Description
Lercanidipine-SZ Pharmacodynamics
A “slow” calcium channel blocker. Lercanidipine is a racemic mixture of right- (R) and left- (S) stereoisomers, a 1,4-dihydropyridine derivative, is able to selectively block the flow of calcium ions inside vascular wall cells, cardiac cells and smooth muscle cells. The mechanism of hypotensive action is due to a direct relaxant effect on vascular smooth muscle cells. It has a prolonged antihypertensive effect. The therapeutic effect is achieved 5-7 hours after oral administration and its duration lasts for 24 hours. Due to high selectivity to vascular smooth muscle cells, there is no negative inotropic effect.
Lercanidipine is metabolically neutral and has no significant effect on serum lipoprotein and apolipoprotein content and does not change the lipid profile in patients with arterial hypertension.
Indications
Arterial hypertension of the 1-2 degrees.
Contraindications .
– Hypersensitivity to lercanidipine, other dihydropyridine-type derivatives or any component of the drug;
– Untreated heart failure;
– unstable angina pectoris;
– Left ventricular outflow tract obstruction;
– period within 1 month after myocardial infarction;
– severe hepatic insufficiency;
– severe renal insufficiency (CKR less than 30 ml/min);
– pregnancy and breastfeeding;
– use in women of childbearing age who do not use reliable contraception;
– Under 18 years of age (efficacy and safety have not been established);
– lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
– concomitant use with CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, erythromycin, ritonavir, roleandomycin) (see section “Interaction with other medicinal products”);
– concomitant use with cyclosporine (see section “Interaction with other medicinal products”);
– concomitant administration with grapefruit juice (see section “Interaction with other medicinal products”).
Dosage and administration
- Orally. Lercanidipine SP is indicated as 10 mg 1 time daily in the morning, at least 15 min before a meal, without chewing and with plenty of water.
- The dose may be increased to 20 mg (if the expected effect is not achieved with 10 mg). The therapeutic dose is adjusted gradually, the dose is increased to 20 mg in 2 weeks after the start of the drug.
- It is unlikely that the drug efficacy will increase with increasing the dose more than 20 mg per day, at the same time the risk of side effects increases.
- Administration in elderly patients
- No dosage adjustment is required, however, constant monitoring of the patients’ condition is necessary during the drug administration.
- Administration in patients with renal or hepatic impairment
- In patients with renal or hepatic insufficiency of mild or moderate severity, as a rule, dosage adjustment is not required; the initial dose is 10 mg, the dose should be increased up to 20 mg per day with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.
