Lercanorm
Lercanorm: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Lerkanorm
ATX code: C08CA13
Active ingredient: lercanidipine (Lercanidipine)
Manufacturer: JSC "VERTEX" (Russia)
Description and photo updated: 2019-29-07
Prices in pharmacies: from 262 rubles.
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Lercanorm is an antihypertensive drug, a latest generation calcium antagonist for the treatment of a wide range of patients, including those with diabetes mellitus, obesity, severe hypertension and elderly patients.
Release form and composition
The drug is produced in the form of film-coated tablets: biconvex, round, yellow film shell, a pale yellow cross-sectional core (10, 15 or 30 pcs. In a blister strip made of PVC film or aluminum foil and PVC film, in a cardboard box 3, 6 or 9 packs of 10 pcs., 2, 4 or 6 - 15 pcs., 1, 2 or 3 - 30 pcs.; 30, 60 or 90 pcs. in a polyethylene can, in cardboard box of 1 can. Each box also contains instructions for the use of Lercanorm).
1 film-coated tablet contains:
- active substance: lercanidipine hydrochloride - 10 or 20 mg;
- additional components: lactose monohydrate, microcrystalline cellulose, sodium carboxymethyl starch (sodium starch glycolate type A), magnesium stearate, poloxamer, povidone K30;
- film shell: hyprolose (hydroxypropyl cellulose), titanium dioxide, hypromellose, talc, yellow iron oxide (iron oxide).
Pharmacological properties
Pharmacodynamics
Lercanidipine belongs to the group of selective slow calcium channel blockers (CCBs), derivatives of 1,4-dihydropyridine. The active substance inhibits the movement of calcium ions through the cell membranes into the smooth muscle cells of the vascular walls. The main mechanism of the antihypertensive action of Lercanorm is a direct relaxing effect on vascular smooth muscle cells, which leads to a decrease in total peripheral vascular resistance (OPSS). Although lercanidipine has a relatively short half-life (T 1/2) from blood plasma, the substance exhibits a long-term antihypertensive effect as a result of a sufficiently high coefficient of membrane distribution.
The therapeutic effect of the drug is observed 5-7 hours after its oral administration and lasts for 24 hours. Lercanidipine has a high selectivity for vascular smooth muscle cells, so it does not have a negative inotropic effect.
Due to the gradual development of vasodilation when using Lercanorm, a significant decrease in blood pressure (BP), accompanied by reflex tachycardia, is rarely observed.
Lercanidipine is a racemic mixture of (+) R- and (-) S-enantiomers, its antihypertensive effect, like other asymmetric derivatives of 1,4-dihydropyridine, mainly determines the S-enantiomer.
Pharmacokinetics
Lercanidipine is completely absorbed after oral administration. In the blood plasma, the maximum concentration (C max) of the active substance is reached 1.5-3 hours after taking a dose of Lercanorm 10 mg and 20 mg and is 3.3 ± 2.09 and 7.66 ± 5.90 ng / ml, respectively …
The (+) R- and (-) S-enantiomers of the drug have a similar pharmacokinetic profile: they have the same T 1/2 and the period of reaching C max. The area under the concentration-time curve (AUC) and plasma C max in blood of the (-) S-enantiomer of lercanidipine are approximately 1.2 times higher than those of the (+) R-enantiomer. In experiments in vivo, the interconversion of enantiomers was not recorded.
With the primary passage through the liver, the absolute bioavailability of lercanidipine due to oral administration after meals is approximately 10%. In the case of using the drug on an empty stomach, bioavailability is ⅓ of the indicator determined after eating. Taking Lercanorm no later than 2 hours after eating food rich in fats increases bioavailability by 4 times, so the drug should be taken before meals.
In the range of therapeutic doses, the pharmacokinetics of the active substance is non-linear. When using Lercanorm doses of 10, 20 and 40 mg, AUC was determined in a ratio of 1: 4: 18, and C max in plasma in a ratio of 1: 3: 8, respectively, this indicates an increasing saturation during primary passage through the liver. Thus, it can be concluded that the bioavailability of the drug increases with an increase in the dose taken.
Lercanidipine is characterized by rapid distribution from plasma to tissues and organs. The active substance binds to blood plasma proteins by more than 98%. In the presence of severe renal and liver dysfunction, the free fraction of lercanidipine may increase, since against the background of such diseases, the plasma level of protein in the blood decreases.
The process of metabolism of the active substance proceeds with the participation of the isoenzyme CYP3A4 with the formation of inactive metabolites. The elimination of lercanidipine is carried out mainly through biotransformation. Approximately 50% of the dose taken is excreted by the kidneys, approximately 50% through the intestines. The T 1/2 value averages 8-10 hours. With repeated oral administration, the accumulation of lercanidipine is not recorded.
The pharmacokinetics of Lercanorm in patients with renal insufficiency with creatinine clearance (CC) above 30 ml / min, in patients with mild to moderate liver dysfunction and in the elderly is similar to the pharmacokinetics in healthy volunteers.
Indications for use
Lercanorm is recommended for the treatment of grade I – II essential hypertension.
