Method of action:
Medically reviewed by Oliinyk Elizabeth Ivanovna, PharmD. Last updated on 2020-04-10
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Top 20 medicines with the same components:
Dosage 10 mg 10 mg: essential hypertension (with the ineffectiveness of lercanidipine 10 mg monotherapy).
Dosage 10 mg 20 mg: essential hypertension (with the ineffectiveness of enalapril 20 mg monotherapy).
Inside, in the morning, at least 15 minutes before meals, without chewing, with a sufficient amount of water. Do not drink grapefruit juice.
Drug Korepin® it is not intended for the initial treatment of hypertension.
Dosage 10 mg 10 mg: after failure of monotherapy with lercanidipine 10 mg, you should start taking the drug Korepin® at a dose of 10 mg, 10 mg.
Dosage 10 mg 20mg: if monotherapy with enalapril 20 mg is ineffective, you should start taking the drug Coripren® in a dose of 20 mg. The dose of the drug is selected by the doctor.
hypersensitivity to lercanidipine, enalapril or to any other ACE inhibitor and other BCC derivatives of dihydropyridine, as well as to any other component of the drug,
the violation of the outflow from the left ventricle, including aortic valve stenosis,
chronic heart failure in the decompensation stage,
hereditary and / or idiopathic angioedema,
the first month after a myocardial infarction (within 28 days),
severe renal insufficiency (creatinine Cl < 30 ml/min), including patients undergoing hemodialysis,
severe liver failure,
concomitant use with potent inhibitors of the CYP3A4 isoenzyme (ketoconazole, itraconazole, erythromycin, ritonavir, troleandomycin), cyclosporine, grapefruit juice,
angioedema from the use of ACE inhibitors in the anamnesis,
a history of hereditary or idiopathic edema,
lactase deficiency, lactose intolerance, and glucose-galactose malabsorption syndrome,
children's age (up to 18 years).
With caution: sinus node weakness syndrome (without simultaneous use of an artificial heart rhythm driver), left ventricular dysfunction and ischemic heart disease, renal failure (creatinine Cl more than 30 ml / min), renovascular hypertension, post-kidney transplant condition (limited experience), liver failure, bone marrow hematopoiesis suppression, severe autoimmune connective tissue diseases (in t.tsch. scleroderma, systemic lupus erythematosus), concomitant use with immunosuppressants, allopurinol, procainamide, diabetes mellitus, surgical interventions and general anesthesia, patients following a diet with limited intake of table salt, hyperkalemia, conditions accompanied by a decrease in BCC, in t.tsch. diarrhea, vomiting, primary hyperaldosteronism
WHO classification: very often-1/10 appointments, often-1/100 appointments, infrequently-1/1000 appointments, rarely-1/10000 appointments, very rarely-less than 1/10000 appointments.
From the central nervous system: often-dizziness, infrequently-headache.
From the side of the psyche: infrequently-anxiety.
From the skin: infrequently-dermatitis, swelling of the lips, erythema, urticaria, rash.
From the genitourinary system: infrequently-erectile dysfunction.
From the urinary system: rarely, pollakiuria, polyuria, nocturia.
On the part of the immune system: infrequently-hypersensitivity to one of the components of the drug, Quincke's edema.
From the side of metabolism: infrequently-hypertriglyceridemia.
From the musculoskeletal system: infrequently-arthralgia.
From the digestive system: infrequently-abdominal pain, nausea, constipation, dyspepsia, glossitis.
From the hematopoietic system: infrequently-thrombocytopenia.
From the respiratory system: often-cough, infrequently-dry throat, pharyngeal-laryngeal pain.
From the CCC side: often-flushes of blood to the skin of the face, infrequently-a feeling of palpitation and tachycardia, a pronounced decrease in blood pressure, circulatory collapse, congestive heart failure.
On the part of the organ of hearing and labyrinth disorders: often-vertigo, including positional vertigo.
