Lernicor
Lernicor: 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: Lernicor
ATX code: C08CA13
Active ingredient: lercanidipine (Lercanidipine)
Manufacturer: JSC "FP" Obolenskoye "(Russia)
Description and photo updated: 2019-29-07
Prices in pharmacies: from 244 rubles.
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Lernicor is an antihypertensive drug.
Release form and composition
Ghtgfhfn is available in the form of film-coated tablets: biconvex, round, with a yellow (10 mg dosage) or pink (20 mg dosage) coating; the core in the cross section has a light yellow color (7, 10, 14 or 28 pcs. in a blister strip made of aluminum foil and polyvinyl chloride film, in a cardboard box 1, 2, 3 or 4 packages and instructions for use of Lernicor).
1 film-coated tablet contains:
- active substance: lercanidipine hydrochloride - 10 or 20 mg;
- additional components: sodium carboxymethyl starch (sodium starch glycolate), microcrystalline cellulose, povidone K30, lactose monohydrate, magnesium stearate;
- film shell: Opadry II 85F38107 yellow (dosage 10 mg) / Opadry II 85F34555 pink (dosage 20 mg) - macrogol (polyethylene glycol), titanium dioxide, polyvinyl alcohol, talc; additionally for a dosage of 10 mg - iron oxide red, aluminum varnish based on quinoline yellow dye; additionally for a dosage of 20 mg - varnish based on charming red dye, aluminum varnish based on azorubine dye, aluminum varnish based on sunset yellow dye.
Pharmacological properties
Pharmacodynamics
Lercanidipine is a 1,4-dihydropyridine derivative, a selective slow calcium channel blocker (BMCC), a calcium antagonist that suppresses the transmembrane flow of calcium ions into the smooth muscle cells of the vascular walls.
Lercanidipine is an equimolar mixture of (+) - R- and (-) S-enantiomers. The antihypertensive effect of the active substance is primarily determined by the S-enantiomer. The mechanism of the antihypertensive action of the agent is due to a direct relaxing effect on the cells of vascular smooth muscles, which in turn causes a decrease in the total peripheral vascular resistance (OPSS).
Despite the relatively short half-life (T ½) of lercanidipine from blood plasma, the drug has a prolonged hypotensive effect due to the high value of the membrane distribution coefficient. The substance does not show a negative inotropic effect due to its inherent high vascular selectivity. Acute arterial hypotension with reflex tachycardia when using the drug rarely occurs due to the gradual development of the vasodilation process.
Lercanidipine is metabolically neutral and does not significantly affect the serum level of lipoproteins and apolipoproteins in the blood, and does not lead to a change in the lipid profile in patients with arterial hypertension.
Pharmacokinetics
After oral administration, the active substance of Lernicor is completely absorbed. In blood plasma, the maximum concentration of lercanidipine (C max) is observed 1.5–3 hours after its administration at a dose of 10 and 20 mg and is equal to 3.3 ± 2.09 and 7.66 ± 5.9 ng / ml, respectively. (+) - R- and (-) S-enantiomers of the agent are characterized by a similar pharmacokinetic profile - they have the same T ½ and time to reach C max (T max); the area under the concentration-time curve (AUC) and C max are about 1.2 times higher for the (-) S-enantiomer. In the course of in vivo experiments, the interconversion of enantiomers was not recorded.
The absolute bioavailability of lercanidipine during its primary passage through the liver when taken orally after meals is approximately 10%, and when used on an empty stomach decreases by ⅓. If the drug is taken no later than 2 hours after eating fatty foods, its bioavailability increases by 4 times, therefore it is not recommended to take Lernicor after meals. In the case of oral use of the drug, the level of its content in the blood plasma is not directly proportional to the administered dose (nonlinear kinetics). The saturation of the presystemic metabolism is carried out gradually, from which it follows that the bioavailability of Lernicor increases with increasing dose.
From blood plasma, the active substance is rapidly and extensively distributed to tissues and organs. It binds to plasma proteins by more than 98%. Lercanidipine is metabolized by the action of the CYP3A4 isoenzyme with the formation of inactive metabolites. Approximately 50% of the dose taken is excreted in the urine, the remaining 50% in the feces. Elimination is carried out mainly through biotransformation. On average, T ½ is 8-10 hours, the duration of the therapeutic effect is 24 hours. With repeated oral administration, the cumulation of the active substance is not observed.
It was found that the pharmacokinetics of lercanidipine in patients with renal dysfunction with creatinine clearance (CC) exceeding 30 ml / min, in patients with mild to moderate hepatic insufficiency and in elderly patients is similar to the pharmacokinetics recorded in the general group of patients.
In the presence of severe renal and / or hepatic failure, due to a decrease in the plasma protein level in the blood, an increase in the free fraction of lercanidipine is possible.
In patients on hemodialysis and in patients with severe renal dysfunction, with a CC below 30 ml / min, there are higher (approximately 70%) plasma concentrations of lercanidipine in the blood.
In patients with moderate and severe hepatic impairment, the systemic bioavailability of lercanidipine is likely to increase, since its biotransformation occurs mainly in the liver.
