Lerkamen tab 10 n / v 10mg film 60 pcs


Lerkamen tab 10 n / v 10mg film 60 pcs



Active substance:
1 tablet contains: lercanidipine hydrochloride – 10.0 mg.
Lactose monohydrate – 30.0 mg Microcrystalline cellulose – 39.0 mg Sodium carboxymethylstarch (type A) – 15.5 mg Povidone – 30 K – 4.5 mg magnesium stearate – 1.0 mg. sheath: Opadry OY-SR-6497 – 3.0 mg consisting of: hypromellose – 1,913 mg talc – 0.150 mg of titanium dioxide – 0.600 mg macrogol 6000 – 0.300 mg iron oxide yellow dye – 0,037 mg.
Round biconvex tablets, film-coated, from pale yellow to light yellow with the mark on one side.
Kind of on a break: light yellow.
Product form:
Tablets, film-coated, 10 mg.
At 7, 10 or 15 tablets in blister [opaque PVC film / aluminum foil].
1 (7 or 14 tablets), 2 (14 tablets), 4 (15 tablets) or 6 (for 15 tablets) of blister packs together with instructions for use placed in a cardboard box.
Hypersensitivity to lercanidipine, other dihydropyridine derivatives or any component of the formulation; untreated heart failure; unstable angina; vascular obstruction originating from the left ventricle of the heart; period within 1 month after myocardial infarction; severe renal impairment (creatinine clearance less than 30 mL / min); lactose intolerance, lactase deficiency, glyukozogalaktoznoy malabsorption syndrome; pregnancy and lactation; use in women of childbearing age who are not using reliable methods of contraception; age 18 years (effectiveness and safety have been studied); simultaneous application of drugs: inhibitors of CYP3A4 (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin); cyclosporine; concomitant use of medication Lerkamen® 10 with grapefruit juice.
Renal failure (creatinine clearance of more than 30 ml / min) and / or liver failure mild to moderate severity, elderly, sick sinus syndrome (without a pacemaker), ischemic heart disease, left ventricular dysfunction.
10 mg
Essential hypertension I – II severity.
Interaction with other drugs
Lercanidipine may be applied simultaneously with beta-blockers, diuretics, angiotensin converting enzyme (ACE) inhibitors.
With simultaneous use of metoprolol, lercanidipine bioavailability is reduced by 50%. This effect may occur, and while the use of other beta-blockers, and may require correction of lercanidipine dosage to achieve a therapeutic effect in the given combination. Lercanidipine is metabolized with the participation of CYP3A4 isoenzyme, therefore, inhibitors and inducers of this isoenzyme, while the application can affect the metabolism and elimination of lercanidipine. Not recommended simultaneous application lercanidipine CYP3A4 inhibitor (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) (see. The section “Contra ‘).
We do not recommend the use of cimetidine and simultaneous lercanidipine, since an increase in concentration of both substances in the blood plasma is observed (see. The section “Contra ‘).
Caution should be exercised while the use of lercanidipine other subsratami CYP3A4 (terfenadine, astemizole, class III antiarrhythmics, e.g., amiodarone, kvinidin).
With simultaneous use of lercanidipine 20 mg midazolam bioavailability of lercanidipine in elderly patients can be increased by approximately 40%.
Lercanidipine may be used with caution in conjunction with inductors CYP3A4, e.g., anticonvulsants (phenytoin, carbamazepine) and rifampicin as possible to reduce the antihypertensive effect of the drug. Requires regular monitoring of blood pressure.
With simultaneous use of lercanidipine 20 mg in patients continuously receiving beta methyldigoxin, there was no pharmacokinetic interaction, while in healthy volunteers treated with digoxin, showed an increase in value of Cmax (maximum concept of plasma) for digoxin in average 33% after receiving 20 mg lercanidipine fasting when it UAC (area under curve – “concentration – time”) and renal clearance changed slightly. It is necessary to control the presence of signs of digoxin toxicity in patients receiving both digoxin and lercanidipine.
The simultaneous use of lercanidipine with cimetidine (800 mg) does not cause significant changes in the concentrations of lercanidipine in the blood plasma. At high doses of cimetidine may increase the bioavailability of lercanidipine and antihypertensive action.
