Contraindications
- Hypersensitivity to the active substance or to any excipient of the drug.
- Obstruction of the vessels leaving the left ventricle.
- Untreated congestive heart failure.
- Unstable angina or recent (within 1 month) myocardial infarction.
- Severe liver dysfunction.
- Severe renal impairment (GFR <30 ml/min), including in patients on dialysis.
- Concomitant use with: strong CYP3A4 inhibitors, cyclosporine, grapefruit or grapefruit juice.
Indications and contraindications
The main indication for the use of tablets is high blood pressure (hypertension) of mild to moderate severity.
In some cases, taking the drug is excluded:
- obstruction of a blood vessel adjacent to the left ventricle of the heart;
- pregnancy period;
- breastfeeding period;
- acute conditions due to myocardial infarction;
- age up to 17 years inclusive;
- insufficient production of the lactase enzyme;
- individual intolerance to the active or auxiliary substances;
- insufficiency of heart function;
- unstable angina;
- weakness of the sinus node (if the patient does not have a pacemaker).
When taking the drug, a number of side effects may occur:
- migraine;
- dizziness;
- sleep problems;
- digestive disorders;
- vomiting, nausea;
- problems with stool;
- rapid pulse;
- pain in the chest area;
- exacerbation of angina attacks;
- decrease in pressure.
In case of overdose, myocardial ischemia, drowsiness, a strong decrease in blood pressure, and the onset of cardiogenic shock are possible. In these cases, it is necessary to induce vomiting, rinse the stomach, and take a laxative. As a rule, treatment in a hospital setting is required. However, hemodialysis does not give any special results.
Mode of application
Safety measures to be observed when taking or handling the medicine:
- The medicine should be taken preferably in the morning, at least 15 minutes before breakfast.
- This medication should not be taken with grapefruit juice.
The recommended dose is 10 mg orally once a day at least 15 minutes before meals, the dose can be increased to 20 mg depending on the individual sensitivity of the patient. The dose selection should be gradual, since the maximum antihypertensive effect may occur 2 weeks after the start of treatment.
Lerkamen® 20 (Lerkamen® 20)
Concomitant use is contraindicated
CYP3A4 inhibitors
It is known that lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme. Therefore, inhibitors of this isoenzyme, when used simultaneously, may affect the metabolism and excretion of lercanidipine.
Concomitant use with the CYP3A4 inhibitor ketoconazole has been shown to increase plasma concentrations of lercanidipine (15-fold increase in AUC and 8-fold increase in Cmax for the S-enantiomer of lercanidipine).
Concomitant use of lercanidipine with CYP3A4 inhibitors (for example, ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin, clarithromycin) is contraindicated.
Cyclosporine
After simultaneous use, increased plasma concentrations of both lercanidipine were observed. and cyclosporine. A study in young healthy volunteers showed that when cyclosporine was administered 3 hours after lercanidipine dosing, plasma levels of lercanidipine were unchanged, while the AUC of cyclosporine increased by 27%. However, simultaneous administration of lercanidipine with cyclosporine caused a 3-fold increase in the concentration of lercanidipine in the blood plasma and an increase in the AUC of cyclosporine by 21%.
Cyclosporine and lercanidipine should not be used simultaneously (see section "Contraindications").
Grapefruit juice
Lercanidipine should not be taken at the same time as grapefruit or grapefruit juice. simultaneous use may lead to an increase in the systemic bioavailability of the drug and enhanced antihypertensive effect (see section “Contraindications”).
Concomitant use is not recommended
CYP3A4 inducers
Lercanidipine should be used with caution concomitantly with inducers of CYP3A4, such as anticonvulsants (phenytoin, phenobarbital, carbamazepine) and rifampicin, since the antihypertensive effect of the drug may be reduced. If co-administration is necessary, more frequent than usual blood pressure monitoring is required (see section "Precautions").
Ethanol (alcohol)
Ethanol may potentiate the antihypertensive effect of lercanidipine. When taking vasodilating antihypertensive drugs, alcohol should be avoided as it may enhance their effect (see section "Precautions").
Concomitant use requires caution (including dose adjustment)
CYP3A4 substrates
Caution should be exercised when lercanidipine is used concomitantly with other CYP3A4 substrates, such as terfenadine, astemizole, quinidine, class III antiarrhythmic drugs (amiodarone, sotalol) (see section "Caution").
Midazolam
When simultaneous oral administration of lercanidipine at a dose of 20 mg with midazolam (CYP3A4 substrate) in healthy elderly volunteers, the absorption of lercanidipine increases (by approximately 40%) and the rate of absorption slows down (increase in TCmax from 1.75 hours to 3 hours). The concentration of midazolam in the blood did not change.