Laboratory parameters: infrequently-a decrease in the level of hemoglobin, an increase in the activity of ALT, AST.
Other: often-peripheral edema, infrequently-asthenia, increased fatigue, a feeling of heat.
From the central nervous system: very often-dizziness, often-headache, infrequently-paresthesia.
From the side of the psyche: often-depression, infrequently-confusion, drowsiness, insomnia, nervousness, rarely-pathological dreams, sleep disorders.
From the skin: often-rash, infrequently-increased sweating, itching, urticaria, alopecia, rarely-erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, Lyell's syndrome, pemphigus.
From the urinary system: infrequently-renal failure, proteinuria, rarely-oliguria.
From the genitourinary system: infrequently-erectile dysfunction, rarely-gynecomastia.
On the part of the immune system: often-hypersensitivity, angioedema of the face, limbs, lips, tongue, glottis and / or larynx, rarely-autoimmune disorders.
From the side of metabolism: infrequently-hypoglycemia, anorexia.
From the musculoskeletal system: infrequently-muscle spasm.
From the digestive system: very often-nausea, often-diarrhea, abdominal pain, taste disorders, infrequently-intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, dry mouth, stomach pain, stomach ulcer or duodenal ulcer, rarely-stomatitis, aphthous stomatitis, glossitis, very rarely-intestinal angioedema.
From the liver and biliary tract: rarely-liver failure, hepatitis (cholestatic or necrotic), cholestasis.
From the hematopoietic system: rarely-anemia, including aplastic and hemolytic, rarely-thrombocytopenia, neutropenia, agranulocytosis, pancytopenia, lymphadenopathy, bone marrow hematopoiesis insufficiency.
From the respiratory system: very often-cough, often — shortness of breath, infrequently-rhinorrhea, pharyngeal pain, dysphonia, bronchospasm, asthma, rarely — lung infiltration, rhinitis, alveolar allergic/eosinophilic pneumonia.
On the part of the visual organ: very often — a decrease in visual acuity.
On the part of the organ of hearing and labyrinth disorders: infrequently-tinnitus, vertigo.
From the CCC side: often-arrhythmia, angina, tachycardia, myocardial infarction, marked decrease in blood pressure, fainting, stroke, due to excessive decrease in blood pressure in patients with increased risk, infrequently-palpitations, flushes of blood to the skin of the face, orthostatic hypotension, rarely-Raynaud's syndrome.
Laboratory parameters: often-hyperkalemia, an increase in creatinine in the blood, not often-an increase in urea in the blood, a decrease in sodium in the blood, rarely-an increase in hemoglobin and hematocrit, an increase in the number of liver enzymes and a decrease in the concentration of bilirubin in the blood.
Other: very often — asthenia, often-increased fatigue, chest pain, infrequently-malaise.
A symptom complex is also described, including facial skin hyperemia, nausea, vomiting, and a marked decrease in blood pressure, which can develop with the simultaneous use of ACE inhibitors and the drug gold (sodium aurothiomalate) in/V.
From the central nervous system: infrequently-dizziness, headache.
From the side of the psyche: rarely-drowsiness.
From the skin: rarely-rash.
On the part of the immune system: very rarely-hypersensitivity.
From the urinary system: rarely-polyuria.
From the musculoskeletal system: rarely-myalgia.
From the digestive system: rarely — nausea, dyspepsia, diarrhea, abdominal pain, vomiting.
From the CCC side: infrequently-tachycardia, palpitations, flushes of blood to the skin of the face, rarely-angina, very rarely-fainting.
Other: infrequently-peripheral edema, rarely-asthenia, increased fatigue.
There is no information about an overdose of the drug. Presumably, in the case of an overdose, it can cause conditions caused by an overdose of any of the active substances.
Symptoms: peripheral vasodilation with a marked decrease in blood pressure and reflex tachycardia, vomiting.
