Lercanidipine is a calcium channel blocker that block the entry of calcium into the muscle cells of the blood vessels that carry blood away from the heart (the arteries). It is the entry of calcium into these cells that causes the arteries to narrow. By blocking the entry of calcium, Lercanidipine dilates (widen) the arteries, and the blood pressure is reduced.
 BRAND NAMES
- Australia: Zanidip, Lercan
- France: Lercan
- International: Zanidip
- Italy: Cardiovasc, Lercadip, Zanedip
- New Zealand: Zanidip PI
- Other brand names: Carbimen
 MECHANISM OF ACTION
Lercanidipine is a dihydropyridine calcium channel blocker with predominant selectivity on calcium channels in vascular smooth muscle than on cardiac smooth muscle. Lercanidipine inhibits the influx of extra cellular calcium across the peripheral arterial smooth muscle cell membranes by binding directly to inactive L-type calcium channels, stabilizing their inactive conformation.
The decrease in intracellular calcium inhibits the contractile processes of the systemic arteries smooth muscle cells, and thus, decreases total peripheral resistance and systemic blood pressure.
Since the vasodilatation induced by lercanidipine hydrochloride is gradual in onset, acute hypotension with reflex tachycardia has rarely been observed in hypertensive patients.
- Treatment of mild to moderate hypertension
- Adults: The usual dose is one 10 mg tablet daily, preferably in the morning at least 15 minutes before breakfast, because a high fat meal significantly increases blood levels of the drug. The dose may be increased to one 20 mg tablet daily, if needed. Dose titration should be gradual, because it may take about 2 weeks before the maximal antihypertensive effect is apparent.
- Elderly: No adjustment of the daily dose is required. However, special care should be exercised in starting treatment
- Hypersensitivity to Lercanidipine or to any dihydropyridine
- Severe hepatic impairment
- Severe renal impairment (creatinine clearance < 12 mL/min).
- Concomitant treatment of Lercanidipine with cyclosporin should be avoided
 WARNINGS AND PRECAUTIONS
- Lercanidipine may lead to reflex tachycardia which, particularly in patients with severe obstructive coronary artery disease, may precipitate angina pectoris. therefore it is not advisable in patients with unstable angina pectoris or recent myocardial infarction
- Lercanidipine is metabolized in humans by CYP3A4:
- CYP3A4 inhibitors : CYP3A4 inhibitors like Ketoconazole, Itraconazole, Nefazodone, erythromycin, Clarithromycin, Isoniazid, fluvoxamine, HIV protease inhibitors (e.g. ritonavir, indinavir, nelfinavir) and Grapefruit juice can potentiate its effect. Such combinations should be used with caution.
- CYP3A4 inducers (e.g. carbamazepine, efavirenz, St John’s wort, nevirapine, phenobarbitol, phenytoin, primidone, rifabutin, rifampicin) are expected to decrease Lercanidipine concentrations and, therefore, blood pressure should be monitored when the co-administration is foreseen
- Cyclosporin: Co-administration of lercanidipine with cyclosporin resulted in a 3 fold increase in the plasma levels of lercanidipine and a 21% increase in the bioavailability of cyclosporin. However, when cyclosporin was administered 3 hours after lercanidipine, no increase in plasma levels was observed for lercanidipine, while the bioavailability of cyclosporin increased by 27%. Therefore, cyclosporin and lercanidipine should not be administered together.
 PREGNANCY AND LACTATION
- Pregnancy Category C (US). There is no clinical experience with lercanidipine in pregnancy, but other dihydropyridine compounds have been found to cause irreversible malformations in animals. Therefore, lercanidipine should not be administered during pregnancy or to women with child-bearing potential unless effective contraception is used.
- There is no clinical experience with lercanidipine in lactation. Distribution into milk may be expected, due to the high lipophilicity of lercanidipine. Therefore, lercanidipine should not be administered to lactating women.
