Lerkamen tablets: instructions for use, price, reviews, analogues

pharmachologic effect

The tablets have a pronounced hypotensive effect. The mechanism of action is based on selective blocking of calcium receptors. Lercanidipine is able to slow down the flow of calcium ions in smooth muscle tissue and cardiomyocytes.

Lerkamen reduces total peripheral vascular resistance and gradually expands the lumen of blood vessels, preventing the development of reflex tachycardia and collapse . The medication does not have a negative inotropic effect.

Pharmacodynamics and pharmacokinetics

The medicine Lerkamen is well absorbed from the digestive system. The maximum plasma concentration is recorded after 1.5-3 hours. Up to 98% of the active substance binds to plasma proteins.

The bioavailability of the drug increases after eating, which is why it is recommended to take the tablets on an empty stomach. As the dose increases, bioavailability increases. Initially, the drug is metabolized in the hepatic system, which explains the low absolute bioavailability of 10%.

The hypotensive effect is observed throughout the day. The active component is excreted through the renal system; the half-life is 10 hours.

Lerkamen 10 tablets p/o film 10mg 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 derivative of the dihydropyridine series, 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® 10 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.

Contraindications

heart failure;
obstruction of the vessels leaving the left ventricle;
individual hypersensitivity to lercanidipine ;
lactase deficiency;
pregnancy;
unstable form of angina ;
acute myocardial infarction ;
sick sinus syndrome (in patients without a pacemaker);
lactation;
age limit – 18 years.

Side effects

Nervous system:

migraine;
dizziness;
sleep and wakefulness disorders.

Digestive tract:

stool disorders;
gastralgia;
dyspepsia (vomiting, nausea);
increased ALT, AST;
disruption of food digestion.

The cardiovascular system:

discomfort behind the sternum;
increased heart rate;
increase in angina ;
drop in blood pressure;
chest pain.

Allergic responses, frequent urination , development of polyuria , swelling, hyperemia , gum hyperplasia , and muscle pain are also possible.

Instructions for use of Lerkamen (Method and dosage)

The tablets are intended for oral administration. It is not allowed to crush the drug or damage the protective shell. The effectiveness of the drug increases when lercanidipine is taken on an empty stomach. The duration of therapy is determined by the doctor.

1 tablet of 10 mg is taken 1 time every 24 hours. If there is insufficient reduction in blood pressure, after 14 days you can switch to a single dose of 20 mg.

Take the tablets with water on an empty stomach. When the dose of the drug is increased (more than 20 mg per day), an increase in the hypotensive effect is not observed, but an increase in the frequency and severity of undesirable side reactions is recorded.

If the medication is ineffective in the treatment of arterial hypertension, it is recommended to prescribe additional antihypertensive drugs from other pharmacological groups.

Lerkamen® 10 (Lerkamen® 10)

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

Increased plasma concentrations of both lercanidipine and cyclosporine were observed after concomitant use. 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 my blood changed.

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 cimetidine, 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 the drug at different times of the day (lercanidipine in the morning, simvastatin in the evening), no unwanted interaction is 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

There is a drop in blood pressure, drowsiness , ischemic changes in myocardial tissue, nausea, and the development of cardiogenic shock . Induction of vomiting, administration of laxatives and enterosorbents are recommended.

In case of severe intoxication, Dopamine , catecholamines , and diuretics are prescribed. It is possible to administer Atropine bradycardia develops , a drop in blood pressure and loss of consciousness. Treatment is carried out in a hospital. Hemodialysis has not proven effective.

Lerkamen® 20 (Lerkamen® 20)

Concomitant use is contraindicated

CYP3A4 inhibitors

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

Concomitant use is not recommended

CYP3A4 inducers

Ethanol (alcohol)

Concomitant use requires caution (including dose adjustment)

CYP3A4 substrates

Midazolam

Metoprolol

Digoxin

Other drug interactions

Fluoxetine

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.

