Lerkamen 10
Lerkamen 10: 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: Lerkamen 10
ATX code: C08CA13
Active ingredient: lercanidipine (lercanidipinum)
Producer: Berlin-Chemie, AG (Germany)
Description and photo update: 2018-25-10
Prices in pharmacies: from 303 rubles.
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Lerkamen 10 is a selective slow calcium channel blocker.
Release form and composition
Lerkamen 10 is produced in the form of film-coated tablets: biconvex, round, from light yellow to pale yellow, with a risk on one side (in blisters of 7, 14 or 15 pcs., In a cardboard box 1 blister of 7 or 14 pcs., 2 blisters of 14 pcs., 4 or 6 blisters of 15 pcs.).
Composition of 1 tablet:
- active substance: lercanidipine hydrochloride - 0.01 g;
- auxiliary components: magnesium stearate - 0.001 g; povidone K-30 - 0.004 5 g; sodium carboxymethyl starch (type A) - 0.015 5 g; microcrystalline cellulose - 0.039 g; lactose monohydrate - 0.03 g;
- shell: opadry OY-SR-6497 - 0.003 g (iron dye yellow oxide - 0.000 037 g; macrogol 6000 - 0.000 3 g; titanium dioxide - 0.000 6 g; talc - 0.000 15 g; hypromellose - 0.001 913 g).
Pharmacological properties
Pharmacodynamics
The active substance of Lerkamen 10 - lercanidipine, is a derivative of dihydropyridine, which inhibits the transmembrane flow of calcium ions into the cells of vascular smooth muscles. The mechanism of its antihypertensive action is due to a direct relaxing effect on vascular smooth muscle cells, due to which the total peripheral resistance decreases.
Due to the high coefficient of membrane distribution, lercanidipine, despite a relatively short half-life from blood plasma, has a prolonged antihypertensive effect.
Due to its high vascular selectivity, lercanidipine has no negative inotropic effect. When it is taken, vasodilation develops gradually, due to which only in rare cases there is acute arterial hypotension with reflex tachycardia.
Lercanidipine is a racemic mixture of the (+) R- and (-) S- enantiomers. Its antihypertensive effect is primarily due to the S-enantiomer.
Pharmacokinetics
The main pharmacokinetic characteristics of lercanidipine:
- absorption: completely absorbed after oral administration; With max (maximum concentration in blood plasma) is achieved after 1.5-3 hours and is 3.3 ± 2.09 or 7.66 ± 5.90 ng per 1 ml after taking 10 or 20 mg of lercanidipine, respectively; (+) - R- and (-) S- enantiomers of lercanidipine have a similar pharmacokinetic profile - the same TC max (time to reach maximum concentration), T½ (half-life); values C maxand AUC (area under the curve - concentration-time) is 1.2 times higher for the (-) - S enantiomer; no interconversion of enantiomers was observed in in vivo experiments; the absolute bioavailability of lercanidipine when taken orally after meals during the initial passage through the liver is approximately 10%, when taken on an empty stomach, the bioavailability value becomes 1/3 less; when taken no later than 2 hours after a fatty meal, it increases by 4 times (in this connection, it should not be taken after a meal); when taken orally, its concentration in blood plasma is not directly proportional to the dose taken (nonlinear kinetics); its bioavailability increases with increasing dose, due to the gradual saturation of the first pass metabolism; the average value of T½ varies from 8 to 10 hours; the duration of the therapeutic effect is 24 hours;upon repeated administration, its cumulation is not observed; its concentration in blood plasma in renal failure (creatinine clearance of 30 ml per minute) and in patients on hemodialysis are higher (approximately 70%); since lercanidipine is mainly metabolized in the liver, in moderate to severe hepatic failure, its systemic bioavailability is likely to increase;
- distribution: from blood plasma, its distribution to organs and tissues occurs extensively and quickly; the connection with blood plasma proteins is> 98%; in severe hepatic and / or renal failure, due to a decrease in the concentration of protein in the blood plasma, its free fraction may increase;
- metabolism: metabolized with the participation of the CYP3A4 isoenzyme with the formation of inactive metabolites;
- excretion: about ½ of the dose taken is excreted through the kidneys, the rest - through the intestines; elimination occurs mainly by biotransformation.
