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Lercanidipine
Tóm tắt
Lercanidipine (Zanidip®) là một chất đối kháng kênh canxi dihydropyridine chọn lọc mạch máu, gây giãn mạch toàn thân bằng cách chặn sự xâm nhập của ion canxi qua kênh canxi loại L trên màng tế bào. Đây là một loại thuốc có tính ưa lipit cao, khởi phát chậm và kéo dài hơn so với các chất đối kháng kênh canxi khác. Hơn nữa, lercanidipine có thể có hoạt động chống xơ vữa không liên quan đến tác dụng hạ huyết áp của nó. Trong hai nghiên cứu lớn, không mù, không so sánh bao gồm khoảng 16.000 bệnh nhân bị tăng huyết áp nhẹ đến trung bình, huyết áp tâm thu (SBP) và huyết áp tâm trương (DBP) đã giảm đáng kể sau 12 tuần điều trị với lercanidipine 10–20 mg/ngày. Trong nghiên cứu lớn nhất, 64% bệnh nhân đã cải thiện (DBP <90mm Hg) sau 12 tuần điều trị và thêm 32% bệnh nhân có huyết áp trở về bình thường (BP <140/90mm Hg). Trong các thử nghiệm so sánh, lercanidipine 10–20 mg/ngày có hiệu quả tương đương nifedipine phóng thích chậm (SR) 20–40 mg hai lần mỗi ngày, amlodipine 10 mg/ngày, felodipine 10–20 mg/ngày, nifedipine hệ thống điều trị đường tiêu hóa (GITS) 30–60 mg một lần mỗi ngày hoặc verapamil SR 240 mg/ngày trong việc giảm SBP và DBP ở bệnh nhân tăng huyết áp nhẹ đến trung bình sau 2–16 tuần điều trị. Ngoài ra, 4 tuần điều trị bằng lercanidipine (10 mg/ngày) có hiệu quả tương tự như captopril 25 mg hai lần một ngày, atenolol 50 mg/ngày hoặc hydrochlorothiazide 12.5 mg/ngày. Lercanidipine 5–30 mg/ngày giảm huyết áp một cách hiệu quả ở bệnh nhân cao tuổi (trên 60 tuổi) mắc tăng huyết áp nhẹ đến trung bình hoặc tăng huyết áp tâm thu đơn độc cũng đạt hiệu quả tương tự như amlodipine 5–10 mg/ngày, nifedipine GITS 30–60 mg/ngày hoặc lacidipine 2–4 mg/ngày sau 24–26 tuần điều trị. Bên cạnh đó, một số nghiên cứu hạn chế cho thấy lercanidipine có thể có hiệu quả hạ huyết áp ở những bệnh nhân mắc tăng huyết áp nặng hoặc chống lại liệu pháp, ở bệnh nhân tăng huyết áp mắc bệnh tiểu đường type 2 và ở phụ nữ mãn kinh có tăng huyết áp thiết yếu nhẹ đến trung bình. Lercanidipine được dung nạp tốt, với hầu hết các sự kiện bất lợi phát sinh từ quá trình điều trị liên quan đến giãn mạch. Các sự kiện bất lợi phổ biến bao gồm đau đầu, đỏ mặt và phù ngoại biên. Quan trọng là, tỷ lệ phù do giãn mạch thấp hơn đáng kể ở bệnh nhân dùng lercanidipine so với ở những người dùng một số chất đối kháng kênh canxi khác. Cuối cùng, lercanidipine một lần mỗi ngày là một tác nhân hạ huyết áp hiệu quả và được dung nạp tốt ở bệnh nhân tăng huyết áp nhẹ đến trung bình. Hơn nữa, trong một số ít các nghiên cứu, thuốc đã chứng minh hiệu quả ở những bệnh nhân có tăng huyết áp nặng hoặc kháng trị (như liệu pháp bổ sung), ở người cao tuổi và ở bệnh nhân mắc bệnh tiểu đường type 2. Quan trọng hơn, lercanidipine dường như có hiệu quả tương đương và ít nhất cũng được dung nạp tốt như nhiều chất đối kháng kênh canxi khác, nhưng có tỷ lệ phù giảm.
