Essential hypertension of mild or moderate severity.
LERCAMEN-20 PHARMACOLOGICAL PROPERTIES
lercanidipine is a selective blocker of calcium channels, dihydropyridine group, with a predominant effect on blood vessels. The mechanism of its hypotensive action is due to a direct relaxing effect on vascular smooth muscles, due to which their peripheral resistance decreases. Despite the short half-life from blood plasma, lercanidipine has a long-term antihypertensive effect due to the high coefficient of membrane distribution. Due to the high vascular selectivity of the drug, its inotropic effect has no clinical significance. Collaptoid reactions with reflex tachycardia are rarely noted due to the gradual development of vasodilation.
Lercanidipine is completely absorbed after oral administration. The maximum concentration in blood plasma is reached after approximately 1.5–3 hours; the degree of binding to serum proteins is 98%. Due to the intensive metabolism during the primary passage through the liver, the absolute bioavailability of lercanidipine taken after meals is approximately 10%, while it decreases to 1/3 of this value if the drug is used in healthy volunteers on an empty stomach. The half-life is 8-10 hours, and the therapeutic effect lasts for 24 hours, due to the high degree of binding to the lipid membrane. No cumulation was observed upon repeated application. The bioavailability of lercanidipine after oral administration increases significantly after meals, so the drug is taken on an empty stomach. The pharmacokinetics of lercanidipine in the elderly and in patients with mild to moderate renal or liver dysfunction is not very different from that in the general population. Lercanidipine is metabolized by the CYP 3A4 enzyme to inactive metabolites, about 50% of which are excreted in the urine. The original substance in urine and feces is not detected.
The recommended dose for adults is 10 mg 1 time per day, not less than 15 minutes before meals. Depending on the individual sensitivity of the patient and the effect achieved, the dose may be increased to 20 mg. The maximum antihypertensive effect develops within 2 weeks of treatment.
hypersensitivity to dihydropyridines or any component of the drug; severe stenosis of the mitral or aortic valve; hypertrophic cardiomyopathy with obstruction of the outflow tract of the left ventricle; decompensated congestive heart failure with unstable angina pectoris; within 1 month after myocardial infarction; severe liver and kidney dysfunction (creatinine clearance ≤10 ml / min). During pregnancy and breastfeeding. The drug is not recommended for women of childbearing age and children and adolescents under the age of 18.
LERCAMEN-20 SIDE EFFECTS
most of the observed adverse reactions are associated with the vasodilating effect of the drug: flushing of the face, peripheral edema, increased heart rate, tachycardia, headache, dizziness, asthenia. Other adverse reactions that occurred in ≤1% of patients were fatigue, gastrointestinal disorders (dyspepsia, nausea, vomiting, epigastric pain, diarrhea), polyuria, skin rash, drowsiness, myalgia. In isolated cases, hypotension. In some cases, gingival hyperplasia, a reversible increase in the activity of hepatic transaminases in the blood serum are revealed (no other clinically significant deviations in laboratory tests of liver function have been identified). There have been reports of increased frequency of urination. In isolated cases, the use of certain dihydropyridines leads to the appearance of angina attacks. Very rarely in patients, the frequency and duration of angina attacks increases, in some cases up to the development of myocardial infarction.
in patients with sick sinus syndrome, Lerkamen should be used with extreme caution (if a pacemaker is not implanted). Although hemodynamic studies have shown no deterioration in ventricular function, special caution is required in baseline dysfunction. Lercanidipine can be prescribed to patients with mild to moderate renal and hepatic dysfunction, but caution is required if they exceed a daily dose of up to 20 mg. The risk of dizziness, drowsiness and increased fatigue caused by taking Lerkamen is low, but it should be taken into account when driving or working with mechanisms. Lercanidipine does not affect serum sugar and lipids.
concomitant use of Lerkamen with CYP 3A4 inhibitors (for example, with ketoconazole, itraconazole, ritonavir, erythromycin or troleandomycin) should be avoided. The combined use of lercanidipine with cyclosporine leads to a 3-fold increase in the concentration of lercanidipine in the blood plasma, therefore, lercanidipine and cyclosporine should not be used simultaneously.