Lercanidipine

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Available since: 2019-09-19

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Clinical Pharmacology

Pharmacological action - hypotensive.
Pharmacodynamics
Lercanidipine is a selective BPC (a derivative of 1,4-dihydropyridine) that inhibits the transmembrane current 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 relaxing effect on vascular smooth muscle cells, resulting in a reduced OSS.
Despite the relatively short T1 / 2 from plasma, lercanidipine has a prolonged antihypertensive effect due to the high coefficient of membrane distribution. Due to the high vascular selectivity does not have a negative inotropic effect. Acute hypotension with reflex tachycardia is rarely due to the gradual development of vasodilation while taking lercanidipine.
Lercanidipine is metabolically neutral and does not have a significant effect on the content of lipoproteins and apolipoproteins in the blood serum, and also does not change the lipid profile in patients with arterial hypertension.
Pharmacokinetics
Suction
Lercanidipine is completely absorbed after ingestion. Cmax in blood plasma is reached in 1.5–3 h and amounts to (3.3 ± 2.09) and (7.66 ± 5.9) ng / ml after taking 10 and 20 mg of lercanidipine, respectively.
(+) - R- and (-) S-enantiomers of lercanidipine demonstrate a similar pharmacokinetic profile: they have the same Tmax and T1 / 2; Cmax and AUC values are 1.2 times higher for the (-) S-enantiomer. Interconversion of enantiomers in in vivo experiments are not observed.
During the initial passage through the liver, the absolute bioavailability of lercanidipine when taken orally after a meal is approximately 10%; when taken on an empty stomach, the value of bioavailability decreases by 1/3. When taking lercanidipine no later than 2 hours after ingestion of fatty foods, its bioavailability increases 4 times, so lercanidipine should not be taken after meals. With oral administration of lercanidipine, its concentration in plasma is not directly proportional to the dose taken (nonlinear kinetics).
Saturation of the presystemic metabolism occurs gradually. Thus, bioavailability increases with increasing doses.
Distribution
Distribution from blood plasma to tissues and organs occurs quickly and extensively. Communication with proteins of a blood plasma exceeds 98%.
Metabolism and excretion
Lercanidipine is metabolized with the participation of CYP3A4 isoenzyme with the formation of inactive metabolites.
About 50% of the dose taken is excreted by the kidneys (about 50% is excreted by the intestine). Elimination occurs mainly by biotransformation. The average T1 / 2 is 8-10 hours. The duration of therapeutic action is 24 hours.
Cumulation of lercanidipine when re-ingestion is not observed.
Special Clinical Cases
It was shown that the pharmacokinetics of lercanidipine in elderly patients, patients with renal insufficiency (Cl creatinine more than 30 ml / min) and in patients with mild and moderate hepatic insufficiency is similar to the pharmacokinetics observed in the general population of patients.
In patients with severe renal and / or hepatic insufficiency, due to a decrease in plasma protein concentration, the free fraction of lercanidipine may increase.
In patients with renal insufficiency (Cl creatinine less than 30 ml / min) and in patients on hemodialysis, plasma concentrations of lercanidipine are higher (approximately 70%).
In patients with moderate and severe liver failure, the systemic bioavailability of lercanidipine is likely to increase, since lercanidipine is metabolized mainly in the liver.

Indications

Arterial hypertension grade 1–2.

Composition

Film Coated pills	1 tab.
active substance:
lercanidipine hydrochloride	10/20 mg
excipients: MCC - 39/78 mg; lactose monohydrate - 30/60 mg; sodium carboxymethyl starch (sodium starch glycolate) - 15.5 / 31 mg; Povidone K30 - 4.5 / 9 mg; magnesium stearate - 1/2 mg
film cover (dosage 10 mg): Opadry II 85F38107 yellow (polyvinyl alcohol - 1.2 mg, titanium dioxide - 0.6684 mg, macrogol (polyethylene glycol) - 0.606 mg, talc - 0.444 mg, aluminum varnish based on quinoline yellow dye - 0.0807 mg, iron oxide red - 0.0009 mg)
film cover (dosage 20 mg): Opadry II 85F34555 pink (polyvinyl alcohol - 2.4 mg, titanium dioxide - 1.4046 mg, macrogol (polyethylene glycol) - 1.212 mg, talc - 0.888 mg, dye-based aluminum varnish “Red charming "- 0.0348 mg, aluminum varnish based on the dye" Solar sunset "yellow - 0.0336 mg, aluminum varnish based on the dye azorubin - 0.027 mg)