Từ khóa
#Lercanidipine #hạ huyết áp #giãn mạch #tăng huyết áp nhẹ đến trung bình #bệnh tiểu đường type 2Tài liệu tham khảo
Age-specific relevance of usual blood pressure to vascular mortality: a meta-analysis of individual data for one million adults in 61 prospective studies. Lancet 2002; 360: 1903–13
Burt VL, Whelton P, Roccella EJ, et al. Prevalence of hypertension in the US adult population: results from the third National Health and Nutrition Examination Survey, 1988–1991. Hypertension 1995; 25: 305–13
Colhoun HM, Dong W, Poulter NR. Blood pressure screening, management and control in England: results from the health survey for England 1994. J Hypertens 1998; 16: 747–52
Scriabine A. Seventeenth annual scientific meeting of the American Society of Hypertension, New York, NY, May 14–18, 2002. Cardiovasc Drug Rev 2002; 20(2): 153–61
McClellan KJ, Jarvis B. Lercanidipine: a review of its use in hypertension. Drugs 2000 Nov; 60(5): 1123–40
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; 7 Suppl. 2: 10–7
Leonardi A, Poggesi E, Taddei C, et al. In vitro calcium antagonist activity of lercanidipine and its enantiomers. J Cardiovasc Pharmacol 1997; 29 Suppl. 1: S10–8
Testa R, Rimoldi E, Sironi G, et al. Hemodynamic effects and power spectral analysis of heart rate and arterial pressure variabilities induced by lercanidipine and its enantiomers in conscious dogs. J Cardiovasc Pharmacol 1997; 29 Suppl. 1: S78–85
Meredith PA. Lercanidipine: a novel lipophilic dihydropyrindine calcium antagonist with long duration of action and high vascular selectivity. Exp Opin Invest Drugs 1999; 8(7): 1043–62
Sironi G, Colombo D, Greto L, et al. Antihypertensive activity of lercanidipine and its enantiomers in animal models. J Cardiovasc Pharmacol 1997; 29 Suppl. 1: S33–40
Guarneri L, Angelico P, Ibba M, et al. Pharmacological in vitro studies of the new 1,4-dihydropyridine calcium antagonist lercanidipine. Arzneimittel Forschung 1996; 46: 15–24
Angelico P, Guarneri L, Leonardi A, et al. Vascular-selective effect of lercanidipine and other 1,4-dihydropyridines in isolated rabbit tissues. J Pharm Pharmacol 1999; 51: 709–14
van der Lee R, Pfaffendorf M, van Zwieten PA. The differential time courses of the vasodilator effects of various 1,4-dihydropyridines in isolated human small arteries are correlated to their lipophilicity. J Hypertens 2000 Nov; 18(11): 1677–82
Ambrosioni E, Circo A. Activity of lercanidipine administered in single and repeated doses once daily as monitored over 24 hours in patients with mild to moderate essential hypertension. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S16–20
Macchiarulo C, Pieri R, Mitolo DC, et al. Antihypertensive effects of six calcium antagonists: evidence from Fourier analysis of 24-hour ambulatory blood pressure recordings. Curr Ther Res 2001; 62(4): 236–53
Omboni S, Zanchetti A. Antihypertensive efficacy of lercanidipine at 2.5, 5 and 10 mg in mild to moderate essential hypertensives assessed by clinic and ambulatory blood pressure measurements. J Hypertens 1998; 16 (Pt 1): 1831–8
Cavallini A, Terzi G. Effects of antihypertensive therapy with lercanidipine and verapamil on cardiac electrical activity in patients with hypertension: a randomized, double-blind pilot study. Curr Ther Res 2000 Jul; 61(7): 477–87
Barbagallo Sangiorgi G, Putignano E, Calcara L, et al. Efficacy and tolerability of lercanidipine vs. captopril in patients with mild to moderate hypertension in a double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S36–9
De Giorgio LA, Orlandini F, Malasoma P, et al. Double-blind, crossover study of lercanidipine versus amlodipine in the treatment of mild-to-moderate essential hypertension. Curr Ther Res 1999 Oct; 60(10): 511–20
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 Aug; 16(8): 605–10
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
Paterna S, Licata A, Arnone S, et al. Lercanidipine in two different dosage regimens as a sole treatment for severe essential hypertension. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S50–3