Treatment: symptomatic, the choice of treatment method depends on the degree of overdose and on the observed symptoms. The following methods of medical care are used — gastric lavage, administration of high doses of catecholamines, furosemide, cardiac glycosides and plasma substitutes, activated charcoal, laxatives, and intravenous administration of dopamine. Also, to prevent the development of bradycardia, it is possible to administer atropine intravenously.
Symptoms: the main sign of overdose is a pronounced decrease in blood pressure, which is accompanied by RAAS blockade and tetanus. You may also develop collapse, electrolyte imbalance, kidney failure, hyperventilation, tachycardia, palpitations, bradycardia, dizziness, anxiety, and coughing.
Treatment: symptomatic. In severe cases, intravenous administration of 0.9% sodium chloride solution and, if possible, infusion of angiotensin II and/or catecholamines is recommended. If the symptoms of overdose developed immediately after taking the drug, it is necessary to induce vomiting, perform gastric lavage and take drugs from the group of adsorbents or sodium sulfate.
The drug is a combination of an ACE inhibitor and BCC.
Lercanidipine. A dihydropyridine derivative, it inhibits the transmembrane flow of calcium into cardiac cells and smooth muscle cells. The mechanism of antihypertensive action is due to a direct relaxing effect on the smooth muscles of the vessels, as a result of which the OPSS is reduced. It has a prolonged antihypertensive effect. Due to the high selectivity for vascular smooth muscle cells of the vessels of the negative inotropic effect is absent.
Enalapril. ACE inhibitor, inhibits the formation of angiotensin II and eliminates its vasoconstrictive effect. Reduces blood pressure, without causing an increase in heart rate and minute volume.
Reduces OPSS, reduces afterload and preload on the heart. Reduces the pressure in the right atrium and the small circle of blood circulation. It does not affect the metabolism of glucose, lipoproteins, as well as the functions of the reproductive system.
No pharmacokinetic interactions have been observed with concomitant administration of lercanidipine and enalapril.
Suction. Lercanidipine is absorbed completely in the gastrointestinal tract after oral administration. During the initial passage through the liver, due to high metabolism, the absolute bioavailability when taken orally after a meal is approximately 10%, when taken on an empty stomach, the bioavailability decreases by 1/3. The bioavailability after the use of lercanidipine increases by 4 times if the drug is taken no later than 2 hours after taking fatty foods. Therefore, the drug should be taken at least 15 minutes before meals. Cmax lercanidipine in the blood plasma is observed after 1.5-3 hours. It does not accumulate with repeated use. The duration of the therapeutic effect of lercanidipine is 24 hours.
The concentration of lercanidipine in the blood plasma when taken orally is not directly proportional to the dosage (nonlinear dependence). When taking 10, 20 or 40 mg Cmax lercanidipine in blood plasma was determined in a ratio of 1:3: 8, respectively, and AUC-in a ratio of 1:4:18, which suggests progressive saturation during the primary passage through the liver. Accordingly, bioavailability increases with increasing dose.
Distribution. The distribution of lercanidipine from the blood plasma to the tissues and organs is rapid and intense. The binding of lercanidipine to plasma proteins exceeds 98%. In patients with renal and hepatic insufficiency, the plasma protein content is reduced, so the free fraction of lercanidipine can be increased.
Metabolism. Lercanidipine is metabolized by the liver isoenzyme CYP3A4 to form inactive metabolites.
Introduction. The drug in its unchanged form is practically not detected in the urine and feces. About 50% of the dose of lercanidipine is excreted by the kidneys, the average value of T1/2 Lercanidipine is 8-10 hours.
In elderly patients and patients with mild or moderate renal insufficiency or mild or moderate hepatic insufficiency, the pharmacokinetic parameters of lercanidipine are the same as in the general group of patients. In patients with severe renal insufficiency or in patients on hemodialysis, lercanidipine is excreted by the kidneys in a higher amount (about 70%). In patients with hepatic insufficiency (moderate to severe), the systemic bioavailability of lercanidipine is increased, since the drug is metabolized mainly in the liver.
