canbolat¹,

Atalık²

2019

Kafkas J Med Sci

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Calcium channel blockers are a group of drugs that commonly prescribed to treat cardiovascular disorders such as; hypertension, angina pectoris, peripheral vascular disorders and some arrhythmias. Calcium channel blockers, particularly the newer, longer-acting agents, are clearly effective in reducing elevated blood pressure with minimal to modest adverse effect profiles, therefore they are used extensively. These drugs reduce the amount of calcium entering cells of the heart and blood vessel walls, and they cause vasodilatation especially in arterioles. These drugs commonly block L-type of voltagegated calcium channels. Recent studies have shown that some calcium channel blockers also bind to N-and T-type channels. N-type channels are located in high amounts at the presynaptic terminals of neurons. T-type calcium channels known to be present in cardiac and smooth muscle, and also in many neuronal cells in the central nervous system. Blockage of these two types of channels leads to decreased glomerular capillary pressures, stabilization of the reninangiotensin-aldosterone system, and sympathetic nervous system. As a result, especially new generation of calcium channel blockers have effects that are defined as pleiotropic effects, such as reno-protective, vascular endothelial protective and cardio-protective effects.ÖZET Kalsiyum kanal blokerleri, hipertansiyon, angina, periferik vasküler bozukluklar ve bazı aritmiler gibi kardiyovasküler hastalıkların tedavisinde yaygın olarak kullanılan bir ilaç grubudur. Kalsiyum kanal blokerlerinden özellikle daha yeni, daha uzun etkili olanlar, daha düşük yan etki profilleri ile hipertansiyon tedavisinde oldukça etkilidir. Bu ilaçlar, damar düz kası ve kalp hücrelerinde, sitoplazma membranındaki voltaj-bağımlı kalsiyum kanallarına veya reseptörlere yüksek afinite ile bağlanarak kalsiyum girişini azaltırlar, özellikle arteriyollerde düz kasları gevşeterek güçlü vazodilatasyon yaparlar. Voltaj-bağımlı kalsiyum kanallarının çoğunlukla L-tipine bağlanırlar. Yakın zamanda yapılan çalışmalar, bazı kalsiyum kanal blokerlerinin N-ve T-tipi kanallara da bağlandığını göstermiştir. Bunlardan N-tipi kanallar sempatik sinir uçlarında, T-tipi kanallar ise kardiyak sinus nodu ile afferent ve efferent arteriyollerde bulunur. Bu iki tip kanalın blokajı, glomerüler kapiller basıncın azalmasına, renin-anjiotensin-aldosteron sisteminin ve sempatik sinir sisteminin stabilizasyonuna neden olur. Sonuçta, özellikle yeni jenerasyon kalsiyum kanal blokerleri, renoprotektif, vasküler endotel koruyucu etki ve kardiyoprotektif etkiler gibi pleiotropik etkiler olarak tanımlananan etkilere sahiptirler.

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Section: Finansal çıKar çAkışmasıunclassified

Pleiotropic Effects of Calcium Channel Blockers

Canbolat¹,

Atalık²

2019

Kafkas J Med Sci

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“…The newer generation dihydropyrine calcium antagonist lercanidipine is found to overcome these drawbacks and already had been proven for its effect on acute models of epilepsy. 10 Comparing the acute animal models of epilepsy, the data obtained from chronic models gives the more predictive validity of the drug tested and henceforth false positive errors are minimized. 11 Moreover chronic models reflect the processes underlying human epilepsy.…”

Section: +mentioning

confidence: 99%

“…Dose calculation for lercanidipine and diazepam were based on earlier published reports. 10 Fresh solution of lercanidipine was made in 99.9% HPLC grade methanol. Diazepam and pentylenetetrazole were dissolved in normal saline and distilled water respectively.…”

Section: Chemicals and Drugsmentioning

confidence: 99%

Anticonvulsant effect of lercanidipine against pentylenetetrazole induced kindling in mice

Selvaraj

Kameswari²,

Gandhi

et al. 2017

Int J Basic Clin Pharmacol

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Background: Emerging evidence has demonstrated the role of high-voltage -sensitive activated dihydropyridine (L-type, CaV1.x) channels in the development of epilepsy. Based on that we hypothesized that lercanidipine, a dihydropyridine calcium channel blocker, would protect against Pentylenetetrazole (PTZ) induced kindling in mice model of epilepsy.Methods: Kindling was induced in Swiss albino mice with PTZ in subconvulsive dose (30 mg/kg i.p.) thrice a week for nine weeks and the effect was scored using ‘4 point scoring system’. Rechallenging on the 3rd and 10th day with the same dose of PTZ was carried out after the last chronic dose.Results: The data of the present study demonstrated that pretreatment with lercanidipine (½ h before PTZ, in doses of 1 and 3 mg/kg i.p. daily) alone and in combination with diazepam (2mg/kg i.p.) had decreased the incidence and severity of seizure as well as prolonged the onset of kindling in a dose-dependent manner (p <0.05). On rechallenging, lercanidipine resulted in reduction of seizure score (p <0.05) and increased the seizure latency.Conclusions: The present study suggested that lercanidipine offered neuroprotection against PTZ induced kindling in mice.

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“…Compared to similar CCBs, it has a longer duration of action and greater lipophilicity. [ 2 , 3 ] Its stable pharmacokinetics, minimal side effects, high tolerability, and safety profile make it a suitable candidate for use in a wide variety of populations. [ 3 ]…”

Section: Introductionmentioning

confidence: 99%

Effects of lercanidipine on traumatic spinal cord injury: an experimental study

Türk

2024

Ulus Travma Acil Cerrahi Derg

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BACKGROUND: Spinal cord injury is a devastating trauma that leaves survivors at risk for several medical complications throughout their lives. Lercanidipine, a third-generation calcium channel blocker, possesses anti-apoptotic, anti-inflammatory, and antioxidative properties. This study aimed to evaluate the neuroprotective effects of lercanidipine in an experimental spinal cord trauma model. METHODS: Twenty-one Wistar rats were randomly assigned to three groups. Group 1 (G1) underwent laminectomy. Group 2 (G2) were subjected to trauma following laminectomy. Group 3 (G3) were exposed to trauma following laminectomy and treated with lercanidipine. Lercanidipine was administered intraperitoneally for seven days. Histopathological and immunohistochemical evaluations were conducted. RESULTS: Regarding Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) staining, there was no significant difference among the groups. However, nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) levels were significantly different across the groups. G2 had significantly higher NF-κB levels compared to G1 and G3. CONCLUSION: Lercanidipine, a third-generation calcium channel blocker, is effective against inflammatory responses induced in spinal cord injury. Further studies are required to determine its capability in preventing apoptosis or improving functional recovery. To the best of our knowledge, this study is the first in the literature to examine the neuroprotective effects of lercanidipine on spinal cord injury.

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Neuroprotective Effect of Lercanidipine- A Novel Calcium Channel Blocker in Albino Mice

Cited by 5 publications

References 17 publications

Pleiotropic Effects of Calcium Channel Blockers

Pleiotropic Effects of Calcium Channel Blockers

Anticonvulsant effect of lercanidipine against pentylenetetrazole induced kindling in mice

Effects of lercanidipine on traumatic spinal cord injury: an experimental study

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