Lercanidipine-SZ, 10 mg 30 pcs

Name: Lercanidipine-SZ, 10 mg 30 pcs
SKU: 296132
Availability: InStock

€7.84

EAN: 4690655017216 SKU: 296132 Categories: Cardiovascular, High pressure, Medicine

Description

Slow calcium channel blocker.

Pharmacodynamics:

Slow calcium channel blocker. Lercanidipine is a racemic mixture of right- (R) and left-rotating (S) stereoisomers, a 1,4-dihydropyridine derivative, capable of selectively blocking the flow of calcium ions inside vascular wall cells, cardiac cells and smooth muscle cells. The mechanism of hypotensive action is due to a direct relaxant effect on vascular smooth muscle cells. It has prolonged antihypertensive effect.

Therapeutic effect is achieved 5-7 hours after oral administration and its duration lasts for 24 hours. Due to high selectivity for vascular smooth muscle cells there is no negative inotropic effect.

Lercanidipine is metabolically neutral and has no significant effect on serum lipoprotein and apolipoprotein content and does not change lipid profile in patients with arterial hypertension.

Pharmacokinetics:

Intake

Lercanidipine is completely absorbed after oral administration. Maximum plasma concentration (Cmax) is reached after 1.5-3 hours and is 3.3±2.09 ng/mL and 7.66±5.90 ng/mL after administration of 10 mg and 20 mg of lercanidipine, respectively.

The (+) R- and (-) S-enantiomers of lercanidipine show a similar pharmacokinetic profile: they have the same time to reach maximum concentration and the same T1/2. Cmax in plasma and area under the curve “concentration-time” (AUC) of (-) S-enantiomer of lercanidipine is, on average, 1.2 times higher than (+) R-enantiomer. No interconversion of the enantiomers was observed in the in-vivo experiments.

In “primary passage” through the liver, the absolute bioavailability of lercanidipine when taken orally after a meal is about 10%. When taken orally on an empty stomach the bioavailability is 1/3 of the bioavailability after a meal.

If lercanidipine is taken orally within 2 hours after a high-fat meal, its bioavailability is increased 4-fold, so lercanidipine should not be taken after a meal. Pharmacokinetics of lercanidipine in the range of therapeutic doses is non-linear. When taking lercanidipine at doses of 10 mg, 20 mg and 40 mg, plasma Cmax was determined in a ratio of 1:3:8, respectively, and AUC in a ratio of 1:4:18, which suggests progressive saturation during “primary passage” through the liver. Thus, bioavailability increases with increasing dose taken.

Distribution

The distribution of lercanidipine from plasma to tissues and organs is rapid. The degree of binding to plasma proteins exceeds 98%. In patients with severe renal and hepatic impairment due to decreased concentration of plasma proteins the free fraction of lercanidipine may increase.

Metabolism

Lercanidipine is metabolized with participation of CYP3A4 isoenzyme to form inactive metabolites.

The excretion of lercanidipine is primarily by biotransformation. About 50% of the administered dose is excreted by the kidneys, about 50% – through the intestine. The average T1/2 is 8-10 hours. There is no accumulation of lercanidipine in repeated oral administration.

Pharmacokinetics in special patient groups

The pharmacokinetics of lercanidipine in elderly patients, patients with renal impairment (creatinine clearance (CK) greater than 30 ml/min) and patients with mild to moderate hepatic impairment are similar to pharmacokinetics in healthy volunteers.

In patients with renal impairment (KC less than 30 ml/min) and in patients on hemodialysis, plasma concentrations of lercanidipine are increased by approximately 70%.

In patients with moderate to severe hepatic impairment, the systemic bioavailability of lercanidipine is probably increased because lercanidipine is metabolized primarily in the liver.

Indications

Arterial hypertension of the 1-2 degree.