Suction. The percentage of absorption of enalapril after oral administration is about 60%. Cmax enalapril in the blood plasma is observed after 1 h. Food intake does not affect the absorption of enalapril.
Distribution. When taken orally, it is rapidly hydrolyzed to enalaprilate, which has an inhibitory effect on ACE. Cmax enalaprilat in the blood serum is observed in 3-4 hours after taking the drug. The binding of enalapril to plasma proteins does not exceed 60%.
Metabolism. When taken orally, it is hydrolyzed to the main metabolite — enalaprilate.
Output. About 40% of enalapril in the form of enalaprilate and about 20% of unchanged enalapril is excreted by the kidneys.
In patients with renal insufficiency, the duration of exposure to enalapril and enalaprilat is increased.
In patients with mild or moderate renal insufficiency (creatinine Cl-40-60 ml / min) when taking 5 mg of enalapril once a day, the plateau stage of the AUC of enalaprilat is doubled compared to patients with normal liver function. In patients with severe renal insufficiency (creatinine Cl < 30 ml/min), the AUC increases approximately 8-fold. In this stage of renal failure, T1/2 enalaprilate increases with repeated administration of enalapril maleate and the time to reach the plateau stage of AUC slows down. Enalaprilate can be removed from the general bloodstream by hemodialysis. The dialysis clearance is 62 ml / min.
- Antihypertensive agent combined (angiotensin-converting enzyme inhibitor calcium channel blocker) [ACE inhibitors in combinations]
- Antihypertensive agent combined (angiotensin-converting enzyme inhibitor calcium channel blocker) [Calcium channel blockers in combinations]
The antihypertensive effect of the drug can be potentiated when used simultaneously with other drugs with a similar effect, such as diuretics, beta -, alpha-blockers, etc. In addition, when used together, the following effects may be observed.
The drug should not be taken in combination with CYP3A4 inhibitors, such as ketoconazole, itraconazole, erythromycin and others, with cyclosporine and grapefruit juice (increase the concentration in the blood and lead to a potentiation of the antihypertensive effect).
Caution should be exercised when taking concomitantly with drugs such as terfenadine, astemizole and class III antiarrhythmic drugs (for example, amiodarone) and quinidine. Concomitant administration with anticonvulsants (e.g. phenytoin, carbamazepine) and rifamycin may reduce the antihypertensive effect of lercanidipine.
The administration of digoxin should be closely monitored to detect clinical symptoms of digoxin toxicity.
Taking the drug with midazolam leads to an increase in the absorption of lercanidipine in the gastrointestinal tract and a decrease in the rate of absorption.
Metoprolol reduces the bioavailability of lercanidipine by 50%.
Cimetidine at a dose of 800 mg per day does not lead to significant changes in the content and concentration of lercanidipine in the blood serum, but with such a combination, special caution is required, since at higher doses of cimetidine, the bioavailability of lercanidipine, and therefore its antihypertensive effect, may increase.
Fluoxetine has no effect on the pharmacokinetics of lercanidipine. In the case of taking the drug with simvastatin, the drug should be taken in the morning, and simvastatin-in the evening. Taking lercanidipine simultaneously with warfarin does not affect the pharmacokinetics of the latter.
Concomitant administration of the drug with potassium salts, with potassium-sparing diuretics (spironolactone, triamterene, eplerenone, amiloride), ACE inhibitors, angiotensin II receptor antagonists, NSAIDs, heparins (low molecular weight or unfractionated), cyclosporine, tacrolimus and trimethoprim increases the risk of hyperkalemia.
It is also not recommended to use it together with lithium salts (if such a combination is necessary, then carefully monitor the concentration of lithium in the blood plasma).
Simultaneous administration with antidiabetic drugs (both oral and insulin) can cause the development of hypoglycemia at the 1st week of treatment.
