Lercanidipine-SZ, 20 mg 30 pcs

Arterial hypertension of the 1-2 degree.

Indications

Arterial hypertension 1-2 degrees.

Pharmacological effect

Blocker of “slow” calcium channels

Special instructions

Below is a list of adverse reactions, distributed by organ system and frequency of occurrence (World Health Organization classification):

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

uncommon – from more than 1/1000 to less than 1/100,

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

very rarely – less than 1/10000, including individual messages.

Nervous system disorders

Uncommon: headache, dizziness;

Rarely: drowsiness.

Cardiovascular disorders

Uncommon: palpitations, tachycardia, flushes of blood to the skin of the face;

Rarely: angina pectoris;

Very rare: fainting, marked decrease in blood pressure, chest pain, myocardial infarction; in patients with angina, the frequency, duration and severity of attacks may increase.

Gastrointestinal disorders

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

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

Skin and subcutaneous tissue disorders

Rarely: skin rash.

Musculoskeletal and connective tissue disorders

Rarely: myalgia.

Renal and urinary tract disorders

Rarely: pollakiuria (increased frequency of urination).

General violations

Uncommon: peripheral edema;

Rarely: asthenia, increased fatigue;

Very rare: gingival hyperplasia.

Immune system disorders:

Very rare: hypersensitivity reactions.

Active ingredient

Lercanidipine

Composition

Active ingredient:

lercanidipine hydrochloride – 20 mg;

Excipients (core):

lactose monohydrate (milk sugar) – 63.0 mg;

microcrystalline cellulose – 77.0 mg;

sodium starch glycolate – 31.0 mg;

hypromellose (hydroxypropyl methylcellulose) – 7.0 mg;

magnesium stearate – 2.0 mg;

Excipients (shell):

Opadry 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 dye yellow oxide E 172 – 0.0858 mg; iron dye red oxide E 172 – 0.0726 mg).

Pregnancy

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

Contraindications

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

– untreated heart failure;

– unstable angina;

– obstruction of the left ventricular outflow tract;

– period within 1 month after myocardial infarction;

– severe liver failure;

– severe renal failure (creatinine clearance less than 30 ml/min);

– pregnancy and breastfeeding;

– use in women of childbearing age who do not use reliable contraception;

– age under 18 years (efficacy and safety have not been established);

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

– simultaneous use with inhibitors of the CYP3A4 isoenzyme (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin);

– simultaneous use with cyclosporine;

– simultaneous use with grapefruit juice.

With caution:

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

– mild to moderate liver dysfunction;

– old age;

– sick sinus syndrome (without pacemaker);

– dysfunction of the left ventricle of the heart and coronary heart disease;

– chronic heart failure;

– simultaneous use with substrates of the CYP3A4 isoenzyme (terfenadine, asmetol, class III antiarrhythmic drugs, for example, amiodarone, quinidine);
– simultaneous use with inducers of the CYP3A4 isoenzyme, for example, anticonvulsants (phenytoin, carbamazepine) and rifampicin;

– simultaneous use with beta-blockers, digoxin.

Side Effects

Below is a list of adverse reactions, distributed by organ system and frequency of occurrence (World Health Organization classification):

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

uncommon – from more than 1/1000 to less than 1/100,

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

very rarely – less than 1/10000, including individual messages.

Nervous system disorders

Uncommon: headache, dizziness;

Rarely: drowsiness.

Cardiovascular disorders

Uncommon: palpitations, tachycardia, flushes of blood to the skin of the face;

Rarely: angina pectoris;

Very rare: fainting, marked decrease in blood pressure, chest pain, myocardial infarction; in patients with angina, the frequency, duration and severity of attacks may increase.

Gastrointestinal disorders

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

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

Skin and subcutaneous tissue disorders

Rarely: skin rash.

Musculoskeletal and connective tissue disorders

Rarely: myalgia.

Renal and urinary tract disorders

Rarely: pollakiuria (increased frequency of urination).

General violations

Uncommon: peripheral edema;

Rarely: asthenia, increased fatigue;

Very rare: gingival hyperplasia.

Immune system disorders:

Very rare: hypersensitivity reactions.

Interaction

The drug should not be used simultaneously with inhibitors of CYP3A4 (liver cytochrome P450 isoenzyme), such as ketoconazole, itraconazole, erythromycin (increase the concentration of lercanidipine in the blood and lead to potentiation of the antihypertensive effect). The simultaneous use of lercanidipine with cyclosporine is contraindicated as this leads to an increase in the content of both substances in the blood plasma.

