Lercamen - instructions for use, analogs, testimonials and release forms (tablets 10 mg and 20 mg) of the drug for the treatment of essential hypertension and pressure reduction in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Lercamen. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Lercamen in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Lercamen in the presence of existing structural analogs. Use to treat essential hypertension and reduce pressure in adults,children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Lercamen - selective blocker of slow calcium channels with a predominant effect on blood vessels, dihydropyridine derivative. Inhibits the transmembrane current of calcium ions into the cells of the smooth muscles of the vessels. The mechanism of antihypertensive action of lercanidipine (the active substance of the drug Lercamen) is due to a direct relaxing action on the smooth muscle cells of the vessels, resulting in a reduced OPSS.

Despite a relatively short half-life from blood plasma, lercanidipine has a prolonged antihypertensive effect due to the high membrane distribution factor. Due to high vascular selectivity does not have a negative inotropic effect. Acute arterial hypotension with reflex tachycardia occurs rarely due to the gradual development of vasodilation with lercanidipine.

The duration of the therapeutic action is 24 hours.

Composition

Lercanidipine hydrochloride + excipients.

Pharmacokinetics

Lercanidipine is completely absorbed after ingestion. Due to the effect of the "first pass" through the liver, the absolute bioavailability of lercanidipine for oral administration after eating is approximately 10%, and when taken on an empty stomach, the bioavailability is reduced by 1/3. When lercanidipine is taken no later than 2 hours after ingestion of fatty foods, its bioavailability is increased 4-fold, so the Lercamen drug should not be taken after meals. When oral lercanidipine is used, its concentration in the blood plasma is not directly proportional to the dose taken (nonlinear kinetics). Saturation of presystemic metabolism occurs gradually. Thus, bioavailability increases with increasing doses. The distribution of blood plasma into tissues and organs occurs quickly and extensively. Binding to plasma proteins exceeds 98%. About 50% of the accepted dose is excreted by the kidneys (about 50% is excreted by the intestine). Elimination occurs mainly through biotransformation. Cumulation of lercanidipine with repeated ingestion is not observed.

Indications

• essential hypertension 1-2 degrees of severity.

Forms of release

Tablets coated with 10 mg and 20 mg.

Instructions for use and dosage

The drug is taken orally, at least 15 minutes before meals, preferably in the morning, without chewing, squeezed with enough water.

Assign 10 mg once a day. Depending on the individual tolerance of the drug to the patient, the dose can be increased to 20 mg.

Therapeutic dose is selected gradually, tk. the maximum antihypertensive effect develops approximately 2 weeks after the start of the drug. It is unlikely that the effectiveness of the drug will increase with an increase in the dose of more than 20 mg per day, while at the same time the risk of side effects increases.

The pharmacokinetic profile and clinical trial data show that in elderly patients, dose adjustment of Lercamen is not required. However, care should be taken at the initial stage of treatment with Lercamen in this group of patients.

Care should be taken when using Lercamen in patients with mild and moderate renal and hepatic insufficiency.

In renal failure (QC more than 30 ml / min) or liver failure of mild or moderate severity, the initial dose is 10 mg, then with caution increase the dose to 20 mg per day.Antihypertensive effect can be increased in patients with mild or moderate hepatic insufficiency and dose correction may be required.

With renal insufficiency (KC less than 30 ml / min) and liver failure of severe severity, the use of Lercamen is contraindicated.

Side effect

• headache;
• dizziness;
• drowsiness;
• a feeling of palpitations;
• tachycardia;
• "tides" of blood to the skin of the face;
• angina pectoris;
• pain behind the sternum;
• fainting;
• nausea, vomiting;
• dyspepsia;
• diarrhea;
• epigastric pain;
• skin rash;
• myalgia;
• polyuria;
• hypersensitivity reactions;
• peripheral edema;
• asthenia;
• increased fatigue;
• myocardial infarction (rarely);
• pollakiuria (increased frequency of urination);
• pain in the chest.

Contraindications

• untreated heart failure;
• unstable angina;
• obstruction of vessels emanating from the left ventricle of the heart;
• the period within 1 month after the transferred myocardial infarction;
• severe hepatic impairment;
• renal failure of severe degree (QC less than 30 ml / min);
• simultaneous application with inhibitors of CYP3A4 (ketoconazole, itraconazole, erythromycin, ritonavir, trolleandomycin);
• simultaneous application with cyclosporine;
• simultaneous reception with grapefruit juice;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
• pregnancy;
• lactation period (breastfeeding);
• use in women of childbearing age who do not use reliable methods of contraception;
• children and adolescents under 18 years of age (efficacy and safety not studied);
• hypersensitivity to the components of the drug;
• hypersensitivity to other dihydropyridine derivatives.