Interaction

Absorption of the drug is enhanced during treatment with midazolam . Inducers of CYP3A4, ethanol, Cyclosporine and grapefruit juice are strictly contraindicated when taking Lerkamen.

Caution is required when taking high doses of cimetidine (more than 800 mg).

The bioavailability of the active substance increases simultaneously with an increase in the negative inotropic effect during therapy with beta-blockers.

A mandatory dose adjustment of Digoxin after starting lercanidipine therapy.

To reduce the risk of negative interactions, it is necessary to maintain a 10-hour window when taking Simvastatin and lercanidipine.

Lerkamen 10, 28 pcs., 10 mg, film-coated tablets

Lercanidipine can be used simultaneously with β-blockers, diuretics, angiotensin-converting enzyme inhibitors (ACEIs).

When used simultaneously with metoprolol, the bioavailability of lercanidipine is reduced by 50%. This effect may also occur when used simultaneously 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, may affect 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 there is an increase in the concentration of both substances in the blood plasma (see section " Contraindications"

»).

Caution should be exercised when lercanidipine is used concomitantly with other CYP3A4 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%.

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 in healthy volunteers treated with digoxin, an increase in digoxin Cmax (maximum plasma concentration) was observed on average by 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 - β-hydroxy acid - by 28%. By taking medications at different times of the day (lercanidipine in the morning, simvastatin 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 to enhance the antihypertensive effect when taking grapefruit juice and lercanidipine simultaneously (see section " Contraindications"

»).

Ethanol may potentiate the antihypertensive effect of lercanidipine.

Impact on the ability to drive vehicles and operate machinery

Since dizziness, asthenia, increased fatigue and, in rare cases, drowsiness may occur during therapy with Lerkamen® 10, during the period of drug use, patients should be especially careful when driving vehicles and engaging in other potentially hazardous activities that require a high speed of psychomotor reactions.

Analogues of Lerkamen

Level 4 ATC code matches:
Lacipil

Cordafen

Azomex

Nimodipine

Felodipin

Nifedipine

Farmadipin

Amlotop

Nimotop

Tenox

Nifecard HL

Cordipin

Felodip

Normodipine

Phenigidine

Norvask

Cordaflex

Corinfar

Vero-Amlodipine

Amlodipine

Analogues of Lerkamen, produced and prescribed in Russia and other countries:

Zanidip-Recordati
Lercanorm
Lernikor
Lerkaton
Lervask
Zanikor

Reviews of analogues are positive and indicate the high effectiveness of the drugs in the treatment of hypertension.

Reviews about Lerkamen

Thematic portals and medical forums, where patients share their impressions of taking medications, contain only positive reviews.

The drug is well tolerated and stabilizes blood pressure after 2 weeks of regular use in patients with stage 1 arterial hypertension.

The incidence of adverse reactions is low; the drug is considered highly effective in the treatment of grade 2.3 hypertension in combination with other antihypertensive drugs.

Lerkamen® Duo

Patients who require special attention when treating arterial hypertension:

- with severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

- with decompensated heart failure.

The drug Lerkamen® Duo should not be used to relieve a hypertensive crisis.

Aortic stenosis/mitral stenosis/hypertrophic obstructive cardiomyopathy

Like all drugs that have a vasodilating effect, ACE inhibitors and BMCCs should be used with caution in patients with left ventricular outflow tract obstruction.

Lerkamen® Duo should be used with extreme caution in patients with aortic stenosis, mitral stenosis or hypertrophic obstructive cardiomyopathy. In patients with hemodynamically significant obstruction of the left ventricular outflow tract (for example, with severe aortic stenosis), the use of the drug is contraindicated.

Alcohol

During treatment, you should avoid drinking alcoholic beverages, since ethanol enhances the antihypertensive effect of vasodilating antihypertensive drugs.

Lactose

The drug Lerkamen® Duo contains lactose monohydrate, therefore its use in patients with rare hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome is contraindicated.

Lercanidipine

Sick sinus syndrome

Lercanidipine should be used with extreme caution in patients with sick sinus syndrome (without a pacemaker).