Active ingredient

Lercanidipine

Composition

1 film-coated tablet contains:

dose 10 mg

the active ingredient:

lercanidipine hydrochloride, 10 mg;

auxiliary substances (core):

Lactose monohydrate (milk sugar) – 31.5 mg;

Microcrystalline cellulose – 38.5 mg;

Starch sodium glycolate – 15.5 mg;

Hypromellose (hydroxypropyl methylcellulose) – 3.5 mg;

Magnesium stearate – 1.0 mg;

Auxiliary substances (coating):

Opadray II (polyvinyl alcohol, partially hydrolyzed, 1.2 mg; E 171 titanium dioxide, 0.67998 mg; talc, 0.444 mg; macrogol (polyethylene glycol) 3350, 0.606 mg; Iron oxide yellow dye E 172 – 0.06825 mg; iron oxide red dye E 172 – 0.00096 mg; iron oxide black dye E 172 – 0.00081 mg).

How to take, the dosage
How to take, the dosage
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 of patients is necessary when 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.

Interaction
Interaction
The drug should not be used concomitantly with CYP3A4 inhibitors (liver cytochrome P450 isoenzyme), such as ketoconazole, itraconazole, erythromycin (which increase the blood concentration of lercanidipine and lead to potentiation of the antihypertensive effect). Concomitant use of lercanidipine with cyclosporine is contraindicated since it leads to increased plasma levels of both substances.
Lercanidipine should not be taken together with grapefruit juice because this inhibits the metabolism of lercanidipine and potentiates the antihypertensive effect.
Caution should be exercised when taking concomitantly with such drugs 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 were taking digoxin, there was a 33% increase in plasma Cmax of digoxin, on average, after an oral fasting dose of 20 mg of lercanidipine, while AUC and renal clearance of digoxin did not change significantly. The presence of signs of digoxin intoxication in patients taking simultaneous digoxin and lercanidipine should be monitored.

Special Instructions
Special Instructions
Caution should be exercised when prescribing to patients with impaired renal function, coronary heart disease (there is a risk of increased angina attacks), with regard to chronic heart failure: it should be compensated before starting the drug.
Particular caution should be used in patients with sinus node weakness syndrome (without a pacemaker).
While controlled studies of hemodynamics have shown no abnormalities in left ventricular function, calcium channel blockers should be used with extreme caution in patients with signs of left ventricular dysfunction. There is also a view that patients with coronary heart disease receiving short-acting dihydropyridines are a high-risk group for cardiovascular disease.
Particular caution should be exercised during the initial stages of treatment in patients with mild to moderate hepatic function impairment.
Influence on driving and mechanic ability:
Attention should be exercised during treatment for work requiring increased attention, driving vehicles, especially at the beginning of treatment and when increasing the dose of the drug (risk of drowsiness, headache and dizziness).
.

Contraindications
Contraindications
– Hypersensitivity to lercanidipine, other dihydropyridine-type derivatives or any component of the drug;
– Untreated heart failure;
– Unstable angina pectoris;
– left ventricular outflow tract obstruction;
– within 1 month after myocardial infarction;
– severe hepatic insufficiency;
– severe renal impairment (CKG less than 30 ml/min);
– pregnancy and breastfeeding;
– use in women of childbearing age who are not using reliable contraception;
– age less than 18 years (efficacy and safety not established);
– lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
– simultaneous use with CYP3A4 isoenzyme inhibitors (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin);
– simultaneous use with cyclosporine;
– simultaneous use 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 a pacemaker);
– left ventricular dysfunction and coronary heart disease;
– chronic heart failure;
– simultaneous use with CYP3A4 isoenzyme substrates (terfenadine, asmetol, class III antiarrhythmic drugs such as amiodarone, quinidine );
– simultaneous use with CYP3A4 isoenzyme inducers, such as anticonvulsants (phenytoin, carbamazepine ) and rifampicin;
– simultaneous use with beta-adrenoblockers, digoxin.
.

Side effects
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: fainting, 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
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, pronounced 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 use
Pregnancy

Similarities
Similarities
Lercamen 20, Lercamen 10, Zanidip-Recordati

Additional information
Weight 0.017 kg
Shelf life
3 years. Do not use after the expiration date stated on the package.
Conditions of storage
In the dark place at a temperature not exceeding 25 °С. Store out of the reach of children.
Manufacturer
North Star NAO, Russia
Medication form
pills
Brand
North Star NAO