Indications for use
According to the instructions, Lerkamen 10 is prescribed for patients with essential hypertension of I and II severity.
Contraindications
Absolute:
- severe renal failure;
- severe liver failure;
- obstruction of blood vessels emanating from the left ventricle of the heart;
- period after myocardial infarction (1 month);
- unstable angina;
- untreated heart failure;
- syndrome of glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
- use in women of childbearing age who do not use reliable methods of contraception;
- simultaneous reception with grapefruit juice;
- combined therapy with cyclosporine, CYP3A4 inhibitors (troleandomycin, ritonavir, erythromycin, itraconazole, ketoconazole);
- age under 18;
- pregnancy;
- lactation period;
- individual intolerance to the components of the drug, other derivatives of the dihydropyridine series.
Relative (diseases / conditions in the presence of which the appointment of Lerkamen 10 requires caution):
- dysfunction of the left ventricle of the heart;
- cardiac ischemia;
- sick sinus syndrome (without a pacemaker);
- mild to moderate liver failure;
- renal failure (creatinine clearance> 30 ml for 1 min);
- simultaneous treatment with other CYP3A4 substrates (astemizole, terfenadine, class III antiarrhythmic drugs, for example, quinidine, amiodarone), CYP3A4 inducers (rifampicin, anticonvulsants, for example, phenytoin, carbamazepine);
- elderly age.
Instructions for the use of Lerkamen 10: method and dosage
Tablets Lerkamen 10 are taken orally, without chewing, drinking water (sufficient amount), 1 pc. per day, preferably in the morning, at least 15 minutes before meals.
The therapeutic dose is selected gradually, since the maximum antihypertensive effect of the drug develops approximately after 14 days from the start of treatment. It is unlikely that increasing the dose to 2 tablets per day will increase the effectiveness of the drug, but may increase the risk of side effects. But with good tolerance of the drug, it is possible to increase the daily dose by 2 times.
The initial dose of Lerkamen 10 in cases of renal or hepatic insufficiency of mild or moderate severity is 1 pc. per day, then it is carefully increased to 2 pcs. in a day. In patients with mild or moderate hepatic impairment, there is a possibility of an increase in the antihypertensive effect and a dose adjustment (reduction) may be required.
Side effects
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):
- nervous system: infrequently - dizziness, headache; rarely - drowsiness;
- cardiovascular system: infrequently - rush of blood to the skin of the face, tachycardia, palpitations; rarely - chest pain, angina pectoris; very rarely - fainting, with angina pectoris, the frequency, duration and severity of attacks may increase;
- gastrointestinal tract: rarely - vomiting, pain in the epigastric region, diarrhea, dyspepsia, nausea;
- skin and subcutaneous tissue: rarely - skin rash;
- musculoskeletal and connective tissue: rarely - myalgia;
- kidneys and urinary tract: rarely - polyuria;
- general disorders: infrequently - peripheral edema; rarely - increased fatigue, asthenia;
- immune system: very rarely - hypersensitivity reactions;
- side effects observed in very rare cases: chest pain, pollakiuria (increased frequency of urination), a marked decrease in blood pressure, a reversible increase in the activity of hepatic transaminases, gingival hyperplasia, myocardial infarction.
Overdose
The main symptoms: presumably - peripheral vasodilation with reflex tachycardia and a pronounced decrease in blood pressure (as with an overdose of other dihydropyridine derivatives).
Therapy: symptomatic treatment. In case of loss of consciousness, a pronounced decrease in blood pressure, cardiovascular therapy is performed, with bradycardia, atropine is administered intravenously.
