Treatment of mild to moderate essential hypertension.
Composition:
1 tabl powl. contains 10 mg or 20 mg of lercanidipine hydrochloride. The tablets contain lactose.
Action:
A Calcium antagonist from the dihydropyridine group. It inhibits transmembrane transport of calcium ions to the heart and smooth muscle cells. The antihypertensive effect is the result of a direct relaxation action of the smooth muscle of the blood vessels, which causes a reduction in the total peripheral vascular resistance. Despite the short T0,5, lercanidipine is characterized by a long-lasting effect due to the high affinity and solubility in lipids of cell membranes. It does not work inotropically negatively, due to its high affinity for vascular smooth muscle cells. The antihypertensive effect of lercanidipine is mainly caused by the S enantiomer. After oral administration, it is completely absorbed and Cmax is reached after about 1.5 -3 h. The degree of binding to plasma proteins is> 98%. It is extensively metabolised by CYP3A4. The starting substance is not found in urine and faeces. Lercanidipine is mainly metabolised to inactive metabolites, approx. 50% of the administered dose is excreted in the urine. T0,5 is 8-10 h, the therapeutic activity is maintained for 24 h due to the strong binding of the drug to the lipid membranes. In patients with severe renal impairment or undergoing dialysis, higher plasma concentrations of lercanidipine (by about 70%) are observed. In patients with moderate or severe hepatic impairment, the absolute bioavailability of lercanidipine is higher due to less pronounced first-pass effect.
Contraindications:
Hypersensitivity to lercanidipine, dihydropyridine derivatives or other components of the preparation. Pregnancy and breastfeeding. Women of childbearing age who do not use effective contraception. Narrowing the outflow of blood from the left ventricle. Untreated congestive heart failure. Unstable angina is painful. Severe kidney or liver problems. Fresh myocardial infarction and 1 month from its occurrence. Co-administration with: strong CYP3A4 inhibitor, antifungal agents (ketoconazole, itraconazole), macrolide antibiotics ( Erythromycin, troleandomycin), antivirals (ritonavir), cyclosporine or grapefruit juice.
Precautions:
Particularly cautiously use in patients with sinus node syndrome who do not have an implanted pacemaker. Although no evidence of deterioration of cardiac ventricular function by lercanidipine has been reported in clinical trials, caution should be used in patients with left ventricular dysfunction. It has been reported that the use of some short-acting dihydropyridine derivatives may increase the risk of cardiovascular events in patients with ischemic heart disease. Although the preparation is a long-acting drug, it should be used with caution in patients with ischemic heart disease. Especially caution should be used in patients with mild to moderate renal or hepatic impairment. The antihypertensive effect of the preparation may be exacerbated in patients with hepatic impairment, dose adjustment should be considered in this patient group. Cytochrome CYP3A4 activators may decrease the plasma concentrations of lercanidipine, impairing the effect of the preparation. Avoid drinking alcohol because it can increase the vasodilator effect of antihypertensive drugs. It is not recommended to give patients <18 years. Due to the lactose content, do not use in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.
Pregnancy and lactation:
The preparation is contraindicated in pregnancy, during breast-feeding and in women of childbearing potential who do not use effective contraception. Due to its high lipophilicity, lercanidipine may enter milk.
Side effects:
Uncommon: pain and dizziness, tachycardia, palpitations, hot flushes, peripheral edema.Rarely: drowsiness, angina, nausea, indigestion, diarrhea, abdominal pain, vomiting, rash, muscle pain, polyuria, weakness, fatigue. Very rare: hypersensitivity, fainting. In addition, post-marketing very rarely: gingival hypertrophy, transient elevation of hepatic transaminases, hypotension, increased frequency of urination, chest pain. Certain dihydropyridine derivatives may in rare cases cause pre-cordial pain or angina. Very rarely, in patients with previously diagnosed angina, aggravation and increased incidence of angina pectoris may occur. In individual cases, a heart attack may occur.
Dosage:
Orally. Adults: 10 mg once a day, the dose can be increased to 20 mg depending on the patient's individual response to treatment. The dose should be increased gradually as the expected full antihypertensive effect can occur within 2 weeks. In the case of insufficient reduction of blood pressure monotherapy, the preparation can be used in combination with β-blockers (eg atenolol), diuretics (eg hydrochlorothiazide) or angiotensin-converting enzyme inhibitors (eg Captopril or enalapril). Because the curve displaying the relationship between dose size and treatment efficacy has an acute course at which for 20-30 mg dosesplateaudo not use doses higher than recommended, as the risk of side effects increases without increasing the effectiveness of treatment. In elderly patients, treatment with the preparation should be started with caution. In patients with mild to moderate renal or hepatic impairment, the usual recommended daily dose may be well tolerated, however caution should be exercised when increasing the dose to 20 mg per day. In patients with hepatic impairment, dosage adjustment should be considered. The tablets should be taken at least 15 minutes before a meal.
(C)
