Lercanorm, 10 mg 30 pcs.

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, like other asymmetric 1,4-dihydropyridine derivatives, is mainly determined by the S-enantiomer.

Indications

Active ingredient

Composition

Associates:

microcrystalline cellulose – 37 mg,

lactose monohydrate – 35 mg,

sodium carboxymethyl starch (sodium starch glycolate, type A) – 10 mg,

povidone K-30 – 4.5 mg,

poloxamer – 2.5 mg,

magnesium stearate – 1 mg.

Composition of the film coating:

[Hypromellose – 1.5 mg, hyprolose (hydroxypropyl cellulose) – 0.582 mg, talc – 0.5778 mg, titanium dioxide – 0.3261 mg, iron oxide yellow (iron oxide) – 0.0141 mg] or [dry film coating mixture containing hypromellose 50%, hyprolose (hydroxypropyl cellulose) 19.4%, talc 19.26%, titanium dioxide 10.87%, iron oxide yellow (iron oxide) 0.47%] – 3 mg.

How to take, the dosage

Ingestion.

Lercanorm is taken 10 mg once daily in the morning, at least 15 minutes before a meal, without chewing, with plenty of water.

Depending on the therapeutic effect and individual tolerance of the patient, the dose can be increased up to 20 mg. The therapeutic dose is adjusted gradually because the maximum antihypertensive effect develops approximately 2 weeks after starting the drug.

The effectiveness of the drug is unlikely to increase with increasing the dose more than 20 mg daily, at the same time the risk of side effects increases.

Use in elderly patients

Lercanorm does not require dose adjustment in elderly patients, but caution should be exercised when taking the drug, especially at the start of treatment.

Use in patients with renal or hepatic impairment

Lercanorm should be used with caution in patients with renal impairment
(CKR over 30 ml/min) or mild to moderate hepatic impairment. The initial dose is 10 mg per day. Increasing the dose to 20 mg per day should be carried out with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.

Lercanorm is contraindicated in renal failure (CKR less than 30 ml/min) and in severe hepatic failure (see section “Contraindications”).

Interaction

Lercanidipine may be used concomitantly with beta-adrenoblockers, diuretics, angiotensin-converting enzyme inhibitors.

The bioavailability of lercanidipine decreases by 50% when used concomitantly with metoprolol. This effect may also be seen with other beta-adrenoceptors; therefore a dose adjustment of lercanidipine may be required to achieve therapeutic effect in this combination.

Lercanidipine is metabolized with participation of CYP3A4 isoenzyme, therefore inhibitors and inducers of CYP3A4 isoenzyme may simultaneously affect metabolism and excretion of lercanidipine. Concomitant use of lercanidipine with CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is contraindicated (see section “Contraindications”).

Cautions must be taken when using lercanidipine concomitantly with other CYP3A4 substrates (terfenadine, asmetol, class III antiarrhythmic drugs such as amiodarone, quinidine).

The bioavailability of lercanidipine at a dose of 20 mg with midazolam may increase by approximately 40% in elderly patients.

Lercanidipine should be used with caution in conjunction with CYP3A4 isoenzyme inducers, e.g., anticonvulsants (phenytoin, carbamazepine) and rifampicin, because the antihypertensive effect of lercanidipine may decrease. Regular BP control is necessary.

In patients who regularly take digoxin, no pharmacokinetic interaction was noted with concomitant use of lercanidipine at a dose of 20 mg. However, in healthy volunteers who took digoxin, there was an increase in plasma Cmax of digoxin by an average of 33% after an oral fasting dose of 20 mg of lercanidipine, while AUC and renal clearance of digoxin did not change significantly. It is necessary to monitor for signs of digoxin intoxication in patients taking digoxin and lercanidipine concomitantly.

The concomitant use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in plasma concentrations of lercanidipine. When using high doses of cimetidine bioavailability of lercanidipine and its antihypertensive effect can increase.