Rimoldi E, Lumina C, Giunta L, et al. Evaluation of the efficacy and tolerability of two different formulations of lercanidipine versus placebo after once-daily administration in mild to moderate hypertensive patients. Curr Ther Res 1993 Aug; 54(2): 248–53
Seravalle G, Stella ML, Foglia G, et al. Temporal profile of antihypertensive drug-induced regression of cardiac and vascular structural alterations in hypertension [abstract no. P0780]. J Hypertens 2002; 20 Suppl. 4: S190–1
Sánchez A, Sayans R, Alvarez JL, et al. Left ventricular hypertrophy regression after a short antihypertensive treatment with lercanidipine vs. enalapril [abstract no. 12]. Fourth European Meeting on Calcium Antagonists; 1999 Oct 27–29; Amsterdam
Fogari R, Mugellini A, Corradi L, et al. Efficacy of lercanidipine vs losartan on left ventricular hypertrophy in hypertensive type 2 diabetic patients [abstract no. P1.191]. J Hypertens 2000; 18 Suppl. 2: S65
Corsini A, Accomazzo MR, Canavesi M, et al. The new calcium antagonist lercanidipine and its enantiomers affect major processes of atherogenesis in vitro: is calcium entry involved? Blood Press 1998; 7 Suppl. 2: 18–22
Taddei S, Virdis A, Ghiadoni L, et al. Calcium antagonist treatment by lercanidipine prevents hyperpolarization in essential hypertension. Hypertension 2003; 41: 950–5
Rachmani R, Levi Z, Zadok BS, et al. Losartan and lercanidipine attenuate low-density lipoprotein oxidation in patients with hypertension and type 2 diabetes mellitus: a randomized, prospective crossover study. Clin Pharmacol Ther 2002 Sep; 72(3): 302–7
Incandela L, Belcaro G, Cesarone MR, et al. Oxygen-free radical decrease in hypertensive patients treated with lercanidipine. Int Angiol 2001 Jun; 20(2): 136–40
Soma MR, Natali M, Donetti E, et al. Effect of lercanidipine and its (R)-enantiomer on atherosclerotic lesions induced in hypercholesterolemic rabbits. Br J Pharmacol 1998; 125: 1471–6
Sabbatini M, Leonardi A, Testa R, et al. Effect of calcium antagonists on glomerular arterioles in spontaneously hypertensive rats. Hypertension 2000; 35: 775–9
Sabbatini M, Vitaioli L, Baldoni E, et al. Nephroprotective effect of treatment with calcium channel blockers in spontaneously hypertensive rats. J Pharmacol Exp Ther 2000; 294: 948–54
Kanda T, Hayashi K, Ozawa Y, et al. Role of T-type calcium channels as a determinant of glomerular microcirculation and subsequent renal protection [abstract no. P0170]. J Hypertens 2002 Jun; 20 Suppl. 4: S48
Notarbartolo A, Rengo F, Scafidi V, et al. Long-term effects of lercanidipine on the lipoprotein and apolipoprotein profile of patients with mild-to-moderate essential hypertension. Curr Ther Res 1999 Apr; 60(4): 228–36
Viviani GL. Lercanidipine in type II diabetic patients with mild to moderate arterial hypertension. J Cardiovasc Pharmacol 2002 Jul; 40(1): 133–9
Fogari R, Malamani GD, Zoppi A, et al. Comparative effect of lercanidipine and nifedipine gastrointestinal therapeutic system on ankle volume and subcutaneous interstitial pressure in hypertensive patients: a double-blind, randomized, parallel-group study. Curr Ther Res Clin Exp 2000 Dec; 61: 850–62
Lund-Johansen P, Stranden E, Helberg S, et al. Quantification of leg oedema in postmenopausal hypertensive patients treated with lercanidipine or amlodipine. J Hypertens 2003 May; 21(5): 1003–10
Harada N, Yamaguchi H, Shigematsu K, et al. Effects of lercanidipine, a novel calcium antagonist, on stroke-prone spontaneously hypertensive rats. SHR Congress; 1999 Aug 26–27; Sapporo, Japan
Amenta F, Leonardi A, Sabbatini M, et al. Glial-fibrillary acidic protein immunoreactive astrocytes in the brain of spontaneously hypertensive rats: sensitivity to pharmacological treatment [abstract]. 28th National Congress of the Italian Society of Histochemistry; 1999 Jun 2–4; Camerino, Italy
Guarneri L, Sironi G, Angelico P, et al. In vitro and in vivo vascular selectivity of lercanidipine and its enantiomers. J Cardiovasc Pharmacol 1997; 29 Suppl. 1: S25–32
