To effectively lower blood pressure, the drug “Lerkamen” is used. This is an effective remedy that is recommended by more than 70% of buyers. It is produced in the form of tablets, which can be purchased with a prescription. The standard course of treatment takes 14 days, after which a second appointment is possible in consultation with the doctor.
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.
Lerkamen 20, 28 pcs., 20 mg, film-coated tablets
Lercanidipine can be used simultaneously with β-blockers, diuretics, angiotensin-converting enzyme inhibitors (ACE inhibitors). When used simultaneously with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect may also occur when used concomitantly with other β-blockers, so dose adjustment of lercanidipine may be required to achieve a therapeutic effect with this combination. Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme, therefore inhibitors and inducers of this isoenzyme, when used simultaneously, can affect the metabolism and excretion of lercanidipine. Concomitant use of lercanidipine with CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is not recommended (see section "Contraindications").
The simultaneous use of cyclosporine and lercanidipine is not recommended, as an increase in the concentration of both substances in the blood plasma is observed (see section “Contraindications”).
Caution should be exercised when lercanidipine is used simultaneously with other CYP3 A4 substrates (terfenadine, astemizole, class III antiarrhythmic drugs, for example, amiodarone, quinidine).
When lercanidipine 20 mg is coadministered with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40 mg. %.
Lercanidipine should be administered with caution concomitantly with inducers of CYP3A4, such as anticonvulsants (phenytoin, carbamazepine) and rifampicin, as the antihypertensive effect of the drug may be reduced. Regular blood pressure monitoring is necessary.
With simultaneous use of lercanidipine at a dose of 20 mg in patients chronically taking betamethyldigoxin, no pharmacokinetic interaction was noted, while in healthy volunteers treated with digoxin, an increase in the Cmax value (maximum plasma concentration) for digoxin was observed by an average of 33 % after taking 20 mg of lercanidipine on an empty stomach, while AUC (area under the concentration-time curve) and renal clearance changed slightly. Patients receiving digoxin and lercanidipine concomitantly should be monitored for signs of digoxin toxicity. The simultaneous use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in the concentration of lercanidipine in the blood plasma. At high doses of cimetidine, the bioavailability and antihypertensive effect of lercanidipine may be increased.
With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), the AUC value for simvastatin increased by 56%,
and the same value for its active metabolite - P-hydroxy acid - by 28
%.
By taking medications at different times of the day (lercanidipine in the morning, simvaetatin in the evening), unwanted interactions can be avoided.
With simultaneous use of 20 mg of lercanidipine and warfarin in healthy volunteers, no changes in the pharmacokinetics of warfarin were observed. Concomitant use with fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients did not have clinically significant changes in the pharmacokinetics of lercanidipine.
It is possible that the antihypertensive effect may be enhanced when grapefruit juice and lercanidipine are taken concomitantly (see section "Contraindications"
»).
Ethanol may potentiate the antihypertensive effect of lercanidipine.
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.
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.
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)
Lercanidipine can be used simultaneously with beta-blockers, diuretics, and ACE inhibitors.
When used simultaneously with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect may also occur when used concomitantly with other beta-blockers, so dose adjustment of lercanidipine may be required to achieve a therapeutic effect with this combination.
Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme, therefore inhibitors and inducers of this isoenzyme, when used simultaneously, can affect the metabolism and excretion of lercanidipine. Concomitant use of lercanidipine with CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir, erythromycin, troleandomycin) is not recommended.
The simultaneous use of cyclosporine and lercanidipine is not recommended, because There is an increase in the concentration of both substances in the blood plasma.
Caution should be exercised when lercanidipine is used concomitantly with other CYP3A4 substrates (terfenadine, astemizole, class III antiarrhythmic drugs, e.g. amiodarone, quinidine).
When lercanidipine 20 mg is coadministered with midazolam, the bioavailability of lercanidipine in elderly patients may increase by approximately 40%.
Lercanidipine should be administered with caution concomitantly with inducers of CYP3A4, such as anticonvulsants (phenytoin, carbamazepine) and rifampicin, as the antihypertensive effect of the drug may be reduced. Regular blood pressure monitoring is necessary.
When lercanidipine was co-administered at a dose of 20 mg in patients chronically taking beta-methyldigoxin, no pharmacokinetic interaction was observed, while healthy volunteers treated with digoxin experienced an average 33% increase in digoxin Cmax after dosing of 20 mg. lercanidipine in the fasted state, with AUC and renal clearance changing slightly. Patients receiving digoxin and lercanidipine concomitantly should be monitored for signs of digoxin toxicity.