 SIDE EFFECTS
Possible side effects include: dizziness, headache, flushing, tachycardia, skin rash or itching, palpitations and localised peripheral edema of non-cardiac origin (local arterial dilatation seems to be involved rather than fluid retention), each occuring in less than 1% of patients.
- Hypersensitivity: symptoms include itching, rash, hives) (Very rare)
- Angina pectoris (Rare)
 RELATED LINKS
|ACE inhibitors||Benazepril (Lotensin) • Captopril (Capoten) • Cilazapril • Delapril • Enalapril (Renitec, Vasotec) • Fosinopril (Monopril) • Lisinopril (Prinivil, Zestril) • Moexipril (Univasc) • Perindopril (Aceon) • Quinapril (Accupril) • Ramipril (Altace, Triatec) • Trandolapril (Mavik) • Zofenopril (Bifril, Zopranol)|
|Angiotensin II receptor antagonist||Azilsartan (Edarbi) • Candesartan (Atacand) • Eprosartan (Teveten) • Irbesartan (Aprovel, Avapro, Karvea) • Losartan (Cozaar) • Olmesartan (Benicar, Olmetec) • Telmisartan (Micadis) • Valsartan (Diovan, Tareg)|
|Renin inhibitors||Aliskiren (Rasilez, Tekturna)|
|Alpha-1 blockers||Doxazosin (Cardura) • Prazosin (Minipress) • Terazosin (Hytrin)|
|Alpha-2 agonists (centrally acting)||Clonidine (Oral route) • Clonidine (Transdermal) (Catapresan) • Guanfacine (Tenex) • Methyldopa (Aldomet)|
|Calcium channel blockers||Dihydropyridines||Amlodipine (Norvasc) • Barnidipine (Vasexten) • Felodipine (Plendil) • Isradipine (Dynacirc) • Lacidipine (Lacipil, Motens) • Lercanidipine (Zanidip) • Manidipine • Nicardipine • Nifedipine (Adalat) • Nisoldipine • Nitrendipine|
|Benzothiazepine||Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)|
|Phenylalkylamine||Gallopamil • Verapamil (Calan)|
|Beta blockers||Beta1 selective (cardioselective)||Acebutolol (Sectral) • Atenolol (Tenormin) • Betaxolol (Kerlon) • Bisoprolol (Concor) • Celiprolol (Cordiax) • Metoprolol (Betaloc, Lopressor, Toprol-XL) • Nebivolol (Bystolic, Lobivon, Nebilox)|
|Nonselective (Beta1 and Beta2 blockers)||Oxprenolol (Trasitensin) • Propranolol (Inderal) • Timolol (Blocadren)|
|Nonselective (Beta1, Beta2 and Alpha1 blockers)||Carvedilol (Dilatrend) • Labetalol (Trandate)|
|Beta blocker with intrinsic sympathomimetic activity (ISA)||Acebutolol (Sectral) • Celiprolol (Cordiax)|
|Lipophilic Beta blockers||Propranolol (Inderal) • Metoprolol (Betaloc, Lopressor, Toprol-XL) • Oxprenolol (Trasitensin)|
|Diuretics||Carbonic anhydrase inhibitors||Acetazolamide (Diamox)|
|Loop diuretics||Bumetanide • Etacrynic acid • Furosemide (Lasix) • Piretanide • Torasemide (Demadex)|
|Thiazide diuretics||Chlorothiazide (Diuril) • Hydrochlorothiazide (Esidrex)|
|Thiazide-like diuretics||Chlortalidone (Hygroton) • Indapamide (Lozol, Lozide) • Metolazone|
|Potassium-sparing diuretics|| Epithelial sodium channel blockers: Amiloride (Midamor) • Triamterene (Dyrenium) |
Aldosterone receptor antagonists: Potassium canrenoate • Eplerenone (Inspra) • Spironolactone (Aldactone)
|Combination therapy||Amiloride/Hydrochlorothiazide (Moduretic) • Spironolactone/Hydrochlorothiazide (Aldactazide)|