Left ventricular dysfunction

Although controlled hemodynamic studies have not revealed any abnormalities in left ventricular function, the use of BMCC in patients with signs of left ventricular dysfunction should be carried out with extreme caution.

Cardiac ischemia

Patients with coronary heart disease receiving short-acting BMCCs, dihydropyridine derivatives, represent a high-risk group for developing complications from the cardiovascular system. Although lercanidipine is a long-acting drug, caution should be exercised when used in patients with coronary artery disease.

In rare cases, in patients with angina pectoris, when using blockers of “slow” calcium channels, an increase in the frequency, duration and/or severity of angina attacks was observed, as well as, in isolated cases, the development of myocardial infarction (see section “Side Effects”).

Chronic heart failure

In patients with chronic heart failure, lercanidipine should be used with extreme caution. Before starting to use the drug, it is necessary to achieve compensation for chronic heart failure.

Unstable angina/myocardial infarction

There is no experience with the clinical use of lercanidipine in acute myocardial infarction and unstable angina, and therefore the use of the drug in these diseases is contraindicated.

Impaired liver or kidney function

Particular caution should be exercised when initiating treatment in patients with mild or moderate renal impairment. Although the usual recommended dose of 10 mg is generally well tolerated by patients, increasing the daily dose of lercanidipine to 20 mg should be approached with caution.

In patients with mild or moderate hepatic impairment, the antihypertensive effect may be enhanced, and therefore caution should be exercised and the need for dosage adjustment of lercanidipine should be considered.

Lercanidipine is contraindicated in patients with severe hepatic impairment or severe renal impairment (GFR < 30 ml/min), as well as in patients on hemodialysis (see sections "Dosage and Administration" and "Contraindications").

Peritoneal dialysis

Patients on peritoneal dialysis may experience cloudiness of the peritoneal exudate, which is due to increased concentrations of triglycerides in the exudate. Although the mechanism is unknown, exudate opacities tend to resolve soon after discontinuation of lercanidipine. This is important to remember, since cloudy peritoneal exudate can be mistakenly regarded as one of the symptoms of infectious peritonitis, followed by unnecessary hospitalization and empirical prescription of antibiotics.

CYP3A4 inducers

Inducers of CYP3A4, such as anticonvulsants (eg, phenytoin, carbamazepine) and rifampicin, may decrease plasma concentrations of lercanidipine; therefore, the effectiveness of lercanidipine may be reduced.

Enalapril

Symptomatic hypotension

Symptomatic hypotension is rarely observed in patients with uncomplicated hypertension. In patients with arterial hypertension taking enalapril, arterial hypotension develops more often against the background of dehydration, which occurs, for example, as a result of diuretic therapy, restriction of dietary salt intake, in patients on dialysis, as well as in patients with diarrhea or vomiting.

Symptomatic hypotension has been observed in patients with chronic heart failure (CHF) with or without chronic renal failure.

Arterial hypotension is more likely to develop in patients with more severe CHF with hyponatremia or impaired renal function in whom higher doses of loop diuretics are used. In such patients, treatment with enalapril should be initiated under medical supervision, which should be especially careful when changing the dose of enalapril and/or diuretic.

Similarly, patients with coronary artery disease or cerebrovascular disease, in whom an excessive decrease in blood pressure may lead to the development of myocardial infarction or stroke, should be monitored.

If arterial hypotension develops, the patient should be placed in a horizontal position and, if necessary, administered a 0.9% sodium chloride solution. Transient arterial hypotension when taking enalapril is not a contraindication to further use and increasing the dose of enalapril, which can be continued after fluid volume is replenished and blood pressure is normalized.

In some patients with CHF and normal or low blood pressure, enalapril may cause an additional decrease in blood pressure. This reaction to taking enalapril is expected and is not a reason to stop treatment. In cases where arterial hypotension becomes stable, the dose should be reduced and/or discontinued use of the diuretic and/or enalapril.