Metoprolol
When lercanidipine was co-administered with metoprolol (a beta blocker that is primarily metabolized in the liver [CYP2D6 substrate]), the bioavailability of metoprolol was not affected, whereas the bioavailability of lercanidipine was reduced by 50%. This effect may be due to a reduction in hepatic blood flow caused by beta-blockers and may occur when lercanidipine is used concomitantly with other drugs of this class. Therefore, lercanidipine can be safely used in combination with beta-blockers, but this combination may require dose adjustment of lercanidipine to achieve a therapeutic effect.
Digoxin
With simultaneous use of lercanidipine at a dose of 20 mg in patients chronically taking beta-methyldigoxin, no pharmacokinetic interaction was noted, while in healthy volunteers treated with digoxin, there was an increase in Cmax (maximum plasma concentration) for digoxin by an average of 33% after administration of 20 mg lercanidipine on an empty stomach, with little change in AUC and renal clearance. Patients taking digoxin and lercanidipine concomitantly should be monitored for signs of digitalis toxicity.
Other drug interactions
Fluoxetine
In a study, simultaneous use of lercanidipine with fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly volunteers (mean age 65 ± 7 years) did not lead to clinically significant changes in the pharmacokinetics of lercanidipine.
Cimetidine
The simultaneous use of lercanidipine with cimetidine (at a dose of 800 mg per day) did not cause significant changes in the concentration of lercanidipine in the blood plasma (increase in Cmax and AUC by an average of 11%). But at higher doses of cimegidine, caution must be exercised as the bioavailability and antihypertensive effect of lercanidipine may increase.
Simvastatin
With repeated co-administration of lercanidipine 20 mg and simvastatin 40 mg, the AUC of lercanidipine did not change significantly, while the AUC of simvastatin increased by 56% and the AUC of its active metabolite (β-hydroxy acid) by 28%. . It is unlikely that such changes are clinically significant. When taking drugs at different times of the day (lercanidipine in the morning, simvastatin in the evening), unwanted interactions are not expected.
Warfarin
With simultaneous use of 20 mg of lercanidipine and warfarin in healthy volunteers, no changes in the pharmacokinetics of warfarin were observed.
Diuretics and ACE inhibitors
Lercanidipine can be used simultaneously with diuretics and ACE inhibitors.
Other drugs that affect blood pressure
An increase in the antihypertensive effect can be observed when lercanidipine is taken simultaneously with alpha-blockers, tricyclic antidepressants, and antipsychotics.
On the contrary, a decrease in the antihypertensive effect may be observed when used simultaneously with glucocorticosteroids.
Overdose
As with other dihydropyridines, overdose with lercanidipine results in excessive peripheral vasodilation with severe hypotension and reflex tachycardia. However, when the drug is used in very high doses, loss of peripheral selectivity is possible, which causes bradycardia and a negative inotropic effect. The most common adverse reactions caused by overdose were hypotension, dizziness, headache and palpitations.
Treatment. Patients with clinically significant hypotension require active cardiovascular support, including frequent monitoring of cardiac and respiratory function, horizontal positioning with lower extremities elevated, control of circulating fluid volume and diuresis
Drug interactions and special instructions
The effect of "Lekarmen" is enhanced in case of simultaneous use of the drug "Midazolam". Use Cimetidine with caution, especially if you need to take high doses. During treatment, alcoholic beverages and grapefruit juice are strictly excluded. If the drug is combined with Simvastatin or Lercanidipine, it is necessary to space the intake at least 10 hours apart.
The drug may weaken psychomotor function. Therefore, drivers of vehicles, operators of machine tools and other moving mechanisms should take Lerkamen tablets with caution.
Note!
Description of the drug Lerkamen 20 tablets. p/o 20 mg No. 60 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Instructions for use "Lerkamen"
The product is taken orally without chewing or dissolving. The tablets are washed down with water, and it is important to prevent damage to the shell. It is best to take it on an empty stomach, and after 20-30 minutes you can eat.
Standard daily dosage is 1 tablet. If the therapeutic effect is insignificant, the amount is increased to 2 tablets so that the daily dose does not exceed 20 mg. The standard course of treatment is 14 days.
The decision on the frequency of doses, duration of therapy and other rules of admission is made by the doctor. If treatment is ineffective, it is possible to replace the drug with another drug.