Lercanidipine is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
			pills
Zanidip-record	Record Chemical and Pharmaceutical Industry	Italy	pills
Lerkamen	Berlin-Chemie/Menarini	Germany	pills

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Dosage and Administration

Orally, at least 15 minutes before meals, preferably in the morning, without chewing, drinking plenty of water.
The recommended dose of the drug is 10 mg / day.
Depending on the individual tolerance of the drug by the patient, the dose may be increased to 20 mg. If necessary, the increase in the daily dose to 20 mg is carried out 2 weeks after the start of the drug.
The therapeutic dose is adjusted gradually, because maximum antihypertensive effect develops approximately 2 weeks after the start of the drug. It is unlikely that the effectiveness of the drug will increase with increasing doses of more than 20 mg / day, at the same time increasing the risk of side effects.
Special patient groups
Elderly age. The pharmacokinetic profile and data from clinical studies show that in elderly patients dose adjustment of lercanidipine is not required. However, caution should be exercised at the initial stage of treatment in this group of patients.
Impaired renal or hepatic function. In the presence of renal (Cl creatinine more than 30 ml / min) or mild or moderate hepatic insufficiency, the initial dose is 10 mg, then it is carefully increased to 20 mg / day. The antihypertensive effect may be exacerbated in patients with mild to moderate hepatic insufficiency, and dose adjustment (reduction) may be required.

Adverse reactions

Possible adverse reactions are listed below in descending frequency of occurrence: often (<1/10,> 1/100); infrequently (<1/100,> 1/1000); rarely (<1/1000,> 1/10000); very rarely (<1 10="" 000="" including="" individual="" messages="" br=""> On the part of the nervous system: infrequently - headache, dizziness; rarely - drowsiness.
From the side of the cardiovascular system: infrequently - feeling of palpitations, tachycardia, flushing of the skin of the face; rarely - angina, chest pain; very rarely - fainting, myocardial infarction, pronounced decrease in blood pressure; in patients with angina pectoris, an increase in the frequency, duration and severity of attacks is possible.
On the part of the digestive tract: rarely - nausea, dyspepsia, diarrhea, epigastric pain, vomiting; very rarely - a reversible increase in liver transaminase activity, gingival hyperplasia.
On the part of the respiratory system, organs of the chest and mediastinum: very rarely - pain in the chest.
On the part of the skin and subcutaneous tissues: rarely - skin rash.
On the part of the musculoskeletal system: rarely - myalgia.
On the part of the kidneys and urinary tract: rarely - polyuria; very rarely - pollakiuria (increased frequency of urination).
On the part of the immune system: very rarely - hypersensitivity reactions.
General disorders and disorders at the injection site: infrequently - peripheral edema; rarely - asthenia, fatigue.

Contraindications

Hypersensitivity to lercanidipine, other derivatives of the dihydropyridine series, or any component of the drug;
untreated chronic heart failure;
unstable angina;
obstruction of the outflow tract of the left ventricle;
a period of 1 month after a myocardial infarction;
severe liver failure;
severe renal impairment (Cl creatinine less than 30 ml / min);
simultaneous use with powerful inhibitors of CYP3A4 (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin);
simultaneous use with cyclosporine;
simultaneous intake with grapefruit juice;
lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
use in women of childbearing age, not using reliable methods of contraception;
pregnancy;
breastfeeding period;
age up to 18 years (efficacy and safety have not been studied).

With caution: renal failure (Cl creatinine more than 30 ml / min) and / or liver failure mild to moderate severity; elderly age; sick sinus syndrome (without pacemaker); coronary heart disease; dysfunction of the left ventricle.