Diuretics (loop and thiazide) can cause a decrease in BCC and thus increase the risk of a pronounced decrease in blood pressure when treated with the drug.
Long-term use of NSAIDs may reduce the antihypertensive effect of ACE inhibitors. Both NSAIDs and ACE inhibitors (enalapril) they contribute to an increase in the content of potassium in the blood, which can lead to impaired kidney function.
Baclofen increases the antihypertensive effect.
Cyclosporine increases the risk of hyperkalemia.
Ethanol increases the antihypertensive effect of ACE inhibitors.
Tricyclic antidepressants/antipsychotics/general anesthetics/narcotic analgesics can lead to a further decrease in blood pressure.
Corticosteroids (except hydrocortisone as a replacement therapy for Addison's disease) reduce the antihypertensive effect (fluid retention with subsequent increase in BCC).
Co-administration with other antihypertensive agents may enhance the antihypertensive effect of enalapril.
Combined use with nitroglycerin and other nitrates and vasodilators leads to an even more pronounced decrease in blood pressure.
Allopurinol, cytostatics, immunosuppressants, systemic corticosteroids, and procainamide may lead to an increased risk of leukopenia.
Antacids help to reduce the bioavailability of ACE inhibitors. Sympathomimetics can reduce the antihypertensive effect.
Enalapril can be used simultaneously with acetylsalicylic acid (as an antiplatelet agent).
When used simultaneously with the preparation of gold (sodium aurothiomalate) in/in, the development of side effects is possible.
At a temperature not exceeding 25 °C.
Keep out of reach of children.The shelf life of the drug Lekamen® Duo2 года.
Do not use after the expiration date indicated on the package.
|Film-coated tablets (dosage 10 mg 10 mg)||1 table.|
|lercanidipine hydrochloride||10 mg|
|enalapril maleat||10 mg|
|excipients: lactose monohydrate-102 mg, MCC-40 mg, sodium carboxymethyl starch-20 mg, povidone K30-8 mg, sodium bicarbonate-8 mg, magnesium stearate-2 mg|
|shell: Opadry white (02F29056) — 6 mg (hypromellose-5) - 3,825 mg, titanium dioxide (E171) - 1,275 mg, talc-0.3 mg, macrogol 6000-0.6 mg)|
|Film-coated tablets (dosage 10 mg 20 mg)||1 table.|
|lercanidipine hydrochloride||10 mg|
|enalapril maleat||20 mg|
|excipients: lactose monohydrate-92 mg, MCC-40 mg, sodium carboxymethyl starch-20 mg, povidone K30-8 mg, sodium bicarbonate-8 mg, magnesium stearate-2 mg|
|shell: Opadry yellow (02F22330) - 6 mg (hypromellose-5sR-3,825 mg, titanium dioxide (E171) - 1,139 mg, talc-0.3 mg, macrogol 6000-0.6 mg, quinoline yellow dye (E104) - 0.121 mg, iron oxide yellow dye (E172) - 0.015 mg)|
Film-coated tablets, 10 mg 10 mg, 10 mg 20 mg. By 7, 10, 14, 28, 30, 35, 42, 50 or 56 tab. in a blister made of an opaque three-layer film (polyamide / aluminum/PVC) and aluminum foil. By 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 blisters in a cardboard box.
The use of the drug Korepin® it is not recommended during pregnancy, and not only in the second and third trimesters.
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 accompanied by negative effects on the fetus and newborn, including the development of arterial hypotension, renal failure, hyperkalemia and / or hypoplasia of the skull bones in the newborn. Possible development of oligohydramnion, apparently, due to a decrease in fetal kidney function. This complication can lead to contracture of the extremities, deformity of the bones of the skull, including its facial part, hypoplasia of the lungs. The teratogenic effect of ACE inhibitors (enalapril) in the first trimester has not been proven, but this possibility should not be excluded. Patients who are on ACE inhibitor therapy during pregnancy planning should switch to alternative antihypertensive treatment regimens
It is not recommended to use the drug in women of childbearing age who do not use reliable contraceptives.
