Современную медицину трудно представить без надежных и безопасных лекарственных средств. Зачастую нежелательные лекарственные реакции являются поводом для отмены средства, которое в целом эффективно. Так, у дигидропиридиновых блокаторов кальциевых каналов основными нежелательными лекарственными реакциями, служащими поводом для отмены данных препаратов, являются отеки голеней и тахикардия. Лерканидипин – относительно новый представитель данного класса, это высоколипофильное соединение, которое долго ингибирует кальциевые каналы L-типа благодаря сохранению высокой внутримембранной концентрации. В обзоре представлены данные об эффективности и безопасности лерканидипина, а также о его плейотропных свойствах.
It is hard to imagine modern medicine without safe drugs (D). Often, adverse drug reactions (ADR) are the reason for drug with drawal, which is quite effective as a whole. The main dihydropyridine calcium channel antagonists (DCCA) ADR are the edema of shin and tachycardia, causing this drug with drawal. Lercanidipine is aquite new member of this class; it is a highly lipophilic compound, which blocking the influx of calcium ions through L-type calcium channels, by maintaining the high intramembrane concentration. This review provides the data on the efficacy and safety of lercanidipine and its pleiotropic features.
1. Grundy JS, Foster RT. The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties. Clin Pharmacokinet 1996; 30 (1): 28–51.
2. Epstein M. Lercanidipine: a novel dihydropyridine calcium channel blocker. Heart Disease 2001; 3: 398–407.
3. Herbette LG, Vecchiarelli M, Sartani A et al. Lercanidipine: short plasma half-life, long duration of action and high cholesterol tolerance. Updated molecular model to rationalize its pharmacokinetic properties. Blood Press 1998; Suppl. 2: 10–7.
4. Vasigar P, Batmanabane M. Anti-inflammatoryactivity of calciumchannel blocker lercanidipine hydrochloride. J Pharmacol Pharmacother 2013; 4 (4): 238–42.
5. Barrios V, Navarro A, Esteras A et al. Antihypertensive efficacy and tolerability of lercanidipine in daily clinical practice. The ELYPSE study. Blood Press 2002; 11: 95–100.
6. James IGV, Jones A, Davies P. A randomised, double-blind, double-dummy comparison of the efficacy and tolerability of lercanidipine tablets and losartan tablets in patients with mild to moderate essential hypertension. J Hum Hypertens 2002; 16: 605–1.
7. Morisco C, Trimarco B. Efficacy and tolerability of lercanidipine in comparison to and in combination with atenolol in patients with mild to moderate hypertension in a double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S26–30.
8. Cherubini A, Fabris F, Ferrari E et al. Comparative effects of lercanidipine, lacidipine and nifedipine gastrointestinal therapeutic system on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Arch Gerontol Geriatr 2003; 37: 203–12.
9. Pedrinelli R, Dell’Omo G, Nuti M et al. Heterogeneous effect of calcium antagonists on leg oedema: a comparison of amlodipine versus lercanidipine in hypertensive patients. J Hypertens 2003; 21: 1969–73.
10. Fogari R, Malamani GD, Zoppi A et al. Comparative effect of lercanidipine and nifedipine gastrointestinal therapeutic system on ankle volume and subcutanous interstitial pressure in hypertensive patients: a double-blind, randomised, parallel-group study. Curr Ther Res Clin Exp 2000; 61: 850–62.
11. Makarounas-Kirchmann K, Glover-Koudounas S, Ferrari P. Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers. Clin Ther 2009; 31 (8): 1652–63.
12. Robles NR, Ocon J, Gomez CF et al. Lercanidipine in patients with chronic renal failure: the ZAFRA study. Ren Fail 2005; 27 (1): 73–80.
13. Robles NR, Romero B et al. Treatment of Proteinuria with Lercanidipine Associated with Renin-Angiotensin Axis-Blocking Drugs. Ren Fail 2010; 32 (2): 192–7.
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1. Grundy JS, Foster RT. The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties. Clin Pharmacokinet 1996; 30 (1): 28–51.
2. Epstein M. Lercanidipine: a novel dihydropyridine calcium channel blocker. Heart Disease 2001; 3: 398–407.
3. Herbette LG, Vecchiarelli M, Sartani A et al. Lercanidipine: short plasma half-life, long duration of action and high cholesterol tolerance. Updated molecular model to rationalize its pharmacokinetic properties. Blood Press 1998; Suppl. 2: 10–7.
4. Vasigar P, Batmanabane M. Anti-inflammatoryactivity of calciumchannel blocker lercanidipine hydrochloride. J Pharmacol Pharmacother 2013; 4 (4): 238–42.
5. Barrios V, Navarro A, Esteras A et al. Antihypertensive efficacy and tolerability of lercanidipine in daily clinical practice. The ELYPSE study. Blood Press 2002; 11: 95–100.
6. James IGV, Jones A, Davies P. A randomised, double-blind, double-dummy comparison of the efficacy and tolerability of lercanidipine tablets and losartan tablets in patients with mild to moderate essential hypertension. J Hum Hypertens 2002; 16: 605–1.
7. Morisco C, Trimarco B. Efficacy and tolerability of lercanidipine in comparison to and in combination with atenolol in patients with mild to moderate hypertension in a double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S26–30.
8. Cherubini A, Fabris F, Ferrari E et al. Comparative effects of lercanidipine, lacidipine and nifedipine gastrointestinal therapeutic system on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Arch Gerontol Geriatr 2003; 37: 203–12.
9. Pedrinelli R, Dell’Omo G, Nuti M et al. Heterogeneous effect of calcium antagonists on leg oedema: a comparison of amlodipine versus lercanidipine in hypertensive patients. J Hypertens 2003; 21: 1969–73.
10. Fogari R, Malamani GD, Zoppi A et al. Comparative effect of lercanidipine and nifedipine gastrointestinal therapeutic system on ankle volume and subcutanous interstitial pressure in hypertensive patients: a double-blind, randomised, parallel-group study. Curr Ther Res Clin Exp 2000; 61: 850–62.
11. Makarounas-Kirchmann K, Glover-Koudounas S, Ferrari P. Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers. Clin Ther 2009; 31 (8): 1652–63.
12. Robles NR, Ocon J, Gomez CF et al. Lercanidipine in patients with chronic renal failure: the ZAFRA study. Ren Fail 2005; 27 (1): 73–80.
13. Robles NR, Romero B et al. Treatment of Proteinuria with Lercanidipine Associated with Renin-Angiotensin Axis-Blocking Drugs. Ren Fail 2010; 32 (2): 192–7.
Авторы
Г.С.Аникин
ГБОУ ВПО Первый Московский государственный медицинский университет им. И.М.Сеченова Минздрава России;
ФГБУ Поликлиника №3 Управления делами Президента РФ