Drug interactions

Lercanidipine can be used simultaneously with beta-blockers, diuretics, ACE inhibitors.
When used simultaneously with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect can also occur with simultaneous use with other beta-blockers.Therefore, it may be necessary to adjust the dose of lercanidipine to achieve a therapeutic effect with this combination.
Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme; therefore, inhibitors and inductors of this isoenzyme with simultaneous use may affect the metabolism and elimination of lercanidipine. The simultaneous use of lercanidipine with potent CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is not recommended.
The simultaneous use of cyclosporine and lercanidipine is not recommended, since there is an increase in the concentration of both substances in the blood plasma.
Caution should be exercised with simultaneous use of lercanidipine with other substrates of CYP3A4 (terfenadine, astemizol, class III antiarrhythmic drugs, such as amiodarone, quinidine).
With simultaneous use of lercanidipine at a dose of 20 mg with midazolam, the bioavailability of lercanidipine in elderly patients can be increased by approximately 40%.
Lercanidipine should be administered with caution simultaneously with inducers of CYP3A4, such as anticonvulsants (phenytoin, carbamazepine) and rifampicin, since antihypertensive action may be reduced. Requires regular monitoring of blood pressure.
With simultaneous use of lercanidipine at a dose of 20 mg in patients constantly taking beta-methyldigoxin, PCV was not observed, while in healthy volunteers who were treated with digoxin, there was an increase in Cmax for digoxin on average by 33% after taking 20 mg of lercanidipine on an empty stomach, while the AUC and renal clearance changed slightly. It is necessary to control the presence of signs of digoxin intoxication in patients taking both digoxin and lercanidipine.
The simultaneous use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in the concentration of lercanidipine in the blood plasma. With high doses of cimetidine, the bioavailability and antihypertensive effect of lercanidipine may increase.
With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), the AUC value for simvastatin increased by 56%, and the same value for its active metabolite - beta hydroxy acid - by 28%. When taking medications at different times of day (lercanidipine in the morning, simvastatin in the evening), unwanted interactions can be avoided.
With simultaneous use of 20 mg of lercanidipine and warfarin in healthy volunteers, no changes in the pharmacokinetics of warfarin were observed.
Simultaneous use with fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients did not have clinically significant changes in the pharmacokinetics of lercanidipine.
It is possible to enhance the antihypertensive effect while taking grapefruit juice and lercanidipine.
Ethanol can potentiate the antihypertensive effects of lercanidipine.

Special instructions

Special care should be taken when prescribing lercanidipine in patients with sick sinus syndrome (without a pacemaker).
Despite the fact that studies with hemodynamic control did not reveal deterioration in ventricular function when taking lercanidipine, care should be taken when prescribing lercanidipine in patients with left ventricular dysfunction.
It has been suggested that taking some dihydropyridines may be associated with the risk of an increase in strokes in patients with coronary artery disease. Therefore, in these patients, lercanidipine therapy should be carried out with extreme caution.
Influence on ability to steer vehicles and work with mechanisms. Since during therapy with the drug, dizziness, asthenia, increased fatigue and, in rare cases, drowsiness may occur during the period of use of the drug, patients should be extremely careful to drive vehicles and engage in other potentially dangerous activities that require high speed psychomotor reactions.

Overdosage

Symptoms: peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia (presumably in the case of an overdose of lercanidipine, symptoms similar to those of an overdose of other dihydropyridine derivatives will be observed).
Treatment: symptomatic.In the case of a pronounced decrease in blood pressure, loss of consciousness, cardiovascular therapy is indicated, with bradycardia, intravenous atropine.
There are data on 3 cases of overdose when taking lercanidipine in doses of 150, 280 and 800 mg for the purpose of suicide.
1. Reception of 150 mg of lercanidipine + alcohol (unspecified amount).
Symptoms: drowsiness.
Treatment: gastric lavage, the appointment of activated carbon.
2. Receive 280 mg of lercanidipine + 5.6 mg of moxonidine.
Symptoms: cardiogenic shock, severe myocardial ischemia, mild renal failure.
Treatment: the appointment of cardiac glycosides, diuretics (furosemide), high doses of catecholamines, plasma substitutes.
3. Acceptance of 800 mg of lercanidipine.
Symptoms: nausea and pronounced decrease in blood pressure.
Treatment: the appointment of activated carbon and laxatives, in / in - dopamine.
In all cases of overdose, all patients remained alive.
Information on the effectiveness of dialysis for lercanidipine is missing. Most likely, due to the high association of lercanidipine with plasma proteins, dialysis may be ineffective.