Application in pregnancy and lactation

The use of Lercamen in pregnancy and during breastfeeding, as well as in women of childbearing age in the absence of reliable contraception is contraindicated.

Pre-clinical studies showed no teratogenic effect of lercanidipine in rats and rabbits, and the reproductive function of rats was unchanged.

In view of the lack of clinical experience with lercanidipine during pregnancy and during breastfeeding, and since it is known,that other dihydropyridine derivatives had a teratogenic effect in animals, lercanidipine is not recommended for use in pregnancy and in women of childbearing age who do not use reliable contraceptive methods.

Due to the high lipophilicity of lercanidipine, it can be assumed that it penetrates into breast milk, so the drug is not recommended for use during breastfeeding

Application in elderly patients

Caution should be used in elderly patients.

Use in children

The drug is contraindicated in children and adolescents under the age of 18

special instructions

It should be used with caution in renal (KC more than 30 ml / min) and / or liver failure of mild and moderate severity, in elderly patients, with SSSU (without a pacemaker), ischemic heart disease, left ventricular dysfunction.

Impact on the ability to drive vehicles and manage mechanisms

Since Lercamen therapy may cause dizziness, asthenia, fatigue and, in rare cases, drowsiness, patients should be particularly careful in managing the vehicle and other potentially hazardous activities,requiring a high rate of psychomotor reactions.

Drug Interactions

Lercamen can be used simultaneously with beta-blockers, diuretics, ACE inhibitors.

When used simultaneously with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect can occur and with simultaneous application with other beta-blockers, so a correction of the dose of lercanidipine may be required to achieve a therapeutic effect in this combination.

Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme, so inhibitors and inducers of this isoenzyme, with simultaneous application, can influence the metabolism and excretion of lercanidipine. It is not recommended simultaneous use of lercanidipine with inhibitors of CYP3A4 (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin).

It is not recommended simultaneous use of cyclosporine and lercanidipine, tk. an increase in the concentration of both substances in the blood plasma is observed.

Caution should be exercised while using lercanidipine with other substrates CYP3A4 (terfenadine, astemizole, antiarrhythmic drugs of the 3rd class, for example, amiodarone, quinidine).

With the simultaneous use of lercanidipine in a dose of 20 mg with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40%.

Lercanidipine should be administered with caution at the same time as CYP3A4 inducers, for example, anticonvulsants (phenytoin, carbamazepine) and rifampicin, since it is possible to reduce the antihypertensive effect of the drug. Regular monitoring of blood pressure is necessary.

It is necessary to monitor the presence of signs of intoxication with Digoxin in patients taking both digoxin and lercanidipine.

Simultaneous use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in the concentration of lercanidipine in blood plasma. At high doses of cimetidine, the bioavailability and antihypertensive effects of lercanidipine may increase.

With simultaneous application of Lercamena (20 mg) and Simvastatin (40 mg), the AUC value for simvastatin increased by 56%, and the same value 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.

With simultaneous use of lercanidipine in a dose of 20 mg and warfarin, no changes in the pharmacokinetics of Warfarin were observed in healthy volunteers.

The simultaneous use of Fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients had no clinically significant changes in the pharmacokinetics of lercanidipine.

It is possible to increase the antihypertensive effect while taking the juice of grapefruit and lercanidipine.

Ethanol (alcohol) can potentiate the antihypertensive effect of lercanidipine.

Analogues of medicinal product Lerkamen

Structural analogs for the active substance:

• Zanidip Recordati;
• Lercamen 10;
• Lercamen 20;
• Lercanidipine hydrochloride.

Analogues on the pharmacological group (calcium channel blockers):

• Agen;
• Adalate;
• Acridipine;
• Altiazem PP;
• Amlodipine;
• Amlotop;
• Verapamil;
• Vertizine;
• Diltiazem;
• Isoptin;
• Kalchek;
• Cardilopin;
• Cordaflex;
• Cordipine;
• Corinfar;
• Corinfar retard;
• Leukoptin;
• Lomir;
• Nicardy;
• Nimotop;
• Nifedikap;
• Nifedipine;
• Nifecard;
• Nifelate;
• Normodipine;
• Prestan;
• The Procurator;
• Stamlo;
• Tenochek;
• Felodipine;
• Finoptin;
• Cinnarizine;
• Ecquard;
• Equator;
• Exforge;
• Enanorm.

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