Lerkamen 20
Lerkamen 20 (active ingredient – lercanidipine) is a calcium antagonist of the dihydropyridine series. Inhibits the flow of calcium ions through the membranes of smooth muscle cells. It has a direct relaxing effect on the smooth muscles of blood vessels, resulting in a decrease in the overall resistance of the circulatory system to blood flow. Having a relatively short half-life, Lerkamen has a long-lasting hypotensive effect. Due to its high selectivity of action on blood vessels, it does not reduce the force of heart contractions (negative inotropic component). Due to the gradual onset of the antihypertensive effect, acute hypotension with a reflex increase in heart rate rarely develops. The duration of the antihypertensive effect of the drug is 24 hours. Lerkamen 20 is completely absorbed in the gastrointestinal tract. It undergoes metabolic transformations before entering the systemic circulation when passing through the liver. When taken on an empty stomach, the bioavailability of the drug is reduced by a third; when taken within 2 hours after a meal, provided there is a high proportion of fat in the diet, the bioavailability increases fourfold. Elimination of the drug is carried out equally through urine and feces. The half-life averages 8-10 hours. When taken repeatedly, it does not accumulate in the body. The indication for use of Lerkamen 20 is primary arterial hypertension of I-II degrees. The optimal time to take it is in the morning, no later than 15 minutes before meals. A single dose at the initial stage of treatment is 10 mg (1/2 tablet), with the possibility of further increasing according to indications depending on individual tolerance to 20 mg, the frequency of administration is 1 time per day. Dose selection is carried out gradually, because The peak of the antihypertensive effect is observed, as a rule, no earlier than 2 weeks after the start of pharmacotherapy. Increasing the dose beyond 20 mg per day is not advisable. For elderly patients, the drug is prescribed on a general basis; no dose adjustment is required, but it is recommended to organize medical supervision of the patient at the initial stage of treatment.
Persons with mild to moderate hepatic or renal impairment should take the drug with extreme caution. The drug has a favorable safety profile and, if the instructions for use are followed, is well tolerated by patients. The most likely unwanted side effects associated with taking Lerkamen 20 are: cephalalgia, dizziness, rapid heartbeat, flushing of the facial skin. The drug is not prescribed for severe forms of cardiac, renal and liver failure, unstable angina, significant reduction in the lumen of vessels extending from the left ventricle, in the post-infarction period, during pregnancy and lactation, fertile women who neglect contraception, individual intolerance to lercanidipine and other dihydropyridine derivatives. The drug is not used in pediatric practice. Considering that one of the undesirable side effects of the drug is dizziness, during the course of medication, special care should be taken when engaging in potentially hazardous activities, including driving. Lerkamen can be taken as part of combination pharmacotherapy together with beta-adrenergic receptor blockers, diuretics, angiotensin-converting enzyme inhibitors. Metoprolol reduces the bioavailability of Lerkamen by half. This effect can also be observed when taking the drug together with other beta-adrenergic receptor blockers, which may require increasing the dose of Lerkamen. Grapefruit juice may potentiate the antihypertensive effect of the drug. Ethanol and ethanol-containing products can also enhance the hypotensive effect of Lerkamen. The drug is incompatible with cyclosporine, because their combined use leads to an increase in the concentration of both drugs in the blood.
Lerkamen
- impaired outflow from the left ventricle, including aortic valve stenosis; — chronic heart failure in the stage of decompensation; - hereditary and/or idiopathic angioedema (including a history); - angioedema when using ACE inhibitors (history); - unstable angina; - the first month after myocardial infarction (within 28 days); - severe renal failure (CC - 30 ml/min), including patients on hemodialysis; - - severe liver failure; - simultaneous use with powerful inhibitors of the CYP3A4 isoenzyme (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin), cyclosporine, grapefruit juice; - lactase deficiency, lactose intolerance, glucose/galactose malabsorption syndrome; - children and adolescents up to 18 years of age; - hypersensitivity to lercanidipine, enalapril or any other ACE inhibitor and other BMCCs, dihydropyridine derivatives, as well as to any other component of the drug. With caution - sick sinus syndrome (without simultaneous use of an artificial heart pacemaker); — dysfunction of the left ventricle and coronary artery disease; — renal failure (creatinine clearance more than 30 ml/min); - renovascular hypertension; — condition after kidney transplantation (experience is limited); - liver failure; - inhibition of bone marrow hematopoiesis; - severe autoimmune connective tissue diseases (including scleroderma, systemic lupus erythematosus); - simultaneous use with immunosuppressants, allopurinol, procainamide; - diabetes; — surgical interventions and general anesthesia; - patients on a diet with limited salt intake; - hyperkalemia; — conditions accompanied by a decrease in blood volume, incl. diarrhea, vomiting, primary aldosteronism. Use during pregnancy and breastfeeding The use of the drug Koripren® is not recommended for use during pregnancy. ACE inhibitors can cause disease or death of the fetus or newborn when prescribed in the second and third trimesters of pregnancy. The use of ACE inhibitors during this period was associated with adverse effects on the fetus and newborn, including the development of arterial hypotension, renal failure, hyperkalemia and/or hypoplasia of the skull in the newborn. Oligohydramnios may develop, apparently due to decreased fetal renal function. This complication can lead to contracture of the limbs, deformation of the bones of the skull, including its facial part, and hypoplasia of the lungs. A teratogenic effect when using ACE inhibitors (enalapril) in the first trimester has not been proven, but this possibility should not be excluded. Patients on therapy with ACE inhibitors when planning pregnancy should switch to alternative antihypertensive treatment regimens. The use of the drug in women of childbearing age who do not use reliable contraception is not recommended. The use of the drug during breastfeeding is not recommended, because enalapril and its main metabolite, enalaprilat, pass into breast milk.