Bianchi G, Passoni A, Griffini PL. Effects of a new calcium antagonist, REC 15/2375, on cardiac contractility of conscious rabbits. Pharmacol Res 1989; 21(2): 193–200
Grassi G, Seravalle G, Turri C, et al. Short-versus long-term effects of different dihydropyridines on sympathetic and baroreflex function in hypertension. Hypertension 2003 Mar; 41(3): 558–62
Fogari R, Mugellini A, Zoppi A, et al. Differential effects of lercanidipine and nifedipine GITS on plasma norepinephrine in chronic treatment of hypertension. Am J Hypertens 2003; 16(7): 596–9
Policicchio D, Magliocca R, Malliani A. Efficacy and tolerability of lercanidipine in patients with mild to moderate essential hypertension: a comparative study with slow-release nifedipine. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S31–5
Barbagallo M, Barbagallo Sangiorgi G. Efficacy and tolerability of lercanidipine in monotherapy in elderly patients with isolated systolic hypertension. Aging Clin Exp Res 2000 Oct; 12(5): 375–9
Romito R, Pansini MI, Perticone F, et al. Comparative effect of lercandipine, felodipine and nifedipine GITS on blood pressure and heart rate in patients with mild to moderate arterial hypertension: the Lercandipine in Adults (LEAD) study. J Clin Hypertens 2003; 5(4): 249–53
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(2): 95–100
Cominacini L, Fratta Pasini A, Garbin U, et al. Antioxidant activity of different dihydropyridines. Biochem Biophys Res Commun 2003 Mar 21; 302(4): 679–84
Lozano JV, Sanchis C, Llisterri JL. Efficacy of lercanidipine in poorly controlled hypertensive patients who follow a home blood pressure measurement training program [abstract no. R190]. J Hypertens 2002 Jun; 20 Suppl. 4: S376
Abellán Alemán J, Martínez García JF, Merino Sanchez J, et al. Evaluation of psychosomatic semiology in hypertensive patients treated with lercanidipine (LERCAPISCO study) [in Italian]. An Med Interna 2003; 20(6): 287–91
Sabbatini M, Leonardi A, Testa R, et al. Effects of dihydropyridine-type Ca2+ antagonists on the renal arterial tree in spontaneously hypertensive rats. J Cardiovasc Pharmacol 2002 Jan; 39(1): 39–48
Zanchetti A, Cifkova R, Fagard S, et al. 2003 European Society of Hypertension — European Society of Cardiology guidelines for the management of arterial hypertension. Guidelines Committee. Journal of Hypertension 2003; 21: 1011–53
Robles NR, Ocon J, Campdera FG, et al. Lercanidipine in chronic renal failure (CRF) [abstract no. P2.225]. J Hypertens 2003; 21 Suppl. 4: S185
Pedrinelli R, Dell'Omo G, Nuti M, et al. Heterogenous effect of calcium antagonists on leg oedema: a comparison of amlodipine versus lercanidipine in hypertensive patients. J Hypertens 2003; 21: 1969–73
Guillen VF, Abellan J, Llisterri JL, et al. Efficacy and safety of Lercanidipine in combination with Enalapril in HBP: preliminary results of ZANYCONTROL Study Group [abstract no. P.212]. Am J Hypertens 2003; 16 (5 Suppl. 1: 115A
Barchielli M, Dolfini E, Farina P, et al. Clinical pharmacokinetics of lercanidipine. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S1–15
Napp Pharmaceuticals Ltd. Zanidip tablets: SPC from the eMC [online]. Available from URL: http://emc.vhn.net/eMC/assets/c/html/DisplayDoc.asp?DocumentId=1234 [Accessed 2003 Oct 10]
Barchielli M, Leoni B, Perego R. Lercanidipine plasma levels monitoring in patients: pharmacokinetic contribution to the study Rec 15/2375-RIC1-0047: dose finding study with lercanidipine in angina pectoris. Double blind randomised multicentre trial. Milan: Recordati, 1999. (Data on file)
Klotz U. Interaction potential of lercanidipine, a new vasoselective dihydropyridine calcium antagonist. Arzneimittel Forschung 2002; 52(3): 155–61
Farina P, Tajana A, Barchielli M, et al. Effect of lercanidipine on CYP2D6 and CYP3A4 activities: in vitro/in vivo correlation [abstract]. 9th North American International Society for the Study of Xenobiotics Meeting; 1999 Oct 24–28; Nashville, TN
Hedner T, Everts B, Kraizci H, et al. Enhanced blood pressure lowering effect in hypertensive patients on combined sildenafil and lercanidipine treatment [abstract no. P3.52]. 10th European Meeting on Hypertension; 2000 May 29–Jun 3; Goteborg, Sweden