The use of the drug during breastfeeding is not recommended, because enalapril and its main metabolite (enalaprilat) penetrate into breast milk.
According to the recipe.
Special attention in the treatment of hypertension is required in patients with severe arterial hypotension (sBP <90 mm Hg) and decompensated heart failure. Transient arterial hypotension is not a contraindication to the continuation of treatment, because after filling the BCC, an adequate response to the drug can be expected.
Special care should be taken at the initial stages of treatment of patients with mild to moderate renal insufficiency. Patients with bilateral renal artery stenosis or stenosis of the artery of a single functioning kidney are particularly at risk of hypotension or renal failure due to ACE inhibitors. For this group of patients, treatment should be carried out under the strict supervision of a doctor, with careful dose selection and the appointment of low doses of the drug. Before and during treatment, it is necessary to monitor kidney function.
Special care should be taken at the initial stages of treatment of patients with mild to moderate severity of liver failure. If jaundice occurs and there is a significant increase in the activity of liver enzymes, it is necessary to urgently stop taking ACE inhibitors and consult a doctor.
Due to the increased risk of anaphylactic reactions, the drug should not be prescribed to patients on hemodialysis using high-strength polyacrylonitrile membranes (AN69®), during LDL apheresis with dextran sulfate and immediately before the desensitization procedure to wasp or bee venom.
Like other ACE inhibitors, it has a less pronounced antihypertensive effect in patients of the black race compared to representatives of other races.
As a result of the use of enalapril, angioedema of the face, limbs, tongue, pharynx or larynx may develop. In this case, you should immediately stop taking the drug. Angioedema of the larynx can be fatal. Angioedema of the tongue, pharynx or larynx can lead to airway obstruction, it is necessary to immediately administer epinephrine (0.3–0.5 ml of epinephrine (epinephrine) solution n / a in a ratio of 1:1000) and maintain airway patency (incubation or tracheostomy). Among non-black patients receiving ACE inhibitor therapy, the incidence of angioedema is higher than among patients of a different race. Patients with a history of angioedema that is not associated with the use of ACE inhibitors have an increased risk of developing angioedema when using any ACE inhibitor.
Before surgery (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors. During surgical procedures and/or general anesthesia with hypotensive agents, ACE inhibitors may block the formation of angiotensin II in response to the compensatory release of renin. If at the same time a pronounced decrease in blood pressure develops, explained by a similar mechanism, it can be corrected by increasing the BCC.
Hyperkalemia may develop on the background of therapy with ACE inhibitors, including enalapril.
Risk factors for hyperkalemia are: renal failure, old age, diabetes mellitus, some concomitant conditions (decreased BCC, acute heart failure in the decompensation stage, metabolic acidosis), simultaneous administration of potassium-sparing diuretics (such as spironolactone, eplerenone, triamterene, amiloride), as well as potassium preparations or potassium-containing substitutes for table salt, and the use of other drugs that increase the potassium content in the blood plasma (for example, heparin). Hyperkalemia can lead to serious cardiac arrhythmias, sometimes fatal. The combined use of the above drugs should be carried out with caution.
It is not recommended to drink alcohol during therapy with the drug.
There is evidence of reversible biochemical changes in the heads of spermatozoa when using BCC, which can disrupt their ability to fertilize.
The effect of a drug for medical use on the ability to drive vehicles, mechanisms. You should keep in mind the possibility of weakness and drowsiness, so you should be careful when performing work that requires increased attention, especially at the beginning of treatment, when increasing the dose of the drug and when driving vehicles.
C09BB02 Enalapril Lercanidipine
Film-coated tablets, 10 mg 10 mg: round, biconvex, covered with a white film shell.
Film-coated tablets, 10 mg 20 mg: round, biconvex, covered with a yellow film shell.
On the cross section - the core is light yellow.