Indications for use
Lernicor is indicated for the treatment of arterial hypertension of 1 and 2 degrees.
Contraindications
Absolute:
- unstable angina;
- a period of one month after myocardial infarction;
- untreated chronic heart failure (CHF);
- obstruction of the outflow tract of the left ventricle;
- severe renal failure (CC less than 30 ml / min);
- severe liver failure;
- use in women of reproductive age who do not use effective contraception;
- syndrome of glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- pregnancy and lactation;
- age up to 18 years;
- combined use with erythromycin, ketoconazole, ritonavir, itraconazole, troleandomycin and other potent inhibitors of the CYP3A4 isoenzyme;
- simultaneous reception with cyclosporine, grapefruit juice;
- hypersensitivity to any component of the drug, as well as to any of the dihydropyridines.
Relative (it is required to take Lernicor tablets with caution):
- sick sinus syndrome (without an artificial pacemaker);
- dysfunction of the left ventricle;
- ischemic heart disease (CHD);
- mild to moderate hepatic dysfunction;
- renal failure (CC more than 30 ml / min);
- elderly age.
Lernicor, instructions for use: method and dosage
Lernicor tablets are taken orally, 1 time per day, preferably in the morning, at least 15 minutes before meals. The tablets are swallowed whole without chewing or crushing, drinking plenty of water.
The recommended daily dose is 10 mg, if necessary, depending on individual tolerance, it is possible to increase the daily dose to 20 mg, performed 14 days after the start of the course. It is required to select a therapeutic dose gradually, due to the fact that the maximum antihypertensive effect is observed on average 14 days after the start of Lernicor's use.
It is unlikely that with an increase in the daily dose above 20 mg, the effectiveness of lercanidipine will increase, but the threat of adverse reactions will increase.
Side effects
Unwanted disorders that may occur when taking Lernicor (classified as follows: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1 / 10 000 and <1/1000, extremely rarely - <1/10 000, including isolated cases):
- digestive system: rarely - epigastric pain, dyspepsia, vomiting, nausea, diarrhea; extremely rare - gingival hyperplasia, increased activity of hepatic transaminases;
- cardiovascular system: infrequently - increased heart rate, flushing of the face, tachycardia; rarely - painful sensations behind the sternum, angina pectoris; extremely rarely - a significant decrease in blood pressure (BP), myocardial infarction, fainting; in patients with angina pectoris, the frequency, duration and severity of attacks may increase;
- nervous system: infrequently - dizziness, headache; rarely - drowsiness;
- respiratory system, chest and mediastinal organs: extremely rare - chest pain;
- musculoskeletal system, connective tissue: rarely - myalgia;
- skin and subcutaneous tissue: rarely - skin rashes;
- immune system: extremely rare - hypersensitivity reactions;
- kidneys and urinary tract: rarely - polyuria; extremely rare - an increase in the frequency of urination;
- general disorders: infrequently - peripheral edema; rarely - asthenia, severe fatigue.
Overdose
Symptoms of an overdose of Lernicor may include peripheral vasodilation with an excessive decrease in blood pressure and reflex tachycardia, since it is assumed that in case of an overdose of lercanidipine, disorders similar to those of an overdose of other dihydropyridine derivatives may occur.
Treatment is symptomatic. With a significant decrease in blood pressure, loss of consciousness, cardiovascular therapy is necessary, with bradycardia - intravenous (iv) administration of atropine. Three cases of lercanidipine overdose for suicide have been reported when using the drug at doses of 150, 280 and 800 mg. All patients survived.
With the combined use of lercanidipine at a dose of 150 mg with ethanol at an unknown dose, the appearance of drowsiness was observed. Gastric lavage and the introduction of activated charcoal were prescribed.
Against the background of the combined use of lercanidipine at a dose of 280 mg and moxonidine at a dose of 5.6 mg, severe myocardial ischemia, cardiogenic shock, and mild renal failure were noted. In this case, therapy was carried out using cardiac glycosides, furosemide or other diuretics, catecholamines in high doses, plasma substitutes.
After taking lercanidipine at a dose of 800 mg, disorders such as nausea and an excessive decrease in blood pressure were recorded. Appointed to take activated charcoal and laxatives, intravenous infusion of dopamine.
There is no data on the effectiveness of hemodialysis in case of an overdose of Lernicor, however, given the high degree of binding of the agent to plasma proteins, it is most likely that its appointment will be ineffective.
special instructions
The intake of certain dihydropyridines in patients with coronary artery disease may be associated with the threat of increased frequency of angina attacks. As a consequence, in such patients, drug treatment must be carried out with extreme caution.
Influence on the ability to drive vehicles and complex mechanisms
Patients driving vehicles or working with other complex mechanisms during the period of Lernicor therapy must be careful due to the possible appearance of increased fatigue, dizziness, asthenia, drowsiness.
Application during pregnancy and lactation
Treatment with Lernicor is contraindicated during pregnancy and in women of childbearing age who do not use reliable contraception. According to the data of preclinical studies of lercanidipine in animals, no teratogenic effect was found, however, when using other derivatives of dihydropyridine, a teratogenic effect was revealed.