Contraindications
Absolute:
- obstruction of the outflow tract of the left ventricle;
- unstable angina;
- untreated heart failure;
- a period of 1 month after suffering a myocardial infarction;
- severe liver failure;
- severe renal failure (CC below 30 ml / min);
- syndrome of glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
- age up to 18 years;
- pregnancy and lactation;
- failure to use reliable methods of contraception by women of childbearing age;
- combination therapy with inhibitors of the CYP3A4 isoenzyme, such as erythromycin, ketoconazole, troleandomycin, ritonavir, itraconazole;
- simultaneous use with cyclosporine and grapefruit juice;
- hypersensitivity to lercanidipine or other dihydropyridine derivatives, or any additional component of the drug.
Relative (you should take Lercanorm tablets with caution):
- dysfunction of the left ventricle;
- sick sinus syndrome, without a pacemaker (due to the existing risk of increased frequency of angina attacks);
- chronic heart failure (CHF) (must be compensated before using the drug);
- ischemic heart disease (CHD);
- mild to moderate renal failure (CC above 30 ml / min);
- mild to moderate liver failure;
- elderly age;
- simultaneous use with substrates and inhibitors of the CYP3A4 isoenzyme, digoxin.
Lercanorm, instructions for use: method and dosage
Lercanorm tablets should be taken orally 1 time a day in the morning, at least 15 minutes before meals, without breaking or chewing, drinking plenty of water.
The recommended starting dose is 10 mg. Given the individual tolerance of Lercanorm and the therapeutic effect, it can be increased to 20 mg. Dose selection is required gradually, since the maximum antihypertensive effect is observed approximately 2 weeks after the start of the course of therapy.
With an increase in the daily dose of more than 20 mg, it is unlikely that the effectiveness of the drug will increase, but the threat of side effects will worsen.
Side effects
- cardiovascular system: infrequently - flushing of the face, tachycardia, palpitations; rarely - chest pain, angina pectoris; extremely rarely - a pronounced decrease in blood pressure, fainting, myocardial infarction; in the presence of angina pectoris, an increase in the duration, frequency and severity of attacks is possible;
- musculoskeletal system: rarely - myalgia;
- nervous system: infrequently - dizziness, headache; rarely - drowsiness;
- digestive system: rarely - dyspepsia, nausea, abdominal pain, diarrhea, vomiting;
- urinary system: rarely - polyuria; extremely rare - an increase in the frequency of urination (pollakiuria);
- allergic reactions: extremely rare - hypersensitivity reactions;
- skin: rarely - skin rash;
- laboratory parameters: extremely rarely - a reversible increase in the activity of hepatic transaminases;
- others: infrequently - peripheral edema; rarely - increased fatigue, asthenia; extremely rare - gingival hyperplasia.
Overdose
Presumably, an overdose of lercanidipine is accompanied by symptoms similar to those of an overdose of other dihydropyridines, namely: peripheral vasodilation with reflex tachycardia and a significant decrease in blood pressure, nausea.
Treatment is symptomatic. With a pronounced decrease in blood pressure and loss of consciousness, cardiovascular therapy is recommended, with the appearance of bradycardia, intravenous (i / v) administration of atropine is indicated. There is no data on the use of hemodialysis, but knowing the high degree of binding of the drug to plasma proteins, it can be assumed that dialysis will be ineffective.
3 cases of lercanidipine overdose were recorded when taken in doses of 150, 280 and 800 mg. The patients survived in all three cases.
Drowsiness was observed against the background of the simultaneous use of lercanidipine at a dose of 150 mg with ethanol at an unknown dose. In this condition, gastric lavage and intake of activated carbon were performed.
In the case of a combination of lercanidipine at a dose of 280 mg and moxonidine at a dose of 5.6 mg, disorders such as mild renal failure, severe myocardial ischemia, and cardiogenic shock were observed. With these symptoms, diuretics (furosemide), cardiac glycosides, catecholamines in large doses, and plasma substitutes were administered.
While taking lercanidipine at a dose of 800 mg, nausea and a significant decrease in blood pressure were observed. Treatment - oral intake of laxatives and activated charcoal, intravenous dopamine.
special instructions
Lercanorm is prescribed with extreme caution in patients with left ventricular dysfunction, although controlled hemodynamic studies have not found any deterioration in left ventricular function.
Patients with coronary artery disease receiving treatment with short-acting dihydropyridines may presumably be at high risk for diseases of the cardiovascular system.
Influence on the ability to drive vehicles and complex mechanisms
During the period of Lercanorm therapy, due to the risk of dizziness, headache, drowsiness and asthenia (especially at the beginning of the course and in case of an increase in the dose), it is necessary to drive vehicles and other complex and potentially dangerous mechanisms with extreme caution.
Application during pregnancy and lactation
According to the results of studies carried out on animals, the drug did not show teratogenic effects. At the same time, this effect was recorded during therapy with other dihydropyridine derivatives. Therefore, the use of Lercanorm during pregnancy and in women of reproductive age who do not use reliable contraception is contraindicated.
During lactation, taking an antihypertensive drug is also contraindicated, since, as a result of high lipophilicity, it is assumed that it can penetrate into breast milk.