With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), AUC value for simvastatin increased by 56%, while the same value for its active metabolite – beta-hydroxy acids – 28%. When receiving the drugs at different times of the day (lercanidipine – morning, simvastatin – in the evening), you can avoid unwanted interaction.
When odvremennom application of 20 mg lercanidipine and warfarin in healthy volunteers changes farmakinetiki warfarin was not observed.
The simultaneous use of fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients had no clinically significant changes in the pharmacokinetics of lercanidipine.
May increase antihypertensive effects while taking grapefruit juice and lercanidipine (see. Section “Contraindications”).
Ethanol can potentiate the antihypertensive effect of lercanidipine.
Presumably, in the case of overdose lercanidipine be observed symptoms similar to those of other derivatives dihydropiridine overdose (peripheral vasodilation with pronounced decrease A and reflex tachycardia).
Treatment is symptomatic; in the case of significant decrease in blood pressure, loss of consciousness is a cardiovascular therapy bradycardia intravenous atropine.
There is evidence of 3 cases of overdose when lercanidipine in doses of 150 mg, 280 mg and 800 mg for the purpose of suicide.
In case of receiving 150 mg lercanidipine + alcohol (unknown number) somnolence observed. Treatment: gastric lavage, administration of activated charcoal.
In case of receiving 280 mg lercanidipine + 5.6 mg moxonidine were observed following symptoms: cardiogenic shock, severe myocardial ischemia, renal failure mild. Treatment: cardiac glycosides, diuretics (furosemide), high doses of catecholamine plasma expanders.
In case of receiving 800 mg lercanidipine and nausea were observed marked reduction in blood pressure.
Treatment: administration of activated charcoal and a laxative, intravenously – dopamine. In all cases of overdose, all patients were alive.
Information on the efficiency of dialysis for lercanidipine absent. Most likely, because of high communication lercanidipine CROI plasma proteins, dialysis can be inefficient.
pharmachologic effect
Pharmacological group:
Selective blockers of calcium channels with advantageous effects on blood vessels.
Lercanidipine is a selective blocker of the “slow” calcium channel dihydropyridine derivative, inhibits the transmembrane current of calcium ions into vascular smooth muscle cells. Mechanism hypotensive action is due to a direct relaxant effect on vascular smooth-muscle cells, resulting in decreased total peripheral vascular resistance. Despite the relatively short elimination half-life from the blood plasma, lercanidipine has a prolonged action because of the high distribution coefficient of the membrane. Due to its high vascular selectivity has no negative inotropic effects. Acute hypotension with reflex tachycardia is rare due to the gradual development of vasodilation when lercanidipine. Lercanidipine is a racemic mixture of (+) – R- and (-) S- enantiomers. Antihypertensive effect of lercanidipine, primarily driven S-enantiomer.
Lercanidipine is completely absorbed after ingestion. Maximum plasma concentration (Cmax) achieved was 1.5-3 hours and 3.3 ± 2.09 ng / ml and 7.66 ± 5.90 ng / ml after receiving the 10 and 20 mg lercanidipine, respectively.
(+) – R- and (-) S- enantiomers of lercanidipine demonstrate similar pharmacokinetic profile: have the same time to reach maximum concentration (TSmax), the same half-life (T 1/2); values ​​Cmax and area under the curve – “concentration-time» (AUC) is 1.2 times higher for (-) – S enantiomer.
Interconversion of enantiomers in In vitro experiments were observed. By “primary pass” through the liver, the absolute bioavailability of lercanidipine when administered after a meal is about 10%, when receiving the value of fasting bioavailability is reduced by 1/3. When lercanidipine not later than 2 hours after a fatty meal bioavailability is increased 4 times, and the drug Lerkamen® 10 not to be taken after meals. Upon oral administration of lercanidipine its plasma concentration is not directly proportional to the dose received (non-linear kinetics). Saturation of first-pass metabolism, occurs gradually. Thus, bioavailability increases with increasing dose. Distribution from plasma into tissues and organs is rapid and extensive. Communication with plasma proteins exceeds 98%. In patients with severe renal and / or hepatic insufficiency, due to the decrease in the concentration of protein in blood plasma free fraction of lercanidipine may be increased. Lercanidipine metabolized involving CYP3A4 isozyme to inactive metabolites. About 50% of the dose is excreted by the kidneys (bowel displayed about 50%). Elimination occurs mainly through biotransformation.