Symptoms and measures used to treat the condition and drugs in special cases (according to the available data of medical observations about 3 episodes of overdose when taking lercanidipine for suicide in doses of 0.15; 0.28 and 0.8 g):
- lercanidipine - 0.15 g in combination with alcohol intake (in an unknown amount): drowsiness was observed; for the purpose of therapy, gastric lavage was carried out, and the intake of activated carbon;
- lercanidipine - 0.28 g in combination with moxonidine - 0.005 6 g: there was mild renal failure, severe myocardial ischemia, cardiogenic shock; for the purpose of therapy, diuretics (furosemide), cardiac glycosides, catecholamines in high doses, plasma substitutes were taken;
- lercanidipine - 0.8 g: there was nausea, a marked decrease in blood pressure; for the purpose of therapy, laxatives and activated carbon were taken, intravenous dopamine was administered.
special instructions
Before using Lerkamen 10, you should consult your doctor.
Influence on the ability to drive vehicles and complex mechanisms
Due to the fact that taking Lerkamen 10 may be accompanied by the development of increased fatigue, asthenia, dizziness, and, in rare cases, drowsiness, patients during the period of therapy should drive vehicles with extreme caution and engage in potentially hazardous activities.
Application during pregnancy and lactation
Lerkamen 10 is contraindicated for use during pregnancy and during breastfeeding, since there is no clinical experience with the use of the drug in such cases.
Pediatric use
The safety and efficacy of using the drug in children under the age of 18 has not been studied, and therefore Lerkamen 10 tablets are contraindicated in patients of this age group.
With impaired renal function
The drug is used with caution in patients with mild to moderate renal failure.
For violations of liver function
Lerkamen 10 is used with caution in mild to moderate hepatic insufficiency.
Use in the elderly
The drug at the beginning of therapy is used with caution in elderly patients.
Drug interactions
The effect of drugs / substances on Lerkamen 10 with combined treatment:
- metoprolol, other β-blockers: reduce its bioavailability by 50%;
- inhibitors and inducers of the CYP3A4 isoenzyme: can affect metabolic processes and the excretion of lercanidipine, since it is metabolized by this isoenzyme;
- cyclosporine: increases its concentration in blood plasma;
- midazolam: reduces the bioavailability of lercanidipine in elderly patients by almost 40% (when taking the drug at a dose of 0.02 g);
- cimetidine (in high doses): may increase the bioavailability and antihypertensive effect of Lerkamen 10;
- ethanol, grapefruit juice: may potentiate its antihypertensive effect.
Influence of Lerkamen 10 on drugs / substances in combination with:
- cyclosporine: its concentration in blood plasma increases;
- digoxin: its Cmax increases by an average of 33% (when taking 0.02 g of lercanidipine on an empty stomach);
- simvastatin (at a dose of 0.04 g): its AUC increases by 56% (when taking 0.02 g of lercanidipine on an empty stomach).
Lerkamen 10 can be used simultaneously with angiotensin-converting enzyme inhibitors, diuretics, β-blockers.
Analogs
Analogues of Lerkamen 10 are: Lernikor, Lerkanorm, Zanidip-Recordati, etc.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 30 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lerkamen 10
According to reviews, Lerkamen 10, subject to regular use in patients with grade I arterial hypertension, is effective for stabilizing pressure and is well tolerated.
Price for Lerkamen 10 in pharmacies
The approximate price of Lerkamena 10 for a pack of 28 tablets. - 303 rubles; for 60 pcs. in the package - 484 rubles.
Lerkamen 10: prices in online pharmacies
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Drug name Price Pharmacy |
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Lerkamen 10 tablets p.p. 28 pcs. 303 RUB Buy |
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Lerkamen 10 10 mg film-coated tablets 28 pcs. 303 RUB Buy |
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Lerkamen 10 10 mg film-coated tablets 60 pcs. RUB 550 Buy |
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Lerkamen 10 tablets p.p. 60 pcs. 659 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!
