Description
Lernicore Pharmacodynamics
Lercanidipine is a selective “slow” calcium channel blocker, a 1,4-dihydropyridine derivative, inhibits transmembrane flow of calcium ions into vascular smooth muscle cells.
Lercanidipine is a racemic mixture of (+)-R- and (-)S- enantiomers. The antihypertensive effect of lercanidipine is primarily due to the S enantiomer.
The mechanism of the antihypertensive effect of lercanidipine is due to a direct relaxant effect on vascular smooth muscle cells, resulting in a reduction of total peripheral resistance. Despite relatively short plasma elimination half-life, lercanidipine has prolonged antihypertensive effect due to high membrane distribution coefficient. Due to high vascular selectivity, it has no negative inotropic effect. Acute arterial hypotension with reflex tachycardia is rare due to the gradual development of vasodilation when taking lercanidipine.
Lercanidipine is metabolically neutral and has no significant effect on serum lipoprotein and apolipoprotein content and does not alter 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 chronic 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).
Concomitant use with potent CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin).
Concomitant use with cyclosporine.
Concomitant use with grapefruit juice.
Lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.
Pregnancy and breast-feeding.
Use in women of childbearing age who do not use reliable methods of contraception.
Age under 18 years (effectiveness and safety are not studied).
Dosage and administration
- Orally, at least 15 minutes before a meal, preferably in the morning, without chewing, with plenty of water.
- Recommended dose is 10 mg once a day. Depending on individual tolerance of a patient, a dose can be increased up to 20 mg. If necessary, the daily dose should be increased to 20 mg in 2 weeks after starting to take the drug.
- The therapeutic dose is adjusted gradually, as the maximum antihypertensive effect develops approximately 2 weeks after the start of the drug. It is unlikely that the drug efficacy will increase with increasing dosage above 20 mg per day, at the same time the risk of side effects increases.
- Use in elderly patients
- The pharmacokinetic profile and data from clinical studies indicate that no adjustment of the dose of lercanidipine is required in elderly patients. However, caution should be exercised during the initial phase of treatment in this group of patients.
- Use in patients with renal or hepatic impairment
- In patients with renal insufficiency (CKR over 30 ml/min) or hepatic insufficiency of mild or moderate degree, the initial dose is 10 mg, then the dose is increased up to 20 mg per day with caution. Antihypertensive effect may increase in patients with mild to moderate hepatic impairment and dose adjustment (reduction) may be required.