Schwinger RHG, Schmidt-Mertens A. The new lipophillic calcium channel blocker lercanidipine combines high antihypertensive efficacy with low side effects [abstract no. P1-7]. Dtsch Med Wochenschr 2002; 127 Suppl. 1: S13
Calvo C, Hermida R, Navarro A. Results from the ZANyCAL study on the treatment of elderly hypertensive patients [abstract no. P343]. Cardiovasc Drugs Ther 2002 May; 16 Suppl. 1: 57
Roma J, Sobrino J, Plana J, et al. Treatment with lercanidipine during six months in hypertensive elderly patients (more than 60 years) [abstract no. R268]. J Hypertens 2002 Jun; 20 Suppl. 4: S391
Leonetti G, Magnani B, Pessina AC, et al. Tolerability of long-term treatment with lercanidipine versus amlodipine and lacidipine in elderly hypertensives. Am J Hypertens 2002 Nov; 15(11): 932–40
Ninci MA, Magliocca R, Malliani A. Efficacy and tolerability of lercanidipine in elderly patients with mild to moderate hypertension in a placebo-controlled, double-blind study. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S40–4
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 LEcandipine (ELLE) study. Arch Gerontol Geriatr 2003; 37: 203–12
Rengo F, Romis L. Activity of lercanidipine in double-blind comparison with nitrendipine in combination treatment of patients with resistant essential hypertension. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S54–8
A multicenter randomized, double-blind trial of the efficacy and safety of lercanidipine in patients with mild to moderate essential hypertension, uncontrolled on hydrochlorothiazide. Milan: Recordati S.p.A, 2000. (Data on file)
Cafiero M, Giasi M. Long-term (12-month) treatment with lercanidipine in patients with mild to moderate hypertension. J Cardiovasc Pharmacol 1997; 29 Suppl. 2: S45–9
Luque M, Ruilope LM, Tamargo J, et al. Drug surveillance study in patients with mild to moderate hypertension treated with lercanidipine: the Zanyten study [abstract no. P068]. J Hypertens 2002 Jun; 20 Suppl. 4: S163
Herrera J, Ghais Z, Gonzalez L. Antihypertensive treatment with a calcium channel blocker in postmenopausal women: prospective study in a primary health care setting [abstract no. P0680]. J Hypertens 2002 Jun; 20 Suppl. 4: S162
Leonetti G. The safety profile of antihypertensive drugs as the key factor for the achievement of blood pressure control: current experience with lercanidipine. High Blood Press 1999; 8: 92–101
Borghi C, Prandin MG, Dormi A, et al. Improved tolerability of the dihydropyridine calcium-channel antagonist lercanidipine: the lercanidipine challenge trial. Blood Press 2003; 12 Suppl. 1: 1–8
Ramsay LE, Williams B, Johnston GD, et al. British Hypertension Society guidelines for hypertension management 1999: summary. BMJ 1999 Sep 4; 319: 630–5
Chobanian AV, Bakris GL, Black HR, et al. The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation and Treatment of High Blood Pressure. JAMA 2003; 289(19): 2560–75
Staessen JA, Wang J-G, Thijs L. Cardiovascular prevention and blood pressure reduction: a quantitative overview updated 1 March 2003. J Hypertens 2003; 21: 1055–76
Sheinfeld GR, Bakris GL. Benefits of combination angiotensin-converting enzyme inhibitor and calcium antagonist therapy for diabetic patients. Am J Hypertens 1999; 12: 80S–5S
Alderman M, Arakawa K, Beilin L, et al. 1999 World Health Organization — International Society of Hypertension Guidelines for the Management of Hypertension. Guidelines Sub-Committee. Blood Press 1999; 8 Suppl. 1: 9–43
Hansson L, Hedner T, Lund-Johansen P, et al. Randomised trial of effects of calcium antagonists compared with diuretics and β-blockers on cardiovascular morbidity and mortality in hypertension: the Nordic Diltiazem (NORDIL) study. Lancet 2000; 356: 359–65
Black HR, Elliot WJ, Grandits G, et al. Principal results of the Controlled Onset Verapamil Investigation of Cardiovascular Endpoints (CONVINCE) trial [abstract]. JAMA 2003; 289(16): 2073–82