Renal dysfunction

In patients with impaired renal function (creatinine clearance <80 ml/min), the initial dose and/or frequency of enalapril should be reduced depending on the creatinine clearance. In such cases, renal function (creatinine and potassium levels in the blood) should be regularly monitored during the first few weeks of treatment.

In some patients, hypotension that develops after initiation of treatment with ACE inhibitors may lead to deterioration of renal function. Cases of the development of oliguria, progressive azotemia and acute renal failure (including fatal outcomes) have been described with the use of ACE inhibitors, mainly in patients with chronic heart failure or concomitant kidney disease (including renal artery stenosis). With timely detection and appropriate treatment, acute renal failure caused by the use of ACE inhibitors is usually reversible.

In some patients without signs of kidney disease before treatment, the use of enalapril in combination with diuretics caused an increase in the concentration of urea and creatinine in the blood serum. In such cases, it may be necessary to reduce the dose and/or discontinue the diuretic and/or enalapril. It is recommended to conduct an appropriate examination, since these abnormalities may be a sign that the patient has previously unrecognized renal artery stenosis.

Renovascular hypertension

Patients with bilateral renal artery stenosis or stenosis of the artery of a solitary kidney have an increased risk of developing arterial hypotension and renal failure when using ACE inhibitors. Renal failure may initially manifest itself as only slight changes in plasma creatinine levels. The use of enalapril in such patients should be started with low doses, under close medical supervision and monitoring of renal function.

Kidney transplant

There is no experience with the use of enalapril in patients who have recently undergone kidney transplantation. Therefore, the use of enalapril in such patients is not recommended.

Liver dysfunction

The use of ACE inhibitors in rare cases has been accompanied by the development of a syndrome starting with cholestatic jaundice or hepatitis and progressing to fulminant liver necrosis, sometimes with death. The mechanism of development of this syndrome is unknown. If jaundice appears or a significant increase in the activity of “liver” transaminases during the use of the drug, you should stop taking enalapril and prescribe appropriate auxiliary therapy. The patient should be under appropriate supervision.

Neutropenia/agranulocytosis/thrombocytopenia/anemia

Cases of neutropenia/agranulocytosis, thrombocytopenia and anemia have been reported in patients taking ACE inhibitors. In patients with normal renal function and no other complicating factors, neutropenia rarely occurs.

Enalapril should be used with extreme caution in patients with systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, etc.) taking immunosuppressive therapy, allopurinol or procainamide, or a combination of these complicating factors, especially if there are impaired renal function. Some patients developed serious infectious diseases, which in some cases did not respond to intensive antibiotic therapy. When using enalapril in patients with a high risk of neutropenia/agranulocytosis, regular monitoring of the number of leukocytes in the blood is recommended. Patients should be warned to seek immediate medical attention if any signs of an infectious disease (eg, fever, sore throat) occur.

Hypersensitivity reactions/angioedema

Rare cases of angioedema of the face, extremities, lips, tongue, vocal folds and/or larynx have been observed with the use of ACE inhibitors, including enalapril. Angioedema may develop at any time during treatment. In such cases, you should immediately stop taking enalapril and carefully monitor the patient's condition in order to monitor and correct clinical symptoms. Even in cases where only swelling of the tongue is observed without the development of respiratory distress syndrome, patients may require long-term observation, since therapy with antihistamines and corticosteroids may not be sufficient.

Angioedema, associated with swelling of the larynx and tongue, can be fatal in very rare cases. Swelling of the tongue, vocal folds, or larynx can lead to airway obstruction, especially in patients who have undergone respiratory surgery. If airway obstruction develops, appropriate treatment should be immediately prescribed, including subcutaneous administration of 0.3-0.5 ml of a 0.1% solution of epinephrine (adrenaline) and/or ensuring airway patency (intubation or tracheostomy).

