Lercanidipine-SZ, 20 mg 30 pcs

Arterial hypertension of the 1-2 degree.

Active ingredient

Lercanidipine

Composition

Active substance:

lercanidipine hydrochloride – 20 mg;

Auxiliary substances (core):

Lactose monohydrate (milk sugar) – 63.0 mg;

Microcrystalline cellulose – 77.0 mg;

Starch sodium glycolate – 31.0 mg;

Hypromellose (hydroxypropyl methylcellulose) – 7.0 mg;

Magnesium stearate – 2.0 mg;

Auxiliary substances (shell):

Opadray II (polyvinyl alcohol, partially hydrolyzed – 2.4 mg; titanium dioxide E 171 – 1.3416 mg; Talc 0.888 mg macrogol(polyethylene glycol) 3350 – 1.212 mg; iron oxide yellow dye E 172 – 0.0858 mg; iron oxide red dye E 172 – 0.0726 mg).

Interaction

The drug should not be used concomitantly with CYP3A4 inhibitors (hepatic cytochrome P450 isoenzyme) such as ketoconazole, itraconazole, erythromycin (they increase the blood concentration of lercanidipine and lead to potentiation of the antihypertensive effect). Concomitant administration of lercanidipine with cyclosporine is contraindicated since it leads to increased plasma levels of both substances.

Lercanidipine should not be taken with grapefruit juice since this inhibits the metabolism of lercanidipine and potentiates the antihypertensive effect.

Caution should be exercised when concomitant administration with drugs such as terfenadine, astemizole, quinidine and antiarrhythmic drugs of class III (e.g., amiodarone).
Concomitant use with anticonvulsants (e.g., phenytoin, carbamazepine) and rifampicin may lead to decreased plasma concentrations of lercanidipine and, in connection with this, to a decrease in the antihypertensive effect of lercanidipine.
No pharmacokinetic interaction has been observed in patients regularly taking digoxin when 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 bioavailability of lercanidipine at a dose of 20 mg with midazolam may increase by approximately 40% in elderly patients.

Metoprolol decreases the bioavailability of lercanidipine by 50%; the bioavailability of metoprolol remains unchanged. This effect may occur due to decreased hepatic blood flow caused by beta-adrenoblockers; therefore, it may also occur when used with other drugs of this group.

Cimetidine at a dose of 800 mg daily does not cause significant changes in plasma concentrations of lercanidipine, however, special caution is required because the bioavailability of lercanidipine, and therefore its antihypertensive effect, may increase at higher doses of cimetidine.

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

simvastatin

– in the evening) undesirable interaction can be avoided.

In concomitant use with fluoxetine (CYP2D6 and CYP3A4 isoenzyme inhibitor) in elderly patients no clinically significant changes of pharmacokinetics of lercanidipine were found.

Taking lercanidipine concomitantly with warfarin has no effect on the pharmacokinetics of the latter.

Lercanidipine may be used concomitantly with beta-adrenoblockers, diuretics, angiotensin-converting enzyme (ACE) inhibitors. Ethanol may increase the antihypertensive effect of lercanidipine.

Directions for use

Ingestion. Lercanidipine-SZ is prescribed 10 mg once daily in the morning, at least 15 minutes before meals, without chewing, 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, increasing the dose to 20 mg in 2 weeks after the start of the drug.

The effectiveness of the drug is unlikely to increase with doses greater than 20 mg daily, while at the same time the risk of side effects increases.

Periodic use in older patients

There is no need for dose adjustment, but constant monitoring is necessary while taking the drug.

Patients with renal or hepatic impairment

In the presence of mild to moderate renal or hepatic impairment, usually no dose adjustment is required; the initial dose is 10 mg; increase in dose to 20 mg per day should be undertaken with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.

Special Instructions

The following is a list of adverse reactions by organ system and frequency of occurrence (World Health Organization classification):

often more than 1/100 to less than 1/10,

infrequently more than 1/1000 to less than 1/100,

rarely more than 1/10000 to less than 1/1000,

very rarely less than 1/10000, including individual reports.

Nervous system disorders

Infrequent: headache, dizziness;

Rare: drowsiness.