In concomitant use of lercanidipine (20 mg) and simvastatin (40 mg) the AUC of simvastatin increased by 56% and for its active metabolite
beta-hydroxy acid – by 28%. When taking the drugs at different time of day (lercanidipine in the morning, simvastatin in the evening) undesirable interaction can be avoided.

When using lercanidipine 20 mg and warfarin simultaneously in healthy volunteers no changes in warfarin pharmacokinetics were observed.

In concomitant use with fluoxetine (CYP2D6 and CYP3A4 isoenzyme inhibitor) in elderly patients no clinically significant changes in the pharmacokinetics of lercanidipine have been observed.

The antihypertensive effect may be enhanced if grapefruit juice and lercanidipine are taken concomitantly (see section “Contraindications”).

Ethanol may potentiate the antihypertensive effect of lercanidipine.

Special Instructions

Synopsis

Contraindications

Side effects

Classification of the frequency of side effects according to World Health Organization (WHO) recommendations:

very frequently ≥ 1/10;

frequently ≥ 1/100 to < 1/10;

infrequently from ≥ 1/1000 to < 1/100;

frequently from ≥ 1/10000 to < 1/1000;

very rarely < 1/10000, including individual reports;

frequency is unknown – it is not possible to determine the frequency of occurrence from the available data.

From the central nervous system:

infrequent – headache, dizziness;

frequent – drowsiness.

Cardiovascular system side:

infrequently – palpitations, tachycardia, “rushes” of blood to the skin of the face;

frequently – angina pectoris, pain behind the chest;

Very rarely – syncope, significant decrease in BP, myocardial infarction; patients with angina pectoris may have increased frequency, duration, and severity of attacks.

Gastrointestinal system:

Infrequent – nausea, dyspepsia, diarrhea, abdominal pain, vomiting.

Skin side:

frequently – skin rash.

Motor system:

not infrequently – myalgia.

Urinary system disorders:

frequent – polyuria;

very rare – pollakiuria (increased frequency of urination).

Allergic reactions:

very rarely – hypersensitivity reactions.

Laboratory findings:

very rarely – reversible increase in the activity of “hepatic” transaminases.

Other:

infrequent – peripheral edema;

frequent – asthenia, increased fatigue;

very rare – gum hyperplasia.

Overdose

Symptoms

In case of overdose of lercanidipine, symptoms similar to those of overdose of other dihydropyridine derivatives (peripheral vasodilation with marked BP decrease and reflex tachycardia), nausea will presumably be observed.

Treatment

Symptomatic. In case of marked BP decrease, loss of consciousness, cardiovascular therapy is indicated, in bradycardia – intravenous injection of atropine. There is no information about the effectiveness of hemodialysis. Given the high degree of binding to blood plasma proteins, dialysis may not be effective.

There are data on three cases of overdose when taking lercanidipine in doses of 150 mg, 280 mg and 800 mg. In all overdose cases, patients survived.

In the case of simultaneous administration of 150 mg of lercanidipine with ethanol (unspecified amount), drowsiness was observed. Treatment: gastric lavage, oral administration of activated charcoal.

In case of concomitant administration of 280 mg of lercanidipine with 5.6 mg of moxonidine the following symptoms were observed: cardiogenic shock, pronounced myocardial ischemia, renal failure of mild degree. Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamines, plasma substitutes. Treatment: oral administration of activated charcoal and laxatives, intravenous dopamine.

Pregnancy use

Pregnancy

Lercanidipine did not have teratogenic effects in animal studies, but teratogenic effects were observed with other dihydropyridine derivatives. Therefore, the use of Lercanorm during pregnancy and in women of childbearing age who do not use reliable contraception is contraindicated.

Breastfeeding period

Because of the high lipophilicity of lercanidipine, its penetration into breast milk can be assumed, therefore the use of Lercanorm during breastfeeding is contraindicated.

Similarities