In rare cases, intestinal edema (angioedema of the intestine) develops during therapy with ACE inhibitors. In this case, patients experience abdominal pain as an isolated symptom or in combination with nausea and vomiting, in some cases without previous angioedema of the face and with normal levels of C1-esterase. Diagnosis is made using abdominal computed tomography, ultrasound, or surgery. Symptoms disappeared after stopping the ACE inhibitors. The possibility of developing intestinal edema must be taken into account when carrying out the differential diagnosis of abdominal pain in patients taking ACE inhibitors.

Patients with a history of angioedema not associated with ACE inhibitors may be at greater risk of developing angioedema during ACE inhibitor therapy.

In black patients taking ACE inhibitors, angioedema was observed more often than in representatives of other races. An increased risk of angioedema was observed in patients concomitantly taking ACE inhibitors and drugs such as mTOR inhibitors (temsirolimus, sirolimus, everolimus), dipeptidyl peptidase type IV inhibitors (sitagliptin, saxagliptin, vildagliptin, linagliptin), estramustine, neutral endopeptidase inhibitors (racecadotril). ).

Anaphylactoid reactions during desensitization with an allergen from Hymenoptera venom

In rare cases, patients taking ACE inhibitors have developed life-threatening anaphylactoid reactions during desensitization with hymenoptera venom allergen. Adverse reactions can be avoided if you temporarily stop taking the ACE inhibitor before starting desensitization. The use of enalapril should be avoided in patients receiving bee venom immunotherapy.

Anaphylactoid reactions during low-density lipoprotein apheresis (LDL apheresis)

Life-threatening anaphylactoid reactions have rarely been observed in patients taking ACE inhibitors during LDL apheresis using dextran sulfate. The development of these reactions can be prevented by temporarily discontinuing the ACE inhibitor before each LDL apheresis procedure.

Hemodialysis using high-flow membranes

Anaphylactoid reactions have been observed in patients on dialysis using high-flux polyacrylonitrile membranes (such as AN69®) and concomitantly receiving ACE inhibitor therapy. In such cases, it is necessary to use a different type of dialysis membrane or use antihypertensive drugs of other classes.

Diabetes

When using enalapril drugs in patients with diabetes mellitus who are receiving oral hypoglycemic agents or insulin, it is necessary to regularly monitor the concentration of glucose in the blood. Patients taking oral hypoglycemic agents or insulin should be informed before starting the use of ACE inhibitors about the need for regular monitoring of blood glucose concentrations (hypoglycemia), especially during the first month of simultaneous use of these drugs (see section “Interaction with other drugs”). means").

Cough

Cases of cough occurring during therapy with ACE inhibitors have been observed. As a rule, the cough is non-productive, constant and stops after discontinuation of the drug. Cough associated with the use of ACE inhibitors should be considered in the differential diagnosis of dry cough.

Surgery/general anesthesia

During major surgical procedures or during general anesthesia with the use of agents with antihypertensive effects, enalaprilat blocks the formation of angiotensin II caused by the compensatory release of renin. If a pronounced decrease in blood pressure, explained by a similar mechanism, develops, it can be corrected by increasing the volume of circulating blood.

Hyperkalemia

Hyperkalemia may develop during therapy with ACE inhibitors, including enalapril. Risk factors for the development of hyperkalemia are renal failure, old age (over 65 years), diabetes mellitus, some concomitant conditions (decrease in blood volume, acute heart failure in the stage of decompensation, metabolic acidosis), simultaneous use of potassium-sparing diuretics (such as spironolactone, eplerenone, triamterene, amiloride), as well as potassium preparations, potassium-containing table salt substitutes and other drugs that increase the level of potassium in the blood plasma (such as heparin, tacrolimus, cyclosporine; drugs containing co-trimoxazole [trimethoprim + sulfamethoxazole]).

The use of potassium supplements, potassium-sparing diuretics, or potassium-containing table salt substitutes, especially in patients with impaired renal function, can lead to a significant increase in serum potassium levels. Hyperkalemia can cause serious heart rhythm disturbances, sometimes fatal.

If it is necessary to simultaneously use enalapril and the above potassium-containing or increasing potassium levels in the blood plasma, caution should be exercised and the potassium content in the blood serum should be regularly monitored.