Mean value of T 1/2 is 8-10 hours. The duration of therapeutic action – 24 hours. Cumulation of lercanidipine with repeated ingestion is not observed. It was proved that lercanidipine farmakinentika, elderly patients, patients with renal failure (creatinine clearance (CC) of more than 30 ml / min) and in patients with hepatic insufficiency mild to moderate severity with pharmacokinetics similar to that observed in the general population of patients. In patients with renal impairment (creatinine clearance less than 30 mL / min) and in patients on hemodialysis, lercanidipine plasma concentrations were higher (approximately 70%). In patients with liver failure secondary to severe, systemic bioavailability of lercanidipine is probably increased because lercanidipine is metabolized primarily in the liver.
Pregnancy and breast-feeding
Use of the drug Lerkamen® 10 during pregnancy and lactation, and in women of childbearing age in the absence of reliable contraception is contraindicated. Preclinical studies revealed no teratogenic effect of lercanidipine in rats and rabbits, reproductive function of rats was unchanged. Since absent clinical experience with lercanidipine in pregnancy and lactation and it is known that other derivatives of dihydropyridine is teratogenic in animals, lercanidipine is not recommended during pregnancy and in women of childbearing age, non-using reliable methods of contraception. Due to the high lipophilicity of lercanidipine, it is possible to assume its penetration into breast milk, therefore not recommended for use during breastfeeding.
Conditions of supply of pharmacies
On prescription.
side effects
Possible side effects are listed below in descending frequency of occurrence: often (1/100) infrequently (1/1000), rare (1/10000), very rarely (
Disorders of the nervous system
Uncommon: headache, dizziness,
Rare: drowsiness.
Violations of the cardiovascular system
Uncommon: palpitations, tachycardia, “tides” of blood to the facial skin;
Rare: angina pectoris, chest pain;
Very rare: syncope, patients with angina may increase the frequency, duration and severity of attacks.
Disorders of the gastrointestinal tract
Rare: nausea, dyspepsia, diarrhea, epigastric pain and vomiting.
Violations of the skin and subcutaneous tissue
Rare: skin rash.
Violations of the kidneys and the urinary tract
Rare: polyuria.
Violation of a general nature
Uncommon: peripheral edema;
Rare: asthenia, fatigue.
Violations by the immune system
Very rare: hypersensitivity reactions.
There are reports on the following side is very rare (
special instructions
Effects on ability to drive vehicles and management mechanisms
Since the therapy drug Lerkamen® 10 may cause dizziness, asthenia, fatigue and in rare cases of drowsiness, during treatment, patients should be with extreme caution to drive and engage in other potentially hazardous activities that require high speed of psychomotor reactions.
Storage conditions
At a temperature of not higher than 30 ° C.
Keep out of the reach of children!.
Dosing and Administration
10 mg (1 tablet formulation Lerkamen® 10) into 1 time a day for at least 15 minutes before a meal, preferably in the morning, without chewing, with a sufficient amount of water. Depending on individual patient tolerance of the drug, the dose may be increased to 20 mg (2 tablets of the preparation Lerkamen® 10). The therapeutic dose is selected gradually as the maximum antihypertensive effects develop approximately 2 weeks after initiation of dosing.
It is unlikely that efficacy will increase with increasing doses of over 20 mg / day, at the same time increases the risk of side effects.
Use in elderly patients
Pharmacokinetic profile and clinical data indicate that elderly patients correction dose Lerkamen® 10 is not required. However, caution should be exercised at the initial stage of treatment Lerkamen® 10 in this group of patients.
The use in patients with impaired renal or hepatic function
In applying the drug Lerkamen® 10 patients with renal or hepatic insufficiency mild or moderate severity caution.
In the presence of renal failure (creatinine clearance of more than 30 ml / min) or hepatic insufficiency mild to moderate severity, the initial dose is 10 mg, and then with caution increasing the dose to 20 mg per day.
The antihypertensive effect can be enhanced in patients with hepatic insufficiency mild to moderate severity and may require adjustment (reduction) dose.
In renal failure (creatinine clearance less than 30 mL / min) or hepatic failure, severe drug use gravity Lerkamen® 10 contraindicated (see. The section “Contra ‘).
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg

Berlin Chemie

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