Cardiovascular system disorders

Infrequent: palpitations, tachycardia, “rushes” of blood to the face;

Rare: angina pectoris;

Very rare: syncope, marked decrease in blood pressure, chest pain, myocardial infarction, in patients with angina pectoris, an increase in the frequency, duration and severity of attacks is possible.

Gastrointestinal disorders

Rare: nausea, vomiting, diarrhea, abdominal pain, dyspepsia;

Very rare: increased activity of “liver” enzymes (reversible).

Skin and subcutaneous tissue disorders

Rarely: skin rash.

Muscular and connective tissue disorders

Rarely: myalgia.

Rarely: pollakiuria (increased frequency of urination).

General disorders

Infrequent: peripheral edema;

Rarely: asthenia, increased fatigue;

Very rare: gum hyperplasia.

Immune system disorders:

Very rare: hypersensitivity reactions.

Contraindications

– Hypersensitivity to lercanidipine, other dihydropyridine-type derivatives or any component of the drug;

– untreated heart failure;

– unstable angina;

– 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;

– age under 18 years (effectiveness and safety not established);

– lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;

– concomitant use with CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin);

– concomitant administration with cyclosporine;

– concomitant administration with grapefruit juice.

With caution:

– Renal insufficiency (creatinine clearance more than 30 ml/min);

– liver function disorders of mild to moderate severity;

– elderly age;

– sinus node weakness syndrome (without pacemaker);

– left ventricular dysfunction and coronary heart disease;

– chronic heart failure;

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– concomitant use with substrates of CYP3A4 isoenzyme (terfenadine, asmetol, class III antiarrhythmic drugs, e.g., amiodarone, quinidine);
– concomitant use with inducers of CYP3A4 isoenzyme, e.g. anticonvulsants (phenytoin, carbamazepine) and rifampicin;

– concomitant use with beta-adrenoblockers, digoxin.

Side effects

The following is a list of adverse reactions by organ system and frequency of occurrence (World Health Organization classification):

often more than 1/100 to less than 1/10,

infrequently more than 1/1000 to less than 1/100,

rarely more than 1/10000 to less than 1/1000,

very rarely less than 1/10000, including individual reports.

Nervous system disorders

Infrequent: headache, dizziness;

Rare: drowsiness.

Cardiovascular system disorders

Infrequent: palpitations, tachycardia, “rushes” of blood to the face;

Rare: angina pectoris;

Very rare: syncope, marked decrease in blood pressure, chest pain, myocardial infarction, in patients with angina pectoris, an increase in the frequency, duration and severity of attacks is possible.

Gastrointestinal disorders

Rare: nausea, vomiting, diarrhea, abdominal pain, dyspepsia;

Very rare: increased activity of “liver” enzymes (reversible).

Skin and subcutaneous tissue disorders

Rarely: skin rash.

Muscular and connective tissue disorders

Rarely: myalgia.

Rarely: pollakiuria (increased frequency of urination).

General disorders

Infrequent: peripheral edema;

Rarely: asthenia, increased fatigue;

Very rare: gum hyperplasia.

Immune system disorders:

Very rare: hypersensitivity reactions.

Overdose

Symptoms

Presumably, 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 be observed.

Treatment

Symptomatic. Cardiovascular therapy is indicated in case of marked BP decrease, loss of consciousness; intravenous injection of atropine is indicated in bradycardia. There is no information about the effectiveness of hemodialysis. Given the high degree of binding to 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 case of concomitant administration of 150 mg of lercanidipine with ethanol (unspecified amount) drowsiness was observed. Treatment: gastric lavage, oral administration of activated charcoal.

In case of simultaneous administration of 280 mg of lercanidipine with 5.6 mg of moxonidine the following symptoms were observed: cardiogenic shock, marked myocardial ischemia, mild renal failure. Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamines, plasma substitutes.
If 800 mg of lercanidipine was administered: nausea and marked BP decrease were observed. Treatment: intravenous administration of activated charcoal and laxatives, intravenous dopamine.

Pregnancy use

Pregnancy In animal studies, lercanidipine did not have teratogenic effects, but teratogenic effects were observed with other dihydropyridine derivatives.

Similarities

Lercamen 20, Lercamen 10, Zanidip-Recordati