Lercanidipine should not be taken with grapefruit juice, as this leads to inhibition of lercanidipine metabolism and potentiation of the antihypertensive effect.

Caution must be exercised when taken concomitantly with drugs such as terfenadine, astemizole, quinidine and class III antiarrhythmic drugs (for example, amiodarone).
Concomitant use with anticonvulsants (for example, phenytoin, carbamazepine) and rifampicin may lead to a decrease in the plasma concentration of lercanidipine and, therefore, a decrease in the antihypertensive effect of lercanidipine.
In patients chronically taking digoxin, no pharmacokinetic interaction was observed with concomitant use of lercanidipine at a dose of 20 mg. However, in healthy volunteers who took

digoxin

, there was an increase in the Cmax value of digoxin in blood plasma by an average of 33% after oral administration of 20 mg lercanidipine on an empty stomach, while the AUC and renal clearance of digoxin changed slightly. Patients receiving digoxin and lercanidipine concomitantly should be monitored for signs of digoxin toxicity.

When lercanidipine 20 mg is co-administered with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40%.

Metoprolol reduces the bioavailability of lercanidipine by 50%, while the bioavailability of metoprolol remains unchanged. This effect may occur due to a decrease in hepatic blood flow, which is caused by beta-blockers, and may therefore also occur when used with other drugs in this group.

Cimetidine at a dose of 800 mg per day does not lead to significant changes in the concentration of lercanidipine in the blood plasma, however, special caution is required, since at higher doses of cimetidine the bioavailability of lercanidipine, and therefore its antihypertensive effect, may increase.

With simultaneous 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 medications at different times of the day (lercanidipine – in the morning,

simvastatin

– in the evening) you can avoid unwanted interactions.

When used simultaneously with fluoxetine (an inhibitor of CYP2D6 and CYP3A4 isoenzymes) in elderly patients, no clinically significant changes in the pharmacokinetics of lercanidipine were detected.

Taking lercanidipine simultaneously with warfarin does not affect the pharmacokinetics of the latter.

Lercanidipine can be used simultaneously with beta-blockers, diuretics, and angiotensin-converting enzyme (ACE) inhibitors. Ethanol may enhance the antihypertensive effect of lercanidipine.

Overdose

Symptoms

Presumably, in case of an overdose of lercanidipine, symptoms will be observed similar to those with an overdose of other dihydropyridine derivatives (peripheral vasodilation with a pronounced decrease in blood pressure and reflex tachycardia), nausea.

Treatment

Symptomatic. In case of a pronounced decrease in blood pressure and loss of consciousness, cardiovascular therapy is indicated; in case of bradycardia, intravenous administration of atropine is indicated. There is no information on the effectiveness of hemodialysis. Given the high degree of binding to plasma proteins, dialysis may be ineffective.

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

Drowsiness has been observed when lercanidipine 150 mg was coadministered with ethanol (unspecified amount). Treatment: gastric lavage, ingestion of activated carbon.

In case of simultaneous administration of 280 mg of lercanidipine with 5.6 mg of moxonidine, the following symptoms were observed: cardiogenic shock, severe myocardial ischemia, mild renal failure. Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamines, plasma expanders.
When taking 800 mg of lercanidipine, the following were observed: nausea, a marked decrease in blood pressure. Treatment: oral administration of activated carbon and laxatives, intravenous dopamine.

Recommendations for use

Inside. The drug Lercanidipine-SZ is prescribed 10 mg 1 time per day in the morning, at least 15 minutes before meals, without chewing, with a sufficient amount of water.

The dose can be increased to 20 mg (if the expected effect is not achieved when taking 10 mg). The therapeutic dose is selected gradually, increasing the dose to 20 mg 2 weeks after starting the drug.

It is unlikely that the effectiveness of the drug will increase with increasing doses above 20 mg per day, and at the same time the risk of side effects increases.

Use in elderly patients

No dose adjustment is required; however, when taking the drug, constant monitoring of the patient’s condition is necessary.

Use in patients with impaired renal or hepatic function

In the presence of mild or moderate renal or hepatic insufficiency, as a rule, no dose adjustment is required; the initial dose is 10 mg, increasing the dose to 20 mg per day should be done with caution. If the antihypertensive effect is too pronounced, the dose should be reduced.

Storage conditions

In a place protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.
Do not use after the expiration date stated on the package.

Manufacturer

North Star NAO, Russia