Pediatric use
For patients under 18 years of age, Lercanorm therapy is contraindicated due to the lack of data confirming its effectiveness and safety in children and adolescents.
With impaired renal function
In patients with severe renal failure, with a CC below 30 ml / min, and in persons receiving hemodialysis treatment, the plasma content of lercanidipine in the blood increases by an average of 70%.
In severe renal failure, the use of Lercanorm is contraindicated. Patients with moderate or mild renal insufficiency should use the drug with caution, starting the course of treatment with a daily dose of 10 mg. In the future, the dose should be increased to 20 mg, taking into account the severity of the hypotensive effect.
For violations of liver function
In the presence of moderate to severe hepatic failure, the systemic bioavailability of lercanidipine is presumably increased, since the drug is metabolized primarily in the liver.
Lercanorm therapy is contraindicated in patients with severe hepatic insufficiency.
In patients with mild or moderate hepatic impairment, the initial daily dose of the drug should not exceed 10 mg. It is recommended to increase the dose to 20 mg per day, especially in the initial stages of therapy, with extreme caution. In the case when a strongly pronounced antihypertensive effect is observed after increasing the dose, the dose should be reduced.
Use in the elderly
Elderly patients do not need to change the dose of Lercanorm, but during the period of treatment, especially at the beginning of the course, it is recommended to be careful.
Drug interactions
- beta-blockers, angiotensin-converting enzyme inhibitors, diuretics: simultaneous administration of these drugs with lercanidipine is allowed;
- erythromycin, itraconazole, ritonavir, ketoconazole, troleandomycin (inhibitors of the CYP3A4 isoenzyme): the combination is contraindicated, since inducers and inhibitors of the CYP3A4 isoenzyme, when used in combination with lercanidipine, may affect its metabolism and excretion;
- metoprolol: there is a 50% decrease in the bioavailability of lercanidipine, a dose adjustment of the latter may be necessary to achieve the effect of therapy;
- cyclosporine: an increase in the plasma level of both substances in the blood is recorded, as a result of which the combination with lercanidipine is contraindicated;
- midazolam: in the elderly, an increase in the bioavailability of lercanidipine by an average of 40% may be observed when combined with the latter at a dose of 20 mg;
- amiodarone, quinidine and other class III antiarrhythmic drugs, astemizole, terfenadine (substrates of the CYP3A4 isoenzyme): care must be taken when combined with lercanidipine;
- inducers of the isoenzyme CYP3A4 [rifampicin, anticonvulsants (carbamazepine, phenytoin)]: possibly weakening of the hypotensive effect of lercanidipine; need regular monitoring of blood pressure;
- digoxin: in patients constantly receiving digoxin, the pharmacokinetic interaction of this agent with lercanidipine, simultaneously taken at a dose of 20 mg, is not recorded; however, healthy volunteers who received digoxin showed an increase in its C max in plasma by about 33% after oral administration of lercanidipine at a dose of 20 mg on an empty stomach, at the same time, there were no significant changes in renal clearance and AUC of digoxin; with this combination, careful monitoring of possible symptoms of digoxin intoxication should be carried out;
- warfarin: no changes in the pharmacokinetic parameters of this substance were observed when combined with lercanidipine at a dose of 20 mg in healthy volunteers;
- simvastatin (40 mg): there is an increase in the AUC value for simvastatin and its active metabolite β-hydroxy acid by 56 and 28%, respectively, when combined with lercanidipine (20 mg); unwanted interactions can be avoided by using agents at different times of the day (simvastatin - in the evening, lercanidipine - in the morning);
- cimetidine (up to 800 mg): no significant changes in the plasma concentration of lercanidipine are detected; in the case of using large doses of cimetidine, it is possible to increase the bioavailability of lercanidipine and the antihypertensive effect of its administration;
- fluoxetine (inhibitor of CYP3A4 and CYP2D6): there are no clinically significant changes in the pharmacokinetic parameters of lercanidipine in elderly patients;
- ethanol, grapefruit juice: may enhance the hypotensive effect of lercanidipine.
Analogs
Lercanorm analogs are: Lercanidipin-SZ, Lerkamen 10, Zanidip-Recordati, Lerkamen 20, Lernikor, etc.
Terms and conditions of storage
Store in a place out of the reach of children, protected from light, at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lercanorm
Currently, there are not enough reviews on Lercanorm left by patients on medical sites, according to which it would be possible to objectively evaluate the effectiveness and disadvantages of an antihypertensive drug.
The price of Lercanorm in pharmacies
Price for Lercanorm, film-coated tablets, per pack containing 30 pcs. may be: 10 mg dosage - 290-320 rubles, 20 mg dosage - 360-480 rubles.
Lercanorm: prices in online pharmacies
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Drug name Price Pharmacy |
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Lercanorm 10 mg film-coated tablets 30 pcs. 262 RUB Buy |
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Lercanorm tablets p.p. 10mg 30 pcs. 292 r Buy |
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Lercanorm 20 mg film-coated tablets 30 pcs. 459 r Buy |
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Lercanorm tablets p.p. 20mg 30 pcs. 483 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