Hypokalemia

When using ACE inhibitors simultaneously with thiazide diuretics, the risk of hypokalemia cannot be excluded, therefore, in such cases, regular monitoring of potassium levels in the blood during therapy should be carried out.

Dual blockade of the renin-angiotensin-aldosterone system (RAAS)

Hypotension, syncope, stroke, hyperkalemia and renal dysfunction (including acute renal failure) have been reported in susceptible patients, especially when combined therapy with drugs that affect the RAAS is used. The simultaneous use of ACE inhibitors with medicinal products containing aliskiren is contraindicated in patients with diabetes mellitus and/or with moderate or severe renal impairment (GFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended in other patients.

Concomitant use of ACE inhibitors with angiotensin II receptor antagonists is contraindicated in patients with diabetic nephropathy and is not recommended in other patients.

In cases where the simultaneous administration of two drugs acting on the RAAS is necessary, their use should be carried out under the supervision of a physician with extreme caution and with regular monitoring of renal function, blood pressure and electrolyte levels in the blood plasma.

Lithium preparations

The simultaneous use of enalapril and drugs containing lithium is not recommended (see section “Interaction with other drugs”).

Use in elderly patients

Clinical studies of the efficacy and safety of enalapril were similar in older and younger patients with hypertension.

Ethnic differences

Enalapril, like other ACE inhibitors, has a less pronounced antihypertensive effect in black patients compared to representatives of other races, which may be explained by a higher prevalence of conditions with low plasma renin activity in black patients with arterial hypertension.

Discontinuation of therapy

Sudden cessation of taking enalapril, as a rule, does not lead to the development of withdrawal syndrome.

Lerkamen price, where to buy

The cost varies depending on the region and pharmacy network. The price of Lerkamen 10 mg is about 400 rubles. for 28 tablets. The price of Lerkamen 20 mg is about 700 rubles. for 28 tablets.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine
Online pharmacies in KazakhstanKazakhstan

ZdravCity

Lerkamen 20 tablets p.p.o.
60 pcs. Berlin-Chemie AG/Menarini Group RUR 1,122 order
Lerkamen 20 tablets p.p.o. 28 pcs.Berlin-Chemie AG/Menarini Group
RUR 682 order
Lerkamen Duo tab. p/o captivity. 10mg + 10mg No. 28Recordati Chemical and Pharmaceutical Industry S.p.A.
RUB 511 order

Pharmacy Dialogue

Lerkamen (tab.p.pl/vol. 20mg No. 60)Berlin-Chemie AG/Menarini
RUB 1,145 order
Lerkamen (tab.p.pl/vol. 20mg No. 28)Berlin-Chemie AG/Menarini
RUR 704 order
Lerkamen Duo (tab.p.pl/vol. 10mg+10mg No. 28)Recordati
510 rub. order
Lerkamen Duo (tab.p.pl/vol.10mg+20mg No. 28)Recordati
608 rub. order
Lerkamen (tab.p.pl/vol. 10mg No. 60)Berlin-Chemie AG/Menarini
RUR 688 order

Pharmacy24

Lerkamen 10 mg No. 28 tablets Berlin Chemi AG, Nimechchina
164 UAH.order
Lerkamen 10 mg N60 tablets Berlin Chemi AG, Nimechchina
297 UAH order
Lerkamen 20 mg No. 28 tablets Berlin Chemi AG, Nimechchina
263 UAH order

PaniPharmacy

Lerkamen tablets Lerkamen tablets. p/o 10 mg No. 60 Germany, Berlin-Chemie
343 UAH. order
Lerkamen tablets Lerkamen tablets. p/o 10 mg No. 28 Germany, Berlin-Chemie
179 UAH. order
Lerkamen tablets Lerkamen tablets. p/o 20 mg No. 28 Germany, Berlin-Chemie
284 UAH order
Lerkamen tablets Lerkamen tablets. p/o 20 mg No. 60 Germany, Berlin-Chemie
509 UAH. order