Since lercanidipine is highly lipophilic, it can be assumed that it is able to penetrate into breast milk. As a result, taking Lernicor during lactation is contraindicated.
Pediatric use
In persons under 18 years of age, Lernicor therapy is contraindicated, since there are no data confirming its effectiveness and safety in patients of this age group.
With impaired renal function
In case of severe renal dysfunction (CC less than 30 ml / min), Lernicor is contraindicated.
In the presence of mild or moderate renal failure, caution should be exercised and therapy should be started with a daily dose of 10 mg with its further gradual increase to 20 mg, taking into account the severity of the hypotensive effect.
For violations of liver function
In the presence of severe hepatic insufficiency, Lernicor therapy is contraindicated.
With hepatic dysfunction of mild or moderate severity, the initial daily dose of Lernicor should be 10 mg, then with caution it can be increased to 20 mg. In the case of an increase in the antihypertensive effect, a dose reduction is required.
Use in the elderly
Elderly patients do not need to change the daily dose of the drug based on the pharmacokinetic profile and data from clinical studies. However, when prescribing Lernicor to patients of this age group, care must be taken, especially at the beginning of the course.
Drug interactions
- metoprolol: there is a 50% decrease in the bioavailability of lercanidipine; this effect can also be recorded when used in combination with other beta-blockers, as a result of which a dose adjustment may be necessary to achieve a positive treatment result;
- angiotensin-converting enzyme inhibitors (ACE inhibitors), diuretics, beta-blockers: combination therapy of these drugs with Lernicor is possible;
- inducers and inhibitors of the CYP3A4 isoenzyme: the CYP3A4 isoenzyme is responsible for the biotransformation of lercanidipine, therefore inhibitors and inducers of this isoenzyme can affect the metabolism and elimination of the drug; concomitant use of lercanidipine with potent CYP3A4 inhibitors is contraindicated;
- cyclosporine: an increase in the content of both drugs in plasma is recorded, therefore, combination therapy of this substance with Lernicor is contraindicated;
- CYP3A4 inducers, including rifampicin and anticonvulsants (carbamazepine, phenytoin): the hypotensive effect of lercanidipine may decrease; systematic monitoring of blood pressure is required;
- midazolam: there is an increase in the bioavailability of lercanidipine in elderly patients by an average of 40% when it is combined at a dose of 20 mg with this substance;
- substrates of the isoenzyme CYP3A4 (quinidine, amiodarone and other class III antiarrhythmics, terfenadine, astemizole): care must be taken with this combination;
- digoxin: no pharmacokinetic interaction was recorded when using Lernicor at a dose of 20 mg against the background of a course of beta-methyldigoxin intake, however, in healthy volunteers who took digoxin, there was an increase in the C max of this substance in plasma by approximately 33% after using an empty stomach of lercanidipine at a dose of 20 mg, while AUC and renal clearance of digoxin did not change significantly; against the background of this combination, it is necessary to control possible signs of digoxin intoxication;
- simvastatin (at a dose of 40 mg): when combined with lercanidipine (at a dose of 20 mg), the AUC value for simvastatin increases by 56%, and for β-hydroxy acid (its active metabolite) - by 28%; you can prevent unwanted interactions when using these drugs at different times of the day - take Lernicor in the morning, and simvastatin in the evening;
- cimetidine (at a dose of less than 800 mg): there are no significant changes in the level of lercanidipine in the blood plasma, however, with the introduction of cimetidine in high doses, caution is required due to the aggravated risk of increased bioavailability of lercanidipine and increased antihypertensive effect;
- warfarin: no change in the pharmacokinetics of this substance is recorded when used simultaneously in healthy volunteers with lercanidipine at a dose of 20 mg;
- ethanol, grapefruit juice: potentiation of the antihypertensive effect of Lernicor is possible;
- fluoxetine (an inhibitor of CYP3A4 and CYP2D6): in elderly patients, no clinically significant changes in the pharmacokinetics of lercanidipine are detected when combined with this substance.
Analogs
Analogs of Lernikor are: Lerkamen 20, Lerkanorm, Lercanidipin-SZ, Lerkamen 10, Zanidip-Recordati, etc.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C, out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lernicor
The few reviews about Lernicor left by patients on medical websites are mostly positive. Many reviews note the good results of treatment with a drug of mild to moderate hypertension. However, patients often also complain of the development of undesirable reactions during therapy in the form of weakness, drowsiness, edema, and flushing of the skin of the face. Some reviews point to a very weak Lernicor effect.
The price of Lernicor in pharmacies
The price of Lernicor for a package containing 28 film-coated tablets can be: 10 mg dosage - 220-265 rubles, 20 mg dosage - 360-407 rubles.
Lernicor: prices in online pharmacies
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Drug name Price Pharmacy |
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Lernicor 10 mg film-coated tablets 28 pcs. 244 RUB Buy |
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Lernicor 20 mg film-coated tablets 28 pcs. 336 r Buy |
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Lernicor tablets p.p. 20mg 28 pcs. 386 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