The simultaneous use of lercanidipine with cimetidine (up to 800 mg) does not cause significant changes in the concentration of lercanidipine in the blood plasma. At high doses of cimetidine, the bioavailability and antihypertensive effect of lercanidipine may be increased.
With simultaneous use of lercanidipine (20 mg) and simvastatin (40 mg), the AUC value for simvastatin increased by 56%, and the same value for its active metabolite - β-hydroxy acid - by 28%.
By taking drugs at different times of the day (lercanidipine in the morning, simvastatin in the evening) you can avoid unwanted interactions.
With simultaneous use of lercanidipine at a dose of 20 mg and warfarin in healthy volunteers, no changes in the pharmacokinetics of warfarin were observed.
Concomitant use with fluoxetine (an inhibitor of CYP2D6 and CYP3A4) in elderly patients did not have clinically significant changes in the pharmacokinetics of lercanidipine.
The antihypertensive effect may be enhanced by simultaneous administration of grapefruit juice and lercanidipine.
Ethanol may potentiate the antihypertensive effect of lercanidipine.
Lerkamen 20 tablets p/o film 20mg 60 pcs
Pharmacological group:
Selective calcium channel blockers with a predominant effect on blood vessels.
Pharmacodynamics:
Lercanidipine is a selective blocker of “slow” calcium channels, a dihydropyridine derivative that inhibits the transmembrane flow of calcium ions into vascular smooth muscle cells. The mechanism of hypotensive action is due to a direct relaxing effect on vascular smooth muscle cells, resulting in a decrease in total peripheral vascular resistance. Despite the relatively short plasma half-life, lercanidipine has a prolonged effect due to its high membrane distribution coefficient. Due to its high vascular selectivity, it does not have a negative inotropic effect. Acute arterial hypotension with reflex tachycardia occurs rarely due to the gradual development of vasodilation when taking lercanidipine. Lercanidipine is a racemic mixture of (+)-R- and (-)S- enantiomers. The antihypertensive effect of lercanidipine is primarily due to the S-enantiomer.
Pharmacokinetics:
Lercanidipine is completely absorbed after oral administration. The maximum plasma concentration (Cmax) is reached within 1.5-3 hours and is 3.3 ± 2.09 ng/ml and 7.66 ± 5.90 ng/ml after taking 10 and 20 mg of lercanidipine, respectively.
(+)-R- and (-)S- enantiomers of lercanidipine demonstrate a similar pharmacokinetic profile: they have the same time to reach maximum concentration (TCmax), the same half-life (T 1/2); Cmax values and area under the concentration-time curve (AUC) are 1.2 times higher for the (-)-S enantiomer.
Interconversion of enantiomers was not observed in in vitro experiments. During the “primary passage” through the liver, the absolute bioavailability of lercanidipine when taken orally after meals is approximately 10%; when taken on an empty stomach, the bioavailability value decreases by 1/3. When taking lercanidipine no later than 2 hours after eating a fatty meal, its bioavailability increases 4 times, so Lerkamen® 20 should not be taken after meals. When lercanidipine is administered orally, its plasma concentration is not directly proportional to the dose taken (nonlinear kinetics). Saturation of presystemic metabolism occurs gradually. Thus, bioavailability increases with increasing dose. Distribution from blood plasma to tissues and organs occurs quickly and extensively. Communication with blood plasma proteins exceeds 98%. In patients with severe renal and/or hepatic impairment, due to a decrease in plasma protein concentrations, the free fraction of lercanidipine may increase. Lercanidipine is metabolized with the participation of the CYP3A4 isoenzyme to form inactive metabolites. About 50% of the dose taken is excreted by the kidneys (about 50% is excreted by the intestines). Elimination occurs mainly through biotransformation.
The average value of T 1/2 is 8-10 hours. The duration of therapeutic action is 24 hours. There is no accumulation of lercanidipine upon repeated oral administration. The pharmacokinetics of lercanidipine in elderly patients, patients with renal impairment (creatinine clearance (CR) greater than 30 ml/min) and patients with mild to moderate hepatic impairment have been shown to be similar to the pharmacokinetics observed in the general patient population. In patients with renal insufficiency (creatinine clearance less than 30 ml/min) and in patients on hemodialysis, plasma concentrations of lercanidipine were higher (approximately 70%). In patients with moderate to severe hepatic impairment, the systemic bioavailability of lercanidipine is likely to be increased since lercanidipine is metabolized primarily in the liver.
